CN102459253A - 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

Info

Publication number
CN102459253A
CN102459253A CN2010800303292A CN201080030329A CN102459253A CN 102459253 A CN102459253 A CN 102459253A CN 2010800303292 A CN2010800303292 A CN 2010800303292A CN 201080030329 A CN201080030329 A CN 201080030329A CN 102459253 A CN102459253 A CN 102459253A
Authority
CN
China
Prior art keywords
methyl
compound
azoles
indazole
disorder
Prior art date
Legal status (The legal status 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 status listed.)
Granted
Application number
CN2010800303292A
Other languages
English (en)
Chinese (zh)
Other versions
CN102459253B (zh
Inventor
J·N·汉布林
P·S·琼斯
S·E·基林
J·勒
C·J·米切尔
N·J·帕
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Glaxo Group Ltd
Original Assignee
Glaxo Group Ltd
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.)
Filing date
Publication date
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of CN102459253A publication Critical patent/CN102459253A/zh
Application granted granted Critical
Publication of CN102459253B publication Critical patent/CN102459253B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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)

Applications Claiming Priority (4)

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

Publications (2)

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

Family

ID=42225106

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201080030329.2A Active CN102459253B (zh) 2009-04-30 2010-04-28 作为pi3-激酶抑制剂的*唑取代的吲唑化合物

Country Status (40)

Country Link
US (14) US20120046286A1 (und)
EP (3) EP2424864B1 (und)
JP (1) JP5570589B2 (und)
KR (2) KR101679642B1 (und)
CN (1) CN102459253B (und)
AR (2) AR076435A1 (und)
AU (1) AU2010243613B2 (und)
BR (1) BRPI1016219B8 (und)
CA (1) CA2759476C (und)
CL (1) CL2011002706A1 (und)
CO (1) CO6390057A2 (und)
CR (1) CR20110603A (und)
CY (1) CY1119515T1 (und)
DK (2) DK2899191T3 (und)
DO (1) DOP2011000328A (und)
EA (1) EA021056B1 (und)
ES (3) ES2531274T3 (und)
HK (2) HK1165801A1 (und)
HR (2) HRP20150173T1 (und)
HU (1) HUE034724T2 (und)
IL (1) IL215803A (und)
JO (1) JO3025B1 (und)
LT (1) LT2899191T (und)
MA (1) MA33304B1 (und)
ME (2) ME02900B (und)
MX (1) MX2011011534A (und)
MY (1) MY160454A (und)
NZ (1) NZ596071A (und)
PE (1) PE20120321A1 (und)
PL (2) PL2899191T3 (und)
PT (2) PT2424864E (und)
RS (2) RS53830B1 (und)
SG (2) SG10201401881QA (und)
SI (2) SI2424864T1 (und)
SM (1) SMT201500043B (und)
TW (3) TWI516487B (und)
UA (1) UA101098C2 (und)
UY (1) UY32585A (und)
WO (1) WO2010125082A1 (und)
ZA (1) ZA201107878B (und)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103270037A (zh) * 2010-10-27 2013-08-28 葛兰素集团有限公司 作为pi3k抑制剂用于治疗例如呼吸系统病症的6-(1h-吲哚-4-基)-4-(5-{[4-(1-甲基乙基)-1-哌嗪基]甲基}-1,3-噁唑-2-基)-1h-吲唑的多晶形物和盐
CN104086538A (zh) * 2014-06-13 2014-10-08 南京药石药物研发有限公司 一种pi3k激酶抑制剂的中间体及其制备方法与应用
CN105611929A (zh) * 2013-10-17 2016-05-25 葛兰素史克知识产权开发有限公司 用于治疗呼吸系统疾病的pi3k抑制剂
CN105658218A (zh) * 2013-10-17 2016-06-08 葛兰素史克知识产权开发有限公司 用于治疗呼吸疾病的pi3k抑制剂

Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009147190A1 (en) 2008-06-05 2009-12-10 Glaxo Group Limited Novel compounds
EP2300437B1 (en) 2008-06-05 2013-11-20 Glaxo Group Limited Benzpyrazol derivatives as inhibitors of pi3 kinases
ES2526966T3 (es) 2008-06-05 2015-01-19 Glaxo Group Limited Compuestos novedosos
US8524751B2 (en) 2009-03-09 2013-09-03 GlaxoSmithKline Intellecutual Property Development 4-oxadiazol-2-YL-indazoles as inhibitors of P13 kinases
CA2759476C (en) 2009-04-30 2018-10-09 Julie Nicole Hamblin Novel compounds
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
JP5876051B2 (ja) * 2010-09-08 2016-03-02 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 インフルエンザウィルス感染の治療に使用するためのインダゾール誘導体
US9102668B2 (en) 2010-09-08 2015-08-11 Glaxo Group Limited Polymorphs and salts
DK2614058T3 (en) 2010-09-08 2015-09-28 Glaxosmithkline Ip Dev Ltd Polymorphs, and the salts of N- [5- [4- (5 - {[(2R, 6S) -2,6-dimethyl-4-morpholinyl] methyl} -1,3-oxazol-2-yl) -1H-indazole -6-yl] -2- (methyloxy) -3-pyridinyl] methanesulfonamide.
AU2011326071A1 (en) 2010-11-08 2013-05-23 Lycera Corporation N- sulfonylated tetrahydroquinolines and related bicyclic compounds inhibition of RORy activity and the treatment of diseases
KR102038462B1 (ko) 2011-12-15 2019-10-31 노파르티스 아게 Pi3k의 활성 또는 기능의 억제제의 용도
JP6242868B2 (ja) 2012-05-08 2017-12-06 リセラ・コーポレイションLycera Corporation RORγのアゴニストとしての使用のためおよび疾患の処置のためのテトラヒドロ[1,8]ナフチリジンスルホンアミドおよび関連化合物
RU2014149136A (ru) 2012-05-08 2016-07-10 Мерк Шарп И Доум Корп. ТЕТРАГИДРОНАФТИРИДИНОВЫЕ И РОДСТВЕННЫЕ БИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ ДЛЯ ИНГИБИРОВАНИЯ RORγ АКТИВНОСТИ И ЛЕЧЕНИЯ ЗАБОЛЕВАНИЯ
MX2015000618A (es) 2012-07-16 2015-04-10 Neuropore Therapies Inc Derivados de di- y tri-heteroarilo como inhibidores de la agregacion de proteinas.
WO2014068070A1 (en) 2012-10-31 2014-05-08 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
US9663502B2 (en) 2013-12-20 2017-05-30 Lycera Corporation 2-Acylamidomethyl and sulfonylamidomethyl benzoxazine carbamates for inhibition of RORgamma activity and the treatment of disease
US9783511B2 (en) 2013-12-20 2017-10-10 Lycera Corporation Carbamate benzoxazine propionic acids and acid derivatives for modulation of RORgamma activity and the treatment of disease
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
CA2937111A1 (en) * 2014-01-24 2015-07-30 Abbvie Inc. 6-phenyl- or 6-(pyridin-3-yl)indazole derivatives and methods of use
MX2016010998A (es) 2014-02-27 2017-03-31 Lycera Corp Terapia celular adoptiva que usa un agonista de receptor huérfano gamma relacionado con receptor de ácido retinoico y métodos terapéuticos relacionados.
US11806266B2 (en) 2014-03-19 2023-11-07 Purewick Corporation Apparatus and methods for receiving discharged urine
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
