JP5847830B2 - オレキシン受容体拮抗薬として有用なラクタム誘導体 - Google Patents

オレキシン受容体拮抗薬として有用なラクタム誘導体 Download PDF

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JP5847830B2
JP5847830B2 JP2013538312A JP2013538312A JP5847830B2 JP 5847830 B2 JP5847830 B2 JP 5847830B2 JP 2013538312 A JP2013538312 A JP 2013538312A JP 2013538312 A JP2013538312 A JP 2013538312A JP 5847830 B2 JP5847830 B2 JP 5847830B2
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dimethoxyphenyl
benzyl
methyl
piperidin
pyrrolidin
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JP2013545744A5 (https=
JP2013545744A (ja
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アイサオウイ ハメッド
アイサオウイ ハメッド
クリストフ ボス
ボス クリストフ
ブロッチ クリスティーン
ブロッチ クリスティーン
ハイドマン ビビア
ハイドマン ビビア
シファーレン ティエリー
シファーレン ティエリー
ティー ウィリアムズ ジョディ
ティー ウィリアムズ ジョディ
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Actelion Pharmaceuticals Ltd
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Actelion Pharmaceuticals Ltd
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  • Anesthesiology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
JP2013538312A 2010-11-10 2011-11-09 オレキシン受容体拮抗薬として有用なラクタム誘導体 Expired - Fee Related JP5847830B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IB2010055105 2010-11-10
IBPCT/IB2010/055105 2010-11-10
PCT/IB2011/054993 WO2012063207A1 (en) 2010-11-10 2011-11-09 Lactam derivatives useful as orexin receptor antagonists

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JP2013545744A JP2013545744A (ja) 2013-12-26
JP2013545744A5 JP2013545744A5 (https=) 2014-12-11
JP5847830B2 true JP5847830B2 (ja) 2016-01-27

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US (1) US9242970B2 (https=)
EP (1) EP2638008B1 (https=)
JP (1) JP5847830B2 (https=)
CN (1) CN103201261A (https=)
CA (1) CA2815179A1 (https=)
WO (1) WO2012063207A1 (https=)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
ES2617863T3 (es) 2012-06-04 2017-06-20 Actelion Pharmaceuticals Ltd. Derivados de bencimidazol-prolina
RS58514B1 (sr) 2012-06-13 2019-04-30 Incyte Holdings Corp Supstituisana triciklična jedinjenja kao inhibitori fgfr
CN107802623B (zh) 2012-07-19 2020-10-30 开曼化学股份有限公司 用于ep4介导的骨相关疾病和病症的二氟内酰胺组合物
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
CA2894399A1 (en) 2012-12-06 2014-06-12 Quanticel Pharmaceuticals, Inc. Histone demethylase inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
JP6368351B2 (ja) 2013-03-15 2018-08-01 ケイマン ケミカル カンパニー, インコーポレーテッド ジフルオロラクタムアナログを合成する方法
EP3235817B1 (en) 2013-03-15 2018-12-12 Cayman Chemical Company, Incorporated Lactam compounds as ep4 receptor-selective agonists for use in the treatment of ep4-mediated diseases and conditions
WO2014144610A1 (en) 2013-03-15 2014-09-18 Cayman Chemical Company, Inc. Lactam compounds as ep4 receptor-selective agonists for use in the treatment of ep4-mediated diseases and conditions
PH12015502383B1 (en) 2013-04-19 2023-02-03 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
CN104133004A (zh) * 2013-05-03 2014-11-05 上海美迪西生物医药有限公司 血浆样品中2,3-吲哚醌的浓度的测定方法
JP2016527006A (ja) 2013-07-19 2016-09-08 ケイマン ケミカル カンパニー, インコーポレーテッド 骨成長を促進するための方法、システム、及び組成物
UA119151C2 (uk) 2013-12-03 2019-05-10 Ідорсія Фармасьютікалз Лтд КРИСТАЛІЧНА СОЛЬОВА ФОРМА (S)-(2-(6-ХЛОР-7-МЕТИЛ-1H-БЕНЗО[d]ІМІДАЗОЛ-2-ІЛ)-2-МЕТИЛПІРОЛІДИН-1-ІЛ)(5-МЕТОКСИ-2-(2H-1,2,3-ТРИАЗОЛ-2-ІЛ)ФЕНІЛ)МЕТАНОНУ ЯК АНТАГОНІСТ ОРЕКСИНОВОГО РЕЦЕПТОРА
MY179862A (en) 2013-12-03 2020-11-18 Idorsia Pharmaceuticals Ltd Crystalline form of (s)-(2-(6-chloro-7-methyl-1h-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1 -yl)(5-methoxy-2-(2h-1,2,3-triazol-2-yl)phenyl)methanone and its use as orexin receptor antagonists
SI3077391T1 (sl) 2013-12-04 2018-11-30 Idorsia Pharmaceuticals Ltd Uporaba benzimidazol-prolinskih derivatov
WO2015088864A1 (en) * 2013-12-09 2015-06-18 Merck Sharp & Dohme Corp. 2-pyridyloxy-3-ester-4-ether orexin receptor antagonists
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
TWI712601B (zh) 2015-02-20 2020-12-11 美商英塞特公司 作為fgfr抑制劑之雙環雜環
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
EP3472129A4 (en) * 2016-06-21 2019-12-04 X4 Pharmaceuticals, Inc. CXCR4 INHIBITORS AND USES THEREOF
ES2870920T3 (es) 2016-06-21 2021-10-28 X4 Pharmaceuticals Inc Inhibidores de CXCR4 y usos de los mismos
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
TWI799435B (zh) * 2017-08-02 2023-04-21 美商維泰克斯製藥公司 製備化合物之製程
HRP20241288T1 (hr) 2018-05-04 2024-12-06 Incyte Corporation Čvrsti oblici fgfr inhibitora i postupci za njihovu proizvodnju
AU2019262579B2 (en) 2018-05-04 2024-09-12 Incyte Corporation Salts of an FGFR inhibitor
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CN110563565A (zh) * 2019-09-02 2019-12-13 南通大学 一种3-溴-6-氟-2-甲氧基苯甲醛的合成方法
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3157361A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
JP7832891B2 (ja) 2019-12-04 2026-03-18 インサイト・コーポレイション Fgfr阻害剤の誘導体
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2022221170A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
CN114456184B (zh) * 2022-02-21 2023-08-22 南华大学附属第一医院 一种3-芳基异喹啉衍生物及其制备与应用
CN115047127B (zh) * 2022-04-25 2024-03-08 中国检验检疫科学研究院 一种利用挥发性代谢组学技术鉴别nfc和fc橙汁的方法
TW202409023A (zh) 2022-07-14 2024-03-01 美商富曼西公司 除草苯并𠯤
WO2025111184A1 (en) 2023-11-21 2025-05-30 Fmc Corporation Substituted tetrahydroquinoline and tetrahydroquinoxaline herbicides
WO2025224168A1 (en) 2024-04-24 2025-10-30 Idorsia Pharmaceuticals Ltd Aryl sulfone and sulfanone derivatives as orexin receptor modulators

