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.)
- Granted
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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 |
|---|---|---|---|---|
| EP1909910A1 (en) * | 2005-08-04 | 2008-04-16 | Sirtris Pharmaceuticals, Inc. | Benzimidazole derivatives as sirtuin modulators |
| WO2007041641A1 (en) * | 2005-10-03 | 2007-04-12 | 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 |
| CL2008001933A1 (es) * | 2007-06-29 | 2009-09-25 | Millennium Pharm Inc | Compuestos derivados de pirimidina, inhibidores de la raf quinasa; compuestos intermediarios; procedimiento de preparacion; composicion farmaceutica; y su uso para tratar trastornos proliferativos, cardiacos, neurodegenerativos, inflamatorios, oseos, inmunologicos enfermedad viral, entre otros. |
| WO2009014637A2 (en) * | 2007-07-19 | 2009-01-29 | Schering Corporation | Heterocyclic amide compounds as protein kinase inhibitors |
| JP2011503066A (ja) * | 2007-11-08 | 2011-01-27 | 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 | 可溶化チアゾロピリジン誘導体 |
| EA021938B1 (ru) * | 2008-05-01 | 2015-10-30 | Сертрис Фармасьютикалз, Инк. | Хинолины и их аналоги в качестве модуляторов сиртуина |
| KR20110036602A (ko) * | 2008-07-03 | 2011-04-07 | 서트리스 파마슈티컬즈, 인코포레이티드 | 시르투인 조절제로서의 벤즈이미다졸 및 관련 유사체 |
| AU2009295948B2 (en) | 2008-09-29 | 2013-12-05 | GlaxoSmithKline, LLC | Quinazolinone, quinolone and related analogs as sirtuin modulators |
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| EA021424B1 (ru) | 2008-12-19 | 2015-06-30 | Сертрис Фармасьютикалз, Инк. | Тиазолопиридиновые соединения, регулирующие сиртуин |
| US9556201B2 (en) | 2009-10-29 | 2017-01-31 | Glaxosmithkline Llc | Bicyclic pyridines and analogs as sirtuin modulators |
| US20130137728A1 (en) * | 2010-03-24 | 2013-05-30 | MUSC Foundation for Research and Development | Compositions and Methods for the Treatment of Degenerative Diseases |
| EP2993236A1 (en) * | 2010-04-15 | 2016-03-09 | Glaxosmithkline LLC | Sirtuin activators and activation assays |
| WO2011139387A1 (en) * | 2010-05-03 | 2011-11-10 | Opko Curna, Llc | Treatment of sirtuin (sirt) related diseases by inhibition of natural antisense transcript to a sirtuin (sirt) |
| EP2423214A1 (en) | 2010-08-13 | 2012-02-29 | Solvay SA | Light emitting materials for Electronics |
| TW201223956A (en) | 2010-08-13 | 2012-06-16 | Solvay | 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 |
| EP3466418A1 (en) | 2011-07-15 | 2019-04-10 | NuSirt Sciences, Inc. | Compositions and methods for modulating metabolic pathways |
| US10342814B2 (en) * | 2011-09-07 | 2019-07-09 | Cornell University | Methods for treatment of cancer by targeting Sirt5 |
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| US9198454B2 (en) | 2012-03-08 | 2015-12-01 | Nusirt Sciences, Inc. | Compositions, methods, and kits for regulating energy metabolism |
| SG11201503774PA (en) | 2012-11-13 | 2015-06-29 | Nusirt Sciences Inc | Compositions and methods for increasing energy metabolism |
| CN105228627B (zh) | 2013-03-15 | 2018-07-13 | 纽斯尔特科学公司 | 亮氨酸和烟酸降低脂质水平 |
| MX2016011063A (es) | 2014-02-27 | 2016-11-30 | Nusirt Sciences Inc | Composiciones y metodos para la reduccion o prevencion de esteatosis hepatica. |
| WO2015143654A1 (en) * | 2014-03-26 | 2015-10-01 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF |
| CN106536535A (zh) | 2014-06-02 | 2017-03-22 | 葛兰素史密斯克莱知识产权（第2 号）有限公司 | 结晶的β‑D‑烟酰胺核苷的制备和用途 |
| WO2015186114A1 (en) | 2014-06-06 | 2015-12-10 | Glaxosmithkline Intellectual Property (No.2) Limited | Nicotinamide riboside analogs and pharmaceutical compositions and uses thereof |
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| 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 |
| JP7526673B2 (ja) | 2018-02-20 | 2024-08-01 | インサイト・コーポレイション | がんを治療するためのｈｐｋ１阻害剤としてのｎ－（フェニル）－２－（フェニル）ピリミジン－４－カルボキサミド誘導体及び関連化合物 |
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| KR20220059480A (ko) | 2019-08-06 | 2022-05-10 | 인사이트 코포레이션 | 고체 형태의 hpk1 억제제 |
| EP4514768A4 (en) * | 2022-04-29 | 2026-04-08 | Univ Michigan Regents | SMALL SIRTUIN INHIBITING MOLECULES AND THEIR USES |
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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 UY UY31169A patent/UY31169A1/es not_active Application Discontinuation
- 2008-06-20 MX MX2009013977A patent/MX2009013977A/es active IP Right Grant
- 2008-06-20 KR KR1020107000400A patent/KR20100051048A/ko not_active Ceased
- 2008-06-20 PE PE2008001058A patent/PE20090694A1/es not_active Application Discontinuation
- 2008-06-20 CN CN200880103654A patent/CN101801981A/zh active Pending
- 2008-06-20 JP JP2010513267A patent/JP5498940B2/ja not_active Expired - Fee Related
- 2008-06-20 US US12/214,805 patent/US7893086B2/en not_active Expired - Fee Related
- 2008-06-20 EP EP08768700A patent/EP2170905A2/en not_active Withdrawn
- 2008-06-20 BR BRPI0813651-3A2A patent/BRPI0813651A2/pt not_active IP Right Cessation
- 2008-06-20 WO PCT/US2008/007776 patent/WO2008156869A2/en not_active Ceased
- 2008-06-20 EA EA201070035A patent/EA018922B1/ru not_active IP Right Cessation
- 2008-06-20 AR ARP080102663A patent/AR067107A1/es not_active Application Discontinuation
- 2008-06-20 AU AU2008266749A patent/AU2008266749C1/en not_active Ceased
- 2008-06-20 CN CN201310744228.7A patent/CN103833775A/zh active Pending
- 2008-06-20 NZ NZ581990A patent/NZ581990A/en not_active IP Right Cessation
- 2008-06-20 CA CA002691733A patent/CA2691733A1/en not_active Abandoned
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2009
- 2009-12-11 DO DO2009000284A patent/DOP2009000284A/es unknown
- 2009-12-14 ZA ZA200908883A patent/ZA200908883B/xx unknown
- 2009-12-14 IL IL202730A patent/IL202730A0/en unknown
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2010
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- 2010-01-08 CO CO10001887A patent/CO6251248A2/es not_active Application Discontinuation
- 2010-01-20 CR CR11232A patent/CR11232A/es not_active Application Discontinuation
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2011
- 2011-01-24 US US13/012,775 patent/US8268862B2/en not_active Expired - Fee Related
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