CA2947290A1 (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
US9127069B1 (en) * 2014-06-11 2015-09-08 Antecip Bioventures LLC Compositions comprising rank/rankl antagonists and related compounds for treating pain
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
WO2016179343A1 (en) 2015-05-05 2016-11-10 Lycera Corporation DIHYDRO-2H-BENZO[b][1,4]OXAZINE SULFONAMIDE AND RELATED COMPOUNDS FOR USE AS AGONISTS OF RORy AND THE TREATMENT OF DISEASE
GB201509492D0 (en) * 2015-06-02 2015-07-15 Glaxosmithkline Ip Dev Ltd Novel processes
US10611740B2 (en) 2015-06-11 2020-04-07 Lycera Corporation Aryl dihydro-2H-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of RORγ and the treatment of disease
US10344000B2 (en) 2015-10-27 2019-07-09 Merck Sharp & Dohme Corp. Substituted bicyclic pyrazole compounds as RORgammaT inhibitors and uses thereof
KR20180070697A (ko) 2015-10-27 2018-06-26 머크 샤프 앤드 돔 코포레이션 Ror감마t 저해제로서의 치환된 인다졸 화합물 및 이의 용도
US10584121B2 (en) 2015-10-27 2020-03-10 Merck Sharp & Dohme Corp. Heteroaryl substituted benzoic acids as RORgammaT inhibitors and uses thereof
EP3402798B1 (en) * 2016-01-14 2021-04-28 Handok Inc. Compounds antagonizing a3 adenosine receptor, method for preparing them, and medical-use thereof
EP3497100A1 (en) * 2016-08-08 2019-06-19 GlaxoSmithKline Intellectual Property Development Limited Chemical compounds
CN112367948A (zh) 2018-05-01 2021-02-12 普利维克公司 流体收集装置、相关系统和相关方法
US11801186B2 (en) 2020-09-10 2023-10-31 Purewick Corporation Urine storage container handle and lid accessories
CN116438200A (zh) 2020-09-10 2023-07-14 普雷西里克斯公司 针对fap的抗体片段
WO2022159392A1 (en) 2021-01-19 2022-07-28 Purewick Corporation Variable fit fluid collection devices, systems, and methods
WO2022182385A1 (en) 2021-02-26 2022-09-01 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
EP0633776B1 (en) 1992-04-02 2001-05-09 Smithkline Beecham Corporation Compounds useful for treating allergic and inflammatory diseases
ES2189322T3 (es) 1994-06-15 2003-07-01 Wellcome Found Intermediarios utiles en la preparacion de inhibidores de encimas.
ES2179192T3 (es) 1995-04-14 2003-01-16 Smithkline Beecham Corp Inhibidor dosificador para 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
SI1070056T1 (en) 1998-03-14 2004-12-31 Altana Pharma Ag Phthalazinone pde iii/iv inhibitors
GB9811599D0 (en) 1998-05-30 1998-07-29 Glaxo Group Ltd Nitric oxide synthase inhibitors
US6352152B1 (en) 1998-12-18 2002-03-05 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
US6390291B1 (en) 1998-12-18 2002-05-21 Smithkline Beecham Corporation Method and package for storing a pressurized container containing a drug
CN1353717A (zh) 1999-05-04 2002-06-12 莱加制药公司 四环黄体酮受体调节剂化合物及其方法
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.
