JP2014506599A5 - - Google Patents

Download PDF

Info

Publication number
JP2014506599A5
JP2014506599A5 JP2013555571A JP2013555571A JP2014506599A5 JP 2014506599 A5 JP2014506599 A5 JP 2014506599A5 JP 2013555571 A JP2013555571 A JP 2013555571A JP 2013555571 A JP2013555571 A JP 2013555571A JP 2014506599 A5 JP2014506599 A5 JP 2014506599A5
Authority
JP
Japan
Prior art keywords
independently selected
alkyl
substituted
fluorophenyl
pyrazolo
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
JP2013555571A
Other languages
English (en)
Japanese (ja)
Other versions
JP5959541B2 (ja
JP2014506599A (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/US2012/026377 external-priority patent/WO2012116217A1/en
Publication of JP2014506599A publication Critical patent/JP2014506599A/ja
Publication of JP2014506599A5 publication Critical patent/JP2014506599A5/ja
Application granted granted Critical
Publication of JP5959541B2 publication Critical patent/JP5959541B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

JP2013555571A 2011-02-25 2012-02-23 Ｔｒｋ阻害剤としてのピラゾロ［１，５−ａ］ピリジン Expired - Fee Related JP5959541B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161446572P 2011-02-25 2011-02-25
US61/446,572 2011-02-25
PCT/US2012/026377 WO2012116217A1 (en) 2011-02-25 2012-02-23 Compounds and compositions as trk inhibitors

Publications (3)

Publication Number Publication Date
JP2014506599A JP2014506599A (ja) 2014-03-17
JP2014506599A5 true JP2014506599A5 (show.php) 2015-03-19
JP5959541B2 JP5959541B2 (ja) 2016-08-02

Family

ID=45815979

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2013555571A Expired - Fee Related JP5959541B2 (ja) 2011-02-25 2012-02-23 Ｔｒｋ阻害剤としてのピラゾロ［１，５−ａ］ピリジン

Country Status (28)

Country Link
US (1) US9102671B2 (show.php)
EP (1) EP2678338B1 (show.php)
JP (1) JP5959541B2 (show.php)
KR (1) KR20140014184A (show.php)
CN (1) CN103492384B (show.php)
AP (1) AP2013007103A0 (show.php)
AU (1) AU2012220572A1 (show.php)
BR (1) BR112013021638A2 (show.php)
CA (1) CA2828219A1 (show.php)
CL (1) CL2013002430A1 (show.php)
CO (1) CO6751270A2 (show.php)
CR (1) CR20130410A (show.php)
CU (1) CU20130115A7 (show.php)
DO (1) DOP2013000192A (show.php)
EA (1) EA201391230A1 (show.php)
ES (1) ES2551592T3 (show.php)
GE (1) GEP20156285B (show.php)
GT (1) GT201300209A (show.php)
IL (1) IL227987A0 (show.php)
MA (1) MA34969B1 (show.php)
MX (1) MX2013009767A (show.php)
NI (1) NI201300073A (show.php)
PE (1) PE20140378A1 (show.php)
PH (1) PH12013501758A1 (show.php)
SG (1) SG192795A1 (show.php)
TN (1) TN2013000348A1 (show.php)
WO (1) WO2012116217A1 (show.php)
ZA (1) ZA201306221B (show.php)

