PE20170672A1 - Espirocicloheptanos como inhibidores de la cinasa rho (rock) - Google Patents
Espirocicloheptanos como inhibidores de la cinasa rho (rock)Info
- Publication number
- PE20170672A1 PE20170672A1 PE2017000041A PE2017000041A PE20170672A1 PE 20170672 A1 PE20170672 A1 PE 20170672A1 PE 2017000041 A PE2017000041 A PE 2017000041A PE 2017000041 A PE2017000041 A PE 2017000041A PE 20170672 A1 PE20170672 A1 PE 20170672A1
- Authority
- PE
- Peru
- Prior art keywords
- rock
- alkyl
- rho kinase
- spirocycloheptans
- inhibitors
- Prior art date
Links
- 102000000568 rho-Associated Kinases Human genes 0.000 title abstract 2
- 108010041788 rho-Associated Kinases Proteins 0.000 title abstract 2
- 239000011435 rock Substances 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 206010002383 Angina Pectoris Diseases 0.000 abstract 1
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 229940124639 Selective inhibitor Drugs 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
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- A61P27/06—Antiglaucoma agents or miotics
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- 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]
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
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- 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
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- 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
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- 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
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/08—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing alicyclic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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- 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
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- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
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- 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
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- 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
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed systems
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- 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
- C07D487/04—Ortho-condensed systems
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- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Ophthalmology & Optometry (AREA)
- Hospice & Palliative Care (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Gynecology & Obstetrics (AREA)
- Urology & Nephrology (AREA)
- Transplantation (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Psychiatry (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se refiere a espirocicloheptanos de formula (I) donde: A es un carbociclo espiro biciclico de 5 a 9 elementos; B es carbociclo C5-C6 o heterociclo de 5 a 6 elementos; ------ es un enlace opcional; M esta ausente, es N o CR10; L es -(CR4R4)0-1-, -(CR4R4)0-1C(O)-, entre otros; R1 es NR5R5, OR5, entre otros; R2 es halogeno, alquilo C1-C6, entre otros; R3 es halogeno, alquilo C1-C6, entre otros; R4 es H, OH, entre otros; R5 es H, alquilo C1-C4, entre otros; R10 es H o alquilo C1-C4. Tambien se refiere a una composicion. Dicho compuesto es un inhibidor selectivo de la cinasa RHO (ROCK) siendo util en el tratamiento de angina, ateroesclerosis, entre otros
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462024555P | 2014-07-15 | 2014-07-15 | |
| US14/797,414 US9902702B2 (en) | 2014-07-15 | 2015-07-13 | Spirocycloheptanes as inhibitors of rock |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20170672A1 true PE20170672A1 (es) | 2017-05-22 |
