JP2011506494A5 - - Google Patents
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- Publication number
- JP2011506494A5 JP2011506494A5 JP2010538297A JP2010538297A JP2011506494A5 JP 2011506494 A5 JP2011506494 A5 JP 2011506494A5 JP 2010538297 A JP2010538297 A JP 2010538297A JP 2010538297 A JP2010538297 A JP 2010538297A JP 2011506494 A5 JP2011506494 A5 JP 2011506494A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- optionally substituted
- phenyl
- halogen
- 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- Withdrawn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
- 125000000217 alkyl group Chemical group 0.000 claims 99
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 78
- 229910052736 halogen Inorganic materials 0.000 claims 61
- 150000002367 halogens Chemical group 0.000 claims 60
- 125000001424 substituent group Chemical group 0.000 claims 47
- -1 hydroxy, nitro, cyano, amino, phenyl Chemical group 0.000 claims 37
- 150000001875 compounds Chemical class 0.000 claims 32
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 30
- 125000004663 dialkyl amino group Chemical group 0.000 claims 30
- 125000001072 heteroaryl group Chemical group 0.000 claims 24
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 23
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 23
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 22
- 125000004093 cyano group Chemical group *C#N 0.000 claims 22
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 21
- 125000001188 haloalkyl group Chemical group 0.000 claims 20
- 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 20
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 19
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 18
- 125000003545 alkoxy group Chemical group 0.000 claims 17
- 125000003282 alkyl amino group Chemical group 0.000 claims 15
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 14
- 125000004438 haloalkoxy group Chemical group 0.000 claims 14
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims 13
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 12
- 125000004103 aminoalkyl group Chemical group 0.000 claims 12
- 125000001931 aliphatic group Chemical group 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- 125000006677 (C1-C3) haloalkoxy group Chemical group 0.000 claims 10
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 10
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 10
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 9
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 9
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 8
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 8
- 229910052799 carbon Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 125000004076 pyridyl group Chemical group 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 6
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 5
- 125000006708 (C5-C14) heteroaryl group Chemical group 0.000 claims 5
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 5
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims 4
- 125000000168 pyrrolyl group Chemical group 0.000 claims 4
- 125000000335 thiazolyl group Chemical group 0.000 claims 4
- 125000001544 thienyl group Chemical group 0.000 claims 4
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 125000004450 alkenylene group Chemical group 0.000 claims 3
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 125000004970 halomethyl group Chemical group 0.000 claims 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 125000005915 C6-C14 aryl group Chemical group 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000021309 Germ cell tumor Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 201000010915 Glioblastoma multiforme Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010027406 Mesothelioma Diseases 0.000 claims 1
