JP2014505033A5 - - Google Patents
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- Publication number
- JP2014505033A5 JP2014505033A5 JP2013543341A JP2013543341A JP2014505033A5 JP 2014505033 A5 JP2014505033 A5 JP 2014505033A5 JP 2013543341 A JP2013543341 A JP 2013543341A JP 2013543341 A JP2013543341 A JP 2013543341A JP 2014505033 A5 JP2014505033 A5 JP 2014505033A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cycloalkyl
- haloalkyl
- compound according
- group
- 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
Links
- 125000000217 alkyl group Chemical group 0.000 claims 39
- 150000001875 compounds Chemical class 0.000 claims 38
- 125000000753 cycloalkyl group Chemical group 0.000 claims 30
- 125000001188 haloalkyl group Chemical group 0.000 claims 26
- 125000001424 substituent group Chemical group 0.000 claims 21
- 229910052736 halogen Inorganic materials 0.000 claims 20
- 125000003118 aryl group Chemical group 0.000 claims 17
- 229910052739 hydrogen Inorganic materials 0.000 claims 17
- 239000001257 hydrogen Substances 0.000 claims 17
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 15
- 125000003710 aryl alkyl group Chemical group 0.000 claims 14
- 125000004093 cyano group Chemical group *C#N 0.000 claims 14
- 150000002367 halogens Chemical class 0.000 claims 14
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 12
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 150000002431 hydrogen Chemical class 0.000 claims 10
- 125000001309 chloro group Chemical group Cl* 0.000 claims 9
- 125000001153 fluoro group Chemical group F* 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 230000000366 juvenile effect Effects 0.000 claims 7
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 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
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 6
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 6
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 208000019069 chronic childhood arthritis Diseases 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 4
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 4
- 150000003839 salts Chemical class 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
- 229910052799 carbon Inorganic materials 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
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 208000002574 reactive arthritis Diseases 0.000 claims 3
- 239000012453 solvate Substances 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
- 125000004429 atom Chemical group 0.000 claims 2
- -1 haloalkyl compound Chemical class 0.000 claims 2
- 125000005549 heteroarylene group Chemical group 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 230000009885 systemic effect Effects 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 1
- 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
- 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
- 125000003545 alkoxy group Chemical group 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
- 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
- 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
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US42095010P | 2010-12-08 | 2010-12-08 | |
| US61/420,950 | 2010-12-08 | ||
| PCT/US2011/063950 WO2012078874A1 (en) | 2010-12-08 | 2011-12-08 | Pyrazolyl guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016216608A Division JP2017061505A (ja) | 2010-12-08 | 2016-11-04 | ピラゾリルグアニジンｆ１ｆ０−ａｔｐアーゼ阻害剤およびその治療的使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014505033A JP2014505033A (ja) | 2014-02-27 |
