JP2008520719A5 - - Google Patents
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- Publication number
- JP2008520719A5 JP2008520719A5 JP2007543334A JP2007543334A JP2008520719A5 JP 2008520719 A5 JP2008520719 A5 JP 2008520719A5 JP 2007543334 A JP2007543334 A JP 2007543334A JP 2007543334 A JP2007543334 A JP 2007543334A JP 2008520719 A5 JP2008520719 A5 JP 2008520719A5
- Authority
- JP
- Japan
- Prior art keywords
- alkylamino
- hydrogen
- aryl
- alkoxy
- amino
- 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.)
- Withdrawn
Links
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 131
- 229910052739 hydrogen Inorganic materials 0.000 claims 124
- 239000001257 hydrogen Substances 0.000 claims 122
- 125000003118 aryl group Chemical group 0.000 claims 93
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 82
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 79
- 125000001072 heteroaryl group Chemical group 0.000 claims 77
- 150000001875 compounds Chemical class 0.000 claims 69
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 67
- 125000000623 heterocyclic group Chemical group 0.000 claims 61
- 150000002431 hydrogen Chemical group 0.000 claims 54
- 125000005843 halogen group Chemical group 0.000 claims 52
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 43
- -1 amino, hydroxy Chemical group 0.000 claims 34
- 125000004093 cyano group Chemical group *C#N 0.000 claims 34
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 34
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 33
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 32
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 24
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 24
- 239000000203 mixture Substances 0.000 claims 15
- 239000012453 solvate Substances 0.000 claims 15
- 125000004404 heteroalkyl group Chemical group 0.000 claims 13
- 150000004677 hydrates Chemical class 0.000 claims 13
- SYSQUGFVNFXIIT-UHFFFAOYSA-N n-[4-(1,3-benzoxazol-2-yl)phenyl]-4-nitrobenzenesulfonamide Chemical class C1=CC([N+](=O)[O-])=CC=C1S(=O)(=O)NC1=CC=C(C=2OC3=CC=CC=C3N=2)C=C1 SYSQUGFVNFXIIT-UHFFFAOYSA-N 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 13
- 206010021143 Hypoxia Diseases 0.000 claims 12
- 125000006727 (C1-C6) alkenyl group Chemical group 0.000 claims 11
- 125000006728 (C1-C6) alkynyl group Chemical group 0.000 claims 11
- 230000007954 hypoxia Effects 0.000 claims 11
- 239000012190 activator Substances 0.000 claims 9
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 9
- 125000003435 aroyl group Chemical group 0.000 claims 8
- 229910052736 halogen Chemical group 0.000 claims 5
- 150000002367 halogens Chemical group 0.000 claims 5
- 150000002772 monosaccharides Chemical class 0.000 claims 5
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 4
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 4
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000004682 aminothiocarbonyl group Chemical group NC(=S)* 0.000 claims 4
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 4
- 125000001153 fluoro group Chemical group F* 0.000 claims 4
- 239000000651 prodrug Substances 0.000 claims 4
- 229940002612 prodrug Drugs 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- YZEUHQHUFTYLPH-UHFFFAOYSA-N 2-nitroimidazole Chemical group [O-][N+](=O)C1=NC=CN1 YZEUHQHUFTYLPH-UHFFFAOYSA-N 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 230000007717 exclusion Effects 0.000 claims 2