Families Citing this family (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2350075B1 (en) 2008-09-22 2014-03-05 Array Biopharma, Inc. Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors
KR101853026B1 (ko) 2008-10-22 2018-04-27 어레이 바이오파마 인크. ＴＲＫ 키나아제 억제제로서 치환된 피라졸로［１,５­ａ］ 피리미딘 화합물
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
CN105693720B (zh) 2010-05-20 2019-01-18 阵列生物制药公司 作为trk激酶抑制剂的大环化合物
CA2858958C (en) * 2011-12-12 2016-10-04 Dr. Reddy's Laboratories Ltd. Substituted pyrazolo[1,5-a]pyridine as tropomyosin receptor kinase (trk) inhibitors
WO2015017533A1 (en) 2013-07-30 2015-02-05 Blueprint Medicines Corporation Ntrk2 fusions
DK3087070T3 (en) * 2013-12-26 2017-12-04 Ignyta Inc PYRAZOLO [1,5-A] PYRIDINE DERIVATIVES AND PROCEDURES FOR THEIR USE
MX375372B (es) * 2014-02-05 2025-03-06 VM Oncology LLC COMPOSICIONES DE COMPUESTOS DE MOLÉCULA PEQUEÑA Y USO DE LOS MISMOS COMO INHIBIDORES TrKA.
CN105524058B (zh) * 2014-10-21 2018-03-27 广州艾格生物科技有限公司 吡唑并[1,5‑a]吡啶类化合物及其应用
TWI746426B (zh) 2014-11-16 2021-11-21 美商亞雷生物製藥股份有限公司 (S)-N-(5-((R)-2-(2,5-二氟苯基)-吡咯啶-1-基)-吡唑并[1,5-a]嘧啶-3-基)-3-羥基吡咯啶-1-甲醯胺硫酸氫鹽結晶型
CN104529815B (zh) * 2014-12-04 2016-08-24 宁波欧迅化学新材料技术有限公司 合成2,4-二硝基苯氧胺的方法
MA43943A (fr) * 2015-05-29 2018-12-12 Ignyta Inc Compositions et procédés pour traiter des patients avec des cellules mutantes rtk
KR20180021745A (ko) 2015-06-01 2018-03-05 록쏘 온콜로지, 인코포레이티드 암을 진단하고 치료하는 방법
EP3322706B1 (en) 2015-07-16 2020-11-11 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
TN2018000138A1 (en) 2015-10-26 2019-10-04 Array Biopharma Inc Point mutations in trk inhibitor-resistant cancer and methods relating to the same
HUE068971T2 (hu) 2016-04-04 2025-02-28 Loxo Oncology Inc (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-A]pirimidin-3-il) -3-hidroxipirrolidin-1-karboxamid folyékony készítményei
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
RS65988B1 (sr) 2016-04-04 2024-10-31 Loxo Oncology Inc Postupak lečenja pedijatrijskih karcinoma
SI3458456T1 (sl) 2016-05-18 2021-04-30 Loxo Oncology, Inc. Priprava (S)-N-(5-((R)-2-(2,5-difluorofenil) pirolidin-1-il) pirazolo (1,5-A) pirimidin-3-il)-3-hidroksipirolidin-1-karboksamida
MX383650B (es) 2016-08-01 2025-03-14 Aptinyx Inc Moduladores del receptor nmda espiro-lactam y uso de los mismos.
SG11201900554YA (en) 2016-08-01 2019-02-27 Aptinyx Inc Spiro-lactam nmda modulators and methods of using same
WO2018026763A1 (en) 2016-08-01 2018-02-08 Aptinyx Inc. Spiro-lactam nmda receptor modulators and uses thereof
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
EP3533796B1 (en) 2016-10-28 2021-09-29 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Amino pyrazolopyrimidine compound used as neurotrophic factor tyrosine kinase receptor inhibitor
CN108003161B (zh) * 2016-10-28 2020-10-09 正大天晴药业集团股份有限公司 神经营养因子酪氨酸激酶受体抑制剂
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
CN110267960B (zh) 2017-01-18 2022-04-26 阿雷生物药品公司 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡嗪化合物
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
PL3674307T3 (pl) 2017-08-23 2023-11-27 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Związek makrocykliczny zawierający ugrupowanie aminopirazolu i pirymidyny oraz kompozycja farmaceutyczna i i ch zastosowanie
TWI812649B (zh) 2017-10-10 2023-08-21 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
EP3700576A1 (en) 2017-10-26 2020-09-02 Array Biopharma Inc. Formulations of a macrocyclic trk kinase inhibitor
TW201938169A (zh) 2018-01-18 2019-10-01 美商亞雷生物製藥股份有限公司 作為RET激酶抑制劑之經取代吡唑并[3,4-d]嘧啶化合物
WO2019143994A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
CN111971286B (zh) 2018-01-18 2023-04-14 阿雷生物药品公司 作为RET激酶抑制剂的取代的吡咯并[2,3-d]嘧啶化合物
CA3095366A1 (en) 2018-03-29 2019-10-03 Loxo Oncology, Inc. Treatment of trk-associated cancers
KR102653681B1 (ko) 2018-07-31 2024-04-03 록쏘 온콜로지, 인코포레이티드 (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의분무-건조된 분산물 및 제제
ES2922314T3 (es) 2018-09-10 2022-09-13 Array Biopharma Inc Compuestos heterocíclicos condensados como inhibidores de cinasa RET
CN111171019A (zh) * 2018-11-13 2020-05-19 上海轶诺药业有限公司 一类五元并六元杂环化合物及其作为蛋白受体激酶抑制剂的用途
WO2020131674A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
US20220177477A1 (en) 2019-03-19 2022-06-09 Central China Normal University Pyrazolopyrimidine compound, pharmaceutical composition, and application therefor
KR20210142154A (ko) 2019-03-21 2021-11-24 옹쎄오 암 치료를 위한 키나제 억제제와 조합된 dbait 분자
JP7420403B2 (ja) 2019-05-08 2024-01-23 ティーワイケー メディシンズ インコーポレーテッド キナーゼ阻害剤として使用される化合物およびその応用
CN110804059B (zh) * 2019-09-30 2024-03-12 郑州泰基鸿诺医药股份有限公司 氨基甲酸酯类化合物、药物组合物及其应用
CN110643672A (zh) * 2019-10-15 2020-01-03 西安交通大学 高表达TrkB作为新型靶点在抑制胰腺癌转移方面的医药用途
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
CN112979654B (zh) * 2019-12-16 2024-03-19 赛诺哈勃药业（成都）有限公司 杂芳基稠环化合物、其制备方法及应用
EP4093376A1 (en) * 2020-01-22 2022-11-30 BenevolentAI Bio Limited Pharmaceutical compositions and their uses
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN112779518B (zh) * 2020-12-17 2022-07-22 东北师范大学 一种高发光强度的薄膜、制备方法及其用途
CN112645955B (zh) * 2020-12-24 2022-11-04 四川国康药业有限公司 一种[1,2,4]三唑并[4,3-b]哒嗪类化合物及其制备方法和用途
CN112979646B (zh) * 2021-03-08 2022-01-14 北京富龙康泰生物技术有限公司 一种咪唑并吡啶类衍生物

