JP2014506601A5 - - Google Patents

Download PDF

Info

Publication number
JP2014506601A5
JP2014506601A5 JP2013555580A JP2013555580A JP2014506601A5 JP 2014506601 A5 JP2014506601 A5 JP 2014506601A5 JP 2013555580 A JP2013555580 A JP 2013555580A JP 2013555580 A JP2013555580 A JP 2013555580A JP 2014506601 A5 JP2014506601 A5 JP 2014506601A5
Authority
JP
Japan
Prior art keywords
item
alkyl
halo
heterocycloalkyl
aryl
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
JP2013555580A
Other languages
English (en)
Japanese (ja)
Other versions
JP5808826B2 (ja
JP2014506601A (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/US2012/026406 external-priority patent/WO2012116237A2/en
Publication of JP2014506601A publication Critical patent/JP2014506601A/ja
Publication of JP2014506601A5 publication Critical patent/JP2014506601A5/ja
Application granted granted Critical
Publication of JP5808826B2 publication Critical patent/JP5808826B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

JP2013555580A 2011-02-23 2012-02-23 複素環化合物およびその使用 Expired - Fee Related JP5808826B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161445999P 2011-02-23 2011-02-23
US61/445,999 2011-02-23
PCT/US2012/026406 WO2012116237A2 (en) 2011-02-23 2012-02-23 Heterocyclic compounds and uses thereof

Publications (3)

Publication Number Publication Date
JP2014506601A JP2014506601A (ja) 2014-03-17
JP2014506601A5 true JP2014506601A5 (enExample) 2015-07-02
JP5808826B2 JP5808826B2 (ja) 2015-11-10

Family

ID=46721464

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2013555580A Expired - Fee Related JP5808826B2 (ja) 2011-02-23 2012-02-23 複素環化合物およびその使用

Country Status (4)

Country Link
US (1) US9127000B2 (enExample)
EP (1) EP2678016B1 (enExample)
JP (1) JP5808826B2 (enExample)
WO (1) WO2012116237A2 (enExample)