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0115862D0 (en) * 2001-06-28 2001-08-22 Smithkline Beecham Plc Compounds
EP1537089A4 (en) * 2002-07-23 2008-04-16 Cytokinetics Inc CONNECTIONS, COMPOSITIONS AND PROCEDURES
CA2557163C (en) 2004-03-01 2011-08-16 Idorsia Pharmaceuticals Ltd Substituted 1,2,3,4-tetrahydroisoquinoline derivatives
WO2006127550A1 (en) * 2005-05-23 2006-11-30 Merck & Co., Inc. Proline bis-amide orexin receptor antagonists
AU2007226203A1 (en) 2006-03-15 2007-09-20 Actelion Pharmaceuticals Ltd Tetrahydroisoquinoline derivatives to enhance memory function
JP2010500401A (ja) * 2006-08-15 2010-01-07 アクテリオン ファーマシューティカルズ リミテッド アゼチジン化合物
JP2010504957A (ja) * 2006-09-29 2010-02-18 アクテリオン ファーマシューティカルズ リミテッド 3−アザ−ビシクロ[3.1.0]ヘキサン誘導体
CL2008000836A1 (es) * 2007-03-26 2008-11-07 Actelion Pharmaceuticals Ltd Compuestos derivados de tiazolidina, antagonistas del receptor de orexina; composicion farmaceutica que los comprende; y su uso en el tratamiento de neurosis emocional, depresion grave, trastornos psicoticos, alzheimer, parkinson, dolor, entre otras.
BRPI0812981A2 (pt) * 2007-07-03 2014-12-16 Glaxo Group Ltd Derivados de piperidina úteis como antagonistas dos receptores de orexina
KR20100055464A (ko) * 2007-08-15 2010-05-26 액테리온 파마슈티칼 리미티드 오렉신 길항제로서의 1,2-디아미도-에틸렌 유도체
JP2010540429A (ja) * 2007-09-24 2010-12-24 アクテリオン ファーマシューティカルズ リミテッド オレキシン受容体拮抗薬としてのピロリジン類及びピペリジン類
PE20091010A1 (es) 2007-10-10 2009-08-08 Actelion Pharmaceuticals Ltd Derivados de tetrahidroquinolina
US20110039857A1 (en) * 2008-04-30 2011-02-17 Hamed Aissaoui Piperidine and pyroolidine compounds
CA2726102A1 (en) * 2008-06-11 2009-12-17 Actelion Pharmaceuticals Ltd Tetrazole compounds as orexin receptor antagonists
WO2010048014A1 (en) * 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. 2,4-disubstituted pyrrolidine orexin receptor antagonists
US20120088759A1 (en) 2009-05-12 2012-04-12 Hamed Aissaoui Thiazolidin-4-one and [1,3]-thiazinan-4-one compounds as orexin receptor antagonists
CA2758675A1 (en) 2009-05-12 2010-11-18 Actelion Pharmaceuticals Ltd Oxazolidinone derivatives

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