JP2010523717A5 - - Google Patents
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- JP2010523717A5 JP2010523717A5 JP2010503257A JP2010503257A JP2010523717A5 JP 2010523717 A5 JP2010523717 A5 JP 2010523717A5 JP 2010503257 A JP2010503257 A JP 2010503257A JP 2010503257 A JP2010503257 A JP 2010503257A JP 2010523717 A5 JP2010523717 A5 JP 2010523717A5
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- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
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- ring
- 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.)
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- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims description 56
- 150000001875 compounds Chemical class 0.000 claims description 47
- 125000005842 heteroatom Chemical group 0.000 claims description 42
- 125000003118 aryl group Chemical group 0.000 claims description 38
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 32
- 229910052760 oxygen Inorganic materials 0.000 claims description 28
- 229910052717 sulfur Inorganic materials 0.000 claims description 28
- 239000000178 monomer Substances 0.000 claims description 16
- 229920006395 saturated elastomer Polymers 0.000 claims description 16
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims description 12
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims description 12
- 125000004429 atom Chemical group 0.000 claims description 12
- 125000004122 cyclic group Chemical group 0.000 claims description 12
- 125000004474 heteroalkylene group Chemical group 0.000 claims description 12
- 125000001072 heteroaryl group Chemical group 0.000 claims description 12
- 125000005647 linker group Chemical group 0.000 claims description 12
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 12
- 150000003839 salts Chemical class 0.000 claims description 12
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims description 10
- 229910052757 nitrogen Inorganic materials 0.000 claims description 10
- 125000004450 alkenylene group Chemical group 0.000 claims description 8
- 125000002947 alkylene group Chemical group 0.000 claims description 8
- 125000004419 alkynylene group Chemical group 0.000 claims description 8
- 125000000217 alkyl group Chemical group 0.000 claims description 6
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 6
- 125000006270 aryl alkenylene group Chemical group 0.000 claims description 6
- 229910052739 hydrogen Inorganic materials 0.000 claims description 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 6
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 4
- 229910052799 carbon Inorganic materials 0.000 claims description 4
- 239000000539 dimer Substances 0.000 claims description 4
- 101100369992 Homo sapiens TNFSF10 gene Proteins 0.000 claims description 3
- 102000046283 TNF-Related Apoptosis-Inducing Ligand Human genes 0.000 claims description 3
- 102000002259 TNF-Related Apoptosis-Inducing Ligand Receptors Human genes 0.000 claims description 3
- 108010000449 TNF-Related Apoptosis-Inducing Ligand Receptors Proteins 0.000 claims description 3
- 108700012411 TNFSF10 Proteins 0.000 claims description 3
- 239000003814 drug Substances 0.000 claims description 3
- VJJPUSNTGOMMGY-MRVIYFEKSA-N etoposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@H](C)OC[C@H]4O3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 VJJPUSNTGOMMGY-MRVIYFEKSA-N 0.000 claims description 3
- 229960005420 etoposide Drugs 0.000 claims description 3
- 239000003481 heat shock protein 90 inhibitor Substances 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 229940124597 therapeutic agent Drugs 0.000 claims description 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 2
