JP2010522750A5 - - Google Patents
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- JP2010522750A5 JP2010522750A5 JP2010500949A JP2010500949A JP2010522750A5 JP 2010522750 A5 JP2010522750 A5 JP 2010522750A5 JP 2010500949 A JP2010500949 A JP 2010500949A JP 2010500949 A JP2010500949 A JP 2010500949A JP 2010522750 A5 JP2010522750 A5 JP 2010522750A5
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- JP
- Japan
- Prior art keywords
- optionally substituted
- independently
- alkyl
- cycloalkyl
- heteroaryl
- Prior art date
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- -1 guanazino Chemical group 0.000 claims description 123
- 150000001875 compounds Chemical class 0.000 claims description 120
- 125000001072 heteroaryl group Chemical group 0.000 claims description 76
- 125000000623 heterocyclic group Chemical group 0.000 claims description 74
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 62
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 60
- 125000004475 heteroaralkyl group Chemical group 0.000 claims description 56
- 125000003107 substituted aryl group Chemical group 0.000 claims description 52
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 47
- 125000005017 substituted alkenyl group Chemical group 0.000 claims description 44
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 44
- 125000004426 substituted alkynyl group Chemical group 0.000 claims description 44
- 229910052757 nitrogen Inorganic materials 0.000 claims description 39
- 125000000217 alkyl group Chemical group 0.000 claims description 32
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 20
- 125000003118 aryl group Chemical group 0.000 claims description 16
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 15
- 229910052717 sulfur Inorganic materials 0.000 claims description 15
- 206010028980 Neoplasm Diseases 0.000 claims description 14
- 229910052799 carbon Inorganic materials 0.000 claims description 14
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 14
- 125000004432 carbon atom Chemical group C* 0.000 claims description 13
- 150000003839 salts Chemical class 0.000 claims description 13
- 125000003545 alkoxy group Chemical group 0.000 claims description 12
- 125000001188 haloalkyl group Chemical group 0.000 claims description 12
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 12
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 12
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 11
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 11
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 11
- 125000001475 halogen functional group Chemical group 0.000 claims description 11
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 11
- 238000011282 treatment Methods 0.000 claims description 11
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims description 8
- 201000011510 cancer Diseases 0.000 claims description 8
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 8
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 8
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 7
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 7
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 7
- 230000002401 inhibitory effect Effects 0.000 claims description 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 7
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 7
- 229910052760 oxygen Inorganic materials 0.000 claims description 7
- 125000001424 substituent group Chemical group 0.000 claims description 7
- WEVYNIUIFUYDGI-UHFFFAOYSA-N 3-[6-[4-(trifluoromethoxy)anilino]-4-pyrimidinyl]benzamide Chemical compound NC(=O)C1=CC=CC(C=2N=CN=C(NC=3C=CC(OC(F)(F)F)=CC=3)C=2)=C1 WEVYNIUIFUYDGI-UHFFFAOYSA-N 0.000 claims description 6
- 101000932478 Homo sapiens Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims description 6
