JP2014505032A5 - - Google Patents
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- Publication number
- JP2014505032A5 JP2014505032A5 JP2013543340A JP2013543340A JP2014505032A5 JP 2014505032 A5 JP2014505032 A5 JP 2014505032A5 JP 2013543340 A JP2013543340 A JP 2013543340A JP 2013543340 A JP2013543340 A JP 2013543340A JP 2014505032 A5 JP2014505032 A5 JP 2014505032A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cycloalkyl
- haloalkyl
- juvenile
- compound according
- 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.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims 24
- 125000000217 alkyl group Chemical group 0.000 claims 19
- 125000001188 haloalkyl group Chemical group 0.000 claims 14
- 125000000753 cycloalkyl group Chemical group 0.000 claims 13
- 229910052736 halogen Inorganic materials 0.000 claims 12
- 125000001424 substituent group Chemical group 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 125000003710 aryl alkyl group Chemical group 0.000 claims 7
- 125000003118 aryl group Chemical group 0.000 claims 7
- 125000001309 chloro group Chemical group Cl* 0.000 claims 7
- 125000001153 fluoro group Chemical group F* 0.000 claims 7
- 230000000366 juvenile effect Effects 0.000 claims 7
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 6
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 6
- 125000005843 halogen group Chemical group 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 5
- 208000019069 chronic childhood arthritis Diseases 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 4
- 206010003246 arthritis Diseases 0.000 claims 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- 201000001981 dermatomyositis Diseases 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 208000002574 reactive arthritis Diseases 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 208000011580 syndromic disease Diseases 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- 206010003267 Arthritis reactive Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 206010047115 Vasculitis Diseases 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 230000009885 systemic effect Effects 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- 208000026872 Addison Disease Diseases 0.000 claims 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- 206010003253 Arthritis enteropathic Diseases 0.000 claims 1
- 208000036487 Arthropathies Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010003827 Autoimmune hepatitis Diseases 0.000 claims 1
- 208000035143 Bacterial infection Diseases 0.000 claims 1
- 208000023328 Basedow disease Diseases 0.000 claims 1
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 1
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 1
- -1 C 1 -C 6 alkoxy Chemical group 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010008609 Cholangitis sclerosing Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000015943 Coeliac disease Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010048768 Dermatosis Diseases 0.000 claims 1
- 206010018691 Granuloma Diseases 0.000 claims 1
- 208000015023 Graves' disease Diseases 0.000 claims 1
- 208000035895 Guillain-Barré syndrome Diseases 0.000 claims 1
- 206010021245 Idiopathic thrombocytopenic purpura Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000012659 Joint disease Diseases 0.000 claims 1
- 208000012528 Juvenile dermatomyositis Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010049567 Miller Fisher syndrome Diseases 0.000 claims 1
- 201000002481 Myositis Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000003076 Osteolysis Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000007048 Polymyalgia Rheumatica Diseases 0.000 claims 1
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 208000020410 Psoriasis-related juvenile idiopathic arthritis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 206010037549 Purpura Diseases 0.000 claims 1
- 241001672981 Purpura Species 0.000 claims 1
- 208000012322 Raynaud phenomenon Diseases 0.000 claims 1
- 208000033464 Reiter syndrome Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 208000034189 Sclerosis Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 208000024340 acute graft versus host disease Diseases 0.000 claims 1
- 229910052783 alkali metal Inorganic materials 0.000 claims 1
- 150000001340 alkali metals Chemical class 0.000 claims 1
- 206010003230 arteritis Diseases 0.000 claims 1
- 230000002917 arthritic effect Effects 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 201000003710 autoimmune thrombocytopenic purpura Diseases 0.000 claims 1
