JP2009504669A5 - - Google Patents
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- JP2009504669A5 JP2009504669A5 JP2008526240A JP2008526240A JP2009504669A5 JP 2009504669 A5 JP2009504669 A5 JP 2009504669A5 JP 2008526240 A JP2008526240 A JP 2008526240A JP 2008526240 A JP2008526240 A JP 2008526240A JP 2009504669 A5 JP2009504669 A5 JP 2009504669A5
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- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims 543
- 150000001875 compounds Chemical class 0.000 claims 81
- 125000001072 heteroaryl group Chemical group 0.000 claims 56
- 125000000623 heterocyclic group Chemical group 0.000 claims 47
- 125000003710 aryl alkyl group Chemical group 0.000 claims 46
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 42
- 125000000547 substituted alkyl group Chemical group 0.000 claims 41
- 125000003107 substituted aryl group Chemical group 0.000 claims 40
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 39
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 39
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 39
- 229910052757 nitrogen Inorganic materials 0.000 claims 34
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 33
- 125000001188 haloalkyl group Chemical group 0.000 claims 32
- 125000005843 halogen group Chemical group 0.000 claims 29
- 125000004404 heteroalkyl group Chemical group 0.000 claims 24
- -1 cyano, nitro, Guanidino Chemical group 0.000 claims 23
- 125000004438 haloalkoxy group Chemical group 0.000 claims 19
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims 16
- 125000003545 alkoxy group Chemical group 0.000 claims 16
- 125000000217 alkyl group Chemical group 0.000 claims 15
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 11
- 239000000651 prodrug Substances 0.000 claims 11
- 229940002612 prodrug Drugs 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 11
- 239000012453 solvate Substances 0.000 claims 11
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 10
- 125000001424 substituent group Chemical group 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 9
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 9
- 229910052717 sulfur Inorganic materials 0.000 claims 9
- 229910052799 carbon Inorganic materials 0.000 claims 8
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 8
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 7
- 125000004432 carbon atom Chemical group C* 0.000 claims 7
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 7
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 7
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 6
- 101100516572 Caenorhabditis elegans nhr-8 gene Proteins 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 6
- 239000000126 substance Substances 0.000 claims 6
- 125000004414 alkyl thio group Chemical group 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 3
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 3
- 125000000131 cyclopropyloxy group Chemical group C1(CC1)O* 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 125000000081 (C5-C8) cycloalkenyl group Chemical group 0.000 claims 2
- 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 2
- 241000124008 Mammalia Species 0.000 claims 2
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 claims 2
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 claims 2
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims 2
- 101710151245 Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 2
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 2
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 claims 2
- 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 2
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 108090000623 proteins and genes Proteins 0.000 claims 2
- 102000004169 proteins and genes Human genes 0.000 claims 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 1
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 claims 1
- RGICCULPCWNRAB-UHFFFAOYSA-N 2-[2-(2-hexoxyethoxy)ethoxy]ethanol Chemical compound CCCCCCOCCOCCOCCO RGICCULPCWNRAB-UHFFFAOYSA-N 0.000 claims 1
- FSPQCTGGIANIJZ-UHFFFAOYSA-N 2-[[(3,4-dimethoxyphenyl)-oxomethyl]amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide Chemical compound C1=C(OC)C(OC)=CC=C1C(=O)NC1=C(C(N)=O)C(CCCC2)=C2S1 FSPQCTGGIANIJZ-UHFFFAOYSA-N 0.000 claims 1
