WO2011090760A4 - Heteroaryl compounds and uses thereof - Google Patents

Heteroaryl compounds and uses thereof Download PDF

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Publication number
WO2011090760A4
WO2011090760A4 PCT/US2010/062432 US2010062432W WO2011090760A4 WO 2011090760 A4 WO2011090760 A4 WO 2011090760A4 US 2010062432 W US2010062432 W US 2010062432W WO 2011090760 A4 WO2011090760 A4 WO 2011090760A4
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WO
WIPO (PCT)
Prior art keywords
sheet
amendment
amended
pct
international application
Prior art date
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PCT/US2010/062432
Other languages
French (fr)
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WO2011090760A1 (en
Inventor
Juswinder Singh
Russell Petter
Richland Wayne Tester
Arthur F. Kluge
Hormoz Mazdiyasni
Iii William Frederick Westlin
Deqiang Niu
Lixin Qiao
Original Assignee
Avila Therapeutics, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Priority to MX2014015883A priority Critical patent/MX341825B/en
Priority to BR112012018345-1A priority patent/BR112012018345B1/en
Application filed by Avila Therapeutics, Inc. filed Critical Avila Therapeutics, Inc.
Priority to CN201080060197.8A priority patent/CN102740847B/en
Priority to KR1020127019713A priority patent/KR101747159B1/en
Priority to CA2783624A priority patent/CA2783624C/en
Priority to AU2010343055A priority patent/AU2010343055B2/en
Priority to EP10844293.0A priority patent/EP2519235B1/en
Priority to MX2012007507A priority patent/MX2012007507A/en
Priority to NZ600631A priority patent/NZ600631A/en
Priority to SG2012047619A priority patent/SG181962A1/en
Priority to JP2012547280A priority patent/JP5879270B2/en
Priority to KR1020177015594A priority patent/KR20170086547A/en
Priority to RU2012123546A priority patent/RU2636584C2/en
Publication of WO2011090760A1 publication Critical patent/WO2011090760A1/en
Publication of WO2011090760A4 publication Critical patent/WO2011090760A4/en
Priority to IL220155A priority patent/IL220155B/en
Priority to IL235621A priority patent/IL235621A0/en
Priority to AU2017200697A priority patent/AU2017200697A1/en

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    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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    • C07D487/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
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Abstract

The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Claims

AMENDED CLAIMS received by the International Bureau on 26 July 2011 (26.07.11)
1. A compound selected from the group consisting of:
Figure imgf000002_0001
Figure imgf000002_0002
Figure imgf000002_0003
Figure imgf000002_0004
Figure imgf000003_0001
Figure imgf000004_0001
Figure imgf000005_0001
a pharmaceutically acceptable salt thereof.

I STATEMENT UNDER ARTICLE 19 (1)

Applicant requests that the above claim amendment be entered pursuant to PCT Article 19. The specific differences between the original claims and the amended ones are detailed above as required by PCT Rule 46.5. Compounds I-362, I-363, I-364, I-36S, I-366, I-367, and I-368 have been cancelled from claim 1. This amendment results in the cancellation of sheet 482 of the international application (PCT Rule 46.5).

The above amendments do not go beyond the disclosure in the international application as filed. A replacement sheet for every sheet which, on account of an amendment, differs from the sheet previously filed, is provided.

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8354420B2 (en) 2010-06-04 2013-01-15 Genentech, Inc. Aminopyrimidine derivatives as LRRK2 inhibitors
US8815882B2 (en) 2010-11-10 2014-08-26 Genentech, Inc. Pyrazole aminopyrimidine derivatives as LRRK2 modulators
US9580432B2 (en) 2013-08-12 2017-02-28 Taiho Pharmaceutical Co., Ltd. Fused pyrimidine compound or salt thereof

Families Citing this family (277)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009051822A1 (en) 2007-10-19 2009-04-23 Avila Therapeutics, Inc. Heteroaryl compounds and uses thereof
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
EA029131B1 (en) 2008-05-21 2018-02-28 Ариад Фармасьютикалз, Инк. Phosphorous derivatives as kinase inhibitors
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
KR20110025224A (en) 2008-06-27 2011-03-09 아빌라 테라퓨틱스, 인크. Heteroaryl compounds and uses thereof
JP5918693B2 (en) 2009-05-05 2016-05-18 ダナ ファーバー キャンサー インスティテュート インコーポレイテッド EGFR inhibitor and disease treatment method
US8367689B2 (en) * 2009-05-06 2013-02-05 Portola Pharmaceuticals, Inc. Inhibitors of JAK
US8586751B2 (en) 2009-06-12 2013-11-19 Bristol-Myers Squibb Company Nicotinamide compounds useful as kinase modulators
KR20120093220A (en) 2009-09-16 2012-08-22 아빌라 테라퓨틱스, 인크. Protein kinase conjugates and inhibitors
US8466155B2 (en) * 2009-10-02 2013-06-18 Boehringer Ingelheim International Gmbh Pyrimidines
WO2011082285A1 (en) 2009-12-30 2011-07-07 Avila Therapeutics, Inc. Ligand-directed covalent modification of protein
US9290499B2 (en) 2010-05-19 2016-03-22 The University Of North Carolina At Chapel Hill Pyrazolopyrimidine compounds for the treatment of cancer
AU2011254550B2 (en) 2010-05-21 2013-11-07 Noviga Research Ab Novel pyrimidine derivatives
JP6068340B2 (en) 2010-08-10 2017-01-25 セルジーン アヴィロミクス リサーチ, インコーポレイテッド Besylate of BTK inhibitor
US9238629B2 (en) 2010-11-01 2016-01-19 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
ES2776002T3 (en) 2010-11-01 2020-07-28 Celgene Car Llc Heterocyclic compounds and their uses
EP2637502B1 (en) 2010-11-10 2018-01-10 Celgene CAR LLC Mutant-selective egfr inhibitors and uses thereof
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
BR112013024378A2 (en) 2011-03-24 2016-12-13 Chemilia Ab new pyrimidine derivatives
JP6147727B2 (en) * 2011-04-01 2017-06-14 ユニヴァーシティー オブ ユタ リサーチ ファウンデーション Substituted N- (3- (pyrimidin-4-yl) phenyl) acrylamide analogs as tyrosine receptor kinase BTK inhibitors
DK2693881T3 (en) 2011-04-01 2019-12-09 Univ Utah Res Found SUBSTITUTED N-PHENYLPYRIMIDIN-2-AMINE ANALOGS AS AXL-KINASE INHIBITORS
RU2697712C2 (en) 2011-04-22 2019-08-19 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Substituted diaminocarboxamide and diaminocarbonitrile derivatives of pyrimidines, compositions thereof and methods of treating use thereof
AU2012249801B2 (en) 2011-04-25 2016-05-19 Usher Iii Initiative, Inc. Pyrazolopyridazines and methods for treating retinal-degenerative diseases and hearing loss associated with Usher syndrome
US9834518B2 (en) 2011-05-04 2017-12-05 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in EGFR-driven cancers
RS56679B1 (en) 2011-07-27 2018-03-30 Astrazeneca Ab 2-(2,4,5-substituted-anilino)pyrimidine derivatives as egfr modulators useful for treating cancer
MX2014004086A (en) 2011-10-03 2014-09-22 Univ North Carolina Pyrrolopyrimidine compounds for the treatment of cancer.
