JP2010523717A5 - - Google Patents
Download PDFInfo
- Publication number
- 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
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- independently
- 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.)
- Granted
Links
- 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 (enExample) | 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 (enExample) |
| EP (1) | EP2079309B1 (enExample) |
| JP (1) | JP5454943B2 (enExample) |
| CN (1) | CN101668426B (enExample) |
| AU (1) | AU2008240153B2 (enExample) |
| BR (1) | BRPI0810178A2 (enExample) |
| CA (1) | CA2684169C (enExample) |
| MX (1) | MX2009010667A (enExample) |
| NZ (1) | NZ580313A (enExample) |
| WO (1) | WO2008128121A1 (enExample) |
Families Citing this family (70)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5230865B2 (ja) | 2004-07-15 | 2013-07-10 | 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 | Ｉａｐ結合性化合物 |
| EA012810B1 (ru) | 2005-02-25 | 2009-12-30 | Тетралоджик Фармасеутикалс | Димерные ингибиторы ингибиторов белков апоптоза (iap) |
| WO2006122408A1 (en) | 2005-05-18 | 2006-11-23 | Aegera Therapeutics Inc. | Bir domain binding compounds |
| US20100256046A1 (en) * | 2009-04-03 | 2010-10-07 | Tetralogic Pharmaceuticals Corporation | Treatment of proliferative disorders |
| AU2006308453B9 (en) | 2005-10-25 | 2011-12-01 | Pharmascience 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 |
| WO2008014229A2 (en) * | 2006-07-24 | 2008-01-31 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| MX2009000824A (es) * | 2006-07-24 | 2009-02-04 | Tetralogic Pharmaceuticals Cor | Antagonistas dimericos de las proteinas inhibidoras de la apoptosis. |
| US20100056495A1 (en) * | 2006-07-24 | 2010-03-04 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| WO2008014240A2 (en) * | 2006-07-24 | 2008-01-31 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| JP5452223B2 (ja) * | 2006-07-24 | 2014-03-26 | 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 | Ｉａｐ阻害剤 |
| 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 |
| CA2686546A1 (en) | 2007-05-10 | 2008-11-20 | Intermune, Inc. | Novel peptide inhibitors of hepatitis c virus replication |
| WO2010031171A1 (en) * | 2008-09-19 | 2010-03-25 | Aegera Therapeutics, Inc. | Iap bir domain binding compounds |
| RU2505539C2 (ru) | 2008-12-23 | 2014-01-27 | Эбботт Лэборетриз | Антивирусные соединения |
| CN102264737A (zh) * | 2008-12-23 | 2011-11-30 | 雅培制药有限公司 | 抗病毒化合物 |
| WO2010120935A1 (en) * | 2009-04-15 | 2010-10-21 | Abbott Laboratories | Anti-viral compounds |
| EP2853531A3 (en) * | 2009-06-11 | 2015-08-12 | AbbVie Bahamas Ltd. | Antiviral compounds |
| US9394279B2 (en) | 2009-06-11 | 2016-07-19 | Abbvie Inc. | Anti-viral compounds |
| US8937150B2 (en) | 2009-06-11 | 2015-01-20 | Abbvie Inc. | Anti-viral compounds |
| US8716454B2 (en) | 2009-06-11 | 2014-05-06 | Abbvie Inc. | Solid compositions |
| US8283372B2 (en) * | 2009-07-02 | 2012-10-09 | Tetralogic Pharmaceuticals Corp. | 2-(1H-indol-3-ylmethyl)-pyrrolidine dimer as a SMAC mimetic |
| EP2493879B1 (en) * | 2009-10-28 | 2014-05-14 | Joyant Pharmaceuticals, Inc. | Dimeric smac mimetics |
| NZ602368A (en) | 2010-02-12 | 2014-10-31 | Pharmascience Inc | Iap bir domain binding compounds |
| UY33236A (es) * | 2010-02-25 | 2011-09-30 | Novartis Ag | Inhibidores dimericos de las iap |
| NZ605440A (en) | 2010-06-10 | 2014-05-30 | Abbvie Bahamas Ltd | Solid compositions comprising an hcv inhibitor |
| UY33794A (es) | 2010-12-13 | 2012-07-31 | Novartis Ag | Inhibidores diméricos de las iap |
| 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 |
| US9603889B2 (en) * | 2012-10-02 | 2017-03-28 | Bristol-Myers Squibb Company | IAP antagonists |
| US11484534B2 (en) | 2013-03-14 | 2022-11-01 | Abbvie Inc. | Methods for treating HCV |
| GB201311888D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| 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 |
| WO2015103490A1 (en) | 2014-01-03 | 2015-07-09 | Abbvie, Inc. | Solid antiviral dosage forms |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| JP6768522B2 (ja) | 2014-06-04 | 2020-10-14 | サンフォード−バーンハム メディカル リサーチ インスティテュート | Ｈｉｖ治療におけるアポトーシスタンパク質阻害剤（ｉａｐ）のアンタゴニストの使用 |
