WO2008049919A2 - Inhibiteurs de kinase - Google Patents

Inhibiteurs de kinase Download PDF

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Publication number
WO2008049919A2
WO2008049919A2 PCT/EP2007/061542 EP2007061542W WO2008049919A2 WO 2008049919 A2 WO2008049919 A2 WO 2008049919A2 EP 2007061542 W EP2007061542 W EP 2007061542W WO 2008049919 A2 WO2008049919 A2 WO 2008049919A2
Authority
WO
WIPO (PCT)
Prior art keywords
alkyl
heteroaryl
aryl
heterocyclyl
cycloalkyl
Prior art date
Application number
PCT/EP2007/061542
Other languages
English (en)
Other versions
WO2008049919A3 (fr
Inventor
Olivier Defert
Dirk Leysen
Philippe Van Rompaey
Original Assignee
Devgen N.V.
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Filing date
Publication date
Application filed by Devgen N.V. filed Critical Devgen N.V.
Publication of WO2008049919A2 publication Critical patent/WO2008049919A2/fr
Publication of WO2008049919A3 publication Critical patent/WO2008049919A3/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems

Abstract

La présente invention concerne de nouveaux inhibiteurs des kinases de la famille AGC, en particulier des composés de formule (I) ou (II), ou un stéréoisomère, un tautomère, un racémique, un métabolite, un pro ou pré-médicament, un sel, un hydrate ou un solvate de ceux-ci, dans lesquelles R1, R2, R4, R5, R7, R8, q s, L et Y ont le sens défini dans les revendications. La présente invention concerne en particulier des inhibiteurs de la ROCK, des compositions, en particulier des produits pharmaceutiques, comprenant de tels inhibiteurs et des utilisations de tels inhibiteurs pour le traitement et la prophylaxie de maladies.
PCT/EP2007/061542 2006-10-26 2007-10-26 Inhibiteurs de kinase WO2008049919A2 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US85444506P 2006-10-26 2006-10-26
EP06447116 2006-10-26
US60/854,445 2006-10-26
EP06447116.2 2006-10-26

Publications (2)

Publication Number Publication Date
WO2008049919A2 true WO2008049919A2 (fr) 2008-05-02
WO2008049919A3 WO2008049919A3 (fr) 2008-07-03

Family

ID=39149206

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2007/061542 WO2008049919A2 (fr) 2006-10-26 2007-10-26 Inhibiteurs de kinase

Country Status (1)

Country Link
WO (1) WO2008049919A2 (fr)

