[go: up one dir, main page]

MX2017000485A - Espirocicloheptanos como inhibidores de la cinasa rho (rock). - Google Patents

Espirocicloheptanos como inhibidores de la cinasa rho (rock).

Info

Publication number
MX2017000485A
MX2017000485A MX2017000485A MX2017000485A MX2017000485A MX 2017000485 A MX2017000485 A MX 2017000485A MX 2017000485 A MX2017000485 A MX 2017000485A MX 2017000485 A MX2017000485 A MX 2017000485A MX 2017000485 A MX2017000485 A MX 2017000485A
Authority
MX
Mexico
Prior art keywords
disorders
compounds
inhibitors
espirocicloheptanos
rock
Prior art date
Application number
MX2017000485A
Other languages
English (en)
Other versions
MX376178B (es
Inventor
Wang Yufeng
W Glunz Peter
Ladziata Vladimir
Hu Zilun
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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (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 true MX2017000485A (es) 2017-04-27
MX376178B 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 (45)

* 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
ES2815681T3 (es) 2015-01-09 2021-03-30 Bristol Myers Squibb Co Ureas cíclicas como inhibidores de 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
TW201706265A (zh) 2015-03-09 2017-02-16 必治妥美雅史谷比公司 做為Rho激酶(ROCK)抑制劑之內醯胺
PT3340796T (pt) 2015-08-28 2021-07-28 Chdi Foundation Inc Sondas para imagens da proteína huntingtina
TWI730032B (zh) * 2016-01-13 2021-06-11 美商必治妥美雅史谷比公司 作為rock抑制劑之螺庚烷水楊酸醯胺及相關化合物
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
US20190256509A1 (en) * 2016-06-08 2019-08-22 Chrysalis, Inc. Histone demethylase inhibitors
WO2018009625A1 (en) 2016-07-07 2018-01-11 Bristol-Myers Squibb Company Spirolactams as inhibitors of rock
US10730858B2 (en) 2016-07-07 2020-08-04 Bristol-Myers Squibb Company Lactam, cyclic urea and carbamate, and triazolone derivatives as potent and selective rock 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
WO2018102325A1 (en) 2016-11-30 2018-06-07 Bristol-Myers Squibb Company Tricyclic rho kinase inhibitors
US11198680B2 (en) 2016-12-21 2021-12-14 BioAxone BioSciences, Inc. Rho kinase inhibitor BA-1049 (R) and active metabolites thereof
PL3558314T3 (pl) * 2016-12-21 2025-02-24 BioAxone BioSciences, Inc. Inhibitor kinazy rho ba-1049 (r) i jego aktywne metabolity
CA3047212A1 (en) * 2017-01-30 2018-08-02 Chiesi Farmaceutici S.P.A. Tyrosine amide derivatives as rho- kinase inhibitors
EP3647311B1 (en) 2017-06-30 2023-11-01 Beijing Tide Pharmaceutical Co., Ltd. Rho-associated protein kinase inhibitor, pharmaceutical composition comprising same, and preparation method and use thereof
CN110582491B (zh) * 2017-06-30 2023-09-29 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
WO2019014322A1 (en) 2017-07-11 2019-01-17 BioAxone BioSciences, Inc. KINASE INHIBITORS FOR THE TREATMENT OF DISEASES
US12060341B2 (en) * 2017-07-12 2024-08-13 Bristol-Myers Squibb Company Spiroheptanyl hydantoins as ROCK inhibitors
EP3652164B1 (en) 2017-07-12 2023-06-21 Bristol-Myers Squibb Company Phenylacetamides as inhibitors of rock
KR102644889B1 (ko) * 2017-07-12 2024-03-06 브리스톨-마이어스 스큅 컴퍼니 Rock 억제제로서의 스피로헵타닐 히단토인
JP7234201B2 (ja) * 2017-07-12 2023-03-07 ブリストル-マイヤーズ スクイブ カンパニー 心不全の治療のためのrockの5員アミノヘテロ環および5,6-または6,6員二環式アミノヘテロ環の阻害剤
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
AU2018326785B2 (en) * 2017-09-03 2023-03-02 Angion Biomedica Corp. Vinylheterocycles as Rho-associated coiled-coil kinase (ROCK) inhibitors
WO2019089868A1 (en) 2017-11-03 2019-05-09 Bristol-Myers Squibb Company Diazaspiro rock inhibitors
WO2020037079A1 (en) 2018-08-14 2020-02-20 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
US11691971B2 (en) 2020-06-19 2023-07-04 Incyte Corporation Naphthyridinone compounds as JAK2 V617F inhibitors
WO2021257863A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Pyrrolotriazine compounds as jak2 v617f inhibitors
BR112023000047A2 (pt) 2020-07-02 2023-03-14 Incyte Corp Compostos de ureia tricíclicos como inibidores da v617f da jak2
US11767323B2 (en) 2020-07-02 2023-09-26 Incyte Corporation Tricyclic pyridone 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
EP4251621A1 (en) * 2020-11-25 2023-10-04 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
TW202302589A (zh) 2021-02-25 2023-01-16 美商英塞特公司 作為jak2 v617f抑制劑之螺環內醯胺
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
EP4493558A1 (en) 2022-03-17 2025-01-22 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
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)

