AU2014363958B2 - Alkylpyrazolyl guanidine F1F0-ATPase inhibitors and therapeutic uses thereof - Google Patents
Alkylpyrazolyl guanidine F1F0-ATPase inhibitors and therapeutic uses thereof Download PDFInfo
- Publication number
- AU2014363958B2 AU2014363958B2 AU2014363958A AU2014363958A AU2014363958B2 AU 2014363958 B2 AU2014363958 B2 AU 2014363958B2 AU 2014363958 A AU2014363958 A AU 2014363958A AU 2014363958 A AU2014363958 A AU 2014363958A AU 2014363958 B2 AU2014363958 B2 AU 2014363958B2
- Authority
- AU
- Australia
- Prior art keywords
- chloro
- compound
- fluorophenyl
- fluoro
- chlorophenyl
- 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.)
- Ceased
Links
- YTARZCOGKBEMSD-UHFFFAOYSA-N Cc1c(C(F)(F)F)[nH]nc1N Chemical compound Cc1c(C(F)(F)F)[nH]nc1N YTARZCOGKBEMSD-UHFFFAOYSA-N 0.000 description 1
- MNRAGHFEGSVXAM-UHFFFAOYSA-N Cc1c(C(F)(F)F)[nH]nc1NC(NC(c(cc1F)ccc1F)=O)=S Chemical compound Cc1c(C(F)(F)F)[nH]nc1NC(NC(c(cc1F)ccc1F)=O)=S MNRAGHFEGSVXAM-UHFFFAOYSA-N 0.000 description 1
- RPQWXGVZELKOEU-UHFFFAOYSA-N O=C(c(cc1)cc(F)c1F)Cl Chemical compound O=C(c(cc1)cc(F)c1F)Cl RPQWXGVZELKOEU-UHFFFAOYSA-N 0.000 description 1
Classifications
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- 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)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Immunology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pulmonology (AREA)
- Endocrinology (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Gastroenterology & Hepatology (AREA)
- Biomedical Technology (AREA)
- Emergency Medicine (AREA)
- Neurosurgery (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Vascular Medicine (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 |
|---|---|
| AU2014363958A1 AU2014363958A1 (en) | 2016-06-30 |
| AU2014363958B2 true AU2014363958B2 (en) | 2018-11-08 |
Family
ID=53371788
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2014363958A Ceased AU2014363958B2 (en) | 2013-12-10 | 2014-12-10 | Alkylpyrazolyl guanidine F1F0-ATPase inhibitors and therapeutic uses thereof |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US9815791B2 (https=) |
| EP (1) | EP3080088B1 (https=) |
| JP (1) | JP2016539983A (https=) |
| AU (1) | AU2014363958B2 (https=) |
| CA (1) | CA2931850A1 (https=) |
| WO (1) | WO2015089131A1 (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2648511T3 (en) | 2010-12-08 | 2017-09-18 | Lycera Corp | PYRAZOLYLGUANIDINE-F1F0 ATPASE INHIBITORS AND THERAPEUTIC APPLICATIONS THEREOF |
| MX2016007445A (es) * | 2013-12-10 | 2016-09-09 | Lycera Corp | Inhibidores de f1f0-atpasa de trifluorometil pirazolil guanidina y usos terapeuticos de los mismos. |
| WO2015089152A1 (en) * | 2013-12-10 | 2015-06-18 | Lycera Corporation | N-substituted pyrazolyl guanidine f1f0-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 (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012078874A1 (en) * | 2010-12-08 | 2012-06-14 | Lycera Corporation | Pyrazolyl guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
Family Cites Families (30)
| 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 |
| CA2360305A1 (en) | 1999-02-09 | 2000-08-17 | 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 |
| CN1202095C (zh) | 1999-07-15 | 2005-05-18 | 住友制药株式会社 | 杂芳环化合物 |
