JP2010530432A5 - - Google Patents
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- Publication number
- JP2010530432A5 JP2010530432A5 JP2010513267A JP2010513267A JP2010530432A5 JP 2010530432 A5 JP2010530432 A5 JP 2010530432A5 JP 2010513267 A JP2010513267 A JP 2010513267A JP 2010513267 A JP2010513267 A JP 2010513267A JP 2010530432 A5 JP2010530432 A5 JP 2010530432A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- compound according
- phenyl
- fluorophenyl
- pyridyl
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 28
- -1 difluorophenylmethylthiazolyl Chemical group 0.000 claims 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 125000004076 pyridyl group Chemical group 0.000 claims 5
- 102000011990 Sirtuin Human genes 0.000 claims 4
- 108050002485 Sirtuin Proteins 0.000 claims 4
- 230000000694 effects Effects 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 230000003381 solubilizing effect Effects 0.000 claims 4
- 125000001207 fluorophenyl group Chemical group 0.000 claims 3
- 230000005764 inhibitory process Effects 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 2
- 206010022489 Insulin Resistance Diseases 0.000 claims 2
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 2
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 2
- 125000000068 chlorophenyl group Chemical group 0.000 claims 2
- 125000004212 difluorophenyl group Chemical group 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000004575 3-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 101000654472 Homo sapiens NAD-dependent protein deacetylase sirtuin-1 Proteins 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 102100030710 NAD-dependent protein deacetylase sirtuin-3, mitochondrial Human genes 0.000 claims 1
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 claims 1
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 claims 1
- 108091005770 SIRT3 Proteins 0.000 claims 1
- 102000000344 Sirtuin 1 Human genes 0.000 claims 1
- 108010041191 Sirtuin 1 Proteins 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 230000002921 anti-spasmodic effect Effects 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 230000006196 deacetylation Effects 0.000 claims 1
- 238000003381 deacetylation reaction Methods 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 1
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 1
- 125000003187 heptyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 102000056482 human SIRT1 Human genes 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 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
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 125000004353 pyrazol-1-yl group Chemical group [H]C1=NN(*)C([H])=C1[H] 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 230000026683 transduction Effects 0.000 claims 1
- 238000010361 transduction Methods 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 230000024883 vasodilation Effects 0.000 claims 1
- LVDUUIXBZXBALU-UHFFFAOYSA-N CC(C)NCc1cnc2[s]c(-c(cccc3)c3NC(c3cc(-c4ccccc4)cnc3)=O)nc2c1 Chemical compound CC(C)NCc1cnc2[s]c(-c(cccc3)c3NC(c3cc(-c4ccccc4)cnc3)=O)nc2c1 LVDUUIXBZXBALU-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US93663607P | 2007-06-20 | 2007-06-20 | |
| US60/936,636 | 2007-06-20 | ||
| PCT/US2008/007776 WO2008156869A2 (en) | 2007-06-20 | 2008-06-20 | Sirtuin modulating thiazolopyridine compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010530432A JP2010530432A (ja) | 2010-09-09 |
| JP2010530432A5 true JP2010530432A5 (enExample) | 2011-08-04 |