Cited By (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7470787B2 (en) 2005-07-11 2008-12-30 Aerie Pharmaceuticals, Inc. Isoquinoline compounds
EP2009004A1 (fr) * 2006-04-18 2008-12-31 Japan Tobacco, Inc. Nouveau compose de piperazine et son utilisation en tant qu'inhibiteur de la polymerase du vhc
WO2011057784A1 (fr) * 2009-11-11 2011-05-19 Sygnis Bioscience Gmbh & Co. Kg Composés pour l'inhibition de la kinase pim et pour le traitement de malignité
WO2012146724A2 (fr) * 2011-04-29 2012-11-01 Amakem Nv Nouveaux inhibiteurs de rock
US8357699B2 (en) 2007-01-10 2013-01-22 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
US8394826B2 (en) 2009-05-01 2013-03-12 Aerie Pharmaceuticals, Inc. Dual mechanism inhibitors for the treatment of disease
US8450344B2 (en) 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
US8455514B2 (en) 2008-01-17 2013-06-04 Aerie Pharmaceuticals, Inc. 6-and 7-amino isoquinoline compounds and methods for making and using the same
EP2699546A1 (fr) * 2011-04-18 2014-02-26 Commonwealth Scientific & Industrial Research Organisation Procédé de capture de gaz
EP2802328A1 (fr) * 2012-01-09 2014-11-19 X-RX, Inc. Dérivés de tryptoline présentant une activité inhibitrice de kinase et utilisations de ceux-ci
WO2016003450A1 (fr) * 2014-07-01 2016-01-07 The Regents Of The University Of California Inhibiteurs de pkc-epsilon
CN105308031A (zh) * 2013-03-04 2016-02-03 加拿大高级医学研究协会 喹啉磺酰基衍生物及其用途
US9376423B2 (en) 2010-08-10 2016-06-28 The Regents Of The University Of California PKC-epsilon inhibitors
US9415043B2 (en) 2013-03-15 2016-08-16 Aerie Pharmaceuticals, Inc. Combination therapy
US9643927B1 (en) 2015-11-17 2017-05-09 Aerie Pharmaceuticals, Inc. Process for the preparation of kinase inhibitors and intermediates thereof
JP2017533244A (ja) * 2014-11-07 2017-11-09 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン ミオカルディン関連転写因子および血清応答因子（ｍｒｔｆ／ｓｒｆ）媒介性遺伝子転写の阻害剤ならびにその使用方法
CN107936003A (zh) * 2017-12-31 2018-04-20 佛山市赛维斯医药科技有限公司 一类含吡啶和噻吩结构的化合物、制备方法及其用途
CN107973777A (zh) * 2017-12-31 2018-05-01 佛山市赛维斯医药科技有限公司 一种含甲基萘和丙二醇噻吩酰胺类rock抑制剂及其用途
CN107973776A (zh) * 2017-12-31 2018-05-01 佛山市赛维斯医药科技有限公司 一种噻吩酰胺类结构化合物及其用途
CN108033954A (zh) * 2017-12-31 2018-05-15 佛山市赛维斯医药科技有限公司 一种含吡啶结构的化合物、制备方法及其用途
CN108033953A (zh) * 2017-12-31 2018-05-15 佛山市赛维斯医药科技有限公司 一类含吡啶和烷氧噻吩结构的化合物、制备方法及其用途
CN108047195A (zh) * 2017-12-31 2018-05-18 佛山市赛维斯医药科技有限公司 一种含丙二醇腈基噻吩酰胺类化合物及其用途
CN108047192A (zh) * 2017-12-31 2018-05-18 佛山市赛维斯医药科技有限公司 甲噻吩酰胺类结构化合物、其制备方法及用途
CN108047197A (zh) * 2017-12-31 2018-05-18 佛山市赛维斯医药科技有限公司 硝基噻吩酰胺rock抑制剂、制备方法及其用途
CN108047215A (zh) * 2017-12-31 2018-05-18 佛山市赛维斯医药科技有限公司 含吡啶结构的化合物、制备方法及其用途
CN108084149A (zh) * 2017-12-31 2018-05-29 佛山市赛维斯医药科技有限公司 含异丙基萘和丙二醇噻吩酰胺类化合物、制备方法及其用途
CN108101884A (zh) * 2017-12-31 2018-06-01 佛山市赛维斯医药科技有限公司 含噻吩酰胺结构衍生物、制备方法及其用途
CN108101885A (zh) * 2017-12-31 2018-06-01 佛山市赛维斯医药科技有限公司 含异丙胺和硝基噻吩酰胺类结构化合物、其制备方法及用途
CN108129449A (zh) * 2017-12-31 2018-06-08 佛山市赛维斯医药科技有限公司 一种含丙二醇噻吩酰胺类化合物、制备方法及其用途
CN108129452A (zh) * 2017-12-31 2018-06-08 佛山市赛维斯医药科技有限公司 一种含异丙基萘和丙二醇硝基噻吩酰胺类化合物及其用途
CN108129451A (zh) * 2017-12-31 2018-06-08 佛山市赛维斯医药科技有限公司 含丙二醇噻吩酰胺类化合物、制备方法及其用途
CN108129448A (zh) * 2017-12-31 2018-06-08 佛山市赛维斯医药科技有限公司 噻吩酰胺类rock抑制剂、制备方法及其用途
CN108129453A (zh) * 2017-12-31 2018-06-08 佛山市赛维斯医药科技有限公司 一种含甲基萘和丙二醇噻吩酰胺类结构的rock抑制剂
CN108129450A (zh) * 2017-12-31 2018-06-08 佛山市赛维斯医药科技有限公司 含烷氧噻吩酰胺和甲基萘结构的化合物、制备方法及其用途
CN108148042A (zh) * 2017-12-31 2018-06-12 佛山市赛维斯医药科技有限公司 一类噻吩酰胺rock抑制剂、制备方法及其用途
CN108191819A (zh) * 2017-12-31 2018-06-22 佛山市赛维斯医药科技有限公司 异丙胺噻吩酰胺类结构化合物、其制备方法及用途
CN108191821A (zh) * 2017-12-31 2018-06-22 佛山市赛维斯医药科技有限公司 一种含甲基萘和腈基噻吩酰胺类结构的rock抑制剂及用途
CN108218829A (zh) * 2017-12-31 2018-06-29 佛山市赛维斯医药科技有限公司 一种噻吩酰胺类rock抑制剂、制备方法及其用途
CN108558823A (zh) * 2017-12-31 2018-09-21 佛山市赛维斯医药科技有限公司 一类腈基噻吩酰胺rock抑制剂、制备方法及其用途
US10550087B2 (en) 2015-11-17 2020-02-04 Aerie Pharmaceuticals, Inc. Process for the preparation of kinase inhibitors and intermediates thereof
WO2020047229A1 (fr) 2018-08-29 2020-03-05 University Of Massachusetts Inhibition de protéines kinases pour traiter la maladie de friedreich
US10624882B2 (en) 2006-09-20 2020-04-21 Aerie Pharmaceuticals, Inc. Rho kinase inhibitors
US10800745B2 (en) * 2017-08-18 2020-10-13 Purdue Research Foundation Methods for 1,4-diazo n-heterocycle synthesis
US10858339B2 (en) 2017-03-31 2020-12-08 Aerie Pharmaceuticals, Inc. Aryl cyclopropyl-amino-isoquinolinyl amide compounds
US11389441B2 (en) 2016-08-31 2022-07-19 Aerie Pharmaceuticals, Inc. Ophthalmic compositions
US11427563B2 (en) 2018-09-14 2022-08-30 Aerie Pharmaceuticals, Inc. Aryl cyclopropyl-amino-isoquinolinyl amide compounds

