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
- 239000005557 antagonist Substances 0.000 title abstract 2
- 150000003217 pyrazoles Chemical class 0.000 title 1
- 101001038037 Homo sapiens Lysophosphatidic acid receptor 5 Proteins 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 5
- 210000003630 histaminocyte Anatomy 0.000 abstract 2
- 210000000274 microglia Anatomy 0.000 abstract 2
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 102100040404 Lysophosphatidic acid receptor 5 Human genes 0.000 abstract 1
- 208000001435 Thromboembolism Diseases 0.000 abstract 1
- 230000004913 activation Effects 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 210000001772 blood platelet Anatomy 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
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)
- 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)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Vascular Medicine (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 (6)
| 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 |
| CA2988983A1 (en) * | 2015-06-12 | 2016-12-15 | Vettore, LLC | Mct4 inhibitors for treating disease |
| JP7123929B2 (ja) | 2016-12-12 | 2022-08-23 | ベットーレ リミテッド ライアビリティー カンパニー | Ｍｃｔ４の複素環阻害剤 |
| 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 |
| 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 |
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 |
| EP1537074B1 (en) | 2002-09-04 | 2019-02-27 | Merck Canada Inc. | 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 |
| WO2009080227A2 (en) | 2007-12-26 | 2009-07-02 | Sanofi-Aventis | Pyrazole-carboxamide derivatives as p2y12 antagonists |
| 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 |
| HUE027098T2 (en) | 2008-03-07 | 2016-08-29 | Acraf | 1-Benzyl-3-hydroxymethylindazole derivatives and their use in the treatment of MCP-1, CX3CR1 expression-based diseases |
| 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 |
| DK2462118T3 (da) * | 2009-08-03 | 2014-08-25 | Acraf | Fremgangsmåde til fremstilling af 1-benzyl-3-hydroxymethyl-1H-indazol og dets derivater og nødvendige magnesiummellemprodukter |
| US8859775B2 (en) | 2010-09-02 | 2014-10-14 | Merck Patent Gmbh | Pyrazolopyridinone derivatives as LPA receptor antagonists |
| WO2013171316A1 (en) | 2012-05-18 | 2013-11-21 | Sanofi | Pyridine derivatives and their use in the treatment of conditions associated with pathological thrombus formation |
-
2013
- 2013-05-16 EP EP13723151.0A patent/EP2882715B1/en not_active Not-in-force
- 2013-05-16 MX MX2014014011A patent/MX347615B/es active IP Right Grant
- 2013-05-16 PT PT137231510T patent/PT2882715T/pt unknown
- 2013-05-16 JP JP2015512072A patent/JP6257596B2/ja not_active Expired - Fee Related
- 2013-05-16 RU RU2014151360A patent/RU2645344C2/ru not_active IP Right Cessation
- 2013-05-16 SI SI201330499A patent/SI2882715T1/sl unknown
- 2013-05-16 CN CN201380025967.9A patent/CN104302625B/zh not_active Expired - Fee Related
- 2013-05-16 WO PCT/EP2013/060171 patent/WO2013171317A1/en not_active Ceased
- 2013-05-16 AU AU2013261718A patent/AU2013261718B2/en not_active Ceased
- 2013-05-16 SG SG11201407210SA patent/SG11201407210SA/en unknown
- 2013-05-16 HU HUE13723151A patent/HUE032890T2/hu unknown
- 2013-05-16 PL PL13723151T patent/PL2882715T3/pl unknown
- 2013-05-16 DK DK13723151.0T patent/DK2882715T3/en active
- 2013-05-16 CA CA2871542A patent/CA2871542A1/en not_active Abandoned
- 2013-05-16 BR BR112014028406A patent/BR112014028406A2/pt not_active Application Discontinuation
- 2013-05-16 HR HRP20170098TT patent/HRP20170098T1/hr unknown
- 2013-05-16 KR KR20147033843A patent/KR20150010973A/ko not_active Ceased
- 2013-05-16 ES ES13723151.0T patent/ES2612205T3/es active Active
- 2013-05-16 LT LTEP13723151.0T patent/LT2882715T/lt unknown
- 2013-05-16 US US14/401,050 patent/US9346762B2/en not_active Expired - Fee Related
-
2014
- 2014-10-20 IL IL235221A patent/IL235221A/en active IP Right Grant
-
2017
- 2017-02-08 CY CY20171100175T patent/CY1118618T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2013261718A1 (en) | 2014-12-18 |
| EP2882715A1 (en) | 2015-06-17 |
| CN104302625B (zh) | 2017-04-19 |
| CA2871542A1 (en) | 2013-11-21 |
| HRP20170098T1 (hr) | 2017-03-24 |
| MX347615B (es) | 2017-05-04 |
| SI2882715T1 (sl) | 2017-03-31 |
| RU2014151360A (ru) | 2016-07-10 |
| HUE032890T2 (hu) | 2017-11-28 |
| IL235221A (en) | 2016-06-30 |
| US9346762B2 (en) | 2016-05-24 |
| RU2645344C2 (ru) | 2018-02-21 |
| JP6257596B2 (ja) | 2018-01-10 |
| SG11201407210SA (en) | 2014-12-30 |
| DK2882715T3 (en) | 2017-02-13 |
| CY1118618T1 (el) | 2017-07-12 |
| BR112014028406A2 (pt) | 2017-06-27 |
| AU2013261718B2 (en) | 2017-10-19 |
| PT2882715T (pt) | 2016-12-30 |
| PL2882715T3 (pl) | 2017-04-28 |
| CN104302625A (zh) | 2015-01-21 |
| EP2882715B1 (en) | 2016-11-09 |
| ES2612205T3 (es) | 2017-05-12 |
| KR20150010973A (ko) | 2015-01-29 |
| JP2015517514A (ja) | 2015-06-22 |
| WO2013171317A1 (en) | 2013-11-21 |
| LT2882715T (lt) | 2017-02-10 |
| US20150141477A1 (en) | 2015-05-21 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration |