CN102459253B - 作为pi3-激酶抑制剂的*唑取代的吲唑化合物 - Google Patents

作为pi3-激酶抑制剂的*唑取代的吲唑化合物 Download PDF

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CN102459253B
CN102459253B CN201080030329.2A CN201080030329A CN102459253B CN 102459253 B CN102459253 B CN 102459253B CN 201080030329 A CN201080030329 A CN 201080030329A CN 102459253 B CN102459253 B CN 102459253B
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base
methyl
compound
indazole
azoles
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CN102459253A (zh
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J·N·汉布林
P·S·琼斯
S·E·基林
J·勒
C·J·米切尔
N·J·帕
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Glaxo Group Ltd
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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CN201080030329.2A 2009-04-30 2010-04-28 作为pi3-激酶抑制剂的*唑取代的吲唑化合物 Active CN102459253B (zh)

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Application Number Priority Date Filing Date Title
US17403309P 2009-04-30 2009-04-30
US61/174033 2009-04-30
US61/174,033 2009-04-30
PCT/EP2010/055666 WO2010125082A1 (en) 2009-04-30 2010-04-28 Oxazole substituted indazoles as pi3-kinase inhibitors

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CN102459253A CN102459253A (zh) 2012-05-16
CN102459253B true CN102459253B (zh) 2015-03-25

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107660204A (zh) * 2015-06-02 2018-02-02 葛兰素史克知识产权开发有限公司 制备吲唑衍生物的方法

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8658635B2 (en) * 2008-06-05 2014-02-25 Glaxosmithkline Intellectual Property Development Limited Benzpyrazol derivatives as inhibitors of PI3 kinases
ES2526966T3 (es) 2008-06-05 2015-01-19 Glaxo Group Limited Compuestos novedosos
EP2280959B1 (en) 2008-06-05 2012-04-04 Glaxo Group Limited 4-amino-indazoles
ES2542551T3 (es) 2009-03-09 2015-08-06 Glaxo Group Limited 4-Oxadiazol-2-il-indazoles como inhibidores de PI3 cinasas
ES2876933T3 (es) 2009-04-30 2021-11-15 Glaxo Group Ltd Indazoles sustituidos con oxazol como inhibidores de PI3-cinasas
CN102372675B (zh) * 2010-08-14 2013-12-18 王娜 6-氯-4-碘吲唑及其制备方法与应用
US9326987B2 (en) 2010-09-08 2016-05-03 Glaxo Group Limited Indazole derivatives for use in the treatment of influenza virus infection
US9102668B2 (en) 2010-09-08 2015-08-11 Glaxo Group Limited Polymorphs and salts
PT2614058E (pt) 2010-09-08 2015-10-27 Glaxosmithkline Ip Dev Ltd Polimorfos e sais de n-[5-[4-(5-{[(2r,6s)-2,6-dimetil-4- morfolinil]metil}-1,3-oxazol-2-il)-1h-indazol-6-il]-2- (metiloxi)-3-piridinil]metanossulfonamida
GB201018124D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts
CA2816753A1 (en) * 2010-11-08 2012-05-18 Lycera Corporation N- sulfonylated tetrahydroquinolines and related bicyclic compounds inhibition of rory activity and the treatment of diseases
CN103998042B (zh) 2011-12-15 2016-12-28 诺华股份有限公司 Pi3k的活性或功能的抑制剂的应用
CA2872014A1 (en) 2012-05-08 2013-11-14 Lycera Corporation Tetrahydro[1,8]naphthyridine sulfonamide and related compounds for use as agonists of ror.gamma. and the treatment of disease
KR20150007300A (ko) 2012-05-08 2015-01-20 머크 샤프 앤드 돔 코포레이션 Ror감마 활성의 억제를 위한 테트라히드로나프티리딘 및 관련 비시클릭 화합물 및 질환의 치료
BR112015001096A2 (pt) 2012-07-16 2017-06-27 Neuropore Therapies Inc derivados de di e tri-heteroaril como inibidores de agregação de proteína
EP2914260A1 (en) 2012-10-31 2015-09-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for preventing antiphospholipid syndrome (aps)
WO2014098232A1 (ja) * 2012-12-21 2014-06-26 Yamashita Chikamasa Ｐｉ３キナーゼ阻害剤を含む医薬組成物、ビタミンｄ受容体に作用する化合物を含む医薬組成物、凍結乾燥組成物、凍結乾燥組成物の製造方法、及び経肺投与用医薬組成物
WO2015055690A1 (en) 2013-10-17 2015-04-23 Glaxosmithkline Intellectual Property Development Limited Pi3k inhibitor for treatment of respiratory disease
JP6475707B2 (ja) * 2013-10-17 2019-02-27 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ 呼吸器疾患の治療のためのｐｉ３ｋ阻害剤
WO2015095795A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. TETRAHYDRONAPHTHYRIDINE, BENZOXAZINE, AZA-BENZOXAZINE, AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE
WO2015095788A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. 2-ACYLAMIDOMETHYL AND SULFONYLAMIDOMETHYL BENZOXAZINE CARBAMATES FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE
WO2015095792A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Carbamate benzoxaxine propionic acids and acid derivatives for modulation of rorgamma activity and the treatment of disease
MX2016009581A (es) * 2014-01-24 2017-04-27 Abbvie Inc Derivados de 6-fenil- o 6-(piridin-3-il) indazol y metodos de uso.
EP3110429A4 (en) 2014-02-27 2018-02-21 Lycera Corporation Adoptive cellular therapy using an agonist of retinoic acid receptor-related orphan receptor gamma & related therapeutic methods
US11806266B2 (en) 2014-03-19 2023-11-07 Purewick Corporation Apparatus and methods for receiving discharged urine
WO2015171610A2 (en) 2014-05-05 2015-11-12 Lycera Corporation Tetrahydroquinoline sulfonamide and related compounds for use as agonists of rory and the treatment of disease
EP3209641A4 (en) 2014-05-05 2018-06-06 Lycera Corporation Benzenesulfonamido and related compounds for use as agonists of ror and the treatement of disease
US9127069B1 (en) * 2014-06-11 2015-09-08 Antecip Bioventures LLC Compositions comprising rank/rankl antagonists and related compounds for treating pain
CN104086538B (zh) * 2014-06-13 2016-07-06 南京药石科技股份有限公司 一种pi3k激酶抑制剂的中间体及其制备方法与应用
WO2016059220A1 (en) 2014-10-16 2016-04-21 INSERM (Institut National de la Santé et de la Recherche Médicale) Tcr-activating agents for use in the treatment of t-all
US10221142B2 (en) 2015-02-11 2019-03-05 Merck Sharp & Dohme Corp. Substituted pyrazole compounds as RORgammaT inhibitors and uses thereof
JP2018515491A (ja) 2015-05-05 2018-06-14 リセラ・コーポレイションＬｙｃｅｒａ Ｃｏｒｐｏｒａｔｉｏｎ ＲＯＲγの作動薬及び疾患の療法として使用するジヒドロ−２Ｈ−ベンゾ［ｂ］［１，４］オキサジンスルホンアミド及び関連化合物
CN107980042B (zh) 2015-06-11 2021-10-08 莱斯拉公司 用作RORγ激动剂和用于治疗疾病的芳基二氢-2H-苯并[b][1,4]噁嗪磺酰胺和相关化合物
CA3002853A1 (en) 2015-10-27 2017-05-04 Merck Sharp & Dohme Corp. Heteroaryl substituted benzoic acids as rorgammat inhibitors and uses thereof
EP3368516B1 (en) 2015-10-27 2020-07-15 Merck Sharp & Dohme Corp. SUBSTITUTED BICYCLIC PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
WO2017075182A1 (en) 2015-10-27 2017-05-04 Merck Sharp & Dohme Corp. Substituted indazole compounds as rorgammat inhibitors and uses thereof
RU2737157C2 (ru) * 2016-01-14 2020-11-25 Хандок Инк. Соединения, являющиеся антагонистами а3-аденозинового рецептора, способ их получения и их медицинское применение
JP2019524792A (ja) * 2016-08-08 2019-09-05 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ 化合物
CA3098570C (en) 2018-05-01 2023-09-26 Purewick Corporation Fluid collection devices, related systems, and related methods
