MX347615B - Derivados de pirazol y su uso como antagonistas de lpar5. - Google Patents

Derivados de pirazol y su uso como antagonistas de lpar5.

Info

Publication number
MX347615B
MX347615B MX2014014011A MX2014014011A MX347615B MX 347615 B MX347615 B MX 347615B MX 2014014011 A MX2014014011 A MX 2014014011A MX 2014014011 A MX2014014011 A MX 2014014011A MX 347615 B MX347615 B MX 347615B
Authority
MX
Mexico
Prior art keywords
compounds
lpa receptor
receptor lpar5
formula
platelet
Prior art date
Application number
MX2014014011A
Other languages
English (en)
Other versions
MX2014014011A (es
Inventor
Nazaré Marc
Kozian Detlef
Evers Andreas
Czechtizky Werngard
Original Assignee
Sanofi Sa
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 Sanofi Sa filed Critical Sanofi Sa
Publication of MX2014014011A publication Critical patent/MX2014014011A/es
Publication of MX347615B publication Critical patent/MX347615B/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente invención se refiere a compuestos de la fórmula I, en donde los residuos R1 a R5, V, G y M tienen los significados que se indican en las reivindicaciones. Los compuestos de la fórmula I son valiosos compuestos farmacológicamente activos para uso en el tratamiento de diversos trastornos, por ejemplo trastornos cardiovasculares tales como enfermedades tromboembólicas o restenosis. Los compuestos de la invención son eficaces antagonistas del receptor LPAR5 (GPR92) plaquetario de LPA y en general se pueden aplicar en condiciones en las cuales esté presente una activación indeseada del receptor LPAR5 plaquetario de LPA, del receptor LPAR5 mastocítico de LPA o del receptor LPAR5 de células microgliales de LPA, o bien para cuya cura o prevención se desee una inhibición del receptor LPAR5 plaquetario, mastocítico o de células microgliales de LPA. La invención se refiere además a procedimientos para preparar compuestos de la fórmula I, a su uso, en particular como ingredientes activos en medicamentos, y a composiciones farmacéuticas que los comprenden. (ver Fórmula).
MX2014014011A 2012-05-18 2013-05-16 Derivados de pirazol y su uso como antagonistas de lpar5. MX347615B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12305552 2012-05-18
PCT/EP2013/060171 WO2013171317A1 (en) 2012-05-18 2013-05-16 Pyrazole derivatives and their use as lpar5 antagonists

Publications (2)

Publication Number Publication Date
MX2014014011A MX2014014011A (es) 2015-02-12
MX347615B true MX347615B (es) 2017-05-04

Family

ID=48446368

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2014014011A MX347615B (es) 2012-05-18 2013-05-16 Derivados de pirazol y su uso como antagonistas de lpar5.

Country Status (22)

Country Link
US (1) US9346762B2 (es)
EP (1) EP2882715B1 (es)
JP (1) JP6257596B2 (es)
KR (1) KR20150010973A (es)
CN (1) CN104302625B (es)
AU (1) AU2013261718B2 (es)
BR (1) BR112014028406A2 (es)
CA (1) CA2871542A1 (es)
CY (1) CY1118618T1 (es)
DK (1) DK2882715T3 (es)
ES (1) ES2612205T3 (es)
HR (1) HRP20170098T1 (es)
HU (1) HUE032890T2 (es)
IL (1) IL235221A (es)
LT (1) LT2882715T (es)
MX (1) MX347615B (es)
PL (1) PL2882715T3 (es)
PT (1) PT2882715T (es)
RU (1) RU2645344C2 (es)
SG (1) SG11201407210SA (es)
SI (1) SI2882715T1 (es)
WO (1) WO2013171317A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015521183A (ja) 2012-05-18 2015-07-27 サノフイ ピリジン誘導体および病理学的血栓形成に関連する状態の治療へのその使用
JP6944442B2 (ja) * 2015-06-12 2021-10-06 ベットーレ リミテッド ライアビリティー カンパニーＶｅｔｔｏｒｅ， Ｌｌｃ 疾患を治療するためのｍｃｔ４阻害剤
WO2018111904A1 (en) * 2016-12-12 2018-06-21 Vettore, LLC Heterocyclic inhibitors of mct4
WO2024092205A1 (en) * 2022-10-27 2024-05-02 The Trustees Of Indiana University Inhibition of ship1 as a therapeutic strategy for the treatment of alzheimer's disease