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- 125000004650 C1-C8 alkynyl group Chemical group 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
- 206010061218 Inflammation Diseases 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 125000003342 alkenyl group Chemical group 0.000 claims description 2
- 150000001412 amines Chemical class 0.000 claims description 2
- 150000001540 azides Chemical class 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 125000003983 fluorenyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3CC12)* 0.000 claims description 2
- 125000000524 functional group Chemical group 0.000 claims description 2
- 125000005843 halogen group Chemical group 0.000 claims description 2
- 125000000623 heterocyclic group Chemical group 0.000 claims description 2
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims description 2
- 230000004054 inflammatory process Effects 0.000 claims description 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 238000000034 method Methods 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims description 2
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 2
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 2
- 230000037361 pathway Effects 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 229940075439 smac mimetic Drugs 0.000 claims description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 claims description 2
- 239000013638 trimer Substances 0.000 claims description 2
- 102100040247 Tumor necrosis factor Human genes 0.000 description 3
- MZOFCQQQCNRIBI-VMXHOPILSA-N (3s)-4-[[(2s)-1-[[(2s)-1-[[(1s)-1-carboxy-2-hydroxyethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-[[2-[[(2s)-2,6-diaminohexanoyl]amino]acetyl]amino]-4-oxobutanoic acid Chemical compound OC[C@@H](C(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@@H](N)CCCCN MZOFCQQQCNRIBI-VMXHOPILSA-N 0.000 description 2
- 0 CC[C@](C[C@](CCCC([C@]1NC([C@](C)NC)=CCCC1(C)C)=O)C(N[C@]1c2ccccc2CCC1)=O)N1N=CC*C(CCCC(N)=CN([C@@](C[C@]2C(N[C@](CCC3)c4c3cccc4)=O)CN2C([C@](C(C)(C)C)NC([C@](C)NC)=N)=O)N)=C1 Chemical compound CC[C@](C[C@](CCCC([C@]1NC([C@](C)NC)=CCCC1(C)C)=O)C(N[C@]1c2ccccc2CCC1)=O)N1N=CC*C(CCCC(N)=CN([C@@](C[C@]2C(N[C@](CCC3)c4c3cccc4)=O)CN2C([C@](C(C)(C)C)NC([C@](C)NC)=N)=O)N)=C1 0.000 description 2
- 108060008682 Tumor Necrosis Factor Proteins 0.000 description 2
- YPTWSOJPLMWQMX-IBGYOADYSA-N C[C@@H](C(N[C@@H](C(C)(C)C)C(N(CC(C1)/C=N/C(c2cc(N)cc(C(N[C@@H](C[C@H]3C(/N=C\C4c5ccccc5CCC4)=O)CN3C([C@H](C(C)(C)C)NC(C(C)NC)=O)=O)=O)c2)=O)[C@@H]1C(N[C@H]1c2ccccc2CCC1)=O)=O)=O)NC Chemical compound C[C@@H](C(N[C@@H](C(C)(C)C)C(N(CC(C1)/C=N/C(c2cc(N)cc(C(N[C@@H](C[C@H]3C(/N=C\C4c5ccccc5CCC4)=O)CN3C([C@H](C(C)(C)C)NC(C(C)NC)=O)=O)=O)c2)=O)[C@@H]1C(N[C@H]1c2ccccc2CCC1)=O)=O)=O)NC YPTWSOJPLMWQMX-IBGYOADYSA-N 0.000 description 1
- CJGPODZBXAXSQQ-CRJUXLEGSA-N C[C@@H](C(N[C@@H](C(C)(C)C)C(N(CC(C1)/C=N\C(C(CC2C3)(C4)CC3CC24C(N[C@@H](C[C@H]2C(N[C@H](CCC3)c4c3cccc4)=O)CN2C([C@H](C(C)(C)C)NC([C@H](C)NC)=O)=O)=O)=O)[C@@H]1C(N[C@H]1c2ccccc2CCC1)=O)=O)=O)NC Chemical compound C[C@@H](C(N[C@@H](C(C)(C)C)C(N(CC(C1)/C=N\C(C(CC2C3)(C4)CC3CC24C(N[C@@H](C[C@H]2C(N[C@H](CCC3)c4c3cccc4)=O)CN2C([C@H](C(C)(C)C)NC([C@H](C)NC)=O)=O)=O)=O)[C@@H]1C(N[C@H]1c2ccccc2CCC1)=O)=O)=O)NC CJGPODZBXAXSQQ-CRJUXLEGSA-N 0.000 description 1
- JPHUVEPVDWCUHS-NLUXXOGOSA-N C[C@@H](C(N[C@@H](C(C)(C)C)C(N(C[C@H](C1)NCc2ccc(CN[C@@H](C[C@H]3C(N[C@H](CCC4)c5c4cccc5)=O)CN3C([C@H](C(C)(C)C)NC([C@H](C)NC)=O)=O)cc2)[C@@H]1C(N[C@H]1C2C=CC=CC2CCC1)=O)=O)=O)NC Chemical compound C[C@@H](C(N[C@@H](C(C)(C)C)C(N(C[C@H](C1)NCc2ccc(CN[C@@H](C[C@H]3C(N[C@H](CCC4)c5c4cccc5)=O)CN3C([C@H](C(C)(C)C)NC([C@H](C)NC)=O)=O)cc2)[C@@H]1C(N[C@H]1C2C=CC=CC2CCC1)=O)=O)=O)NC JPHUVEPVDWCUHS-NLUXXOGOSA-N 0.000 description 1
