RU2760366C2 - Производные бензимидазола в качестве модуляторов ror-гамма - Google Patents

Производные бензимидазола в качестве модуляторов ror-гамма Download PDF

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RU2760366C2
RU2760366C2 RU2018127360A RU2018127360A RU2760366C2 RU 2760366 C2 RU2760366 C2 RU 2760366C2 RU 2018127360 A RU2018127360 A RU 2018127360A RU 2018127360 A RU2018127360 A RU 2018127360A RU 2760366 C2 RU2760366 C2 RU 2760366C2
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Russia
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methyl
benzo
imidazole
carboxamide
dioxol
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RU2018127360A
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Russian (ru)
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RU2018127360A (ru
RU2018127360A3 (enExample
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Дэвид А. Клэрмон
Лоуренс Уэйн Диллард
И Фань
Стивен Д. Лотеста
Суреш Б. СИНГХ
Колин М. ТАЙС
Веи ЧЖАО
Линхан Чжуан
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Вайтаи Фармасьютиклз, Ллк
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Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3527569B1 (en) 2014-02-03 2021-08-25 Vitae Pharmaceuticals, LLC Dihydropyrrolopyridine inhibitors of ror-gamma for use in treating drye eye
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
CU24487B1 (es) 2015-05-15 2020-11-30 Aurigene Discovery Tech Ltd Compuestos de tetrahidroquinolinona sustituidos como moduladores de gamma ror
ES2856931T3 (es) 2015-08-05 2021-09-28 Vitae Pharmaceuticals Llc Moduladores de ROR-gamma
EP3868750A1 (en) 2015-11-20 2021-08-25 Vitae Pharmaceuticals, LLC Modulators of ror-gamma
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
MA49685A (fr) 2017-07-24 2021-04-14 Vitae Pharmaceuticals Llc INHIBITEURS DE ROR gamma
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
CN109593068B (zh) * 2017-09-30 2022-12-27 广东东阳光药业有限公司 一种RORγ抑制剂的中间体及其制备方法
HUE062273T2 (hu) * 2018-05-03 2023-10-28 Jiangsu Hengrui Pharmaceuticals Co Ltd Benzimidazolszármazékok mint a retinsavreceptor rokon árvareceptor-gamma (RORy) modulátorai és gyógyszerészeti felhasználásaik
CN110483437B (zh) * 2018-05-14 2022-12-06 嘉兴维眸生物科技有限公司 一种含五元环的化合物及其制备和应用
WO2020082921A1 (zh) * 2018-10-24 2020-04-30 上海和誉生物医药科技有限公司 一种氮杂芳基酰胺衍生物及其制备方法和应用
CN111320609A (zh) 2018-12-13 2020-06-23 拓臻股份有限公司 一种THRβ受体激动剂化合物及其制备方法和用途
AU2020336272A1 (en) 2019-08-23 2022-04-14 Terns Pharmaceuticals, Inc. Thyroid hormone receptor beta agonist compounds
EP4028008A4 (en) 2019-09-12 2023-09-13 Terns Pharmaceuticals, Inc. Thyroid hormone receptor beta agonist compounds
AU2020377114A1 (en) * 2019-10-31 2022-06-16 Jiangsu Hengrui Medicine Co., Ltd. Acid addition salt of RORγ regulator
CN112745268B (zh) * 2019-10-31 2022-09-16 江苏恒瑞医药股份有限公司 苯并咪唑衍生物的晶型及制备方法
TW202136237A (zh) 2020-01-06 2021-10-01 大陸商廣東東陽光藥業有限公司 RORγt抑制劑及其製備方法和用途
CN111333552B (zh) * 2020-04-09 2021-07-20 广州安岩仁医药科技有限公司 β-苯并氨基酸类化合物的合成方法
