JP6257596B2 - ピラゾール誘導体およびｌｐａｒ５アンタゴニストとしてのその使用 - Google Patents
ピラゾール誘導体およびｌｐａｒ５アンタゴニストとしてのその使用 Download PDFInfo
- Publication number
- JP6257596B2 JP6257596B2 JP2015512072A JP2015512072A JP6257596B2 JP 6257596 B2 JP6257596 B2 JP 6257596B2 JP 2015512072 A JP2015512072 A JP 2015512072A JP 2015512072 A JP2015512072 A JP 2015512072A JP 6257596 B2 JP6257596 B2 JP 6257596B2
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- series consisting
- cycloalkyl
- unsubstituted
- phenyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
- 0 CC(CC(C(O*)=O)=NOC)=O Chemical compound CC(CC(C(O*)=O)=NOC)=O 0.000 description 2
- ALCUPGQAVZDLII-UHFFFAOYSA-N CC(C(Nc(cc1)ccc1C(O)=O)=O)OCc(c(C)c1-c2ccc(C(F)(F)F)cc2)n[n]1-c(cc1)ccc1Cl Chemical compound CC(C(Nc(cc1)ccc1C(O)=O)=O)OCc(c(C)c1-c2ccc(C(F)(F)F)cc2)n[n]1-c(cc1)ccc1Cl ALCUPGQAVZDLII-UHFFFAOYSA-N 0.000 description 1
- DYFZSMCIWRJDNT-UHFFFAOYSA-N CC(C(Nc(cc1)ccc1C(O)=O)=O)OCc1c[n](-c2ccccc2)nc1-c1cc(cccc2)c2cc1 Chemical compound CC(C(Nc(cc1)ccc1C(O)=O)=O)OCc1c[n](-c2ccccc2)nc1-c1cc(cccc2)c2cc1 DYFZSMCIWRJDNT-UHFFFAOYSA-N 0.000 description 1
- IIUYCDJVRPBYSE-UHFFFAOYSA-N CC(C)C(C(Nc(cc1)ccc1C(O)=O)=O)OCc(c(C)c1-c2ccc(C)cc2)n[n]1-c(c(Cl)c1)ccc1Cl Chemical compound CC(C)C(C(Nc(cc1)ccc1C(O)=O)=O)OCc(c(C)c1-c2ccc(C)cc2)n[n]1-c(c(Cl)c1)ccc1Cl IIUYCDJVRPBYSE-UHFFFAOYSA-N 0.000 description 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)
- 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)
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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2015517514A JP2015517514A (ja) | 2015-06-22 |
| JP2015517514A5 JP2015517514A5 (enExample) | 2016-06-23 |
| JP6257596B2 true JP6257596B2 (ja) | 2018-01-10 |
Family
ID=48446368
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015512072A Expired - Fee Related JP6257596B2 (ja) | 2012-05-18 | 2013-05-16 | ピラゾール誘導体およびｌｐａｒ５アンタゴニストとしてのその使用 |
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)
| 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 |
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 |
| 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 |
-
2013
- 2013-05-16 DK DK13723151.0T patent/DK2882715T3/en active
- 2013-05-16 HU HUE13723151A patent/HUE032890T2/hu unknown
- 2013-05-16 HR HRP20170098TT patent/HRP20170098T1/hr unknown
- 2013-05-16 AU AU2013261718A patent/AU2013261718B2/en not_active Ceased
- 2013-05-16 MX MX2014014011A patent/MX347615B/es active IP Right Grant
- 2013-05-16 PT PT137231510T patent/PT2882715T/pt unknown
- 2013-05-16 ES ES13723151.0T patent/ES2612205T3/es active Active
- 2013-05-16 BR BR112014028406A patent/BR112014028406A2/pt not_active Application Discontinuation
- 2013-05-16 KR KR20147033843A patent/KR20150010973A/ko not_active Ceased
- 2013-05-16 EP EP13723151.0A patent/EP2882715B1/en not_active Not-in-force
- 2013-05-16 SI SI201330499A patent/SI2882715T1/sl unknown
- 2013-05-16 SG SG11201407210SA patent/SG11201407210SA/en unknown
- 2013-05-16 PL PL13723151T patent/PL2882715T3/pl unknown
- 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
- 2013-05-16 CA CA2871542A patent/CA2871542A1/en not_active Abandoned
- 2013-05-16 WO PCT/EP2013/060171 patent/WO2013171317A1/en not_active Ceased
- 2013-05-16 RU RU2014151360A patent/RU2645344C2/ru not_active IP Right Cessation
- 2013-05-16 JP JP2015512072A patent/JP6257596B2/ja not_active Expired - Fee Related
- 2013-05-16 CN CN201380025967.9A patent/CN104302625B/zh 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 |
|---|---|
| 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 |
| AU2013261718B2 (en) | 2017-10-19 |
| 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 |
| 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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