Family Cites Families (197)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1219606A (en) 1968-07-15 1971-01-20 Rech S Et D Applic Scient Soge Quinuclidinol derivatives and preparation thereof
GB8334494D0 (en) 1983-12-24 1984-02-01 Tanabe Seiyaku Co Carbostyril derivatives
JPS6235216A (ja) 1985-08-09 1987-02-16 Noritoshi Nakabachi 不均質物質層の層厚非破壊測定方法および装置
GB8916480D0 (en) 1989-07-19 1989-09-06 Glaxo Group Ltd Chemical process
GB8923590D0 (en) 1989-10-19 1989-12-06 Pfizer Ltd Antimuscarinic bronchodilators
PT100441A (pt) 1991-05-02 1993-09-30 Smithkline Beecham Corp Pirrolidinonas, seu processo de preparacao, composicoes farmaceuticas que as contem e uso
US5451700A (en) 1991-06-11 1995-09-19 Ciba-Geigy Corporation Amidino compounds, their manufacture and methods of treatment
WO1993018007A1 (fr) 1992-03-13 1993-09-16 Tokyo Tanabe Company Limited Nouveau derive de carbostyrile
SK279958B6 (sk) 1992-04-02 1999-06-11 Smithkline Beecham Corporation Zlúčeniny s protialergickým a protizápalovým účink
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
GB9301000D0 (en) 1993-01-20 1993-03-10 Glaxo Group Ltd Chemical compounds
GB9414208D0 (en) 1994-07-14 1994-08-31 Glaxo Group Ltd Compounds
GB9414193D0 (en) 1994-07-14 1994-08-31 Glaxo Group Ltd Compounds
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
AU9281298A (en) 1997-10-01 1999-04-23 Kyowa Hakko Kogyo Co. Ltd. Benzodioxole derivatives
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
GB9723566D0 (en) 1997-11-08 1998-01-07 Glaxo Group Ltd Chemical compounds
YU44900A (sh) 1998-01-31 2003-01-31 Glaxo Group Limited Derivati 2-(purin-9-il)tetrahidrofuran-3,4-diola
CO4990969A1 (es) 1998-02-14 2000-12-26 Glaxo Group Ltd Derivados de 2-(purin-9-il)-tetrahidrofuran-3,4-diol
US6541669B1 (en) 1998-06-08 2003-04-01 Theravance, Inc. β2-adrenergic receptor agonists
GB9813535D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
GB9813540D0 (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
DE69910213T2 (de) 1998-06-23 2004-07-01 Glaxo Group Ltd., Greenford 2-(purin-9-yl)-tetrahydrofuran-3,4-diol derivate
BR9815931A (pt) 1998-06-30 2001-02-20 Dow Chemical Co Polióis poliméricos, um processo para sua produção, e espuma de poliuretanoobtida
ATE331726T1 (de) 1998-10-16 2006-07-15 Pfizer Adenine-derivate
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
YU25500A (sh) 1999-05-11 2003-08-29 Pfizer Products Inc. Postupak za sintezu analoga nukleozida
US6683115B2 (en) 1999-06-02 2004-01-27 Theravance, Inc. β2-adrenergic receptor agonists
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.
HU229439B1 (hu) 1999-08-21 2013-12-30 Takeda Gmbh Roflumilast és salmeterol szinergetikus kombinációja
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
GB9924361D0 (en) 1999-10-14 1999-12-15 Pfizer Ltd Purine derivatives
GB9924363D0 (en) 1999-10-14 1999-12-15 Pfizer Central Res Purine derivatives
OA11558A (en) 1999-12-08 2004-06-03 Advanced Medicine Inc Beta 2-adrenergic receptor agonists.
GB0003960D0 (en) 2000-02-18 2000-04-12 Pfizer Ltd Purine derivatives
PL362868A1 (en) 2000-04-27 2004-11-02 Boehringer Ingelheim Pharma Gmbh & Co.Kg Novel, slow-acting betamimetics, a method for their production and their use as medicaments
TWI227240B (en) 2000-06-06 2005-02-01 Pfizer 2-aminocarbonyl-9H-purine derivatives
IL153707A0 (en) 2000-06-27 2003-07-06 S A L V A T Lab Sa Carbamates derived from arylalkylamines
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
JP2002114788A (ja) * 2000-08-03 2002-04-16 Banyu Pharmaceut Co Ltd カルバペネム誘導体の製造方法及び合成中間体
CZ304043B6 (cs) 2000-08-05 2013-09-04 Glaxo Group Limited Estery steroidních thiokyselin
GB0022695D0 (en) 2000-09-15 2000-11-01 Pfizer Ltd Purine Derivatives
GB0028383D0 (en) 2000-11-21 2001-01-03 Novartis Ag Organic compounds