US11801186B2 (en) 2020-09-10 2023-10-31 Purewick Corporation Urine storage container handle and lid accessories
KR20230093251A (ko) 2020-09-10 2023-06-27 프리시릭스 엔.브이. Fap에 대한 항체 단편
JP2023515438A (ja) 2021-01-19 2023-04-13 ピュアウィック コーポレイション 可変流体収集デバイス、システム、及び方法
EP4274524A1 (en) 2021-02-26 2023-11-15 Purewick Corporation Fluid collection devices having a sump between a tube opening and a barrier, and related systems and methods
WO2023147603A2 (en) * 2022-01-31 2023-08-03 Intra-Cellular Therapies, Inc. Salt crystals
WO2023203135A1 (en) 2022-04-22 2023-10-26 Precirix N.V. Improved radiolabelled antibody
WO2023213801A1 (en) 2022-05-02 2023-11-09 Precirix N.V. Pre-targeting

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1688582A (zh) * 2002-09-30 2005-10-26 拜尔药品公司 稠合吡咯－嘧啶衍生物
CN1816549A (zh) * 2003-05-02 2006-08-09 诺瓦提斯公司 磷脂酰肌醇3－激酶抑制剂
CN1838953A (zh) * 2003-08-28 2006-09-27 诺瓦提斯公司 用于治疗炎性气道疾病的磷脂酰肌醇3－激酶(pi3)抑制剂5－苯基－4－甲基－噻唑－2－基－胺衍生物
US20080032960A1 (en) * 2006-04-04 2008-02-07 Regents Of The University Of California PI3 kinase antagonists

Family Cites Families (148)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9127376D0 (en) 1991-12-24 1992-02-19 Wellcome Found Amidino derivatives
CA2133439C (en) 1992-04-02 2005-07-26 Siegfried Benjamin Christensen, Iv Compounds useful for treating allergic and inflammatory diseases
DK0957087T3 (da) 1994-06-15 2003-03-24 Wellcome Found Intermediater, der er anvendelige til fremstilling af enzym-inhibitorer
WO1996032099A1 (en) 1995-04-14 1996-10-17 Glaxo Wellcome Inc. Metered dose inhaler for albuterol
US5821243A (en) 1996-07-22 1998-10-13 Viropharma Incorporated Compounds compositions and methods for treating influenza
MY117948A (en) 1997-01-13 2004-08-30 Glaxo Group Ltd Nitride oxide synthase inhibitors.
DE19723722A1 (de) 1997-05-30 1998-12-10 Schering Ag Nichtsteroidale Gestagene
TW533865U (en) 1997-06-10 2003-05-21 Glaxo Group Ltd Dispenser for dispensing medicament and actuation indicating device
AU9281298A (en) 1997-10-01 1999-04-23 Kyowa Hakko Kogyo Co. Ltd. Benzodioxole derivatives
US6506766B1 (en) 1998-02-13 2003-01-14 Abbott Laboratories Glucocortiocoid-selective antinflammatory agents
PT1070056E (pt) 1998-03-14 2004-11-30 Altana Pharma Ag Inibidores de pde iii/iv a base de ftalazinona
GB9811599D0 (en) 1998-05-30 1998-07-29 Glaxo Group Ltd Nitric oxide synthase inhibitors
US6390291B1 (en) 1998-12-18 2002-05-21 Smithkline Beecham Corporation Method and package for storing a pressurized container containing a drug
US6119853A (en) 1998-12-18 2000-09-19 Glaxo Wellcome Inc. Method and package for storing a pressurized container containing a drug
US6315112B1 (en) 1998-12-18 2001-11-13 Smithkline Beecham Corporation Method and package for storing a pressurized container containing a drug
US6352152B1 (en) 1998-12-18 2002-03-05 Smithkline Beecham Corporation Method and package for storing a pressurized container containing a drug
AU4501800A (en) 1999-05-04 2000-11-17 American Home Products Corporation Tetracyclic progesterone receptor modulator compounds and methods
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
CO5180649A1 (es) 1999-09-01 2002-07-30 Abbott Lab Antagonistas de los receptores de los glucocorticoides para el tratamiento de la diabetes para el tratamiento de la diabetes
OA11558A (en) 1999-12-08 2004-06-03 Advanced Medicine Inc Beta 2-adrenergic receptor agonists.
