CN107074852B - ROR-γ的二氢吡咯并吡啶抑制剂 - Google Patents

ROR-γ的二氢吡咯并吡啶抑制剂 Download PDF

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CN107074852B
CN107074852B CN201580056193.5A CN201580056193A CN107074852B CN 107074852 B CN107074852 B CN 107074852B CN 201580056193 A CN201580056193 A CN 201580056193A CN 107074852 B CN107074852 B CN 107074852B
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mixture
tert
mmol
compound
pharmaceutically acceptable
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CN107074852A (zh
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大卫·A·克莱蒙
劳伦斯·韦恩·迪拉德
董成国
范怡
贾兰齐
斯蒂芬·D·罗特斯塔
安德鲁·马库斯
苏雷什·B·辛格
科林·M·泰斯
苑晶
赵伟
郑亚军
庄凌航
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Life Medicine Co Ltd
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    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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CN201580056193.5A 2014-10-14 2015-10-14 ROR-γ的二氢吡咯并吡啶抑制剂 Expired - Fee Related CN107074852B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201462063912P 2014-10-14 2014-10-14
US62/063,912 2014-10-14
US201462074406P 2014-11-03 2014-11-03
US62/074,406 2014-11-03
PCT/US2015/055420 WO2016061160A1 (en) 2014-10-14 2015-10-14 Dihydropyrrolopyridine inhibitors of ror-gamma

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CN107074852A CN107074852A (zh) 2017-08-18
CN107074852B true CN107074852B (zh) 2019-08-16

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US (3) US9796710B2 (enExample)
EP (1) EP3207043B3 (enExample)
JP (1) JP6564029B2 (enExample)
KR (1) KR20170066628A (enExample)
CN (1) CN107074852B (enExample)
AU (1) AU2015333610B2 (enExample)
BR (1) BR112017007460A2 (enExample)
CA (1) CA2963140A1 (enExample)
CL (1) CL2017000902A1 (enExample)
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Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI633087B (zh) 2012-06-13 2018-08-21 赫孚孟拉羅股份公司 新穎二氮雜螺環烷及氮雜螺環烷
RS59512B1 (sr) 2012-09-25 2019-12-31 Hoffmann La Roche Derivati heksahidropirolo[3,4−c]pirola i srodna jedinjenja kao inhibitori autotaksina (atx) i kao inhibitori proizvodnje lizofosfatidne kiseline (lpa) za lečenje npr. bubrežnih bolesti
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
WO2015078803A1 (en) 2013-11-26 2015-06-04 F. Hoffmann-La Roche Ag NEW OCTAHYDRO-CYCLOBUTA [1,2-c;3,4-c']DIPYRROL-2-YL
RS59007B1 (sr) 2014-02-03 2019-08-30 Vitae Pharmaceuticals Llc Dihidropirolopiridinski inhibitori ror-gama
CN106103446B (zh) 2014-03-26 2019-07-30 豪夫迈·罗氏有限公司 作为自分泌运动因子(atx)和溶血磷脂酸(lpa)生产抑制剂的二环化合物
KR20160128428A (ko) 2014-03-26 2016-11-07 에프. 호프만-라 로슈 아게 오토탁신(atx) 및 리소포스파티드산(lpa) 생성 억제제로서의 축합형 [1,4]다이아제핀 화합물
EA031967B1 (ru) 2014-10-14 2019-03-29 Вайтаи Фармасьютиклз, Инк. ДИГИДРОПИРРОЛОПИРИДИНОВЫЕ ИНГИБИТОРЫ ROR-γ
US9663515B2 (en) * 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
MX394388B (es) 2015-05-15 2025-03-21 Aurigene Discovery Tech Ltd Compuestos de tetrahidroquinolinona sustituidos como moduladores de ror gamma
US10106501B2 (en) 2015-06-09 2018-10-23 Abbvie Inc. Nuclear receptor modulators
WO2017024018A1 (en) 2015-08-05 2017-02-09 Vitae Pharmaceuticals, Inc. Modulators of ror-gamma
CN108026077B (zh) 2015-09-04 2021-11-05 豪夫迈·罗氏有限公司 苯氧基甲基衍生物
KR20180054635A (ko) 2015-09-24 2018-05-24 에프. 호프만-라 로슈 아게 오토탁신(atx) 억제제로서 이환형 화합물
CR20180143A (es) 2015-09-24 2018-05-03 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores duales de atx/ca
EP3353178B1 (en) 2015-09-24 2021-07-14 F. Hoffmann-La Roche AG Bicyclic compounds as dual atx/ca inhibitors