AU2002228015B2 (en) 2000-12-22 2007-08-23 Almirall, S.A. Quinuclidine carbamate derivatives and their use as M3 antagonists
CA2433128C (en) 2000-12-28 2010-05-25 Almirall Prodesfarma Ag Novel quinuclidine derivatives and medicinal compositions containing the same
GB0103630D0 (en) 2001-02-14 2001-03-28 Glaxo Group Ltd Chemical compounds
ATE365720T1 (de) 2001-03-08 2007-07-15 Glaxo Group Ltd Agonisten von beta-adrenorezeptoren
EP1241176A1 (en) 2001-03-16 2002-09-18 Pfizer Products Inc. Purine derivatives for the treatment of ischemia
WO2002076933A1 (en) 2001-03-22 2002-10-03 Glaxo Group Limited Formailide derivatives as beta2-adrenoreceptor agonists
US7291608B2 (en) 2001-04-30 2007-11-06 Glaxo Group Limited Anti-inflammatory 17.β.-carbothioate ester derivatives of androstane with a cyclic ester group in position 17.α
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
ES2307751T3 (es) 2001-06-12 2008-12-01 Glaxo Group Limited Nuevos esteres heterociclicos centi-inflamatorios 17 alfa de derivados 17 beta de carbotioato de androstano.
DK2327765T3 (en) 2001-06-21 2015-07-13 Basf Enzymes Llc nitrilases
BRPI0212455B8 (pt) 2001-09-14 2021-05-25 Glaxo Group Ltd composto derivado de fenetanolamina para o tratamento de doenças respiratórias, formulação farmacêutica, combinação, e, uso do mesmo
HUP0401849A3 (en) 2001-10-17 2007-05-02 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
PT1444233E (pt) 2001-11-09 2011-09-29 Gilead Palo Alto Inc Antagonistas de receptor de adenosina a2b
US6653323B2 (en) 2001-11-13 2003-11-25 Theravance, Inc. Aryl aniline β2 adrenergic receptor agonists
TWI249515B (en) 2001-11-13 2006-02-21 Theravance Inc Aryl aniline beta2 adrenergic receptor agonists
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
EA006505B1 (ru) 2001-12-20 2005-12-29 Лабораториос С.А.Л.В.А.Т.,С.А. Производные карбамата 1-алкил-1-азониабицикло[2.2.2]октана и их применение в качестве антагонистов мускаринового рецептора
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
AU2003201693A1 (en) 2002-01-21 2003-09-02 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
GB0204719D0 (en) 2002-02-28 2002-04-17 Glaxo Group Ltd Medicinal compounds
EA008830B1 (ru) 2002-03-26 2007-08-31 Бёрингер Ингельхайм Фармасьютиклз, Инк. Миметики глюкокортикоидов, способы их получения, фармацевтические композиции и их применение
WO2003082787A1 (en) 2002-03-26 2003-10-09 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
WO2003086408A1 (en) 2002-04-10 2003-10-23 University Of Virginia Patent Foundation Use of a2a adenosine receptor agonists for the treatment of inflammatory diseases
ATE496620T1 (de) 2002-04-11 2011-02-15 Merck Sharp & Dohme 1h-benzo(f)indazol-5-yl-derivate als selektive glucocorticoid-rezeptor-modulatoren
ES2206021B1 (es) 2002-04-16 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de pirrolidinio.
EP1497261B1 (en) 2002-04-25 2007-12-19 Glaxo Group Limited Phenethanolamine derivatives
JP2005527618A (ja) 2002-05-28 2005-09-15 セラヴァンス インコーポレーテッド アルコキシアリールβ２アドレナリン作動性レセプターアゴニスト
US7186864B2 (en) 2002-05-29 2007-03-06 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
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
WO2004000814A1 (en) 2002-06-25 2003-12-31 Merck Frosst Canada & Co. 8-(biaryl) quinoline pde4 inhibitors
US20060004056A1 (en) 2002-07-02 2006-01-05 Bernard Cote Di-aryl-substituted-ethan pyridone pde4 inhibitors
ES2204295B1 (es) 2002-07-02 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de quinuclidina-amida.
DK1521733T3 (da) 2002-07-08 2014-10-13 Pfizer Prod Inc Modulatorer af glucocorticoid receptoren
GB0217225D0 (en) 2002-07-25 2002-09-04 Glaxo Group Ltd Medicinal compounds
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
