JP2013533239A5 - - Google Patents
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- Publication number
- JP2013533239A5 JP2013533239A5 JP2013515921A JP2013515921A JP2013533239A5 JP 2013533239 A5 JP2013533239 A5 JP 2013533239A5 JP 2013515921 A JP2013515921 A JP 2013515921A JP 2013515921 A JP2013515921 A JP 2013515921A JP 2013533239 A5 JP2013533239 A5 JP 2013533239A5
- Authority
- JP
- Japan
- Prior art keywords
- halo
- alkyl
- alkyloxy
- hydroxy
- independently selected
- 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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- 125000005843 halogen group Chemical group 0.000 claims description 91
- 125000001424 substituent group Chemical group 0.000 claims description 69
- 125000004043 oxo group Chemical group O=* 0.000 claims description 51
- 229910052739 hydrogen Inorganic materials 0.000 claims description 49
- 239000001257 hydrogen Substances 0.000 claims description 49
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 43
- -1 aryl C 1-6 alkylthio Chemical group 0.000 claims description 41
- 125000001153 fluoro group Chemical group F* 0.000 claims description 31
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 25
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 10
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 8
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 7
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 7
- CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 claims description 6
- 150000004820 halides Chemical class 0.000 claims description 6
- 125000001972 isopentyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 claims description 6
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 5
- 125000005448 ethoxyethyl group Chemical group [H]C([H])([H])C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims description 5
- 125000005745 ethoxymethyl group Chemical group [H]C([H])([H])C([H])([H])OC([H])([H])* 0.000 claims description 5
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims description 4
- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 claims description 4
- 125000000286 phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims description 4
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 claims 65
- 125000003545 alkoxy group Chemical group 0.000 claims 63
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 42
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 36
- 125000004093 cyano group Chemical group *C#N 0.000 claims 29
- 150000002431 hydrogen Chemical group 0.000 claims 29
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 29
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 28
- 125000004076 pyridyl group Chemical group 0.000 claims 26
- 150000001875 compounds Chemical class 0.000 claims 21
- 125000001624 naphthyl group Chemical group 0.000 claims 20
- 125000002757 morpholinyl group Chemical group 0.000 claims 19
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 18
- 239000005977 Ethylene Substances 0.000 claims 18
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 18
- 125000003118 aryl group Chemical group 0.000 claims 13
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 12
- 125000003282 alkyl amino group Chemical group 0.000 claims 12
- 125000004414 alkyl thio group Chemical group 0.000 claims 12
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 125000000623 heterocyclic group Chemical group 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 4
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 4
- 125000006625 (C3-C8) cycloalkyloxy group Chemical group 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- 125000001769 aryl amino group Chemical group 0.000 claims 4
- 125000005110 aryl thio group Chemical group 0.000 claims 4
- 125000004104 aryloxy group Chemical group 0.000 claims 4
- 125000006310 cycloalkyl amino group Chemical group 0.000 claims 4
- 125000005366 cycloalkylthio group Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000005241 heteroarylamino group Chemical group 0.000 claims 4
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 4
- 125000005368 heteroarylthio group Chemical group 0.000 claims 4
- 125000004468 heterocyclylthio group Chemical group 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 230000002062 proliferating effect Effects 0.000 claims 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 150000001449 anionic compounds Chemical class 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 102000015694 estrogen receptors Human genes 0.000 claims 2
- 108010038795 estrogen receptors Proteins 0.000 claims 2
- 229910001412 inorganic anion Inorganic materials 0.000 claims 2
- 150000002891 organic anions Chemical class 0.000 claims 2
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims 2
- 102000003998 progesterone receptors Human genes 0.000 claims 2
- 108090000468 progesterone receptors Proteins 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 101150029707 ERBB2 gene Proteins 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 1
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 claims 1
- 230000006907 apoptotic process Effects 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 1
- 208000022679 triple-negative breast carcinoma Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US35860910P | 2010-06-25 | 2010-06-25 | |
| EP2010059083 | 2010-06-25 | ||