- 208000022362 bacterial infectious disease Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 210000000845 cartilage Anatomy 0.000 claims 1
- 201000010415 childhood type dermatomyositis Diseases 0.000 claims 1
- 208000017760 chronic graft versus host disease Diseases 0.000 claims 1
- 208000025302 chronic primary adrenal insufficiency Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000036566 epidermal hyperplasia Effects 0.000 claims 1
- 125000005549 heteroarylene group Chemical group 0.000 claims 1
- 208000026278 immune system disease Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 208000029791 lytic metastatic bone lesion Diseases 0.000 claims 1
- 230000002438 mitochondrial effect Effects 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 201000006292 polyarteritis nodosa Diseases 0.000 claims 1
- 208000005987 polymyositis Diseases 0.000 claims 1
- 201000000306 sarcoidosis Diseases 0.000 claims 1
- 208000010157 sclerosing cholangitis Diseases 0.000 claims 1
- 208000017520 skin disease Diseases 0.000 claims 1
- 210000002435 tendon Anatomy 0.000 claims 1
- MTIYYDLOEXFNAD-BQGCWICQSA-N CCC(C)C(CC)/C=C\C=C(/N)\O Chemical compound CCC(C)C(CC)/C=C\C=C(/N)\O MTIYYDLOEXFNAD-BQGCWICQSA-N 0.000 description 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N c1ccncc1 Chemical compound c1ccncc1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US42093410P | 2010-12-08 | 2010-12-08 | |
| US61/420,934 | 2010-12-08 | ||
| PCT/US2011/063945 WO2012078869A1 (en) | 2010-12-08 | 2011-12-08 | Pyridonyl guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014505032A JP2014505032A (ja) | 2014-02-27 |
| JP2014505032A5 true JP2014505032A5 (2) | 2015-01-29 |
| JP6050242B2 JP6050242B2 (ja) | 2016-12-21 |
Family
ID=46207514
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013543340A Expired - Fee Related JP6050242B2 (ja) | 2010-12-08 | 2011-12-08 | ピリドニルグアニジンｆ１ｆ０−ａｔｐアーゼ阻害剤およびその治療的使用 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US9000014B2 (2) |
| EP (1) | EP2648710B1 (2) |
| JP (1) | JP6050242B2 (2) |
| CN (1) | CN103458886B (2) |
| AU (1) | AU2011338304B2 (2) |
| CA (1) | CA2820044A1 (2) |
| ES (1) | ES2591156T3 (2) |
| IL (1) | IL226790A (2) |
| MX (1) | MX2013006398A (2) |
| WO (1) | WO2012078869A1 (2) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| DK2648511T3 (en) | 2010-12-08 | 2017-09-18 | Lycera Corp | PYRAZOLYLGUANIDINE-F1F0 ATPASE INHIBITORS AND THERAPEUTIC APPLICATIONS THEREOF |
| US9221814B2 (en) | 2012-06-08 | 2015-12-29 | Lycera Corporation | Heterocyclic 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 |
| US9920012B2 (en) | 2012-06-08 | 2018-03-20 | Lycera Corporation | Indazole guanidine F1F0-ATPase inhibitors and therapeutic uses thereof |
| EP3080088B1 (en) * | 2013-12-10 | 2019-07-31 | Lycera Corporation | Alkylpyrazolyl 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. |
| WO2015089152A1 (en) * | 2013-12-10 | 2015-06-18 | Lycera Corporation | N-substituted pyrazolyl guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
| US9553382B2 (en) * | 2014-06-27 | 2017-01-24 | Xiaomi Inc. | Headphone socket assembly and electronic equipment including same |
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 |
| DK2648511T3 (en) | 2010-12-08 | 2017-09-18 | Lycera Corp | PYRAZOLYLGUANIDINE-F1F0 ATPASE INHIBITORS AND THERAPEUTIC APPLICATIONS 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 |
| MX2016007445A (es) | 2013-12-10 | 2016-09-09 | Lycera Corp | Inhibidores de f1f0-atpasa de trifluorometil pirazolil guanidina y usos terapeuticos de los mismos. |
-
2011
- 2011-12-08 MX MX2013006398A patent/MX2013006398A/es unknown
- 2011-12-08 AU AU2011338304A patent/AU2011338304B2/en not_active Ceased
- 2011-12-08 US US13/992,254 patent/US9000014B2/en not_active Expired - Fee Related
- 2011-12-08 JP JP2013543340A patent/JP6050242B2/ja not_active Expired - Fee Related
- 2011-12-08 CN CN201180065932.9A patent/CN103458886B/zh not_active Expired - Fee Related
- 2011-12-08 ES ES11846398.3T patent/ES2591156T3/es active Active
- 2011-12-08 EP EP11846398.3A patent/EP2648710B1/en not_active Not-in-force
- 2011-12-08 WO PCT/US2011/063945 patent/WO2012078869A1/en not_active Ceased
- 2011-12-08 CA CA2820044A patent/CA2820044A1/en not_active Abandoned
-
2013
- 2013-06-06 IL IL226790A patent/IL226790A/en active IP Right Grant
-
2015
- 2015-04-01 US US14/675,832 patent/US9370507B2/en not_active Expired - Fee Related
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