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
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- optionally substituted
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- Prior art date
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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 heteroatoms Chemical group 0.000 claims description 42
- 125000003118 aryl group Chemical group 0.000 claims description 33
- 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
- 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 atoms 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
- 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
- 239000011780 sodium chloride Substances 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
- 125000005418 aryl aryl group Chemical group 0.000 claims description 9
- 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
- 125000000732 arylene 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
- 150000002829 nitrogen Chemical group 0.000 claims description 6
- 125000004433 nitrogen atoms Chemical group N* 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
- 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
- 102000007193 TNF-Related Apoptosis-Inducing Ligand Human genes 0.000 claims description 3
- 108010008478 TNF-Related Apoptosis-Inducing Ligand Proteins 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
- 102000004965 antibodies Human genes 0.000 claims description 3
- 108090001123 antibodies Proteins 0.000 claims description 3
- 239000003814 drug Substances 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
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 2
- 206010003816 Autoimmune disease Diseases 0.000 claims description 2
- 125000004650 C1-C8 alkynyl group Chemical group 0.000 claims description 2
- 102100013714 DIABLO Human genes 0.000 claims description 2
- 101710002761 DIABLO Proteins 0.000 claims description 2
- 206010061218 Inflammation 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
- 201000009596 autoimmune hypersensitivity disease Diseases 0.000 claims description 2
- IVRMZWNICZWHMI-UHFFFAOYSA-N azide Chemical compound [N-]=[N+]=[N-] IVRMZWNICZWHMI-UHFFFAOYSA-N 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 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 pharmaceutic aid 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
- 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
- -1 TNF- [alpha] Proteins 0.000 claims 1
- 102100009534 TNF Human genes 0.000 description 3
- 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
- 108010001801 Tumor Necrosis Factor-alpha Proteins 0.000 description 2
- 238000004166 bioassay Methods 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
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 (US07794700-20100914-C00152.png) | 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)
Families Citing this family (61)
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| CA2574040C (en) | 2004-07-15 | 2014-05-06 | Tetralogic Pharmaceuticals Corporation | Iap binding compounds |
| CA2598995C (en) * | 2005-02-25 | 2014-07-15 | Stephen M. Condon | Dimeric iap inhibitors |
| JP4954983B2 (ja) | 2005-05-18 | 2012-06-20 | ファーマサイエンス・インコーポレイテッド | Ｂｉｒドメイン結合化合物 |
| US20100256046A1 (en) * | 2009-04-03 | 2010-10-07 | Tetralogic Pharmaceuticals Corporation | Treatment of proliferative disorders |
| BRPI0617751A2 (pt) | 2005-10-25 | 2011-08-02 | Aegera Therapeutics Inc | compostos de ligação do domìnio iap bir |
| 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 |
| KR20090024834A (ko) | 2006-07-05 | 2009-03-09 | 인터뮨, 인크. | Ｃ형 간염 바이러스 복제의 신규 억제제 |
| WO2008014236A1 (en) * | 2006-07-24 | 2008-01-31 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| US7985735B2 (en) * | 2006-07-24 | 2011-07-26 | Tetralogic Pharmaceuticals Corporation | Dimeric IAP inhibitors |
| US20100113326A1 (en) * | 2006-07-24 | 2010-05-06 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| EP2049524A2 (en) * | 2006-07-24 | 2009-04-22 | Tetralogic Pharmaceuticals Corporation | Iap inhibitors |
| US20100144650A1 (en) * | 2006-07-24 | 2010-06-10 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| WO2008014238A2 (en) * | 2006-07-24 | 2008-01-31 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| JP2010528587A (ja) * | 2007-05-07 | 2010-08-26 | テトラロジック ファーマシューティカルズ コーポレーション | アポトーシス阻害タンパク質のアンタゴニストに対する感受性のバイオマーカーとしてＴＮＦα遺伝子の発現を用いる方法 |
| JP2010526834A (ja) | 2007-05-10 | 2010-08-05 | インターミューン・インコーポレーテッド | Ｃ型肝炎ウイルス複製の新規ペプチド阻害剤 |
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| CA2950911C (en) | 2014-06-04 | 2023-10-10 | Sanford-Burnham Medical Research Institute | Use of inhibitor of apoptosis protein (iap) antagonists in hiv therapy |
| KR20230119040A (ko) | 2015-01-20 | 2023-08-14 | 아비나스 오퍼레이션스, 인코포레이티드 | 안드로겐 수용체의 표적화된 분해를 위한 화합물 및방법 |
| US20170327469A1 (en) | 2015-01-20 | 2017-11-16 | Arvinas, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| WO2016197114A1 (en) | 2015-06-05 | 2016-12-08 | Arvinas, Inc. | Tank-binding kinase-1 protacs and associated methods of use |
| WO2017030814A1 (en) | 2015-08-19 | 2017-02-23 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| JP6953435B2 (ja) * | 2016-05-09 | 2021-10-27 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | 二量体化合物 |
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| KR102173464B1 (ko) | 2016-12-01 | 2020-11-04 | 아비나스 오퍼레이션스, 인코포레이티드 | 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체 |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| KR102564201B1 (ko) | 2016-12-23 | 2023-08-07 | 아비나스 오퍼레이션스, 인코포레이티드 | 급속 진행성 섬유육종 폴리펩티드의 표적화 분해를 위한 화합물 및 방법 |
| EP3559006A4 (en) | 2016-12-23 | 2021-03-03 | Arvinas Operations, Inc. | COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF FETAL LIVER KINASE POLYPEPTIDES |
| EP3559002A4 (en) | 2016-12-23 | 2021-02-17 | Arvinas Operations, Inc. | CHEMERICAL MOLECULES TARGETING EGFR PROTEOLYSIS AND RELATED METHODS OF USE |
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| EP3573977A4 (en) | 2017-01-26 | 2020-12-23 | Arvinas Operations, Inc. | EESTROGEN RECEPTOR PROTEOLYSIS MODULATORS AND RELATED METHOD OF USE |
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| ATE477254T1 (de) | 2004-12-20 | 2010-08-15 | Genentech Inc | Pyrrolidine als inhibitoren von iap |
| CA2598995C (en) * | 2005-02-25 | 2014-07-15 | Stephen M. Condon | Dimeric iap inhibitors |
| JP4954983B2 (ja) * | 2005-05-18 | 2012-06-20 | ファーマサイエンス・インコーポレイテッド | Ｂｉｒドメイン結合化合物 |
| 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 MX MX2009010667A patent/MX2009010667A/es active IP Right Grant
- 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 NZ NZ580313A patent/NZ580313A/en not_active IP Right Cessation
- 2008-04-11 BR BRPI0810178-7A patent/BRPI0810178A2/pt not_active IP Right Cessation
- 2008-04-11 WO PCT/US2008/060140 patent/WO2008128121A1/en active Application Filing
- 2008-04-11 CA CA2684169A patent/CA2684169C/en not_active Expired - Fee Related
- 2008-04-11 JP JP2010503257A patent/JP5454943B2/ja not_active Expired - Fee Related
- 2008-04-11 AU AU2008240153A patent/AU2008240153B2/en not_active Ceased
- 2008-04-11 EP EP08745697.6A patent/EP2079309B1/en not_active Withdrawn - After Issue
-
2014
- 2014-01-16 US US14/156,522 patent/US20140127155A1/en not_active Abandoned
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