JP5769326B2 - Rhoキナーゼ阻害薬 - Google Patents
Rhoキナーゼ阻害薬 Download PDFInfo
- 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
Links
- 0 Cc1nc(CCC(*)C2)c2[s]1 Chemical compound Cc1nc(CCC(*)C2)c2[s]1 0.000 description 7
- LAGNMUUUMQJXBF-UHFFFAOYSA-N C#Cc(cc1)ccc1C#N Chemical compound C#Cc(cc1)ccc1C#N LAGNMUUUMQJXBF-UHFFFAOYSA-N 0.000 description 1
- DIGYMFWDGBBUAI-UHFFFAOYSA-N CC(CC1=C=CC(CCN(C)C2)=C2S1)(c1cc(CCC2C=NC(c(cc3)ccc3NC)=C2)ccc1)O Chemical compound CC(CC1=C=CC(CCN(C)C2)=C2S1)(c1cc(CCC2C=NC(c(cc3)ccc3NC)=C2)ccc1)O DIGYMFWDGBBUAI-UHFFFAOYSA-N 0.000 description 1
- YUHSMQQNPRLEEJ-UHFFFAOYSA-N COC(c1cc(CBr)ccc1)=O Chemical compound COC(c1cc(CBr)ccc1)=O YUHSMQQNPRLEEJ-UHFFFAOYSA-N 0.000 description 1
- VCMJMVRVIJNLAF-GEQMXUHSSA-N N#CC12C=CC[C@@H]3[C@@H]1N(CC(C1)C=CC=C1C(O)=C1CC1)NNCC23 Chemical compound N#CC12C=CC[C@@H]3[C@@H]1N(CC(C1)C=CC=C1C(O)=C1CC1)NNCC23 VCMJMVRVIJNLAF-GEQMXUHSSA-N 0.000 description 1
- VKAUWSOZLFBABP-NSHDSACASA-N N[C@@H](CC1)Cc2c1nc(NC(OCc1ccccc1)=O)[s]2 Chemical compound N[C@@H](CC1)Cc2c1nc(NC(OCc1ccccc1)=O)[s]2 VKAUWSOZLFBABP-NSHDSACASA-N 0.000 description 1
- HIMUCQLOWQLZGY-VIFPVBQESA-N Nc1nc(CC[C@@H](C2)N3CCCCC3)c2[s]1 Chemical compound Nc1nc(CC[C@@H](C2)N3CCCCC3)c2[s]1 HIMUCQLOWQLZGY-VIFPVBQESA-N 0.000 description 1
- XUUQJYXFUYMIEN-INIZCTEOSA-N O=C(Nc1nc(CC[C@@H](C2)N3CCCCC3)c2[s]1)OCc1ccccc1 Chemical compound O=C(Nc1nc(CC[C@@H](C2)N3CCCCC3)c2[s]1)OCc1ccccc1 XUUQJYXFUYMIEN-INIZCTEOSA-N 0.000 description 1
- VCVOSERVUCJNPR-SYDPRGILSA-N O[C@H](CCC1)[C@H]1O Chemical compound O[C@H](CCC1)[C@H]1O VCVOSERVUCJNPR-SYDPRGILSA-N 0.000 description 1
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)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Ophthalmology & Optometry (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Gynecology & Obstetrics (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Vascular Medicine (AREA)
- Psychiatry (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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 (https=) | 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 (https=) |
| EP (1) | EP2630144B1 (https=) |
| JP (1) | JP5769326B2 (https=) |
| WO (1) | WO2012054367A1 (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9079880B2 (en) | 2010-07-07 | 2015-07-14 | Boehringer Ingelheim International Gmbh | Rho kinase inhibitors |
| US8697911B2 (en) | 2010-07-07 | 2014-04-15 | 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 |
| EP3016950B1 (en) * | 2013-07-02 | 2017-06-07 | Bristol-Myers Squibb Company | Tricyclic pyrido-carboxamide derivatives as rock inhibitors |
| US9914740B2 (en) | 2013-07-02 | 2018-03-13 | Bristol-Myers Squibb Company | Tricyclic pyrido-carboxamide derivatives as rock inhibitors |
| US10123993B2 (en) * | 2015-01-09 | 2018-11-13 | Bristol-Myers Squibb Company | Cyclic ureas as inhibitors of rock |