Families Citing this family (83)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
HUE042374T2 (hu) 2012-06-13 2019-06-28 Incyte Holdings Corp Szubsztituált triciklusos vegyületek mint FGFR inhibitorok
ES2689429T3 (es) 2012-07-13 2018-11-14 Ucb Biopharma Sprl Derivados de imidazopiridina como moduladores de actividad de TNF
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
JP6434416B2 (ja) 2012-11-08 2018-12-05 ライゼン・ファーマシューティカルズ・エスアー PDE4阻害剤とPI3δ阻害剤または二重PI3δ−γキナーゼ阻害剤とを含有する薬学的組成物
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
KR102469849B1 (ko) 2013-04-19 2022-11-23 인사이트 홀딩스 코포레이션 Fgfr 저해제로서 이환식 헤테로사이클
WO2015123437A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
WO2015123408A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
TWI664164B (zh) 2014-02-13 2019-07-01 美商英塞特控股公司 作為lsd1抑制劑之環丙胺
PE20161573A1 (es) 2014-02-13 2017-01-19 Incyte Corp Ciclopropilamina como inhibidor de la lsd1
US9695168B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]pyrazines as LSD1 inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
US9695180B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors
CN105503877A (zh) * 2014-09-24 2016-04-20 和记黄埔医药(上海)有限公司 咪唑并哒嗪类化合物及其用途
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US20170333435A1 (en) 2014-11-06 2017-11-23 Lysosomal Therapeutics Inc. Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders
WO2016073891A1 (en) 2014-11-06 2016-05-12 Lysosomal Therapeutics Inc. Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders
KR102662215B1 (ko) 2014-11-06 2024-05-02 비알 - 알&디 인베스트먼츠, 에스.에이. 치환된 피라졸로(1,5-a)피리미딘 및 의학적 장애의 치료에서의 그의 용도
JP6568588B2 (ja) 2014-12-19 2019-08-28 ヤンセン ファーマシューティカ エヌ.ベー. PI3Kβ阻害剤としてのイミダゾピリダジン誘導体
SI3233839T1 (sl) 2014-12-19 2019-12-31 Janssen Pharmaceutica Nv Heterociklil vezani derivati imidazopiridazina kot inhibitorji PI3Kbeta
JP6385584B2 (ja) 2014-12-24 2018-09-05 ギリアード サイエンシーズ, インコーポレイテッド Hivの処置のための縮合ピリミジン化合物
TWI770552B (zh) 2014-12-24 2022-07-11 美商基利科學股份有限公司 喹唑啉化合物
PT3237397T (pt) 2014-12-24 2019-02-08 Gilead Sciences Inc Compostos de isoquinolina para o tratamento de hiv
AU2016219822B2 (en) 2015-02-20 2020-07-09 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MY191796A (en) 2015-04-03 2022-07-15 Incyte Corp Heterocyclic compounds as lsd1 inhibitors
HK1255074A1 (zh) 2015-07-01 2019-08-02 Crinetics Pharmaceuticals, Inc. 生长抑素调节剂及其用途
KR102710120B1 (ko) 2015-08-12 2024-09-27 인사이트 홀딩스 코포레이션 Lsd1 저해제의 염
CN105130984B (zh) * 2015-09-23 2017-03-29 前湾医药科技(深圳)有限公司 一种咪唑并吡啶类化合物与在制备pi3k抑制剂中的应用
JP6912460B2 (ja) 2015-10-09 2021-08-04 ヤンセン ファーマシューティカ エヌ.ベー. PI3Kβ阻害剤としてのキノキサリンおよびピリドピラジン誘導体
PT3436461T (pt) 2016-03-28 2024-01-23 Incyte Corp Compostos de pirrolotriazina como inibidores de tam
US11192892B2 (en) 2016-04-06 2021-12-07 Bial—R&D Investments, S.A. Substituted pyrazolo[1,5-a]pyrimidines for the treatment of medical disorders
JP7034935B2 (ja) 2016-04-06 2022-03-14 リソソーマル・セラピューティクス・インコーポレイテッド ピロロ[1,2-a]ピリミジニルカルボキサミド化合物および医学的障害の処置におけるその使用
WO2017176961A1 (en) 2016-04-06 2017-10-12 Lysosomal Therapeutics Inc. Imidazo [1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
PE20190377A1 (es) 2016-04-22 2019-03-08 Incyte Corp Formulaciones de un inhibidor de lsd 1
WO2017192930A1 (en) 2016-05-05 2017-11-09 Lysosomal Therapeutics Inc. SUBSTITUTED IMIDAZO[1,2-b]PYRIDAZINES, SUBSTITUTED IMIDAZO[1,5-b]PYRIDAZINES, RELATED COMPOUNDS, AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
US11345698B2 (en) 2016-05-05 2022-05-31 Bial—R&D Investments, S.A. Substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-a]pyrazines, related compounds, and their use in the treatment of medical disorders
JP7149854B2 (ja) 2016-06-16 2022-10-07 ヤンセン ファーマシューティカ エヌ.ベー. Pi3k beta阻害薬としての二環式ピリジン、ピラジンおよびピリミジン誘導体
ES2818620T3 (es) 2016-06-16 2021-04-13 Janssen Pharmaceutica Nv Derivados de azabencimidazol como inhibidores de pi3k beta
US11352328B2 (en) 2016-07-12 2022-06-07 Arisan Therapeutics Inc. Heterocyclic compounds for the treatment of arenavirus
AU2017296289A1 (en) 2016-07-12 2019-01-31 Revolution Medicines, Inc. 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric SHP2 inhibitors
JP7240319B2 (ja) 2017-01-23 2023-03-15 レヴォリューション・メディスンズ,インコーポレイテッド アロステリックshp2阻害剤としての二環式化合物
CN110431134A (zh) 2017-01-23 2019-11-08 锐新医药公司 作为变构shp2抑制剂的吡啶化合物
CN110461827A (zh) 2017-03-29 2019-11-15 詹森药业有限公司 作为PI3K-β抑制剂的喹喔啉和吡啶并吡嗪衍生物
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
WO2019023278A1 (en) 2017-07-25 2019-01-31 Crinetics Pharmaceuticals, Inc. MODULATORS OF SOMATOSTATIN AND USES THEREOF
EP3694848A1 (en) 2017-10-12 2020-08-19 Revolution Medicines, Inc. Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors
CN107935918A (zh) * 2017-11-15 2018-04-20 山东潍坊润丰化工股份有限公司 一种百草枯的制备方法
TW201927791A (zh) 2017-12-15 2019-07-16 美商銳新醫藥公司 作為變構shp2抑制劑的多環化合物
WO2019168847A1 (en) 2018-02-27 2019-09-06 Incyte Corporation Imidazopyrimidines and triazolopyrimidines as a2a / a2b inhibitors
EP3788046B1 (en) 2018-05-04 2025-12-10 Incyte Corporation Salts of an fgfr inhibitor
EP4309737A3 (en) 2018-05-04 2024-03-27 Incyte Corporation Solid forms of an fgfr inhibitor and processes for preparing the same
US11168089B2 (en) 2018-05-18 2021-11-09 Incyte Corporation Fused pyrimidine derivatives as A2A / A2B inhibitors
JP7768505B2 (ja) 2018-06-01 2025-11-12 コーネル・ユニバーシティー Pi3kに関連する疾患または障害に対する併用療法
JOP20200342A1 (ar) 2018-07-05 2020-12-30 Incyte Corp مشتقات بيرازين مدمجة كمثبطات a2a/a2b
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
US12419865B2 (en) 2018-12-06 2025-09-23 Arisan Therapeutics Inc. Compounds for the treatment of arenavirus infection
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021076602A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US11884647B2 (en) 2019-10-18 2024-01-30 The Regents Of The University Of California Compounds and methods for targeting pathogenic blood vessels
KR20220131900A (ko) 2019-12-04 2022-09-29 인사이트 코포레이션 Fgfr 억제제의 유도체
JP7720840B2 (ja) 2019-12-04 2025-08-08 インサイト・コーポレイション Fgfr阻害剤としての三環式複素環
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021257863A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Pyrrolotriazine compounds as jak2 v617f inhibitors
US11691971B2 (en) 2020-06-19 2023-07-04 Incyte Corporation Naphthyridinone compounds as JAK2 V617F inhibitors
US11767323B2 (en) 2020-07-02 2023-09-26 Incyte Corporation Tricyclic pyridone compounds as JAK2 V617F inhibitors
IL299612A (en) 2020-07-02 2023-03-01 Incyte Corp Tricyclic urea compounds as JAK2 V617F inhibitors
US11661422B2 (en) 2020-08-27 2023-05-30 Incyte Corporation Tricyclic urea compounds as JAK2 V617F inhibitors
WO2022140231A1 (en) 2020-12-21 2022-06-30 Incyte Corporation Deazaguaine compounds as jak2 v617f inhibitors
US11958861B2 (en) 2021-02-25 2024-04-16 Incyte Corporation Spirocyclic lactams as JAK2 V617F inhibitors
CA3215903A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
EP4352059A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2022261159A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
EP4493558A1 (en) 2022-03-17 2025-01-22 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
WO2023239846A1 (en) * 2022-06-10 2023-12-14 Synnovation Therapeutics, Inc. Heterocyclic compounds as pi3kα inhibitors
CN116425743B (zh) * 2022-12-30 2025-06-17 贵州医科大学 一种作为PI3Kα激酶抑制剂的苯并杂环类化合物及其制备方法与应用