AR088570A1 (en) 2011-10-28 2014-06-18 Celgene Avilomics Res Inc METHODS TO TREAT AN ILLNESS OR DISORDER RELATED TO BRUTON TYROSINE KINASE
US9586965B2 (en) 2012-01-13 2017-03-07 Acea Biosciences Inc. Pyrrolo[2,3-d]pyrimidine compounds as inhibitors of protein kinases
CN104203924B (en) * 2012-01-13 2019-06-11 艾森生物科学公司 Heterocyclic compound and its purposes as anticarcinogen
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
US9464089B2 (en) 2012-01-13 2016-10-11 Acea Biosciences Inc. Heterocyclic compounds and uses thereof
PT2805940T (en) 2012-01-17 2017-02-03 Astellas Pharma Inc Pyrazine carboxamide compound
CA2866852C (en) 2012-03-15 2020-12-29 Celgene Avilomics Research, Inc. Solid forms of an epidermal growth factor receptor kinase inhibitor
LT2825042T (en) 2012-03-15 2018-12-10 Celgene Car Llc Salts of an epidermal growth factor receptor kinase inhibitor
AU2013204563B2 (en) * 2012-05-05 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
US9133134B2 (en) 2012-05-16 2015-09-15 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
IN2014DN09610A (en) * 2012-05-22 2015-07-31 Univ North Carolina
WO2014007951A2 (en) 2012-06-13 2014-01-09 Incyte Corporation Substituted tricyclic compounds as fgfr inhibitors
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
EP2892538A4 (en) * 2012-09-04 2016-04-20 Celgene Avilomics Res Inc Methods of treating a bruton's tyrosine kinase disease or disorder
CN104822663B (en) 2012-10-04 2017-03-08 犹他大学研究基金会 Substituted N (3 (4 base of pyrimidine) phenyl) acrylamide as tyrosine receptor kinase BTK inhibitor is similar to thing
EP3680238A1 (en) * 2012-10-04 2020-07-15 University of Utah Research Foundation Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors
WO2014062774A1 (en) 2012-10-17 2014-04-24 The University Of North Carolina At Chapel Hill Pyrazolopyrimidine compounds for the treatment of cancer
US9227976B2 (en) 2012-10-25 2016-01-05 Usher Iii Initiative, Inc. Pyrazolopyridazines and methods for treating retinal-degenerative diseases and hearing loss associated with usher syndrome
US8765762B2 (en) 2012-10-25 2014-07-01 Usher III, Initiative, Inc. Pyrazolopyridazines and methods for treating retinal-degerative diseases and hearing loss associated with usher syndrome
WO2014081709A2 (en) * 2012-11-20 2014-05-30 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with bruton's tyrosine kinase
TW201427667A (en) * 2012-11-20 2014-07-16 Celgene Avilomics Res Inc Methods of treating a disease or disorder associated with Bruton's tyrosine kinase
TW201427668A (en) * 2012-11-20 2014-07-16 Celgene Avilomics Res Inc Methods of treating a disease or disorder associated with Bruton's tyrosine kinase
US20140142128A1 (en) * 2012-11-20 2014-05-22 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with bruton's tyrosine kinase
US9771330B2 (en) 2012-11-27 2017-09-26 The University Of North Carolina At Chapel Hill Pyrimidine compounds for the treatment of cancer
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
EP2935226A4 (en) * 2012-12-21 2016-11-02 Celgene Avilomics Res Inc Heteroaryl compounds and uses thereof
EP2948150A1 (en) 2013-01-25 2015-12-02 Rigel Pharmaceuticals, Inc. Compounds and methods for treating inflammatory bowel diseases
TW201446745A (en) 2013-02-08 2014-12-16 Celgene Avilomics Res Inc ERK inhibitors and uses thereof
US20140357636A1 (en) * 2013-02-21 2014-12-04 Wayne Rothbaum Treatment of Skeletal-Related Disorders
WO2014134391A1 (en) 2013-02-28 2014-09-04 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent rock1 and rock2 inhibitors
TW201444798A (en) 2013-02-28 2014-12-01 必治妥美雅史谷比公司 Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors
MX2015012062A (en) 2013-03-14 2016-05-05 Tolero Pharmaceuticals Inc Jak2 and alk2 inhibitors and methods for their use.
EP2970190A1 (en) 2013-03-14 2016-01-20 Respivert Limited Kinase inhibitors
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
TWI715901B (en) 2013-04-19 2021-01-11 美商英塞特控股公司 Bicyclic heterocycles as fgfr inhibitors
KR101793807B1 (en) 2013-04-25 2017-11-03 베이진 엘티디 Fused heterocyclic compounds as protein kinase inhibitors
WO2014182593A1 (en) * 2013-05-06 2014-11-13 Clovis Oncology, Inc. Salts of an epidermal growth factor receptor kinase inhibitor
GB201309085D0 (en) 2013-05-20 2013-07-03 Redx Pharma Ltd Compounds
WO2014210255A1 (en) 2013-06-26 2014-12-31 Abbvie Inc. Primary carboxamides as btk inhibitors
CN105377835B (en) * 2013-07-11 2018-08-17 贝达药业股份有限公司 Tyrosine protein kinase conditioning agent and its application process
SG11201600062RA (en) * 2013-07-11 2016-02-26 Acea Biosciences Inc Pyrimidine derivatives as kinase inhibitors
US9492471B2 (en) 2013-08-27 2016-11-15 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase
RS63571B9 (en) 2013-09-13 2023-02-28 Beigene Switzerland Gmbh Anti-pd1 antibodies and their use as therapeutics and diagnostics
CN104262328B (en) * 2013-09-18 2016-09-07 北京韩美药品有限公司 The compound of suppression BTK and/or JAK3 kinase activity
KR20160063366A (en) 2013-10-21 2016-06-03 메르크 파텐트 게엠베하 Heteroaryl compounds as btk inhibitorsand uses thereof
EP3060218A4 (en) 2013-10-25 2017-07-19 Pharmacyclics LLC Methods of treating and preventing graft versus host disease
US9415049B2 (en) * 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
NZ715903A (en) 2014-01-30 2017-06-30 Signal Pharm Llc Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use
US11039621B2 (en) 2014-02-19 2021-06-22 Corning Incorporated Antimicrobial glass compositions, glasses and polymeric articles incorporating the same
US9622483B2 (en) 2014-02-19 2017-04-18 Corning Incorporated Antimicrobial glass compositions, glasses and polymeric articles incorporating the same
US11039620B2 (en) 2014-02-19 2021-06-22 Corning Incorporated Antimicrobial glass compositions, glasses and polymeric articles incorporating the same
CN104860941B (en) * 2014-02-25 2017-03-22 上海海雁医药科技有限公司 2,4-disubstituted phenyl-1,5-diamine derivatives and use thereof, and pharmaceutical composition and medicinal composition prepared from 2,4-disubstituted phenyl-1,5-diamine derivative
ES2921874T3 (en) 2014-02-28 2022-09-01 Nimbus Lakshmi Inc TYK2 inhibitors and uses thereof
WO2015134805A1 (en) * 2014-03-07 2015-09-11 Celgene Avilomics Research, Inc. Methods of treating a bruton's tyrosine kinase disease or disorder
US20150291606A1 (en) 2014-04-11 2015-10-15 The University Of North Carolina At Chapel Hill Mertk-specific pyrrolopyrimidine compounds
JP6321821B2 (en) 2014-04-14 2018-05-09 シャンハイ ハイヤン ファーマシューティカル テクノロジー カンパニー リミテッドShanghai Haiyan Pharmaceutical Technology Co., Ltd. 2,3,4,6-4-substituted benzene-1,5-diamine derivatives, their production and use in pharmaceuticals
JP2017514805A (en) * 2014-04-16 2017-06-08 シグナル ファーマシューティカルズ,エルエルシー Methods of treating cancer using TOR kinase inhibitor combination therapy
CN106536503B (en) * 2014-04-18 2019-09-06 北京澳合药物研究院有限公司 A kind of tyrosine kinase inhibitor and application thereof
