JP2011509238A5 - - Google Patents
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- JP2011509238A5 JP2011509238A5 JP2010524985A JP2010524985A JP2011509238A5 JP 2011509238 A5 JP2011509238 A5 JP 2011509238A5 JP 2010524985 A JP2010524985 A JP 2010524985A JP 2010524985 A JP2010524985 A JP 2010524985A JP 2011509238 A5 JP2011509238 A5 JP 2011509238A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- alkyl
- aryl
- heteroaryl
- hydrogen
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 63
- 125000001072 heteroaryl group Chemical group 0.000 claims description 47
- 125000003118 aryl group Chemical group 0.000 claims description 46
- 125000000217 alkyl group Chemical group 0.000 claims description 45
- 229910052739 hydrogen Inorganic materials 0.000 claims description 42
- 239000001257 hydrogen Substances 0.000 claims description 42
- 238000000034 method Methods 0.000 claims description 42
- 150000002431 hydrogen Chemical class 0.000 claims description 33
- 229910052736 halogen Inorganic materials 0.000 claims description 25
- 150000002367 halogens Chemical class 0.000 claims description 25
- 125000001188 haloalkyl group Chemical group 0.000 claims description 22
- 239000000203 mixture Substances 0.000 claims description 19
- -1 imidazolidonyl Chemical group 0.000 claims description 13
- 239000008194 pharmaceutical composition Substances 0.000 claims description 12
- 125000003545 alkoxy group Chemical group 0.000 claims description 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 9
- 150000002148 esters Chemical class 0.000 claims description 9
- 229940002612 prodrug Drugs 0.000 claims description 9
- 239000000651 prodrug Substances 0.000 claims description 9
- 150000003839 salts Chemical class 0.000 claims description 9
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 8
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 7
- 229910052757 nitrogen Inorganic materials 0.000 claims description 7
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 7
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 6
- 230000004064 dysfunction Effects 0.000 claims description 6
- 125000004475 heteroaralkyl group Chemical group 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims description 4
- 208000035143 Bacterial infection Diseases 0.000 claims description 3
- 208000022362 bacterial infectious disease Diseases 0.000 claims description 3
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 2
- 208000009329 Graft vs Host Disease Diseases 0.000 claims description 2
- 206010025323 Lymphomas Diseases 0.000 claims description 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 2
- 201000004681 Psoriasis Diseases 0.000 claims description 2
- 201000011529 cardiovascular cancer Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 208000024908 graft versus host disease Diseases 0.000 claims description 2
- 125000000623 heterocyclic group Chemical group 0.000 claims description 2
- 206010025135 lupus erythematosus Diseases 0.000 claims description 2
- 201000000050 myeloid neoplasm Diseases 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 230000002438 mitochondrial effect Effects 0.000 description 25
- 239000000362 adenosine triphosphatase inhibitor Substances 0.000 description 16
- 229940121819 ATPase inhibitor Drugs 0.000 description 15
- 230000000694 effects Effects 0.000 description 8
- CHJJGSNFBQVOTG-UHFFFAOYSA-N N-methyl-guanidine Natural products CNC(N)=N CHJJGSNFBQVOTG-UHFFFAOYSA-N 0.000 description 5
- ZRALSGWEFCBTJO-UHFFFAOYSA-N anhydrous guanidine Natural products NC(N)=N ZRALSGWEFCBTJO-UHFFFAOYSA-N 0.000 description 5
- SWSQBOPZIKWTGO-UHFFFAOYSA-N dimethylaminoamidine Natural products CN(C)C(N)=N SWSQBOPZIKWTGO-UHFFFAOYSA-N 0.000 description 5
- 230000001225 therapeutic effect Effects 0.000 description 5
- 0 CC*(*(*(CC)I)=*)N Chemical compound CC*(*(*(CC)I)=*)N 0.000 description 4
- 208000024891 symptom Diseases 0.000 description 3
- 102100021870 ATP synthase subunit O, mitochondrial Human genes 0.000 description 2
- YXFVVABEGXRONW-UHFFFAOYSA-N Cc1ccccc1 Chemical compound Cc1ccccc1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 2
- OUUQCZGPVNCOIJ-UHFFFAOYSA-M Superoxide Chemical compound [O-][O] OUUQCZGPVNCOIJ-UHFFFAOYSA-M 0.000 description 2
- 230000006907 apoptotic process Effects 0.000 description 2