CN1294142C (zh) 2000-08-05 2007-01-10 葛兰素集团有限公司 作为抗炎剂的17β－硫代羧酸酯17α－芳基羰氧基雄甾烷衍生物
US7101882B2 (en) 2000-09-29 2006-09-05 Glaxo Group Limited Morpholin-acetamide derivatives for the treatment of inflammatory diseases
GB0031179D0 (en) 2000-12-21 2001-01-31 Glaxo Group Ltd Nitric oxide synthase inhibitors
US6484903B2 (en) 2001-01-09 2002-11-26 Riverwood International Corporation Carton with an improved dispensing feature in combination with a unique handle
GB0103630D0 (en) 2001-02-14 2001-03-28 Glaxo Group Ltd Chemical compounds
WO2002067683A1 (en) 2001-02-26 2002-09-06 Merck & Co., Inc. Hiv protease inhibitors supported on cation exchange resins for oral administration
WO2002070490A1 (en) 2001-03-08 2002-09-12 Glaxo Group Limited Agonists of beta-adrenoceptors
EP1370521B1 (en) 2001-03-22 2007-12-19 Glaxo Group Limited Formanilide derivatives as beta2-adrenoreceptor agonists
KR100863659B1 (ko) 2001-04-16 2008-10-15 미쓰비시 타나베 파마 코퍼레이션 질소-함유 헤테로시클릭 화합물 및 이를 포함하는 제약 조성물
PL366937A1 (en) 2001-04-30 2005-02-07 Glaxo Group Limited Anti-inflammatory 17.beta.-carbothioate ester derivatives of androstane with a cyclic ester group in position 17.alpha
EP1395604B1 (en) 2001-06-12 2008-06-25 Glaxo Group Limited Novel anti inflammatory 17.alpha.-heterocyclic-esters of 17.beta.-carbothioate androstane derivatives
EP1407770B1 (en) 2001-06-26 2013-06-05 Takeda Pharmaceutical Company Limited Tgf-beta superfamily production/secretion promoter
KR100912324B1 (ko) 2001-09-14 2009-08-14 글락소 그룹 리미티드 호흡기 질환 치료용 펜에탄올아민 유도체
WO2003042160A1 (en) 2001-11-13 2003-05-22 Theravance, Inc. Aryl aniline beta-2 adrenergic receptor agonists
AU2002353186A1 (en) 2001-12-19 2003-06-30 Smithkline Beecham P.L.C. (1-h-indazol-3-yl) -amide derivatives as gsk-3 inhibitors
DE60309829T2 (de) 2002-01-14 2007-09-13 Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield Glucocorticoidmimetika, verfahren zu ihrer herstellung, diese enthaltende pharmazeutische formulierungen und ihre verwendungen
EP1467730A4 (en) 2002-01-22 2010-03-10 Univ California Non-steroid ligands for the glucocorticoid receptor, compositions and uses thereof
TW200306819A (en) 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
GB0204719D0 (en) 2002-02-28 2002-04-17 Glaxo Group Ltd Medicinal compounds
FR2836915B1 (fr) 2002-03-11 2008-01-11 Aventis Pharma Sa Derives d'aminoindazoles, procede de preparation et intermediaires de ce procede a titre de medicaments et compositions pharmaceutiques les renfermant
US7268152B2 (en) 2002-03-26 2007-09-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
WO2003082280A1 (en) 2002-03-26 2003-10-09 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE10215316C1 (de) 2002-04-02 2003-12-18 Schering Ag Chinolin- und Isochinolin-Derivate, ein pharmazeutisches Mittel und ihre Verwendung als Entzündungshemmer
EP1496892B1 (en) 2002-04-11 2011-01-26 Merck Sharp & Dohme Corp. 1h-benzo(f)indazol-5-yl derivatives as selective glucocorticoid receptor modulators
ES2298511T3 (es) 2002-04-25 2008-05-16 Glaxo Group Limited Derivados de fenetanolamina.
