EA201790202A1 - Фталазиноны и изохинолиноны в качестве ингибиторов rock - Google Patents

Фталазиноны и изохинолиноны в качестве ингибиторов rock

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Publication number
EA201790202A1
EA201790202A1 EA201790202A EA201790202A EA201790202A1 EA 201790202 A1 EA201790202 A1 EA 201790202A1 EA 201790202 A EA201790202 A EA 201790202A EA 201790202 A EA201790202 A EA 201790202A EA 201790202 A1 EA201790202 A1 EA 201790202A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
rock inhibitors
phthalasinones
isohinolinones
relates
Prior art date
Application number
EA201790202A
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English (en)
Other versions
EA033220B1 (ru
Inventor
Питер В. Гланц
Янь Цзоу
Мими Л. Кван
Владимир Ладзиата
Original Assignee
Бристол-Майерс Сквибб Компани
Priority date (The priority date 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 date listed.)
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Publication date
Application filed by Бристол-Майерс Сквибб Компани filed Critical Бристол-Майерс Сквибб Компани
Publication of EA201790202A1 publication Critical patent/EA201790202A1/ru
Publication of EA033220B1 publication Critical patent/EA033220B1/ru

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    • C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/30—Phthalazines
    • C07D237/32—Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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Abstract

Настоящее изобретение относится к соединениям формулы (I)или их стереоизомерам, таутомерам или фармацевтически приемлемым солям, где все переменные являются таковыми, как определено в данном описании. Эти соединения представляют собой селективные ROCK ингибиторы. Настоящее изобретение также относится к фармацевтическим композициям, содержащим эти соединения, и способам лечения сердечно-сосудистых, гладкой мускулатуры, онкологических, невропатологических, аутоиммунных, фиброзных и/или воспалительных заболеваний с их применением.
EA201790202A 2013-01-18 2014-01-17 Фталазиноны и изохинолиноны в качестве ингибиторов rock EA033220B1 (ru)