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 2
- 230000003463 hyperproliferative effect Effects 0.000 claims 2
- 125000001483 monosaccharide substituent group Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 230000006553 hypoxic activation Effects 0.000 claims 1
- 230000001146 hypoxic effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 0 CCC1[C@@](**2(C)CCCC2)C1 Chemical compound CCC1[C@@](**2(C)CCCC2)C1 0.000 description 8
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63042204P | 2004-11-22 | 2004-11-22 | |
| US72692805P | 2005-10-14 | 2005-10-14 | |
| PCT/US2005/042095 WO2006057946A2 (en) | 2004-11-22 | 2005-11-17 | Tubulin binding anti cancer agents and prodrugs thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008520719A JP2008520719A (ja) | 2008-06-19 |
| JP2008520719A5 true JP2008520719A5 (OSRAM) | 2009-01-22 |
Family
ID=36498450
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007543334A Withdrawn JP2008520719A (ja) | 2004-11-22 | 2005-11-17 | チューブリン結合抗癌剤およびそれらのプロドラッグ |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20090042820A1 (OSRAM) |
| EP (1) | EP1819338A4 (OSRAM) |
| JP (1) | JP2008520719A (OSRAM) |
| KR (1) | KR20070086595A (OSRAM) |
| AU (1) | AU2005309761A1 (OSRAM) |
| CA (1) | CA2587210A1 (OSRAM) |
| IL (1) | IL183212A0 (OSRAM) |
| MX (1) | MX2007006102A (OSRAM) |
| NO (1) | NO20073211L (OSRAM) |
| WO (1) | WO2006057946A2 (OSRAM) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA200507752B (en) | 2003-03-28 | 2007-01-31 | Threshold Pharmaceuticals Inc | Compositions and methods for treating cancer |
| CA2613312C (en) | 2005-06-29 | 2014-10-14 | Threshold Pharmaceuticals, Inc. | Phosphoramidate alkylator prodrugs |
| KR20090025367A (ko) * | 2006-06-28 | 2009-03-10 | 가부시키가이샤산와카가쿠켄큐쇼 | 신규 6-5계 이환식 복소환 유도체 및 그 의약용도 |
| US8552048B2 (en) | 2006-12-26 | 2013-10-08 | Threshold Pharmaceuticals, Inc. | Phosphoramidate alkylator prodrugs for the treatment of cancer |
| WO2008124691A1 (en) | 2007-04-05 | 2008-10-16 | Threshold Pharmaceuticals, Inc. | Glufosfamide combination therapy |
| WO2008151253A1 (en) * | 2007-06-04 | 2008-12-11 | Threshold Pharmaceuticals, Inc. | Hypoxia activated prodrugs of antineoplastic agents |
| EP2350664B1 (en) | 2008-10-21 | 2021-05-19 | ImmunoGenesis, Inc. | Treatment of cancer using the hypoxia activated prodrug th-302 in combination with docetaxel or pemetrexed |
| FR2962437B1 (fr) * | 2010-07-06 | 2012-08-17 | Sanofi Aventis | Derives d'imidazopyridine, leur procede de preparation et leur application en therapeutique |
| US9487506B2 (en) | 2011-04-13 | 2016-11-08 | Merck Sharp & Dohme Corp. | Mineralocorticoid receptor antagonists |
| US10037382B2 (en) | 2012-10-29 | 2018-07-31 | Kyocera Corporation | Surface acoustic wave sensor |
| WO2015048553A1 (en) * | 2013-09-27 | 2015-04-02 | Allergan, Inc. | Compounds and methods for skin repair |
| TWI720451B (zh) | 2014-02-13 | 2021-03-01 | 美商英塞特控股公司 | 作為lsd1抑制劑之環丙胺 |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| KR102421235B1 (ko) | 2014-02-13 | 2022-07-15 | 인사이트 코포레이션 | Lsd1 저해제로서 사이클로프로필아민 |
| US9493442B2 (en) | 2014-02-13 | 2016-11-15 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| TWI687419B (zh) | 2014-07-10 | 2020-03-11 | 美商英塞特公司 | 作為ｌｓｄ１抑制劑之咪唑并吡啶及咪唑并吡嗪 |