PE20180461A1 (es) 2015-09-24 2018-03-06 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores de la atx
KR20180086221A (ko) 2015-11-20 2018-07-30 비타이 파마슈티컬즈, 인코포레이티드 Ror-감마의 조절물질
CN109071516B (zh) 2015-12-15 2021-08-31 阿斯利康(瑞典)有限公司 新颖的化合物
TW202220968A (zh) 2016-01-29 2022-06-01 美商維它藥物有限責任公司 ROR-γ調節劑
JP2020059651A (ja) * 2016-12-26 2020-04-16 科研製薬株式会社 ピラゾール誘導体及びそれを含有する医薬
RU2019132254A (ru) 2017-03-16 2021-04-16 Ф. Хоффманн-Ля Рош Аг Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca
CN110382484B (zh) 2017-03-16 2022-12-06 豪夫迈·罗氏有限公司 新的作为atx抑制剂的二环化合物
WO2018229155A1 (en) 2017-06-14 2018-12-20 Astrazeneca Ab 2,3-dihydroisoindole-1-carboxamides useful as ror-gamma modulators
JP2020142989A (ja) * 2017-06-21 2020-09-10 Meiji Seikaファルマ株式会社 イミダゾール誘導体及びそれを含有する医薬
CN109952298B (zh) 2017-07-06 2021-09-03 江苏恒瑞医药股份有限公司 吲哚甲酰胺类衍生物、其制备方法及其在医药上的应用
WO2019018975A1 (en) * 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
MA49685A (fr) 2017-07-24 2021-04-14 Vitae Pharmaceuticals Llc INHIBITEURS DE ROR gamma
US11466024B2 (en) 2017-08-01 2022-10-11 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Bicylic compound acting as an inhibitor
CN109384711A (zh) * 2017-08-07 2019-02-26 南京柯菲平盛辉制药有限公司 一类茚满-5-甲酰胺RORγ调节剂及其用途
EP3689860A4 (en) 2017-09-30 2021-06-02 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. SULFONYL-SUBSTITUTED BICYCLIC COMPOUNDS AS ROR INHIBITOR
WO2020172467A1 (en) * 2019-02-20 2020-08-27 The Regents Of The University Of California Treatment for retinoic acid receptor-related orphan receptor ɣ (rorɣ)-dependent cancers
WO2023232870A1 (en) 2022-05-31 2023-12-07 Immunic Ag Rorg/rorgt modulators for the treatment of virus infections like covid-19

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013019682A1 (en) * 2011-07-29 2013-02-07 Tempero Pharmaceuticals, Inc. Compounds and methods
WO2014026327A1 (en) * 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 4-heteroaryl substituted benzoic acid compounds as rorgammat inhibitors and uses thereof
CN104024239A (zh) * 2011-12-22 2014-09-03 弗·哈夫曼-拉罗切有限公司 作为RORc调节剂的苄基磺酰胺衍生物

Family Cites Families (212)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE128129T1 (de) 1986-07-28 1995-10-15 American Cyanamid Co 5(und/oder6) substituierte 2-(2-imidazolin-2- yl)nicotinsäuren, ester und salze, verwendbar als herbizide mittel und zwischenverbindungen für die herstellung dieser nikotinsäuren, ester und salze.
FR2624698A1 (fr) 1987-12-18 1989-06-23 Bernard Lyon I Universite Clau Derives heterocycliques de n-carbamoyl-, n-thiocarbamoyl- ou n-amidino-aminomalonyl ou aminosuccinyl amides utiles comme agents edulcorants
WO1990009787A1 (en) 1989-02-27 1990-09-07 The Du Pont Merck Pharmaceutical Company Novel sulfonamides as radiosensitizers
US5776963A (en) 1989-05-19 1998-07-07 Hoechst Marion Roussel, Inc. 3-(heteroaryl)-1- (2,3-dihydro-1h-isoindol-2-yl)alkyl!pyrrolidines and 3-(heteroaryl)-1- (2,3-dihydro-1h-indol-1-yl)alkyl!pyrrolidines and related compounds and their therapeutic untility
GB8927872D0 (en) 1989-12-08 1990-02-14 Beecham Group Plc Pharmaceuticals
JP2807577B2 (ja) 1990-06-15 1998-10-08 エーザイ株式会社 環状アミド誘導体
EP0520573A1 (en) 1991-06-27 1992-12-30 Glaxo Inc. Cyclic imide derivatives
DE4121214A1 (de) 1991-06-27 1993-01-14 Bayer Ag 7-azaisoindolinyl-chinolon- und -naphthyridoncarbonsaeure-derivate
US5378620A (en) 1991-08-30 1995-01-03 Beckman Instruments, Inc. Streptolysin O derivatives
US5272158A (en) 1991-10-29 1993-12-21 Merck & Co., Inc. Fibrinogen receptor antagonists