| US12312316B2 (en) | 2015-01-20 | 2025-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| JP6817962B2 (ja) | 2015-01-20 | 2021-01-20 | アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． | ターゲティングされたアンドロゲン受容体分解のための化合物および方法 |
| WO2016197114A1 (en) | 2015-06-05 | 2016-12-08 | Arvinas, Inc. | Tank-binding kinase-1 protacs and associated methods of use |
| EP3337476A4 (en) | 2015-08-19 | 2019-09-04 | 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 |
| MX2019005007A (es) | 2016-11-01 | 2019-07-18 | Arvinas Inc | Protac dirigidos a la proteína tau y métodos asociados de uso. |
| IL266842B (en) | 2016-12-01 | 2022-09-01 | Arvinas Operations Inc | History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists |
| IL325835A (en) | 2016-12-23 | 2026-03-01 | Univ Yale | Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides |
| CN110753693A (zh) | 2016-12-23 | 2020-02-04 | 阿尔维纳斯运营股份有限公司 | Egfr蛋白水解靶向嵌合分子和相关使用方法 |
| US10806737B2 (en) | 2016-12-23 | 2020-10-20 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of fetal liver kinase polypeptides |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| US11191741B2 (en) | 2016-12-24 | 2021-12-07 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide |
| IL300417A (en) | 2017-01-26 | 2023-04-01 | Arvinas Operations Inc | Bifunctional benzothiophene compounds, preparations containing them and their use in therapy |
| US11065231B2 (en) | 2017-11-17 | 2021-07-20 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides |
| BR112020020307A2 (pt) | 2018-04-04 | 2021-01-12 | Arvinas Operations, Inc. | Moduladores de proteólise e métodos de uso associados |
| US11707452B2 (en) | 2018-08-20 | 2023-07-25 | Arvinas Operations, Inc. | Modulators of alpha-synuclein proteolysis and associated methods of use |
| AU2020252216B2 (en) * | 2019-04-05 | 2026-02-26 | Hepagene Therapeutics (HK) Limited | Bivalent antagonists of inhibitors of apoptosis proteins |
| EP3999182A1 (en) | 2019-07-17 | 2022-05-25 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated methods of use |
| WO2021041348A1 (en) | 2019-08-26 | 2021-03-04 | Arvinas Operations, Inc. | Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders |
| US12678509B2 (en) | 2019-11-08 | 2026-07-14 | Sanford Burnham Prebys Medical Discovery Institute | Inhibitor of apoptosis (IAP) protein antagonists |
| US20230056604A1 (en) | 2020-01-20 | 2023-02-23 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
| WO2022047145A1 (en) | 2020-08-28 | 2022-03-03 | Arvinas Operations, Inc. | Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use |
| US12503475B2 (en) | 2020-09-03 | 2025-12-23 | Centessa Pharmaceuticals (Uk) Limited | Bicyclic-heterocycle derivatives and their uses as orexin-2 receptor agonists |
| AU2021342287A1 (en) | 2020-09-14 | 2023-04-13 | Arvinas Operations, Inc. | Crystalline forms of a compound for the targeted degradation of estrogen receptor |
| WO2022164900A1 (en) * | 2021-01-27 | 2022-08-04 | Unm Rainforest Innovations | Pyrazole and pyrazoline-containing peptides, high throughput click libraries, and methods |
| EP4308095A4 (en) | 2021-03-15 | 2025-02-19 | Maze Therapeutics, Inc. | GLYCOGEN SYNTHASE 1 (GYS1) INHIBITORS AND METHODS OF USE THEREOF |
| WO2022207935A1 (en) | 2021-04-02 | 2022-10-06 | Orexia Therapeutics Limited | 2-(3-ethynylbenzyl)-substituted heterocycle derivatives as orexin-2 agonists |
| KR20240132251A (ko) | 2021-10-22 | 2024-09-03 | 유니버시티 오브 휴스턴 시스템 | 상피 조직의 만성 염증성 손상, 화생, 이형성증 및 암을 치료하기 위한 방법 및 조성물 |
| EP4584258A1 (en) | 2022-09-07 | 2025-07-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use |
| PE20260006A1 (es) | 2023-01-26 | 2026-01-06 | Arvinas Operations Inc | Protacs degradadores de kras basados en cereblon y usos relacionados con los mismos |
| CN120957983A (zh) * | 2023-04-17 | 2025-11-14 | 亚飞络思制药公司 | 取代的乙炔化合物衍生物及其药物用途 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4261989A (en) * | 1979-02-19 | 1981-04-14 | Kaken Chemical Co. Ltd. | Geldanamycin derivatives and antitumor drug |
| US5387584A (en) * | 1993-04-07 | 1995-02-07 | Pfizer Inc. | Bicyclic ansamycins |
| US5932566A (en) * | 1994-06-16 | 1999-08-03 | Pfizer Inc. | Ansamycin derivatives as antioncogene and anticancer agents |