- SIKJAQJRHWYJAI-UHFFFAOYSA-N c1c[nH]c2ccccc12 Chemical compound c1c[nH]c2ccccc12 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 108010007425 oligomycin sensitivity conferring protein Proteins 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- RAXXELZNTBOGNW-UHFFFAOYSA-N c1cnc[nH]1 Chemical compound c1cnc[nH]1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 description 1
- 230000030833 cell death Effects 0.000 description 1
- 230000003833 cell viability Effects 0.000 description 1
- 230000001413 cellular effect Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 230000008482 dysregulation Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 230000000977 initiatory effect Effects 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US97255307P | 2007-09-14 | 2007-09-14 | |
| US60/972,553 | 2007-09-14 | ||
| PCT/US2008/076021 WO2009036175A2 (en) | 2007-09-14 | 2008-09-11 | F1f0-atpase inhibitors and related methods |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011509238A JP2011509238A (ja) | 2011-03-24 |
| JP2011509238A5 true JP2011509238A5 (https=) | 2011-10-27 |
| JP5416122B2 JP5416122B2 (ja) | 2014-02-12 |
Family
ID=40452820
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010524985A Expired - Fee Related JP5416122B2 (ja) | 2007-09-14 | 2008-09-11 | Ｆ１Ｆ０−ＡＴＰａｓｅインヒビターおよび関連の方法 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US8324258B2 (https=) |
| EP (1) | EP2200977B1 (https=) |
| JP (1) | JP5416122B2 (https=) |
| CN (1) | CN101855203B (https=) |
| AU (1) | AU2008298870C1 (https=) |
| CA (1) | CA2698248C (https=) |
| ES (1) | ES2614498T3 (https=) |
| IL (1) | IL204442A (https=) |
| MX (1) | MX2010002732A (https=) |
| NZ (1) | NZ583689A (https=) |
| WO (1) | WO2009036175A2 (https=) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2359831A3 (en) | 1999-04-30 | 2012-02-01 | The Regents of the University of Michigan | Therapeutic applications of pro-apoptotic benzodiazepines |
| US7144880B2 (en) | 1999-04-30 | 2006-12-05 | Regents Of The University Of Michigan | Compositions relating to novel compounds and targets thereof |
| EP1948191B1 (en) | 2005-11-01 | 2013-01-16 | The Regents of the University of Michigan | Novel 1,4-benzodiazepine-2,5-diones with therapeutic properties |
| CA2680017C (en) | 2007-03-09 | 2013-11-12 | The Regents Of The University Of Michigan | Compositions and methods relating to novel compounds and targets thereof |
| EP2200977B1 (en) | 2007-09-14 | 2016-11-09 | The Regents of the University of Michigan | F1f0-atpase inhibitors and related methods |
| MX2010004857A (es) | 2007-11-06 | 2010-07-28 | Univ Michigan | Compuestos de benzodiazepinona utiles en el tratamiento de afecciones de la piel. |
| EP2352724B1 (en) * | 2008-09-11 | 2015-04-22 | The Regents of the University of Michigan | Aryl guanidine f1f0-atpase inhibitors and their medical use |
| WO2010121164A2 (en) | 2009-04-17 | 2010-10-21 | The Regents Of The University Of Michigan | 1,4-benzodiazepinone compounds and their use in treating cancer |
| US8673897B2 (en) | 2009-09-18 | 2014-03-18 | The Regents Of The University Of Michigan | Benzodiazepinone compounds and methods of treatment using same |
| WO2011062765A2 (en) | 2009-11-17 | 2011-05-26 | The Regents Of The University Of Michigan | 1,4-benzodiazepine-2,5-diones and related compounds with therapeutic properties |
| CN102753544A (zh) | 2009-11-17 | 2012-10-24 | 密执安大学评议会 | 具有治疗性能的1，4-苯并二氮杂*-2，5-二酮和相关化合物 |
| CA2820044A1 (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 |
| AU2011338302A1 (en) * | 2010-12-08 | 2013-07-11 | Lycera Corporation | Cycloalkyl guanidine F1F0-ATPase inhibitors and therapeutic uses thereof |
| SMT201700445T1 (it) * | 2010-12-08 | 2017-11-15 | Lycera Corporation| | Inibitori della f1f0-atpasi della pirazolilguanidina e loro usi terapeutici |
| EP2861225A4 (en) | 2012-06-08 | 2015-11-18 | Lycera Corp | Saturated acylguanidine for the inhibition of F1F0-ATPASE |
| US9221814B2 (en) | 2012-06-08 | 2015-12-29 | Lycera Corporation | Heterocyclic guanidine F1F0-atpase inhibitors and therapeutic uses thereof |
| WO2013185045A1 (en) | 2012-06-08 | 2013-12-12 | Lycera Corporation | Indazole guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
| CA2879454A1 (en) | 2012-07-19 | 2014-01-23 | Drexel University | Novel sigma receptor ligands and methods of modulating cellular protein homeostasis using same |
| CA2931851A1 (en) * | 2013-12-10 | 2015-06-18 | Lycera Corporation | Trifluoromethyl pyrazolyl guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