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1230441B (it) 1989-02-07 1991-10-23 Acraf Eteri della serie dell'indazolo
EP1537074B1 (en) 2002-09-04 2019-02-27 Merck Canada Inc. Cathepsin cysteine protease inhibitors
AU2008215490A1 (en) 2007-02-09 2008-08-21 Takeda Pharmaceutical Company Limited Fused ring compounds as partial agonists of PPAR-gamma
JP5560202B2 (ja) 2007-12-26 2014-07-23 サノフイ Ｐ２ｙ１２拮抗薬としてのピラゾール−カルボキサミド誘導体
PL2254869T3 (pl) 2008-03-07 2017-10-31 Acraf Nowe pochodne 1-benzylo-3-hydroksymetyloindazolu i ich zastosowanie w leczeniu chorób bazujących na ekspresji CX3CR1 i p40
PL2262778T3 (pl) 2008-03-07 2020-02-28 Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. Pochodne 1-benzylo-3-hydroksymetyloindazolu i ich zastosowanie w leczeniu chorób opartych na ekspresji MCP-1, CXCR1 i p40
AR075874A1 (es) * 2009-03-19 2011-05-04 Sanofi Aventis Derivados de indazol inhibidores de hsp90 composiciones que los contienen y utilizacion
KR101736301B1 (ko) * 2009-08-03 2017-05-29 아지엔드 키미쉐 리유나이트 안젤리니 프란체스코 에이.씨.알.에이.에프. 에스.피.에이 1-벤질-3-하이드록시메틸-1ｈ-인다졸 및 이의 유도체 및 필요한 마그네슘 중간체들의 제조 방법
WO2012028243A1 (en) * 2010-09-02 2012-03-08 Merck Patent Gmbh Pyrazolopyridinone derivatives as lpa receptor antagonists
JP2015521183A (ja) 2012-05-18 2015-07-27 サノフイ ピリジン誘導体および病理学的血栓形成に関連する状態の治療へのその使用

Also Published As

Publication number Publication date
DK2882715T3 (en) 2017-02-13
WO2013171317A1 (en) 2013-11-21
US20150141477A1 (en) 2015-05-21
US9346762B2 (en) 2016-05-24
RU2645344C2 (ru) 2018-02-21
LT2882715T (lt) 2017-02-10
BR112014028406A2 (pt) 2017-06-27
IL235221A (en) 2016-06-30
CN104302625B (zh) 2017-04-19
CA2871542A1 (en) 2013-11-21
CY1118618T1 (el) 2017-07-12
EP2882715B1 (en) 2016-11-09
HRP20170098T1 (hr) 2017-03-24
JP6257596B2 (ja) 2018-01-10
AU2013261718B2 (en) 2017-10-19
AU2013261718A1 (en) 2014-12-18
JP2015517514A (ja) 2015-06-22
HUE032890T2 (hu) 2017-11-28
EP2882715A1 (en) 2015-06-17
ES2612205T3 (es) 2017-05-12
SI2882715T1 (sl) 2017-03-31
MX2014014011A (es) 2015-02-12
KR20150010973A (ko) 2015-01-29
SG11201407210SA (en) 2014-12-30
CN104302625A (zh) 2015-01-21
PT2882715T (pt) 2016-12-30
RU2014151360A (ru) 2016-07-10
PL2882715T3 (pl) 2017-04-28

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