| JP2004517805A (ja) | 2000-06-30 | 2004-06-17 | ブリストル−マイヤーズ・スクイブ・ファーマ・カンパニー | ケモカイン受容体活性調節剤としてのn−ウレイドヘテロシクロアルキル−ピペリジン |
| US6916813B2 (en) | 2001-12-10 | 2005-07-12 | Bristol-Myers Squibb Co. | (1-phenyl-2-heteoaryl)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 |
| US7365070B2 (en) | 2002-12-04 | 2008-04-29 | Ore Pharmaceuticals 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 |
| WO2006007532A2 (en) | 2004-07-01 | 2006-01-19 | Synta Pharmaceuticals Corp. | 2-substituted heteroaryl compounds |
| EP2418206A3 (en) | 2006-06-09 | 2012-06-27 | The Regents of the University of Michigan | Benzodiazepine derivatives useful in the treatment of autoimmune disorders |
| MX2010002732A (es) | 2007-09-14 | 2010-06-02 | Univ Michigan | Inhibidores de f1f0-atpasa y metodos relacionados. |
| WO2009086303A2 (en) | 2007-12-21 | 2009-07-09 | 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 |
| US8497307B2 (en) | 2008-09-11 | 2013-07-30 | The Regents Of The University Of Michigan | Aryl guanidine F1F0-ATPase inhibitors and related methods |
| MX2013006398A (es) | 2010-12-08 | 2013-12-02 | Lycera Corp | Inhibidores de f1f0-atpasas de tipo piridonilguanidina y usos terapeúticos. |
| US9169199B2 (en) | 2010-12-08 | 2015-10-27 | Lycera Corporation | Cycloalkyl guanidine F1F0-ATPase inhibitors and therapeutic uses thereof |
| WO2012078867A2 (en) * | 2010-12-08 | 2012-06-14 | Lycera Corporation | Cycloalkyl guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
| US9580391B2 (en) | 2012-06-08 | 2017-02-28 | Lycera Corporation | Saturated acyl guanidine for inhibition of F1F0-ATPase |
| US9221814B2 (en) | 2012-06-08 | 2015-12-29 | Lycera Corporation | Heterocyclic guanidine F1F0-atpase inhibitors and therapeutic uses thereof |
| US9920012B2 (en) | 2012-06-08 | 2018-03-20 | Lycera Corporation | Indazole guanidine F1F0-ATPase inhibitors and therapeutic uses thereof |
| WO2015089152A1 (en) * | 2013-12-10 | 2015-06-18 | Lycera Corporation | N-substituted pyrazolyl guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
| MX2016007445A (es) | 2013-12-10 | 2016-09-09 | Lycera Corp | Inhibidores de f1f0-atpasa de trifluorometil pirazolil guanidina y usos terapeuticos de los mismos. |
-
2014
- 2014-12-10 EP EP14869679.2A patent/EP3080088B1/en not_active Not-in-force
- 2014-12-10 CA CA2931850A patent/CA2931850A1/en not_active Abandoned
- 2014-12-10 AU AU2014363958A patent/AU2014363958B2/en not_active Ceased
- 2014-12-10 WO PCT/US2014/069453 patent/WO2015089131A1/en not_active Ceased
- 2014-12-10 JP JP2016537963A patent/JP2016539983A/ja active Pending
- 2014-12-10 US US15/101,129 patent/US9815791B2/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012078874A1 (en) * | 2010-12-08 | 2012-06-14 | Lycera Corporation | Pyrazolyl guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CA2931850A1 (en) | 2015-06-18 |
| EP3080088B1 (en) | 2019-07-31 |
| EP3080088A4 (en) | 2017-05-10 |
| WO2015089131A1 (en) | 2015-06-18 |
| AU2014363958A1 (en) | 2016-06-30 |
| EP3080088A1 (en) | 2016-10-19 |
| US9815791B2 (en) | 2017-11-14 |
| JP2016539983A (ja) | 2016-12-22 |
| US20160304465A1 (en) | 2016-10-20 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FGA | Letters patent sealed or granted (standard patent) | ||
| MK14 | Patent ceased section 143(a) (annual fees not paid) or expired |