| CA2931850A1 (en) | 2013-12-10 | 2015-06-18 | Lycera Corporation | Alkylpyrazolyl guanidine f1f0-atpase inhibitors and therapeutic uses thereof |
| US9914706B2 (en) | 2013-12-10 | 2018-03-13 | Lycera Corporation | N-substituted pyrazolyl guanidine F1F0-ATPase inhibitors and therapeutic uses thereof |
| DK3416964T3 (da) | 2016-02-19 | 2021-02-22 | Phoenix Molecular Designs | 6-Oxo-N-(1-(benzyl)-1H-pyrazol-4-YL)-6,7,8,9-tetrahydropyrido[3',2':4,5]pyrrolo[1,2-A]pyrazin-2-carboxamid-derivater som P90 ribosomal S6 kinase- (RSK-) hæmmere til behandling af cancer |
| WO2019089902A1 (en) | 2017-11-01 | 2019-05-09 | Drexel University | Compounds, compositions, and methods for treating diseases |
| CN108486117B (zh) * | 2018-04-27 | 2020-09-08 | 浙江大学 | 一种rna抑制剂及其在抑制f1f0-atp合成酶活性中的应用 |
| US12378245B2 (en) | 2019-02-11 | 2025-08-05 | Phoenix Molecular Designs | Crystalline forms of an RSK inhibitor |
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| ATE440827T1 (de) * | 2002-12-04 | 2009-09-15 | Ore Pharmaceuticals Inc | Melanocortin-rezeptormodulatoren |
| AU2004255153B2 (en) | 2003-05-01 | 2007-11-22 | The Regents Of The University Of Michigan | Compositions and methods relating to novel compounds and targets thereof |
| US7351241B2 (en) | 2003-06-02 | 2008-04-01 | Carl Zeiss Meditec Ag | Method and apparatus for precision working of material |
| 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 |
| 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 |
| EP1765325A4 (en) * | 2004-07-01 | 2009-08-12 | Synta Pharmaceuticals Corp | HETEROARYL COMPOUNDS SUBSTITUTED IN 2 |
| US20060052369A1 (en) | 2004-09-07 | 2006-03-09 | The Regents Of The University Of Michigan | Compositions and methods relating to novel compounds and targets thereof |
| JP2008528448A (ja) | 2005-01-03 | 2008-07-31 | ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン | 新規化合物に関連する組成物および方法、ならびにその標的 |
| WO2007053193A2 (en) | 2005-06-01 | 2007-05-10 | The Regents Of The University Of Michigan | Unsolvated benzodiazepine compositions and methods |
| EP1742460A1 (en) | 2005-06-18 | 2007-01-10 | TTE Germany GmbH | Raster distortion correction circuit |
| US20070105844A1 (en) | 2005-10-26 | 2007-05-10 | Regents Of The University Of Michigan | Therapeutic compositions and methods |
| JP2009513644A (ja) | 2005-10-26 | 2009-04-02 | ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン | 治療組成物および方法 |
| EP1948191B1 (en) | 2005-11-01 | 2013-01-16 | The Regents of the University of Michigan | Novel 1,4-benzodiazepine-2,5-diones with therapeutic properties |
| US7759338B2 (en) | 2006-04-27 | 2010-07-20 | The Regents Of The University Of Michigan | Soluble 1,4 benzodiazepine compounds and stable salts thereof |
| EP2418206A3 (en) | 2006-06-09 | 2012-06-27 | The Regents of the University of Michigan | Benzodiazepine derivatives useful in the treatment of autoimmune disorders |
| GB0615068D0 (en) | 2006-07-28 | 2006-09-06 | Ttp Communications Ltd | Digital radio systems |
| CA2680017C (en) * | 2007-03-09 | 2013-11-12 | The Regents Of The University Of Michigan | Compositions and methods relating to novel compounds and targets thereof |
| EP2200977B1 (en) | 2007-09-14 | 2016-11-09 | The Regents of the University of Michigan | F1f0-atpase inhibitors and related methods |
| MX2010004857A (es) | 2007-11-06 | 2010-07-28 | Univ Michigan | Compuestos de benzodiazepinona utiles en el tratamiento de afecciones de la piel. |
| CN111381371B (zh) | 2018-12-27 | 2022-04-15 | 中强光电股份有限公司 | 头戴式显示装置 |
-
2008
- 2008-09-11 EP EP08831237.6A patent/EP2200977B1/en not_active Not-in-force
- 2008-09-11 MX MX2010002732A patent/MX2010002732A/es not_active Application Discontinuation
- 2008-09-11 JP JP2010524985A patent/JP5416122B2/ja not_active Expired - Fee Related
- 2008-09-11 WO PCT/US2008/076021 patent/WO2009036175A2/en not_active Ceased
- 2008-09-11 CN CN200880115526.7A patent/CN101855203B/zh not_active Expired - Fee Related
- 2008-09-11 US US12/677,598 patent/US8324258B2/en not_active Expired - Fee Related
- 2008-09-11 CA CA2698248A patent/CA2698248C/en not_active Expired - Fee Related
- 2008-09-11 ES ES08831237.6T patent/ES2614498T3/es active Active
- 2008-09-11 AU AU2008298870A patent/AU2008298870C1/en not_active Ceased
- 2008-09-11 NZ NZ583689A patent/NZ583689A/en not_active IP Right Cessation
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2010
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