MX376178B - Espirocicloheptanos como inhibidores de la cinasa rho (rock). - Google Patents

Espirocicloheptanos como inhibidores de la cinasa rho (rock).

Info

Publication number
MX376178B
MX376178B MX2017000485A MX2017000485A MX376178B MX 376178 B MX376178 B MX 376178B MX 2017000485 A MX2017000485 A MX 2017000485A MX 2017000485 A MX2017000485 A MX 2017000485A MX 376178 B MX376178 B MX 376178B
Authority
MX
Mexico
Prior art keywords
spirocycloheptanes
rock
kinase inhibitors
rho kinase
compounds
Prior art date
Application number
MX2017000485A
Other languages
English (en)
Other versions
MX2017000485A (es
Inventor
Peter W Glunz
Vladimir Ladziata
Yufeng Wang
Zilun Hu
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of MX2017000485A publication Critical patent/MX2017000485A/es
Publication of MX376178B publication Critical patent/MX376178B/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/30Phthalazines
    • C07D237/32Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/502Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • 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
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • 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
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/08Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente invención se refiere a compuestos de la Fórmula (I): (ver Fórmula) o estereoisómeros, tautómeros o sales de los mismos farmacéuticamente aceptables, en donde todas las variables son como se definen en la presente. Estos compuestos son inhibidores de ROCK selectivos. La presente invención también se refiere a composiciones farmacéuticas que comprenden estos compuestos y a métodos para tratar trastornos cardiovasculares, trastornos relacionados con el músculo liso, trastornos oncológicos, trastornos neuropatológicos, trastornos autoinmunitarios, trastornos fibróticos y/o trastornos inflamatorios mediante su uso.
MX2017000485A 2014-07-15 2015-07-14 Espirocicloheptanos como inhibidores de la cinasa rho (rock). MX376178B (es)

Applications Claiming Priority (3)

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
PCT/US2015/040254 WO2016010950A1 (en) 2014-07-15 2015-07-14 Spirocycloheptanes as inhibitors of rock

Publications (2)

Publication Number Publication Date
MX2017000485A MX2017000485A (es) 2017-04-27
MX376178B true MX376178B (es) 2025-03-07

Family

ID=55073996

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2017000485A MX376178B (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 (46)