* 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
ATE124408T1 (de) 1990-10-16 1995-07-15 Takeda Chemical Industries Ltd Heterozyklische aminderivate, deren herstellung und deren verwendung.
EP0634402A1 (en) 1993-07-14 1995-01-18 Takeda Chemical Industries, Ltd. Isochinolinone derivatives, their production and use
WO1998038168A1 (en) 1997-02-27 1998-09-03 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
EA006300B1 (ru) 2000-10-30 2005-10-27 Кудос Фармасеутикалс Лимитед Производные фталазинона
US7402595B2 (en) 2002-02-13 2008-07-22 Takeda Pharmaceutical Company Limited 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)
WO2006036981A2 (en) 2004-09-28 2006-04-06 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
RU2008148962A (ru) * 2006-05-12 2010-06-20 Вертекс Фармасьютикалз Инкорпорейтед (Us) Избирательно действующие ингибиторы rоск протеинкиназы и их применение
RU2008152065A (ru) * 2006-06-08 2010-07-20 Убе Индастриз, Лтд (Jp) Новое производное имидазола со спироциклической структурой в боковой цепи
EP2526948A1 (en) 2006-09-20 2012-11-28 Aerie Pharmaceuticals, Inc. RHO kinase inhibitors
WO2008077551A1 (en) 2006-12-27 2008-07-03 Sanofi-Aventis Cycloalkylamine substituted isoquinolone derivatives
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
WO2008086014A2 (en) 2007-01-09 2008-07-17 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
US20120190668A1 (en) 2009-08-12 2012-07-26 Oehlen Lambertus J W M Enhancement of cellular transplantation using small moleucle modulators of 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
EA033220B1 (ru) 2013-01-18 2019-09-30 Бристол-Майерс Сквибб Компани Фталазиноны и изохинолиноны в качестве ингибиторов rock
US9828345B2 (en) 2013-02-28 2017-11-28 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent ROCK1 and ROCK2 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
JP6370368B2 (ja) * 2013-03-27 2018-08-08 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Brd4阻害剤としてのインドリノン類似体
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
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
CN105518005B (zh) 2013-07-02 2018-07-20 百时美施贵宝公司 作为rock抑制剂的三环吡啶-甲酰胺衍生物
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

