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

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=)

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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
EP3942934A1 (en) 2015-06-12 2022-01-26 Vettore, LLC Mct4 inhibitors for treating disease
US10214492B2 (en) 2016-12-12 2019-02-26 Vettore, LLC Heterocyclic inhibitors of MCT4
CN114555573B (zh) 2019-10-02 2025-08-15 多曼治疗学公司 前列腺素e2(pge2)ep4受体拮抗剂
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

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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
EP1537074B1 (en) 2002-09-04 2019-02-27 Merck Canada Inc. Cathepsin cysteine protease inhibitors
JP2010517935A (ja) 2007-02-09 2010-05-27 武田薬品工業株式会社 Ppar−ガンマのパーシャルアゴニストとしての縮合環化合物
EP2238127B1 (en) 2007-12-26 2012-08-15 Sanofi Pyrazole-carboxamide derivatives as p2y12 antagonists
HRP20191953T8 (hr) 2008-03-07 2021-06-25 Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. DERIVATI 1-BENZIL-3-HIDROKSIMETILINDAZOLA I NJIHOVA UPORABA U LIJEČENJU BOLESTI KOJE SE BAZIRAJU NA EKSPRESIJI MCP-1, CX3CR1 i P40
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
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

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

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