US5389631A (en) 1991-10-29 1995-02-14 Merck & Co., Inc. Fibrinogen receptor antagonists
US5416099A (en) 1991-10-29 1995-05-16 Merck & Co., Inc. Fibrinogen receptor antagonists
US5238950A (en) 1991-12-17 1993-08-24 Schering Corporation Inhibitors of platelet-derived growth factor
US5364869A (en) 1992-03-09 1994-11-15 Abbott Laboratories Heterocycle-substituted benzyaminopyridine angiotensin II receptor antagonists
US5326760A (en) 1992-06-29 1994-07-05 Glaxo, Inc. Aminobutanoic acid compounds having metalloprotease inhibiting properties
JPH06236056A (ja) 1993-02-10 1994-08-23 Fuji Xerox Co Ltd 電子写真感光体
JP3760474B2 (ja) 1993-04-22 2006-03-29 ダイキン工業株式会社 電気エネルギーを発生させる方法、装置およびそれに用いるn−f結合を有する化合物
CA2134192A1 (en) 1993-11-12 1995-05-13 Michael L. Denney 5, 6-bicyclic glycoprotein iib/iiia antagonists
DE4343922A1 (de) 1993-12-22 1995-06-29 Basf Ag Pyridin-2,3-dicarbonsäureimide, Verfahren zu ihrer Herstellung und ihre Verwendung zur Bekämpfung unerwünschten Pflanzenwuchses
KR970007419B1 (ko) 1993-12-30 1997-05-08 한솔제지 주식회사 승화형 열전사 기록용 색소
FR2725946A1 (fr) 1994-10-24 1996-04-26 Lohr Ind Cale a rapporter sur un plan porteur presentant des perforations
US5719144A (en) 1995-02-22 1998-02-17 Merck & Co., Inc. Fibrinogen receptor antagonists
US5770590A (en) 1995-03-24 1998-06-23 Takeda Chemical Industries, Ltd. Cyclic compounds, their prudiction and use
NO309272B1 (no) 1995-03-24 2001-01-08 Takeda Chemical Industries Ltd Cykliske forbindelser, preparater inneholdende forbindelsene samt mellomprodukter for fremstilling av forbindelsene
DE19608791A1 (de) 1996-03-07 1997-09-11 Hoechst Ag Verfahren zur Herstellung von fluorierten Aromaten und fluorierten stickstoffhaltigen Heteroaromaten
DE19702282C2 (de) 1997-01-23 1998-11-19 Hoechst Ag Katalysator für Halex-Reaktionen
AU6290998A (en) 1997-03-07 1998-09-29 Novo Nordisk A/S 4,5,6,7-tetrahydro-thieno{3,2-c}pyridine derivatives, their preparation and use
US6177443B1 (en) 1997-03-07 2001-01-23 Novo Nordisk A/S 4,5,6,7-tetrahydro-thieno[3, 2-C]pyridine derivatives, their preparation and use
KR19980074060A (ko) 1997-03-21 1998-11-05 김윤배 신규한 치환된 3,4-디알콕시페닐 유도체
JPH1143489A (ja) 1997-05-30 1999-02-16 Takeda Chem Ind Ltd ヘテロ環化合物、その製造法および剤
JPH11143489A (ja) 1997-11-10 1999-05-28 Sony Corp 音声操作機能付き電子機器、電子機器における音声操作方法、及び音声操作機能付き電子機器を備える自動車
BR9908895A (pt) 1998-03-19 2000-12-05 Takeda Chemical Industries Ltd Composição farmacêutica, composto, pró-medicamento, composições para antagonizar um receptor, uso de um composto, e, processos para produzir um composto, para antagonizar um receptor, para evitar ou tratar distúrbios de micção em mamìferos e distúrbios de asma, artrite reumatóide, osteoartrite, dor, tosse, sìndrome do intestino irritável ou vÈmitos em mamìferos
US20020132817A1 (en) 1998-03-19 2002-09-19 Hideaki Natsugari Heterocyclic compounds, their production and use
FR2778662B1 (fr) 1998-05-12 2000-06-16 Adir Nouveaux composes cycliques substitues, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
JP2000007661A (ja) 1998-06-23 2000-01-11 Nippon Nohyaku Co Ltd 複素環ジカルボン酸ジアミド誘導体及びその中間体並びに除草剤
CN1311778A (zh) 1998-07-28 2001-09-05 日本农药株式会社 稠杂环二羧酸二酰胺衍生物或其盐,应用上述物质的除草剂及其使用方法
EP1145714A4 (en) 1998-11-27 2004-12-15 Takeda Chemical Industries Ltd DRUGS
US6417207B1 (en) 1999-05-12 2002-07-09 Nitromed, Inc. Nitrosated and nitrosylated potassium channel activators, compositions and methods of use
MXPA02000670A (es) 1999-07-21 2002-07-02 Astrazeneca Ab Nuevos compuestos.
MXPA02000828A (es) 1999-08-02 2002-07-30 Hoffmann La Roche Nuevos antagonistas retinoiides selectivos.
