JP5769326B2 - Ｒｈｏキナーゼ阻害薬 - Google Patents

Ｒｈｏキナーゼ阻害薬 Download PDF

Info

Publication number
JP5769326B2
JP5769326B2 JP2013534982A JP2013534982A JP5769326B2 JP 5769326 B2 JP5769326 B2 JP 5769326B2 JP 2013534982 A JP2013534982 A JP 2013534982A JP 2013534982 A JP2013534982 A JP 2013534982A JP 5769326 B2 JP5769326 B2 JP 5769326B2
Authority
JP
Japan
Prior art keywords
compound
cyano
phenyl
ylmethyl
mmol
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
JP2013534982A
Other languages
English (en)
Japanese (ja)
Other versions
JP2013544797A5 (enExample
JP2013544797A (ja
Inventor
ジュニア トーマス マーティン カーレーン
ジュニア トーマス マーティン カーレーン
ダニエル リチャード マーシャル
ダニエル リチャード マーシャル
ロバート シブリー
ロバート シブリー
スノー　ロジャー　ジョン
ロジャー ジョン スノー
ファリバ ソレイマンザデー
ファリバ ソレイマンザデー
ロナルド ジョン ソルセク
ロナルド ジョン ソルセク
Original Assignee
ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
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.)
Filing date
Publication date
Application filed by ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング, ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング filed Critical ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
Publication of JP2013544797A publication Critical patent/JP2013544797A/ja
Publication of JP2013544797A5 publication Critical patent/JP2013544797A5/ja
Application granted granted Critical
Publication of JP5769326B2 publication Critical patent/JP5769326B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2013534982A 2010-10-19 2011-10-17 Ｒｈｏキナーゼ阻害薬 Active JP5769326B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US39441410P 2010-10-19 2010-10-19
US61/394,414 2010-10-19
PCT/US2011/056505 WO2012054367A1 (en) 2010-10-19 2011-10-17 Rho kinase inhibitors

Publications (3)

Publication Number Publication Date
JP2013544797A JP2013544797A (ja) 2013-12-19
JP2013544797A5 JP2013544797A5 (enExample) 2014-12-04
JP5769326B2 true JP5769326B2 (ja) 2015-08-26

Family

ID=44898209

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2013534982A Active JP5769326B2 (ja) 2010-10-19 2011-10-17 Ｒｈｏキナーゼ阻害薬

Country Status (4)

Country Link
US (1) US9000154B2 (enExample)
EP (1) EP2630144B1 (enExample)
JP (1) JP5769326B2 (enExample)
WO (1) WO2012054367A1 (enExample)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8697911B2 (en) 2010-07-07 2014-04-15 Boehringer Ingelheim International Gmbh Rho kinase inhibitors
US9079880B2 (en) 2010-07-07 2015-07-14 Boehringer Ingelheim International Gmbh Rho kinase inhibitors
EP2630144B1 (en) 2010-10-19 2016-09-07 Boehringer Ingelheim International GmbH Rho kinase inhibitors
US9499553B2 (en) 2013-03-13 2016-11-22 Chugai Seiyaku Kabushiki Kaisha Dihydropyridazine-3,5-dione derivative and pharmaceuticals containing the same
TW201506024A (zh) * 2013-07-02 2015-02-16 必治妥美雅史谷比公司 作為有效ｒｏｃｋ抑制劑的三環甲醯胺衍生物
JP6522602B2 (ja) * 2013-07-02 2019-05-29 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｒｏｃｋ阻害剤としての三環式ピリド−カルボキサミド誘導体
AR103990A1 (es) * 2015-01-09 2017-06-21 Bristol Myers Squibb Co Ureas cíclicas como inhibidoras de rock
JP6883173B2 (ja) 2015-05-12 2021-06-09 ヘモストッド エスエー 改善された血小板産生のための薬理学的特徴およびマイクロ流体特徴の組み合わせ
US12281308B2 (en) 2018-08-29 2025-04-22 University Of Massachusetts Inhibition of protein kinases to treat Friedreich ataxia

