JP2016539983A - アルキルピラゾリルグアニジンf1f0−atpアーゼ阻害剤及びその治療用途 - Google Patents
アルキルピラゾリルグアニジンf1f0−atpアーゼ阻害剤及びその治療用途 Download PDFInfo
- Publication number
- JP2016539983A JP2016539983A JP2016537963A JP2016537963A JP2016539983A JP 2016539983 A JP2016539983 A JP 2016539983A JP 2016537963 A JP2016537963 A JP 2016537963A JP 2016537963 A JP2016537963 A JP 2016537963A JP 2016539983 A JP2016539983 A JP 2016539983A
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- Prior art keywords
- compound according
- chloro
- disease
- fluoro
- compound
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- 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.)
- Pending
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- 0 C*C=C(C=C)C(N=C(NC)NC1N(*)N=*C1*)=O Chemical compound C*C=C(C=C)C(N=C(NC)NC1N(*)N=*C1*)=O 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
- C07D231/14—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/38—Nitrogen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
-
- 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
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- 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
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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
- A61P37/02—Immunomodulators
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
- A61P5/40—Mineralocorticosteroids, e.g. aldosterone; Drugs increasing or potentiating the activity of mineralocorticosteroids
-
- 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
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hematology (AREA)
- Neurology (AREA)
- Endocrinology (AREA)
- Dermatology (AREA)
- Biomedical Technology (AREA)
- Oncology (AREA)
- Gastroenterology & Hepatology (AREA)
- Vascular Medicine (AREA)
- Communicable Diseases (AREA)
- Neurosurgery (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361914088P | 2013-12-10 | 2013-12-10 | |
| US61/914,088 | 2013-12-10 | ||
| PCT/US2014/069453 WO2015089131A1 (en) | 2013-12-10 | 2014-12-10 | Alkylpyrazolyl guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016539983A true JP2016539983A (ja) | 2016-12-22 |
| JP2016539983A5 JP2016539983A5 (enExample) | 2018-01-25 |
Family
ID=53371788
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016537963A Pending JP2016539983A (ja) | 2013-12-10 | 2014-12-10 | アルキルピラゾリルグアニジンf1f0−atpアーゼ阻害剤及びその治療用途 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US9815791B2 (enExample) |
| EP (1) | EP3080088B1 (enExample) |
| JP (1) | JP2016539983A (enExample) |
| AU (1) | AU2014363958B2 (enExample) |
| CA (1) | CA2931850A1 (enExample) |
| WO (1) | WO2015089131A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2016539993A (ja) * | 2013-12-10 | 2016-12-22 | リセラ・コーポレイションLycera Corporation | N−置換ピラゾリルグアニジンf1f0−atpアーゼ阻害剤及びその治療用途 |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2639439T3 (es) | 2010-12-08 | 2017-10-26 | Lycera Corporation | Inhibidores de F1F0-ATPasas de tipo pirazolilguanidina y sus usos terapéuticos de éstos |
| WO2015089149A1 (en) | 2013-12-10 | 2015-06-18 | Lycera Corporation | Trifluoromethyl pyrazolyl guanidine f1fo-atpase inhibitors and therapeutic uses thereof |
| CN116570589B (zh) * | 2023-05-30 | 2025-02-11 | 南阳理工学院 | 化合物Parimifasor在制备抗肿瘤药物中的应用 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012078867A2 (en) * | 2010-12-08 | 2012-06-14 | Lycera Corporation | Cycloalkyl guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
| WO2012078869A1 (en) * | 2010-12-08 | 2012-06-14 | Lycera Corporation | Pyridonyl guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
| WO2012078874A1 (en) * | 2010-12-08 | 2012-06-14 | Lycera Corporation | Pyrazolyl guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
| JP2016539993A (ja) * | 2013-12-10 | 2016-12-22 | リセラ・コーポレイションLycera Corporation | N−置換ピラゾリルグアニジンf1f0−atpアーゼ阻害剤及びその治療用途 |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4977189A (en) | 1986-05-07 | 1990-12-11 | American Cyanamid Company | Substituted guanidinedicarbonyl derivatives |
| JPH07188197A (ja) | 1993-11-17 | 1995-07-25 | Fujisawa Pharmaceut Co Ltd | オキサゾール誘導体 |
| DE4344550A1 (de) | 1993-12-24 | 1995-06-29 | Hoechst Ag | Substituierte 1-Oxo-1,2-dihydro-isochinolinoyl- und 1,1-Dioxo-2H-1,2-benzothiazinoylguanidine, Verfahrenzu ihrer Herstellung, ihre Verwendung als Medikamentt oder Diagnostikum sowie sie enthaltendes Medikamen |
| US7041702B1 (en) | 1997-10-21 | 2006-05-09 | Scion Pharmaceuticals, Inc. | Pharmaceutically active compounds and methods of use |
| AU760174B2 (en) | 1999-02-09 | 2003-05-08 | Bristol-Myers Squibb Company | Lactam inhibitors of FXa and method |
| US7276348B2 (en) | 1999-04-30 | 2007-10-02 | Regents Of The University Of Michigan | Compositions and methods relating to F1F0-ATPase inhibitors and targets thereof |