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 claims description 6
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 claims description 6
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims description 6
- 230000015556 catabolic process Effects 0.000 claims description 6
- 238000006731 degradation reaction Methods 0.000 claims description 6
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims description 6
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims description 6
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 6
- 125000004076 pyridyl group Chemical group 0.000 claims description 6
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims description 5
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 5
- 125000004414 alkyl thio group Chemical group 0.000 claims description 5
- 230000001939 inductive effect Effects 0.000 claims description 5
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 5
- 125000005334 azaindolyl group Chemical group N1N=C(C2=CC=CC=C12)* 0.000 claims description 4
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims description 4
- 125000005605 benzo group Chemical group 0.000 claims description 4
- 125000004618 benzofuryl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims description 4
- 125000005874 benzothiadiazolyl group Chemical group 0.000 claims description 4
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims description 4
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims description 4
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims description 4
- 125000000000 cycloalkoxy group Chemical group 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- 125000004857 imidazopyridinyl group Chemical group N1C(=NC2=C1C=CC=N2)* 0.000 claims description 4
- 210000000987 immune system Anatomy 0.000 claims description 4
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 4
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 claims description 4
- 125000001041 indolyl group Chemical group 0.000 claims description 4
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims description 4
- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 claims description 4
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 4
- DTXOCJGLLMAFBX-UHFFFAOYSA-N oxo-[[1-[2-[[4-(oxoazaniumylmethylidene)pyridin-1-yl]methoxy]ethoxymethyl]pyridin-4-ylidene]methyl]azanium;dichloride Chemical compound [Cl-].[Cl-].C1=CC(=C[NH+]=O)C=CN1COCCOCN1C=CC(=C[NH+]=O)C=C1 DTXOCJGLLMAFBX-UHFFFAOYSA-N 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims description 4
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 4
- 125000005888 tetrahydroindolyl group Chemical group 0.000 claims description 4
- 125000001544 thienyl group Chemical group 0.000 claims description 4
- 208000035143 Bacterial infection Diseases 0.000 claims description 3
- 206010017533 Fungal infection Diseases 0.000 claims description 3
- 208000031888 Mycoses Diseases 0.000 claims description 3
- 208000030852 Parasitic disease Diseases 0.000 claims description 3
- 102000007537 Type II DNA Topoisomerases Human genes 0.000 claims description 3
- 108010046308 Type II DNA Topoisomerases Proteins 0.000 claims description 3
- 208000022362 bacterial infectious disease Diseases 0.000 claims description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 3
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 3
- 208000026278 immune system disease Diseases 0.000 claims description 3
- 208000027866 inflammatory disease Diseases 0.000 claims description 3
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims description 3
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 3
- 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 230000002062 proliferating effect Effects 0.000 claims description 3
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 claims description 3