Family Cites Families (193)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2313993A (en) 1939-02-04 1943-03-16 Chromogen Inc Organic sulphur and selenium compounds
GB1219606A (en) 1968-07-15 1971-01-20 Rech S Et D Applic Scient Soge Quinuclidinol derivatives and preparation thereof
US3657744A (en) 1970-05-08 1972-04-25 Univ Minnesota Method for fixing prosthetic implants in a living body
FR2102541A5 (enExample) 1970-08-07 1972-04-07 Aquitaine Total Organico
US4733665C2 (en) 1985-11-07 2002-01-29 Expandable Grafts Partnership Expandable intraluminal graft and method and apparatus for implanting an expandable intraluminal graft
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US5061273A (en) 1989-06-01 1991-10-29 Yock Paul G Angioplasty apparatus facilitating rapid exchanges
US5350395A (en) 1986-04-15 1994-09-27 Yock Paul G Angioplasty apparatus facilitating rapid exchanges
US5040548A (en) 1989-06-01 1991-08-20 Yock Paul G Angioplasty mehtod
US4748982A (en) 1987-01-06 1988-06-07 Advanced Cardiovascular Systems, Inc. Reinforced balloon dilatation catheter with slitted exchange sleeve and method
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US5093330A (en) 1987-06-15 1992-03-03 Ciba-Geigy Corporation Staurosporine derivatives substituted at methylamino nitrogen
CA1322628C (en) 1988-10-04 1993-10-05 Richard A. Schatz Expandable intraluminal graft
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
GB8916480D0 (en) 1989-07-19 1989-09-06 Glaxo Group Ltd Chemical process
US5674278A (en) 1989-08-24 1997-10-07 Arterial Vascular Engineering, Inc. Endovascular support device
US6344053B1 (en) 1993-12-22 2002-02-05 Medtronic Ave, Inc. Endovascular support device and method
US5292331A (en) 1989-08-24 1994-03-08 Applied Vascular Engineering, Inc. Endovascular support device
GB8923590D0 (en) 1989-10-19 1989-12-06 Pfizer Ltd Antimuscarinic bronchodilators
US5395855A (en) 1990-05-07 1995-03-07 Ciba-Geigy Corporation Hydrazones
US5614519A (en) 1991-02-06 1997-03-25 Karl Thomae Gmbh (1-(2,3 or 4-N-morpholinoalkyl)-imidazol-4-yl)-benizimidazol-1-yl-methyl]-biphenyls useful as angiotensin-II antagonists
PT100441A (pt) 1991-05-02 1993-09-30 Smithkline Beecham Corp Pirrolidinonas, seu processo de preparacao, composicoes farmaceuticas que as contem e uso
US5710158A (en) 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5480883A (en) 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5451700A (en) 1991-06-11 1995-09-19 Ciba-Geigy Corporation Amidino compounds, their manufacture and methods of treatment
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
WO1993019749A1 (en) 1992-04-02 1993-10-14 Smithkline Beecham Corporation Compounds useful for treating allergic and inflammatory diseases
JP3192424B2 (ja) 1992-04-02 2001-07-30 スミスクライン・ビーチャム・コーポレイション アレルギーまたは炎症疾患の治療用化合物
WO1993019751A1 (en) 1992-04-02 1993-10-14 Smithkline Beecham Corporation Compounds useful for treating inflammatory diseases and inhibiting production of tumor necrosis factor
TW225528B (enExample) 1992-04-03 1994-06-21 Ciba Geigy Ag
AU687727B2 (en) 1992-10-28 1998-03-05 Genentech Inc. Vascular endothelial cell growth factor antagonists
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
GB9301000D0 (en) 1993-01-20 1993-03-10 Glaxo Group Ltd Chemical compounds
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
US5681835A (en) 1994-04-25 1997-10-28 Glaxo Wellcome Inc. Non-steroidal ligands for the estrogen receptor
GB9414193D0 (en) 1994-07-14 1994-08-31 Glaxo Group Ltd Compounds
GB9414208D0 (en) 1994-07-14 1994-08-31 Glaxo Group Ltd Compounds
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
EP0817775B1 (en) 1995-03-30 2001-09-12 Pfizer Inc. Quinazoline derivatives
FI973974A7 (fi) 1995-04-20 1997-10-16 Pfizer Aryylisulfonyylihydroksaamihappojohdannaisia MMP- ja TNF-inhibiittorei na
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