AU2001276497B2 (en) 2000-08-05 2005-04-07 Glaxo Group Limited 17.beta.-carbothioate 17.alpha.-arylcarbonyloxyloxy androstane derivative as anti-inflammatory agents
NZ525056A (en) 2000-09-29 2004-11-26 Glaxo Group Ltd 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
DE60220887T2 (de) 2001-03-08 2008-02-28 Glaxo Group Ltd., Greenford Agonisten von beta-adrenorezeptoren
JP4143413B2 (ja) 2001-03-22 2008-09-03 グラクソ グループ リミテッド β2−アドレナリン受容体アゴニストとしてのホルムアニリド誘導体
KR100863659B1 (ko) 2001-04-16 2008-10-15 미쓰비시 타나베 파마 코퍼레이션 질소-함유 헤테로시클릭 화합물 및 이를 포함하는 제약 조성물
KR100831534B1 (ko) 2001-04-30 2008-05-22 글락소 그룹 리미티드 17.알파 위치에 시클릭 에스테르기를 지닌 항염증성의안드로스탄의 17.베타.-카르보티오에이트 에스테르 유도체
ATE399174T1 (de) 2001-06-12 2008-07-15 Glaxo Group Ltd Neue anti inflammatorische 17.alpha.- heterozyklische ester von 17.beta.-carbothioat androstan derivativen
US7498352B2 (en) 2001-06-26 2009-03-03 Takeda Pharmaceutical Company Limited TGF-β superfamily production/secretion promoter
US7361787B2 (en) 2001-09-14 2008-04-22 Glaxo Group Limited Phenethanolamine derivatives for treatment of respiratory diseases
US6653323B2 (en) 2001-11-13 2003-11-25 Theravance, Inc. Aryl aniline β2 adrenergic receptor agonists
WO2003051847A1 (en) 2001-12-19 2003-06-26 Smithkline Beecham P.L.C. (1-h-indazol-3-yl) -amide derivatives as gsk-3 inhibitors
WO2003059899A1 (en) 2002-01-14 2003-07-24 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical formulations containing them and uses thereof
AU2003214879B2 (en) 2002-01-22 2008-02-07 The Regents Of The University Of California Non-steroidal 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
PL373043A1 (en) 2002-03-26 2005-08-08 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
CA2477764A1 (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
AU2003221706B2 (en) 2002-04-11 2008-02-28 Merck Sharp & Dohme Corp. 1H-Benzo[F]indazol-5-YL derivatives as selective glucocorticoid receptor modulators
JP2005523920A (ja) 2002-04-25 2005-08-11 グラクソ グループ リミテッド フェネタノールアミン誘導体
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
BR0312575A (pt) 2002-07-08 2005-05-03 Pfizer Prod Inc Moduladores do receptor de glicocorticóides
JP2006508042A (ja) 2002-07-18 2006-03-09 ブリストル−マイヤーズ スクイブ カンパニー グルココルチコイド受容体の修飾物質および方法
GB0217225D0 (en) 2002-07-25 2002-09-04 Glaxo Group Ltd Medicinal compounds
WO2004014902A2 (en) 2002-08-09 2004-02-19 Astrazeneca Ab Compounds having an activity at metabotropic glutamate receptors
CA2495120A1 (en) 2002-08-09 2004-02-19 Astrazeneca Ab Oxadiazoles as modulators of metabotropic glutamate receptor-5
UA87653C2 (en) 2002-08-09 2009-08-10 Астразенека Аб 1,2,4-oxadiazols as modulators of receptor-5 for metabotropic glutamate
US20040224986A1 (en) 2002-08-16 2004-11-11 Bart De Corte Piperidinyl targeting compounds that selectively bind integrins