CA2674424C (en) 1999-11-09 2012-10-02 Abbott Laboratories Hydromorphinone and hydrocodeinone compositions and methods for their synthesis
RU2223761C2 (ru) 1999-12-27 2004-02-20 Джапан Тобакко Инк. Соединения с конденсированным кольцом и их использование в качестве лекарственных средств
US6770666B2 (en) 1999-12-27 2004-08-03 Japan Tobacco Inc. Fused-ring compounds and use thereof as drugs
US6350755B1 (en) 2000-01-12 2002-02-26 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
JP2003531894A (ja) 2000-04-25 2003-10-28 サムスン エレクトロニクス カンパニー リミテッド マトリックスメタロプロテアーゼ阻害剤としてのビフェニルブチル酸誘導体
KR100608405B1 (ko) 2000-05-02 2006-08-02 에프. 호프만-라 로슈 아게 신규한 감마 선택적인 레티노이드
HK1050008A1 (zh) 2000-05-05 2003-06-06 Portola Pharmaceuticals, Inc. 杂双环磺胺剂及以其作为血小板腺苷二磷酸(adp)受体抑制剂
CA2354606C (en) 2000-08-03 2005-12-06 Pfizer Products Inc. Azabicycloalkane derivatives and therapeutic uses thereof
AU2002212598A1 (en) 2000-09-19 2002-04-02 Centre National De La Recherche Scientifique (Cnrs) Pyridinone and pyridinethione derivatives having hiv inhibiting properties
US6884782B2 (en) 2000-11-08 2005-04-26 Amgen Inc. STAT modulators
TWI236474B (en) 2001-04-03 2005-07-21 Telik Inc Antagonists of MCP-1 function and methods of use thereof
WO2002081447A1 (en) 2001-04-06 2002-10-17 Daewoong Pharmaceutical Co., Ltd. 3-cyclopentyloxy-4-methoxyphenyl-isothiazolinone derivatives and the use thereof
ES2278016T3 (es) 2001-04-09 2007-08-01 Novartis Vaccines And Diagnostics, Inc. Compuestos guanidino como agonistas del receptor de melanocortina 4 (mc4-r).
DE60231608D1 (de) 2001-04-19 2009-04-30 Eisai R&D Man Co Ltd Cyclische amidinderivate
CN1250550C (zh) 2001-07-16 2006-04-12 盐野义制药株式会社 脒衍生物的制备方法
JP2003171380A (ja) 2001-09-28 2003-06-20 Takeda Chem Ind Ltd 三環性化合物の製造法
WO2003029254A1 (en) 2001-09-28 2003-04-10 Takeda Chemical Industries, Ltd. Process for preparation of tricyclic compounds
EA007429B1 (ru) 2001-10-02 2006-10-27 Фармация Энд Апджон Компани Азабициклические замещённые конденсированные гетероарильные соединения
DE10207037A1 (de) 2002-02-20 2003-08-28 Bayer Cropscience Gmbh 2-Amino-4-bicyclyamino-6H-1,3.5-triazine, Verfahren zu deren Herstellung und deren Verwendung als Herbizide und Pflanzenwachstumsregulatoren
WO2003076440A1 (en) 2002-03-06 2003-09-18 Smithkline Beecham Corporation Condensed heterocyclic compounds as calcitonin agonists
WO2003104216A1 (en) 2002-06-10 2003-12-18 Acadia Pharmaceuticals Inc. Urotensin ii receptor modulators
AU2003250482A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc Phthalimide derivatives as matrix metalloproteinase inhibitors
US8604183B2 (en) 2002-11-05 2013-12-10 Isis Pharmaceuticals, Inc. Compositions comprising alternating 2′-modified nucleosides for use in gene modulation
JP2004203791A (ja) 2002-12-25 2004-07-22 Dai Ichi Seiyaku Co Ltd 芳香族化合物
CN1212674C (zh) 2003-01-08 2005-07-27 东南大学 横向缓冲p型金属氧化物半导体管
TW200503994A (en) 2003-01-24 2005-02-01 Novartis Ag Organic compounds
GB0308025D0 (en) 2003-04-07 2003-05-14 Glaxo Group Ltd Compounds
CN1791395B (zh) 2003-05-19 2012-09-26 Irm责任有限公司 免疫抑制剂化合物及组合物
MY150088A (en) 2003-05-19 2013-11-29 Irm Llc Immunosuppressant compounds and compositions
BRPI0410439A (pt) 2003-05-19 2006-06-06 Irm Llc compostos e composições imunossupressoras
WO2004113330A1 (en) 2003-05-19 2004-12-29 Irm Llc Immunosuppressant compounds and compositions
WO2004108133A2 (en) 2003-06-05 2004-12-16 Vertex Pharmaceuticals Incorporated Modulators of vr1 receptor
CN1566099A (zh) 2003-06-13 2005-01-19 中国科学院上海药物研究所 异喹啉-1,3,4-三酮类化合物、制备方法及其用途
EP1660454A1 (en) 2003-07-07 2006-05-31 Vernalis (R&D) Limited Azacyclic compounds as inhibitors of sensory neurone specific channels
FR2857966A1 (fr) 2003-07-24 2005-01-28 Aventis Pharma Sa Produits aryl-heteroaromatiques, compositions les contenant et utilisation
CA2533554A1 (en) 2003-08-01 2005-02-10 Pfizer Products Inc. 6-membered heteroaryl compounds for the treatment of neurodegenerative disorders
WO2005028480A2 (en) 2003-09-03 2005-03-31 Neurogen Corporation 5-aryl-pyrazolo[4,3-d]pyrimidines, pyridines, and pyrazines and related compounds
JP2007504271A (ja) 2003-09-05 2007-03-01 ニューロジェン・コーポレーション Crf1受容体リガンドである、ヘテロアリール縮合ピリジン類、ピラジン類及びピリミジン類
US20070088163A1 (en) 2003-09-12 2007-04-19 Kemia, Inc. Modulators of calcitonin and amylin activity
US20050182061A1 (en) 2003-10-02 2005-08-18 Jeremy Green Phthalimide compounds useful as protein kinase inhibitors
JP4768628B2 (ja) 2003-11-19 2011-09-07 アレイ バイオファーマ、インコーポレイテッド Mekの二環系阻害剤及びその使用方法
US7732616B2 (en) 2003-11-19 2010-06-08 Array Biopharma Inc. Dihydropyridine and dihydropyridazine derivatives as inhibitors of MEK and methods of use thereof
WO2005060958A1 (en) 2003-12-19 2005-07-07 Kalypsys, Inc. (5- (2-phenyl)-thiazol-5-ylmethoxy)-indol-1-yl) -acetic acid derivatives and related compounds as modulators of the human ppar-delta receptor for the treatment of metabolic disorders such as type 2 diabetes
MXPA06007213A (es) 2003-12-23 2006-08-18 Pfizer Prod Inc Combinacion terapeutica para la mejora de la cognicion y trastornos sicoticos.