ATE212993T1 (de) 1995-07-06 2002-02-15 Novartis Erfind Verwalt Gmbh Pyrolopyrimidine und verfahren zu ihrer herstellung
DE69624081T2 (de) 1995-12-20 2003-06-12 Agouron Pharmaceuticals, Inc. Matrix-metalloprotease Inhibitoren
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
EP0892789B2 (en) 1996-04-12 2009-11-18 Warner-Lambert Company LLC Irreversible inhibitors of tyrosine kinases
DE69734513T2 (de) 1996-06-24 2006-07-27 Pfizer Inc. Phenylamino-substituierte tricyclische derivate zur behandlung hyperproliferativer krankheiten
HUP9903014A3 (en) 1996-07-18 2000-08-28 Pfizer Phosphinate derivatives having matrix metalloprotease inhibitor effect and medicaments containing the same
IL128189A0 (en) 1996-08-23 1999-11-30 Pfizer Arylsulfonylamino hydroxamic acid derivatives
DE19638745C2 (de) 1996-09-11 2001-05-10 Schering Ag Monoklonale Antikörper gegen die extrazelluläre Domäne des menschlichen VEGF - Rezeptorproteins (KDR)
AU4342997A (en) 1996-09-13 1998-04-02 Sugen, Inc. Use of quinazoline derivatives for the manufacture of a medicament in the reatment of hyperproliferative skin disorders
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
GB9622386D0 (en) 1996-10-28 1997-01-08 Sandoz Ltd Organic compounds
TW528755B (en) 1996-12-24 2003-04-21 Glaxo Group Ltd 2-(purin-9-yl)-tetrahydrofuran-3,4-diol derivatives
ES2224277T3 (es) 1997-01-06 2005-03-01 Pfizer Inc. Derivados de sulfonas ciclicas.
PT977733E (pt) 1997-02-03 2003-12-31 Pfizer Prod Inc Derivados de acido arilsulfonilamino-hidroxamico
JP2000507975A (ja) 1997-02-07 2000-06-27 ファイザー・インク N−ヒドロキシ−β−スルホニルプロピオンアミド誘導体類及びそれらのマトリックスメタロプロテイナーゼ阻害薬としての使用
IL131123A0 (en) 1997-02-11 2001-01-28 Pfizer Arylsulfonyl hydroxamic acid derivatives
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
CO4940418A1 (es) 1997-07-18 2000-07-24 Novartis Ag Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
ES2216293T3 (es) 1997-08-08 2004-10-16 Pfizer Products Inc. Derivados de acido ariloxiarilsulfonilamino-hidroxamico.
US6166037A (en) 1997-08-28 2000-12-26 Merck & Co., Inc. Pyrrolidine and piperidine modulators of chemokine receptor activity
WO1999016766A1 (en) 1997-10-01 1999-04-08 Kyowa Hakko Kogyo Co., Ltd. Benzodioxole derivatives
GB9723566D0 (en) 1997-11-08 1998-01-07 Glaxo Group Ltd Chemical compounds
GB9723590D0 (en) 1997-11-08 1998-01-07 Glaxo Group Ltd Chemical compounds
GB9723589D0 (en) 1997-11-08 1998-01-07 Glaxo Group Ltd Chemical compounds
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
YU44900A (sh) 1998-01-31 2003-01-31 Glaxo Group Limited Derivati 2-(purin-9-il)tetrahidrofuran-3,4-diola
PE20000270A1 (es) 1998-02-14 2000-05-20 Glaxo Group Ltd Derivados de 2-(purin-9-il)-tetrahidrofuran-3,4-diol
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
GB9813535D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
GB9813565D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
YU81100A (sh) 1998-06-23 2003-10-31 Glaxo Group Limited Derivati 2-(purin-9-il)tetrahidrofuran-3,4 diola
GB9813540D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
DE69827673T2 (de) 1998-06-30 2005-04-21 Dow Global Technologies Inc Polymerpolyole und ein verfahren zu ihrer darstellung
CN1152031C (zh) 1998-08-11 2004-06-02 诺瓦提斯公司 具有血管生成抑制活性的异喹啉衍生物
EP1121372B1 (en) 1998-10-16 2006-06-28 Pfizer Limited Adenine derivatives
UA71587C2 (uk) 1998-11-10 2004-12-15 Шерінг Акцієнгезелльшафт Аміди антранілової кислоти та їхнє застосування як лікарських засобів
GB9824579D0 (en) 1998-11-10 1999-01-06 Novartis Ag Organic compounds
ATE300957T1 (de) 1998-12-22 2005-08-15 Genentech Inc Antagonisten von vaskular-endothelialen zellwachstumsfaktoren und ihre anwendung
PT1165085E (pt) 1999-03-30 2006-10-31 Novartis Ag Derivados de ftalazina para tratar doencas inflamatorias
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