Family
ID=55073996
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2017000041A PE20170672A1 (es) | 2014-07-15 | 2015-07-14 | Espirocicloheptanos como inhibidores de la cinasa rho (rock) |
Country Status (24)
| Country | Link |
|---|---|
| US (2) | US9902702B2 (es) |
| EP (1) | EP3169682B1 (es) |
| JP (2) | JP6499749B2 (es) |
| KR (1) | KR102420938B1 (es) |
| CN (1) | CN106817899B (es) |
| AR (1) | AR101208A1 (es) |
| AU (1) | AU2015289897B2 (es) |
| BR (1) | BR112017000808A2 (es) |
| CA (1) | CA2954976A1 (es) |
| CL (1) | CL2017000089A1 (es) |
| CO (1) | CO2017001152A2 (es) |
| EA (1) | EA033061B1 (es) |
| ES (1) | ES2716415T3 (es) |
| IL (1) | IL250046B (es) |
| MA (1) | MA39554B1 (es) |
| MX (1) | MX376178B (es) |
| PE (1) | PE20170672A1 (es) |
| PH (1) | PH12017500072A1 (es) |
| SG (1) | SG11201700251PA (es) |
| TN (1) | TN2017000009A1 (es) |
| TW (1) | TW201607933A (es) |
| UY (1) | UY36215A (es) |
| WO (1) | WO2016010950A1 (es) |
| ZA (1) | ZA201700304B (es) |
Families Citing this family (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9902702B2 (en) * | 2014-07-15 | 2018-02-27 | Bristol-Myers Squibb Company | Spirocycloheptanes as inhibitors of rock |
| US10123993B2 (en) | 2015-01-09 | 2018-11-13 | Bristol-Myers Squibb Company | Cyclic ureas as inhibitors of rock |
| US10857157B2 (en) | 2015-01-26 | 2020-12-08 | BioAxone BioSciences, Inc. | Treatment of cerebral cavernous malformations and cerebral aneurysms with rho kinase inhibitors |
| US10106525B2 (en) | 2015-01-26 | 2018-10-23 | BioAxone BioSciences, Inc. | Rho kinase inhibitor BA-1049 (R) and active metabolites thereof |
| ES2730112T3 (es) | 2015-03-09 | 2019-11-08 | Bristol Myers Squibb Co | Lactamas como inhibidores de ROCK |
| AU2016315648B2 (en) | 2015-08-28 | 2021-04-01 | Chdi Foundation, Inc. | Probes for imaging huntingtin protein |
| AR107354A1 (es) * | 2016-01-13 | 2018-04-18 | Bristol Myers Squibb Co | Salicilamidas espiroheptanos y compuestos relacionados como inhibidores de rock |
| US10562887B2 (en) | 2016-05-27 | 2020-02-18 | Bristol-Myers Squibb Company | Triazolones and tetrazolones as inhibitors of ROCK |
| WO2017214413A1 (en) * | 2016-06-08 | 2017-12-14 | Chrysalis, Inc. | Imidazo[1,2-a]pyridine derivatives as histone demethylase inhibitors |
| JP7155102B2 (ja) | 2016-07-07 | 2022-10-18 | 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縮合環尿素 |
| JP6903731B2 (ja) * | 2016-07-07 | 2021-07-14 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 強力で選択的なrock阻害剤としてのラクタム、環状尿素、およびカルバメート、およびトリアゾロン誘導体 |
| US10696674B2 (en) | 2016-07-07 | 2020-06-30 | Bristol-Myers Squibb Company | Spirolactams as inhibitors of ROCK |
| ES2829400T3 (es) | 2016-11-30 | 2021-05-31 | Bristol Myers Squibb Co | Inhibidores tricíclicos de Rho cinasa |
| WO2018118109A1 (en) * | 2016-12-21 | 2018-06-28 | BioAxone BioSciences, Inc. | Rho kinase inhibitor ba-1049 (r) and active metabolites thereof |
| US11198680B2 (en) | 2016-12-21 | 2021-12-14 | BioAxone BioSciences, Inc. | Rho kinase inhibitor BA-1049 (R) and active metabolites thereof |
| PL3573987T3 (pl) * | 2017-01-30 | 2021-08-30 | Chiesi Farmaceutici S.P.A. | Pochodne amidu tyrozynowego jako inhibitory kinazy Rho |
| WO2019000683A1 (zh) * | 2017-06-30 | 2019-01-03 | 北京泰德制药股份有限公司 | Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途 |
| US11390609B2 (en) | 2017-06-30 | 2022-07-19 | Beijing Tide Pharmaceutical Co., Ltd. | Rho-associated protein kinase inhibitor, pharmaceutical composition comprising same, and preparation method and use thereof |
| WO2019014322A1 (en) | 2017-07-11 | 2019-01-17 | BioAxone BioSciences, Inc. | KINASE INHIBITORS FOR THE TREATMENT OF DISEASES |