CN111606868B (zh) * 2020-06-23 2023-02-17 温州大学新材料与产业技术研究院 一种双齿噁唑啉手性配体的制备方法
CN113912563B (zh) * 2020-07-10 2025-05-27 中国科学院广州生物医药与健康研究院 一种苯并五元氮杂环化合物及其应用
PE20240097A1 (es) * 2021-03-03 2024-01-18 Terns Pharmaceuticals Inc Compuestos agonistas beta del receptor de la hormona tiroidea
US20240417486A1 (en) * 2021-10-04 2024-12-19 Bolt Biotherapeutics, Inc. Asymmetric bis-benzimidazole sting agonist immunoconjugates and uses thereof
WO2024211898A1 (en) 2023-04-07 2024-10-10 Terns Pharmaceuticals, Inc. Combination comprising a thrbeta agonist anda glp-1r agonist for use in treating a liver disorder or a cardiometabolic disease

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2261248C2 (ru) * 1999-06-23 2005-09-27 Авентис Фарма Дойчланд Гмбх Замещенные бензимидазолы и лекарственное средство на их основе
WO2009083526A1 (en) * 2008-01-02 2009-07-09 Smithkline Beecham Corporation Novel compounds
WO2013078240A1 (en) * 2011-11-22 2013-05-30 Ripka Amy S N-biphenylmethylbenzimidazole modulators of pparg
WO2013078233A1 (en) * 2011-11-22 2013-05-30 Ripka Amy S N-benzylbenzimidazole modulators of pparg

Family Cites Families (253)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3751524T2 (de) 1986-07-28 1996-06-13 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
AU5175490A (en) 1989-02-27 1990-09-26 Du Pont Merck Pharmaceutical Company, The 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
DE4121214A1 (de) 1991-06-27 1993-01-14 Bayer Ag 7-azaisoindolinyl-chinolon- und -naphthyridoncarbonsaeure-derivate
EP0520573A1 (en) 1991-06-27 1992-12-30 Glaxo Inc. Cyclic imide 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
TW394773B (en) 1995-03-24 2000-06-21 Takeda Chemical Industries Ltd Cyclic compounds for antagonizing tachykinin receptor, substance p receptor and neurokinin a receptor, their production and pharmaceutical composition
US5770590A (en) 1995-03-24 1998-06-23 Takeda Chemical Industries, Ltd. Cyclic compounds, their prudiction and use
EP0882718B1 (en) * 1995-12-28 2005-08-31 Fujisawa Pharmaceutical Co., Ltd. Benzimidazole derivatives
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
EP0973778A1 (en) 1997-03-07 2000-01-26 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
KR20010041991A (ko) 1998-03-19 2001-05-25 다케다 야쿠힌 고교 가부시키가이샤 복소환식 화합물, 그의 제조법 및 타키키닌 수용체길항약으로서의 용도
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
WO2000006549A1 (en) 1998-07-28 2000-02-10 Nihon Nohyaku Co., Ltd. Fused-heterocycle dicarboxylic diamide derivatives or salts thereof, herbicides and usage thereof
US6348032B1 (en) * 1998-11-23 2002-02-19 Cell Pathways, Inc. Method of inhibiting neoplastic cells with benzimidazole derivatives
AU1409100A (en) 1998-11-27 2000-06-19 Takeda Chemical Industries Ltd. Drugs
AU4841700A (en) 1999-05-12 2000-11-21 Nitromed, Inc. Nitrosated and nitrosylated potassium channel activators, compositions and methods of use
TR200200118T2 (tr) 1999-07-21 2002-12-23 Astrazeneca Ab Yeni bileşimler