EP1175402B1 (en) 1999-05-04 2005-07-20 Schering Corporation Piperidine derivatives useful as ccr5 antagonists
CZ20013940A3 (cs) 1999-05-04 2002-04-17 Schering Corporation Piperazinové deriváty uľitečné jako CCR5 antagonisté
YU25500A (sh) 1999-05-11 2003-08-29 Pfizer Products Inc. Postupak za sintezu analoga nukleozida
GB9913932D0 (en) 1999-06-15 1999-08-18 Pfizer Ltd Purine derivatives
US6322771B1 (en) 1999-06-18 2001-11-27 University Of Virginia Patent Foundation Induction of pharmacological stress with adenosine receptor agonists
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
SI1212089T1 (sl) 1999-08-21 2006-08-31 Altana Pharma Ag Sinergisticna kombinacija roflumilasta in salmeterola
CO5180581A1 (es) 1999-09-30 2002-07-30 Pfizer Prod Inc Compuestos para el tratamiento de la isquemia ciones farmaceuticas que los contienen para el tratamiento de la isquemia
GB9924363D0 (en) 1999-10-14 1999-12-15 Pfizer Central Res Purine derivatives
GB9924361D0 (en) 1999-10-14 1999-12-15 Pfizer Ltd Purine derivatives
GB0003960D0 (en) 2000-02-18 2000-04-12 Pfizer Ltd Purine derivatives
WO2001081346A2 (en) 2000-04-25 2001-11-01 Icos Corporation Inhibitors of human phosphatidyl-inositol 3-kinase delta
TWI227240B (en) 2000-06-06 2005-02-01 Pfizer 2-aminocarbonyl-9H-purine derivatives
BR0112297A (pt) 2000-06-27 2003-05-06 S A L V A T Lab Sa Compostos carbamatos derivados de arilalquilaminas
GB0015727D0 (en) 2000-06-27 2000-08-16 Pfizer Ltd Purine derivatives
GB0015876D0 (en) 2000-06-28 2000-08-23 Novartis Ag Organic compounds
DE10038639A1 (de) 2000-07-28 2002-02-21 Schering Ag Nichtsteroidale Entzündungshemmer
CO5310534A1 (es) 2000-08-05 2003-08-29 Glaxo Group Ltd Nuevos derivados de androstano anti-inflamatorios
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
GB0022695D0 (en) 2000-09-15 2000-11-01 Pfizer Ltd Purine Derivatives
GB0028383D0 (en) 2000-11-21 2001-01-03 Novartis Ag Organic compounds
SI1341769T1 (sl) 2000-12-15 2008-02-29 Vertex Pharma Inhibitorji bakterijske giraze in njihove uporabe
EP1345937B1 (en) 2000-12-22 2005-09-28 Almirall Prodesfarma AG Quinuclidine carbamate derivatives and their use as m3 antagonists
EE05404B1 (et) 2000-12-28 2011-04-15 Almirall Prodesfarma Ag Kinuklidiini derivaat, selle saamine ja kasutamine ravimi valmistamiseks, mis on ette n„htud respiratoorsete, kuseelundite v?i mao-soolte haiguste ravimiseks, ning seda sisaldav ravimkompositsioon
EP1241176A1 (en) 2001-03-16 2002-09-18 Pfizer Products Inc. Purine derivatives for the treatment of ischemia
ES2314052T3 (es) 2001-04-30 2009-03-16 Glaxo Group Limited Derivados de ester de 17beta-carbotioato de androstano con un grupo ester ciclico en la posicion 17alfa.
AR035885A1 (es) 2001-05-14 2004-07-21 Novartis Ag Derivados de 4-amino-5-fenil-7-ciclobutilpirrolo (2,3-d)pirimidina, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos derivados para la preparacion de una composicion farmaceutica
BR0209986A (pt) 2001-05-25 2004-04-06 Pfizer Agonista de a2a em combinação com um agente anticolinérgico, para o tratamento de doenças obstrutivas das vias respiratórias
US20040248867A1 (en) 2001-06-12 2004-12-09 Keith Biggadike Novel anti-inflammatory 17.alpha.-heterocyclic-esters of 17.beta.carbothioate androstane derivatives
DK2327766T3 (en) 2001-06-21 2016-03-07 Basf Enzymes Llc nitrilases
GB0119249D0 (en) 2001-08-07 2001-10-03 Novartis Ag Organic compounds
IL160896A0 (en) 2001-10-17 2004-08-31 Ucb Sa Quinuclidine derivatives, processes for preparing them and their uses as m2 and/or m3 muscarinic receptor inhibitors
GB0125259D0 (en) 2001-10-20 2001-12-12 Glaxo Group Ltd Novel compounds
MY130622A (en) 2001-11-05 2007-07-31 Novartis Ag Naphthyridine derivatives, their preparation and their use as phosphodiesterase isoenzyme 4 (pde4) inhibitors
WO2003048181A1 (en) 2001-12-01 2003-06-12 Glaxo Group Limited 17.alpha. -cyclic esters of 16-methylpregnan-3,20-dione as anti-inflammatory agents
