JP2009512719A5 - - Google Patents
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- Publication number
- JP2009512719A5 JP2009512719A5 JP2008536890A JP2008536890A JP2009512719A5 JP 2009512719 A5 JP2009512719 A5 JP 2009512719A5 JP 2008536890 A JP2008536890 A JP 2008536890A JP 2008536890 A JP2008536890 A JP 2008536890A JP 2009512719 A5 JP2009512719 A5 JP 2009512719A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkynyl
- cycloalkyl
- alkenyl
- heterocyclyl
- 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.)
- Pending
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- 125000000753 cycloalkyl group Chemical group 0.000 claims 30
- 125000000623 heterocyclic group Chemical group 0.000 claims 27
- 125000003118 aryl group Chemical group 0.000 claims 24
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 24
- 125000001072 heteroaryl group Chemical group 0.000 claims 22
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical group [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 17
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 16
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 15
- 125000000217 alkyl group Chemical group 0.000 claims 14
- 125000001188 haloalkyl group Chemical group 0.000 claims 13
- 125000003342 alkenyl group Chemical group 0.000 claims 11
- 125000000304 alkynyl group Chemical group 0.000 claims 11
- 102000009058 Death Domain Receptors Human genes 0.000 claims 7
- 108010049207 Death Domain Receptors Proteins 0.000 claims 7
- 239000003814 drug Substances 0.000 claims 6
- 101100369992 Homo sapiens TNFSF10 gene Proteins 0.000 claims 5
- 102000046283 TNF-Related Apoptosis-Inducing Ligand Human genes 0.000 claims 5
- 108700012411 TNFSF10 Proteins 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 239000003607 modifier Substances 0.000 claims 5
- 230000002062 proliferating effect Effects 0.000 claims 5
- 229940044601 receptor agonist Drugs 0.000 claims 5
- 239000000018 receptor agonist Substances 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 239000007801 affinity label Substances 0.000 claims 2
- 239000000556 agonist Substances 0.000 claims 2
- 230000006907 apoptotic process Effects 0.000 claims 2
- 235000010290 biphenyl Nutrition 0.000 claims 2
- 239000004305 biphenyl Substances 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N phenylbenzene Natural products C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 102100032187 Androgen receptor Human genes 0.000 claims 1
- 102000004127 Cytokines Human genes 0.000 claims 1
- 108090000695 Cytokines Proteins 0.000 claims 1
- 102100038595 Estrogen receptor Human genes 0.000 claims 1
- 229940122440 HIV protease inhibitor Drugs 0.000 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- 102000006992 Interferon-alpha Human genes 0.000 claims 1
- 108010047761 Interferon-alpha Proteins 0.000 claims 1
- 102000015696 Interleukins Human genes 0.000 claims 1
- 229940113306 Ligase inhibitor Drugs 0.000 claims 1
- 108010016731 PPAR gamma Proteins 0.000 claims 1
- 229940122054 Peroxisome proliferator-activated receptor delta agonist Drugs 0.000 claims 1
- 102100038825 Peroxisome proliferator-activated receptor gamma Human genes 0.000 claims 1
- 102000004245 Proteasome Endopeptidase Complex Human genes 0.000 claims 1
- 108090000708 Proteasome Endopeptidase Complex Proteins 0.000 claims 1
- 229940079156 Proteasome inhibitor Drugs 0.000 claims 1
- 229940123468 Transferase inhibitor Drugs 0.000 claims 1