ATE403648T1 (de) 2002-08-21 2008-08-15 Boehringer Ingelheim Pharma Substituierte dihydrochinoline als glucocorticoid-mmimetika,verfahren zu deren herstellung, pharmazeutische zubereitungen und deren verwendung
GB0220730D0 (en) 2002-09-06 2002-10-16 Glaxo Group Ltd Medicinal compounds
DK1539753T3 (da) 2002-09-16 2010-01-04 Glaxo Group Ltd Pyrazolo(3,4B9pyridin-forbindelser og deres anvendelse som phosphodiesterase-inhibitorer
GB0230045D0 (en) 2002-12-23 2003-01-29 Glaxo Group Ltd Compounds
JP4520309B2 (ja) 2002-09-20 2010-08-04 メルク・シャープ・エンド・ドーム・コーポレイション 選択的糖質コルチコイド受容体調節剤としてのオクタヒドロ−2−H−ナフト[1,2−f]インドール−4−カルボキサミド誘導体
GB0224084D0 (en) 2002-10-16 2002-11-27 Glaxo Group Ltd Novel compounds
JP2006506373A (ja) 2002-10-22 2006-02-23 グラクソ グループ リミテッド 医薬アリールエタノールアミン化合物
DE60320007T2 (de) 2002-10-28 2009-06-18 Glaxo Group Ltd., Greenford Phenthanolamin-Derivate zur Behandlung von Atemwegserkrankungen
GB0225030D0 (en) 2002-10-28 2002-12-04 Glaxo Group Ltd Medicinal compounds
GB0225535D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
GB0225540D0 (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
CA2528938A1 (en) 2003-06-13 2005-02-24 Zentaris Gmbh Compounds having inhibitive activity of phosphatidylinositol 3-kinase and methods of use thereof
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
MY143366A (en) 2003-10-14 2011-04-29 Glaxo Group Ltd Muscarinic acetylcholine receptor antagonists
EP1679308B1 (en) * 2003-10-15 2013-07-24 Ube Industries, Ltd. Novel indazole derivative
PT1699512E (pt) 2003-11-03 2012-09-11 Glaxo Group Ltd Dispositivo distribuidor de fluido
TW200524577A (en) 2003-11-04 2005-08-01 Glaxo Group Ltd Muscarinic acetylcholine receptor antagonists
WO2005058892A1 (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
CN100432075C (zh) 2004-02-04 2008-11-12 神经研究公司 作为烟碱样乙酰胆碱受体配体的二氮杂双环芳基衍生物
GB0405937D0 (en) 2004-03-16 2004-04-21 Glaxo Group Ltd Compounds
GB0405933D0 (en) 2004-03-16 2004-04-21 Glaxo Group Ltd Compounds
RU2378274C2 (ru) 2004-03-16 2010-01-10 Глаксо Груп Лимитед ПИРАЗОЛО[3,4-b]ПИРИДИНОВОЕ СОЕДИНЕНИЕ И ЕГО ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРА ФДЭ4
MY144753A (en) 2004-04-27 2011-10-31 Glaxo Group Ltd Muscarinic acetylcholine receptor antagonists
MXPA06014574A (es) 2004-06-24 2007-03-12 Incyte Corp Piperidinas n-sustituidas y su uso como farmaceuticos.
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
WO2006045416A1 (en) 2004-10-19 2006-05-04 F. Hoffmann-La Roche Ag Quinoline derivatives
US20060122210A1 (en) 2004-11-18 2006-06-08 Wenqing Yao Inhibitors of 11-beta hydroxyl steroid dehydrogenase type I and methods of using the same
CA2589896A1 (en) 2004-11-30 2006-06-08 Plexxikon, Inc. Indole derivatives for use as ppar active compounds
EP1841780B1 (en) 2005-01-10 2011-07-27 Glaxo Group Limited Androstane 17-alpha-carbonate derivatives for use in the treatment of allergic and inflammatory conditions