CN104130265B (en) * 2014-04-29 2017-01-25 苏州景泓生物技术有限公司 Spiral ring or bridged ring containing pyrimidine compound
GB201410430D0 (en) 2014-06-11 2014-07-23 Redx Pharma Ltd Compounds
KR102130600B1 (en) 2014-07-03 2020-07-08 베이진 엘티디 Anti-PD-L1 Antibodies and Their Use as Therapeutics and Diagnostics
CN105315285B (en) * 2014-07-25 2017-12-08 上海海雁医药科技有限公司 2,4 2 substitution 7H pyrrolo-es [2,3 d] pyrimidine derivatives, its preparation method and purposes pharmaceutically
CN106661002B (en) 2014-08-04 2021-06-29 纽韦卢森公司 Pyrimidine derivatives for the treatment of inflammatory, metabolic, neoplastic and autoimmune diseases
CN106715456B (en) 2014-08-12 2023-08-29 莫纳什大学 Prodrugs of directed lymphatics
ES2741785T3 (en) 2014-08-13 2020-02-12 Celgene Car Llc Forms and compositions of an ERK inhibitor
EP3185868B1 (en) * 2014-08-25 2022-04-06 Salk Institute for Biological Studies Novel ulk1 inhibitors and methods using same
CN105399685B (en) * 2014-09-16 2018-05-22 深圳微芯生物科技有限责任公司 The alternatively preparation method and applications of the heteroaromatic compounds of property JAK3 and/or JAK1 kinase inhibitors
CN105399686B (en) * 2014-09-16 2018-05-22 深圳微芯生物科技有限责任公司 Pyrimidine derivatives, its preparation method and its application
CN105481778B (en) * 2014-09-16 2019-06-04 深圳微芯生物科技股份有限公司 Pyrimidine derivatives, preparation method and its application
PT3193611T (en) 2014-09-17 2021-05-28 Celgene Car Llc Mk2 inhibitors and uses thereof
CN117069700A (en) * 2014-10-11 2023-11-17 上海翰森生物医药科技有限公司 EGFR inhibitor and preparation and application thereof
JP6649540B2 (en) 2014-10-14 2020-02-19 ノース・アンド・サウス・ブラザー・ファーマシー・インベストメント・カンパニー・リミテッド Substituted heteroaryl compounds and methods of use
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
CN105601573B (en) 2014-11-24 2021-07-02 中国科学院上海药物研究所 2-aminopyrimidine compound and pharmaceutical composition and application thereof
JP2017537327A (en) * 2014-12-11 2017-12-14 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung BTK inhibitor assay
AU2015362728B2 (en) 2014-12-16 2020-06-25 Signal Pharmaceuticals, Llc Formulations of 2-(tert-butylamino)-4-((1R,3R,4R)-3-hydroxy-4-methycyclohexylamino)-pyrimidine-5-carboxamide
ES2882954T3 (en) 2014-12-16 2021-12-03 Signal Pharm Llc Medical uses comprising methods for the measurement of inhibition of c-Jun N-terminal kinase in the skin
EP3250557A4 (en) 2015-01-29 2018-06-20 Signal Pharmaceuticals, LLC Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
HUE038041T2 (en) 2015-01-30 2018-10-29 Taiho Pharmaceutical Co Ltd Novel salt of fused pyrimidine compound and crystal thereof
SG11201704430SA (en) * 2015-01-30 2017-08-30 Taiho Pharmaceutical Co Ltd Preventive and/or therapeutic agent of immune disease
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41551A (en) 2015-02-20 2017-12-26 Incyte Corp BICYCLIC HETEROCYCLES USED AS FGFR4 INHIBITORS
TWI712601B (en) 2015-02-20 2020-12-11 美商英塞特公司 Bicyclic heterocycles as fgfr inhibitors
ES2930585T3 (en) 2015-02-27 2022-12-19 Nimbus Lakshmi Inc TYK2 inhibitors and uses thereof
WO2017004134A1 (en) 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
KR20180041119A (en) * 2015-07-09 2018-04-23 메르크 파텐트 게엠베하 Pyrimidine Derivatives as BTK Inhibitors and Their Uses
WO2017019487A1 (en) 2015-07-24 2017-02-02 Celgene Corporation Methods of synthesis of (1r,2r,5r)-5-amino-2-methylcyclohexanol hydrochloride and intermediates useful therein
MX2018002554A (en) 2015-08-31 2018-08-14 Pharmacyclics Llc Btk inhibitor combinations for treating multiple myeloma.
EP3344624B8 (en) 2015-09-02 2023-11-29 Takeda Pharmaceutical Company Limited Tyk2 inhibitors and uses thereof
EP3347340A4 (en) 2015-09-08 2019-01-23 Monash University Lymph directing prodrugs
WO2017044720A1 (en) 2015-09-11 2017-03-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
MX2018003351A (en) 2015-09-16 2018-09-17 Loxo Oncology Inc Pyrazolopyrimidine derivatives as btk inhibitors for the treatment of cancer.
CN106554347B (en) * 2015-09-25 2020-10-30 浙江博生医药有限公司 EGFR kinase inhibitor and preparation method and application thereof
BR112018006939A2 (en) 2015-10-09 2018-10-16 Acea Therapeutics Inc pharmaceutical salts, physical forms, and compositions of pyrrole-pyrimidine kinase inhibitors, and methods for producing them
MA47013A (en) 2015-10-21 2018-08-29 Otsuka Pharma Co Ltd BENZOLACTAM COMPOUNDS USED AS KINASE PROTEIN INHIBITORS
ES2941969T3 (en) 2015-10-23 2023-05-29 Navitor Pharm Inc Modulators of the Sestrin-GATOR2 Interaction and Their Uses
EP3389664A4 (en) 2015-12-14 2020-01-08 Raze Therapeutics Inc. Caffeine inhibitors of mthfd2 and uses thereof
AU2016373530B2 (en) 2015-12-16 2021-01-21 Loxo Oncology, Inc. Compounds useful as kinase inhibitors
CN107021963A (en) 2016-01-29 2017-08-08 北京诺诚健华医药科技有限公司 Pyrazole fused ring analog derivative, its preparation method and its application in treating cancer, inflammation and immunity disease
US11014882B2 (en) * 2016-03-09 2021-05-25 Raze Therapeutics, Inc. 3-phosphoglycerate dehydrogenase inhibitors and uses thereof
PL3426243T3 (en) 2016-03-09 2021-10-04 Raze Therapeutics, Inc. 3-phosphoglycerate dehydrogenase inhibitors and uses thereof
US10709708B2 (en) 2016-03-17 2020-07-14 The University Of North Carolina At Chapel Hill Method of treating cancer with a combination of MER tyrosine kinase inhibitor and an epidermal growth factor receptor (EGFR) inhibitor
CN109153722A (en) 2016-04-08 2019-01-04 X4 制药有限公司 Method for treating cancer
CN105968056A (en) * 2016-05-28 2016-09-28 大连医科大学 Diarylpyrimidine compound, composition and application
EP3472129A4 (en) 2016-06-21 2019-12-04 X4 Pharmaceuticals, Inc. Cxcr4 inhibitors and uses thereof
EP3471726A4 (en) 2016-06-21 2019-10-09 X4 Pharmaceuticals, Inc. Cxcr4 inhibitors and uses thereof
US10759796B2 (en) 2016-06-21 2020-09-01 X4 Pharmaceuticals, Inc. CXCR4 inhibitors and uses thereof
EP3481393B1 (en) 2016-07-05 2021-04-14 Beigene, Ltd. Combination of a pd-1 antagonist and a raf inhibitor for treating cancer
SG11201901141WA (en) 2016-08-16 2019-03-28 Beigene Ltd Crystalline form of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof
US11701357B2 (en) 2016-08-19 2023-07-18 Beigene Switzerland Gmbh Treatment of B cell cancers using a combination comprising Btk inhibitors
CN106316886A (en) * 2016-08-24 2017-01-11 泰州精英化成医药科技有限公司 Cis form-3- (tert butoxycarbonylamino) naphthenic acid preparing method
CN109982687A (en) 2016-09-19 2019-07-05 梅制药公司 Conjoint therapy
JP7082130B2 (en) 2016-10-14 2022-06-07 ニンバス ラクシュミ, インコーポレイテッド TYK2 inhibitors and their use
JP7082120B2 (en) 2016-10-21 2022-06-07 ニンバス ラクシュミ, インコーポレイテッド TYK2 inhibitors and their use
CN107973754B (en) * 2016-10-25 2020-04-14 清华大学 Small molecule inhibitor, preparation method thereof and application thereof in treatment of multiple myeloma
JP2020023441A (en) * 2016-11-02 2020-02-13 国立大学法人九州大学 Novel compound useful for egfr inhibition and tumor treatment
MX2019005029A (en) 2016-11-03 2019-10-24 Juno Therapeutics Inc Combination therapy of a t cell therapy and a btk inhibitor.