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Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201443023A (zh) 2013-01-18 2014-11-16 必治妥美雅史谷比公司 作爲ｒｏｃｋ抑制劑之酞□酮及異喹啉酮
US9828345B2 (en) 2013-02-28 2017-11-28 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors
AR094929A1 (es) 2013-02-28 2015-09-09 Bristol Myers Squibb Co Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2
US9902702B2 (en) * 2014-07-15 2018-02-27 Bristol-Myers Squibb Company Spirocycloheptanes as inhibitors of rock
WO2016028971A1 (en) 2014-08-21 2016-02-25 Bristol-Myers Squibb Company Tied-back benzamide derivatives as potent rock inhibitors
WO2016112236A1 (en) 2015-01-09 2016-07-14 Bristol-Myers Squibb Company Cyclic ureas as inhibitors of rock
US11072592B2 (en) 2015-02-27 2021-07-27 The Regents Of The University Of California Small molecules that enable cartilage rejuvenation
WO2016144936A1 (en) 2015-03-09 2016-09-15 Bristol-Myers Squibb Company Lactams as inhibitors of rock
CA3001484A1 (en) 2015-10-19 2017-04-27 Board Of Regents, The University Of Texas System Piperazinyl norbenzomorphan compounds and methods for using the same
CN105232542B (zh) * 2015-11-10 2016-03-30 王秀珍 一种治疗小儿肺炎的药物组合物
CN106928252B (zh) * 2015-12-31 2019-09-27 成都先导药物开发股份有限公司 一种抑制rock的化合物及其制备方法与应用
TWI730032B (zh) 2016-01-13 2021-06-11 美商必治妥美雅史谷比公司 作為ｒｏｃｋ抑制劑之螺庚烷水楊酸醯胺及相關化合物
CA3019145A1 (en) 2016-03-28 2017-10-05 Incyte Corporation Pyrrolotriazine compounds as tam inhibitors
EP3448520A4 (en) * 2016-04-29 2020-07-29 Board Of Regents, The University Of Texas System SIGMA RECEIVER BINDERS
ES2781309T3 (es) 2016-05-27 2020-09-01 Bristol Myers Squibb Co Triazolonas y tetrazolonas como inhibidores de ROCK
US10730858B2 (en) 2016-07-07 2020-08-04 Bristol-Myers Squibb Company Lactam, cyclic urea and carbamate, and triazolone derivatives as potent and selective rock inhibitors
JP7113810B2 (ja) 2016-07-07 2022-08-05 ブリストル－マイヤーズ スクイブ カンパニー Ｒｏｃｋ阻害剤としてのスピロラクタム
CN109661396B (zh) * 2016-07-07 2022-07-01 百时美施贵宝公司 作为rock抑制剂的螺稠合环状脲
JP7191826B2 (ja) 2016-11-30 2022-12-19 ブリストル－マイヤーズ スクイブ カンパニー 三環式ｒｈｏキナーゼ阻害剤
TW201908293A (zh) 2017-07-12 2019-03-01 美商必治妥美雅史谷比公司 作為rock抑制劑之5員及雙環雜環醯胺
JP7313331B2 (ja) 2017-07-12 2023-07-24 ブリストル－マイヤーズ スクイブ カンパニー Ｒｏｃｋ阻害剤としてのスピロヘプタニルヒダントイン
JP7234201B2 (ja) 2017-07-12 2023-03-07 ブリストル－マイヤーズ スクイブ カンパニー 心不全の治療のためのｒｏｃｋの５員アミノヘテロ環および５，６－または６，６員二環式アミノヘテロ環の阻害剤
JP7206253B2 (ja) 2017-07-12 2023-01-17 ブリストル－マイヤーズ スクイブ カンパニー Ｒｏｃｋ阻害剤としてのフェニルアセトアミド
ES2937039T3 (es) 2017-11-03 2023-03-23 Bristol Myers Squibb Co Inhibidores diazaespiro de ROCK
CN110041328A (zh) * 2019-05-22 2019-07-23 南京合巨药业有限公司 一种5-氟-1H-吡咯并[2,3-b]吡啶-3-羧酸的制备方法
UY39309A (es) 2020-07-02 2021-12-31 Pi Industries Ltd Compuestos de isoxazolina y su uso como agentes para el control de plagas
US11351149B2 (en) 2020-09-03 2022-06-07 Pfizer Inc. Nitrile-containing antiviral compounds
CN114106211A (zh) * 2021-08-31 2022-03-01 海南医学院 一种云南鸡油菌多糖及其分离纯化方法
WO2023037253A1 (en) 2021-09-08 2023-03-16 Pi Industries Ltd Isoxazoline compounds and their use as pest control agents
CA3238227A1 (en) 2021-11-11 2023-05-19 The Doshisha Cryopreservation preparation for corneal endothelial cells and method for producing said cryopreservation preparation
TW202411211A (zh) * 2022-05-25 2024-03-16 比利時魯汶大學 用於治療trpm3介導病症之新型衍生物
WO2023230542A2 (en) * 2022-05-25 2023-11-30 Katholieke Universiteit Leuven PYRAZOLO[1,5-a]PYRIDINE DERIVATIVES FOR TREATING TRPM3-MEDIATED DISORDERS