- 208000034176 Neoplasms, Germ Cell and Embryonal Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- VEQOALNAAJBPNY-UHFFFAOYSA-N antipyrine Chemical group CN1C(C)=CC(=O)N1C1=CC=CC=C1 VEQOALNAAJBPNY-UHFFFAOYSA-N 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- VKYKSIONXSXAKP-UHFFFAOYSA-N hexamethylenetetramine Chemical compound C1N(C2)CN3CN1CN2C3 VKYKSIONXSXAKP-UHFFFAOYSA-N 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229960005222 phenazone Drugs 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 0 *N(C(CCCCCC1)=C1C1=*c2cc(***3)c3cc2)C1=O Chemical compound *N(C(CCCCCC1)=C1C1=*c2cc(***3)c3cc2)C1=O 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US886507P | 2007-12-21 | 2007-12-21 | |
| US13171708P | 2008-06-11 | 2008-06-11 | |
| PCT/CA2008/002227 WO2009079767A1 (en) | 2007-12-21 | 2008-12-19 | Indazolyl, benzimidazolyl, benzotriazolyl substituted indolinone derivatives as kinase inhibitors useful in the treatment of cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011506494A JP2011506494A (ja) | 2011-03-03 |
| JP2011506494A5 true JP2011506494A5 (enExample) | 2012-02-16 |
Family
ID=40800609
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010538297A Withdrawn JP2011506494A (ja) | 2007-12-21 | 2008-12-19 | 癌の治療に有用なキナーゼ阻害剤としてのインダゾリル、ベンズイミダゾリル、ベンゾトリアゾリル置換インドルモン誘導体 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US8765748B2 (enExample) |
| EP (1) | EP2235004A4 (enExample) |
| JP (1) | JP2011506494A (enExample) |
| CN (1) | CN101970426A (enExample) |
| AU (1) | AU2008340991B2 (enExample) |
| CA (1) | CA2709536C (enExample) |
| WO (1) | WO2009079767A1 (enExample) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2011506494A (ja) | 2007-12-21 | 2011-03-03 | ユニバーシティ・ヘルス・ネットワーク | 癌の治療に有用なキナーゼ阻害剤としてのインダゾリル、ベンズイミダゾリル、ベンゾトリアゾリル置換インドルモン誘導体 |
| CA2756568C (en) | 2009-04-06 | 2018-02-13 | University Health Network | Kinase inhibitors and method of treating cancer with same |
| PT2556071T (pt) | 2010-04-06 | 2016-11-22 | Univ Health Network | Inibidores de quinase e seus usos no tratamento de cancro |
| US8933070B2 (en) | 2010-07-02 | 2015-01-13 | University Health Network | Methods of targeting PTEN mutant diseases and compositions therefor |
| WO2012048411A1 (en) * | 2010-10-13 | 2012-04-19 | University Health Network | Plk-4 inhibitors and method of treating cancer with same |
| CN102295640B (zh) * | 2011-06-29 | 2013-09-18 | 南京工业大学 | 3-杂环席夫碱-5-氟-吲哚-2-酮类化合物及其制备方法和应用 |
| CN103006642B (zh) * | 2013-01-04 | 2014-10-22 | 中国药科大学 | 一类炔亚甲基吲哚-2-酮类衍生物的用途 |
| JP2016533350A (ja) | 2013-10-04 | 2016-10-27 | バイエル・クロップサイエンス・アクチェンゲゼルシャフト | 植物のストレス耐性を増大させるための置換されているジヒドロオキシインドリルスルホンアミド類又はその塩の使用 |
| PT3057965T (pt) | 2013-10-18 | 2019-04-23 | Univ Health Network | Formas de sal e cristal de inibidor de plk-4 |
| JP6525983B2 (ja) | 2013-10-18 | 2019-06-05 | ユニバーシティー ヘルス ネットワーク | 膵癌の治療法 |
| WO2015164956A1 (en) * | 2014-04-29 | 2015-11-05 | The University Of British Columbia | Benzisothiazole derivative compounds as therapeutics and methods for their use |
| US10633375B2 (en) | 2016-08-31 | 2020-04-28 | Jinagsu Hengrui Medicine Co., Ltd | Oxopicolinamide derivative, preparation method therefor and pharmaceutical use thereof |
| CN106916143B (zh) * | 2017-03-14 | 2019-09-27 | 哈尔滨医科大学 | 一种预防和治疗冠心病的药物及其应用 |
| BR112021021106A2 (pt) | 2019-04-24 | 2021-12-14 | Univ Health Network | Forma cristalina s4 do inibidor plk4 fumarato (ir,2s)-(e)-2-(3-(4-((cis-2,6-dimetilmorfolino)metil)estiril)-1h-imidazol-6-il)-5'-metoxiespiro[ciclopropano-1,3'-indolin]-2'ona |
| TW202300485A (zh) * | 2021-03-02 | 2023-01-01 | 大陸商上海齊魯製藥研究中心有限公司 | Plk4抑制劑及其用途 |
| IL308346A (en) | 2021-05-11 | 2024-01-01 | Oric Pharmaceuticals Inc | Polo like kinase 4 inhibitors |