* Cited by examiner, † Cited by third party
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
AR103990A1 (es) 2015-01-09 2017-06-21 Bristol Myers Squibb Co Ureas cíclicas como inhibidoras de rock
US10106525B2 (en) 2015-01-26 2018-10-23 BioAxone BioSciences, Inc. Rho kinase inhibitor BA-1049 (R) and active metabolites thereof
US10857157B2 (en) 2015-01-26 2020-12-08 BioAxone BioSciences, Inc. Treatment of cerebral cavernous malformations and cerebral aneurysms with rho kinase inhibitors
US10112929B2 (en) 2015-03-09 2018-10-30 Bristol-Myers Squibb Company Lactams as inhibitors of rock
HRP20211156T1 (hr) * 2015-08-28 2021-12-24 Chdi Foundation, Inc. Kontrastna sredstva za slikovnu dijagnostiku huntingtin proteina
AR107354A1 (es) * 2016-01-13 2018-04-18 Bristol Myers Squibb Co Salicilamidas espiroheptanos y compuestos relacionados como inhibidores de rock
CN109153663B (zh) 2016-05-27 2021-08-13 百时美施贵宝公司 作为rock抑制剂的三唑酮类化合物和四唑酮类化合物
WO2017214413A1 (en) * 2016-06-08 2017-12-14 Chrysalis, Inc. Imidazo[1,2-a]pyridine derivatives as histone demethylase inhibitors
JP7113810B2 (ja) 2016-07-07 2022-08-05 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ラクタム
ES2829550T3 (es) 2016-07-07 2021-06-01 Bristol Myers Squibb Co Ureas cíclicas espiro-condensadas como inhibidores de ROCK
ES2814325T3 (es) * 2016-07-07 2021-03-26 Bristol Myers Squibb Co Derivados de lactama, urea cíclica y carbamato y de triazolona como inhibidores potentes y selectivos de ROCK
WO2018102325A1 (en) 2016-11-30 2018-06-07 Bristol-Myers Squibb Company Tricyclic rho kinase inhibitors
FI3558314T3 (fi) * 2016-12-21 2024-11-29 Bioaxone Biosciences Inc Rho-kinaasin estäjä ba-1049 (r) ja sen aktiivisia aineenvaihduntatuotteita
US11198680B2 (en) 2016-12-21 2021-12-14 BioAxone BioSciences, Inc. Rho kinase inhibitor BA-1049 (R) and active metabolites thereof
CA3047212A1 (en) * 2017-01-30 2018-08-02 Chiesi Farmaceutici S.P.A. Tyrosine amide derivatives as rho- kinase inhibitors
WO2019001572A1 (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
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
US10537567B2 (en) 2017-07-11 2020-01-21 BioAxone BioSciences, Inc. Kinase inhibitors for treatment of disease
EP3652167B1 (en) 2017-07-12 2021-06-02 Bristol-Myers Squibb Company Spiroheptanyl hydantoins as rock inhibitors
WO2019014303A1 (en) 2017-07-12 2019-01-17 Bristol-Myers Squibb Company 5-OR 6,6-CHANNEL BICYCLIC CHAINS AND AMINOHETEROCYCLIC AMINOHETEROCYCLIC INHIBITORS FOR THE TREATMENT OF CARDIAC INSUFFICIENCY
US12060341B2 (en) * 2017-07-12 2024-08-13 Bristol-Myers Squibb Company Spiroheptanyl hydantoins as ROCK inhibitors
CN110869360B (zh) 2017-07-12 2023-12-15 百时美施贵宝公司 作为rock抑制剂的苯乙酰胺类
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
KR20200052294A (ko) 2017-08-14 2020-05-14 에피자임, 인코포레이티드 Setd2의 저해에 의한 암의 치료 방법
US11542256B2 (en) 2017-09-03 2023-01-03 Angion Biomedica Corp. Vinylheterocycles as Rho-associated coiled-coil kinase (ROCK) inhibitors
US11192891B2 (en) 2017-11-03 2021-12-07 Bristol-Myers Squibb Company Diazaspiro ROCK inhibitors
CN112585119A (zh) * 2018-08-14 2021-03-30 Epizyme股份有限公司 经取代的吲哚及其使用方法
CN112654620B (zh) * 2018-09-06 2023-08-04 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的新型吡唑并吡啶化合物
IL289884B2 (en) * 2019-07-17 2026-01-01 Cytokinetics Inc Oral formulations of cardiac sarcomere inhibitors
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
US11767323B2 (en) 2020-07-02 2023-09-26 Incyte Corporation Tricyclic pyridone compounds as JAK2 V617F inhibitors
KR20230057341A (ko) 2020-07-02 2023-04-28 인사이트 코포레이션 Jak2 v617f 억제제로서 삼환계 우레아 화합물
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
WO2022112207A1 (en) * 2020-11-25 2022-06-02 F. Hoffmann-La Roche Ag Aromatic spiro ring amide derivatives for the treatment and prophylaxis of hepatitis b virus infection
WO2022140231A1 (en) 2020-12-21 2022-06-30 Incyte Corporation Deazaguaine compounds as jak2 v617f inhibitors
AR125273A1 (es) 2021-02-25 2023-07-05 Incyte Corp Lactamas espirocíclicas como inhibidores de jak2 v617f
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
PE20251706A1 (es) 2022-03-17 2025-07-02 Incyte Corp Compuestos de urea triciclica como inhibidores de v617f de jak2
JP2025511160A (ja) * 2022-04-01 2025-04-15 サノフイ ピラゾロピラジノン化合物、その調製のための方法及びその治療的使用
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
CN117327016A (zh) * 2023-09-12 2024-01-02 湖北泰盛化工有限公司 一种砜吡草唑中间体的制备方法