| WO2016180918A1 (en) | 2015-05-12 | 2016-11-17 | Platod | Combination of pharmacological and microfluidic features for improved platelets production |
| EP3843845B1 (en) | 2018-08-29 | 2026-03-11 | University Of Massachusetts | Inhibition of protein kinases to treat friedreich ataxia |
Family Cites Families (30)
| 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 |
| AU8181701A (en) * | 2000-06-21 | 2002-01-02 | Hoffmann La Roche | Benzothiazole derivatives |
| CA2430409A1 (en) | 2000-11-28 | 2002-06-06 | Guilford Pharmaceuticals Inc. | Bisubstituted carbocyclic cyclophilin binding compounds and their use |
| DE10112768A1 (de) | 2001-03-16 | 2002-09-19 | Merck Patent Gmbh | Phenylderivate 3 |
| JPWO2002100833A1 (ja) | 2001-06-12 | 2004-09-24 | 住友製薬株式会社 | Rhoキナーゼ阻害剤 |
| 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 |
| NZ541824A (en) * | 2003-02-26 | 2010-04-30 | Banyu Pharma Co Ltd | Heteroarylcarbamoylbenzene derivatives as glucokinase activators |
| 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. |
| AU2005286648A1 (en) | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors |
| CA2579227A1 (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 |
| WO2007008926A1 (en) | 2005-07-11 | 2007-01-18 | Aerie Pharmaceuticals, Inc. | Isoquinoline compounds |
| WO2008036540A2 (en) | 2006-09-20 | 2008-03-27 | Boehringer Ingelheim International Gmbh | Rho kinase inhibitors |
| WO2008053319A1 (en) | 2006-10-30 | 2008-05-08 | Pfizer Products Inc. | Amide resorcinol compounds |
| CA2674237C (en) | 2006-12-28 | 2015-11-24 | 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 |
| CN101842357A (zh) | 2007-08-30 | 2010-09-22 | 武田药品工业株式会社 | 取代的吡唑衍生物 |
| BRPI0820171B8 (pt) | 2007-11-16 | 2021-05-25 | Rigel Pharmaceuticals Inc | compostos de carboxamida, sulfonamida e amina para distúrbios metabólicos, composição farmacêutica, e, uso dos mesmos |
| WO2009119880A1 (en) | 2008-03-26 | 2009-10-01 | Takeda Pharmaceutical Company Limited | Substituted pyrazole derivatives and use thereof |
| US9079880B2 (en) | 2010-07-07 | 2015-07-14 | Boehringer Ingelheim International Gmbh | Rho kinase inhibitors |
| US8697911B2 (en) | 2010-07-07 | 2014-04-15 | Boehringer Ingelheim International Gmbh | Rho kinase inhibitors |
| EP2630144B1 (en) | 2010-10-19 | 2016-09-07 | Boehringer Ingelheim International GmbH | Rho kinase inhibitors |
-
2011
- 2011-10-17 EP EP11776653.5A patent/EP2630144B1/en active Active
- 2011-10-17 WO PCT/US2011/056505 patent/WO2012054367A1/en not_active Ceased
- 2011-10-17 JP JP2013534982A patent/JP5769326B2/ja active Active
- 2011-10-17 US US13/274,610 patent/US9000154B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US9000154B2 (en) | 2015-04-07 |
| WO2012054367A1 (en) | 2012-04-26 |
| US20120270868A1 (en) | 2012-10-25 |
| EP2630144B1 (en) | 2016-09-07 |
| JP2013544797A (ja) | 2013-12-19 |
| EP2630144A1 (en) | 2013-08-28 |
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