AU2013261718B2 - Pyrazole derivatives and their use as LPAR5 antagonists - Google Patents

Pyrazole derivatives and their use as LPAR5 antagonists Download PDF

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Publication number
AU2013261718B2
AU2013261718B2 AU2013261718A AU2013261718A AU2013261718B2 AU 2013261718 B2 AU2013261718 B2 AU 2013261718B2 AU 2013261718 A AU2013261718 A AU 2013261718A AU 2013261718 A AU2013261718 A AU 2013261718A AU 2013261718 B2 AU2013261718 B2 AU 2013261718B2
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AU
Australia
Prior art keywords
alkyl
series consisting
crc4
cycloalkyl
substituted
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Ceased
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AU2013261718A
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English (en)
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AU2013261718A1 (en
Inventor
Werngard Czechtizky
Andreas Evers
Detlef Kozian
Marc Nazare
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Sanofi SA
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Sanofi SA
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Publication of AU2013261718A1 publication Critical patent/AU2013261718A1/en
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Publication of AU2013261718B2 publication Critical patent/AU2013261718B2/en
Ceased legal-status Critical Current
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    • 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
    • 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
    • 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)
  • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2013261718A 2012-05-18 2013-05-16 Pyrazole derivatives and their use as LPAR5 antagonists Ceased AU2013261718B2 (en)

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
AU2013261718A1 AU2013261718A1 (en) 2014-12-18
AU2013261718B2 true AU2013261718B2 (en) 2017-10-19

Family

ID=48446368

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2013261718A Ceased AU2013261718B2 (en) 2012-05-18 2013-05-16 Pyrazole derivatives and their use as LPAR5 antagonists

Country Status (22)

Country Link
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 (6)

* 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
AU2016277126A1 (en) * 2015-06-12 2017-12-14 Vettore, LLC MCT4 inhibitors for treating disease
BR112019011825A2 (pt) 2016-12-12 2019-10-22 Vettore, LLC composto, enantiômero isolado, composição farmacêutica, método para inibir a atividade do transportador de monocarboxilato mct4, ou um mutante do mesmo, em uma amostra biológica, método para inibir a atividade do transportador de monocarboxilato mct4, ou um mutante do mesmo, em relação ao transportador de monocarboxilato mct1, ou um mutante do mesmo, em um paciente, método para tratar um distúrbio mediado por transportador de monocarboxilato mct4 em um sujeito que necessite do mesmo, uso de um composto e método para obter um efeito em um paciente
KR20220077140A (ko) 2019-10-02 2022-06-08 도메인 테라퓨틱스 프로스타글란딘 e2(pge2) ep4 수용체 길항제
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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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
AU2008215490A1 (en) 2007-02-09 2008-08-21 Takeda Pharmaceutical Company Limited Fused ring compounds as partial agonists of PPAR-gamma
EP2238127B1 (en) 2007-12-26 2012-08-15 Sanofi Pyrazole-carboxamide derivatives as p2y12 antagonists
DK2254869T3 (en) 2008-03-07 2017-09-04 Acraf 1-BENZYL-3-HYDROXYMETHYL INDAZOLE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF DISEASES BASED ON THE EXPRESSION OF CX3CR1 AND P40
MX2010009625A (es) 2008-03-07 2010-09-28 Acraf Derivados de 1-bencil-3-hidroximetilindazol y uso de los mismos en el tratamiento de enfermedades basadas en la expresion de mcp-1, cx3cr1 y p40.
AU2010224652A1 (en) * 2009-03-19 2011-10-13 Sanofi Hsp90 inhibiting indazole derivatives, compositions containing same and use thereof
BR112012002130A2 (pt) * 2009-08-03 2015-09-15 Aziende Chimique Riunite Angelini Francesco A C R A F S P A processo para a preparação de composto,e, composto intermediário
JP6039559B2 (ja) * 2010-09-02 2016-12-07 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ Ｌｐａ受容体アンタゴニストとしてのピラゾロピリジノン誘導体
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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CAS Registry Accession Number: RN 1279828-94-2, Date Entered: 14/04/2011 *
CAS Registry Accession Number: RN 1279830-96-4, Date Entered: 14/04/2011 *
CAS Registry Accession Number: RN 1279831-82-1, Date Entered: 14/04/2011 *
CAS Registry Accession Number: RN 1279842-08-8, Date Entered: 14/04/2011 *
CAS Registry Accession Number: RN 1279845-01-0, Date Entered: 14/04/2011 *
CAS Registry Accession Number: RN 1279877-48-3, Date Entered: 24/04/2011 *

Also Published As

Publication number Publication date
EP2882715A1 (en) 2015-06-17
MX2014014011A (es) 2015-02-12
RU2014151360A (ru) 2016-07-10
AU2013261718A1 (en) 2014-12-18
CN104302625B (zh) 2017-04-19
BR112014028406A2 (pt) 2017-06-27
CN104302625A (zh) 2015-01-21
CY1118618T1 (el) 2017-07-12
US9346762B2 (en) 2016-05-24
WO2013171317A1 (en) 2013-11-21
HUE032890T2 (hu) 2017-11-28
PL2882715T3 (pl) 2017-04-28
LT2882715T (lt) 2017-02-10
PT2882715T (pt) 2016-12-30
RU2645344C2 (ru) 2018-02-21
JP2015517514A (ja) 2015-06-22
IL235221A (en) 2016-06-30
CA2871542A1 (en) 2013-11-21
US20150141477A1 (en) 2015-05-21
HRP20170098T1 (hr) 2017-03-24
JP6257596B2 (ja) 2018-01-10
MX347615B (es) 2017-05-04
SI2882715T1 (sl) 2017-03-31
DK2882715T3 (en) 2017-02-13
KR20150010973A (ko) 2015-01-29
EP2882715B1 (en) 2016-11-09
ES2612205T3 (es) 2017-05-12
SG11201407210SA (en) 2014-12-30

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