WO2005100334A1 (en) 2004-04-14 2005-10-27 Pfizer Products Inc. Dipeptidyl peptidase-iv inhibitors
NZ553646A (en) 2004-09-22 2010-07-30 Janssen Pharmaceutica Nv Inhibitors of the interaction between MDM2 and p53
US20060128710A1 (en) 2004-12-09 2006-06-15 Chih-Hung Lee Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof
WO2006065842A2 (en) 2004-12-13 2006-06-22 Synta Pharmaceuticals Corp. 5,6,7,8-tetrahydroquinolines and related compounds and uses thereof
MX2007008328A (es) 2005-01-07 2008-01-16 Univ Emory Antagonistas cxcr4 para el tratamiento de trastornos medicos.
SI1848694T1 (sl) 2005-02-07 2010-01-29 Hoffmann La Roche Heterocikliäśni substituirani fenil metanoni kot inhibitorji glicinskega transporterja 1
GB0504556D0 (en) 2005-03-04 2005-04-13 Pfizer Ltd Novel pharmaceuticals
CA2604042C (en) 2005-04-13 2016-06-21 Astex Therapeutics Limited Pharmaceutical compounds
WO2007050124A1 (en) 2005-05-19 2007-05-03 Xenon Pharmaceuticals Inc. Fused piperidine derivatives and their uses as therapeutic agents
WO2007007054A1 (en) 2005-07-08 2007-01-18 Cancer Research Technology Limited Phthalamides, succinimides and related compounds and their use as pharmaceuticals
WO2007036734A1 (en) 2005-09-29 2007-04-05 Glaxo Group Limited Pyrazolo[3,4-b]pyridine compound, and its use as a pde4 inhibitor
WO2007055418A1 (ja) 2005-11-10 2007-05-18 Banyu Pharmaceutical Co., Ltd. アザ置換スピロ誘導体
PE20071241A1 (es) 2006-01-17 2008-01-14 Schering Corp Compuestos derivados de hidantoina para el tratamiento de trastornos inflamatorios
WO2007097931A2 (en) 2006-02-15 2007-08-30 Merck & Co., Inc. Aminotetrahydropyrans as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
US20090291857A1 (en) 2006-02-27 2009-11-26 The Board Of Trustees Of The Leland Stanford Junior University Methods to identify inhibitors of the unfolded protein response
US7977351B2 (en) 2006-03-22 2011-07-12 Allergan, Inc. Heteroaryl dihydroindolones as kinase inhibitors
ATE470665T1 (de) 2006-03-22 2010-06-15 Janssen Pharmaceutica Nv Cycloalkylaminderivate als inhibitoren der wechselwirkung zwischen mdm2 und p53
WO2008118122A2 (en) 2006-05-08 2008-10-02 Molecular Neuroimaging, Llc Compounds and amyloid probes thereof for therapeutic and imaging uses
EA200802210A1 (ru) 2006-05-16 2009-06-30 Бёрингер Ингельхайм Интернациональ Гмбх Замещенные пролинамиды, их получение и их применение в качестве лекарственных средств
CN1869036A (zh) 2006-06-30 2006-11-29 中国药科大学 7-取代-3-氯吡咯并[3,4-b]吡啶化合物
EP2051964A4 (en) 2006-07-28 2012-03-07 Univ Connecticut INHIBITORS OF FATTY ACID AMIDHYDROLASE
US8389739B1 (en) 2006-10-05 2013-03-05 Orphagen Pharmaceuticals Modulators of retinoid-related orphan receptor gamma
EP2073804B1 (en) 2006-10-12 2017-09-13 Astex Therapeutics Limited Hydroxy-substituted benzoic acid amide compounds for use in the treatment of pain
WO2008044029A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
WO2008044027A2 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical compounds having hsp90 inhibitory or modulating activity
JP5528807B2 (ja) 2006-10-12 2014-06-25 アステックス、セラピューティックス、リミテッド 複合薬剤
US8916552B2 (en) 2006-10-12 2014-12-23 Astex Therapeutics Limited Pharmaceutical combinations
AR063311A1 (es) 2006-10-18 2009-01-21 Novartis Ag Compuestos organicos
US20100016387A1 (en) 2006-12-11 2010-01-21 Avirup Bose Method of treatment
WO2008083070A1 (en) 2006-12-29 2008-07-10 Neurogen Corporation Crf1 receptor ligands comprising fused bicyclic heteroaryl moieties
KR20090101372A (ko) 2007-01-08 2009-09-25 페노믹스 코포레이션 매크로시클릭 c형 간염 프로테아제 억제제
WO2009004496A2 (en) 2007-04-13 2009-01-08 University Of Manitoba Bisanthrapyrazoles as anti-cancer agents
US20110189167A1 (en) 2007-04-20 2011-08-04 Flynn Daniel L Methods and Compositions for the Treatment of Myeloproliferative Diseases and other Proliferative Diseases