WO2004018457A1 (en) 2002-08-10 2004-03-04 Altana Pharma Ag Pyrrolidinedione substituted piperidine-phthalazones as pde4 inhibitors
AU2003260371A1 (en) 2002-08-10 2004-03-11 Altana Pharma Ag Piperidine-n-oxide-derivatives
JP2005538138A (ja) 2002-08-10 2005-12-15 アルタナ　ファルマ　アクチエンゲゼルシャフト Ｐｄｅ４インヒビターとしてのピリダジノン誘導体
AU2003255376A1 (en) 2002-08-10 2004-03-11 Altana Pharma Ag Piperidine-derivatives as pde4 inhibitors
WO2004018431A2 (en) 2002-08-17 2004-03-04 Altana Pharma Ag Novel phenanthridines
JP2005537313A (ja) 2002-08-17 2005-12-08 アルタナ　ファルマ　アクチエンゲゼルシャフト 新規のベンゾナフチリジン
CA2496175A1 (en) 2002-08-21 2004-03-04 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted hihydroquinolines as glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE60231341D1 (de) 2002-08-23 2009-04-09 Ranbaxy Lab Ltd Fluor- und sulfonylaminohaltige, 3,6-disubstituierptorantagonisten
NZ538932A (en) 2002-08-29 2007-04-27 Boehringer Ingelheim Pharma 3-(sulfonamidoethyl)-indole derivatives for use as glucocorticoid mimetics in the treatment of inflammatory, allergic and proliferative disease
ES2281658T3 (es) 2002-08-29 2007-10-01 Nycomed Gmbh 3-hidroxi-6-fenilfenantridinas como inhibidores de pde-4.
WO2004019944A1 (en) 2002-08-29 2004-03-11 Altana Pharma Ag 2-hydroxy-6-phenylphenanthridines as pde-4 inhibitors
GB0220730D0 (en) 2002-09-06 2002-10-16 Glaxo Group Ltd Medicinal compounds
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
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
CA2499150A1 (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
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
BR0315234A (pt) 2002-10-11 2005-08-23 Pfizer Derivados de indol como agonistas beta-2
EP1440966A1 (en) 2003-01-10 2004-07-28 Pfizer Limited Indole derivatives useful for the treatment of diseases
WO2004037807A2 (en) 2002-10-22 2004-05-06 Glaxo Group Limited Medicinal arylethanolamine compounds
DE60317918T2 (de) 2002-10-23 2009-01-29 Glenmark Pharmaceuticals Ltd. Tricyclische verbindungen zur behandlung von entzündlichen und allergischen erkrankungen verfahren zu deren herstellung und sie enthaltende pharmazeutische zusammensetzungen
GB0225030D0 (en) 2002-10-28 2002-12-04 Glaxo Group Ltd Medicinal compounds
NZ539676A (en) 2002-10-28 2006-10-27 Glaxo Group Ltd Phenethanolamine derivative for the treatment of respiratory diseases
GB0225287D0 (en) 2002-10-30 2002-12-11 Glaxo Group Ltd Novel 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
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
DE10253282A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Arzneimittel zur Behandlung von chronisch obstruktiver Lungenerkrankung
DE10261874A1 (de) 2002-12-20 2004-07-08 Schering Ag Nichtsteroidale Entzündungshemmer
RU2328499C2 (ru) 2003-01-09 2008-07-10 Астеллас Фарма Инк. Производные пирролопиридазина, фармацевтическая композиция, способ профилактики или лечения заболеваний, применение в качестве ингибитора фосфодиэстеразы iv, и/или продуцирования tnf
WO2004066920A2 (en) 2003-01-21 2004-08-12 Merck & Co. Inc. 17-carbamoyloxy cortisol derivatives as selective glucocorticoid receptor modulators
PE20040950A1 (es) 2003-02-14 2005-01-01 Theravance Inc DERIVADOS DE BIFENILO COMO AGONISTAS DE LOS RECEPTORES ADRENERGICOS ß2 Y COMO ANTAGONISTAS DE LOS RECEPTORES MUSCARINICOS
JP2007524596A (ja) 2003-02-28 2007-08-30 トランスフォーム・ファーマシューティカルズ・インコーポレイテッド 共結晶医薬組成物
EP1460064A1 (en) 2003-03-14 2004-09-22 Pfizer Limited Indole-2-carboxamide derivatives useful as beta-2 agonists
JP4767842B2 (ja) 2003-04-01 2011-09-07 セラヴァンス， インコーポレーテッド β２アドレナリン作用性レセプターアゴニスト活性およびムスカリン性レセプターアンタゴニスト活性を有するジアリールメチル化合物および関連化合物
AU2004226824B2 (en) 2003-04-04 2008-05-01 Novartis Ag Quinoline-2-one-derivatives for the treatment of airways diseases