EP3538091A4 (en) 2016-11-08 2020-06-10 Navitor Pharmaceuticals, Inc. PHENYL AMINO PIPERIDINE mTORC INHIBITORS AND USES THEREOF
EP3548005A4 (en) 2016-11-29 2020-06-17 Puretech Health LLC Exosomes for delivery of therapeutic agents
US11091451B2 (en) 2016-12-05 2021-08-17 Raze Therapeutics, Inc. SHMT inhibitors and uses thereof
EP3559018A1 (en) 2016-12-23 2019-10-30 Bicyclerd Limited Peptide derivatives having novel linkage structures
CN106632273A (en) * 2016-12-29 2017-05-10 大连医科大学 Pyrimidine compound containing azole heterocycle, composition and applications of pyrimidine compound and combination
EP3565638B8 (en) 2017-01-06 2024-04-10 BicycleRD Limited Bicycle conjugate for treating cancer
CN108329274B (en) * 2017-01-13 2021-09-03 正大天晴药业集团股份有限公司 Bruton's tyrosine kinase inhibitors
TWI774726B (en) 2017-01-25 2022-08-21 英屬開曼群島商百濟神州有限公司 Crystalline forms of (s)-7-(1-(but-2-ynoyl)piperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof
CN108498477A (en) * 2017-02-27 2018-09-07 江苏奥赛康药业股份有限公司 A kind of Pharmaceutical composition and preparation method thereof of 2- amino-metadiazine compounds
WO2018165240A1 (en) 2017-03-08 2018-09-13 Nimbus Lakshmi, Inc. Tyk2 inhibitors, uses, and methods for production thereof
EP3375778A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aryl-piperidine derivatives
EP3375784A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aza-dihydro-acridone derivatives
BR112019020840A2 (en) 2017-04-07 2020-04-28 Acea Therapeutics Inc pharmaceutical salts, physical forms and compositions of pyrrolopyrimidine kinase inhibitors and methods of producing them
JOP20190233A1 (en) 2017-04-14 2019-10-02 Biogen Ma Inc Benzoazepine analogs as inhibiting agents for bruton's tyrosine kinase
GB201706327D0 (en) 2017-04-20 2017-06-07 Otsuka Pharma Co Ltd A pharmaceutical compound
EP3615550A1 (en) 2017-04-27 2020-03-04 BicycleTx Limited Bicyclic peptide ligands and uses thereof
AR111960A1 (en) 2017-05-26 2019-09-04 Incyte Corp CRYSTALLINE FORMS OF A FGFR INHIBITOR AND PROCESSES FOR ITS PREPARATION
CN110996955A (en) 2017-06-22 2020-04-10 细胞基因公司 Treatment of hepatocellular carcinoma characterized by hepatitis B virus infection
WO2019002842A1 (en) 2017-06-26 2019-01-03 Bicyclerd Limited Bicyclic peptide ligands with detectable moieties and uses thereof
EP3645569A4 (en) 2017-06-26 2021-03-24 BeiGene, Ltd. Immunotherapy for hepatocellular carcinoma
US11046698B2 (en) 2017-07-28 2021-06-29 Nimbus Lakshmi, Inc. TYK2 inhibitors and uses thereof
CN110997677A (en) 2017-08-12 2020-04-10 百济神州有限公司 Btk inhibitors with improved dual selectivity
US20200283482A1 (en) 2017-08-14 2020-09-10 Bicyclerd Limited Bicyclic peptide ligand prr-a conjugates and uses thereof
EP3668887A1 (en) 2017-08-14 2020-06-24 Bicyclerd Limited Bicyclic peptide ligand sting conjugates and uses thereof
WO2019034153A1 (en) * 2017-08-18 2019-02-21 北京韩美药品有限公司 Chemical compound, pharmaceutical composition thereof, and use and application thereof
WO2019046491A1 (en) 2017-08-29 2019-03-07 Ariya Therapeutics, Inc. Lymphatic system-directing lipid prodrugs
US11883497B2 (en) 2017-08-29 2024-01-30 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
KR102383561B1 (en) * 2017-09-07 2022-04-06 한국화학연구원 Tetrahydroisoquinoline substituted pyrimidine derivative, optical isomer thereof, or pharmaceutically acceptable salts thereof, and composition comprising its same for preventing or treating of cancer
IL295603B2 (en) 2017-09-22 2024-03-01 Kymera Therapeutics Inc Protein degraders and uses thereof
EP3684366A4 (en) 2017-09-22 2021-09-08 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
EP3707138B1 (en) 2017-11-06 2022-07-13 Bristol-Myers Squibb Company Isofuranone compounds useful as hpk1 inhibitors
US10683297B2 (en) 2017-11-19 2020-06-16 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
US11786529B2 (en) 2017-11-29 2023-10-17 Beigene Switzerland Gmbh Treatment of indolent or aggressive B-cell lymphomas using a combination comprising BTK inhibitors
TWI825046B (en) 2017-12-19 2023-12-11 英商拜西可泰克斯有限公司 Bicyclic peptide ligands specific for epha2
GB201721265D0 (en) 2017-12-19 2018-01-31 Bicyclerd Ltd Bicyclic peptide ligands specific for EphA2
EP3727362A4 (en) 2017-12-19 2021-10-06 PureTech LYT, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
US11304954B2 (en) 2017-12-19 2022-04-19 Puretech Lyt, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
US11608345B1 (en) 2017-12-19 2023-03-21 Puretech Lyt, Inc. Lipid prodrugs of rapamycin and its analogs and uses thereof
US10874743B2 (en) 2017-12-26 2020-12-29 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
US11485743B2 (en) 2018-01-12 2022-11-01 Kymera Therapeutics, Inc. Protein degraders and uses thereof
US11512080B2 (en) 2018-01-12 2022-11-29 Kymera Therapeutics, Inc. CRBN ligands and uses thereof
BR112020015328A2 (en) 2018-01-29 2020-12-08 Merck Patent Gmbh GCN2 INHIBITORS AND USES OF THE SAME
BR112020015396A2 (en) 2018-01-29 2020-12-08 Merck Patent Gmbh GCN2 INHIDERS AND USES OF THE SAME
TWI798334B (en) 2018-01-31 2023-04-11 大陸商迪哲(江蘇)醫藥股份有限公司 Erbb/btk inhibitors
AU2019229258B2 (en) 2018-02-27 2023-09-14 Artax Biopharma Inc. Chromene derivatives as inhibitors of TCR-Nck interaction
AU2019247498A1 (en) 2018-04-05 2020-11-26 Sumitomo Pharma Oncology, Inc. AXL kinase inhibitors and use of the same
US10815225B2 (en) 2018-04-24 2020-10-27 Merck Patent Gmbh Antiproliferation compounds and uses thereof
CA3097774A1 (en) 2018-04-24 2019-10-31 Vertex Pharmaceuticals Incorporated Pteridinone compounds and uses thereof
CA3098283C (en) 2018-04-26 2023-05-23 Pfizer Inc. 2-amino-pyridine or 2-amino-pyrimidine derivatives as cyclin dependent kinase inhibitors
KR20210044736A (en) 2018-05-03 2021-04-23 주노 쎄러퓨티크스 인코퍼레이티드 Combination therapy of chimeric antigen receptor (CAR) T cell therapy and kinase inhibitor
BR112020022392A2 (en) 2018-05-04 2021-02-02 Incyte Corporation solid forms of a fgfr inhibitor and processes for preparing them
US11174257B2 (en) 2018-05-04 2021-11-16 Incyte Corporation Salts of an FGFR inhibitor
US10980784B2 (en) 2018-06-15 2021-04-20 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
GB201810316D0 (en) 2018-06-22 2018-08-08 Bicyclerd Ltd Peptide ligands for binding to EphA2
US11180531B2 (en) 2018-06-22 2021-11-23 Bicycletx Limited Bicyclic peptide ligands specific for Nectin-4
EP3817748A4 (en) 2018-07-06 2022-08-24 Kymera Therapeutics, Inc. Tricyclic crbn ligands and uses thereof
KR20210038906A (en) 2018-07-26 2021-04-08 스미토모 다이니폰 파마 온콜로지, 인크. Methods of treating diseases associated with abnormal ACVR1 expression and ACVR1 inhibitors for use therein
US10548889B1 (en) 2018-08-31 2020-02-04 X4 Pharmaceuticals, Inc. Compositions of CXCR4 inhibitors and methods of preparation and use
US20220089587A1 (en) 2018-09-07 2022-03-24 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
EP3866789A4 (en) 2018-10-15 2022-07-06 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
JP2022512779A (en) 2018-10-23 2022-02-07 バイスクルテクス・リミテッド Bicyclic peptide ligands and their use
CN109608444B (en) * 2018-11-27 2022-02-11 中国药科大学 Isoindolinone-containing ERK inhibitor and preparation method and application thereof
EP3886904A4 (en) 2018-11-30 2022-07-13 Kymera Therapeutics, Inc. Irak degraders and uses thereof
CA3120866A1 (en) 2018-11-30 2020-06-04 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
EP3670659A1 (en) 2018-12-20 2020-06-24 Abivax Biomarkers, and uses in treatment of viral infections, inflammations, or cancer
US11174264B2 (en) 2019-01-23 2021-11-16 Nimbus Lakshmi, Inc. TYK2 inhibitors and uses thereof
CN109776495A (en) * 2019-01-31 2019-05-21 李佳睿 Antitumoral compounds and preparation method thereof and purposes