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
EP1848428A4 (en) 2005-02-18 2012-04-18 Neurogen Corp THIAZOLE AMIDES, IMIDAZOLE AMIDES AND RELATED ANALOGS
JP2008534004A (ja) 2005-03-31 2008-08-28 ローネン カハナ, ウイルス性疾患に対して抵抗の鳥および他の動物の作製
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
US20070066624A1 (en) 2005-08-16 2007-03-22 Anormed, Inc. Chemokine receptor binding compounds
RU2008140144A (ru) 2006-03-10 2010-04-20 Оно Фармасьютикал Ко., Лтд. (Jp) Азотосодержащее гетероциклическое производное и фармацевтическое средство, включающее такое производное в качестве активного ингредиента
JP2009531443A (ja) 2006-03-29 2009-09-03 フォールドアールエックス ファーマシューティカルズ インコーポレーティッド α−シヌクレイン毒性の抑制
CA2644910C (en) 2006-03-31 2014-01-28 Abbott Laboratories Indazole compounds
GB0608820D0 (en) 2006-05-04 2006-06-14 Piramed Ltd Pharmaceutical compounds
US8492378B2 (en) 2006-08-03 2013-07-23 Takeda Pharmaceutical Company Limited GSK-3β inhibitor
WO2008020229A2 (en) 2006-08-17 2008-02-21 Astrazeneca Ab Antibacterial pyrrolecarboxamides
WO2008024945A1 (en) 2006-08-25 2008-02-28 Abbott Laboratories Indazole derivatives that inhibit trpv1 and uses thereof
US7948877B2 (en) * 2006-09-07 2011-05-24 Via Technologies, Inc. Systems and methods for packet forward control
AU2007301607A1 (en) 2006-09-25 2008-04-03 Mutabilis Sa Substituted heterocyclylcarbonylamino-acetic-acid-derivatives as inhibitors of bacterial heptose synthesis, methods for their preparation and biological applications of said inhibitors
JP2010504933A (ja) 2006-09-29 2010-02-18 ノバルティス アーゲー Pi3k脂質キナーゼ阻害剤としてのピラゾロピリミジン
TWI404532B (zh) 2006-11-02 2013-08-11 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
US20100210644A1 (en) 2007-06-25 2010-08-19 Boehringer Ingelheim International Gmbh Chemical compounds
ATE554078T1 (de) * 2007-07-26 2012-05-15 Vitae Pharmaceuticals Inc Synthese von 11-beta-hydroxysteroid-dehydrogenase-1-hemmern
WO2009042607A1 (en) 2007-09-24 2009-04-02 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
WO2009134384A1 (en) * 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CA2722427A1 (en) * 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
WO2009134387A1 (en) 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
US8569292B2 (en) * 2008-05-01 2013-10-29 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1
US8163743B2 (en) * 2008-06-05 2012-04-24 GlaxoGroupLimited 4-carboxamide indazole derivatives useful as inhibitors of PI3-kinases
ES2526966T3 (es) 2008-06-05 2015-01-19 Glaxo Group Limited Compuestos novedosos
EP2300437B1 (en) 2008-06-05 2013-11-20 Glaxo Group Limited Benzpyrazol derivatives as inhibitors of pi3 kinases
WO2009147190A1 (en) 2008-06-05 2009-12-10 Glaxo Group Limited Novel compounds
US10322469B2 (en) * 2008-06-11 2019-06-18 Hamamatsu Photonics K.K. Fusion bonding process for glass