AR044134A1 (es) 2003-05-02 2005-08-24 Novartis Ag Derivados de quinuclidina, metodo de preparacion y composiciones farmaceuticas.
US7268147B2 (en) 2003-05-15 2007-09-11 Pfizer Inc Compounds useful for the treatment of diseases
EP1477167A1 (en) 2003-05-15 2004-11-17 Pfizer Limited [(2-hydroxy-2-(4-hydroxy-3-hydroxymethylphenyl)-ethylamino)-propyl] phenyl derivatives as beta2 agonists
TWI328009B (en) 2003-05-21 2010-08-01 Glaxo Group Ltd Quinoline derivatives as phosphodiesterase inhibitors
US7358244B2 (en) 2003-05-28 2008-04-15 Theravance, Inc. Azabicycloalkane compounds
ATE384697T1 (de) 2003-06-04 2008-02-15 Pfizer 2-amino-pyridin-derivate als beta-2 adrenoreceptor agonisten
GB0312832D0 (en) 2003-06-04 2003-07-09 Pfizer Ltd 2-amino-pyridine derivatives useful for the treatment of diseases
AU2004245146B2 (en) 2003-06-11 2010-01-21 Merck Frosst Canada Ltd 7-(1,3-thiazol-2-yl)thio-coumarin derivatives and their use as leukotriene biosynthesis inhibitors
WO2004111044A1 (en) 2003-06-17 2004-12-23 Glenmark Pharmaceuticals Ltd. Tricyclic compounds useful for the treatment of inflammatory and allergic disorders:process for their preparation
GB0316290D0 (en) 2003-07-11 2003-08-13 Glaxo Group Ltd Novel compounds
ITMI20031451A1 (it) 2003-07-16 2005-01-17 Zambon Spa Derivati diidro-ftalazinici inibitori della fosfodiesterasi 4
JP2007500685A (ja) 2003-07-31 2007-01-18 アルタナ　ファルマ　アクチエンゲゼルシャフト 新規の６−フェニルフェナントリジン
CA2533636A1 (en) 2003-07-31 2005-02-10 Altana Pharma Ag Novel 6-phenylphenanthridines
ES2319429T3 (es) * 2003-08-15 2009-05-07 MERCK & CO., INC. Inhibidores de cinesina mitotica.
GB0322722D0 (en) 2003-09-27 2003-10-29 Glaxo Group Ltd Compounds
GB0322726D0 (en) 2003-09-27 2003-10-29 Glaxo Group Ltd Compounds
WO2005033121A2 (en) 2003-10-03 2005-04-14 King Pharmaceuticals Research & Development, Inc. Synthesis of 2-aralkyloxyadenosines, 2-alkoxyadenosines, and their analogs
GB0323701D0 (en) 2003-10-09 2003-11-12 Glaxo Group Ltd Formulations
GB0324654D0 (en) 2003-10-22 2003-11-26 Glaxo Group Ltd Medicinal compounds
GB0324886D0 (en) 2003-10-24 2003-11-26 Glaxo Group Ltd Medicinal compounds
GB0329182D0 (en) 2003-12-17 2004-01-21 Glaxo Group Ltd Chemical compounds
US8025794B2 (en) 2003-12-19 2011-09-27 Shell Oil Company Systems, methods, and catalysts for producing a crude product
JP2005187357A (ja) 2003-12-25 2005-07-14 Nippon Suisan Kaisha Ltd 選択的なβ２受容体アゴニスト活性を有するベンゾチアゾロン誘導体の製造方法
DE102004001413A1 (de) 2004-01-09 2005-08-18 Boehringer Ingelheim Pharma Gmbh & Co. Kg 3-Hydroxymethyl-4-Hydroxy-Phenyl-Derivate zur Behandlung von chronisch obstruktiver Lungenerkrankung
TW200531692A (en) 2004-01-12 2005-10-01 Theravance Inc Aryl aniline derivatives as β2 adrenergic receptor agonists
PT1708992E (pt) 2004-01-22 2007-11-16 Pfizer Derivados de sulfonamida para o tratamento de doenças
NZ548318A (en) 2004-01-22 2009-03-31 Pfizer Sulfonamide derivatives for the treatment of diseases
DE102004003428A1 (de) 2004-01-23 2005-08-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue langwirksame Beta-2-Agonisten, und deren Verwendung als Arzneimittel
GB0402797D0 (en) 2004-02-09 2004-03-10 Novartis Ag Organic compounds
WO2005080375A1 (en) 2004-02-13 2005-09-01 Theravance, Inc. Crystalline form of a biphenyl compound
ES2349470T3 (es) 2004-02-14 2011-01-03 Boehringer Ingelheim International Gmbh Nuevos beta-2-agonistas de acción de larga duración y su utilización como medicamentos.
JP2007527900A (ja) 2004-03-10 2007-10-04 アルタナ　ファルマ　アクチエンゲゼルシャフト チオ含有の新規のヒドロキシ−６−フェニルフェナントリジン及びｐｄｅ４インヒビターとしてのそれらの使用
EP1725534A1 (en) 2004-03-10 2006-11-29 Altana Pharma AG Novel amido-substituted hydroxy-6-phenylphenanthridines and their use as pde4 inhibitors
EP1574501A1 (en) 2004-03-11 2005-09-14 Pfizer Limited Quinolinone derivatives, pharmaceutical compositions containing them and their use