- 102000004083 Lymphotoxin-alpha Human genes 0.000 description 1
- 108090000542 Lymphotoxin-alpha Proteins 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 238000004166 bioassay Methods 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91147207P | 2007-04-12 | 2007-04-12 | |
| US60/911,472 | 2007-04-12 | ||
| US95249307P | 2007-07-27 | 2007-07-27 | |
| US60/952,493 | 2007-07-27 | ||
| PCT/US2008/060140 WO2008128121A1 (en) | 2007-04-12 | 2008-04-11 | Smac mimetic dimers and trimers useful as anti-cancer agents |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010523717A JP2010523717A (ja) | 2010-07-15 |
| JP2010523717A5 true JP2010523717A5 (cg-RX-API-DMAC7.html) | 2012-02-09 |
| JP5454943B2 JP5454943B2 (ja) | 2014-03-26 |
Family
ID=39864357
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010503257A Expired - Fee Related JP5454943B2 (ja) | 2007-04-12 | 2008-04-11 | 抗癌剤として有用なｓｍａｃ模倣二量体及び三量体 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US8642554B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2079309B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP5454943B2 (cg-RX-API-DMAC7.html) |
| CN (1) | CN101668426B (cg-RX-API-DMAC7.html) |
| AU (1) | AU2008240153B2 (cg-RX-API-DMAC7.html) |
| BR (1) | BRPI0810178A2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2684169C (cg-RX-API-DMAC7.html) |
| MX (1) | MX2009010667A (cg-RX-API-DMAC7.html) |
| NZ (1) | NZ580313A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2008128121A1 (cg-RX-API-DMAC7.html) |
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| EP1773766B1 (en) | 2004-07-15 | 2014-04-02 | Tetralogic Pharmaceuticals Corporation | Iap binding compounds |
| AU2006216450C1 (en) | 2005-02-25 | 2013-01-10 | Medivir Ab | Dimeric IAP inhibitors |
| CA2607940C (en) | 2005-05-18 | 2009-12-15 | Aegera Therapeutics Inc. | Bir domain binding compounds |
| US20100256046A1 (en) * | 2009-04-03 | 2010-10-07 | Tetralogic Pharmaceuticals Corporation | Treatment of proliferative disorders |
| WO2007048224A1 (en) | 2005-10-25 | 2007-05-03 | Aegera Therapeutics Inc. | Iap bir domain binding compounds |
| TWI504597B (zh) | 2006-03-16 | 2015-10-21 | Pharmascience Inc | 結合於細胞凋亡抑制蛋白（ｉａｐ）之桿狀病毒ｉａｐ重複序列（ｂｉｒ）區域之化合物 |
| RU2008152171A (ru) | 2006-07-05 | 2010-08-10 | Интермьюн, Инк. (Us) | Новые ингибиторы вирусной репликации гепатита с |
| US20100143499A1 (en) * | 2006-07-24 | 2010-06-10 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| EP2049524A2 (en) * | 2006-07-24 | 2009-04-22 | Tetralogic Pharmaceuticals Corporation | Iap inhibitors |
| AU2007276760B2 (en) * | 2006-07-24 | 2012-01-19 | Tetralogic Pharmaceuticals Corporation | Dimeric IAP antagonists |
| WO2008014240A2 (en) * | 2006-07-24 | 2008-01-31 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| US20100144650A1 (en) * | 2006-07-24 | 2010-06-10 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| US20100056495A1 (en) * | 2006-07-24 | 2010-03-04 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| EP2156189A1 (en) * | 2007-05-07 | 2010-02-24 | Tetralogic Pharmaceuticals Corp. | Tnf gene expression as a biomarker of sensitivity to antagonists of inhibitor of apoptosis proteins |
| US7932277B2 (en) | 2007-05-10 | 2011-04-26 | Intermune, Inc. | Peptide inhibitors of hepatitis C virus replication |
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| RU2505540C2 (ru) | 2008-12-23 | 2014-01-27 | Эббви Инк. | Антивирусные соединения |
| WO2010120935A1 (en) * | 2009-04-15 | 2010-10-21 | Abbott Laboratories | Anti-viral compounds |