| CA2377527A1 (en) | 1999-07-15 | 2001-01-25 | Sumitomo Pharmaceuticals Co., Ltd. | Heteroaromatic ring compounds |
| AR034257A1 (es) | 2000-06-30 | 2004-02-18 | Du Pont Pharm Co | Compuesto ureido, composicion farmaceutica que lo comprende y metodo para modular la actividad del receptor de quimiocinas |
| WO2003050261A2 (en) | 2001-12-10 | 2003-06-19 | Bristol-Myers Squibb Company | (1-phenyl-2-heteroaryl)ethyl-guanidine compounds as inhibitors of mitochondrial f1f0 atp hydrolase |
| GB0208224D0 (en) | 2002-04-10 | 2002-05-22 | Celltech R&D Ltd | Chemical compounds |
| US20040009972A1 (en) | 2002-06-17 | 2004-01-15 | Ding Charles Z. | Benzodiazepine inhibitors of mitochondial F1F0 ATP hydrolase and methods of inhibiting F1F0 ATP hydrolase |
| AU2003295402A1 (en) | 2002-11-06 | 2004-06-03 | Bristol-Myers Squibb Company | Acyl guanidine compounds and use thereof |
| WO2004050610A2 (en) | 2002-12-04 | 2004-06-17 | Gene Logic Inc. | Modulators of melanocortin receptor |
| DE102004008141A1 (de) | 2004-02-19 | 2005-09-01 | Abbott Gmbh & Co. Kg | Guanidinverbindungen und ihre Verwendung als Bindungspartner für 5-HT5-Rezeptoren |
| US20090275099A1 (en) | 2004-04-27 | 2009-11-05 | Regents Of The University Of Michigan | Methods and compositions for treating diseases and conditions associated with mitochondrial function |
| US20050272723A1 (en) | 2004-04-27 | 2005-12-08 | The Regents Of The University Of Michigan | Methods and compositions for treating diseases and conditions associated with mitochondrial function |
| TW200612948A (en) | 2004-07-01 | 2006-05-01 | Synta Pharmaceuticals Corp | 2-substituted heteroaryl compounds |
| JP5264716B2 (ja) | 2006-06-09 | 2013-08-14 | ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン | 化合物およびその標的に関連する組成物および方法 |
| ES2614498T3 (es) | 2007-09-14 | 2017-05-31 | The Regents Of The University Of Michigan | Inhibidores de ATPasa F1F0 y métodos relacionados |
| US8642660B2 (en) | 2007-12-21 | 2014-02-04 | The University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| KR100982661B1 (ko) | 2008-04-22 | 2010-09-17 | 전남대학교산학협력단 | 플라스멥신 ⅱ 활성을 저해하는 화합물을 유효성분으로함유하는 말라리아 예방 및 치료를 위한 약학 조성물 및이를 이용한 말라리아 치료방법 |
| WO2010030891A2 (en) | 2008-09-11 | 2010-03-18 | The Regents Of The University Of Michigan | Aryl guanidine f1f0-atpase inhibitors and related methods |
| US9169199B2 (en) | 2010-12-08 | 2015-10-27 | Lycera Corporation | Cycloalkyl guanidine F1F0-ATPase inhibitors and therapeutic uses thereof |
| EP2861225A4 (en) | 2012-06-08 | 2015-11-18 | Lycera Corp | Saturated acylguanidine for the inhibition of F1F0-ATPASE |
| US9920012B2 (en) | 2012-06-08 | 2018-03-20 | Lycera Corporation | Indazole guanidine F1F0-ATPase inhibitors and therapeutic uses thereof |
| US9221814B2 (en) | 2012-06-08 | 2015-12-29 | Lycera Corporation | Heterocyclic guanidine F1F0-atpase inhibitors and therapeutic uses thereof |
| WO2015089149A1 (en) | 2013-12-10 | 2015-06-18 | Lycera Corporation | Trifluoromethyl pyrazolyl guanidine f1fo-atpase inhibitors and therapeutic uses thereof |
-
2014
- 2014-12-10 JP JP2016537963A patent/JP2016539983A/ja active Pending
- 2014-12-10 AU AU2014363958A patent/AU2014363958B2/en not_active Ceased
- 2014-12-10 US US15/101,129 patent/US9815791B2/en not_active Expired - Fee Related
- 2014-12-10 CA CA2931850A patent/CA2931850A1/en not_active Abandoned
- 2014-12-10 WO PCT/US2014/069453 patent/WO2015089131A1/en not_active Ceased
- 2014-12-10 EP EP14869679.2A patent/EP3080088B1/en not_active Not-in-force
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012078867A2 (en) * | 2010-12-08 | 2012-06-14 | Lycera Corporation | Cycloalkyl guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
| WO2012078869A1 (en) * | 2010-12-08 | 2012-06-14 | Lycera Corporation | Pyridonyl guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
| WO2012078874A1 (en) * | 2010-12-08 | 2012-06-14 | Lycera Corporation | Pyrazolyl guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
| JP2016539993A (ja) * | 2013-12-10 | 2016-12-22 | リセラ・コーポレイションLycera Corporation | N−置換ピラゾリルグアニジンf1f0−atpアーゼ阻害剤及びその治療用途 |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2016539993A (ja) * | 2013-12-10 | 2016-12-22 | リセラ・コーポレイションLycera Corporation | N−置換ピラゾリルグアニジンf1f0−atpアーゼ阻害剤及びその治療用途 |
Also Published As
| Publication number | Publication date |
|---|---|
| US9815791B2 (en) | 2017-11-14 |
| EP3080088A4 (en) | 2017-05-10 |
| CA2931850A1 (en) | 2015-06-18 |
| AU2014363958A1 (en) | 2016-06-30 |
| US20160304465A1 (en) | 2016-10-20 |
| EP3080088A1 (en) | 2016-10-19 |
| AU2014363958B2 (en) | 2018-11-08 |
| WO2015089131A1 (en) | 2015-06-18 |
| EP3080088B1 (en) | 2019-07-31 |
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