US7186864B2 (en) 2002-05-29 2007-03-06 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
US7074806B2 (en) 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
EP1519723A1 (en) 2002-06-27 2005-04-06 Novo Nordisk A/S Novel glucagon antagonists/inverse agonists
EP1521733B1 (en) 2002-07-08 2014-08-20 Pfizer Products Inc. Modulators of the glucocorticoid receptor
AU2003251970A1 (en) 2002-07-18 2004-02-09 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor and method
GB0217225D0 (en) 2002-07-25 2002-09-04 Glaxo Group Ltd Medicinal compounds
CA2495120A1 (en) 2002-08-09 2004-02-19 Astrazeneca Ab Oxadiazoles as modulators of metabotropic glutamate receptor-5
WO2004014902A2 (en) 2002-08-09 2004-02-19 Astrazeneca Ab Compounds having an activity at metabotropic glutamate receptors
MXPA05001594A (es) 2002-08-09 2005-09-20 Astrazeneca Ab 1,2,4" oxadiazoles como moduladores de receptor-5 metabotropico de glutamato.
US20040224986A1 (en) 2002-08-16 2004-11-11 Bart De Corte Piperidinyl targeting compounds that selectively bind integrins
AU2003259747A1 (en) 2002-08-21 2004-03-11 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted hihydroquinolines as glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
GB0220730D0 (en) 2002-09-06 2002-10-16 Glaxo Group Ltd Medicinal compounds
GB0230045D0 (en) 2002-12-23 2003-01-29 Glaxo Group Ltd Compounds
ES2331119T3 (es) 2002-09-16 2009-12-22 Glaxo Group Limited Compuestos de pirazolo(3,4-b)piridina, y su uso como inhibidores de fosfodiesterasa.
WO2004026248A2 (en) 2002-09-20 2004-04-01 Merck & Co., Inc. Octahydro-2-h-naphtho[1,2-f] indole-4-carboxamide derivatives as selective glucocorticoid receptor modulators
GB0224084D0 (en) 2002-10-16 2002-11-27 Glaxo Group Ltd Novel compounds
DE60315492T2 (de) 2002-10-22 2008-04-24 Glaxo Group Ltd., Greenford Medizinisch verwendbare arylethanolamin verbindungen
EP1556342B1 (en) 2002-10-28 2008-03-26 Glaxo Group Limited Phenethanolamine derivative for the treatment of respiratory diseases
GB0225030D0 (en) 2002-10-28 2002-12-04 Glaxo Group Ltd Medicinal compounds
GB0225540D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
GB0225535D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
US7202257B2 (en) 2003-12-24 2007-04-10 Deciphera Pharmaceuticals, Llc Anti-inflammatory medicaments
TWI328009B (en) 2003-05-21 2010-08-01 Glaxo Group Ltd Quinoline derivatives as phosphodiesterase inhibitors
JP2007500249A (ja) 2003-06-13 2007-01-11 ツェンタリス ゲゼルシャフト ミット ベシュレンクテル ハフツング ホスファチジルイノシトール３−キナーゼ阻害活性を有する化合物及びその使用方法
GB0316290D0 (en) 2003-07-11 2003-08-13 Glaxo Group Ltd Novel compounds
US20050090529A1 (en) 2003-07-31 2005-04-28 Pfizer Inc 3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
AP2007004238A0 (en) 2003-10-14 2007-12-31 Glaxo Group Ltd Muscarinic acetycholine receptor antagonists
TWI344961B (en) * 2003-10-15 2011-07-11 Ube Industries Novel indazole derivative
WO2005044354A1 (en) 2003-11-03 2005-05-19 Glaxo Group Limited A fluid dispensing device
PE20050489A1 (es) 2003-11-04 2005-09-02 Glaxo Group Ltd Antagonistas de receptores de acetilcolina muscarinicos
AU2004299277A1 (en) 2003-12-19 2005-06-30 Glaxo Group Limited Pyrazolo (3,4-b) pyridine compounds, and their use as phosphodiesterase inhibitors
WO2005077368A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