DK1206436T3 (da) 1999-08-02 2005-02-14 Hoffmann La Roche Retinoider til behandling af emfysem
US6512117B1 (en) 1999-11-09 2003-01-28 Abbott Laboratories Hydromorphone and hydrocodone compositions and methods for their synthesis
EP1162196A4 (en) 1999-12-27 2003-04-16 Japan Tobacco Inc COMPOUNDS WITH JOINED CYCLES AND THEIR USE AS MEDICAMENTS
US6770666B2 (en) 1999-12-27 2004-08-03 Japan Tobacco Inc. Fused-ring compounds and use thereof as drugs
WO2001051128A1 (en) 2000-01-12 2001-07-19 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
WO2001083445A1 (en) 2000-04-25 2001-11-08 Samsung Electronics Co., Ltd. Biphenyl butyric acid derivative as a matrix metalloproteinase inhibitor
US6552015B2 (en) 2000-08-03 2003-04-22 Pfizer Inc. Azabicycloalkane derivatives and therapeutic uses thereof
US6884782B2 (en) 2000-11-08 2005-04-26 Amgen Inc. STAT modulators
US6677365B2 (en) 2001-04-03 2004-01-13 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
EP1767525A1 (en) 2001-04-09 2007-03-28 Novartis Vaccines and Diagnostics, Inc. Guanidino compounds as melanocortin-4 receptor (MC4-R) agonists
US7476688B2 (en) 2001-04-19 2009-01-13 Eisai R&D Management Co., Ltd. Cyclic amidine derivatives
HRP20030961B1 (en) 2001-05-24 2012-01-31 Eli Lilly And Company Novel pyrrole derivatives as pharmaceutical agents
KR20040027878A (ko) 2001-07-16 2004-04-01 시오노기 앤드 컴파니, 리미티드 아미딘 유도체의 제조 방법
WO2003029254A1 (en) 2001-09-28 2003-04-10 Takeda Chemical Industries, Ltd. Process for preparation of tricyclic compounds
JP2003171380A (ja) 2001-09-28 2003-06-20 Takeda Chem Ind Ltd 三環性化合物の製造法
EP1432707B1 (en) 2001-10-02 2012-03-28 Pharmacia & Upjohn Company LLC Azabicyclic-substituted fused-heteroaryl compounds for the treatment of disease
DE10156719A1 (de) 2001-11-19 2003-05-28 Bayer Ag Heteroarylcarbonsäureamide
TWI263640B (en) 2001-12-19 2006-10-11 Bristol Myers Squibb Co Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
JP4216196B2 (ja) 2002-02-04 2009-01-28 エフ．ホフマン−ラ ロシュ アーゲー Ｎｐｙアンタゴニストとしてのキノリン誘導体
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
AU2003213266A1 (en) 2002-03-06 2003-09-22 Smithkline Beecham Corporation Condensed heterocyclic compounds as calcitonin agonists
US20040077529A1 (en) 2002-06-10 2004-04-22 Per-Fredrik Lehmann Urotensin II receptor agents
AU2003250482A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc Phthalimide derivatives as matrix metalloproteinase inhibitors
EP1543001B1 (en) 2002-09-17 2007-08-15 Eli Lilly And Company Pyrazolopyridine derivatives as tgf beta signal transduction inhibitors for the treatment of cancer
WO2004043979A2 (en) 2002-11-05 2004-05-27 Isis Pharmaceuticals, Inc. Sugar surrogate-containing oligomeric compounds and compositions 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
MY150088A (en) 2003-05-19 2013-11-29 Irm Llc Immunosuppressant compounds and compositions
AU2004251146A1 (en) 2003-05-19 2005-01-06 Irm, Llc Immunosuppressant compounds and compositions