Family Cites Families (40)

* Cited by examiner, † Cited by third party
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
DE19804085A1 (de) 1998-02-03 1999-08-05 Boehringer Ingelheim Pharma 5-Gliedrige heterocyclische kondensierte Benzoderivate, deren Herstellung und deren Verwendung als Arzneimittel
AU2720199A (en) 1998-02-03 1999-08-23 Boehringer Ingelheim Pharma Kg Five-membered, benzo-condensed heterocycles used as antithrombotic agents
JP2000072675A (ja) 1998-08-26 2000-03-07 Tanabe Seiyaku Co Ltd 医薬組成物
EP1148053A4 (en) 1999-01-26 2002-03-06 Ono Pharmaceutical Co 2H-PHTHALAZIN-1-ON DERIVATIVES AND DRUG COMPOSITIONS THAT CONTAIN THESE DERIVATIVES AS ACTIVE INGREDIENTS
DE19907813A1 (de) 1999-02-24 2000-08-31 Boehringer Ingelheim Pharma Substituierte bicyclische Heterocyclen, deren Herstellung und deren Verwendung als Arzneimittel
HU228960B1 (hu) 2000-10-30 2013-07-29 Kudos Pharm Ltd Ftalazinon-származékok
AU2003211931A1 (en) 2002-02-13 2003-09-04 Takeda Chemical Industries, Ltd. Jnk inhibitor
WO2004024694A1 (ja) 2002-09-10 2004-03-25 Kyorin Pharmaceutical Co., Ltd. 4-置換アリール-5-ヒドロキシイソキノリノン誘導体
PE20060285A1 (es) 2004-03-30 2006-05-08 Aventis Pharma Inc Piridonas sustituidas como inhibidores de pol(adp-ribosa)-polimerasa (parp)
EP1799651A2 (en) 2004-09-28 2007-06-27 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
AU2007249891A1 (en) * 2006-05-12 2007-11-22 Vertex Pharmaceuticals Incorporated Selective inhibitors of ROCK protein kinase and uses thereof
JPWO2007142323A1 (ja) 2006-06-08 2009-10-29 宇部興産株式会社 側鎖にスピロ環構造を有する新規インダゾール誘導体
CA2664335C (en) 2006-09-20 2014-12-02 Boehringer Ingelheim International Gmbh Rho kinase inhibitors
JP5405314B2 (ja) * 2006-12-27 2014-02-05 サノフイ シクロアルキルアミン置換イソキノロン誘導体
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
ES2449482T3 (es) 2007-01-09 2014-03-19 Amgen Inc. Derivados de bis-aril-amida útiles para el tratamiento de cáncer
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
PE20140913A1 (es) 2010-11-15 2014-08-22 Abbvie Inc Inhibidores de nampt y rock
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
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
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
WO2014079850A1 (en) 2012-11-23 2014-05-30 F. Hoffmann-La Roche Ag Substituted heterocyclic derivatives
US9221767B2 (en) 2013-01-18 2015-12-29 Bristol-Myers Squibb Company Substituted phthalazinones as rock inhibitors
TW201444798A (zh) 2013-02-28 2014-12-01 必治妥美雅史谷比公司 作爲強效rock1及rock2抑制劑之苯基吡唑衍生物
EP2961746B1 (en) 2013-02-28 2018-01-03 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent rock1 and rock2 inhibitors
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
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
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
RU2016131875A (ru) 2014-01-20 2018-02-26 Ф. Хоффманн-Ля Рош Аг Производные n-фениллактама, способные стимулировать нейрогенез, и их применение при лечении заболеваний нервной системы
US9902702B2 (en) * 2014-07-15 2018-02-27 Bristol-Myers Squibb Company Spirocycloheptanes as inhibitors of rock