| US5624677A (en) * | 1995-06-13 | 1997-04-29 | Pentech Pharmaceuticals, Inc. | Controlled release of drugs delivered by sublingual or buccal administration |
| SE9603466D0 (sv) * | 1996-09-23 | 1996-09-23 | Astra Ab | New compounds |
| US6916846B2 (en) * | 2000-05-12 | 2005-07-12 | Merck & Co. Inc. | Coumermycin analogs as chemical dimerizers of chimeric proteins |
| US7439359B2 (en) | 2000-11-02 | 2008-10-21 | Sloan-Kettering Institute For Cancer Research | Small molecule compositions for binding to hsp90 |
| WO2003086470A2 (en) | 2002-04-17 | 2003-10-23 | Deutsches Krebsforschungszentrum | Smac-peptides as therapeutics against cancer and autoimmune diseases |
| CA2491041A1 (en) * | 2002-07-02 | 2004-01-15 | Novartis Ag | Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap) |
| NZ546611A (en) | 2003-09-18 | 2010-02-26 | Conforma Therapeutics Corp | Novel heterocyclic compounds as HSP90-inhibitors |
| EP1723122B1 (en) * | 2004-03-01 | 2014-11-19 | Board of Regents, The University of Texas System | Dimeric small molecule potentiators of apoptosis |
| US7345081B2 (en) | 2004-03-23 | 2008-03-18 | Genentech, Inc. | Azabicyclo-octane inhibitors of IAP |
| PL2253614T3 (pl) | 2004-04-07 | 2013-03-29 | Novartis Ag | Inhibitory IAP |
| KR100926203B1 (ko) * | 2004-07-02 | 2009-11-09 | 제넨테크, 인크. | Ｉａｐ의 억제제 |
| JP5230865B2 (ja) * | 2004-07-15 | 2013-07-10 | 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 | Ｉａｐ結合性化合物 |
| MX2007007195A (es) | 2004-12-20 | 2007-10-08 | Genentech Inc | Inhibidores de pirrolidina de iap. |
| EA012810B1 (ru) * | 2005-02-25 | 2009-12-30 | Тетралоджик Фармасеутикалс | Димерные ингибиторы ингибиторов белков апоптоза (iap) |
| WO2006122408A1 (en) * | 2005-05-18 | 2006-11-23 | 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 CA CA2684169A patent/CA2684169C/en not_active Expired - Fee Related
- 2008-04-11 AU AU2008240153A patent/AU2008240153B2/en not_active Ceased
- 2008-04-11 CN CN200880011260.1A patent/CN101668426B/zh not_active Expired - Fee Related
- 2008-04-11 NZ NZ580313A patent/NZ580313A/en not_active IP Right Cessation
- 2008-04-11 JP JP2010503257A patent/JP5454943B2/ja not_active Expired - Fee Related
- 2008-04-11 BR BRPI0810178-7A patent/BRPI0810178A2/pt not_active IP Right Cessation
- 2008-04-11 US US12/101,733 patent/US8642554B2/en not_active Expired - Fee Related
- 2008-04-11 WO PCT/US2008/060140 patent/WO2008128121A1/en not_active Ceased
- 2008-04-11 MX MX2009010667A patent/MX2009010667A/es active IP Right Grant
- 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
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2009530424A5 (enExample) | ||
| CA2684169A1 (en) | Smac mimetic dimers and trimers useful as anti-cancer agents | |
| ES2670571T3 (es) | Derivados de pirrolamida sustituidos con glioxamida y su uso como medicamentos para el tratamiento de la hepatitis B | |
| JP2019514426A5 (enExample) | ||
| JP2021531826A5 (enExample) | ||
| TW201625626A (zh) | 作爲蛋白質激酶抑制劑之胺基噠嗪酮化合物 | |
| HU229076B1 (en) | Farnesyl protein transferase inhibitors with in vivo radiosensitizing properties | |
| IL311010A (en) | Enpp1 inhibitors and their use for the treatment of cancer | |
| CN101679246A (zh) | 新型吡咯啉酮衍生物以及包含其的药物组合物 | |
| JP2007511535A5 (enExample) | ||
| RU2009104764A (ru) | Производные пурина, как антангонисты a2a | |
| JP2008517983A5 (enExample) | ||
| JP7429726B2 (ja) | α４β７インテグリンを標的とする環状ペプチド多量体 | |
| TWI916398B (zh) | 含有烷基－氧雜環烷基部分之胺磺醯基脲衍生物及其用途 | |
| RU2009135621A (ru) | Хинолиновые производные для лечения воспалительных заболеваний | |
| JP2011500725A5 (enExample) | ||
| CA2565660A1 (en) | Ortho substituted aryl or heteroaryl amide compounds | |
| CN101304748A (zh) | Tlr激动剂 | |
| RU2007136535A (ru) | Пептидомиметические соединения и получение биологически активных производных | |
| RU2007120454A (ru) | Производные хинуклидина и их применение в качестве антагонистов мускариновых рецепторов м3 | |
| JP2013537198A5 (enExample) | ||
| CN108778288A (zh) | 可用于治疗疾病的FimH的甘露糖衍生的拮抗剂 | |
| TW200806652A (en) | N-hydroxyacrylamide compounds | |
| RU2007130144A (ru) | Гетероциклические соединения в качестве антагонистов cccr2b | |
| ES2351393T3 (es) | Sulfopirroles. |