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2531776A1 (de) 1975-07-16 1977-02-03 Basf Ag Azopigmente mit einem phthalazonrest
GB8903130D0 (en) * 1989-02-11 1989-03-30 Orion Yhtymae Oy Substituted pyridazinones
TW245719B (ru) 1990-09-10 1995-04-21 Sterling Winthrop Inc
ATE124408T1 (de) 1990-10-16 1995-07-15 Takeda Chemical Industries Ltd Heterozyklische aminderivate, deren herstellung und deren verwendung.
EP0634402A1 (en) 1993-07-14 1995-01-18 Takeda Chemical Industries, Ltd. Isochinolinone derivatives, their production and use
AU6230098A (en) 1997-02-27 1998-09-18 Tanabe Seiyaku Co., Ltd. Isoquinolinone derivatives, process for preparing the same, and their use as phosphodiesterase inhibitors
DE19804085A1 (de) 1998-02-03 1999-08-05 Boehringer Ingelheim Pharma 5-Gliedrige heterocyclische kondensierte Benzoderivate, deren Herstellung und deren Verwendung als Arzneimittel
AU2720199A (en) 1998-02-03 1999-08-23 Boehringer Ingelheim Pharma Kg Five-membered, benzo-condensed heterocycles used as antithrombotic agents
JP2000072675A (ja) 1998-08-26 2000-03-07 Tanabe Seiyaku Co Ltd 医薬組成物
EP1148053A4 (en) 1999-01-26 2002-03-06 Ono Pharmaceutical Co 2H-PHTHALAZIN-1-ON DERIVATIVES AND DRUG COMPOSITIONS THAT CONTAIN THESE DERIVATIVES AS ACTIVE INGREDIENTS
DE19907813A1 (de) 1999-02-24 2000-08-31 Boehringer Ingelheim Pharma Substituierte bicyclische Heterocyclen, deren Herstellung und deren Verwendung als Arzneimittel
FI20000577A0 (fi) * 2000-03-13 2000-03-13 Orion Yhtymae Oy Pyridatsinyylifenyylihydratsoneja
KR100804564B1 (ko) * 2000-10-30 2008-02-20 쿠도스 파마슈티칼스 리미티드 프탈라지논 유도체
CA2476162A1 (en) 2002-02-13 2003-08-21 Takeda Chemical Industries, Ltd. Jnk inhibitor
JP2004043458A (ja) * 2002-05-22 2004-02-12 Kyorin Pharmaceut Co Ltd ４−アリール−５−ヒドロキシイソキノリン誘導体およびその製造法
AU2003264386A1 (en) 2002-09-10 2004-04-30 Kyorin Pharmaceutical Co., Ltd. 4-(substituted aryl)-5-hydroxyisoquinolinone derivative
JP2007008816A (ja) * 2003-10-15 2007-01-18 Ube Ind Ltd 新規イソキノリン誘導体
PE20060285A1 (es) 2004-03-30 2006-05-08 Aventis Pharma Inc Piridonas sustituidas como inhibidores de pol(adp-ribosa)-polimerasa (parp)
WO2006036981A2 (en) 2004-09-28 2006-04-06 Angion Biomedica Corp. Small molecule modulators of cytokine activity
WO2006124874A2 (en) * 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
RU2440988C2 (ru) * 2005-07-26 2012-01-27 Санофи-Авентис ПРОИЗВОДНЫЕ ЦИКЛОГЕКСИЛАМИНИЗОХИНОЛОНА В КАЧЕСТВЕ ИНГИБИТОРОВ Rho-КИНАЗЫ
WO2008036540A2 (en) 2006-09-20 2008-03-27 Boehringer Ingelheim International Gmbh Rho kinase inhibitors
CL2007003874A1 (es) 2007-01-03 2008-05-16 Boehringer Ingelheim Int Compuestos derivados de benzamida; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar enfermedades cardiovasculares, hipertension, aterosclerosis, reestenosis, ictus, insuficiencia cardiaca, lesion isquemica, hipertensio
ES2449482T3 (es) 2007-01-09 2014-03-19 Amgen Inc. Derivados de bis-aril-amida útiles para el tratamiento de cáncer
AU2008317417A1 (en) * 2007-10-22 2009-04-30 Angion Biomedica Corp. Small molecule inhibitors of PARP activity
US8193177B2 (en) 2007-11-13 2012-06-05 Angion Biomedica Corp. Hepatocyte growth factor pathway activators in fibrotic connective tissue diseases
US20120190668A1 (en) 2009-08-12 2012-07-26 Oehlen Lambertus J W M Enhancement of cellular transplantation using small moleucle modulators of hepatocyte growth factor (scatter factor) activity
BR112013012078A2 (pt) 2010-11-15 2019-09-24 Abbvie Inc inibidores de nampt e rock
CN102485721B (zh) 2010-12-03 2015-12-09 曹亚 取代的2,3-二氮杂萘酮化合物及其用途
CN102180909B (zh) 2011-03-18 2014-10-22 南京邮电大学 以酞嗪衍生物为配体的铱配合物磷光材料及其制备方法
TW201443023A (zh) 2013-01-18 2014-11-16 必治妥美雅史谷比公司 作爲ｒｏｃｋ抑制劑之酞□酮及異喹啉酮
CN103242647B (zh) 2013-04-27 2015-06-17 大连理工大学 一种阻燃耐热聚氨酯泡沫塑料及其制备方法

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