| JP2014505033A5 true JP2014505033A5 (OSRAM) | 2015-01-29 |
| JP6096673B2 JP6096673B2 (ja) | 2017-03-15 |
Family
ID=46207516
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013543341A Expired - Fee Related JP6096673B2 (ja) | 2010-12-08 | 2011-12-08 | ピラゾリルグアニジンｆ１ｆ０−ａｔｐアーゼ阻害剤およびその治療的使用 |
| JP2016216608A Pending JP2017061505A (ja) | 2010-12-08 | 2016-11-04 | ピラゾリルグアニジンｆ１ｆ０−ａｔｐアーゼ阻害剤およびその治療的使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016216608A Pending JP2017061505A (ja) | 2010-12-08 | 2016-11-04 | ピラゾリルグアニジンｆ１ｆ０−ａｔｐアーゼ阻害剤およびその治療的使用 |
Country Status (20)
| Country | Link |
|---|---|
| US (4) | US9139532B2 (OSRAM) |
| EP (1) | EP2648511B1 (OSRAM) |
| JP (2) | JP6096673B2 (OSRAM) |
| CN (1) | CN103476252B (OSRAM) |
| AU (1) | AU2011338309B2 (OSRAM) |
| CA (1) | CA2820065C (OSRAM) |
| CY (1) | CY1119432T1 (OSRAM) |
| DK (1) | DK2648511T3 (OSRAM) |
| ES (1) | ES2639439T3 (OSRAM) |
| HR (1) | HRP20171280T1 (OSRAM) |
| HU (1) | HUE035881T2 (OSRAM) |
| IL (1) | IL226789A (OSRAM) |
| LT (1) | LT2648511T (OSRAM) |
| MX (1) | MX344590B (OSRAM) |
| PL (1) | PL2648511T3 (OSRAM) |
| PT (1) | PT2648511T (OSRAM) |
| RS (1) | RS56457B1 (OSRAM) |
| SI (1) | SI2648511T1 (OSRAM) |
| SM (1) | SMT201700445T1 (OSRAM) |
| WO (1) | WO2012078874A1 (OSRAM) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012078869A1 (en) | 2010-12-08 | 2012-06-14 | Lycera Corporation | Pyridonyl guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
| US9169199B2 (en) | 2010-12-08 | 2015-10-27 | Lycera Corporation | Cycloalkyl guanidine F1F0-ATPase inhibitors and therapeutic uses thereof |
| ES2639439T3 (es) | 2010-12-08 | 2017-10-26 | Lycera Corporation | Inhibidores de F1F0-ATPasas de tipo pirazolilguanidina y sus usos terapéuticos de éstos |
| EP2866893A4 (en) | 2012-06-08 | 2015-12-23 | Lycera Corp | HETEROCYCLIC GUANIDINE F1FO ATPASE INHIBITORS |
| WO2013185045A1 (en) | 2012-06-08 | 2013-12-12 | Lycera Corporation | Indazole 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 |
| AU2014363958B2 (en) * | 2013-12-10 | 2018-11-08 | Lycera Corporation | Alkylpyrazolyl guanidine F1F0-ATPase inhibitors and therapeutic uses thereof |
| CA2931792A1 (en) | 2013-12-10 | 2015-06-18 | Lycera Corporation | N-substituted pyrazolyl guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
| EP3080089B1 (en) | 2013-12-10 | 2019-05-08 | Lycera Corporation | Trifluoromethyl pyrazolyl guanidine f1fo-atpase inhibitors and therapeutic uses thereof |
| WO2017135399A1 (ja) * | 2016-02-04 | 2017-08-10 | 塩野義製薬株式会社 | ＴｒｋＡ阻害活性を有する含窒素複素環および炭素環誘導体 |
Family Cites Families (32)
| 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 |
| AU5852300A (en) | 1999-07-15 | 2001-02-05 | Sumitomo Pharmaceuticals Company, Limited | Heteroaromatic ring compounds |
| EP1296978A2 (en) | 2000-06-30 | 2003-04-02 | Bristol-Myers Squibb Company | N-ureidoheterocycloaklyl-piperidines as modulators of chemokine receptor activity |
| 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 |
| WO2003106628A2 (en) | 2002-06-17 | 2003-12-24 | Bristol-Myers Squibb Company | Benzodiazepine inhibitors of mitochondial f1f0 atp hydrolase and methods of inhibiting f1f0 atp hydrolase |
| WO2004043362A2 (en) | 2002-11-06 | 2004-05-27 | Bristol-Myers Squibb Company | Acyl guanidine compounds and use thereof |
| ATE440827T1 (de) | 2002-12-04 | 2009-09-15 | Ore Pharmaceuticals Inc | Melanocortin-rezeptormodulatoren |
| 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 |