WO2005077373A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
WO2005077345A1 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Compounds for the treatment of gastro-esophageal reflux disease
BRPI0506881A (pt) 2004-02-04 2007-06-26 Neurosearch As derivado de arila diazabicìclica, composição farmacêutica, uso de um derivado de arila diazabicìclica, e, método de tratamento, prevenção ou alìvio de uma doença ou distúrbio ou condição de um corpo de animal vivo
GB0405937D0 (en) 2004-03-16 2004-04-21 Glaxo Group Ltd Compounds
GB0405933D0 (en) 2004-03-16 2004-04-21 Glaxo Group Ltd Compounds
CA2559629A1 (en) 2004-03-16 2005-09-29 Glaxo Group Limited Pyrazolo[3,4-b]pyridine compound, and its use as a pde4 inhibitor
MY144753A (en) 2004-04-27 2011-10-31 Glaxo Group Ltd Muscarinic acetylcholine receptor antagonists
JP2008504275A (ja) 2004-06-24 2008-02-14 インサイト・コーポレイション Ｎ−置換ピペリジンおよびその医薬としての使用
WO2006000401A1 (en) 2004-06-28 2006-01-05 Glaxo Group Limited Substituted oxazines as glucocorticoid receptor modulators
WO2006000398A1 (en) 2004-06-28 2006-01-05 Glaxo Group Limited 2,3-benzoxazin derivatives as non-steroidal glucocorticoid receptor modulators
US20060013540A1 (en) * 2004-07-19 2006-01-19 Chao Zhang Single fiber optical transceiver module
WO2006135383A2 (en) 2004-08-04 2006-12-21 Myriad Genetics, Inc. Indazoles
GB0418045D0 (en) 2004-08-12 2004-09-15 Glaxo Group Ltd Compounds
CN101044135B (zh) 2004-10-19 2011-11-23 霍夫曼-拉罗奇有限公司 喹啉衍生物
BRPI0518281A2 (pt) 2004-11-18 2008-11-18 Incyte Corp inibidores de 11-beta hidroxilesteràide desidrogenase do tipo i e mÉtodos uso dos mesmos
EP1833787A2 (en) 2004-11-30 2007-09-19 Plexxikon, Inc. Indole derivatives for use as ppar active compounds
JP5281291B2 (ja) 2005-01-10 2013-09-04 グラクソ グループ リミテッド 新規化合物
US20090124588A1 (en) 2005-01-10 2009-05-14 Glaxo Group Limited Androstane 17-Alpha-Carbonate for Use in the Treatment of Inflammatory and Allergic Conditions
US7728009B1 (en) 2005-02-18 2010-06-01 Neurogen Corporation Thiazole amides, imidazole amides and related analogues
WO2007017759A2 (en) 2005-03-31 2007-02-15 Ronen Kahana Creating poultry and other animals resistant to viral disease
US20060264433A1 (en) 2005-05-23 2006-11-23 Backes Bradley J Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
TW200800946A (en) 2005-08-15 2008-01-01 Astrazeneca Ab Substituted piperazines as metabotropic glutamate receptor antagonists
JP2009504769A (ja) 2005-08-16 2009-02-05 ジェンザイム・コーポレーション ケモカイン受容体結合化合物
US8003642B2 (en) 2006-03-10 2011-08-23 Ono Pharmaceutical Co., Ltd. Nitrogenated heterocyclic derivative, and pharmaceutical agent comprising the derivative as active ingredient
BRPI0709699A2 (pt) 2006-03-29 2011-07-26 Foldrx Pharmaceuticals Inc inibiÇço da toxidez da alfa-sinucleina
JP5255559B2 (ja) 2006-03-31 2013-08-07 アボット・ラボラトリーズ インダゾール化合物
GB0608820D0 (en) 2006-05-04 2006-06-14 Piramed Ltd Pharmaceutical compounds
WO2008016123A1 (fr) 2006-08-03 2008-02-07 Takeda Pharmaceutical Company Limited INHIBITEUR DE LA GSK-3β
WO2008020229A2 (en) 2006-08-17 2008-02-21 Astrazeneca Ab Antibacterial pyrrolecarboxamides
MX2009002018A (es) 2006-08-25 2009-03-05 Abbott Lab Derivados de indazol que inhiben vanilloide-1 potencial de receptor pasajero (trpv1) y usos de los mismos.