US20100129933A1 (en) 2007-04-26 2010-05-27 Forschungszentrum Karlsruhe Gmbh Method for detecting the binding between mdm2 and the proteasome
TW200902533A (en) 2007-05-02 2009-01-16 Boehringer Ingelheim Int Carboxylic acid amides, manufacturing and use thereof as medicaments
WO2008135524A2 (en) 2007-05-02 2008-11-13 Boehringer Ingelheim International Gmbh Substituted anthranilamides and analogues, manufacturing and use thereof as medicaments
WO2008141185A1 (en) 2007-05-10 2008-11-20 Constar International, Inc. Oxygen scavenging molecules, articles containing same, and methods of their use
TW200902499A (en) 2007-05-15 2009-01-16 Astrazeneca Ab New compounds
GB0710844D0 (en) 2007-06-06 2007-07-18 Lectus Therapeutics Ltd Potassium ion channel modulators & uses thereof
DE102007034620A1 (de) 2007-07-25 2009-01-29 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue B1-Antagonisten
WO2009026248A2 (en) 2007-08-17 2009-02-26 The Government Of The United States, As Represented By The Secretary Of Health And Human Services, National Institutes Of Health, Office Of Technology Transfer Hydrazide, amide, phthalimide and phthalhydrazide analogs as inhibitors of retroviral integrase
EP2725015A1 (en) 2007-09-17 2014-04-30 AbbVie Bahamas Ltd. Uracil or thymine derivative for treating hepatitis c
US20090076275A1 (en) 2007-09-19 2009-03-19 David Robert Bolin Diacylglycerol acyltransferase inhibitors
WO2009052319A1 (en) 2007-10-16 2009-04-23 Northeastern University Monoacylglycerol lipase inhibitors for modulation of cannabinoid activity
MX2010004246A (es) 2007-10-18 2010-04-30 Novartis Ag Inhibidores de csf-1r para el tratamiento de cancer y de enfermedades oseas.
WO2009068463A2 (en) 2007-11-29 2009-06-04 F. Hoffmann-La Roche Ag Process for the preparation of isoindole derivatives as well as a process for the preparation of their intermediates
WO2009073788A1 (en) 2007-12-07 2009-06-11 Firestone Leigh H Compositions and methods for treating menopausal females
FR2926554B1 (fr) 2008-01-22 2010-03-12 Sanofi Aventis Derives de carboxamides azabicycliques, leur preparation et leur application en therapeutique
CN101225070B (zh) 2008-01-31 2010-04-14 上海交通大学 用于抗肿瘤的药物
SI2242740T1 (sl) 2008-02-05 2013-03-29 Sanofi SF5-derivati kot PAR1 inhibitorji, njihova priprava in uporaba kot zdravila
WO2009112445A1 (en) 2008-03-10 2009-09-17 Novartis Ag Method of increasing cellular phosphatidyl choline by dgat1 inhibition
GB0804701D0 (en) 2008-03-13 2008-04-16 Amura Therapeutics Ltd Compounds
GB0804702D0 (en) 2008-03-13 2008-04-16 Amura Therapeutics Ltd Compounds
WO2009124755A1 (en) 2008-04-08 2009-10-15 European Molecular Biology Laboratory (Embl) Compounds with novel medical uses and method of identifying such compounds
US7863291B2 (en) 2008-04-23 2011-01-04 Bristol-Myers Squibb Company Quinuclidine compounds as alpha-7 nicotinic acetylcholine receptor ligands
US8309577B2 (en) 2008-04-23 2012-11-13 Bristol-Myers Squibb Company Quinuclidine compounds as α-7 nicotinic acetylcholine receptor ligands
GB0809776D0 (en) 2008-05-29 2008-07-09 Amura Therapeutics Ltd Compounds
CN102137843A (zh) 2008-07-01 2011-07-27 健泰科生物技术公司 作为mek激酶抑制剂的异吲哚酮衍生物及其使用方法
JP5559174B2 (ja) 2008-08-19 2014-07-23 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 冷感−メントール受容体拮抗剤
WO2010033350A1 (en) 2008-09-16 2010-03-25 Merck & Co., Inc. Sulfonamide derivative metabotropic glutamate r4 ligands
WO2010056194A1 (en) 2008-11-14 2010-05-20 Astrazeneca Ab 5h-pyrrolo [ 3, 4-b] pyridin derivatives and their use
US20100125087A1 (en) 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 575
CN101455661B (zh) 2008-11-19 2012-10-10 中国科学院上海有机化学研究所 3-取代苯酞及其类似物的用途
EP2376495A4 (en) 2008-12-08 2012-10-31 Vm Pharma Llc COMPOSITIONS OF PROTEIN RECEPTOR TYROSINE KINASE INHIBITORS