| US61/358,609 | 2010-06-25 | ||
| EPPCT/EP2010/059083 | 2010-06-25 | ||
| PCT/EP2011/060658 WO2011161256A1 (en) | 2010-06-25 | 2011-06-24 | Beta carboline derivatives useful in the treatment of proliferative disorders |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013533239A JP2013533239A (ja) | 2013-08-22 |
| JP2013533239A5 true JP2013533239A5 (enExample) | 2014-06-26 |
Family
ID=44453837
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013515921A Pending JP2013533239A (ja) | 2010-06-25 | 2011-06-24 | 増殖性疾患の治療に有用なβカルボリン誘導体 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US9168247B2 (enExample) |
| EP (1) | EP2585463A1 (enExample) |
| JP (1) | JP2013533239A (enExample) |
| CA (1) | CA2803697A1 (enExample) |
| WO (1) | WO2011161256A1 (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2968284B1 (en) | 2013-03-14 | 2021-04-21 | Osteoqc Inc. | Alkyl-amine harmine derivatives for promoting bone growth |
| US10092550B2 (en) | 2014-10-21 | 2018-10-09 | Ions Pharmaceutical S.À R.L. | Therapeutic compositions containing curcumin, harmine, and isovanillin components, and methods of use thereof |
| US9907786B2 (en) | 2014-10-21 | 2018-03-06 | Ions Pharmaceutical S.À R.L. | Therapeutic compositions containing harmine and isovanillin components, and methods of use thereof |
| US20160106721A1 (en) | 2014-10-21 | 2016-04-21 | Life Plus, LLC | Human therapeutic agents |
| CN104530043B (zh) * | 2014-12-03 | 2017-06-06 | 西北农林科技大学 | 9‑取代β‑咔啉类化合物及其用于制备预防或治疗肿瘤药物的应用 |
| CN105753860B (zh) * | 2014-12-16 | 2018-03-06 | 兰州大学 | β‑咔啉类生物碱及其在制备抗肿瘤药物中的应用 |
| WO2018119208A1 (en) | 2016-12-22 | 2018-06-28 | Global Blood Therapeutics, Inc. | Histone methyltransferase inhibitors |
| WO2018226998A1 (en) * | 2017-06-09 | 2018-12-13 | Global Blood Therapeutics, Inc. | Azaindole compounds as histone methyltransferase inhibitors |
| EP3717475B1 (en) | 2017-11-20 | 2023-06-07 | Icahn School of Medicine at Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| AU2019205944A1 (en) | 2018-01-05 | 2020-07-09 | Icahn School Of Medicine At Mount Sinai | Method of increasing proliferation of pancreatic beta cells, treatment method, and composition |
| AU2019240065A1 (en) | 2018-03-20 | 2020-09-24 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| US11903949B2 (en) | 2018-08-14 | 2024-02-20 | Ossifi Therapeutics Llc | Fluoro beta-carboline compounds |
| AU2019321434B2 (en) | 2018-08-14 | 2025-05-08 | Ossifi Therapeutics Llc | Pyrrolo - dipyridine compounds |
| US10947253B2 (en) | 2019-08-05 | 2021-03-16 | Ankh Life Sciences Limited | Fused polycyclic dimers |
| US12129265B2 (en) | 2020-07-21 | 2024-10-29 | Ankh Life Sciences Limited | Therapeutic agents and uses thereof |
| CN114644626A (zh) * | 2020-12-18 | 2022-06-21 | 南京施江医药科技有限公司 | 一种苯环类化合物及其应用 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0357122A3 (en) | 1988-08-29 | 1991-10-23 | Duphar International Research B.V | Use of beta-carbolines, their bio-isosteric benzofuran and benzothiophene analogues for the manufacture of a medicament having cytostatic properties |
| IS2334B (is) | 1992-09-08 | 2008-02-15 | Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) | Aspartyl próteasi hemjari af nýjum flokki súlfonamíða |
| US6043358A (en) | 1995-11-01 | 2000-03-28 | Merck & Co., Inc. | Hexahydro-5-imino-1,4-heteroazepine derivatives as inhibitors of nitric oxide synthases |
| GB9718913D0 (en) | 1997-09-05 | 1997-11-12 | Glaxo Group Ltd | Substituted oxindole derivatives |
| DE19807993A1 (de) * | 1998-02-26 | 1999-09-02 | Bayer Ag | Verwendung von ß-Carbolinderivaten zur Bekämpfung von TNF-alpha-abhängigen Krankheiten |
| US6369087B1 (en) | 1999-08-26 | 2002-04-09 | Robert R. Whittle | Alkoxy substituted benzimidazole compounds, pharmaceutical preparations containing the same, and methods of using the same |
| EP1268477B1 (en) | 2000-03-15 | 2010-04-21 | Sanofi-Aventis Deutschland GmbH | Substituted beta-carbolines with ikb-kinase inhibiting activity |
| KR100826817B1 (ko) * | 2000-03-15 | 2008-05-02 | 사노피-아벤티스 도이칠란트 게엠베하 | 치환된 베타-카볼린 |
| CN100503607C (zh) * | 2003-06-02 | 2009-06-24 | 新疆华世丹药物研究有限责任公司 | 去氢骆驼蓬碱衍生物类化合物及其应用 |
| GB0705566D0 (en) * | 2007-03-23 | 2007-05-02 | Univ Dundee | Method of treating learning impairment in down's syndrome subjects |
| WO2008157358A1 (en) * | 2007-06-15 | 2008-12-24 | University Of Medicine And Dentistry Of New Jersey | Methods for treating neoplasia and for identifying compositions useful in such therapy |
| EP2050747A1 (en) * | 2007-10-12 | 2009-04-22 | BioAlliance Pharma | Dimers of harmol or of its derivatives and uses thereof |
| CN101139347B (zh) | 2007-10-15 | 2010-11-24 | 新疆华世丹药物研究有限责任公司 | 去氢骆驼蓬碱衍生物类化合物及其应用 |
| CN101429198B (zh) | 2007-11-09 | 2013-10-23 | 新疆华世丹药物研究有限责任公司 | 去氢骆驼蓬碱衍生物及其应用 |
| EP2151441A1 (en) * | 2008-08-06 | 2010-02-10 | Julius-Maximilians-Universität Würzburg | Beta-carbolin-derivates as substrates for an enzyme |
| JP2012051804A (ja) * | 2008-12-26 | 2012-03-15 | Kyoto Univ | Ｅｇ５阻害剤 |
-
2011
- 2011-06-24 US US13/704,109 patent/US9168247B2/en not_active Expired - Fee Related
- 2011-06-24 EP EP11736303.6A patent/EP2585463A1/en not_active Withdrawn
- 2011-06-24 JP JP2013515921A patent/JP2013533239A/ja active Pending
- 2011-06-24 CA CA2803697A patent/CA2803697A1/en not_active Abandoned
- 2011-06-24 WO PCT/EP2011/060658 patent/WO2011161256A1/en not_active Ceased
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