WO2020165600A1 (en) 2019-02-14 2020-08-20 Bicycletx Limited Bicyclic peptide ligand sting conjugates and uses thereof
WO2020168197A1 (en) 2019-02-15 2020-08-20 Incyte Corporation Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors
TW202100520A (en) 2019-03-05 2021-01-01 美商英塞特公司 Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11919904B2 (en) 2019-03-29 2024-03-05 Incyte Corporation Sulfonylamide compounds as CDK2 inhibitors
JP2022528887A (en) 2019-04-02 2022-06-16 バイスクルテクス・リミテッド Bicycle toxin conjugates and their use
AU2020253633A1 (en) 2019-04-05 2021-11-04 Kymera Therapeutics, Inc. STAT degraders and uses thereof
WO2020223558A1 (en) 2019-05-01 2020-11-05 Incyte Corporation Tricyclic amine compounds as cdk2 inhibitors
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
CN114072397A (en) 2019-05-10 2022-02-18 德西费拉制药有限责任公司 Heteroaryl aminopyrimidine amide autophagy inhibitors and methods of use thereof
LT3966207T (en) 2019-05-10 2023-12-11 Deciphera Pharmaceuticals, Llc Phenylaminopyrimidine amide autophagy inhibitors and methods of use thereof
BR112021024224A2 (en) 2019-05-31 2022-04-26 Ikena Oncology Inc Tead inhibitors and uses thereof
MA56191A (en) 2019-06-17 2022-04-20 Deciphera Pharmaceuticals Llc AMINOPYRIMIDINE AMIDE AUTOPHAGY INHIBITORS AND METHODS OF USE THEREOF
US20220388968A1 (en) * 2019-06-18 2022-12-08 Purdue Research Foundation Inhibitors of erythrocyte band 3 tyrosine phosphorylation and uses thereof
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CN110305140B (en) * 2019-07-30 2020-08-04 上海勋和医药科技有限公司 Dihydropyrrolopyrimidines selective JAK2 inhibitors
CN116348458A (en) 2019-08-14 2023-06-27 因赛特公司 Imidazolylpyrimidinylamine compounds as CDK2 inhibitors
WO2021050992A1 (en) 2019-09-11 2021-03-18 Vincere Biosciences, Inc. Usp30 inhibitors and uses thereof
BR112022004451A2 (en) 2019-09-13 2022-06-21 Nimbus Saturn Inc hpk1 antagonists and uses thereof
CN112574207B (en) * 2019-09-30 2023-04-11 南京药石科技股份有限公司 ERK1/2 protein kinase inhibitor and application thereof
BR112022006977A2 (en) 2019-10-11 2022-09-20 Incyte Corp BICYCLIC AMINES AS CDK2 INHIBITORS
MX2022004513A (en) 2019-10-14 2022-07-19 Incyte Corp Bicyclic heterocycles as fgfr inhibitors.
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN112773802B (en) * 2019-11-08 2023-11-21 深圳微芯生物科技股份有限公司 Use of compound for preventing or treating graft-versus-host disease
EP4066838A4 (en) * 2019-11-26 2023-12-27 Shenzhen Chipscreen Biosciences Co., Ltd. Composition containing aromatic heterocyclic compound in amorphous form, and preparation method therefor and use thereof
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
EP4069695A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Derivatives of an fgfr inhibitor
BR112022010754A2 (en) 2019-12-05 2022-08-23 Anakuria Therapeutics Inc RAPAMICIN ANALOGS AND USES THEREOF
TW202136251A (en) 2019-12-17 2021-10-01 美商凱麥拉醫療公司 Irak degraders and uses thereof
WO2021127283A2 (en) 2019-12-17 2021-06-24 Kymera Therapeutics, Inc. Irak degraders and uses thereof
MX2022007265A (en) 2019-12-20 2022-09-09 Nuevolution As Compounds active towards nuclear receptors.
KR20220151160A (en) 2019-12-23 2022-11-14 카이메라 쎄라퓨틱스 인코포레이티드 SMARCA disintegrant and its uses
CN111620852B (en) * 2020-01-19 2023-05-09 镇江植生源农业科技有限公司 5-chloro-pyrimidine-2, 4-diamine compound, and preparation method and application thereof
CN115515685A (en) 2020-03-03 2022-12-23 皮克医疗公司 EIF4E inhibitor and application thereof
CN115776887A (en) 2020-03-19 2023-03-10 凯麦拉医疗公司 MDM2 degrading agents and uses thereof
CA3174176A1 (en) 2020-03-31 2021-10-07 Sanne Schroder Glad Compounds active towards nuclear receptors
WO2021198955A1 (en) 2020-03-31 2021-10-07 Nuevolution A/S Compounds active towards nuclear receptors
TW202210483A (en) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Crystalline forms of irak degraders
CN111646978B (en) * 2020-06-11 2021-12-21 浙江大学 N2-substituted alkoxy aromatic ring-2-aminopyrimidine derivatives and application thereof
US20230257350A1 (en) * 2020-07-02 2023-08-17 The Cleveland Clinic Foundation Compounds and methods of promoting oligodendrocyte precursor differentiation
EP4196792A1 (en) 2020-08-17 2023-06-21 BicycleTX Limited Bicycle conjugates specific for nectin-4 and uses thereof
WO2022072632A1 (en) * 2020-09-30 2022-04-07 Scorpion Therapeutics, Inc. Bicyclic compounds for use in the treatment cancer
CA3200814A1 (en) 2020-12-02 2022-06-09 Alfredo C. Castro Tead inhibitors and uses thereof
WO2022120353A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead inhibitors and uses thereof
AU2022216810A1 (en) 2021-02-02 2023-08-24 Liminal Biosciences Limited Gpr84 antagonists and uses thereof
JP2024506858A (en) * 2021-02-02 2024-02-15 リミナル・バイオサイエンシーズ・リミテッド GPR84 antagonists and their uses
US11773103B2 (en) 2021-02-15 2023-10-03 Kymera Therapeutics, Inc. IRAK4 degraders and uses thereof
WO2022187856A1 (en) 2021-03-05 2022-09-09 Nimbus Saturn, Inc. Hpk1 antagonists and uses thereof
WO2022212893A1 (en) 2021-04-02 2022-10-06 Biogen Ma Inc. Combination treatment methods of multiple sclerosis
CA3215081A1 (en) 2021-04-16 2022-10-20 Alfredo C. Castro Mek inhibitors and uses thereof
WO2022261160A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US20230150997A1 (en) 2021-08-25 2023-05-18 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
US20230134932A1 (en) 2021-08-25 2023-05-04 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
WO2023114984A1 (en) 2021-12-17 2023-06-22 Ikena Oncology, Inc. Tead inhibitors and uses thereof
WO2023173057A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023173053A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023211889A1 (en) 2022-04-25 2023-11-02 Ikena Oncology, Inc. Polymorphic compounds and uses thereof
WO2023220655A1 (en) 2022-05-11 2023-11-16 Celgene Corporation Methods to overcome drug resistance by re-sensitizing cancer cells to treatment with a prior therapy via treatment with a t cell therapy
US11878958B2 (en) 2022-05-25 2024-01-23 Ikena Oncology, Inc. MEK inhibitors and uses thereof
US11786531B1 (en) 2022-06-08 2023-10-17 Beigene Switzerland Gmbh Methods of treating B-cell proliferative disorder
WO2024028364A1 (en) 2022-08-02 2024-02-08 Liminal Biosciences Limited Aryl-triazolyl and related gpr84 antagonists and uses thereof
WO2024028363A1 (en) 2022-08-02 2024-02-08 Liminal Biosciences Limited Heteroaryl carboxamide and related gpr84 antagonists and uses thereof
WO2024028365A1 (en) 2022-08-02 2024-02-08 Liminal Biosciences Limited Substituted pyridone gpr84 antagonists and uses thereof
CN115448906B (en) * 2022-09-26 2024-04-02 深圳大学 2-anilinopyrimidine derivative and preparation method and application thereof

Family Cites Families (174)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4032637A (en) 1972-09-26 1977-06-28 Sandoz Ltd. Method of promoting sleep
US5650270A (en) 1982-02-01 1997-07-22 Northeastern University Molecular analytical release tags and their use in chemical analysis
US4709016A (en) 1982-02-01 1987-11-24 Northeastern University Molecular analytical release tags and their use in chemical analysis
US4650750A (en) 1982-02-01 1987-03-17 Giese Roger W Method of chemical analysis employing molecular release tag compounds
US5516931A (en) 1982-02-01 1996-05-14 Northeastern University Release tag compounds producing ketone signal groups
GB8608335D0 (en) 1986-04-04 1986-05-08 Pfizer Ltd Pharmaceutically acceptable salts
US5453510A (en) 1990-07-13 1995-09-26 Burroughs Wellcome Co. Neuromuscular blocking agents
JPH0741461A (en) 1993-05-27 1995-02-10 Eisai Co Ltd Sulfonic acid ester derivative
ES2208737T3 (en) 1995-03-10 2004-06-16 Berlex Laboratories, Inc. DERIVATIVES OF BENZAMIDINE, ITS PREPARATION AND ITS USE AS ANTICOAGULANTS.