KR20110050459A (ko) 2008-07-25 2011-05-13 비타이 파마슈티컬즈, 인코포레이티드 11베타-하이드록시스테로이드 탈수소효소 1의 고리형 억제제
US8245111B2 (en) * 2008-12-09 2012-08-14 Intel Corporation Performing multi-bit error correction on a cache line
US20110237633A1 (en) 2008-12-11 2011-09-29 Bijoy Panicker Small molecule modulators of hepatocyte growth factor (scatter factor) activity
WO2010083163A1 (en) 2009-01-13 2010-07-22 Philadelphia Health And Education Corporation The role of p110 delta signaling in morbidity and lung pathology induced by influenza virus infection
US8524751B2 (en) 2009-03-09 2013-09-03 GlaxoSmithKline Intellecutual Property Development 4-oxadiazol-2-YL-indazoles as inhibitors of P13 kinases
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
BRPI1014641A2 (pt) 2009-04-30 2019-09-24 Bayer Cropscience Ag arilpirrolidinas pesticidas
CA2759476C (en) * 2009-04-30 2018-10-09 Julie Nicole Hamblin Novel compounds
KR20120061771A (ko) 2009-04-30 2012-06-13 비타이 파마슈티컬즈, 인코포레이티드 11베타-하이드록시스테로이드 탈수소효소 1의 고리형 억제제
CN102459197B (zh) 2009-04-30 2015-08-19 Abbvie公司 适用于治疗响应血清素5-ht6受体的调节的病症的n-苯基-(哌嗪基或高哌嗪基)-苯磺酰胺或苯磺酰基-苯基-(哌嗪或高哌嗪)化合物
MA33216B1 (fr) 2009-04-30 2012-04-02 Boehringer Ingelheim Int Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1
JP2013512878A (ja) 2009-12-03 2013-04-18 グラクソ グループ リミテッド 新規化合物
EP2507231A1 (en) 2009-12-03 2012-10-10 Glaxo Group Limited Indazole derivatives as pi 3 - kinase inhibitors
WO2011067365A1 (en) * 2009-12-03 2011-06-09 Glaxo Group Limited Benzpyrazole derivatives as inhibitors of p13 kinases
US9102668B2 (en) 2010-09-08 2015-08-11 Glaxo Group Limited Polymorphs and salts
JP5876051B2 (ja) 2010-09-08 2016-03-02 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 インフルエンザウィルス感染の治療に使用するためのインダゾール誘導体
DK2614058T3 (en) 2010-09-08 2015-09-28 Glaxosmithkline Ip Dev Ltd Polymorphs, and the salts of N- [5- [4- (5 - {[(2R, 6S) -2,6-dimethyl-4-morpholinyl] methyl} -1,3-oxazol-2-yl) -1H-indazole -6-yl] -2- (methyloxy) -3-pyridinyl] methanesulfonamide.
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
JEROEN C. VERHEIJEN,等: ""Phosphatidylinositol 3-kinase (PI3K) inhibitors as anticancer drugs"", 《DRUGS OF THE FUTURE》, vol. 32, no. 6, 31 December 2007 (2007-12-31), pages 537 - 547, XP002503896, DOI: doi:10.1358/DOF.2007.03206.1107995 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103270037A (zh) * 2010-10-27 2013-08-28 葛兰素集团有限公司 作为pi3k抑制剂用于治疗例如呼吸系统病症的6-(1h-吲哚-4-基)-4-(5-{[4-(1-甲基乙基)-1-哌嗪基]甲基}-1,3-噁唑-2-基)-1h-吲唑的多晶形物和盐
CN103270037B (zh) * 2010-10-27 2015-10-21 葛兰素集团有限公司 作为pi3k抑制剂用于治疗例如呼吸系统病症的6-(1h-吲哚-4-基)-4-(5-{[4-(1-甲基乙基)-1-哌嗪基]甲基}-1,3-噁唑-2-基)-1h-吲唑的多晶形物和盐
CN105611929A (zh) * 2013-10-17 2016-05-25 葛兰素史克知识产权开发有限公司 用于治疗呼吸系统疾病的pi3k抑制剂
CN105658218A (zh) * 2013-10-17 2016-06-08 葛兰素史克知识产权开发有限公司 用于治疗呼吸疾病的pi3k抑制剂
CN104086538A (zh) * 2014-06-13 2014-10-08 南京药石药物研发有限公司 一种pi3k激酶抑制剂的中间体及其制备方法与应用