WO2005087749A1 (ja) 2004-03-15 2005-09-22 Kyowa Hakko Kogyo Co., Ltd. ２−アミノキナゾリン誘導体
US7244728B2 (en) 2004-03-17 2007-07-17 Boehringer Ingelheim International Gmbh Long acting betamimetics for the treatment of respiratory diseases
EP1577292A1 (en) 2004-03-17 2005-09-21 Pfizer Limited Phenylaminoethanol derivatives as beta2 receptor agonists
EA200601510A1 (ru) 2004-03-17 2007-04-27 Пфайзер Инк. Производные фенилэтаноламина в качестве бета-2-агонистов
WO2005090345A1 (en) 2004-03-17 2005-09-29 Altana Pharma Ag Novel n- (alkoxyalkyl) carbamoyl - substituted 6-phenyl-benzonaphthyridine derivatives and their use as pde3/4 inhibitors
US20050215542A1 (en) 2004-03-23 2005-09-29 Pfizer Inc Compounds for the treatment of diseases
EP1730141B1 (en) 2004-03-23 2009-05-27 Pfizer Limited Compounds for the treatment of diseases
AP2315A (en) 2004-03-23 2011-11-04 Pfizer Formamide derivatives useful as adrenoceptor.
WO2005092860A1 (en) 2004-03-23 2005-10-06 Pfizer Limited Compounds for the treatment of diseases
EP1730104A1 (en) 2004-04-02 2006-12-13 Glaxo Group Limited Chemical process and new crystalline form
DE102004019539A1 (de) 2004-04-22 2005-11-10 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Arzneimittel zur Behandlung von Atemwegserkrankungen
US20050239778A1 (en) 2004-04-22 2005-10-27 Boehringer Ingelheim International Gmbh Novel medicament combinations for the treatment of respiratory diseases
US7307076B2 (en) 2004-05-13 2007-12-11 Boehringer Ingelheim International Gmbh Beta agonists for the treatment of respiratory diseases
US7745621B2 (en) 2004-05-14 2010-06-29 Boehringer Ingelheim International Gmbh Long acting bronchodilators for the treatment of respiratory diseases
US20050256115A1 (en) 2004-05-14 2005-11-17 Boehringer Ingelheim International Gmbh Aerosol formulation for the inhalation of beta-agonists
PE20060426A1 (es) * 2004-06-02 2006-06-28 Schering Corp DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa
RU2006146042A (ru) 2004-06-03 2008-07-20 Тереванс Диаминные агонисты 2-адренергических рецепторов
US7317023B2 (en) 2004-07-21 2008-01-08 Theravance, Inc. Diaryl ether β2 adrenergic receptor agonists
GB0416397D0 (en) 2004-07-22 2004-08-25 Glaxo Group Ltd Pharmaceutical formulations
US7569586B2 (en) 2004-08-16 2009-08-04 Theravance, Inc. Compounds having β2 adrenergic receptor agonist and muscarinic receptor antagonist activity
US7838597B2 (en) 2004-08-20 2010-11-23 Sekisui Specialty Chemicals America, Llc Fluid loss concentrate for hydraulic cement
EP1786762A2 (en) 2004-09-10 2007-05-23 Theravance, Inc. Amidine substituted aryl aniline compounds
GB0424284D0 (en) 2004-11-02 2004-12-01 Novartis Ag Organic compounds
GB0426164D0 (en) 2004-11-29 2004-12-29 Novartis Ag Organic compounds
CN101137625A (zh) 2005-01-11 2008-03-05 葛兰素集团有限公司 β2肾上腺素能激动剂的肉桂酸盐
WO2006124447A2 (en) * 2005-05-13 2006-11-23 Eli Lilly And Company Substituted n-arylpyrrolidines as selective androgen receptor modulators
US8304547B2 (en) * 2007-10-24 2012-11-06 Astellas Pharma Inc. Azolecarboxamide compound or salt thereof
BRPI0912668A2 (pt) * 2008-05-13 2016-01-26 Irm Llc composto e composições como inibidores de quinase
ES2612731T3 (es) * 2008-08-19 2017-05-18 Janssen Pharmaceutica Nv Antagonistas de receptores al frío de mentol
KR101853026B1 (ko) 2008-10-22 2018-04-27 어레이 바이오파마 인크. ＴＲＫ 키나아제 억제제로서 치환된 피라졸로［１,５­ａ］ 피리미딘 화합물
TW201022233A (en) * 2008-11-04 2010-06-16 Organon Nv (Pyrrolidin-2-yl)phenyl derivatives
US8927545B2 (en) * 2009-03-30 2015-01-06 Duke University Inhibiting Eph B-3 kinase
AR077468A1 (es) * 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
UY33597A (es) 2010-09-09 2012-04-30 Irm Llc Compuestos y composiciones como inhibidores de la trk