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CN107915717A (zh) * 2017-12-31 2018-04-17 佛山市赛维斯医药科技有限公司 一类含异丙基萘和丙二醇噻吩酰胺类化合物及其用途
CN108047193A (zh) * 2017-12-31 2018-05-18 佛山市赛维斯医药科技有限公司 烷氧噻吩酰胺类rock抑制剂、制备方法及其用途
CN108191820A (zh) * 2017-12-31 2018-06-22 佛山市赛维斯医药科技有限公司 一种含异丙胺和噻吩酰胺类结构的化合物
CN107903250A (zh) * 2017-12-31 2018-04-13 佛山市赛维斯医药科技有限公司 一种含吡啶和硝基噻吩结构的化合物、制备方法及其用途
CN108047214A (zh) * 2017-12-31 2018-05-18 佛山市赛维斯医药科技有限公司 一种含吡啶和硝基噻吩结构化合物及其用途
CN107935986A (zh) * 2017-12-31 2018-04-20 佛山市赛维斯医药科技有限公司 异丙胺和卤代噻吩酰胺类结构化合物、其制备方法及用途
CN107935987A (zh) * 2017-12-31 2018-04-20 佛山市赛维斯医药科技有限公司 含甲基萘和噻吩酰胺结构的rock抑制剂、制备方法及其用途

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Cited By (98)