Family Cites Families (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5210208A (en) 1990-09-24 1993-05-11 Rhone-Poulenc Rorer Pharmaceuticals Inc. Disubstituted aryl compounds exhibiting selective leukotriene b4 antagonist activity
NZ240863A (en) 1991-09-11 1995-04-27 Mcneilab Inc Substituted 4-aryl piperidine and 4-aryl piperazine derivatives, preparation and pharmaceutical compositions thereof
JPH11130751A (ja) 1997-10-30 1999-05-18 Yoshitomi Pharmaceut Ind Ltd アミド化合物およびそれらの酸付加塩の標識化合物
US7217722B2 (en) 2000-02-01 2007-05-15 Kirin Beer Kabushiki Kaisha Nitrogen-containing compounds having kinase inhibitory activity and drugs containing the same
CZ2003182A3 (cs) * 2000-06-21 2003-06-18 F. Hoffmann-La Roche Ag Deriváty benzothiazolu
EP1339668A2 (en) 2000-11-28 2003-09-03 Guilford Pharmaceuticals Inc. Bisubstituted carbocyclic cyclophilin binding compounds and theirus
DE10112768A1 (de) 2001-03-16 2002-09-19 Merck Patent Gmbh Phenylderivate 3
US7199147B2 (en) 2001-06-12 2007-04-03 Dainippon Sumitomo Pharma Co., Ltd. Rho kinase inhibitors
SE0102764D0 (sv) * 2001-08-17 2001-08-17 Astrazeneca Ab Compounds
JP2003321472A (ja) * 2002-02-26 2003-11-11 Takeda Chem Ind Ltd Ｇｒｋ阻害剤
WO2004071448A2 (en) 2003-02-12 2004-08-26 Transtech Pharma Inc. Substituted azole derivatives as inhibitors of protein tyrosine phosphatases
WO2004076420A1 (ja) * 2003-02-26 2004-09-10 Banyu Pharmaceutical Co., Ltd. ヘテロアリールカルバモイルベンゼン誘導体
WO2004101529A1 (ja) * 2003-05-19 2004-11-25 Ono Pharmaceutical Co., Ltd. 含窒素複素環化合物およびその医薬用途
FR2862965B1 (fr) 2003-11-27 2007-09-07 Merck Sante Sas Nouveaux derives de phenoxyacetamides et leur utilisation pour la preparation de diphenylamides.
US8071603B2 (en) 2004-09-20 2011-12-06 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
AU2005305140A1 (en) 2004-11-04 2006-05-18 Neurogen Corporation Arylalkyl ureas as CB1 antagonists
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
ES2580108T3 (es) 2005-07-11 2016-08-19 Aerie Pharmaceuticals, Inc Compuestos de isoquinolina
CA2664335C (en) 2006-09-20 2014-12-02 Boehringer Ingelheim International Gmbh Rho kinase inhibitors
WO2008053319A1 (en) 2006-10-30 2008-05-08 Pfizer Products Inc. Amide resorcinol compounds
US8012955B2 (en) 2006-12-28 2011-09-06 Rigel Pharmaceuticals, Inc. N-substituted-heterocycloalkyloxybenzamide compounds and methods of use
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
WO2008157330A1 (en) 2007-06-14 2008-12-24 Smithkline Beecham Corporation Chemical compounds
US8445686B2 (en) 2007-08-27 2013-05-21 Abbvie Inc. 4-(4-pyridinyl)-benzamides and their use as rock activity modulators
US20100227846A1 (en) 2007-08-30 2010-09-09 Takeda Pharmaceutical Company Limited Substituted pyrazole derivative
JP5544296B2 (ja) 2007-11-16 2014-07-09 ライジェル ファーマシューティカルズ， インコーポレイテッド 代謝障害のためのカルボキサミド、スルホンアミド、およびアミン化合物
TW200944506A (en) 2008-03-26 2009-11-01 Takeda Pharmaceutical Substituted pyrazole derivatives and use thereof
US8697911B2 (en) 2010-07-07 2014-04-15 Boehringer Ingelheim International Gmbh Rho kinase inhibitors
US9079880B2 (en) 2010-07-07 2015-07-14 Boehringer Ingelheim International Gmbh Rho kinase inhibitors
EP2630144B1 (en) 2010-10-19 2016-09-07 Boehringer Ingelheim International GmbH Rho kinase inhibitors

Also Published As

Publication number Publication date
EP2630144B1 (en) 2016-09-07
US9000154B2 (en) 2015-04-07
WO2012054367A1 (en) 2012-04-26
US20120270868A1 (en) 2012-10-25
EP2630144A1 (en) 2013-08-28
JP2013544797A (ja) 2013-12-19

Similar Documents

Publication Publication Date Title
JP5769326B2 (ja) Ｒｈｏキナーゼ阻害薬
JP5799479B2 (ja) Ｒｈｏキナーゼインヒビター
JP5739527B2 (ja) ＲｈｏキナーゼインヒビターとしてのＮ−環式−３−（環状カルボニルアミノメチル）ベンズアミド誘導体
EP2114869B1 (en) Rho kinase inhibitors
US8063034B2 (en) Oxadiazole derivatives and thiadiazole derivatives having neovascularization inhibitory activity
KR101014525B1 (ko) 신규 화합물
KR100394761B1 (ko) 헤테로바이사이클릭유도체
US7345043B2 (en) Inhibitors of histone deacetylase
US20030232860A1 (en) Medicine comprising dicyanopyridine derivative
TWI434834B (zh) 作為蛋白質激酶抑制劑之吡唑化合物及噻唑化合物、其醫藥組成物及用途
AU2004224302A1 (en) Methods for treating or preventing an inflammatory or metabolic condition by inhibiting JNK
US20160194311A1 (en) Substituted nicotinamide derivatives as kinase inhibitors
NZ550114A (en) Substituted thiazole and pyrimidine derivatives as melanocortin receptor modulators
CA2504320A1 (en) Compositions useful as inhibitors of rock and other protein kinases
US7683067B2 (en) 3-heterocyclyl-indole derivatives as inhibitors of glycogen synthase kinase-3 (GSK-3)
US20090203692A1 (en) Novel chemical compounds

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20141017

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20141017

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20150617

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20150618

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20150619

R150 Certificate of patent or registration of utility model

Ref document number: 5769326

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250