PL211250B1 (pl) 2001-12-20 2012-04-30 Chiesi Farma Spa Pochodne karbaminianu 1-alkilo-1-azoniabicyklo [2.2.2] oktanu, jej zastosowania, kompozycja farmaceutyczna zawierająca ten związek oraz związek pośredni
WO2003072592A1 (en) 2002-01-15 2003-09-04 Glaxo Group Limited 17.alpha-cycloalkyl/cycloylkenyl esters of alkyl-or haloalkyl-androst-4-en-3-on-11.beta.,17.alpha.-diol 17.beta.-carboxylates as anti-inflammatory agents
WO2003062259A2 (en) 2002-01-21 2003-07-31 Glaxo Group Limited Non-aromatic 17.alpha.-esters of androstane-17.beta.-carboxylate esters as anti-inflammatory agents
GB0202216D0 (en) 2002-01-31 2002-03-20 Glaxo Group Ltd Novel compounds
EP1490317A1 (en) 2002-03-26 2004-12-29 Boehringer Ingelheim Pharmaceuticals Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
HRP20040887A2 (en) 2002-03-26 2005-04-30 Boehringer Ingelheim Pharmaceuticals Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
US20090170803A1 (en) 2002-04-10 2009-07-02 Linden Joel M Adjunctive treatment of biological diseases
ES2206021B1 (es) 2002-04-16 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de pirrolidinio.
ES2201907B1 (es) 2002-05-29 2005-06-01 Almirall Prodesfarma, S.A. Nuevos derivados de indolilpiperidina como potentes agentes antihistaminicos y antialergicos.
DE10224888A1 (de) 2002-06-05 2003-12-24 Merck Patent Gmbh Pyridazinderivate
US7074806B2 (en) 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE10225574A1 (de) 2002-06-10 2003-12-18 Merck Patent Gmbh Aryloxime
DE10227269A1 (de) 2002-06-19 2004-01-08 Merck Patent Gmbh Thiazolderivate
AU2003243870B2 (en) 2002-06-25 2008-11-20 Merck Frosst Canada Ltd 8-(biaryl) quinoline PDE4 inhibitors
AU2003281219A1 (en) 2002-07-02 2004-01-23 Bernard Cote Di-aryl-substituted-ethane pyridone pde4 inhibitors
ES2204295B1 (es) 2002-07-02 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de quinuclidina-amida.
AU2003281355A1 (en) 2002-07-08 2004-01-23 Pfizer Products Inc. Modulators of the glucocorticoid receptor
AR040962A1 (es) 2002-08-09 2005-04-27 Novartis Ag Compuestos derivados de tiazol 1,3-2-ona, composicion farmaceutica y proceso de preparacion del compuesto
AU2003260371A1 (en) 2002-08-10 2004-03-11 Altana Pharma Ag Piperidine-n-oxide-derivatives
AU2003251693A1 (en) 2002-08-10 2004-03-11 Altana Pharma Ag Pyridazinone-derivatives as pde4 inhibitors
BR0313330A (pt) 2002-08-10 2005-06-14 Altana Pharma Ag Piperidina-ftalazonas substituìdas com pirrolidinadiona como inibidores de pde4
WO2004018449A1 (en) 2002-08-10 2004-03-04 Altana Pharma Ag Piperidine-derivatives as pde4 inhibitors
PL373598A1 (en) 2002-08-17 2005-09-05 Altana Pharma Ag Novel benzonaphthyridines
WO2004018431A2 (en) 2002-08-17 2004-03-04 Altana Pharma Ag Novel phenanthridines
SE0202483D0 (sv) 2002-08-21 2002-08-21 Astrazeneca Ab Chemical compounds
ATE423769T1 (de) 2002-08-23 2009-03-15 Ranbaxy Lab Ltd Fluor- und sulfonylaminohaltige, 3,6- disubstituierte azabicyclo 3.1.0 hexanderivate als muscarinrezeptorantagonisten
JP4587295B2 (ja) 2002-08-29 2010-11-24 ニコメッド ゲゼルシャフト ミット ベシュレンクテル ハフツング Pde4インヒビターとしての3−ヒドロキシ−6−フェニルフェナントリジン
AU2003255493B8 (en) 2002-08-29 2009-03-26 Takeda Gmbh 2-hydroxy-6-phenylphenanthridines as PDE-4 inhibitors
JP2006096662A (ja) 2002-09-18 2006-04-13 Sumitomo Pharmaceut Co Ltd 新規6−置換ウラシル誘導体及びアレルギー性疾患の治療剤
KR20050057408A (ko) 2002-09-18 2005-06-16 오노 야꾸힝 고교 가부시키가이샤 트리아자스피로[5.5]운데칸 유도체 및 이를 유효 성분으로하는 약제
JP2004107299A (ja) 2002-09-20 2004-04-08 Japan Energy Corp 新規1−置換ウラシル誘導体及びアレルギー性疾患の治療剤
DE10246374A1 (de) 2002-10-04 2004-04-15 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Betamimetika mit verlängerter Wirkungsdauer, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
ATE380185T1 (de) 2002-10-23 2007-12-15 Glenmark Pharmaceuticals Ltd Tricyclische verbindungen zur behandlung von entzündlichen- und allergischen erkrankungen: verfahren zu deren herstellung und sie enthaltende pharmazeutische zusammensetzungen