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US8455647B2 (en) 2005-07-11 2013-06-04 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
US7671205B2 (en) 2005-07-11 2010-03-02 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
US7470787B2 (en) 2005-07-11 2008-12-30 Aerie Pharmaceuticals, Inc. Isoquinoline compounds
US8034943B2 (en) 2005-07-11 2011-10-11 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
EP2009004A1 (fr) * 2006-04-18 2008-12-31 Japan Tobacco, Inc. Nouveau compose de piperazine et son utilisation en tant qu'inhibiteur de la polymerase du vhc
EP2009004A4 (fr) * 2006-04-18 2010-08-25 Japan Tobacco Inc Nouveau compose de piperazine et son utilisation en tant qu'inhibiteur de la polymerase du vhc
US8017612B2 (en) 2006-04-18 2011-09-13 Japan Tobacco Inc. Piperazine compound and use thereof as a HCV polymerase inhibitor
US10624882B2 (en) 2006-09-20 2020-04-21 Aerie Pharmaceuticals, Inc. Rho kinase inhibitors
US9365518B2 (en) 2007-01-10 2016-06-14 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
US8921392B2 (en) 2007-01-10 2014-12-30 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
US8357699B2 (en) 2007-01-10 2013-01-22 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
US9890123B2 (en) 2007-01-10 2018-02-13 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
US10899714B2 (en) 2007-01-10 2021-01-26 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
US10472327B2 (en) 2007-01-10 2019-11-12 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
US8455513B2 (en) 2007-01-10 2013-06-04 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
US8455514B2 (en) 2008-01-17 2013-06-04 Aerie Pharmaceuticals, Inc. 6-and 7-amino isoquinoline compounds and methods for making and using the same
US8871757B2 (en) 2008-01-17 2014-10-28 Aerie Pharmaceuticals, Inc. 6-and 7-amino isoquinoline compounds and methods for making and using the same
US10882840B2 (en) 2008-07-25 2021-01-05 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
US8450344B2 (en) 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
US11021456B2 (en) 2008-07-25 2021-06-01 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
US10112920B2 (en) 2008-07-25 2018-10-30 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
US9884840B2 (en) 2008-07-25 2018-02-06 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
US10532993B2 (en) 2008-07-25 2020-01-14 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
US9512101B2 (en) 2008-07-25 2016-12-06 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
US11618748B2 (en) 2009-05-01 2023-04-04 Aerie Pharmaceuticals, Inc. Dual mechanism inhibitors for the treatment of disease
US10316029B2 (en) 2009-05-01 2019-06-11 Aerie Pharmaceuticals, Inc. Dual mechanism inhibitors for the treatment of disease
US10174017B2 (en) 2009-05-01 2019-01-08 Aerie Pharmaceuticals, Inc. Dual mechanism inhibitors for the treatment of disease
US9951059B2 (en) 2009-05-01 2018-04-24 Aerie Pharmaceuticals, Inc. Dual mechanism inhibitors for the treatment of disease
US10654844B2 (en) 2009-05-01 2020-05-19 Aerie Pharmaceuticals, Inc. Dual mechanism inhibitors for the treatment of disease
US8394826B2 (en) 2009-05-01 2013-03-12 Aerie Pharmaceuticals, Inc. Dual mechanism inhibitors for the treatment of disease
US11028081B2 (en) 2009-05-01 2021-06-08 Aerie Pharmaceuticals, Inc. Dual mechanism inhibitors for the treatment of disease
EP2332917A1 (fr) * 2009-11-11 2011-06-15 Sygnis Bioscience GmbH & Co. KG Composés pour l'inhibition de kinase PIM et pour le traitement des tumeurs
WO2011057784A1 (fr) * 2009-11-11 2011-05-19 Sygnis Bioscience Gmbh & Co. Kg Composés pour l'inhibition de la kinase pim et pour le traitement de malignité
US9376423B2 (en) 2010-08-10 2016-06-28 The Regents Of The University Of California PKC-epsilon inhibitors
EP2699546A1 (fr) * 2011-04-18 2014-02-26 Commonwealth Scientific & Industrial Research Organisation Procédé de capture de gaz
US9409122B2 (en) 2011-04-18 2016-08-09 Commonwealth Scientific And Industrial Research Organisation Gas capture process
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