MX2014014011A - 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
- MX2014014011A MX2014014011A MX2014014011A MX2014014011A MX2014014011A MX 2014014011 A MX2014014011 A MX 2014014011A MX 2014014011 A MX2014014011 A MX 2014014011A MX 2014014011 A MX2014014011 A MX 2014014011A MX 2014014011 A MX2014014011 A MX 2014014011A
- Authority
- MX
- Mexico
- Prior art keywords
- compounds
- lpa receptor
- receptor lpar5
- formula
- platelet
- Prior art date
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
- 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
Landscapes
- 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)
- Hematology (AREA)
- Neurology (AREA)
- Diabetes (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)
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).
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 true MX2014014011A (es) | 2015-02-12 |
MX347615B 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)
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 |
EP3307068B1 (en) * | 2015-06-12 | 2021-08-25 | Vettore, LLC | Mct4 inhibitors for treating disease |
US10214492B2 (en) * | 2016-12-12 | 2019-02-26 | 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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IT1230441B (it) | 1989-02-07 | 1991-10-23 | Acraf | Eteri della serie dell'indazolo |
JP4505329B2 (ja) | 2002-09-04 | 2010-07-21 | メルク フロスト カナダ リミテツド | カテプシンシステインプロテアーゼ阻害薬 |
WO2008099794A1 (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 |
KR101581828B1 (ko) | 2008-03-07 | 2015-12-31 | 아지엔드 키미쉐 리유나이트 안젤리니 프란체스코 에이.씨.알.에이.에프. 에스.피.에이 | 신규한 1-벤질-3-하이드록시메틸인다졸 유도체들 및 mcp-1, cx3cr1 및 p40의 발현을 기초로 한 질환들의 치료에서 이의 용도 |
KR101640844B1 (ko) | 2008-03-07 | 2016-07-19 | 아지엔드 키미쉐 리유나이트 안젤리니 프란체스코 에이.씨.알.에이.에프. 에스.피.에이 | 1-벤질-3-하이드록시메틸인다졸 유도체들 및 mcp-1, cx3cr1 및 p40의 발현을 기초로 한 질환들의 치료에서 이의 용도 |
AR075874A1 (es) * | 2009-03-19 | 2011-05-04 | Sanofi Aventis | Derivados de indazol inhibidores de hsp90 composiciones que los contienen y utilizacion |
ES2481393T3 (es) * | 2009-08-03 | 2014-07-30 | Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. | Procedimiento para la preparación de 1-bencil-3-hidroximetil-1H-indazol y sus derivados y productos intermedios de magnesio requeridos |
CN103189378B (zh) * | 2010-09-02 | 2016-03-02 | 默克专利股份公司 | 作为lpa受体拮抗剂的吡唑并吡啶酮衍生物 |
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 |
-
2013
- 2013-05-16 CN CN201380025967.9A patent/CN104302625B/zh not_active Expired - Fee Related
- 2013-05-16 LT LTEP13723151.0T patent/LT2882715T/lt unknown
- 2013-05-16 ES ES13723151.0T patent/ES2612205T3/es active Active
- 2013-05-16 US US14/401,050 patent/US9346762B2/en active Active
- 2013-05-16 MX MX2014014011A patent/MX347615B/es active IP Right Grant
- 2013-05-16 EP EP13723151.0A patent/EP2882715B1/en not_active Expired - Fee Related
- 2013-05-16 PL PL13723151T patent/PL2882715T3/pl unknown
- 2013-05-16 BR BR112014028406A patent/BR112014028406A2/pt not_active Application Discontinuation
- 2013-05-16 JP JP2015512072A patent/JP6257596B2/ja not_active Expired - Fee Related
- 2013-05-16 SG SG11201407210SA patent/SG11201407210SA/en unknown
- 2013-05-16 CA CA2871542A patent/CA2871542A1/en not_active Abandoned
- 2013-05-16 SI SI201330499A patent/SI2882715T1/sl unknown
- 2013-05-16 KR KR20147033843A patent/KR20150010973A/ko not_active Application Discontinuation
- 2013-05-16 PT PT137231510T patent/PT2882715T/pt unknown
- 2013-05-16 RU RU2014151360A patent/RU2645344C2/ru not_active IP Right Cessation
- 2013-05-16 AU AU2013261718A patent/AU2013261718B2/en not_active Ceased
- 2013-05-16 WO PCT/EP2013/060171 patent/WO2013171317A1/en active Application Filing
- 2013-05-16 HU HUE13723151A patent/HUE032890T2/hu unknown
- 2013-05-16 DK DK13723151.0T patent/DK2882715T3/en active
-
2014
- 2014-10-20 IL IL235221A patent/IL235221A/en active IP Right Grant
-
2017
- 2017-01-20 HR HRP20170098TT patent/HRP20170098T1/hr unknown
- 2017-02-08 CY CY20171100175T patent/CY1118618T1/el unknown
Also Published As
Publication number | Publication date |
---|---|
WO2013171317A1 (en) | 2013-11-21 |
SI2882715T1 (sl) | 2017-03-31 |
KR20150010973A (ko) | 2015-01-29 |
DK2882715T3 (en) | 2017-02-13 |
HRP20170098T1 (hr) | 2017-03-24 |
PL2882715T3 (pl) | 2017-04-28 |
PT2882715T (pt) | 2016-12-30 |
CN104302625B (zh) | 2017-04-19 |
JP6257596B2 (ja) | 2018-01-10 |
BR112014028406A2 (pt) | 2017-06-27 |
MX347615B (es) | 2017-05-04 |
LT2882715T (lt) | 2017-02-10 |
US20150141477A1 (en) | 2015-05-21 |
EP2882715A1 (en) | 2015-06-17 |
CN104302625A (zh) | 2015-01-21 |
AU2013261718B2 (en) | 2017-10-19 |
RU2645344C2 (ru) | 2018-02-21 |
CA2871542A1 (en) | 2013-11-21 |
ES2612205T3 (es) | 2017-05-12 |
JP2015517514A (ja) | 2015-06-22 |
HUE032890T2 (hu) | 2017-11-28 |
IL235221A (en) | 2016-06-30 |
SG11201407210SA (en) | 2014-12-30 |
US9346762B2 (en) | 2016-05-24 |
EP2882715B1 (en) | 2016-11-09 |
AU2013261718A1 (en) | 2014-12-18 |
RU2014151360A (ru) | 2016-07-10 |
CY1118618T1 (el) | 2017-07-12 |
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Legal Events
Date | Code | Title | Description |
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FG | Grant or registration |