CN1787817B (zh) 2003-05-19 2011-09-07 Irm责任有限公司 免疫抑制剂化合物及组合物
WO2004113330A1 (en) 2003-05-19 2004-12-29 Irm Llc Immunosuppressant compounds and compositions
EP1628661A2 (en) 2003-06-05 2006-03-01 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
WO2005005392A1 (en) 2003-07-07 2005-01-20 Ionix Pharmaceuticals 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
BRPI0413245A (pt) 2003-08-01 2006-10-03 Pfizer Prod Inc compostos heteroarila de 6 membros para o tratamento de distúrbio neurodegenerativos
WO2005028480A2 (en) 2003-09-03 2005-03-31 Neurogen Corporation 5-aryl-pyrazolo[4,3-d]pyrimidines, pyridines, and pyrazines and related compounds
BRPI0414087A (pt) 2003-09-05 2006-10-31 Neurogen Corp composto, métodos para tratar um distúrbio, para demostrar a presença de receptores de crf em amostras de célula ou tecido, e para inibir a ligação de crf a um receptor de crf1, composição farmacêutica, e, embalagem
WO2005025504A2 (en) 2003-09-12 2005-03-24 Kemia, Inc. Modulators of calcitonin and amylin activity
WO2005039564A1 (en) 2003-10-02 2005-05-06 Vertex Pharmaceuticals Incorporated Phthalimide compounds useful as protein kinase inhibitors
NZ547481A (en) 2003-11-19 2009-12-24 Array Biopharma Inc Heterocyclic inhibitors of mek and methods of use thereof
US7732616B2 (en) 2003-11-19 2010-06-08 Array Biopharma Inc. Dihydropyridine and dihydropyridazine derivatives as inhibitors of MEK and methods of use thereof
US20050203151A1 (en) 2003-12-19 2005-09-15 Kalypsys, Inc. Novel compounds, compositions and uses thereof for treatment of metabolic disorders and related conditions
CA2549638A1 (en) 2003-12-23 2005-07-14 Pfizer Products Inc. Therapeutic combination for cognition enhancement and psychotic disorders
JP2007531744A (ja) 2004-04-05 2007-11-08 武田薬品工業株式会社 ６−アザインドール化合物
WO2005100334A1 (en) 2004-04-14 2005-10-27 Pfizer Products Inc. Dipeptidyl peptidase-iv inhibitors
GB0412467D0 (en) 2004-06-04 2004-07-07 Astrazeneca Ab Chemical compounds
SI1809622T1 (sl) 2004-09-22 2010-11-30 Janssen Pharmaceutica Nv Inhibitorji interakcije med MDM in P
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
RU2007130077A (ru) 2005-01-07 2009-02-20 Эмори Юниверсити (Us) Антагонисты cxcr4 и их применение для лечения вич-инфекции
UA91536C2 (uk) 2005-02-07 2010-08-10 Ф. Хоффманн-Ля Рош Аг Гетероциклічні заміщені фенілметанони як інгібітори переносника гліцину 1
GB0504556D0 (en) 2005-03-04 2005-04-13 Pfizer Ltd Novel pharmaceuticals
DE102005012872A1 (de) * 2005-03-19 2006-09-28 Sanofi-Aventis Deutschland Gmbh Substituierte, bizyklische 8-Pyrrolidino-benzimidazole, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US20080306054A1 (en) 2005-04-13 2008-12-11 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
JP2009504759A (ja) 2005-08-16 2009-02-05 メモリ ファーマセチカル コーポレーション ホスホジエステラーゼ１０阻害剤
ES2363795T3 (es) 2005-09-29 2011-08-16 Glaxo Group Limited Compuestos de pirazolo[3,4-b]piridina, y su uso como inhibidores de pde4.
