RU2645344C2 - Производные пиразола и их применение в качестве lpar5 антагонистов - Google Patents

Производные пиразола и их применение в качестве lpar5 антагонистов Download PDF

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RU2645344C2
RU2645344C2 RU2014151360A RU2014151360A RU2645344C2 RU 2645344 C2 RU2645344 C2 RU 2645344C2 RU 2014151360 A RU2014151360 A RU 2014151360A RU 2014151360 A RU2014151360 A RU 2014151360A RU 2645344 C2 RU2645344 C2 RU 2645344C2
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alkyl
group
methyl
pyrazol
substituted
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RU2014151360A
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Russian (ru)
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RU2014151360A (ru
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Марк Назаре
Детлеф КОЦИАН
Андреас ЭФЕРС
Вернгард ЧЕХТИЗКИЙ
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Санофи
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic 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
    • C07D231/12Heterocyclic 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
    • 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
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/10Drugs 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
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic 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
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
RU2014151360A 2012-05-18 2013-05-16 Производные пиразола и их применение в качестве lpar5 антагонистов RU2645344C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12305552.7 2012-05-18
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
RU2014151360A RU2014151360A (ru) 2016-07-10
RU2645344C2 true RU2645344C2 (ru) 2018-02-21

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

Families Citing this family (6)

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Publication number Priority date Publication date Assignee Title
EP2850062B1 (en) 2012-05-18 2017-07-19 Sanofi Pyridine derivatives and their use in the treatment of conditions associated with pathological thrombus formation
BR112017026535B1 (pt) 2015-06-12 2023-12-19 Vettore, LLC Composto e composição farmacêutica
WO2018111904A1 (en) 2016-12-12 2018-06-21 Vettore, LLC Heterocyclic inhibitors of mct4
PL4038052T3 (pl) 2019-10-02 2024-08-26 Domain Therapeutics Antagoniści receptora ep4 prostaglandyny e2 (pge2)
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
CN119930520B (zh) * 2023-11-03 2026-03-06 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 (3)

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WO2009109618A2 (en) * 2008-03-07 2009-09-11 Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. Novel 1-benzyl-3-hydroxymethylindazole derivatives and use thereof in the treatment of diseases based on the expression of mcp-1, cx3cr1 and p40
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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IT1230441B (it) 1989-02-07 1991-10-23 Acraf Eteri della serie dell'indazolo
US7279478B2 (en) 2002-09-04 2007-10-09 Merck Frosst Canada & Co. Cathepsin cysteine protease inhibitors
EP2118066A1 (en) 2007-02-09 2009-11-18 Takeda Pharmaceutical Company Limited Fused ring compounds as partial agonists of ppar-gamma
WO2009080227A2 (en) 2007-12-26 2009-07-02 Sanofi-Aventis Pyrazole-carboxamide derivatives as p2y12 antagonists
JP5509100B2 (ja) 2008-03-07 2014-06-04 アジェンデ・キミケ・リウニテ・アンジェリニ・フランチェスコ・ア・チ・エレ・ア・エフェ・ソシエタ・ペル・アチオニ 新規な1−ベンジル−3−ヒドロキシメチルインダゾール誘導体及びそのMCP−1,CX3CR1及びp40の発現に基づく疾病の治療への使用
KR20110128942A (ko) * 2009-03-19 2011-11-30 사노피 Hsp90 억제 인다졸 유도체, 그를 함유하는 조성물 및 그의 용도
EP2850062B1 (en) 2012-05-18 2017-07-19 Sanofi Pyridine derivatives and their use in the treatment of conditions associated with pathological thrombus formation

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WO2009109618A2 (en) * 2008-03-07 2009-09-11 Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. Novel 1-benzyl-3-hydroxymethylindazole derivatives and use thereof in the treatment of diseases based on the expression of mcp-1, cx3cr1 and p40
EA201071038A1 (ru) * 2008-03-07 2011-02-28 Ацьенде Кимике Рьюните Анджелини Франческо А.К.Р.А.Ф. С.П.А. Производные 1-бензил-3-гидроксиметилиндазола и их применение для лечения заболеваний, основанных на экспрессии mcp-1, cx3cr1 и p40
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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FRIGOLA J ET AL. Synthesis, structure and inhibitory effects on cyclooxygenase, lipoxygenase, thromboxane synthetase and platelet aggregation of 3-amino-4,5-dihydro-1H-pyrazole derivatives, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1989, vol. 24, no. 4, (1989), pages 435-445. *
GUOGANG TU ET AL. Design, synthesis and biological evaluation of CB1 cannabinoid receptor ligands derived from the 1,5-diarylpyrazole scaffold, JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2011, vol. 26, no. 2, pages 222-230. *
GUOGANG TU ET AL. Design, synthesis and biological evaluation of CB1 cannabinoid receptor ligands derived from the 1,5-diarylpyrazole scaffold, JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2011, vol. 26, no. 2, pages 222-230. WONG PANCRAS C ET AL. NONPEPTIDE FACTOR XA INHIBITORS: DPC423, A HIGHLY POTENT AND ORALLY BIOAVAILABLE PYRAZOLE ANTITHROMBOTIC AGENT, CARDIOVASCULAR DRUG REVIEWS, 2002, vol. 20, no. 2, pages 137-152. FRIGOLA J ET AL. Synthesis, structure and inhibitory effects on cyclooxygenase, lipoxygenase, thromboxane synthetase and platelet aggregation of 3-amino-4,5-dihydro-1H-pyrazole derivatives, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1989, vol. 24, no. 4, (1989), pages 435-445. База данных REGYSTRY [онлайн], соединения с *
WONG PANCRAS C ET AL. NONPEPTIDE FACTOR XA INHIBITORS: DPC423, A HIGHLY POTENT AND ORALLY BIOAVAILABLE PYRAZOLE ANTITHROMBOTIC AGENT, CARDIOVASCULAR DRUG REVIEWS, 2002, vol. 20, no. 2, pages 137-152. *
База данных REGYSTRY [онлайн], соединения с RN 1279877-48-3, 14.04.2011; 1279828-94-2, 14.04.2011; 1279874-70-2, 14.04.2011; 1279835-18-5, 14.04.2011; 1279832-42-6, 14.04.2011; 1279831-87-6, 14.04.2011; 1279845-01-0, 14.04.2011; 1279842-08-8, 14.04.2011; 1279831-82-1, 14.04.2011; 1279830-96-4, 14.04.2011. *

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Publication number Publication date
SI2882715T1 (sl) 2017-03-31
EP2882715A1 (en) 2015-06-17
SG11201407210SA (en) 2014-12-30
US9346762B2 (en) 2016-05-24
JP6257596B2 (ja) 2018-01-10
DK2882715T3 (en) 2017-02-13
CA2871542A1 (en) 2013-11-21
AU2013261718A1 (en) 2014-12-18
KR20150010973A (ko) 2015-01-29
RU2014151360A (ru) 2016-07-10
CN104302625B (zh) 2017-04-19
US20150141477A1 (en) 2015-05-21
CN104302625A (zh) 2015-01-21
PL2882715T3 (pl) 2017-04-28
CY1118618T1 (el) 2017-07-12
MX2014014011A (es) 2015-02-12
HUE032890T2 (hu) 2017-11-28
IL235221A (en) 2016-06-30
BR112014028406A2 (pt) 2017-06-27
WO2013171317A1 (en) 2013-11-21
JP2015517514A (ja) 2015-06-22
ES2612205T3 (es) 2017-05-12
LT2882715T (lt) 2017-02-10
PT2882715T (pt) 2016-12-30
EP2882715B1 (en) 2016-11-09
HRP20170098T1 (hr) 2017-03-24
MX347615B (es) 2017-05-04
AU2013261718B2 (en) 2017-10-19

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