Also Published As

Publication number Publication date
CN106817899A (zh) 2017-06-09
PH12017500072A1 (en) 2017-05-15
JP2017520604A (ja) 2017-07-27
MA39554A2 (es) 2018-01-31
UY36215A (es) 2016-01-29
AU2015289897A1 (en) 2017-03-09
CN106817899B (zh) 2021-03-09
ZA201700304B (en) 2018-12-19
US20160016914A1 (en) 2016-01-21
IL250046B (en) 2020-03-31
SG11201700251PA (en) 2017-02-27
US20180155296A1 (en) 2018-06-07
MA39554B1 (fr) 2020-05-29
BR112017000808A2 (pt) 2017-12-05
CL2017000089A1 (es) 2017-09-15
ES2716415T3 (es) 2019-06-12
JP6721741B2 (ja) 2020-07-15
US9902702B2 (en) 2018-02-27
KR20170023187A (ko) 2017-03-02
MX376178B (es) 2025-03-07
WO2016010950A1 (en) 2016-01-21
AR101208A1 (es) 2016-11-30
JP2019112447A (ja) 2019-07-11
KR102420938B1 (ko) 2022-07-14
MA39554A3 (fr) 2019-05-31
CA2954976A1 (en) 2016-01-21
AU2015289897B2 (en) 2019-07-18
EP3169682A1 (en) 2017-05-24
PE20170672A1 (es) 2017-05-22
EA033061B1 (ru) 2019-08-30
CO2017001152A2 (es) 2017-05-19
TN2017000009A1 (en) 2018-07-04
EP3169682B1 (en) 2018-12-26
TW201607933A (zh) 2016-03-01
EA201790062A1 (ru) 2017-08-31
JP6499749B2 (ja) 2019-04-10

Similar Documents

Publication Publication Date Title
MX2017000485A (es) Espirocicloheptanos como inhibidores de la cinasa rho (rock).
CO2018008173A2 (es) Salicilamidas de espiroheptanos y compuestos relacionados como inhibidores de cinasa rho (rock)
AR103895A1 (es) Lactamas como inhibidores de rock
CO2017003833A2 (es) Pirimidinonas como inhibidores del factor xia
UY35971A (es) Macrociclos con grupos p2? aromáticos como inhibidores del factor xia
CL2017000902A1 (es) Dihidropirrolopiridinas inhibidoras de ror-gamma
CU20160167A7 (es) Compuestos de pirazolopiridinas y pirazolopirimidinas útiles en el tratamiento de condiciones alérgicas y respiratorias
CO2019014455A2 (es) Amidas heterocíclicas de 5 miembros y bicíclicas como inhibidores de rock
EA201790202A1 (ru) Фталазиноны и изохинолиноны в качестве ингибиторов rock
UY35972A (es) Inhibidores macrocíclicos de fxia que tienen grupos heterocíclicos
EA201890308A1 (ru) Замещенные азасоединения как ингибиторы irak-4
PH12016502382A1 (en) Substituted indazole compounds as irak4 inhibitors
UY34960A (es) Dihidropiridona p1 como inhibidores del factor xia
UY34959A (es) Dihidropiridona p1 como inhibidores del factor xia
EA201890307A1 (ru) Индазольные и азаиндазольные соединения как ингибиторы irak-4
DOP2015000158A (es) Inhibidores de prmt5 y sus usos
ECSP17021897A (es) Compuestos y composiciones como inhibidores de quinasa raf
EA201790395A1 (ru) Производные аминотриазина, подходящие для применения в качестве соединений-ингибиторов tank-связывающей киназы
MX2015012867A (es) Compuestos aromaticos multisustituidos como inhibidores de serina proteasa.
MX2021005052A (es) Oxiesteroles y métodos de uso de los mismos.
EA201591634A1 (ru) Дигидропиридопиримидиновые соединения
DOP2015000201A (es) Compuestos de azabencimidazol como inhibidores de pde4 isoenzimas para el tratamiento del snc y otros trastornos
EA201691670A1 (ru) Тетразолонзамещенные дигидропиридиноновые ингибиторы mgat2
CO2017000011A2 (es) Derivados de quinolizinona como inhibidores de pi3k
CL2017000484A1 (es) Compuestos de azetidiniloxifenilpirrolidina

Legal Events

Date Code Title Description
FG Grant or registration