ES2381205T3 (es) 2005-11-10 2012-05-24 Msd K.K. Derivado espiro aza-sustituido
PE20071240A1 (es) 2006-01-17 2008-01-14 Schering Corp Compuestos derivados de hidantoina para el tratamiento de trastornos inflamatorios
US20080108611A1 (en) 2006-01-19 2008-05-08 Battista Kathleen A Substituted thienopyrimidine kinase inhibitors
WO2007087231A2 (en) 2006-01-25 2007-08-02 Merck & Co., Inc. Aminocyclohexanes as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
JP5161795B2 (ja) 2006-02-15 2013-03-13 メルク・シャープ・エンド・ドーム・コーポレイション 糖尿病の治療又は予防のためのジペプチジルペプチダーゼｉｖインヒビターとしてのアミノテトラヒドロピラン
AU2007220039A1 (en) 2006-02-27 2007-09-07 The Board Of Trustees Of The Leland Stanford Junior University Inhibitors of the unfolded protein response and methods for their use
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
US7700616B2 (en) 2006-05-08 2010-04-20 Molecular Neuroimaging, Llc. Compounds and amyloid probes thereof for therapeutic and imaging uses
PE20080702A1 (es) 2006-05-16 2008-07-10 Boehringer Ingelheim Int PROLINAMIDAS SUSTITUIDAS COMO INHIBIDORES DEL FACTOR Xa
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
DE102006032824A1 (de) 2006-07-14 2008-01-17 Bayer Healthcare Ag Substituierte Indazole
CA2657287A1 (en) 2006-07-17 2008-01-24 Merck & Co., Inc. 1-hydroxy naphthyridine compounds as anti-hiv agents
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
WO2008044027A2 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical compounds having hsp90 inhibitory or modulating activity
WO2008044041A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
JP5518478B2 (ja) 2006-10-12 2014-06-11 アステックス、セラピューティックス、リミテッド 医薬化合物
WO2008044045A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
JP5721949B2 (ja) 2006-10-12 2015-05-20 アステックス、セラピューティックス、リミテッドＡｓｔｅｘ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｌｉｍｉｔｅｄ 複合薬剤
PE20080888A1 (es) 2006-10-18 2008-08-26 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE LA ACIL-TRANSFERASA DE ACIL-CoA-DIACIL-GLICEROL 1 (DGAT1)
WO2008073865A2 (en) 2006-12-11 2008-06-19 Novartis Ag Method of preventing or treating myocardial ischemia
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
AR066379A1 (es) 2007-05-02 2009-08-12 Boehringer Ingelheim Int Amidas de acido carboxilico su preparacion y su uso como medicamentos
WO2008135524A2 (en) 2007-05-02 2008-11-13 Boehringer Ingelheim International Gmbh Substituted anthranilamides and analogues, manufacturing and use thereof as medicaments
DK2152794T3 (da) 2007-05-10 2014-03-31 Constar Internat Llc Oxygen-fjernende molekyler, artikler indeholdende disse, og fremgangsmåde til deres anvendelse
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
TWI534137B (zh) 2007-09-17 2016-05-21 艾伯維巴哈馬有限公司 抗感染劑及其用途
US20090076275A1 (en) 2007-09-19 2009-03-19 David Robert Bolin Diacylglycerol acyltransferase inhibitors
US20100210655A1 (en) 2007-10-11 2010-08-19 Yun Ding NOVEL sEH INHIBITORS AND THEIR USE
EP2203058A4 (en) 2007-10-16 2011-08-31 Univ Northeastern METHOD AND COMPOUNDS FOR MODULATING CANNABINOIDACTIVITY
US20100261679A1 (en) 2007-10-18 2010-10-14 James Sutton CSF-1R, Inhibitors, Compositions, and Methods of Use
CN101874019B (zh) 2007-11-29 2013-06-12 弗·哈夫曼-拉罗切有限公司 制备异吲哚衍生物的方法以及制备它们的中间体的方法
WO2009073788A1 (en) 2007-12-07 2009-06-11 Firestone Leigh H Compositions and methods for treating menopausal females
AU2008338965A1 (en) * 2007-12-18 2009-06-25 Arena Pharmaceuticals, Inc. Tetrahydrocyclopenta[b]indol-3-yl carboxylic acid derivatives useful in the treatment of autoimmune and inflammatory disorders
EP2078711A1 (en) 2007-12-28 2009-07-15 AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A. (Aza)indole derivative substituted in position 5, pharmaceutical composition comprising it, intermediate compounds and preparation process therefor
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
GB0804702D0 (en) 2008-03-13 2008-04-16 Amura Therapeutics Ltd Compounds
GB0804701D0 (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