- 239000012453 solvate Substances 0.000 claims description 3
- NCKKMYKNYLIUDP-UHFFFAOYSA-N 3-(2,4-dihydroxy-5-propan-2-ylphenyl)-4-(1-methylindol-5-yl)-1,5-dihydro-1,2,4-triazin-6-one Chemical compound C1=C(O)C(C(C)C)=CC(C=2N(CC(=O)NN=2)C=2C=C3C=CN(C)C3=CC=2)=C1O NCKKMYKNYLIUDP-UHFFFAOYSA-N 0.000 claims description 2
- QZHIIMRXMPTCDV-UHFFFAOYSA-N 3-(2,4-dihydroxy-5-propan-2-ylphenyl)-4-(4-morpholin-4-ylphenyl)-1,5-dihydro-1,2,4-triazin-6-one Chemical compound C1=C(O)C(C(C)C)=CC(C=2N(CC(=O)NN=2)C=2C=CC(=CC=2)N2CCOCC2)=C1O QZHIIMRXMPTCDV-UHFFFAOYSA-N 0.000 claims description 2
- NVSARGIJVCFALM-UHFFFAOYSA-N 3-(2,4-dihydroxy-5-propan-2-ylphenyl)-4-[4-(dimethylamino)phenyl]-1,5-dihydro-1,2,4-triazin-6-one Chemical compound C1=C(O)C(C(C)C)=CC(C=2N(CC(=O)NN=2)C=2C=CC(=CC=2)N(C)C)=C1O NVSARGIJVCFALM-UHFFFAOYSA-N 0.000 claims description 2
- ASXZYSYWBDYVJK-UHFFFAOYSA-N 4-(2,4-dihydroxy-5-propan-2-ylphenyl)-1,3,4,7-tetrahydrofuro[3,4-d]pyrimidine-2,5-dione Chemical compound C1=C(O)C(C(C)C)=CC(C2C3=C(COC3=O)NC(=O)N2)=C1O ASXZYSYWBDYVJK-UHFFFAOYSA-N 0.000 claims description 2
- GKHMRQSMULFODR-UHFFFAOYSA-N 4-(2,4-dihydroxy-5-propan-2-ylphenyl)-6-ethyl-1,3,4,7-tetrahydropyrrolo[3,4-d]pyrimidine-2,5-dione Chemical compound O=C1N(CC)CC(NC(=O)N2)=C1C2C1=CC(C(C)C)=C(O)C=C1O GKHMRQSMULFODR-UHFFFAOYSA-N 0.000 claims description 2
- 230000033115 angiogenesis Effects 0.000 claims description 2
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 claims description 2
- 125000000522 cyclooctenyl group Chemical group C1(=CCCCCCC1)* 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- SWYKTNAHDMJKJU-UHFFFAOYSA-N ethyl 4-(2,4-dihydroxy-5-propan-2-ylphenyl)-6-methyl-2-oxo-3,4-dihydro-1h-pyrimidine-5-carboxylate Chemical compound CCOC(=O)C1=C(C)NC(=O)NC1C1=CC(C(C)C)=C(O)C=C1O SWYKTNAHDMJKJU-UHFFFAOYSA-N 0.000 claims description 2
- 230000014399 negative regulation of angiogenesis Effects 0.000 claims description 2
- 230000001629 suppression Effects 0.000 claims description 2
- 125000003342 alkenyl group Chemical group 0.000 claims 16
- 125000000304 alkynyl group Chemical group 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 230000001580 bacterial effect Effects 0.000 claims 2
- 230000002538 fungal effect Effects 0.000 claims 2
- 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 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- JZTHQIOOVSRSAV-UHFFFAOYSA-N OC1=C(C=C(C(=C1)O)C(C)C)N1N=CN(CC1=O)CC1=CC=C(C=C1)OC Chemical compound OC1=C(C=C(C(=C1)O)C(C)C)N1N=CN(CC1=O)CC1=CC=C(C=C1)OC JZTHQIOOVSRSAV-UHFFFAOYSA-N 0.000 claims 1
- UTCSSFWDNNEEBH-UHFFFAOYSA-N imidazo[1,2-a]pyridine Chemical class C1=CC=CC2=NC=CN21 UTCSSFWDNNEEBH-UHFFFAOYSA-N 0.000 claims 1
- 230000006698 induction Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 125000001844 prenyl group Chemical group [H]C([*])([H])C([H])=C(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 238000000034 method Methods 0.000 description 32
- 241000124008 Mammalia Species 0.000 description 17
- 239000000651 prodrug Substances 0.000 description 7
- 229940002612 prodrug Drugs 0.000 description 7
- 210000004027 cell Anatomy 0.000 description 5
- 125000000131 cyclopropyloxy group Chemical group C1(CC1)O* 0.000 description 4
- 102100034051 Heat shock protein HSP 90-alpha Human genes 0.000 description 3
- 101001016865 Homo sapiens Heat shock protein HSP 90-alpha Proteins 0.000 description 3
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 description 3
- 239000002246 antineoplastic agent Substances 0.000 description 3
- 229940127089 cytotoxic agent Drugs 0.000 description 3
- RGICCULPCWNRAB-UHFFFAOYSA-N 2-[2-(2-hexoxyethoxy)ethoxy]ethanol Chemical compound CCCCCCOCCOCCOCCO RGICCULPCWNRAB-UHFFFAOYSA-N 0.000 description 2
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 description 2
- 208000028564 B-cell non-Hodgkin lymphoma Diseases 0.000 description 2