- 108060008683 Tumor Necrosis Factor Receptor Proteins 0.000 claims 1
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 claims 1
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 claims 1
- 108010080146 androgen receptors Proteins 0.000 claims 1
- 208000007502 anemia Diseases 0.000 claims 1
- 239000004037 angiogenesis inhibitor Substances 0.000 claims 1
- 229940121369 angiogenesis inhibitor Drugs 0.000 claims 1
- 230000003474 anti-emetic effect Effects 0.000 claims 1
- 230000001028 anti-proliverative effect Effects 0.000 claims 1
- 229940125683 antiemetic agent Drugs 0.000 claims 1
- 239000002111 antiemetic agent Substances 0.000 claims 1
- 244000052616 bacterial pathogen Species 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 230000037012 chymotrypsin-like activity Effects 0.000 claims 1
- 239000002254 cytotoxic agent Substances 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 231100000599 cytotoxic agent Toxicity 0.000 claims 1
- 108010038795 estrogen receptors Proteins 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 229940121372 histone deacetylase inhibitor Drugs 0.000 claims 1
- 239000003276 histone deacetylase inhibitor Substances 0.000 claims 1
- 239000004030 hiv protease inhibitor Substances 0.000 claims 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 1
- 210000000987 immune system Anatomy 0.000 claims 1
- 230000000091 immunopotentiator Effects 0.000 claims 1
- 108010093036 interleukin receptors Proteins 0.000 claims 1
- 230000005865 ionizing radiation Effects 0.000 claims 1
- 239000003446 ligand Substances 0.000 claims 1
- 239000000436 ligase inhibitor Substances 0.000 claims 1
- 229950001869 mapatumumab Drugs 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000036457 multidrug resistance Effects 0.000 claims 1
- 208000004235 neutropenia Diseases 0.000 claims 1
- 239000003207 proteasome inhibitor Substances 0.000 claims 1
- 102000027483 retinoid hormone receptors Human genes 0.000 claims 1
- 108091008679 retinoid hormone receptors Proteins 0.000 claims 1
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 230000002195 synergetic effect Effects 0.000 claims 1
- 239000003558 transferase inhibitor Substances 0.000 claims 1
- 102000003298 tumor necrosis factor receptor Human genes 0.000 claims 1
- 0 C*(C)NC(N*C1CC1)=O Chemical compound C*(C)NC(N*C1CC1)=O 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US72972705P | 2005-10-25 | 2005-10-25 | |
| US83066206P | 2006-07-14 | 2006-07-14 | |
| PCT/CA2006/001721 WO2007048224A1 (en) | 2005-10-25 | 2006-10-20 | Iap bir domain binding compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009512719A JP2009512719A (ja) | 2009-03-26 |
| JP2009512719A5 true JP2009512719A5 (https=) | 2009-12-03 |
Family
ID=37965208
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008536890A Pending JP2009512719A (ja) | 2005-10-25 | 2006-10-20 | Iapbirドメイン結合化合物 |
Country Status (10)
| Country | Link |
|---|---|
| US (4) | US7589118B2 (https=) |
| EP (1) | EP1951698A4 (https=) |
| JP (1) | JP2009512719A (https=) |
| KR (1) | KR20080067357A (https=) |
| AU (1) | AU2006308453B9 (https=) |
| BR (1) | BRPI0617751A2 (https=) |
| CA (1) | CA2564872C (https=) |
| IL (1) | IL190936A0 (https=) |
| RU (1) | RU2418807C2 (https=) |
| WO (1) | WO2007048224A1 (https=) |
Families Citing this family (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2475207T3 (es) | 2004-07-15 | 2014-07-10 | Tetralogic Pharmaceuticals Corporation | Compuestos de unión a IAP |