| JP4990766B2 (ja) | 2004-07-01 | 2012-08-01 | シンタ ファーマシューティカルズ コーポレーション | 二置換型ヘテロアリール化合物 |
| CA2659549C (en) | 2006-06-09 | 2013-07-30 | The Regents Of The University Of Michigan | Compositions and methods relating to novel compounds and targets thereof |
| ES2614498T3 (es) * | 2007-09-14 | 2017-05-31 | The Regents Of The University Of Michigan | Inhibidores de ATPasa F1F0 y métodos relacionados |
| CA2709784A1 (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 |
| JP5567573B2 (ja) | 2008-09-11 | 2014-08-06 | ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン | アリールグアニジンｆ１ｆ０−ａｔｐアーゼ阻害剤およびそれと関連する方法 |
| US9169199B2 (en) | 2010-12-08 | 2015-10-27 | Lycera Corporation | Cycloalkyl guanidine F1F0-ATPase inhibitors and therapeutic uses thereof |
| ES2639439T3 (es) | 2010-12-08 | 2017-10-26 | Lycera Corporation | Inhibidores de F1F0-ATPasas de tipo pirazolilguanidina y sus usos terapéuticos de éstos |
| CA2820035A1 (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 |
| US9580391B2 (en) | 2012-06-08 | 2017-02-28 | Lycera Corporation | Saturated acyl guanidine for inhibition of F1F0-ATPase |
| WO2013185045A1 (en) | 2012-06-08 | 2013-12-12 | Lycera Corporation | Indazole guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
| EP2866893A4 (en) | 2012-06-08 | 2015-12-23 | Lycera Corp | HETEROCYCLIC GUANIDINE F1FO ATPASE INHIBITORS |
| EP3080089B1 (en) | 2013-12-10 | 2019-05-08 | Lycera Corporation | Trifluoromethyl pyrazolyl guanidine f1fo-atpase inhibitors and therapeutic uses thereof |
| CA2931792A1 (en) | 2013-12-10 | 2015-06-18 | Lycera Corporation | N-substituted pyrazolyl guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
| AU2014363958B2 (en) | 2013-12-10 | 2018-11-08 | Lycera Corporation | Alkylpyrazolyl guanidine F1F0-ATPase inhibitors and therapeutic uses thereof |
-
2011
- 2011-12-08 ES ES11846595.4T patent/ES2639439T3/es active Active
- 2011-12-08 HR HRP20171280TT patent/HRP20171280T1/hr unknown
- 2011-12-08 LT LTEP11846595.4T patent/LT2648511T/lt unknown
- 2011-12-08 HU HUE11846595A patent/HUE035881T2/en unknown
- 2011-12-08 WO PCT/US2011/063950 patent/WO2012078874A1/en not_active Ceased
- 2011-12-08 RS RS20170875A patent/RS56457B1/sr unknown
- 2011-12-08 MX MX2013006446A patent/MX344590B/es active IP Right Grant
- 2011-12-08 DK DK11846595.4T patent/DK2648511T3/en active
- 2011-12-08 PL PL11846595T patent/PL2648511T3/pl unknown
- 2011-12-08 SM SM20170445T patent/SMT201700445T1/it unknown
- 2011-12-08 PT PT118465954T patent/PT2648511T/pt unknown
- 2011-12-08 JP JP2013543341A patent/JP6096673B2/ja not_active Expired - Fee Related
- 2011-12-08 US US13/992,255 patent/US9139532B2/en not_active Expired - Fee Related
- 2011-12-08 CA CA2820065A patent/CA2820065C/en not_active Expired - Fee Related
- 2011-12-08 AU AU2011338309A patent/AU2011338309B2/en not_active Ceased
- 2011-12-08 EP EP11846595.4A patent/EP2648511B1/en active Active
- 2011-12-08 SI SI201131285T patent/SI2648511T1/sl unknown
- 2011-12-08 CN CN201180065940.3A patent/CN103476252B/zh not_active Expired - Fee Related
-
2013
- 2013-06-06 IL IL226789A patent/IL226789A/en active IP Right Grant
-
2015
- 2015-07-16 US US14/800,969 patent/US9580388B2/en not_active Expired - Fee Related
-
2016
- 2016-11-04 JP JP2016216608A patent/JP2017061505A/ja active Pending
-
2017
- 2017-02-01 US US15/421,729 patent/US9932313B2/en not_active Expired - Fee Related
- 2017-09-20 CY CY20171100992T patent/CY1119432T1/el unknown
-
2018
- 2018-03-14 US US15/920,690 patent/US20180334438A1/en not_active Abandoned
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