GB9523675D0 (en) * 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
GB9619284D0 (en) * 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
GB9622363D0 (en) * 1996-10-28 1997-01-08 Celltech Therapeutics Ltd Chemical compounds
EP1054004B1 (en) 1997-12-15 2008-07-16 Astellas Pharma Inc. Novel pyrimidine-5-carboxamide derivatives
US6303652B1 (en) * 1998-08-21 2001-10-16 Hughes Institute BTK inhibitors and methods for their identification and use
ES2274634T3 (en) * 1998-08-29 2007-05-16 Astrazeneca Ab PIRIMIDINE COMPOUNDS.
IL143023A0 (en) 1998-11-10 2002-04-21 Janssen Pharmaceutica Nv Hiv replication inhibiting pyrimidines
US6262088B1 (en) * 1998-11-19 2001-07-17 Berlex Laboratories, Inc. Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants
US6127376A (en) * 1998-12-04 2000-10-03 Berlex Laboratories, Inc. Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants
GB9828511D0 (en) * 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
US6495558B1 (en) * 1999-01-22 2002-12-17 Amgen Inc. Kinase inhibitors
AU2871900A (en) 1999-02-04 2000-08-25 Millennium Pharmaceuticals, Inc. G-protein coupled heptahelical receptor binding compounds and methods of use thereof
GB9914258D0 (en) * 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
PL352476A1 (en) 1999-06-29 2003-08-25 Egyt Gyogyszervegyeszeti Gyar Novel derivatives of piperazinylalkylthiopyrimidine, parmacological compositions containing tese compounds and method of obtaining active substance
CA2394727A1 (en) 1999-12-28 2001-07-05 Pharmacopeia, Inc. Pyrimidine and triazine kinase inhibitors
CN1429222A (en) * 2000-02-17 2003-07-09 安姆根有限公司 Kinase inhibitors
GB0004887D0 (en) * 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004888D0 (en) * 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US7034019B2 (en) 2000-05-08 2006-04-25 Janssen Pharmaceutica N.V. Prodrugs of HIV replication inhibiting pyrimidines
GB0016877D0 (en) * 2000-07-11 2000-08-30 Astrazeneca Ab Chemical compounds
US7427689B2 (en) 2000-07-28 2008-09-23 Georgetown University ErbB-2 selective small molecule kinase inhibitors
US6881737B2 (en) 2001-04-11 2005-04-19 Amgen Inc. Substituted triazinyl acrylamide derivatives and methods of use
JO3429B1 (en) 2001-08-13 2019-10-20 Janssen Pharmaceutica Nv Hiv inhibiting pyrimidines derivatives
US6939874B2 (en) * 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
WO2003030909A1 (en) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
CA2463822A1 (en) * 2001-11-01 2003-05-08 Janssen Pharmaceutica N.V. Heteroaryl amines as glycogen synthase kinase 3beta inhibitors (gsk3 inhibitors)
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
JP2005522438A (en) 2002-02-08 2005-07-28 スミスクライン ビーチャム コーポレーション Pyrimidine compounds
GB0206215D0 (en) * 2002-03-15 2002-05-01 Novartis Ag Organic compounds
EP1579186A4 (en) * 2002-03-21 2008-10-08 Sunesis Pharmaceuticals Inc Identification of kinase inhibitors
US20040002395A1 (en) * 2002-06-27 2004-01-01 Poynor Raymond L. Bridge weight for metal wood golf club
BR0313059B8 (en) 2002-07-29 2021-07-27 Rigel Pharmaceuticals compound, and, pharmaceutical composition
CA2439440A1 (en) * 2002-09-05 2004-03-05 Emory University Treatment of tuberous sclerosis associated neoplasms
AU2002951853A0 (en) 2002-10-04 2002-10-24 Commonwealth Scientific And Industrial Research Organisation Crystal structure of erbb2 and uses thereof
AU2002350719A1 (en) 2002-11-29 2004-06-23 Janssen Pharmaceutica N.V. Pharmaceutical compositions comprising a basic respectively acidic drug compound, a surfactant and a physiologically tolerable water-soluble acid respectively base
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
WO2004069812A1 (en) 2003-02-07 2004-08-19 Janssen Pharmaceutica N.V. Pyrimidine derivatives for the prevention of hiv infection
EP1597251B1 (en) * 2003-02-20 2009-06-10 SmithKline Beecham Corporation Pyrimidine compounds
GB0305929D0 (en) * 2003-03-14 2003-04-23 Novartis Ag Organic compounds
US20050014753A1 (en) * 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
US20050043233A1 (en) 2003-04-29 2005-02-24 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis
US7504396B2 (en) * 2003-06-24 2009-03-17 Amgen Inc. Substituted heterocyclic compounds and methods of use
PT1656372E (en) 2003-07-30 2013-06-27 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
DK1663242T3 (en) * 2003-08-07 2011-08-01 Rigel Pharmaceuticals Inc 2,4-Pyrimidinediamine compounds and use as antiproliferative agents
PL1660458T3 (en) * 2003-08-15 2012-07-31 Novartis Ag 2, 4-pyrimidinediamines useful in the treatment of neoplastic diseases, inflammatory and immune system disorders
GB0321710D0 (en) * 2003-09-16 2003-10-15 Novartis Ag Organic compounds
CA2538413A1 (en) 2003-09-18 2005-03-24 Novartis Ag 2,4-di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
EP1694652A1 (en) 2003-12-19 2006-08-30 Rigel Pharmaceuticals, Inc. Stereoisomers and stereoisomeric mixtures of 1-(2,4-pyrimidinediamino)-2-cyclopentanecarboxamide synthetic intermediates
ES2389203T3 (en) * 2004-01-12 2012-10-24 Ym Biosciences Australia Pty Ltd Selective kinase inhibitors
GT200500008A (en) 2004-01-16 2005-08-16 QUINOLINE INTERMEDIARIES AS INHIBITORS OF THIROSINE KINASE RECEPTORS AND THE SYNTHESIS OF THE SAME
CA2557794A1 (en) * 2004-03-15 2005-10-06 Eli Lilly And Company Opioid receptor antagonists
WO2005105988A2 (en) * 2004-04-28 2005-11-10 Vertex Pharmaceuticals Incorporated Crystal structure of human jak3 kinase domain complex and binding pockets thereof
JP4812763B2 (en) * 2004-05-18 2011-11-09 ライジェル ファーマシューティカルズ, インコーポレイテッド Cycloalkyl-substituted pyrimidinediamine compounds and uses thereof
EP1598343A1 (en) * 2004-05-19 2005-11-23 Boehringer Ingelheim International GmbH 2-Arylaminopyrimidine derivatives as PLK inhibitors
CA2569520C (en) * 2004-06-04 2023-03-14 Genentech, Inc. Kras mutations for identifying colorectal tumors responsive to cetuximab or panitumumab
US7521457B2 (en) 2004-08-20 2009-04-21 Boehringer Ingelheim International Gmbh Pyrimidines as PLK inhibitors
GB0419161D0 (en) * 2004-08-27 2004-09-29 Novartis Ag Organic compounds
CA2581454A1 (en) * 2004-09-23 2006-03-30 Reddy Us Therapeutics, Inc. Novel pyrimidine compounds, process for their preparation and compositions containing them
BRPI0515935B8 (en) * 2004-09-30 2021-05-25 Janssen Sciences Ireland Uc heterocyclyl- or 5-carbo substituted pyrimidines for inhibition of hiv, and pharmaceutical composition
CA2580913A1 (en) * 2004-10-13 2006-04-27 Wyeth N-benzenesulfonyl substituted anilino-pyrimidine analogs
EP2100899A3 (en) 2004-10-20 2009-09-30 Proteolix, Inc. Compounds for proteasome enzyme inhibition