- 102100034051 Heat shock protein HSP 90-alpha Human genes 0.000 claims 1
- 101001016865 Homo sapiens Heat shock protein HSP 90-alpha Proteins 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 230000015556 catabolic process Effects 0.000 claims 1
- 238000006731 degradation reaction Methods 0.000 claims 1
- 125000004663 dialkyl amino group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 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 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 0 *C(CCC*CC1)C1c1c(*)c(*)n[n]1 Chemical compound *C(CCC*CC1)C1c1c(*)c(*)n[n]1 0.000 description 5
- VZYNAEAVUATNDU-UHFFFAOYSA-N CCc(c(O)c1)cc(-c([nH]nc2S)c2-c(c(C)c2)ccc2F)c1O Chemical compound CCc(c(O)c1)cc(-c([nH]nc2S)c2-c(c(C)c2)ccc2F)c1O VZYNAEAVUATNDU-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US70783605P | 2005-08-12 | 2005-08-12 | |
| US60/707,836 | 2005-08-12 | ||
| PCT/US2006/031430 WO2007021966A1 (en) | 2005-08-12 | 2006-08-10 | Pyrazole compounds that modulate hsp90 activity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009504669A JP2009504669A (ja) | 2009-02-05 |
| JP2009504669A5 true JP2009504669A5 (https=) | 2009-09-24 |
| JP5178515B2 JP5178515B2 (ja) | 2013-04-10 |
Family
ID=37433864
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008526240A Expired - Fee Related JP5178515B2 (ja) | 2005-08-12 | 2006-08-10 | Ｈｓｐ９０活性を調節するピラゾール化合物 |
Country Status (7)
| Country | Link |
|---|---|
| US (4) | US7608635B2 (https=) |
| EP (1) | EP1934185A1 (https=) |
| JP (1) | JP5178515B2 (https=) |
| AU (1) | AU2006279794B2 (https=) |
| CA (1) | CA2618377A1 (https=) |
| TW (1) | TW200740762A (https=) |
| WO (1) | WO2007021966A1 (https=) |
Families Citing this family (43)
| 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 |
| JP5118039B2 (ja) | 2005-08-18 | 2013-01-16 | シンタ ファーマシューティカルズ コーポレーション | Ｈｓｐ９０活性を調節するトリアゾール化合物 |
| 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 |
| SI2035396T1 (sl) | 2006-05-25 | 2014-08-29 | Synta Pharmaceuticals Corp. | Triazolne spojine, ki modulirajo aktivnost HSP90 |
| WO2007139955A2 (en) | 2006-05-25 | 2007-12-06 | Synta Pharmaceuticals Corp. | Triazole compounds that modulate hsp90 activity |
| US8063083B2 (en) | 2006-05-25 | 2011-11-22 | Synta Pharmaceuticals Corp. | Method for treating non-Hodgkin's lymphoma |
| AU2007267843B2 (en) | 2006-05-25 | 2011-10-13 | Synta Pharmaceuticals Corp. | Method for treating proliferative disorders associated with protooncogene products |
| CA2653327A1 (en) * | 2006-05-25 | 2007-12-06 | Synta Pharmaceuticals Corp. | Compounds that modulate hsp90 activity and methods for identifying same |
| WO2008057246A2 (en) * | 2006-10-26 | 2008-05-15 | Synta Pharmaceuticals Corp. | Method for treating inflammatory disorders |
| WO2008112199A1 (en) | 2007-03-12 | 2008-09-18 | Synta Pharmaceuticals Corp. | Method for inhibiting topoisomerase ii |
| WO2008153730A2 (en) * | 2007-05-25 | 2008-12-18 | Synta Pharmaceuticals Corp. | Method for treating proliferative disorders associated with mutations in c-met |
| CN101821247A (zh) * | 2007-10-12 | 2010-09-01 | 艾科尔公司 | 作为hsp90抑制剂的抗癌用5-(2-羟基苯基)四唑化合物 |
| GB0722680D0 (en) * | 2007-11-19 | 2007-12-27 | Topotarget As | Therapeutic compounds and their use |
| LT5623B (lt) | 2008-04-30 | 2010-01-25 | Biotechnologijos Institutas, , | 5-aril-4-(5-pakeistieji 2,4-dihidroksifenil)-1,2,3-tiadiazolai kaip hsp90 šaperono slopikliai ir tarpiniai junginiai jiems gauti |
| 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 |
| US9126953B2 (en) * | 2008-08-08 | 2015-09-08 | Synta Pharmaceuticals Corp. | Triazole compounds that modulate HSP90 activity |
| WO2010017545A2 (en) | 2008-08-08 | 2010-02-11 | Synta Pharamceuticals Corp. | Triazole compounds that modulate hsp90 activity |
| PT2452940E (pt) * | 2009-07-10 | 2015-02-27 | Taiho Pharmaceutical Co Ltd | Composto azabiciclo e seu sal |
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| 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 |
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| WO2012116247A1 (en) * | 2011-02-25 | 2012-08-30 | Synta Pharmaceuticals Corp. | Hsp90 inhibitory compounds in treating jak/stat signaling-mediated cancers |
| US9169260B2 (en) | 2011-03-22 | 2015-10-27 | Merck Sharp & Dohme Corp. | Amidopyrazole inhibitors of interleukin receptor-associated kinases |
| CA2840986A1 (en) | 2011-07-07 | 2013-01-10 | Synta Pharmaceuticals Corp. | Treating cancer with hsp90 inhibitory compounds |
| 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 |
| RU2622015C2 (ru) | 2011-11-11 | 2017-06-08 | Новартис Аг | Способ лечения пролиферативного заболевания |
| US9402831B2 (en) | 2011-11-14 | 2016-08-02 | Synta Pharmaceutical Corp. | Combination therapy of HSP90 inhibitors with BRAF inhibitors |
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| CA2868323A1 (en) * | 2012-04-04 | 2013-10-10 | Synta Pharmaceuticals Corp. | Novel triazole compounds that modulate hsp90 activity |
| KR20210033067A (ko) | 2012-06-04 | 2021-03-25 | 파마싸이클릭스 엘엘씨 | 브루톤 타이로신 키나아제 저해제의 결정 형태 |
| CN103724269B (zh) * | 2012-10-11 | 2016-12-21 | 中国科学院上海药物研究所 | 苯基1,2-异噁唑或苯基1,2-吡唑类化合物及其用途 |
| 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 |
| SG11201608303QA (en) | 2014-04-04 | 2016-11-29 | Del Mar Pharmaceuticals | Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer |
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| EP3248968A4 (en) * | 2015-01-22 | 2018-11-07 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Resorcinol derivative as hsp90 inhibitor |
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| WO2020227368A1 (en) * | 2019-05-08 | 2020-11-12 | Trustees Of Boston University | Hsp90 inhibitors and uses thereof |
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| 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 |
| WO2007139952A2 (en) | 2006-05-25 | 2007-12-06 | Synta Pharmaceuticals Corp. | Method for the preparation of triazole compounds with hsp90 modulating activity |
| EP2038262B1 (en) | 2006-05-25 | 2014-11-12 | Synta Pharmaceuticals Corp. | Triazole compounds that modulate hsp90 activity |
| SI2035396T1 (sl) | 2006-05-25 | 2014-08-29 | Synta Pharmaceuticals Corp. | Triazolne spojine, ki modulirajo aktivnost HSP90 |
| 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 |
| AU2007284537B2 (en) | 2006-08-17 | 2012-04-12 | Synta Pharmaceuticals Corp. | Triazole compounds that modulate HSP90 activity |
| US20110046125A1 (en) | 2006-10-19 | 2011-02-24 | Synta Pharmaceuticals Corp. | Method for treating infections |
| WO2008057246A2 (en) | 2006-10-26 | 2008-05-15 | Synta Pharmaceuticals Corp. | Method for treating inflammatory disorders |
| PL2118077T3 (pl) | 2007-02-08 | 2015-05-29 | Synta Pharmaceuticals Corp | Związki triazolowe modulujące aktywność hsp90 |
| WO2008112199A1 (en) | 2007-03-12 | 2008-09-18 | Synta Pharmaceuticals Corp. | Method for inhibiting topoisomerase ii |
| EP2155694B1 (en) | 2007-03-27 | 2012-01-04 | Synta Pharmaceuticals Corp. | Triazinone and diazinone derivatives useful as hsp90 inhibitors |
| WO2008153730A2 (en) | 2007-05-25 | 2008-12-18 | Synta Pharmaceuticals Corp. | Method for treating proliferative disorders associated with mutations in c-met |
| AU2008287367B2 (en) | 2007-08-13 | 2012-02-23 | Synta Pharmaceuticals Corp. | Triazole compounds that modulate HSP90 activity |
| 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 |
| EP2490688B1 (en) | 2009-10-19 | 2014-10-08 | Synta Pharmaceuticals Corp. | Combination cancer therapy with hsp90 inhibitory compounds |
| CN103269701A (zh) | 2010-09-13 | 2013-08-28 | 辛塔医药品有限公司 | 用于治疗野生型egfr和/或kras患者的非小细胞肺癌的hsp90抑制剂 |
-
2006
- 2006-08-10 US US11/502,346 patent/US7608635B2/en active Active
- 2006-08-10 WO PCT/US2006/031430 patent/WO2007021966A1/en not_active Ceased
- 2006-08-10 AU AU2006279794A patent/AU2006279794B2/en not_active Ceased
- 2006-08-10 CA CA002618377A patent/CA2618377A1/en not_active Abandoned
- 2006-08-10 JP JP2008526240A patent/JP5178515B2/ja not_active Expired - Fee Related
- 2006-08-10 EP EP06801286A patent/EP1934185A1/en not_active Ceased
- 2006-08-11 TW TW095129520A patent/TW200740762A/zh unknown
-
2009
- 2009-09-14 US US12/559,155 patent/US20100069442A1/en not_active Abandoned
-
2011
- 2011-02-14 US US13/026,981 patent/US8329899B2/en not_active Expired - Fee Related
-
2012
- 2012-11-13 US US13/675,294 patent/US8921407B2/en active Active
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