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| US10201584B1 (en) | 2011-05-17 | 2019-02-12 | Abbvie Inc. | Compositions and methods for treating HCV |
| US9034832B2 (en) | 2011-12-29 | 2015-05-19 | Abbvie Inc. | Solid compositions |
| WO2014055461A1 (en) * | 2012-10-02 | 2014-04-10 | Bristol-Myers Squibb Company | Iap antagonists |
| US11484534B2 (en) | 2013-03-14 | 2022-11-01 | Abbvie Inc. | Methods for treating HCV |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
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| CN104710510A (zh) * | 2013-12-12 | 2015-06-17 | 深圳先进技术研究院 | Smac蛋白二聚拟合物及其鉴定方法 |
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| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
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| US10398702B2 (en) * | 2016-05-09 | 2019-09-03 | Hoffmann-La Roche Inc. | Dimeric compounds |
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| AU2020336309A1 (en) | 2019-08-26 | 2022-03-17 | Arvinas Operations, Inc. | Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders |
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| JP2005519848A (ja) | 2000-11-02 | 2005-07-07 | スローン−ケッタリング・インスティテュート・フォー・キャンサー・リサーチ | Ｈｓｐ９０に結合するための小分子組成物 |
| EP1495124A2 (en) | 2002-04-17 | 2005-01-12 | Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts | Smac-peptides as therapeutics against cancer and autoimmune diseases |
| US20060128632A1 (en) * | 2002-07-02 | 2006-06-15 | Sharma Sushil K | Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap) |
| BRPI0414533A (pt) | 2003-09-18 | 2006-11-07 | Conforma Therapeutics Corp | composto, composição farmacêutica, e, métodos para inibir um hsp90 e para tratar um indivìduo tendo um distúrbio mediado por hsp90 |
| JP4674231B2 (ja) * | 2004-03-01 | 2011-04-20 | ボード・オブ・リージエンツ，ザ・ユニバーシテイ・オブ・テキサス・システム | ２量体小分子アポトーシス増強剤 |
| EP1740173A4 (en) | 2004-03-23 | 2009-05-27 | Genentech Inc | AZABICYCLOOCTAN IAP INHIBITORS |
| DK2253614T3 (da) | 2004-04-07 | 2013-01-07 | Novartis Ag | IAP-inhibitorer |
| MXPA06014969A (es) | 2004-07-02 | 2007-02-08 | Genentech Inc | Inhibidores de iap. |
| EP1773766B1 (en) * | 2004-07-15 | 2014-04-02 | Tetralogic Pharmaceuticals Corporation | Iap binding compounds |
| EA019420B1 (ru) | 2004-12-20 | 2014-03-31 | Дженентех, Инк. | Пирролидиновые ингибиторы иап (ингибиторов апоптоза) |
| AU2006216450C1 (en) * | 2005-02-25 | 2013-01-10 | Medivir Ab | Dimeric IAP inhibitors |
| CA2607940C (en) * | 2005-05-18 | 2009-12-15 | Aegera Therapeutics Inc. | Bir domain binding compounds |
| TWI504597B (zh) * | 2006-03-16 | 2015-10-21 | Pharmascience Inc | 結合於細胞凋亡抑制蛋白（ｉａｐ）之桿狀病毒ｉａｐ重複序列（ｂｉｒ）區域之化合物 |
-
2008
- 2008-04-11 AU AU2008240153A patent/AU2008240153B2/en not_active Ceased
- 2008-04-11 WO PCT/US2008/060140 patent/WO2008128121A1/en not_active Ceased
- 2008-04-11 JP JP2010503257A patent/JP5454943B2/ja not_active Expired - Fee Related
- 2008-04-11 MX MX2009010667A patent/MX2009010667A/es active IP Right Grant
- 2008-04-11 NZ NZ580313A patent/NZ580313A/en not_active IP Right Cessation
- 2008-04-11 CN CN200880011260.1A patent/CN101668426B/zh not_active Expired - Fee Related
- 2008-04-11 US US12/101,733 patent/US8642554B2/en not_active Expired - Fee Related
- 2008-04-11 EP EP08745697.6A patent/EP2079309B1/en not_active Withdrawn - After Issue
- 2008-04-11 CA CA2684169A patent/CA2684169C/en not_active Expired - Fee Related
- 2008-04-11 BR BRPI0810178-7A patent/BRPI0810178A2/pt not_active IP Right Cessation
-
2014
- 2014-01-16 US US14/156,522 patent/US20140127155A1/en not_active Abandoned
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