CN104302625B - 吡唑衍生物及其作为lpar5拮抗剂的用途 - Google Patents

吡唑衍生物及其作为lpar5拮抗剂的用途 Download PDF

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Publication number
CN104302625B
CN104302625B CN201380025967.9A CN201380025967A CN104302625B CN 104302625 B CN104302625 B CN 104302625B CN 201380025967 A CN201380025967 A CN 201380025967A CN 104302625 B CN104302625 B CN 104302625B
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China
Prior art keywords
alkyl
methyl
phenyl
benzoic acid
pyrazole
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Expired - Fee Related
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CN201380025967.9A
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Chinese (zh)
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CN104302625A (zh
Inventor
M·纳扎雷
D·科齐安
A·埃弗斯
W·切赫蒂泽凯
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Sanofi Aventis France
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Sanofi Aventis France
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    • 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
    • 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
    • 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
    • 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

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  • 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)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201380025967.9A 2012-05-18 2013-05-16 吡唑衍生物及其作为lpar5拮抗剂的用途 Expired - Fee Related CN104302625B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12305552 2012-05-18
EP12305552.7 2012-05-18
PCT/EP2013/060171 WO2013171317A1 (en) 2012-05-18 2013-05-16 Pyrazole derivatives and their use as lpar5 antagonists

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Publication Number Publication Date
CN104302625A CN104302625A (zh) 2015-01-21
CN104302625B true CN104302625B (zh) 2017-04-19

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CN201380025967.9A Expired - Fee Related CN104302625B (zh) 2012-05-18 2013-05-16 吡唑衍生物及其作为lpar5拮抗剂的用途

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

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013171316A1 (en) 2012-05-18 2013-11-21 Sanofi Pyridine derivatives and their use in the treatment of conditions associated with pathological thrombus formation
KR102653599B1 (ko) 2015-06-12 2024-04-01 베토어 엘엘씨 질환 치료용 mct4 저해제
KR102615828B1 (ko) 2016-12-12 2023-12-20 베토어 엘엘씨 Mct4 의 헤테로시클릭 저해제
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
CN119930520A (zh) * 2023-11-03 2025-05-06 中国药科大学 N-芳基吡唑类化合物及其药物组合物和应用

Citations (4)

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CN101945855A (zh) * 2008-03-07 2011-01-12 方济各安吉利克化学联合股份有限公司 1-苄基-3-羟基甲基吲唑衍生物及其在治疗基于mcp-1、cx3cr1表达的疾病中的用途
WO2011015501A1 (en) * 2009-08-03 2011-02-10 Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. Process for the preparation of 1-benzyl-3-hydr0xymethyl-1h-indaz0le and its derivatives and required magnesium intermediates
WO2012028243A1 (en) * 2010-09-02 2012-03-08 Merck Patent Gmbh Pyrazolopyridinone derivatives as lpa receptor antagonists
CN102439003A (zh) * 2009-03-19 2012-05-02 赛诺菲 抑制hsp90的吲唑衍生物、含有所述衍生物的组合物及其用途

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IT1230441B (it) 1989-02-07 1991-10-23 Acraf Eteri della serie dell'indazolo
CA2495939A1 (en) 2002-09-04 2004-03-18 Merck Frosst Canada & Co./Merck Frosst Canada & Cie Cathepsin cysteine protease inhibitors
BRPI0807014A2 (pt) 2007-02-09 2014-04-22 Takeda Pharmaceutical Composto, pró-droga, agente farmacêutico, métodos para melhorar a resistência a insulina em um mamífero, método para a profilaxia ou o tratamento de diabetes em um mamífero, e, uso de um composto.
WO2009080227A2 (en) 2007-12-26 2009-07-02 Sanofi-Aventis Pyrazole-carboxamide derivatives as p2y12 antagonists
DK2262778T5 (da) 2008-03-07 2020-06-08 Acraf 1-benzyl-3-hydroxymethylindazolderivativer og brug deraf i behandling af sygdomme baseret på ekspression af mcp-1, cx3cr1 og p40
WO2013171316A1 (en) 2012-05-18 2013-11-21 Sanofi Pyridine derivatives and their use in the treatment of conditions associated with pathological thrombus formation

Patent Citations (4)

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CN101945855A (zh) * 2008-03-07 2011-01-12 方济各安吉利克化学联合股份有限公司 1-苄基-3-羟基甲基吲唑衍生物及其在治疗基于mcp-1、cx3cr1表达的疾病中的用途
CN102439003A (zh) * 2009-03-19 2012-05-02 赛诺菲 抑制hsp90的吲唑衍生物、含有所述衍生物的组合物及其用途
WO2011015501A1 (en) * 2009-08-03 2011-02-10 Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. Process for the preparation of 1-benzyl-3-hydr0xymethyl-1h-indaz0le and its derivatives and required magnesium intermediates
WO2012028243A1 (en) * 2010-09-02 2012-03-08 Merck Patent Gmbh Pyrazolopyridinone derivatives as lpa receptor antagonists

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Nonpeptide Factor Xa Inhibitors: DPC423, A Highly Potent and Orally Bioavailable Pyrazole Antithrombotic Agent;Pancras C. Wong，等;《Cardiovascular Drug Reviews》;20021231;第20卷(第2期);137-152 *
Synthesis, structure and inhibitory effects on cyclooxygenase,lipoxygenase, thromboxane synthetase and platelet aggregation of 3-amino-4,5-dihydro-1H-pyrazole derivatives;Jordi FRIGOLA，等;《Eur. J. Med. Chem.》;19891231;第24卷;435-445 *

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HUE032890T2 (hu) 2017-11-28
US20150141477A1 (en) 2015-05-21
CN104302625A (zh) 2015-01-21
EP2882715A1 (en) 2015-06-17
IL235221A (en) 2016-06-30
SG11201407210SA (en) 2014-12-30
SI2882715T1 (sl) 2017-03-31
PT2882715T (pt) 2016-12-30
US9346762B2 (en) 2016-05-24
RU2645344C2 (ru) 2018-02-21
CY1118618T1 (el) 2017-07-12
PL2882715T3 (pl) 2017-04-28
EP2882715B1 (en) 2016-11-09
CA2871542A1 (en) 2013-11-21
JP6257596B2 (ja) 2018-01-10
LT2882715T (lt) 2017-02-10
DK2882715T3 (en) 2017-02-13
BR112014028406A2 (pt) 2017-06-27
HRP20170098T1 (hr) 2017-03-24
ES2612205T3 (es) 2017-05-12
KR20150010973A (ko) 2015-01-29
WO2013171317A1 (en) 2013-11-21
MX2014014011A (es) 2015-02-12
AU2013261718A1 (en) 2014-12-18
AU2013261718B2 (en) 2017-10-19
RU2014151360A (ru) 2016-07-10
JP2015517514A (ja) 2015-06-22
MX347615B (es) 2017-05-04

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