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
DE10253282A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Arzneimittel zur Behandlung von chronisch obstruktiver Lungenerkrankung
DE10253220A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Dihydroxy-Methyl-Phenyl-Derivate, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
DE10253426B4 (de) 2002-11-15 2005-09-22 Elbion Ag Neue Hydroxyindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung
AU2004259012C1 (en) 2003-07-23 2012-08-02 Exelixis, Inc. Anaplastic lymphoma kinase modulators and methods of use
AR046845A1 (es) 2003-11-21 2005-12-28 Novartis Ag Derivados de 1h-imidazo[4,5-c]quinolina para tratamiento de enfermedades dependientes de las proteino-quinasas
KR100629060B1 (ko) 2004-08-11 2006-09-26 주식회사 엘지화학 새로운 벤즈이미다졸계 화합물
AU2005293607A1 (en) 2004-10-07 2006-04-20 Boehringer Ingelheim International Gmbh PI3 kinases
CN101384586A (zh) 2006-02-14 2009-03-11 诺华公司 Pi-3激酶抑制剂及其应用方法
PE20070978A1 (es) 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
WO2007127175A2 (en) 2006-04-26 2007-11-08 F. Hoffmann-La Roche Ag Pharmaceutical compounds
PL2057148T3 (pl) 2006-07-31 2010-06-30 Rottapharm Spa Amidynowe pochodne 2-heteroarylochinazolin i chinolin, silne środki przeciwbólowe i środki przeciwzapalne
JP5095736B2 (ja) 2006-08-03 2012-12-12 ロッタファルム・ソシエタ・ペル・アチオニ 6−1h−イミダゾ−キナゾリンおよびキノリン誘導体、新規有効鎮痛剤および抗炎症剤
MX2009002171A (es) 2006-08-30 2009-05-28 Cellzome Ltd Derivados de triazol como inhibidores de cinasas.
US20080234262A1 (en) 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
WO2008118486A1 (en) 2007-03-27 2008-10-02 Sandisk 3D, Llc Memory cell comprising a carbon nanotube fabric element and a steering element and methods of forming the same
PE20090717A1 (es) 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
WO2008152394A1 (en) 2007-06-12 2008-12-18 F.Hoffmann-La Roche Ag Pharmaceutical compounds
ES2401557T3 (es) 2007-08-02 2013-04-22 Amgen, Inc Moduladores de Pl3 cinasas y métodos de uso
EP2217601A1 (en) 2007-11-08 2010-08-18 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyridazines for use as protein kinase inhibitors
WO2009068482A1 (en) 2007-11-27 2009-06-04 Cellzome Limited Amino triazoles as pi3k inhibitors
US8153813B2 (en) 2007-12-20 2012-04-10 Abbott Laboratories Benzothiazole and benzooxazole derivatives and methods of use
CN101981037B (zh) 2008-01-30 2013-09-04 吉宁特有限公司 吡唑并嘧啶pi3k抑制剂化合物及使用方法
US20090192176A1 (en) 2008-01-30 2009-07-30 Wyeth 1H-PYRAZOLO[3,4-D]PYRIMIDINE, PURINE, 7H-PURIN-8(9H)-ONE, 3H-[1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE, AND THIENO[3,2-D]PYRIMIDINE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES
JP2011525535A (ja) * 2008-06-24 2011-09-22 武田薬品工業株式会社 PI3K/mTOR阻害剤
KR20110039558A (ko) * 2008-07-18 2011-04-19 사노피-아벤티스 신규 트리아졸로(4,3-a)피리딘 유도체, 그의 제조 방법, 의약으로서의 그의 용도, 제약 조성물, 및 특히 met 억제제로서의 신규 용도
CA2738429C (en) * 2008-09-26 2016-10-25 Intellikine, Inc. Heterocyclic kinase inhibitors
US8476282B2 (en) 2008-11-03 2013-07-02 Intellikine Llc Benzoxazole kinase inhibitors and methods of use
EP3123864A1 (en) 2008-12-08 2017-02-01 Gilead Connecticut, Inc. Imidazopyrazine syk inhibitors
US8491869B2 (en) 2009-03-23 2013-07-23 Eli Lilly And Company Imaging agents for detecting neurological disorders
JP2012526836A (ja) * 2009-05-13 2012-11-01 アムジエン・インコーポレーテツド Pikk阻害薬としてのヘテロアリール化合物
CN102459248A (zh) * 2009-05-26 2012-05-16 埃克塞里艾克西斯公司 作为PI3K/mTOR抑制剂的苯并氧杂环庚三烯以及它们使用与制造方法
UA111579C2 (uk) 2009-08-17 2016-05-25 Інтеллікіне Ллк ГЕТЕРОЦИКЛІЧНІ ПОХІДНІ 2-АМІНОБЕНЗО[d]ОКСАЗОЛУ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ НА ЇХ ОСНОВІ ТА ЇХ ЗАСТОСУВАННЯ ДЛЯ ЛІКУВАННЯ ЗАХВОРЮВАННЯ, ПОВ'АНОГО З РІ3-КІНАЗОЮ
CN103153062B (zh) 2010-05-24 2015-07-15 因特利凯有限责任公司 杂环化合物及其用途
TWI592411B (zh) 2011-02-23 2017-07-21 英特爾立秦有限責任公司 激酶抑制劑之組合及其用途