JP5615274B2 (ja) 2008-07-01 2014-10-29 ジェネンテック， インコーポレイテッド Ｍｅｋキナーゼインヒビターとしてのイソインドロン誘導体及びその使用方法
US8143259B2 (en) 2008-08-19 2012-03-27 Janssen Pharmaceutica, Nv Cold menthol receptor antagonists
EP2327704A4 (en) 2008-08-29 2012-05-09 Shionogi & Co RING-CONDENSED AZOL DERIVATIVE WITH PI3K-INHIBITING EFFECT
WO2010033350A1 (en) 2008-09-16 2010-03-25 Merck & Co., Inc. Sulfonamide derivative metabotropic glutamate r4 ligands
US20100125087A1 (en) 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 575
US20100125081A1 (en) 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 574
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
CN106336400A (zh) 2008-12-08 2017-01-18 萌蒂制药国际有限公司 酪氨酸激酶蛋白受体拮抗剂
EP2391608B8 (en) 2009-01-28 2013-04-10 Bayer Intellectual Property GmbH Fungicide n-cycloalkyl-n-bicyclicmethylene-carboxamide derivatives
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
CN102770431A (zh) * 2009-12-23 2012-11-07 赛诺菲 [4[4-(5-氨基甲基-2-氟-苯基)-哌啶-1-基]-(1h-吡咯并吡啶-基)-甲酮及其合成
CA2785791A1 (en) 2010-01-19 2011-07-28 Research Triangle Institute Kappa opioid receptor binding ligands
MX336731B (es) 2010-01-28 2016-01-28 Harvard College Composiciones y metodos para potenciar la actividad de proteasoma.
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
US8980929B2 (en) 2010-05-21 2015-03-17 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
WO2012031197A1 (en) 2010-09-03 2012-03-08 Forma Therapeutics, Inc. 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
JP6063870B2 (ja) 2010-11-08 2017-01-18 ライセラ・コーポレイション ＲＯＲγ活性の阻害用のＮ−スルホニル化テトラヒドロキノリンおよび関連二環化合物および病気の治療
CA2816769A1 (en) 2010-11-10 2012-05-18 Gruenenthal Gmbh Substituted heteroaromatic carboxamide and urea derivatives as vanilloid receptor ligands
WO2012100732A1 (en) 2011-01-24 2012-08-02 Glaxo Group Limited Retinoid-related orphan receptor gamma modulators, composition containing them and uses thereof
WO2012100734A1 (en) 2011-01-24 2012-08-02 Glaxo Group Limited Compounds useful as retinoid-related orphan receptor gamma modulators
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
EP2686305B1 (en) 2011-03-14 2020-09-16 Impact Therapeutics, Inc. Quinazolinediones and their use
CN103635458B (zh) 2011-03-25 2016-10-19 艾伯维公司 Trpv1拮抗剂
US9469667B2 (en) 2011-04-04 2016-10-18 Merck Patent Gmbh Metal complexes
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
EP2927217B1 (en) 2011-04-28 2018-01-17 Japan Tobacco Inc. Amide compound and pharmaceutical application therefor
US9938269B2 (en) 2011-06-30 2018-04-10 Abbvie Inc. Inhibitor compounds of phosphodiesterase type 10A
EP2747560A4 (en) 2011-07-29 2015-02-25 Tempero Pharmaceuticals Inc CONNECTIONS 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
US20140315881A1 (en) 2011-07-29 2014-10-23 Tempero Pharmaceuticals, Inc. Compounds and methods
WO2013019653A1 (en) 2011-07-29 2013-02-07 Tempero Pharmaceuticals, Inc. Compounds 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
US9120776B2 (en) 2011-09-22 2015-09-01 Takeda Pharmaceutical Company Limited Condensed heterocyclic compound
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
US9815851B2 (en) 2011-12-02 2017-11-14 Phenex Pharmaceuticals Ag Pyrrolo carboxamides as modulators of orphan nuclear receptor RAR-related orphan receptor-gamma (RORγ, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune diseases
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
US9216988B2 (en) 2011-12-22 2015-12-22 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
CN104379559B (zh) 2012-04-27 2016-11-09 葛兰素集团有限公司 化合物
GB201207406D0 (en) 2012-04-27 2012-06-13 Glaxo Group Ltd Novel compounds
EP2844259A4 (en) 2012-04-30 2015-11-11 Anderson Gaweco MMR MODULATORS AND USES THEREOF
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
MX367341B (es) 2012-05-08 2019-08-14 Merck Sharp & Dohme Tetrahidronaftiridina y compuestos biciclicos relacionados para la inhibicion de la actividad de rorgamma y el tratamiento de enfermedades.
