CN109952289B - Trpv4拮抗剂 - Google Patents

Trpv4拮抗剂 Download PDF

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Publication number
CN109952289B
CN109952289B CN201780057993.8A CN201780057993A CN109952289B CN 109952289 B CN109952289 B CN 109952289B CN 201780057993 A CN201780057993 A CN 201780057993A CN 109952289 B CN109952289 B CN 109952289B
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sulfonyl
hydroxy
hydroxymethyl
oxy
pyrrolidin
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CN201780057993.8A
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Chinese (zh)
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CN109952289A (zh
Inventor
E.J.伯纳尔迪克
C.A.布鲁克斯
B.G.拉夫霍恩
G.叶
L.S.巴顿
B.W.布德齐克
J.M.马修斯
J.J.麦卡蒂
J.R.帕特森
J.E.佩罗
R.桑切兹
M.R.森德尔
L.R.特雷尔
D.J.贝姆
J.V.托马斯
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GlaxoSmithKline LLC
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GlaxoSmithKline LLC
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Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10590077B2 (en) 2016-09-20 2020-03-17 Glaxosmithkline Intellectual Property Development Limited TRPV4 antagonists
JP7106528B2 (ja) 2016-09-20 2022-07-26 グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー2)、リミテッド Trpv4拮抗薬
TW201825458A (zh) * 2016-09-20 2018-07-16 英商葛蘭素史克智慧財產(第二)有限公司 Trpv4拮抗劑
CN108836972A (zh) * 2018-08-16 2018-11-20 青岛大学 Ws6对trp通道的作用
JP6994061B2 (ja) 2019-02-15 2022-01-14 ノバルティス アーゲー 4-(7-ヒドロキシ-2-イソプロピル-4-オキソ-4h-キナゾリン-3-イル)-ベンゾニトリルの製剤
JOP20210217A1 (ar) 2019-02-15 2023-01-30 Novartis Ag طرق لعلاج ألم سطح عين
CA3157279A1 (en) * 2019-11-21 2021-05-27 Paul Richard Sebahar Trpv4 receptor ligands
CN115427409B (zh) 2020-04-30 2025-02-25 拉夸里亚创药株式会社 作为trpv4拮抗剂的嘧啶-4(3h)-酮衍生物
WO2021233752A1 (en) 2020-05-19 2021-11-25 Bayer Aktiengesellschaft Trpa1 antagonists for the treatment of diseases associated with pain and inflammation
CA3185968A1 (en) 2020-07-13 2022-01-20 Tony Lahoutte Antibody fragment against folr1
TW202216143A (zh) 2020-07-16 2022-05-01 日商拉夸里亞創藥股份有限公司 作為眼疾病的治療藥之trpv4抑制藥
CN112574090B (zh) * 2020-11-23 2022-04-29 浙大城市学院 一种含硫的多取代吡咯类化合物及其制备方法
WO2023203135A1 (en) 2022-04-22 2023-10-26 Precirix N.V. Improved radiolabelled antibody
IL318992A (en) 2022-05-02 2025-04-01 Precirix N V Cancer treatment through advance directives

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007082262A2 (en) * 2006-01-11 2007-07-19 Smithkline Beecham Corporation Novel compounds
CN103896946A (zh) * 2012-12-28 2014-07-02 浙江导明医药科技有限公司 用于预防及治疗多种自身免疫疾病的新化合物