US7948877B2 (en) * 2006-09-07 2011-05-24 Via Technologies, Inc. Systems and methods for packet forward control
JP2010504369A (ja) 2006-09-25 2010-02-12 ミュタビリス エス アー 細菌ヘプトース合成の新規化学阻害剤、それらの調製方法および前記阻害剤の生物学的適用
EP2081933B1 (en) 2006-09-29 2011-03-23 Novartis AG Pyrazolopyrimidines as pi3k lipid kinase inhibitors
TWI454262B (zh) 2006-11-02 2014-10-01 Targacept Inc 菸鹼乙醯膽鹼受體亞型選擇性之二氮雜雙環烷類醯胺
GB0701426D0 (en) 2007-01-25 2007-03-07 Univ Sheffield Compounds and their use
US8450348B2 (en) 2007-02-21 2013-05-28 Forma Tm, Llc Derivatives of squaric acid with anti-proliferative activity
JP2010116389A (ja) 2008-10-17 2010-05-27 Bayer Cropscience Ag 殺虫性アリールピロリジン類
GB0709031D0 (en) 2007-05-10 2007-06-20 Sareum Ltd Pharmaceutical compounds
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
CA2691888A1 (en) 2007-06-25 2008-12-31 Boehringer Ingelheim International Gmbh New chemical compounds
EP2183228B1 (en) 2007-07-26 2014-08-20 Vitae Pharmaceuticals, Inc. CYCLIC INHIBITORS OF 11ß -HYDROXYSTERIOD DEHYDROGENASE 1
CA2704711C (en) 2007-09-24 2016-07-05 Genentech, Inc. Thiazolopyrimidine p13k inhibitor compounds and methods of use
JP2009127226A (ja) * 2007-11-21 2009-06-11 Seiji Ohara 温水プールに雪を落し込む手段を持つ融雪装置
AU2009241727B2 (en) 2008-05-01 2013-05-02 Vitae Pharmaceuticals, Inc Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CA2723032A1 (en) 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
WO2009134392A1 (en) 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CA2723034A1 (en) 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
US8658635B2 (en) 2008-06-05 2014-02-25 Glaxosmithkline Intellectual Property Development Limited Benzpyrazol derivatives as inhibitors of PI3 kinases
JP5502858B2 (ja) 2008-06-05 2014-05-28 グラクソ グループ リミテッド Ｐｉ３キナーゼの阻害剤として有用な４−カルボキサミドインダゾール誘導体
EP2280959B1 (en) 2008-06-05 2012-04-04 Glaxo Group Limited 4-amino-indazoles
ES2526966T3 (es) 2008-06-05 2015-01-19 Glaxo Group Limited Compuestos novedosos
KR101665727B1 (ko) 2008-06-11 2016-10-12 하마마츠 포토닉스 가부시키가이샤 유리 용착 방법
WO2010011314A1 (en) 2008-07-25 2010-01-28 Boehringer Ingelheim International Gmbh Cyclic inhibitors of 11 beta-hydroxysteroid dehydrogenase 1
WO2010127237A2 (en) 2009-04-30 2010-11-04 Boehringer Ingelheim International Gmbh Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
US8245111B2 (en) * 2008-12-09 2012-08-14 Intel Corporation Performing multi-bit error correction on a cache line
WO2010068287A2 (en) 2008-12-11 2010-06-17 Angion Biomedica Corp. Small molecule modulators of hepatocyte growth factor (scatter factor) activity