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 description 2
- 206010061309 Neoplasm progression Diseases 0.000 description 2
- 206010029113 Neovascularisation Diseases 0.000 description 2
- 208000009052 Precursor T-Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 description 2
- 230000017531 blood circulation Effects 0.000 description 2
- 210000004204 blood vessel Anatomy 0.000 description 2
- 230000037361 pathway Effects 0.000 description 2
- 102000004169 proteins and genes Human genes 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- 229940124597 therapeutic agent Drugs 0.000 description 2
- 230000005751 tumor progression Effects 0.000 description 2
- 0 ***(*1)C(c2c(*)cc(*)c(*)c2)=**[C@]1O Chemical compound ***(*1)C(c2c(*)cc(*)c(*)c2)=**[C@]1O 0.000 description 1
- NQSKYRRKRPDMFI-UHFFFAOYSA-N 3-(2,4-dihydroxy-5-propan-2-ylphenyl)-4-[(4-methoxyphenyl)methyl]-1,5-dihydro-1,2,4-triazin-6-one Chemical compound C1=CC(OC)=CC=C1CN1C(C=2C(=CC(O)=C(C(C)C)C=2)O)=NNC(=O)C1 NQSKYRRKRPDMFI-UHFFFAOYSA-N 0.000 description 1
- 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 description 1
- 208000011691 Burkitt lymphomas Diseases 0.000 description 1
- 102000003676 Glucocorticoid Receptors Human genes 0.000 description 1
- 108090000079 Glucocorticoid Receptors Proteins 0.000 description 1
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 description 1
- 208000032004 Large-Cell Anaplastic Lymphoma Diseases 0.000 description 1
- 206010025323 Lymphomas Diseases 0.000 description 1
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 description 1
- 206010029461 Nodal marginal zone B-cell lymphomas Diseases 0.000 description 1
- 208000027190 Peripheral T-cell lymphomas Diseases 0.000 description 1
- 208000033014 Plasma cell tumor Diseases 0.000 description 1
- 208000007452 Plasmacytoma Diseases 0.000 description 1
- 102000001253 Protein Kinase Human genes 0.000 description 1
- 208000031672 T-Cell Peripheral Lymphoma Diseases 0.000 description 1
- 206010042971 T-cell lymphoma Diseases 0.000 description 1
- 208000020982 T-lymphoblastic lymphoma Diseases 0.000 description 1
- 108091023040 Transcription factor Proteins 0.000 description 1
- 102000040945 Transcription factor Human genes 0.000 description 1
- 208000036142 Viral infection Diseases 0.000 description 1
- 208000016025 Waldenstroem macroglobulinemia Diseases 0.000 description 1
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 description 1
- 125000003282 alkyl amino group Chemical group 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 description 1
- 125000004663 dialkyl amino group Chemical group 0.000 description 1
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 description 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 description 1
- 201000003444 follicular lymphoma Diseases 0.000 description 1
- 239000003481 heat shock protein 90 inhibitor Substances 0.000 description 1
- 230000001401 hemangioblastic effect Effects 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000002452 interceptive effect Effects 0.000 description 1
- 208000020968 mature T-cell and NK-cell non-Hodgkin lymphoma Diseases 0.000 description 1
- 208000010626 plasma cell neoplasm Diseases 0.000 description 1
- 108060006633 protein kinase Proteins 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 230000019491 signal transduction Effects 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 230000009385 viral infection Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US92032707P | 2007-03-27 | 2007-03-27 | |
| US60/920,327 | 2007-03-27 | ||
| PCT/US2008/003810 WO2008118391A2 (en) | 2007-03-27 | 2008-03-24 | Triazinone and diazinone derivatives useful as hsp90 inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010522750A JP2010522750A (ja) | 2010-07-08 |
| JP2010522750A5 true JP2010522750A5 (enExample) | 2011-05-06 |