Family Cites Families (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2064336B (en) 1979-12-06 1984-03-14 Glaxo Group Ltd Device for dispensing medicaments
DE3274065D1 (de) 1981-07-08 1986-12-11 Draco Ab Powder inhalator
GB2169265B (en) 1982-10-08 1987-08-12 Glaxo Group Ltd Pack for medicament
US4778054A (en) 1982-10-08 1988-10-18 Glaxo Group Limited Pack for administering medicaments to patients
ES286422Y (es) 1982-10-08 1986-09-16 Glaxo Group Limited Dispositivo para administrar medicamentos a pacientes
AT396872B (de) 1985-07-30 1993-12-27 Glaxo Group Ltd Gerät zur verabreichung von medikamenten in pulverform
US6536427B2 (en) 1990-03-02 2003-03-25 Glaxo Group Limited Inhalation device
SK280967B6 (sk) 1990-03-02 2000-10-09 Glaxo Group Limited Inhalačný prístroj
GB9004781D0 (en) 1990-03-02 1990-04-25 Glaxo Group Ltd Device
SK25099A3 (en) 1996-08-28 2000-02-14 Procter & Gamble Substituted cyclic amine metalloprotease inhibitors
GB9700226D0 (en) 1997-01-08 1997-02-26 Glaxo Group Ltd Inhalation device
DE60233163D1 (de) 2001-12-06 2009-09-10 Cornell Res Foundation Inc Katalytische carbonylierung von drei- und viergliedrigen heterocyklen
GB0201677D0 (en) 2002-01-25 2002-03-13 Glaxo Group Ltd Medicament dispenser
ATE524452T1 (de) 2003-03-27 2011-09-15 Cytokinetics Inc Sulfonamide zur behandlung von kongestivem herzversagen, deren zusammensetzungen und verwendungen.
GB0317374D0 (en) 2003-07-24 2003-08-27 Glaxo Group Ltd Medicament dispenser
KR101105909B1 (ko) 2004-02-16 2012-01-17 글락소 그룹 리미티드 약품 분배기에 사용되는 카운터
AR048523A1 (es) 2004-04-07 2006-05-03 Kalypsys Inc Compuestos con estructura de aril sulfonamida y sulfonilo como moduladores de ppar y metodos para tratar trastornos metabolicos
US7566726B2 (en) 2004-04-28 2009-07-28 Merck & Co. Inc. 3,3-disubstituted tetrahydropyranyl cyclopentyl amide modulators of chemokine receptor activity
EP1758884A2 (en) 2004-05-20 2007-03-07 Elan Pharmaceuticals, Inc. N-cyclic sulfonamido inhibitors of gamma secretase
CN1329374C (zh) 2004-06-09 2007-08-01 上海靶点药物有限公司 作为ccr5拮抗剂的化合物
US20080064736A1 (en) 2004-07-12 2008-03-13 Bayer Cropscience Ag Substituted 2-Pyrrolidone Derivatives as Fungicides and Insecticides
GB0418278D0 (en) 2004-08-16 2004-09-15 Glaxo Group Ltd Medicament dispenser
DOP2006000010A (es) 2005-01-10 2006-07-31 Arena Pharm Inc Procedimiento para preparar eteres aromáticos
GB0515584D0 (en) 2005-07-28 2005-09-07 Glaxo Group Ltd Medicament dispenser
AR058289A1 (es) 2005-12-12 2008-01-30 Glaxo Group Ltd Colector para ser usado en dispensador de medicamento
KR20080080201A (ko) 2005-12-21 2008-09-02 쉐링 코포레이션 히스타민 h3 길항제로서 유용한 치환된 아닐린 유도체
WO2008005268A1 (en) 2006-06-30 2008-01-10 Schering Corporation Substituted piperidines that increase p53 activity and the uses thereof
US20080176861A1 (en) 2007-01-23 2008-07-24 Kalypsys, Inc. Sulfonyl-substituted bicyclic compounds as ppar modulators for the treatment of non-alcoholic steatohepatitis
EP2244571A4 (en) 2008-01-17 2014-02-19 Purdue Research Foundation SMALL MOLECULAR INHIBITORS OF HIV PROTEASES
DE102008008838A1 (de) * 2008-02-13 2009-08-20 Bayer Healthcare Ag Cycloalkoxy-substituierte 4-Phenyl-3,5-dicyanopyridine und ihre Verwendung
AU2009271414A1 (en) 2008-06-20 2010-01-21 Metabolex, Inc. Aryl GPR119 agonists and uses thereof
ES2605856T3 (es) 2012-11-16 2017-03-16 Bristol-Myers Squibb Company Moduladores GPR40 de dihidropirazol
AU2014239542A1 (en) 2013-03-15 2015-10-01 Araxes Pharma Llc Covalent inhibitors of KRas G12C
CN105209457A (zh) 2013-03-15 2015-12-30 艾伯维德国有限责任两合公司 吡咯烷衍生物,含有其的药物组合物及其在治疗中的用途
WO2014163161A1 (ja) 2013-04-04 2014-10-09 武田薬品工業株式会社 複素環化合物
BR112017002001B1 (pt) 2014-07-31 2022-10-25 INSERM (Institut National de la Santé et de la Recherche Médicale) Compostos e composição farmacêutica
JP7106528B2 (ja) 2016-09-20 2022-07-26 グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー2)、リミテッド Trpv4拮抗薬
TW201825458A (zh) * 2016-09-20 2018-07-16 英商葛蘭素史克智慧財產(第二)有限公司 Trpv4拮抗劑
US10590077B2 (en) 2016-09-20 2020-03-17 Glaxosmithkline Intellectual Property Development Limited TRPV4 antagonists

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007082262A2 (en) * 2006-01-11 2007-07-19 Smithkline Beecham Corporation Novel compounds
CN103896946A (zh) * 2012-12-28 2014-07-02 浙江导明医药科技有限公司 用于预防及治疗多种自身免疫疾病的新化合物

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Copper(II)-Catalyzed Monoarylation of Vicinal Diols with Diaryliodonium Salts;Masami Kuriyama等;《CHEMISTRY》;20121231;第18卷(第6期);表3 *
Identification of false positives in "HTS hits to lead": The application of Bayesian models in HTS triage to rapidly deliver a series of selective TRPV4 antagonists;Sarah E. Skerratt等;《MedChemComm》;20131231;第4卷(第1期);图3,表1 *

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