| US9758523B2 (en) | 2014-07-10 | 2017-09-12 | Incyte Corporation | Triazolopyridines and triazolopyrazines as LSD1 inhibitors |
| TW201613925A (en) | 2014-07-10 | 2016-04-16 | Incyte Corp | Imidazopyrazines as LSD1 inhibitors |
| US10131683B2 (en) | 2014-07-17 | 2018-11-20 | Molecular Templates, Inc. | TH-302 solid forms and methods related thereto |
| ES2896960T3 (es) | 2015-03-10 | 2022-02-28 | Obi Pharma Inc | Agentes alquilantes del ADN para su uso en el tratamiento del cáncer |
| CN112142692A (zh) * | 2015-04-02 | 2020-12-29 | 深圳艾欣达伟医药科技有限公司 | 硝基苄基衍生物抗癌试剂 |
| SG11201708047UA (en) | 2015-04-03 | 2017-10-30 | Incyte Corp | Heterocyclic compounds as lsd1 inhibitors |
| JP7327900B2 (ja) | 2015-06-24 | 2023-08-16 | スレッシュホールド ファーマシューティカルズ， インコーポレイテッド | アジリジン含有ｄｎａアルキル化剤 |
| CN110402244B (zh) | 2015-08-12 | 2023-02-03 | 因赛特公司 | Lsd1抑制剂的盐 |
| SG10202010414QA (en) | 2016-04-22 | 2020-11-27 | Incyte Corp | Formulations of an lsd1 inhibitor |
| WO2020047198A1 (en) | 2018-08-31 | 2020-03-05 | Incyte Corporation | Salts of an lsd1 inhibitor and processes for preparing the same |
| WO2020079652A1 (en) * | 2018-10-17 | 2020-04-23 | Insilico Medicine Hong Kong Limited | Kinase inhibitors |
| CN115403483B (zh) * | 2021-07-02 | 2024-01-26 | 河南省儿童医院郑州儿童医院 | 含二苯乙烯或二苯甲酮骨架的ca-4衍生物、药物组合物及其制备方法和应用 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004099139A1 (en) * | 2000-09-15 | 2004-11-18 | Baylor University | Indole-containing compounds with anti-tubulin and vascular targeting activity |
| WO2001068654A2 (en) * | 2000-03-10 | 2001-09-20 | Baylor University | Tubulin binding ligands and corresponding prodrug constructs |
| FR2816938B1 (fr) * | 2000-11-22 | 2003-01-03 | Sanofi Synthelabo | Derives de 3-aroylindole, leur procede de preparation et les compositions pharmaceutiques en contenant |
| FR2838123B1 (fr) * | 2002-04-04 | 2005-06-10 | Sanofi Synthelabo | Nouveaux derives d'indolozine-1,2,3 substituee, inhibiteurs selectifs du b-fgf |
| FR2839718B1 (fr) * | 2002-05-17 | 2004-06-25 | Sanofi Synthelabo | Derives d'indole, leur procede de preparation et les compositions pharmaceutiques en contenant |
| EP1506960B1 (en) * | 2003-08-07 | 2011-04-06 | National Health Research Institutes | Indole compounds as inhibitors of tubulin polymerisation for the treatment of angiogenesis-related disorders |
| US7456289B2 (en) * | 2004-12-31 | 2008-11-25 | National Health Research Institutes | Anti-tumor compounds |
-
2005
- 2005-11-17 JP JP2007543334A patent/JP2008520719A/ja not_active Withdrawn
- 2005-11-17 WO PCT/US2005/042095 patent/WO2006057946A2/en not_active Ceased
- 2005-11-17 US US11/791,420 patent/US20090042820A1/en not_active Abandoned
- 2005-11-17 AU AU2005309761A patent/AU2005309761A1/en not_active Abandoned
- 2005-11-17 CA CA002587210A patent/CA2587210A1/en not_active Abandoned
- 2005-11-17 EP EP05826480A patent/EP1819338A4/en not_active Withdrawn
- 2005-11-17 MX MX2007006102A patent/MX2007006102A/es not_active Application Discontinuation
- 2005-11-17 KR KR1020077014342A patent/KR20070086595A/ko not_active Withdrawn
-
2007
- 2007-05-15 IL IL183212A patent/IL183212A0/en unknown
- 2007-06-22 NO NO20073211A patent/NO20073211L/no not_active Application Discontinuation
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