| JP5498940B2 JP5498940B2 (ja) | 2014-05-21 |
Family
ID=39798234
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010513267A Expired - Fee Related JP5498940B2 (ja) | 2007-06-20 | 2008-06-20 | サーチュイン調節性チアゾロピリジン化合物 |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US7893086B2 (enExample) |
| EP (1) | EP2170905A2 (enExample) |
| JP (1) | JP5498940B2 (enExample) |
| KR (1) | KR20100051048A (enExample) |
| CN (2) | CN101801981A (enExample) |
| AR (1) | AR067107A1 (enExample) |
| AU (1) | AU2008266749C1 (enExample) |
| BR (1) | BRPI0813651A2 (enExample) |
| CA (1) | CA2691733A1 (enExample) |
| CL (1) | CL2008001822A1 (enExample) |
| CO (1) | CO6251248A2 (enExample) |
| CR (1) | CR11232A (enExample) |
| DO (1) | DOP2009000284A (enExample) |
| EA (1) | EA018922B1 (enExample) |
| IL (1) | IL202730A0 (enExample) |
| MA (1) | MA31506B1 (enExample) |
| MX (1) | MX2009013977A (enExample) |
| NZ (1) | NZ581990A (enExample) |
| PE (1) | PE20090694A1 (enExample) |
| TW (1) | TW200916472A (enExample) |
| UY (1) | UY31169A1 (enExample) |
| WO (1) | WO2008156869A2 (enExample) |
| ZA (1) | ZA200908883B (enExample) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2397275T3 (es) * | 2005-08-04 | 2013-03-05 | Sirtris Pharmaceuticals, Inc. | Derivados de imidazopiridina como agentes moduladores de la sirtuína |
| US20070077310A1 (en) * | 2005-10-03 | 2007-04-05 | University Of Tennessee Research Foundation | Methods of reducing the production of reactive oxygen species and methods of screening or identifying compounds and compositions that reduce the production of reactive oxygen species |
| CL2008001822A1 (es) * | 2007-06-20 | 2009-03-13 | Sirtris Pharmaceuticals Inc | Compuestos derivados de tiazolo[5,4-b]piridina; composicion farmaceutica que comprende a dichos compuestos; y uso del compuesto en el tratamiento de la resistencia a la insulina, sindrome metabolico, diabetes, entre otras. |
| TW200918542A (en) | 2007-06-20 | 2009-05-01 | Sirtris Pharmaceuticals Inc | Sirtuin modulating compounds |
| TWI444379B (zh) * | 2007-06-29 | 2014-07-11 | Sunesis Pharmaceuticals Inc | 有用於作為Ｒａｆ激酶抑制劑之化合物 |
| KR101552742B1 (ko) * | 2007-07-19 | 2015-09-11 | 머크 샤프 앤드 돔 코포레이션 | 단백질 키나제 억제제로서의 헤테로사이클릭 아미드 화합물 |
| CN101910184A (zh) * | 2007-11-08 | 2010-12-08 | 西特里斯药业公司 | 可溶性噻唑并吡啶 |
| EA021938B1 (ru) | 2008-05-01 | 2015-10-30 | Сертрис Фармасьютикалз, Инк. | Хинолины и их аналоги в качестве модуляторов сиртуина |
| CN104193740A (zh) | 2008-07-03 | 2014-12-10 | 西特里斯药业公司 | 作为沉默调节蛋白调节剂的苯并咪唑类和相关的类似物 |
| RU2519779C2 (ru) | 2008-09-29 | 2014-06-20 | Сертрис Фармасьютикалз Инк. | Хиназолинон, хинолон и родственные аналоги в качестве модуляторов сиртуина |
| AU2009333588A1 (en) | 2008-12-08 | 2011-07-21 | Northwestern University | Method of modulating HSF-1 |
| CN102388054B (zh) * | 2008-12-19 | 2015-03-04 | 西特里斯药业公司 | 噻唑并吡啶沉默调节蛋白调节剂的化合物 |
| JP2013509442A (ja) | 2009-10-29 | 2013-03-14 | サートリス ファーマシューティカルズ， インコーポレイテッド | サーチュイン調節因子としての二環式ピリジンおよび類似体 |
| CA2794018C (en) * | 2010-03-24 | 2016-05-10 | Medical University Of South Carolina | Compositions and methods for the treatment of degenerative diseases |
| JP6038773B2 (ja) * | 2010-04-15 | 2016-12-07 | サートリス ファーマシューティカルズ， インコーポレイテッド | サーチュイン活性化因子および活性化アッセイ |
| CN107988228B (zh) * | 2010-05-03 | 2022-01-25 | 库尔纳公司 | 通过抑制沉默调节蛋白(sirt)的天然反义转录物而治疗沉默调节蛋白(sirt)相关疾病 |
| TW201223956A (en) | 2010-08-13 | 2012-06-16 | Solvay | Light emitting materials for electronics |
| EP2423214A1 (en) | 2010-08-13 | 2012-02-29 | Solvay SA | Light emitting materials for Electronics |
| KR20120047341A (ko) * | 2010-10-21 | 2012-05-14 | 경상대학교산학협력단 | 니코틴아미드를 유효성분으로 포함하는 알킬화 약물-유도성 신경퇴행의 예방 또는 치료용 조성물 |
| DK2670404T3 (en) | 2011-02-02 | 2018-11-19 | Univ Princeton | CIRCUIT MODULATORS AS VIRUS PRODUCTION MODULATORS |
| KR101329524B1 (ko) | 2011-05-23 | 2013-11-13 | 연세대학교 산학협력단 | 미분화 전능성 줄기세포의 선택적 세포사멸 방법 |
| RU2631597C2 (ru) | 2011-07-15 | 2017-09-25 | Нусерт Сайенсиз, Инк. | Композиции и способы модулирования метаболических путей |
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| EP2567959B1 (en) | 2011-09-12 | 2014-04-16 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| US9198454B2 (en) | 2012-03-08 | 2015-12-01 | Nusirt Sciences, Inc. | Compositions, methods, and kits for regulating energy metabolism |
| CN108452311A (zh) | 2012-11-13 | 2018-08-28 | 纽斯尔特科学公司 | 用于增强能量代谢的组合物和方法 |
| EP2968333B1 (en) | 2013-03-15 | 2022-01-12 | NuSirt Sciences, Inc. | Leucine and nicotinic acid for the reduction of lipid levels |
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| WO2018049214A1 (en) | 2016-09-09 | 2018-03-15 | Incyte Corporation | Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer |
| CN107496410A (zh) * | 2017-09-21 | 2017-12-22 | 上海华堇生物技术有限责任公司 | 洋槐黄素的药物用途 |
| CN111885914B (zh) * | 2017-10-27 | 2022-05-13 | 投资健康有限责任公司 | 使用芴衍生物制造扩增的造血干细胞的组合物和方法 |
| HUE059624T2 (hu) | 2018-02-20 | 2022-11-28 | Incyte Corp | N-(fenil)-2-(fenil)pirimidin-4-karboxamid származékok és rokon vegyületek HPK1-inhibitorokként rák kezelésére |
| US10899755B2 (en) | 2018-08-08 | 2021-01-26 | Incyte Corporation | Benzothiazole compounds and uses thereof |
| PH12022550271A1 (en) | 2019-08-06 | 2023-06-26 | Incyte Corp | Solid forms of an hpk1 inhibitor |
| WO2024005905A2 (en) * | 2022-04-29 | 2024-01-04 | The Regents Of The University Of Michigan | Small molecule sirtuin inhibitors and uses thereof |
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-
2008
- 2008-06-19 CL CL2008001822A patent/CL2008001822A1/es unknown
- 2008-06-19 TW TW097122810A patent/TW200916472A/zh unknown
- 2008-06-20 KR KR1020107000400A patent/KR20100051048A/ko not_active Ceased
- 2008-06-20 EA EA201070035A patent/EA018922B1/ru not_active IP Right Cessation
- 2008-06-20 CA CA002691733A patent/CA2691733A1/en not_active Abandoned
- 2008-06-20 BR BRPI0813651-3A2A patent/BRPI0813651A2/pt not_active IP Right Cessation
- 2008-06-20 CN CN200880103654A patent/CN101801981A/zh active Pending
- 2008-06-20 AU AU2008266749A patent/AU2008266749C1/en not_active Ceased
- 2008-06-20 UY UY31169A patent/UY31169A1/es not_active Application Discontinuation
- 2008-06-20 EP EP08768700A patent/EP2170905A2/en not_active Withdrawn
- 2008-06-20 NZ NZ581990A patent/NZ581990A/en not_active IP Right Cessation
- 2008-06-20 JP JP2010513267A patent/JP5498940B2/ja not_active Expired - Fee Related
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- 2008-06-20 MX MX2009013977A patent/MX2009013977A/es active IP Right Grant
- 2008-06-20 CN CN201310744228.7A patent/CN103833775A/zh active Pending
- 2008-06-20 PE PE2008001058A patent/PE20090694A1/es not_active Application Discontinuation
- 2008-06-20 US US12/214,805 patent/US7893086B2/en not_active Expired - Fee Related
- 2008-06-20 WO PCT/US2008/007776 patent/WO2008156869A2/en not_active Ceased
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2009
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- 2009-12-14 IL IL202730A patent/IL202730A0/en unknown
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