AU2013259904A1 (en) 2012-05-08 2014-10-02 Lycera Corporation Bicyclic sulfone compounds for inhibition of RORy activity and the treatment of disease
NZ702539A (en) 2012-05-31 2016-11-25 Phenex Pharmaceuticals Ag Carboxamide or sulfonamide substituted thiazoles and related derivatives as modulators for the orphan nuclear receptor ror[gamma]
WO2014008214A1 (en) 2012-07-02 2014-01-09 Biogen Idec Ma Inc. Biaryl-containing compounds as inverse agonists of ror-gamma receptors
AR092348A1 (es) 2012-07-11 2015-04-15 Hoffmann La Roche DERIVADOS DE ARIL-SULTAMO COMO MODULADORES DE RORc
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
WO2014026327A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 4-heteroaryl substituted benzoic acid 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
WO2014028669A1 (en) 2012-08-15 2014-02-20 Biogen Idec Ma Inc. Novel compounds for modulation of ror-gamma activity
WO2014026330A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 3-AMINOCYCLOALKYL COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
ES2623528T3 (es) 2012-09-21 2017-07-11 Sanofi Derivados de amida de ácido benzoimidazolcarboxílico para tratar enfermedades metabólicas o cardiovasculares
US9309222B2 (en) * 2012-10-16 2016-04-12 Janssen Pharmaceutica Nv Phenyl linked quinolinyl modulators of RORγt
WO2014062938A1 (en) 2012-10-19 2014-04-24 Bristol-Myers Squibb Company Rory modulators
AR093818A1 (es) 2012-12-06 2015-06-24 Glaxo Group Ltd Compuesto de 1-(bencil sustituido)piperazina sustituida
WO2013171729A2 (en) 2013-01-08 2013-11-21 Glenmark Pharmaceuticals S.A. Aryl and heteroaryl amide compounds as rorgamat modulator
WO2014179564A1 (en) 2013-05-01 2014-11-06 Vitae Pharmaceuticals, Inc. Thiazalopyrrolidine inhibitors of ror-gamma
TWI652014B (zh) 2013-09-13 2019-03-01 美商艾佛艾姆希公司 雜環取代之雙環唑殺蟲劑
BR112016008183A2 (pt) * 2013-10-15 2017-10-03 Janssen Pharmaceutica Nv Moduladores de ror-gama-t de quinolinila ligados à fenila
WO2015083130A1 (en) 2013-12-06 2015-06-11 Aurigene Discovery Technologies Limited Fused pyridine and pyrimidine derivatives as ror gamma modulators
CA2934819A1 (en) 2013-12-24 2015-07-02 President And Fellows Of Harvard College Cortistatin analogues and syntheses and uses thereof
JP2015124178A (ja) 2013-12-26 2015-07-06 東レ株式会社 環状アミン誘導体及びその医薬用途
WO2015101928A1 (en) 2013-12-31 2015-07-09 Aurigene Discovery Technologies Limited Fused thiophene and thiazole derivatives as ror gamma modulators
PE20161239A1 (es) 2014-02-03 2016-11-09 Basf Se Compuesto de ciclopenteno y ciclopentadieno para controlar plagas de invertebrados
EP3527569B1 (en) 2014-02-03 2021-08-25 Vitae Pharmaceuticals, LLC Dihydropyrrolopyridine inhibitors of ror-gamma for use in treating drye eye
WO2015139619A1 (zh) * 2014-03-18 2015-09-24 北京韩美药品有限公司 作为RORγ调节剂的化合物
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
MA39792B1 (fr) 2014-03-26 2019-12-31 Hoffmann La Roche Composés bicycliques en tant qu'inhibiteurs de production d'autotaxine (atx) et d'acide lysophosphatidique (lpa)