Also Published As

Publication number Publication date
ZA201700304B (en) 2018-12-19
TN2017000009A1 (en) 2018-07-04
TW201607933A (zh) 2016-03-01
EP3169682B1 (en) 2018-12-26
PE20170672A1 (es) 2017-05-22
WO2016010950A1 (en) 2016-01-21
KR20170023187A (ko) 2017-03-02
MX2017000485A (es) 2017-04-27
CL2017000089A1 (es) 2017-09-15
CN106817899A (zh) 2017-06-09
CO2017001152A2 (es) 2017-05-19
AR101208A1 (es) 2016-11-30
CA2954976A1 (en) 2016-01-21
CN106817899B (zh) 2021-03-09
BR112017000808A2 (pt) 2017-12-05
JP6499749B2 (ja) 2019-04-10
ES2716415T3 (es) 2019-06-12
JP2019112447A (ja) 2019-07-11
US9902702B2 (en) 2018-02-27
AU2015289897B2 (en) 2019-07-18
EP3169682A1 (en) 2017-05-24
SG11201700251PA (en) 2017-02-27
JP2017520604A (ja) 2017-07-27
US20180155296A1 (en) 2018-06-07
MA39554A2 (es) 2018-01-31
EA201790062A1 (ru) 2017-08-31
UY36215A (es) 2016-01-29
JP6721741B2 (ja) 2020-07-15
EA033061B1 (ru) 2019-08-30
PH12017500072A1 (en) 2017-05-15
IL250046B (en) 2020-03-31
US20160016914A1 (en) 2016-01-21
AU2015289897A1 (en) 2017-03-09
MA39554A3 (fr) 2019-05-31
MA39554B1 (fr) 2020-05-29
KR102420938B1 (ko) 2022-07-14

Similar Documents

Publication Publication Date Title
MX376178B (es) Espirocicloheptanos como inhibidores de la cinasa rho (rock).
MX382434B (es) Salicilamidas de espiroheptanos y compuestos relacionados como inhibidores de cinasa rho (rock).
MX2015008741A (es) Ftalazinonas e isoquinolinonas como inhibidores de cinasa rho.
EA201891910A1 (ru) Гетероарильные ингибиторы pad4
PH12018500177A1 (en) Compositions useful for treating disorders related to kit and pdfgr
PH12018500457A1 (en) New phenoxymethyl derivatives
EA201891251A1 (ru) Бициклические ингибиторы pad4
MX376056B (es) Pirimidinonas como inhibidores del factor xia.
MX2020011774A (es) Compuestos de naftiridina como inhibidores de quinasa jak.
GEAP201914692A (en) Substituted oxopyridine derivatives
EA201792205A1 (ru) Гетероциклические соединения как ингибиторы lsd1
EA201891347A1 (ru) Аза-бензимидазольные ингибиторы pad4
EA201792535A1 (ru) Гетероциклические амиды в качестве ингибиторов киназ
PH12018500408A1 (en) Bicyclic compounds as atx inhibitors
EA201792536A1 (ru) Триазоловые агонисты рецептора apj
EA201790395A1 (ru) Производные аминотриазина, подходящие для применения в качестве соединений-ингибиторов tank-связывающей киназы
MX2018001890A (es) Compuestos biciclicos como inhibidores de autotaxina (atx).
PH12018500409A1 (en) New bicyclic compounds as dual atx/ca inhibitors
EA201591889A1 (ru) 6-(5-гидрокси-1h-пиразол-1-ил)никотинамидные ингибиторы phd
JO3793B1 (ar) مثبطات تيروزين كاينيز بروتون وأساليب استخدامها
CL2017000484A1 (es) Compuestos de azetidiniloxifenilpirrolidina
PH12018500406A1 (en) Bicyclic compounds as atx inhibitors

Legal Events

Date Code Title Description
FG Grant or registration