| DK1836201T4 (da) | 2004-12-20 | 2013-11-11 | Genentech Inc | Pyrrolidininhibitorer af IAP. |
| MX2007010371A (es) * | 2005-02-25 | 2008-01-11 | Tetralogic Pharmaceuticals | Inhibidores dimericos iap. |
| 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 |
| WO2007048224A1 (en) * | 2005-10-25 | 2007-05-03 | Aegera Therapeutics Inc. | Iap bir domain binding compounds |
| CN101374829A (zh) | 2005-12-19 | 2009-02-25 | 健泰科生物技术公司 | Iap的抑制剂 |
| 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 |
| US7807699B2 (en) * | 2006-03-21 | 2010-10-05 | Joyant Pharmaceuticals, Inc. | Dimeric pyrrolidine amide-containing small molecule apoptosis promoters |
| CN101535300B (zh) | 2006-05-16 | 2014-05-28 | 埃格拉医疗公司 | Iap bir域结合化合物 |
| 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 |
| WO2008014240A2 (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. |
| 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 |
| US20100056495A1 (en) * | 2006-07-24 | 2010-03-04 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| WO2008134679A1 (en) * | 2007-04-30 | 2008-11-06 | Genentech, Inc. | Inhibitors of iap |
| 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 |
| US20100203012A1 (en) * | 2007-05-30 | 2010-08-12 | Aegera Therapeutics, Inc. | Iap bir domain binding compounds |
| US20120141496A1 (en) * | 2007-12-17 | 2012-06-07 | Aegera Therapeutics, Inc. | Iap bir domain binding compounds |
| AU2009203971A1 (en) * | 2008-01-11 | 2009-07-16 | Genentech, Inc. | Inhibitors of IAP |
| WO2009136290A1 (en) * | 2008-05-05 | 2009-11-12 | Aegera Therapeutics, Inc. | Functionalized pyrrolidines and use thereof as iap inhibitors |
| AU2009261919A1 (en) * | 2008-06-27 | 2009-12-30 | Pharmascience Inc. | Bridged secondary amines and use thereof as IAP BIR domain binding compounds |
| JP2011529962A (ja) * | 2008-08-02 | 2011-12-15 | ジェネンテック, インコーポレイテッド | Iapのインヒビター |
| US20100317593A1 (en) * | 2009-06-12 | 2010-12-16 | Astrazeneca Ab | 2,3-dihydro-1h-indene compounds |
| US8283372B2 (en) | 2009-07-02 | 2012-10-09 | Tetralogic Pharmaceuticals Corp. | 2-(1H-indol-3-ylmethyl)-pyrrolidine dimer as a SMAC mimetic |
| US8779280B2 (en) * | 2009-08-18 | 2014-07-15 | Lg Electronics Inc. | Solar cell and method of manufacturing the same |
| US8551955B2 (en) | 2009-10-28 | 2013-10-08 | Joyant Pharmaceuticals, Inc. | Dimeric Smac mimetics |
| US9284350B2 (en) | 2010-02-12 | 2016-03-15 | Pharmascience Inc. | IAP BIR domain binding compounds |
| UY33236A (es) * | 2010-02-25 | 2011-09-30 | Novartis Ag | Inhibidores dimericos de las iap |
| US8263578B2 (en) | 2010-03-18 | 2012-09-11 | Innopharma, Inc. | Stable bortezomib formulations |
| AU2011227083B2 (en) * | 2010-03-18 | 2013-07-18 | Innopharma, Inc. | Stable bortezomib formulations |
| UY33794A (es) | 2010-12-13 | 2012-07-31 | Novartis Ag | Inhibidores diméricos de las iap |
| US20140243276A1 (en) | 2011-09-30 | 2014-08-28 | Tetralogic Pharmaceuticals Corporation | Smac mimetic (birinapant) for use in the treatment of proliferative diseases (cancer) |
| KR20160030099A (ko) | 2013-06-25 | 2016-03-16 | 더 월터 앤드 엘리자 홀 인스티튜트 오브 메디컬 리서치 | 세포내 감염의 치료 방법 |
| 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 |
| WO2016079527A1 (en) | 2014-11-19 | 2016-05-26 | Tetralogic Birinapant Uk Ltd | Combination therapy |