WO2006053109A1 (en) 2004-11-10 2006-05-18 Synta Pharmaceuticals Corp. Heteroaryl compounds
GB2420559B (en) 2004-11-15 2008-08-06 Rigel Pharmaceuticals Inc Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
US7557207B2 (en) 2004-11-24 2009-07-07 Rigel Pharmaceuticals, Inc. Spiro 2,4-pyrimidinediamine compounds and their uses
MY169441A (en) 2004-12-08 2019-04-11 Janssen Pharmaceutica Nv 2,4, (4,6) pyrimidine derivatives
WO2006074057A2 (en) 2004-12-30 2006-07-13 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
EP1856053A1 (en) 2005-01-14 2007-11-21 Millennium Pharmaceuticals, Inc. Cinnamide and hydrocinnamide derivatives with raf-kinase inhibitory activity
RU2416616C2 (en) 2005-01-19 2011-04-20 Райджел Фармасьютикалз, Инк. Prodrugs of 2,4-pyrimidine diamine compounds and use thereof
US8067175B2 (en) * 2005-02-11 2011-11-29 Memorial Sloan-Kettering Cancer Center Methods and compositions for detecting a drug resistant EGFR mutant
EP1863794A2 (en) * 2005-03-16 2007-12-12 Targegen, Inc. Pyrimidine compounds and methods of use
DE102005016634A1 (en) 2005-04-12 2006-10-19 Merck Patent Gmbh Novel aza heterocycles as kinase inhibitors
US20060270694A1 (en) * 2005-05-03 2006-11-30 Rigel Pharmaceuticals, Inc. JAK kinase inhibitors and their uses
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
WO2006128129A2 (en) 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating cancer
WO2006128172A2 (en) * 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating b cell regulated autoimmune disorders
WO2006129100A1 (en) 2005-06-03 2006-12-07 Glaxo Group Limited Novel compounds
KR101312225B1 (en) * 2005-06-08 2013-09-26 리겔 파마슈티칼스, 인크. Compositions and methods for inhibition of the jak pathway
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
UA96265C2 (en) * 2005-06-08 2011-10-25 Райджел Фармасьютикалс, Инк. Composition and method for inhibition of the jak pathway
EP1926734A1 (en) 2005-08-22 2008-06-04 Amgen Inc. Pyrazolopyridine and pyrazolopyrimidine compounds useful as kinase enzymes modulators
WO2007048064A2 (en) 2005-10-21 2007-04-26 Exelixis, Inc. Amino-pyrimidines as casein kinase ii (ck2) modulators
EP1951684B1 (en) * 2005-11-01 2016-07-13 TargeGen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
JP2009514876A (en) * 2005-11-03 2009-04-09 アイアールエム・リミテッド・ライアビリティ・カンパニー Compounds and compositions for protein kinases
US7713987B2 (en) 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
US20080318989A1 (en) 2005-12-19 2008-12-25 Burdick Daniel J Pyrimidine Kinase Inhibitors
TW200736232A (en) * 2006-01-26 2007-10-01 Astrazeneca Ab Pyrimidine derivatives
AU2007209928B2 (en) * 2006-01-30 2013-03-28 Exelixis, Inc. 4-aryl-2-amino-pyrimidines or 4-aryl-2-aminoalkyl-pyrimidines as JAK-2 modulators and pharmaceutical compositions containing them
PT1984357E (en) 2006-02-17 2013-12-23 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds for treating or preventing autoimmune diseases
EP1991532B1 (en) * 2006-02-24 2017-01-11 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
BRPI0709690B8 (en) 2006-03-30 2021-05-25 Janssen R & D Ireland 5-starch substituted pyrimidines and pharmaceutical composition comprising them
WO2007113256A1 (en) 2006-03-30 2007-10-11 Tibotec Pharmaceuticals Ltd. Hiv inhibiting 5-(hydroxymethylene and aminomethylene) substituted pyrimidines
GB0608386D0 (en) 2006-04-27 2006-06-07 Senexis Ltd Compounds
WO2007136790A2 (en) 2006-05-18 2007-11-29 Mannkind Corporation Intracellular kinase inhibitors
DE102006027156A1 (en) * 2006-06-08 2007-12-13 Bayer Schering Pharma Ag New sulfimide compounds are protein kinase inhibitors useful to treat e.g. cancer, Hodgkin's lymphoma, Kaposi's sarcoma, cardiovascular disease, Crohn's disease, endometriosis and hemangioma
AU2007269540B2 (en) 2006-07-05 2013-06-27 Exelixis, Inc. Methods of using IGF1R and Abl kinase modulators
CA2657260A1 (en) 2006-07-21 2008-01-24 Novartis Ag 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors
DE102006041382A1 (en) 2006-08-29 2008-03-20 Bayer Schering Pharma Ag Carbamoyl sulfoximides as protein kinase inhibitors
DK2526934T3 (en) 2006-09-22 2016-03-07 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase
WO2008049123A2 (en) * 2006-10-19 2008-04-24 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine derivatives as inhibitors of jak kinases for the treatment of autoimmune diseases
ES2403546T3 (en) * 2006-11-03 2013-05-20 Pharmacyclics, Inc. Bruton tyrosine kinase activity probe and method of use
EP2420505A1 (en) 2006-11-21 2012-02-22 Rigel Pharmaceuticals, Inc. Prodrug salts of 2, 4- pyrimidinediamine compounds and their uses
DK2091918T3 (en) * 2006-12-08 2014-12-01 Irm Llc Compounds and Compositions as Protein Kinase Inhibitors
CN101563327A (en) * 2006-12-19 2009-10-21 健泰科生物技术公司 Pyrimidine kinase inhibitors
EP1939185A1 (en) 2006-12-20 2008-07-02 Bayer Schering Pharma Aktiengesellschaft New types of hetaryl-phenylendiamin-pyrimidines as protein kinase inhibitors for the treatment of cancer
CA2674178C (en) 2006-12-29 2015-11-10 Tibotec Pharmaceuticals Ltd. Hiv inhibiting 6-substituted pyrimidines
JP5283633B2 (en) 2006-12-29 2013-09-04 テイボテク・フアーマシユーチカルズ HIV inhibitory 5,6-substituted pyrimidines
TW200902010A (en) * 2007-01-26 2009-01-16 Smithkline Beecham Corp Anthranilamide inhibitors of aurora kinase
ES2702362T3 (en) 2007-01-31 2019-02-28 Ym Biosciences Australia Pty Compounds based on thiopyrimidine and uses thereof
DE102007010801A1 (en) 2007-03-02 2008-09-04 Bayer Cropscience Ag Use of new and known 2,4-diaminopyrimidine derivatives as fungicides, especially for controlling phytopathogenic fungi
AU2008229147A1 (en) 2007-03-20 2008-09-25 Smithkline Beecham Corporation Chemical compounds
KR20090121399A (en) 2007-03-20 2009-11-25 스미스클라인 비참 코포레이션 Chemical compounds
WO2008118822A1 (en) 2007-03-23 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US7834024B2 (en) * 2007-03-26 2010-11-16 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
US20120101113A1 (en) 2007-03-28 2012-04-26 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
US20120065201A1 (en) 2007-03-28 2012-03-15 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
TWI433677B (en) * 2007-06-04 2014-04-11 Avila Therapeutics Inc Heterocyclic compounds and uses thereof
AU2008275918B2 (en) * 2007-07-17 2014-01-30 Rigel Pharmaceuticals, Inc. Cyclic amine substituted pyrimidinediamines as PKC inhibitors
WO2009017838A2 (en) * 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
US20090088371A1 (en) 2007-08-28 2009-04-02 Rigel Pharmaceuticals, Inc. Combination therapy with syk kinase inhibitor
MX2010002336A (en) 2007-08-28 2010-03-25 Irm Llc Compounds and compositions as kinase inhibitors.