| ES2878054T3 (es) | 2017-07-12 | 2021-11-18 | Bristol Myers Squibb Co | Espiroheptanil hidantoínas como inhibidores de ROCK |
| EP3652164B1 (en) | 2017-07-12 | 2023-06-21 | Bristol-Myers Squibb Company | Phenylacetamides as inhibitors of rock |
| 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 |
| US12060341B2 (en) * | 2017-07-12 | 2024-08-13 | Bristol-Myers Squibb Company | Spiroheptanyl hydantoins as ROCK inhibitors |
| EP3652165B1 (en) * | 2017-07-12 | 2021-08-25 | Bristol-Myers Squibb Company | Five membered-aminoheterocyclic and 5,6-or 6,6-membered bicyclic aminoheterocyclic inhibitors of rock for the treatment of heart failure |
| IL272379B2 (en) | 2017-08-14 | 2025-11-01 | Epizyme Inc | Methods of treating cancer by inhibiting setd2 |
| JP2020532551A (ja) | 2017-09-03 | 2020-11-12 | アンジオン バイオメディカ コーポレーション | Rho関連コイルドコイルキナーゼ(ROCK)阻害剤としてのビニルヘテロ環 |
| KR102716960B1 (ko) | 2017-11-03 | 2024-10-11 | 브리스톨-마이어스 스큅 컴퍼니 | 디아자스피로 rock 억제제 |
| IL310632A (en) * | 2018-08-14 | 2024-04-01 | Epizyme Inc | Substituted indoles and methods of use thereof |
| US12252484B2 (en) | 2018-09-06 | 2025-03-18 | Hoffmann-La Roche Inc. | Pyrazolopyridine compounds for the treatment of autoimmune disease |
| KR20220082804A (ko) * | 2019-07-17 | 2022-06-17 | 싸이토키네틱스, 인코포레이티드 | 심장 근섬유분절 억제제 경구 제제들 |
| WO2021257857A1 (en) | 2020-06-19 | 2021-12-23 | Incyte Corporation | Naphthyridinone compounds as jak2 v617f inhibitors |
| US11753413B2 (en) | 2020-06-19 | 2023-09-12 | Incyte Corporation | Substituted pyrrolo[2,1-f][1,2,4]triazine compounds as JAK2 V617F inhibitors |
| WO2022006456A1 (en) | 2020-07-02 | 2022-01-06 | Incyte Corporation | Tricyclic pyridone compounds as jak2 v617f inhibitors |
| AU2021300429A1 (en) | 2020-07-02 | 2023-02-16 | Incyte Corporation | Tricyclic urea compounds as JAK2 V617F inhibitors |
| TWI854147B (zh) * | 2020-08-21 | 2024-09-01 | 南韓商治納輔醫藥科技有限公司 | 對前列腺素e2受體具有抑制活性的新穎化合物及其用途 |
| WO2022046989A1 (en) | 2020-08-27 | 2022-03-03 | Incyte Corporation | Tricyclic urea compounds as jak2 v617f inhibitors |
| CN116390920A (zh) * | 2020-11-25 | 2023-07-04 | 豪夫迈·罗氏有限公司 | 用于治疗和预防乙型肝炎病毒感染的芳族螺环酰胺衍生物 |
| WO2022140231A1 (en) | 2020-12-21 | 2022-06-30 | Incyte Corporation | Deazaguaine compounds as jak2 v617f inhibitors |
| WO2022182839A1 (en) | 2021-02-25 | 2022-09-01 | Incyte Corporation | Spirocyclic lactams as jak2 v617f inhibitors |
| CN117321047A (zh) * | 2021-05-14 | 2023-12-29 | 武汉朗来科技发展有限公司 | 化合物的晶型、含晶型组合物及其制备方法和应用 |
| CN113861223B (zh) * | 2021-09-07 | 2022-09-16 | 暨南大学 | 一种噻唑并[3,2-a]苯并咪唑类化合物的合成方法及其应用 |
| CN119173514A (zh) | 2022-03-17 | 2024-12-20 | 因赛特公司 | 作为jak2 v617f抑制剂的三环脲化合物 |
| EP4504728A1 (en) * | 2022-04-01 | 2025-02-12 | Sanofi | Pyrazolopyrazinone compounds, process for their preparation and therapeutic uses thereof |
| TW202402269A (zh) * | 2022-05-26 | 2024-01-16 | 大陸商迪哲(江蘇)醫藥股份有限公司 | ROCK(Rho相關激酶)抑制劑及其用途 |
| CN115894141B (zh) * | 2022-10-13 | 2023-12-22 | 贺州学院 | 酰基茚烷类衍生物的合成方法 |
Family Cites Families (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2531776A1 (de) | 1975-07-16 | 1977-02-03 | Basf Ag | Azopigmente mit einem phthalazonrest |
| TW245719B (es) | 1990-09-10 | 1995-04-21 | Sterling Winthrop Inc | |
| EP0481383B1 (en) | 1990-10-16 | 1995-06-28 | Takeda Chemical Industries, Ltd. | Heterocyclic amine derivatives, their production and use |
| 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 |
| JP2002502844A (ja) | 1998-02-03 | 2002-01-29 | ベーリンガー インゲルハイム ファルマ コマンディトゲゼルシャフト | 5員複素環縮合ベンゾ誘導体、その調製及び医薬品としてのそれらの使用 |
| DE19804085A1 (de) | 1998-02-03 | 1999-08-05 | Boehringer Ingelheim Pharma | 5-Gliedrige heterocyclische kondensierte Benzoderivate, deren Herstellung und deren Verwendung als Arzneimittel |
