CN104822676B - 新rock抑制剂 - Google Patents

新rock抑制剂 Download PDF

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Publication number
CN104822676B
CN104822676B CN201380056608.XA CN201380056608A CN104822676B CN 104822676 B CN104822676 B CN 104822676B CN 201380056608 A CN201380056608 A CN 201380056608A CN 104822676 B CN104822676 B CN 104822676B
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alkyl
compound
disease
group
hydrogen
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Expired - Fee Related
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CN201380056608.XA
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English (en)
Chinese (zh)
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CN104822676A (zh
Inventor
A·P·J·布兰
D·雷森
O·戴非尔特
S·波兰德
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Ph Pharmaceutical Co ltd
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Amakem NV
Ph Pharmaceutical Co ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/04Drugs for disorders of the respiratory system for throat disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02Heterocyclic 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
    • C07D217/04Heterocyclic 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 with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Otolaryngology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Epidemiology (AREA)
CN201380056608.XA 2012-10-31 2013-10-31 新rock抑制剂 Expired - Fee Related CN104822676B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12190859.4 2012-10-31
EP12190859 2012-10-31
PCT/EP2013/072774 WO2014068035A1 (en) 2012-10-31 2013-10-31 Novel rock inhibitors

Publications (2)

Publication Number Publication Date
CN104822676A CN104822676A (zh) 2015-08-05
CN104822676B true CN104822676B (zh) 2019-11-05

Family

ID=47148627

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201380056608.XA Expired - Fee Related CN104822676B (zh) 2012-10-31 2013-10-31 新rock抑制剂

Country Status (20)

Country Link
US (1) US9394286B2 (enExample)
EP (1) EP2914590B1 (enExample)
JP (1) JP6205425B2 (enExample)
KR (1) KR102242280B1 (enExample)
CN (1) CN104822676B (enExample)
AU (1) AU2013340854B2 (enExample)
BR (1) BR112015009504A2 (enExample)
CA (1) CA2922312C (enExample)
DK (1) DK2914590T3 (enExample)
EA (1) EA026629B1 (enExample)
ES (1) ES2617495T3 (enExample)
IL (1) IL238391A (enExample)
IN (1) IN2015DN04311A (enExample)
MX (1) MX362485B (enExample)
NZ (1) NZ708526A (enExample)
PL (1) PL2914590T3 (enExample)
PT (1) PT2914590T (enExample)
SG (1) SG11201503134WA (enExample)
WO (1) WO2014068035A1 (enExample)
ZA (1) ZA201503544B (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20170114323A1 (en) 2014-06-19 2017-04-27 Whitehead Institute For Biomedical Research Uses of kinase inhibitors for inducing and maintaining pluripotency
WO2016172159A1 (en) * 2015-04-20 2016-10-27 University Of Houston System Locally bioavailable drugs
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
EP3693380A1 (en) * 2019-02-11 2020-08-12 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Dual inhibition of plexin-b1 and plexin-b2
US12371667B2 (en) 2021-05-13 2025-07-29 Washington University Enhanced methods for inducing and maintaining naive human pluripotent stem cells
CA3238227A1 (en) 2021-11-11 2023-05-19 The Doshisha Cryopreservation preparation for corneal endothelial cells and method for producing said cryopreservation preparation
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ras相關疾病或病症之組合療法
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
WO2025080946A2 (en) 2023-10-12 2025-04-17 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008077057A2 (en) * 2006-12-18 2008-06-26 Inspire Pharmaceuticals, Inc. Cytoskeletal active rho kinase inhibitor compounds, composition and use
WO2011075415A1 (en) * 2009-12-14 2011-06-23 Inspire Pharmaceuticals, Inc. Bridged bicyclic rho kinase inhibitor compounds, composition and use
EP1256574B1 (en) * 2000-02-01 2012-01-18 Kyowa Hakko Kirin Co., Ltd. Nitrogen-containing compounds having kinase inhibitory activity and drugs containing the same
WO2012012282A1 (en) * 2010-07-19 2012-01-26 Inspire Pharmaceuticals, Inc. Bifunctional rho kinase inhibitor compounds, composition and use
WO2012015760A1 (en) * 2010-07-27 2012-02-02 Inspire Pharmaceuticals, Inc. Method for treating ophthalmic diseases using kinase inhibitor compounds in prodrug forms

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090325960A1 (en) 2008-06-26 2009-12-31 Fulcher Emilee H Method for treating inflammatory diseases using rho kinase inhibitor compounds
US20090325959A1 (en) 2008-06-26 2009-12-31 Vittitow Jason L Method for treating ophthalmic diseases using rho kinase inhibitor compounds
WO2009158587A1 (en) 2008-06-26 2009-12-30 Inspire Pharmaceuticals, Inc. Method for treating pulmonary diseases using rho kinase inhibitor compounds
WO2010065782A1 (en) 2008-12-04 2010-06-10 Inspire Pharmaceuticals, Inc. Method for treating pulmonary diseases using rho kinase inhibitor compounds
GB201107223D0 (en) * 2011-04-29 2011-06-15 Amakem Nv Novel rock inhibitors

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1256574B1 (en) * 2000-02-01 2012-01-18 Kyowa Hakko Kirin Co., Ltd. Nitrogen-containing compounds having kinase inhibitory activity and drugs containing the same
WO2008077057A2 (en) * 2006-12-18 2008-06-26 Inspire Pharmaceuticals, Inc. Cytoskeletal active rho kinase inhibitor compounds, composition and use
WO2011075415A1 (en) * 2009-12-14 2011-06-23 Inspire Pharmaceuticals, Inc. Bridged bicyclic rho kinase inhibitor compounds, composition and use
WO2012012282A1 (en) * 2010-07-19 2012-01-26 Inspire Pharmaceuticals, Inc. Bifunctional rho kinase inhibitor compounds, composition and use
WO2012015760A1 (en) * 2010-07-27 2012-02-02 Inspire Pharmaceuticals, Inc. Method for treating ophthalmic diseases using kinase inhibitor compounds in prodrug forms

Also Published As

Publication number Publication date
IL238391A (en) 2017-08-31
EA026629B1 (ru) 2017-04-28
CA2922312C (en) 2020-10-20
IN2015DN04311A (enExample) 2015-10-16
PT2914590T (pt) 2017-02-27
IL238391A0 (en) 2015-06-30
KR102242280B1 (ko) 2021-04-20
MX362485B (es) 2019-01-21
DK2914590T3 (en) 2017-03-06
CA2922312A1 (en) 2014-05-08
JP2015535270A (ja) 2015-12-10
US20150299173A1 (en) 2015-10-22
AU2013340854B2 (en) 2017-06-08
WO2014068035A1 (en) 2014-05-08
US9394286B2 (en) 2016-07-19
HK1213550A1 (zh) 2016-07-08
EP2914590B1 (en) 2016-11-30
EA201590847A1 (ru) 2015-08-31
SG11201503134WA (en) 2015-05-28
KR20150084027A (ko) 2015-07-21
AU2013340854A1 (en) 2015-06-11
EP2914590A1 (en) 2015-09-09
BR112015009504A2 (pt) 2017-07-04
ES2617495T3 (es) 2017-06-19
MX2015005459A (es) 2015-07-21
JP6205425B2 (ja) 2017-09-27
ZA201503544B (en) 2017-09-27
PL2914590T3 (pl) 2017-06-30
CN104822676A (zh) 2015-08-05
NZ708526A (en) 2018-08-31

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