| JP5529004B2 JP5529004B2 (ja) | 2014-06-25 |
Family
ID=39739347
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010500949A Expired - Fee Related JP5529004B2 (ja) | 2007-03-27 | 2008-03-24 | Ｈｓｐ９０阻害剤として有用なトリアジノンおよびジアジノン誘導体 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US8524712B2 (enExample) |
| EP (1) | EP2155694B1 (enExample) |
| JP (1) | JP5529004B2 (enExample) |
| AT (1) | ATE540028T1 (enExample) |
| AU (1) | AU2008232354B9 (enExample) |
| CA (1) | CA2682665C (enExample) |
| ES (1) | ES2395114T3 (enExample) |
| TW (1) | TWI427068B (enExample) |
| WO (1) | WO2008118391A2 (enExample) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1817295B1 (en) | 2004-11-18 | 2012-11-07 | Synta Pharmaceuticals Corp. | Triazole compounds that modulate hsp90 activity |
| US7608635B2 (en) | 2005-08-12 | 2009-10-27 | Synta Pharmaceuticals Corp. | Pyrazole compounds that modulate HSP90 activity |
| US20070250391A1 (en) * | 2006-04-05 | 2007-10-25 | Prade Hendrik D | Merchandising system and method for food and non-food items for a meal kit |
| WO2007139955A2 (en) | 2006-05-25 | 2007-12-06 | Synta Pharmaceuticals Corp. | Triazole compounds that modulate hsp90 activity |
| AU2007267843B2 (en) | 2006-05-25 | 2011-10-13 | Synta Pharmaceuticals Corp. | Method for treating proliferative disorders associated with protooncogene products |
| SI2035396T1 (sl) | 2006-05-25 | 2014-08-29 | Synta Pharmaceuticals Corp. | Triazolne spojine, ki modulirajo aktivnost HSP90 |
| US8063083B2 (en) | 2006-05-25 | 2011-11-22 | Synta Pharmaceuticals Corp. | Method for treating non-Hodgkin's lymphoma |
| CA2653327A1 (en) * | 2006-05-25 | 2007-12-06 | Synta Pharmaceuticals Corp. | Compounds that modulate hsp90 activity and methods for identifying same |
| US9156836B2 (en) * | 2008-05-16 | 2015-10-13 | Synta Pharmaceuticals Corp. | Tricyclic triazole compounds that modulate HSP90 activity |
| US8450500B2 (en) | 2008-06-04 | 2013-05-28 | Synta Pharmaceuticals Corp. | Pyrrole compounds that modulate HSP90 activity |
| US8648071B2 (en) | 2008-06-27 | 2014-02-11 | Synta Pharmaceuticals Corp. | Hydrazonamide compounds that modulate Hsp90 activity |
| WO2010017545A2 (en) | 2008-08-08 | 2010-02-11 | Synta Pharamceuticals Corp. | Triazole compounds that modulate hsp90 activity |
| US9126953B2 (en) * | 2008-08-08 | 2015-09-08 | Synta Pharmaceuticals Corp. | Triazole compounds that modulate HSP90 activity |
| PT2452940E (pt) * | 2009-07-10 | 2015-02-27 | Taiho Pharmaceutical Co Ltd | Composto azabiciclo e seu sal |
| AR077405A1 (es) | 2009-07-10 | 2011-08-24 | Sanofi Aventis | Derivados del indol inhibidores de hsp90, composiciones que los contienen y utilizacion de los mismos para el tratamiento del cancer |
| FR2949467B1 (fr) | 2009-09-03 | 2011-11-25 | Sanofi Aventis | Nouveaux derives de 5,6,7,8-tetrahydroindolizine inhibiteurs d'hsp90, compositions les contenant et utilisation |
| WO2011038204A1 (en) | 2009-09-25 | 2011-03-31 | N30 Pharmaceuticals, Llc | Novel dihydropyrimidin-2(1h)-one compounds as s-nitrosoglutathione reductase inhibitors |
| EP2560640A1 (en) | 2010-04-19 | 2013-02-27 | Synta Pharmaceuticals Corp. | Cancer therapy using a combination of a hsp90 inhibitory compounds and a egfr inhibitor |
| US8906933B2 (en) | 2010-09-24 | 2014-12-09 | N30 Pharmaceuticals, Inc. | Dihydropyrimidin-2(1H)-one compounds as neurokinin-3 receptor antagonists |
| WO2012087943A2 (en) * | 2010-12-20 | 2012-06-28 | The Regents Of The University Of Michigan | Inhibitors of the epidermal growth factor receptor-heat shock protein 90 binding interaction |
| US9540443B2 (en) | 2011-01-26 | 2017-01-10 | Kolltan Pharmaceuticals, Inc. | Anti-kit antibodies |
| CA2840986A1 (en) | 2011-07-07 | 2013-01-10 | Synta Pharmaceuticals Corp. | Treating cancer with hsp90 inhibitory compounds |
| CN103717591B (zh) * | 2011-07-27 | 2016-08-24 | Ab科学有限公司 | 作为选择性蛋白激酶(c-kit)抑制剂的噁唑和噻唑衍生物 |