WO2009032703A1 (en) 2007-08-28 2009-03-12 Irm Llc 2- (het) arylamino-6-aminopyridine derivatives and fused forms thereof as anaplastic lymphoma kinase inhibitors
US7989465B2 (en) * 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
WO2009051822A1 (en) * 2007-10-19 2009-04-23 Avila Therapeutics, Inc. Heteroaryl compounds and uses thereof
WO2009080638A2 (en) 2007-12-20 2009-07-02 Cellzome Limited Sulfamides as zap-70 inhibitors
CN102014917A (en) 2008-02-22 2011-04-13 里格尔药品股份有限公司 Use of 2,4-pyrimidinediamines for the treatment of atherosclerosis
WO2009112490A1 (en) 2008-03-11 2009-09-17 Cellzome Limited Sulfonamides as zap-70 inhibitors
US8205348B2 (en) * 2008-03-19 2012-06-26 Zashiki-Warashi Manufacturing Inc. Tile spacer and holder therefor
CL2009000600A1 (en) 2008-03-20 2010-05-07 Bayer Cropscience Ag Use of diaminopyrimidine compounds as phytosanitary agents; diaminopyrimidine compounds; its preparation procedure; agent that contains them; procedure for the preparation of said agent; and method for combating pests of animals and / or harmful plant pathogenic fungi.
DE102008018910A1 (en) * 2008-04-14 2009-12-31 Basf Coatings Ag Process for the preparation of color pigments containing effect pigments
WO2009127642A2 (en) 2008-04-15 2009-10-22 Cellzome Limited Use of lrrk2 inhibitors for neurodegenerative diseases
CA2728893C (en) * 2008-04-16 2017-03-14 Portola Pharmaceuticals, Inc. Inhibitors of syk protein kinase
PT2321283T (en) 2008-04-16 2016-10-19 Portola Pharm Inc 2,6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinases inhibitors
US8138339B2 (en) * 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
EP2274288A2 (en) 2008-04-24 2011-01-19 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
EA029131B1 (en) 2008-05-21 2018-02-28 Ариад Фармасьютикалз, Инк. Phosphorous derivatives as kinase inhibitors
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
KR20110025224A (en) 2008-06-27 2011-03-09 아빌라 테라퓨틱스, 인크. Heteroaryl compounds and uses thereof
MX2011000661A (en) 2008-07-16 2011-05-25 Pharmacyclics Inc Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors.
JP2012501980A (en) 2008-09-03 2012-01-26 バイエル・クロップサイエンス・アーゲー Alkoxy-substituted and alkylthio-substituted anilinopyrimidines
WO2010077740A2 (en) 2008-12-09 2010-07-08 Cytokine Pharmasciences, Inc. Novel antiviral compounds, compositions, and methods of use
EP2387586B1 (en) 2009-01-15 2014-12-17 F. Hoffmann-La Roche AG Antibodies against human epo receptor
ES2423804T3 (en) 2009-04-03 2013-09-24 Cellzome Gmbh Methods for the identification of molecules that interact with kinases and for the purification of kinase proteins
JP5918693B2 (en) * 2009-05-05 2016-05-18 ダナ ファーバー キャンサー インスティテュート インコーポレイテッド EGFR inhibitor and disease treatment method
TWI484961B (en) 2009-05-08 2015-05-21 Astellas Pharma Inc Diamine heterocyclic methyl ester compounds
EP2443095A1 (en) 2009-06-18 2012-04-25 Cellzome Limited Sulfonamides and sulfamides as zap-70 inhibitors
US7741330B1 (en) 2009-10-12 2010-06-22 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of Bruton's tyrosine kinase
WO2011079231A1 (en) 2009-12-23 2011-06-30 Gatekeeper Pharmaceutical, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
US20130137709A1 (en) 2010-05-05 2013-05-30 Nathanael S. Gray Compounds that modulate EGFR activity and methods for treating or preventing conditions therewith
MY191929A (en) 2010-06-03 2022-07-18 Pharmacyclics Llc The use of inhibitors of bruton's tyrosine kinase (btk)
US20120071497A1 (en) 2010-06-03 2012-03-22 Pharmacyclics, Inc. Methods of treating abc-dlbcl using inhibitors of bruton's tyrosine kinase
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
JP6068340B2 (en) 2010-08-10 2017-01-25 セルジーン アヴィロミクス リサーチ, インコーポレイテッド Besylate of BTK inhibitor
US9238629B2 (en) 2010-11-01 2016-01-19 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
US20130317029A1 (en) 2010-11-01 2013-11-28 Portola Pharmaceuticals, Inc. Oxypyrimidines as syk modulators
ES2776002T3 (en) 2010-11-01 2020-07-28 Celgene Car Llc Heterocyclic compounds and their uses
EP2637502B1 (en) 2010-11-10 2018-01-10 Celgene CAR LLC Mutant-selective egfr inhibitors and uses thereof
CN102558149A (en) 2010-12-29 2012-07-11 中国医学科学院药物研究所 Pyrimidine derivative, preparation method thereof, medicinal composition and application thereof
US9834518B2 (en) 2011-05-04 2017-12-05 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in EGFR-driven cancers
KR102052670B1 (en) 2011-05-17 2019-12-06 더 리젠츠 오브 더 유니버시티 오브 캘리포니아 Kinase inhibitors
EA201892766A1 (en) 2011-10-19 2019-08-30 Фармасайкликс Элэлси USE OF BRUTON TYROSINKINASE INHIBITORS (Btk)
CN103159742B (en) 2011-12-16 2015-08-12 北京韩美药品有限公司 5-chloropyrimide compounds and the application as EGFR tyrosine kinase inhibitor thereof
CA2866852C (en) 2012-03-15 2020-12-29 Celgene Avilomics Research, Inc. Solid forms of an epidermal growth factor receptor kinase inhibitor
KR20150080592A (en) 2012-11-02 2015-07-09 파마시클릭스, 인코포레이티드 Tec family kinase inhibitor adjuvant therapy
JP6800750B2 (en) 2013-08-02 2020-12-16 ファーマサイクリックス エルエルシー Treatment method for solid tumors

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8354420B2 (en) 2010-06-04 2013-01-15 Genentech, Inc. Aminopyrimidine derivatives as LRRK2 inhibitors
US8815882B2 (en) 2010-11-10 2014-08-26 Genentech, Inc. Pyrazole aminopyrimidine derivatives as LRRK2 modulators
US9580432B2 (en) 2013-08-12 2017-02-28 Taiho Pharmaceutical Co., Ltd. Fused pyrimidine compound or salt thereof

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