EP3122751B1 (en) 2014-03-26 2019-10-30 F.Hoffmann-La Roche Ag Condensed [1,4]diazepine compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors
BR112016020117B1 (pt) 2014-03-26 2020-03-17 Basf Se “compostos, composição e método para o combate dos fungos fitopatogênicos
WO2015145371A1 (en) * 2014-03-27 2015-10-01 Piramal Enterprises Limited Ror-gamma modulators and uses thereof
AP2016009542A0 (en) 2014-04-16 2016-11-30 Glenmark Pharmaceuticals Sa Aryl and heteroaryl ether compounds as ror gamma modulators
TWI675032B (zh) 2014-10-14 2019-10-21 美商維它藥物公司 ＲＯＲ-γ之二氫吡咯并吡啶抑制劑
EP3209299A4 (en) 2014-10-22 2018-04-04 The Board of Regents of The University of Texas System Small-molecule inhibitors targeting discoidin domain receptor 1 and uses thereof
US9845308B2 (en) 2014-11-05 2017-12-19 Vitae Pharmaceuticals, Inc. Isoindoline inhibitors of ROR-gamma
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
CN112608300B (zh) 2015-03-11 2024-04-26 Fmc公司 杂环取代的二环唑杀有害生物剂
ES2856931T3 (es) 2015-08-05 2021-09-28 Vitae Pharmaceuticals Llc Moduladores de ROR-gamma
EP3868750A1 (en) 2015-11-20 2021-08-25 Vitae Pharmaceuticals, LLC Modulators of ror-gamma
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
US9481674B1 (en) 2016-06-10 2016-11-01 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2261248C2 (ru) * 1999-06-23 2005-09-27 Авентис Фарма Дойчланд Гмбх Замещенные бензимидазолы и лекарственное средство на их основе
WO2009083526A1 (en) * 2008-01-02 2009-07-09 Smithkline Beecham Corporation Novel compounds
WO2013078240A1 (en) * 2011-11-22 2013-05-30 Ripka Amy S N-biphenylmethylbenzimidazole modulators of pparg
WO2013078233A1 (en) * 2011-11-22 2013-05-30 Ripka Amy S N-benzylbenzimidazole modulators of pparg

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
Sime, M. и др. "Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPARγ partial agonist", Bioorganic & Medicinal Chemistry Letters, 21(18), 2011, с.5568-5572 (doi:10.1016/j.bmcl.2011.06.088). *
Vourloumis, D. и др. "Solid-phase synthesis of benzimidazole libraries biased for RNA targets", Tetrahedron Letters, 44(14), 2003, с.2807-2811 (doi:10.1016/s0040-4039(03)00453-2). *
Yan, B. и др. "Quality Control in Combinatorial Chemistry: Determination of the Quantity, Purity, and Quantitative Purity of Compounds in Combinatorial Libraries", Journal of Combinatorial Chemistry, 5(5), 2003, с.547-559 (doi:10.1021/cc030008f). *
Yan, B. и др. "Quality Control in Combinatorial Chemistry: Determination of the Quantity, Purity, and Quantitative Purity of Compounds in Combinatorial Libraries", Journal of Combinatorial Chemistry, 5(5), 2003, с.547-559 (doi:10.1021/cc030008f). Vourloumis, D. и др. "Solid-phase synthesis of benzimidazole libraries biased for RNA targets", Tetrahedron Letters, 44(14), 2003, с.2807-2811 (doi:10.1016/s0040-4039(03)00453-2). *

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