| JP2014534228A (ja) | 2011-11-02 | 2014-12-18 | シンタ ファーマシューティカルズ コーポレーション | 白金含有剤とｈｓｐ９０阻害剤の組合せ療法 |
| CA2853799A1 (en) | 2011-11-02 | 2013-05-10 | Synta Pharmaceuticals Corp. | Cancer therapy using a combination of hsp90 inhibitors with topoisomerase i inhibitors |
| US9402831B2 (en) | 2011-11-14 | 2016-08-02 | Synta Pharmaceutical Corp. | Combination therapy of HSP90 inhibitors with BRAF inhibitors |
| NZ630363A (en) | 2012-07-25 | 2018-09-28 | Celldex Therapeutics Inc | Anti-kit antibodies and uses thereof |
| EP2972394A4 (en) | 2013-03-15 | 2016-11-02 | Sloan Kettering Inst Cancer | HSP90-DESIGNING AND THERAPY |
| US20170209408A1 (en) | 2014-04-03 | 2017-07-27 | The Children's Medical Center Corporation | Hsp90 inhibitors for the treatment of obesity and methods of use thereof |
| CN113975386A (zh) | 2014-05-23 | 2022-01-28 | 塞尔德克斯医疗公司 | 嗜酸性粒细胞或肥大细胞相关病症的治疗 |
| MX387627B (es) | 2014-09-17 | 2025-03-18 | Memorial Sloan Kettering Cancer Center | Formación de imágenes de inflamación e infección dirigida a hsp90 y terapia |
| WO2018049092A1 (en) * | 2016-09-09 | 2018-03-15 | University Of Cincinnati | Small molecule prolactin receptor inhibitors, pharmaceutical compositions and treatment methods using such inhibitors |
| US10767164B2 (en) | 2017-03-30 | 2020-09-08 | The Research Foundation For The State University Of New York | Microenvironments for self-assembly of islet organoids from stem cells differentiation |
| CN109666024A (zh) * | 2018-03-20 | 2019-04-23 | 兰州大学 | 2-氧嘧啶类化合物及其制备方法和用途 |
| CN110105365B (zh) * | 2019-05-29 | 2021-08-10 | 华中农业大学 | 一种喹啉衍生物VCTb5及其在制备抗癌药物中的应用 |
| CN110105366B (zh) * | 2019-05-29 | 2021-06-01 | 华中农业大学 | 一种喹啉衍生物VCTb9及其在制备抗癌药物中的应用 |
| KR20230035049A (ko) * | 2020-07-02 | 2023-03-10 | 데날리 테라퓨틱스 인크. | 화합물, 조성물 및 방법 |
| WO2025188973A1 (en) * | 2024-03-06 | 2025-09-12 | Ovid Therapeutics Inc. | Fused amino pyrimidine compounds for treatment of 22q11.2 deletion/duplication syndromes |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4239540A1 (de) * | 1992-11-25 | 1994-05-26 | Asta Medica Ag | Neue heterocyclische Verbindungen mit antiasthmatischer/antiallergischer, entzündungshemmender, positiv inotroper und blutdrucksenkender Wirkung |
| GB0315111D0 (en) | 2003-06-27 | 2003-07-30 | Cancer Rec Tech Ltd | Substituted 5-membered ring compounds and their use |
| GB0320300D0 (en) * | 2003-08-29 | 2003-10-01 | Cancer Rec Tech Ltd | Pyrimidothiophene compounds |
| WO2005037799A1 (en) * | 2003-10-16 | 2005-04-28 | Cytokinetics, Inc. | Compounds, compositions, and methods |
| US20070265289A1 (en) * | 2004-04-15 | 2007-11-15 | Yoshinori Okamoto | 2-Aminopyrimidine Derivative |
| JP2008545622A (ja) * | 2005-05-03 | 2008-12-18 | ダウ アグロサイエンシィズ エルエルシー | 置換４，５−ジヒドロ−１，２，４−トリアジン−６−オン類、１，２，４−トリアジン−６−オン類およびそれらの殺真菌剤としての用途 |
| EP2049497A2 (en) * | 2005-05-19 | 2009-04-22 | Astex Therapeutics Limited | Pyrimidine derivatives as hsp90 inhibitors |
| DE102005022977A1 (de) * | 2005-05-19 | 2006-12-07 | Merck Patent Gmbh | Phenylchinazolinderivate |
-
2008
- 2008-03-24 EP EP08742209A patent/EP2155694B1/en not_active Not-in-force
- 2008-03-24 ES ES08742209T patent/ES2395114T3/es active Active
- 2008-03-24 AT AT08742209T patent/ATE540028T1/de active
- 2008-03-24 JP JP2010500949A patent/JP5529004B2/ja not_active Expired - Fee Related
- 2008-03-24 CA CA2682665A patent/CA2682665C/en not_active Expired - Fee Related
- 2008-03-24 WO PCT/US2008/003810 patent/WO2008118391A2/en not_active Ceased
- 2008-03-24 US US12/593,147 patent/US8524712B2/en not_active Expired - Fee Related
- 2008-03-24 AU AU2008232354A patent/AU2008232354B9/en not_active Ceased
- 2008-03-27 TW TW097110954A patent/TWI427068B/zh not_active IP Right Cessation
-
2013
- 2013-08-28 US US14/012,408 patent/US20130345219A1/en not_active Abandoned
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