US20120039905A1 (en) 2009-01-13 2012-02-16 The Babraham Institute The Role of p110 delta Signaling in Morbidity and Lung Pathology Induced by Influenza Virus Infection
ES2542551T3 (es) * 2009-03-09 2015-08-06 Glaxo Group Limited 4-Oxadiazol-2-il-indazoles como inhibidores de PI3 cinasas
EP2424838A1 (en) 2009-04-30 2012-03-07 Bayer CropScience AG Pesticidal arylpyrrolidines
MA33216B1 (fr) 2009-04-30 2012-04-02 Boehringer Ingelheim Int Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1
WO2010125134A1 (en) 2009-04-30 2010-11-04 Abbott Gmbh & Co. Kg N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds suitable for treating disorders that respond to modulation of the serotonin 5-ht6 receptor
ES2876933T3 (es) 2009-04-30 2021-11-15 Glaxo Group Ltd Indazoles sustituidos con oxazol como inhibidores de PI3-cinasas
US8343959B2 (en) 2009-04-30 2013-01-01 Abbott Gmbh & Co. Kg N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor
EP2507226A1 (en) 2009-12-03 2012-10-10 Glaxo Group Limited Novel compounds
JP2013512879A (ja) 2009-12-03 2013-04-18 グラクソ グループ リミテッド Ｐｉ３キナーゼの阻害剤としてのベンズピラゾール誘導体
EP2507231A1 (en) 2009-12-03 2012-10-10 Glaxo Group Limited Indazole derivatives as pi 3 - kinase inhibitors
PT2614058E (pt) 2010-09-08 2015-10-27 Glaxosmithkline Ip Dev Ltd Polimorfos e sais de n-[5-[4-(5-{[(2r,6s)-2,6-dimetil-4- morfolinil]metil}-1,3-oxazol-2-il)-1h-indazol-6-il]-2- (metiloxi)-3-piridinil]metanossulfonamida
US9102668B2 (en) 2010-09-08 2015-08-11 Glaxo Group Limited Polymorphs and salts
US9326987B2 (en) 2010-09-08 2016-05-03 Glaxo Group Limited Indazole derivatives for use in the treatment of influenza virus infection
GB201018124D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts
US10642898B1 (en) * 2017-04-11 2020-05-05 Northrop Grumman Systems Corporation Three-dimensional graph

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1688582A (zh) * 2002-09-30 2005-10-26 拜尔药品公司 稠合吡咯－嘧啶衍生物
CN1816549A (zh) * 2003-05-02 2006-08-09 诺瓦提斯公司 磷脂酰肌醇3－激酶抑制剂
CN1838953A (zh) * 2003-08-28 2006-09-27 诺瓦提斯公司 用于治疗炎性气道疾病的磷脂酰肌醇3－激酶(pi3)抑制剂5－苯基－4－甲基－噻唑－2－基－胺衍生物
US20080032960A1 (en) * 2006-04-04 2008-02-07 Regents Of The University Of California PI3 kinase antagonists

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
"Phosphatidylinositol 3-kinase (PI3K) inhibitors as anticancer drugs";Jeroen C. Verheijen，等;《Drugs of the Future》;20071231;第32卷(第6期);第537-547页 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107660204A (zh) * 2015-06-02 2018-02-02 葛兰素史克知识产权开发有限公司 制备吲唑衍生物的方法

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