Similar Documents

Publication Publication Date Title
JP2014506601A5 (enExample)
JP2013502423A5 (enExample)
JP2012526143A5 (enExample)
Paul et al. Synthesis and in vitro antitumor evaluation of primary amine substituted quinazoline linked benzimidazole
KR101958501B1 (ko) 설폭시민기 함유 4-아릴-n-페닐-1,3,5-트리아진-2-아민
Al-Sanea et al. Sulfonamide-based 4-anilinoquinoline derivatives as novel dual Aurora kinase (AURKA/B) inhibitors: Synthesis, biological evaluation and in silico insights
Ferroni et al. 1, 4-Substituted triazoles as nonsteroidal anti-androgens for prostate cancer treatment
Amin et al. New series of 6-substituted coumarin derivatives as effective factor Xa inhibitors: Synthesis, in vivo antithrombotic evaluation and molecular docking
Li et al. Novel EGFR inhibitors prepared by combination of dithiocarbamic acid esters and 4-anilinoquinazolines
Vasbinder et al. Discovery and optimization of a novel series of potent mutant B-RafV600E selective kinase inhibitors
GEP201706639B (en) Heterocyclic compounds and uses thereof
AU2019372121A1 (en) Heterocyclic compounds as BET inhibitors
Yu et al. Novel 4-anilinoquinazoline derivatives featuring an 1-adamantyl moiety as potent EGFR inhibitors with enhanced activity against NSCLC cell lines
Raghav et al. Acyl hydrazides and triazoles as novel inhibitors of mammalian cathepsin B and cathepsin H
ATE532780T1 (de) Chinoline und ihre therapeutische verwendung
Czako et al. Discovery of IACS-9439, a potent, exquisitely selective, and orally bioavailable inhibitor of CSF1R
Saidahmatov et al. Discovery of Novel 2-Aminopyridine-Based and 2-Aminopyrimidine-Based Derivatives as Potent CDK/HDAC Dual Inhibitors for the Treatment of Refractory Solid Tumors and Hematological Malignancies
Ochiana et al. Repurposing Human PDE 4 Inhibitors for Neglected Tropical Diseases. Evaluation of Analogs of the Human PDE 4 Inhibitor GSK‐256066 as Inhibitors of PDEB 1 of Trypanosoma brucei
Feng et al. Synthesis and biological evaluation of 4-(piperid-3-yl) amino substituted 6-pyridylquinazolines as potent PI3Kδ inhibitors
WO2014086964A1 (en) New derivatives of indole for the treatment of cancer, viral infections and lung diseases
Jawed Ahsan et al. Synthesis of 2, 5-disubstituted-1, 3, 4-oxadiazole analogs as novel anticancer and antimicrobial agents
CA2964696C (en) Fluorinated benzofuranyl-pyrimidine derivatives containing a sulfoximine group
Sun et al. Synthesis and primary anticonvulsant activity evaluation of 6-alkyoxyl-tetrazolo [5, 1-a] phthalazine derivatives
Nilewski et al. 1-Aminomethyl SAR in a novel series of flavagline-inspired eIF4A inhibitors: Effects of amine substitution on cell potency and in vitro PK properties
Bondock et al. Tandem synthesis and computational insights into triazole and pyrazole-based pyridine derivatives targeting EGFR-TK in cancer therapy