| JP2000072675A (ja) | 1998-08-26 | 2000-03-07 | Tanabe Seiyaku Co Ltd | 医薬組成物 |
| US6677333B1 (en) | 1999-01-26 | 2004-01-13 | Ono Pharmaceutical Co., Ltd. | 2H-phthalazin-1-one derivatives and drug containing its derivatives as active ingredient |
| DE19907813A1 (de) | 1999-02-24 | 2000-08-31 | Boehringer Ingelheim Pharma | Substituierte bicyclische Heterocyclen, deren Herstellung und deren Verwendung als Arzneimittel |
| CN100400518C (zh) | 2000-10-30 | 2008-07-09 | 库多斯药物有限公司 | 2,3-二氮杂萘酮衍生物 |
| CA2476162A1 (en) | 2002-02-13 | 2003-08-21 | Takeda Chemical Industries, Ltd. | Jnk inhibitor |
| AU2003264386A1 (en) | 2002-09-10 | 2004-04-30 | Kyorin Pharmaceutical Co., Ltd. | 4-(substituted aryl)-5-hydroxyisoquinolinone derivative |
| PE20060285A1 (es) | 2004-03-30 | 2006-05-08 | Aventis Pharma Inc | Piridonas sustituidas como inhibidores de pol(adp-ribosa)-polimerasa (parp) |
| US7648978B2 (en) | 2004-09-28 | 2010-01-19 | Angion Biomedica Corp. | Small molecule modulators of cytokine activity |
| WO2006124874A2 (en) | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibitors of b-raf kinase |
| CN101296904A (zh) * | 2005-07-11 | 2008-10-29 | 德福根有限公司 | 作为激酶抑制剂的酰胺衍生物 |
| ATE478865T1 (de) * | 2006-05-12 | 2010-09-15 | Vertex Pharma | Selektive rock-proteinkinasehemmer und ihre verwendung |
| CA2653424A1 (en) * | 2006-06-08 | 2007-12-13 | Ube Industries, Ltd. | Novel indazole derivative having spiro ring structure in side chain |
| JP5235887B2 (ja) | 2006-09-20 | 2013-07-10 | アエリー ファーマシューティカルズ インコーポレイテッド | Rhoキナーゼ阻害剤 |
| CN101595094B (zh) * | 2006-12-27 | 2013-02-20 | 塞诺菲-安万特股份有限公司 | 环烷基胺取代的异喹诺酮衍生物 |
| 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 |
| AU2008205252B2 (en) | 2007-01-09 | 2013-02-21 | Amgen Inc. | Bis-aryl amide derivatives useful for the treatment of cancer |
| WO2009064422A2 (en) | 2007-11-13 | 2009-05-22 | Angion Biomedica Corp. | Hepatocyte growth factor pathway activators in fibrotic connective tissue diseases |
| WO2011019400A2 (en) | 2009-08-12 | 2011-02-17 | Angion Biomedica Corp. | Enhancement of cellular transplantation using small molecule modulators hepatocyte growth factor (scatter factor) activity |
| AU2011329233A1 (en) | 2010-11-15 | 2013-05-23 | Abbvie Deutschland Gmbh & Co Kg | NAMPT and ROCK inhibitors |
| 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 |
| CN102432612B (zh) * | 2011-09-07 | 2014-09-17 | 苏州大学 | 4,7-二氢四唑[1,5-a]嘧啶衍生物及其在制备抗肿瘤药物中的应用 |
| CN102327275B (zh) * | 2011-09-07 | 2013-03-20 | 苏州大学 | 3-[4-(磺酰)苯]脲类化合物在制备抗肿瘤药物中的应用 |
| WO2014079850A1 (en) | 2012-11-23 | 2014-05-30 | F. Hoffmann-La Roche Ag | Substituted heterocyclic derivatives |
| BR112015017008A2 (pt) | 2013-01-18 | 2017-07-11 | Bristol Myers Squibb Co | ftalazinonas e isoquinolinonas como inibidores de rock |
| EP2961746B1 (en) | 2013-02-28 | 2018-01-03 | 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 |
| EP2978757B1 (en) * | 2013-03-27 | 2017-02-08 | Boehringer Ingelheim International GmbH | Indolinone analogues as brd4 inhibitors |
| 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 |
| AR096788A1 (es) | 2013-07-02 | 2016-02-03 | Bristol Myers Squibb Co | Compuestos tricíclicos de carboxamida como inhibidores potentes de rock |
| ES2634628T3 (es) | 2013-07-02 | 2017-09-28 | Bristol-Myers Squibb Company | Derivados tricíclicos de pirido-carboxamida como inhibidores ROCK |
| CN106061964B (zh) | 2014-01-20 | 2019-10-25 | 豪夫迈·罗氏有限公司 | 能够刺激神经发生的n-苯基-内酰胺衍生物及其在神经性病症的治疗中的用途 |
| US9902702B2 (en) * | 2014-07-15 | 2018-02-27 | Bristol-Myers Squibb Company | Spirocycloheptanes as inhibitors of rock |
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