ES2406131T3 (es) 2009-01-28 2013-06-05 Bayer Intellectual Property Gmbh Derivados fungicidas de N-cicloalquil-N-biciclometileno-carboxamina
WO2011078143A1 (ja) 2009-12-22 2011-06-30 塩野義製薬株式会社 ピリミジン誘導体およびそれらを含有する医薬組成物
EP2563124A4 (en) 2010-01-19 2013-10-16 Res Triangle Inst KAPPA OPIOID RECEPTOR BINDING LIGANDS
RU2012136451A (ru) 2010-01-28 2014-03-10 Президент Энд Феллоуз Оф Гарвард Колледж Композиции и способы улучшения активности протеасомы
EP2368886A1 (en) 2010-03-01 2011-09-28 Phenex Pharmaceuticals AG Novel compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-gamma (ROR gamma, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune desease
CN102241621A (zh) 2010-05-11 2011-11-16 江苏恒瑞医药股份有限公司 5,5-双取代-2-亚氨基吡咯烷类衍生物、其制备方法及其在医药上的应用
EP2571876B1 (en) 2010-05-21 2016-09-07 Merck Sharp & Dohme Corp. Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
US8299117B2 (en) 2010-06-16 2012-10-30 Metabolex Inc. GPR120 receptor agonists and uses thereof
CA2801182A1 (en) 2010-06-16 2011-12-22 Metabolex, Inc. Gpr120 receptor agonists and uses thereof
WO2012027965A1 (en) 2010-09-01 2012-03-08 Glaxo Group Limited Novel compounds
WO2012028100A1 (en) 2010-09-01 2012-03-08 Glaxo Group Limited Novel compounds
SG188367A1 (en) 2010-09-03 2013-04-30 Forma Tm Llc Novel compounds and compositions for the inhibition of nampt
CN103119035B (zh) 2010-09-27 2015-09-30 雅培股份有限两合公司 杂环化合物和它们作为糖原合成酶激酶-3抑制剂的用途
JP2013253019A (ja) 2010-09-28 2013-12-19 Kowa Co 新規なピペリジン誘導体及びこれを含有する医薬
CA2816753A1 (en) 2010-11-08 2012-05-18 Lycera Corporation N- sulfonylated tetrahydroquinolines and related bicyclic compounds inhibition of rory activity and the treatment of diseases
AR083817A1 (es) 2010-11-10 2013-03-27 Gruenenthal Gmbh Derivados de carboxamida y urea heteroaromaticos sustituidos como ligandos del receptor vanilloide
WO2012100734A1 (en) 2011-01-24 2012-08-02 Glaxo Group Limited Compounds useful as retinoid-related orphan receptor gamma modulators
WO2012100732A1 (en) 2011-01-24 2012-08-02 Glaxo Group Limited Retinoid-related orphan receptor gamma modulators, composition containing them and uses thereof
EP2487159A1 (en) 2011-02-11 2012-08-15 MSD Oss B.V. RorgammaT inhibitors
CN102180780A (zh) 2011-03-07 2011-09-14 中国科学技术大学 茚酮类衍生物及其作为淀粉样蛋白沉积物和神经纤维缠结的显像剂和聚集抑制剂的用途
US9090568B2 (en) 2011-03-14 2015-07-28 Impact Therapeutics, Inc. Quinazolinediones and their use
CN103635458B (zh) 2011-03-25 2016-10-19 艾伯维公司 Trpv1拮抗剂
EP2694523B1 (de) 2011-04-04 2017-01-11 Merck Patent GmbH Metallkomplexe
EP2511263A1 (en) 2011-04-14 2012-10-17 Phenex Pharmaceuticals AG Pyrrolo sulfonamide compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-gamma (RORgamma, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune diseases
TWI532728B (zh) 2011-04-28 2016-05-11 日本煙草產業股份有限公司 醯胺化合物及其醫藥用途
US9938269B2 (en) 2011-06-30 2018-04-10 Abbvie Inc. Inhibitor compounds of phosphodiesterase type 10A
WO2013019653A1 (en) 2011-07-29 2013-02-07 Tempero Pharmaceuticals, Inc. Compounds and methods
WO2013018695A1 (ja) 2011-07-29 2013-02-07 武田薬品工業株式会社 複素環化合物
EP2747560A4 (en) 2011-07-29 2015-02-25 Tempero Pharmaceuticals Inc CONNECTIONS AND METHODS
US20140155419A1 (en) 2011-07-29 2014-06-05 Erkan Baloglu Compounds and methods
WO2013029338A1 (en) 2011-09-01 2013-03-07 Glaxo Group Limited Novel compounds
WO2013042782A1 (ja) 2011-09-22 2013-03-28 武田薬品工業株式会社 縮合複素環化合物
GB201116641D0 (en) 2011-09-27 2011-11-09 Glaxo Group Ltd Novel compounds
WO2013064231A1 (en) 2011-10-31 2013-05-10 Phenex Pharmaceuticals Ag SEVEN-MEMBERED SULFONAMIDES AS MODULATORS OF RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORγ, NR1F3)
US20140256767A1 (en) 2011-10-31 2014-09-11 The Broad Institute, Inc. Direct inhibitors of keap1-nrf2 interaction as antioxidant inflammation modulators