| WO2024209363A1 (en) | 2023-04-06 | 2024-10-10 | Pfizer Inc. | Substituted indazole propionic acid derivative compounds and uses thereof as ampk activators |
| ES3022196A1 (es) * | 2023-11-27 | 2025-05-28 | Univ Madrid Complutense | Derivados de 2-indolinona y usos de los mismos |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US1326A (en) * | 1839-09-17 | Improvement in the mode of setting and arranging sugar-kettles | ||
| DE3310891A1 (de) * | 1983-03-25 | 1984-09-27 | Boehringer Mannheim Gmbh, 6800 Mannheim | Neue indolinon-(2)-derivate, verfahren zu ihrer herstellung, diese verbindungen enthaltende arzneimittel und zwischenprodukte |
| US5182397A (en) * | 1990-05-31 | 1993-01-26 | American Cyanamid Company | Aryloxyspiroalkylindolinone herbicides |
| GB9507298D0 (en) | 1995-04-07 | 1995-05-31 | Pharmacia Spa | Substituted indolylmethylene-oxindale analogues as tyrosine kinase inhibitors |
| US5880141A (en) | 1995-06-07 | 1999-03-09 | Sugen, Inc. | Benzylidene-Z-indoline compounds for the treatment of disease |
| ATE308520T1 (de) * | 1996-08-23 | 2005-11-15 | Sugen Inc | Kombinatorische bibliotheken von indolinone und verwandte produkte und verfahren zur behandlung von krankheiten |
| GB9716557D0 (en) | 1997-08-06 | 1997-10-08 | Glaxo Group Ltd | Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity |
| US6133305A (en) * | 1997-09-26 | 2000-10-17 | Sugen, Inc. | 3-(substituted)-2-indolinones compounds and use thereof as inhibitors of protein kinase activity |
| AU5468499A (en) * | 1998-08-04 | 2000-02-28 | Sugen, Inc. | 3-methylidenyl-2-indolinone modulators of protein kinase |
| EP1165513A1 (en) | 1999-03-24 | 2002-01-02 | Sugen, Inc. | Indolinone compounds as kinase inhibitors |
| US7148249B2 (en) | 2002-09-12 | 2006-12-12 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Indolinones substituted by heterocycles, the preparation thereof and their use as medicaments |
| US7205328B2 (en) * | 2002-10-21 | 2007-04-17 | Irm Llc | Oxindoles with anti-HIV activity |
| WO2005058309A1 (en) * | 2003-12-16 | 2005-06-30 | Leo Pharma A/S | Novel therapeutic use of indolinone derivatives |
| US7309787B2 (en) | 2005-07-13 | 2007-12-18 | Allergan, Inc. | Kinase inhibitors |
| US20070135509A1 (en) * | 2005-12-09 | 2007-06-14 | Blackburn Thomas P | Indolone compounds useful to treat cognitive impairment |
| US8207179B2 (en) | 2007-06-12 | 2012-06-26 | Boehringer Ingelheim International Gmbh | Substituted indolines as tyrosine kinase inhibitors |
| JP2011506494A (ja) | 2007-12-21 | 2011-03-03 | ユニバーシティ・ヘルス・ネットワーク | 癌の治療に有用なキナーゼ阻害剤としてのインダゾリル、ベンズイミダゾリル、ベンゾトリアゾリル置換インドルモン誘導体 |
| EP2108641A1 (en) | 2008-04-11 | 2009-10-14 | Laboratorios Almirall, S.A. | New substituted spiro[cycloalkyl-1,3'-indo]-2'(1'H)-one derivatives and their use as p38 mitogen-activated kinase inhibitors |
| EP2113503A1 (en) | 2008-04-28 | 2009-11-04 | Laboratorios Almirall, S.A. | New substituted indolin-2-one derivatives and their use as p39 mitogen-activated kinase inhibitors |
| CA2756568C (en) | 2009-04-06 | 2018-02-13 | University Health Network | Kinase inhibitors and method of treating cancer with same |
| PT2556071T (pt) * | 2010-04-06 | 2016-11-22 | Univ Health Network | Inibidores de quinase e seus usos no tratamento de cancro |
-
2008
- 2008-12-19 JP JP2010538297A patent/JP2011506494A/ja not_active Withdrawn
- 2008-12-19 US US12/808,961 patent/US8765748B2/en active Active
- 2008-12-19 CN CN2008801272472A patent/CN101970426A/zh active Pending
- 2008-12-19 EP EP08865534A patent/EP2235004A4/en not_active Withdrawn
- 2008-12-19 AU AU2008340991A patent/AU2008340991B2/en not_active Ceased
- 2008-12-19 CA CA2709536A patent/CA2709536C/en active Active
- 2008-12-19 WO PCT/CA2008/002227 patent/WO2009079767A1/en not_active Ceased
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