Similar Documents

Publication Publication Date Title
JP2014506599A5 (show.php)
AU2019283921B2 (en) Indole carboxamide compounds useful as kinase inhibitors
KR102588955B1 (ko) 이환식 화합물 및 암의 치료에서의 이의 용도
JP6013375B2 (ja) キナーゼ阻害剤としてのチアゾリルフェニル−ベンゼンスルホンアミド誘導体
CN107922431B (zh) Hpk1抑制剂及其使用方法
CA2971872C (en) Mutant idh1 inhibitors useful for treating cancer
JP2019536785A5 (show.php)
AU2019293235B2 (en) Immunomodulatory compounds
CA3208313A1 (en) Isoindolinone compounds
JP7175888B2 (ja) 選択的ｈｄａｃ１、２阻害剤としてのピペラジン誘導体
JP6964576B2 (ja) 置換４−アザインドール及びｇｌｕｎ２ｂ受容体調節因子としてのそれらの使用
KR20130129244A (ko) 치환된 6,6-융합된 질소 헤테로환형 화합물 및 이의 용도
JP2016513660A5 (show.php)
KR102493943B1 (ko) 포유류 티로신 키나제 ROR1 활성의 저해제로서 유용한 2-페닐-3H-이미다조[4,5-b]피리딘 유도체
AU2014234909B2 (en) Acyclic cyanoethylpyrazolo pyridones as Janus kinase inhibitors
JP2008528467A5 (show.php)
JP2016516043A5 (show.php)
JP2009529047A5 (show.php)
JP2012511588A5 (show.php)
JP2020517595A (ja) サイクリン依存性キナーゼｃｄｋ９の新規阻害剤
JP2016540803A5 (show.php)
JP2012522766A5 (show.php)
JP2015502371A5 (show.php)
CA3172589A1 (en) Piperidine-2,6-diones as small molecule degraders of helios and methods of use
JP2015500856A5 (show.php)