CA2856946C (en) 2011-12-02 2016-08-02 Phenex Pharmaceuticals Ag Pyrrolo carboxamides as modulators of orphan nuclear receptor rar-related orphan receptor-gamma (rory, nr1f3) activity and for the treatment of chronic inflammatory and autoimmunediseases
US8741892B2 (en) 2011-12-05 2014-06-03 Boehringer Ingelheim International Gmbh Compounds
US8642774B2 (en) 2011-12-08 2014-02-04 Boehringer Ingelheim International Gmbh Compounds
US8796467B2 (en) 2011-12-13 2014-08-05 Boehringer Ingelheim International Gmbh Compounds
WO2013092460A1 (en) 2011-12-20 2013-06-27 Syngenta Participations Ag Cyclic bisoxime microbicides
US9567328B2 (en) 2011-12-21 2017-02-14 Allergan, Inc. Compounds acting at multiple prostaglandin receptors giving a general anti-inflammatory response
US20130190356A1 (en) 2011-12-22 2013-07-25 Genentech, Inc. Benzyl sulfonamide derivatives as rorc modulators
WO2013100027A1 (ja) * 2011-12-28 2013-07-04 武田薬品工業株式会社 複素環化合物
US9321750B2 (en) 2012-04-20 2016-04-26 Innov17 Llc ROR modulators and their uses
GB201207406D0 (en) 2012-04-27 2012-06-13 Glaxo Group Ltd Novel compounds
CN104379559B (zh) 2012-04-27 2016-11-09 葛兰素集团有限公司 化合物
WO2013166013A1 (en) 2012-04-30 2013-11-07 Anderson Gaweco Ror modulators and their uses
US9266827B2 (en) 2012-05-08 2016-02-23 Merck Sharp & Dohme Corp. Bicyclic sulfone compounds for inhibition of RORgamma activity and the treatment of disease
WO2013169864A2 (en) 2012-05-08 2013-11-14 Lycera Corporation TETRAHYDRO[1,8]NAPHTHYRIDINE SULFONAMIDE AND RELATED COMPOUNDS FOR USE AS AGONISTS OF RORƴ AND THE TREATMENT OF DISEASE
KR20150007300A (ko) 2012-05-08 2015-01-20 머크 샤프 앤드 돔 코포레이션 Ror감마 활성의 억제를 위한 테트라히드로나프티리딘 및 관련 비시클릭 화합물 및 질환의 치료
KR101742954B1 (ko) 2012-05-31 2017-06-02 페넥스 파마슈티컬스 아게 고아 핵 수용체 ror[감마]의 조절제로서의 카복사미드 또는 설폰아미드가 치환된 티아졸 및 관련된 유도체
TW201414704A (zh) 2012-07-02 2014-04-16 Biogen Idec Inc 作爲ROR-γ受體之反向促效劑之含聯芳化合物
TW201408652A (zh) 2012-07-11 2014-03-01 Hoffmann La Roche 作爲RORc調節劑之芳基磺內醯胺衍生物
WO2014026330A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 3-AMINOCYCLOALKYL COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
WO2014028669A1 (en) 2012-08-15 2014-02-20 Biogen Idec Ma Inc. Novel compounds for modulation of ror-gamma activity
WO2014026328A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 3-cyclohexenyl substituted indole and indazole compounds as rorgammat inhibitors and uses thereof
WO2014026329A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. N-alkylated indole and indazole compounds as rorgammat inhibitors and uses thereof
WO2014062938A1 (en) 2012-10-19 2014-04-24 Bristol-Myers Squibb Company Rory modulators
SG11201504200TA (en) 2012-12-06 2015-06-29 Glaxo Group Ltd Modulators of the retinoid-related orphan receptor gamma (ror-gamma) for use in the treatment of autoimmune and inflammatory diseases
WO2013171729A2 (en) 2013-01-08 2013-11-21 Glenmark Pharmaceuticals S.A. Aryl and heteroaryl amide compounds as rorgamat modulator
RS59007B1 (sr) * 2014-02-03 2019-08-30 Vitae Pharmaceuticals Llc Dihidropirolopiridinski inhibitori ror-gama
EA031967B1 (ru) 2014-10-14 2019-03-29 Вайтаи Фармасьютиклз, Инк. ДИГИДРОПИРРОЛОПИРИДИНОВЫЕ ИНГИБИТОРЫ ROR-γ
US9663515B2 (en) * 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
US9481674B1 (en) * 2016-06-10 2016-11-01 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013019682A1 (en) * 2011-07-29 2013-02-07 Tempero Pharmaceuticals, Inc. Compounds and methods
CN104024239A (zh) * 2011-12-22 2014-09-03 弗·哈夫曼-拉罗切有限公司 作为RORc调节剂的苄基磺酰胺衍生物
WO2014026327A1 (en) * 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 4-heteroaryl substituted benzoic acid compounds as rorgammat inhibitors and uses thereof

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