Also Published As

Publication number Publication date
ZA201107878B (en) 2013-04-24
BRPI1016219A2 (pt) 2016-04-26
CY1119515T1 (el) 2018-03-07
TW201604192A (zh) 2016-02-01
IL215803A (en) 2014-11-30
LT2899191T (lt) 2017-10-25
AR108388A2 (es) 2018-08-15
EP3260453B1 (en) 2021-03-31
US20150328226A1 (en) 2015-11-19
BRPI1016219B1 (pt) 2020-09-01
PL2899191T3 (pl) 2018-01-31
TW201444832A (zh) 2014-12-01
HUE034724T2 (hu) 2018-02-28
MA33304B1 (fr) 2012-05-02
US8580797B2 (en) 2013-11-12
TW201103927A (en) 2011-02-01
US20190328744A1 (en) 2019-10-31
EP2424864B1 (en) 2014-12-03
AU2010243613A1 (en) 2011-11-17
HK1165801A1 (en) 2012-10-12
US20140080830A1 (en) 2014-03-20
US20180325911A1 (en) 2018-11-15
CL2011002706A1 (es) 2012-04-09
SG10201401881QA (en) 2014-07-30
PL2424864T3 (pl) 2015-05-29
ES2876933T3 (es) 2021-11-15
US20100280029A1 (en) 2010-11-04
PT2899191T (pt) 2017-11-14
ME02053B (me) 2015-05-20
CA2759476C (en) 2018-10-09
ES2644724T3 (es) 2017-11-30
TWI466884B (zh) 2015-01-01
MX2011011534A (es) 2012-02-28
DOP2011000328A (es) 2016-12-30
CO6390057A2 (es) 2012-02-29
US20190175608A1 (en) 2019-06-13
JP5570589B2 (ja) 2014-08-13
PT2424864E (pt) 2015-02-27
US20130096117A1 (en) 2013-04-18
US20120046286A1 (en) 2012-02-23
US10946025B2 (en) 2021-03-16
AR076435A1 (es) 2011-06-08
EA021056B1 (ru) 2015-03-31
ME02900B (me) 2018-04-20
RS56433B1 (sr) 2018-01-31
EP2899191A1 (en) 2015-07-29
SI2424864T1 (sl) 2015-03-31
BRPI1016219B8 (pt) 2021-05-25
WO2010125082A1 (en) 2010-11-04
NZ596071A (en) 2013-12-20
TWI562992B (en) 2016-12-21
US10383879B2 (en) 2019-08-20
KR20160135852A (ko) 2016-11-28
EP3260453A1 (en) 2017-12-27
KR20120079852A (ko) 2012-07-13
DK2899191T3 (da) 2017-11-13
EP2424864A1 (en) 2012-03-07
MY160454A (en) 2017-03-15
US8586583B2 (en) 2013-11-19
US20130029985A1 (en) 2013-01-31
RS53830B1 (en) 2015-06-30
US8609657B2 (en) 2013-12-17
CR20110603A (es) 2012-02-28
DK2424864T3 (en) 2015-02-23
SMT201500043B (it) 2015-05-05
US20170015656A1 (en) 2017-01-19
AU2010243613B2 (en) 2015-05-07
JO3025B1 (ar) 2016-09-05
EA201190227A1 (ru) 2012-05-30
US8575162B2 (en) 2013-11-05
PE20120321A1 (es) 2012-04-19
UA101098C2 (en) 2013-02-25
SI2899191T1 (sl) 2017-11-30
UY32585A (es) 2010-11-30
US20170157136A1 (en) 2017-06-08
SG175782A1 (en) 2011-12-29
CN102459253B (zh) 2015-03-25
TWI516487B (zh) 2016-01-11
US10624898B2 (en) 2020-04-21
US20100280045A1 (en) 2010-11-04
HRP20171450T1 (hr) 2017-11-17
HRP20150173T1 (hr) 2015-05-22
HK1209102A1 (en) 2016-03-24
ES2531274T3 (es) 2015-03-12
IL215803A0 (en) 2012-01-31
US20200206237A1 (en) 2020-07-02
EP2899191B1 (en) 2017-08-09
CA2759476A1 (en) 2010-11-04
KR101771193B1 (ko) 2017-09-05
JP2012525349A (ja) 2012-10-22
KR101679642B1 (ko) 2016-11-25
US20130131080A1 (en) 2013-05-23
US8586590B2 (en) 2013-11-19

Similar Documents

Publication Publication Date Title
CN102459253A (zh) 作为pi3-激酶抑制剂的*唑取代的吲唑化合物
ES2548036T3 (es) Polimorfos y sales 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]metanosulfonamida
CN103270037B (zh) 作为pi3k抑制剂用于治疗例如呼吸系统病症的6-(1h-吲哚-4-基)-4-(5-{[4-(1-甲基乙基)-1-哌嗪基]甲基}-1,3-噁唑-2-基)-1h-吲唑的多晶形物和盐
ES2526966T3 (es) Compuestos novedosos
EP2507223A1 (en) Benzpyrazole derivatives as inhibitors of p13 kinases
JP2013512880A (ja) Pi3−キナーゼ阻害剤としてのインダゾール誘導体
CN108884046A (zh) 作为激酶活性的抑制剂的化学化合物
ES2906956T3 (es) Derivados de oxepinopirazol como inhibidores de la actividad de PI3-cinasa

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant