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 |
|---|---|---|---|---|
| CA2618370A1 (en) * | 2005-08-04 | 2007-02-15 | Sirtris Pharmaceuticals, Inc. | Oxazolopyridine derivatives as sirtuin modulators |
| WO2007041643A1 (en) * | 2005-10-03 | 2007-04-12 | University Of Tennessee Research Foundation | Dietary calcium for reducing the production of reactive oxygen species |
| CL2008001821A1 (es) | 2007-06-20 | 2009-03-13 | Sirtris Pharmaceuticals Inc | Compuestos derivados de imidazo[2,1-b]-tiazol; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de diabetes, sindrome metabolico, resistencia a la insulina, entre otras. |
| 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. |
| 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 |
| US8293747B2 (en) * | 2007-07-19 | 2012-10-23 | Merck Sharp & Dohme Corp. | Heterocyclic amide compounds as protein kinase inhibitors |
| CN101910184A (zh) * | 2007-11-08 | 2010-12-08 | 西特里斯药业公司 | 可溶性噻唑并吡啶 |
| JP5425891B2 (ja) | 2008-05-01 | 2014-02-26 | 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 | サーチュイン調節薬としてのキノリンおよび関連する類似体 |
| AU2009266889B2 (en) | 2008-07-03 | 2013-05-02 | Glaxosmithkline Llc | Benzimidazoles and related analogs as sirtuin modulators |
| CN102227420B (zh) | 2008-09-29 | 2015-06-24 | 西特里斯药业公司 | 作为沉默调节蛋白调节剂的喹唑啉酮、喹诺酮和相关的类似物 |
| WO2010077642A1 (en) | 2008-12-08 | 2010-07-08 | Northwestern University | Method of modulating hsf-1 |
| JP5628828B2 (ja) | 2008-12-19 | 2014-11-19 | 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 | チアゾロピリジンサーチュイン調節化合物 |
| US9556201B2 (en) | 2009-10-29 | 2017-01-31 | Glaxosmithkline Llc | Bicyclic pyridines and analogs as sirtuin modulators |
| CA2794018C (en) * | 2010-03-24 | 2016-05-10 | Medical University Of South Carolina | Compositions and methods for the treatment of degenerative diseases |
| WO2011130595A2 (en) * | 2010-04-15 | 2011-10-20 | Sirtris Pharmaceuticals, Inc. | Sirtuin activators and activation assays |
| RU2693462C2 (ru) * | 2010-05-03 | 2019-07-03 | Курна, Инк. | Лечение заболеваний, связанных с сиртуином (sirt), путем ингибирования природного антисмыслового транскрипта к сиртуину (sirt) |
| 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 |
| EP2670404B1 (en) | 2011-02-02 | 2018-08-29 | The Trustees of Princeton University | Sirtuin modulators as virus production modulators |
| KR101329524B1 (ko) | 2011-05-23 | 2013-11-13 | 연세대학교 산학협력단 | 미분화 전능성 줄기세포의 선택적 세포사멸 방법 |
| PH12014500198A1 (en) | 2011-07-15 | 2017-02-10 | Nusirt Sciences Inc | Compositions and methods for modulating metabolic pathways |
| WO2013036720A1 (en) | 2011-09-07 | 2013-03-14 | Cornell University | Methods for treatment of cancer by targeting sirt5 |
| 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 |
| JP6469015B2 (ja) | 2012-11-13 | 2019-02-13 | ニューサート サイエンシーズ, インコーポレイテッド | エネルギー代謝を増大させるための組成物および方法 |
| US9585876B2 (en) | 2013-03-15 | 2017-03-07 | Nusirt Sciences, Inc. | Leucine and nicotinic acid reduces lipid levels |
| JP2017506651A (ja) | 2014-02-27 | 2017-03-09 | ニューサート サイエンシーズ, インコーポレイテッド | 脂肪肝の低減または予防のための組成物および方法 |
| WO2015143654A1 (en) * | 2014-03-26 | 2015-10-01 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF |
| WO2015186068A1 (en) | 2014-06-02 | 2015-12-10 | Glaxosmithkline Intellectual Property (No.2) Limited | Preparation and use of crystalline beta-d-nicotinamide riboside |
| RU2016149767A (ru) | 2014-06-06 | 2018-07-16 | Глэксосмитклайн Интеллекчуал Проперти (Но.2) Лимитед | Аналоги никотинамидрибозида и фармацевтические композиции и их применение |
| WO2018049214A1 (en) | 2016-09-09 | 2018-03-15 | Incyte Corporation | Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer |
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| JP2021501198A (ja) * | 2017-10-27 | 2021-01-14 | トランスフュージョン ヘルス,リミティド ライアビリティ カンパニー | フルオレンの誘導体を用いて造血幹細胞を増殖する組成物および方法 |
| US10800761B2 (en) | 2018-02-20 | 2020-10-13 | Incyte Corporation | Carboxamide compounds and uses thereof |
| US10899755B2 (en) | 2018-08-08 | 2021-01-26 | Incyte Corporation | Benzothiazole compounds and uses thereof |
| PE20221419A1 (es) | 2019-08-06 | 2022-09-20 | Incyte Corp | Formas solidas de un inhibidor de hpk1 |
| 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 CA CA002691733A patent/CA2691733A1/en not_active Abandoned
- 2008-06-20 AR ARP080102663A patent/AR067107A1/es not_active Application Discontinuation
- 2008-06-20 MX MX2009013977A patent/MX2009013977A/es active IP Right Grant
- 2008-06-20 CN CN200880103654A patent/CN101801981A/zh active Pending
- 2008-06-20 WO PCT/US2008/007776 patent/WO2008156869A2/en not_active Ceased
- 2008-06-20 AU AU2008266749A patent/AU2008266749C1/en not_active Ceased
- 2008-06-20 US US12/214,805 patent/US7893086B2/en not_active Expired - Fee Related
- 2008-06-20 KR KR1020107000400A patent/KR20100051048A/ko not_active Ceased
- 2008-06-20 JP JP2010513267A patent/JP5498940B2/ja not_active Expired - Fee Related
- 2008-06-20 BR BRPI0813651-3A2A patent/BRPI0813651A2/pt not_active IP Right Cessation
- 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 EP EP08768700A patent/EP2170905A2/en not_active Withdrawn
- 2008-06-20 EA EA201070035A patent/EA018922B1/ru not_active IP Right Cessation
- 2008-06-20 PE PE2008001058A patent/PE20090694A1/es not_active Application Discontinuation
- 2008-06-20 UY UY31169A patent/UY31169A1/es not_active Application Discontinuation
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2009
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- 2009-12-14 IL IL202730A patent/IL202730A0/en unknown
- 2009-12-14 ZA ZA200908883A patent/ZA200908883B/xx unknown
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2010
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- 2010-01-08 CO CO10001887A patent/CO6251248A2/es not_active Application Discontinuation
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