| WO2016097773A1 (en) | 2014-12-19 | 2016-06-23 | Children's Cancer Institute | Therapeutic iap antagonists for treating proliferative disorders |
| WO2020027225A1 (ja) | 2018-07-31 | 2020-02-06 | ファイメクス株式会社 | 複素環化合物 |
| CN113677399B (zh) * | 2019-04-05 | 2024-10-11 | 和博医药有限公司 | 凋亡蛋白抑制剂的二价拮抗剂 |
| JP7764027B2 (ja) | 2019-07-31 | 2025-11-05 | ファイメクス株式会社 | 複素環化合物 |
| WO2021148396A1 (en) | 2020-01-20 | 2021-07-29 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
| CN119677743A (zh) * | 2023-02-08 | 2025-03-21 | 成都先导药物开发股份有限公司 | 杂环化合物及其用途 |
| KR102848239B1 (ko) * | 2023-04-13 | 2025-08-19 | 성신여자대학교 연구 산학협력단 | 비천연 아미노산을 포함하는 htra 표적 테트라펩타이드 프로브 |
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| US20100143499A1 (en) | 2006-07-24 | 2010-06-10 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
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| NZ577150A (en) | 2006-12-19 | 2012-04-27 | Genentech Inc | Imidazopyridine inhibitors of iap |
| JP5454943B2 (ja) | 2007-04-12 | 2014-03-26 | ジョイアント ファーマスーティカルズ、インク. | 抗癌剤として有用なsmac模倣二量体及び三量体 |
| WO2008128171A2 (en) | 2007-04-13 | 2008-10-23 | The Regents Of The University Of Michigan | Diazo bicyclic smac mimetics and the uses thereof |
| WO2008134679A1 (en) | 2007-04-30 | 2008-11-06 | Genentech, Inc. | Inhibitors of iap |
| US20100203012A1 (en) | 2007-05-30 | 2010-08-12 | Aegera Therapeutics, Inc. | Iap bir domain binding compounds |
| EP2058312A1 (en) | 2007-11-09 | 2009-05-13 | Universita' degli Studi di Milano | SMAC mimetic compounds as apoptosis inducers |
| WO2009136290A1 (en) | 2008-05-05 | 2009-11-12 | Aegera Therapeutics, Inc. | Functionalized pyrrolidines and use thereof as iap inhibitors |
| CN102099035A (zh) | 2008-05-16 | 2011-06-15 | 诺瓦提斯公司 | Iap抑制剂的免疫调节 |
| TW201011006A (en) | 2008-06-16 | 2010-03-16 | Nuevolution As | IAP binding compounds |
| AU2009261919A1 (en) | 2008-06-27 | 2009-12-30 | Pharmascience Inc. | Bridged secondary amines and use thereof as IAP BIR domain binding compounds |
| JP2011529962A (ja) | 2008-08-02 | 2011-12-15 | ジェネンテック, インコーポレイテッド | Iapのインヒビター |
| US20120009141A1 (en) | 2008-08-07 | 2012-01-12 | Pharmascience Inc. | Functionalized pyrrolidines and use thereof as iap inhibitors |
| WO2010033531A1 (en) | 2008-09-17 | 2010-03-25 | Tetralogic Pharmaceuticals Corp. | Iap inhibitors |
| US20110177060A1 (en) | 2008-09-19 | 2011-07-21 | Aegera Therapeutics, Inc. | Iap bir domain binding compounds |
-
2006
- 2006-10-20 WO PCT/CA2006/001721 patent/WO2007048224A1/en not_active Ceased
- 2006-10-20 RU RU2008120408/04A patent/RU2418807C2/ru not_active IP Right Cessation
- 2006-10-20 AU AU2006308453A patent/AU2006308453B9/en not_active Ceased
- 2006-10-20 JP JP2008536890A patent/JP2009512719A/ja active Pending
- 2006-10-20 KR KR1020087012374A patent/KR20080067357A/ko not_active Withdrawn
- 2006-10-20 EP EP06790872A patent/EP1951698A4/en not_active Withdrawn
- 2006-10-20 BR BRPI0617751-4A patent/BRPI0617751A2/pt not_active IP Right Cessation
- 2006-10-20 CA CA2564872A patent/CA2564872C/en not_active Expired - Fee Related
- 2006-10-20 US US11/583,816 patent/US7589118B2/en not_active Expired - Fee Related
- 2006-12-01 US US11/606,883 patent/US7547724B2/en not_active Expired - Fee Related
- 2006-12-04 US US11/607,998 patent/US7795298B2/en not_active Expired - Fee Related
- 2006-12-04 US US11/607,964 patent/US8063095B2/en not_active Expired - Fee Related
-
2008
- 2008-04-17 IL IL190936A patent/IL190936A0/en unknown
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