CN101258149B - 噻唑衍生物及其应用 - Google Patents
噻唑衍生物及其应用 Download PDFInfo
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- CN101258149B CN101258149B CN2006800270305A CN200680027030A CN101258149B CN 101258149 B CN101258149 B CN 101258149B CN 2006800270305 A CN2006800270305 A CN 2006800270305A CN 200680027030 A CN200680027030 A CN 200680027030A CN 101258149 B CN101258149 B CN 101258149B
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- BFARCRHWIUKSFT-UHFFFAOYSA-N CC(Nc([s]1)nc(C)c1I)=O Chemical compound CC(Nc([s]1)nc(C)c1I)=O BFARCRHWIUKSFT-UHFFFAOYSA-N 0.000 description 1
- DUEYALCGWXEBKG-UHFFFAOYSA-N CC(Nc1nc(C)c(-c([s]2)ccc2S(N(CC2)CCC2O)(=O)=O)[s]1)=O Chemical compound CC(Nc1nc(C)c(-c([s]2)ccc2S(N(CC2)CCC2O)(=O)=O)[s]1)=O DUEYALCGWXEBKG-UHFFFAOYSA-N 0.000 description 1
- XKFUSJFEAVNFIR-UHFFFAOYSA-N CC(Nc1nc(C)c(-c2ccc(N)[s]2)[s]1)=O Chemical compound CC(Nc1nc(C)c(-c2ccc(N)[s]2)[s]1)=O XKFUSJFEAVNFIR-UHFFFAOYSA-N 0.000 description 1
- WUDMILNJRHIHKJ-HZMBPMFUSA-N C[C@@H]1[C@@H](c2c(C)nc(NC(C)=O)[s]2)SC(CNCC=C)=CC1 Chemical compound C[C@@H]1[C@@H](c2c(C)nc(NC(C)=O)[s]2)SC(CNCC=C)=CC1 WUDMILNJRHIHKJ-HZMBPMFUSA-N 0.000 description 1
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Abstract
Description
实施例 序号 | 化学名称 |
1 | N-[5-(5-甲酰基-2-噻吩基)-4-甲基-1,3-噻唑-2-基]乙酰胺; |
2 | N-(5-{5-[(烯丙氨基)甲基]-2-噻吩基}-4-甲基-1,3-噻唑-2-基)乙酰胺; |
3 | N-{5-[5-(羟甲基)-2-噻吩基]-4-甲基-1,3-噻唑-2-基}乙酰胺; |
4 | 5-[2-(乙酰氨基)-4-甲基-1,3-噻唑-5-基]噻吩-2-羧酸; |
5 | N-{4-甲基-5-[5-(吗啉-4-基-羰基)-2-噻吩基]-1,3-噻唑-2-基}乙酰胺; |
6 | N-[4-甲基-5-(2-噻吩基)-1,3-噻唑-2-基]乙酰胺; |
实施例 序号 | 化学名称 |
7 | N-(5-{5-[(4-羟基哌啶-1-基)羰基]-2-噻吩基}-4-甲基-1,3-噻唑-2-基)乙酰 胺; |
8 | N-(5-{5-[(3-羟基哌啶-1-基)羰基]-2-噻吩基}-4-甲基-1,3-噻唑-2-基)乙酰 胺; |
9 | N-(5-{5-[(3-羟基哌啶-1-基)磺酰基]-2-噻吩基}-4-甲基-1,3-噻唑-2-基)乙 酰胺; |
10 | N-(5-{5-[(4-羟基哌啶-1-基)磺酰基]-2-噻吩基}-4-甲基-1,3-噻唑-2-基)乙 酰胺; |
11 | N-[5-(5-{[(2-羟乙基)氨基]磺酰基}-2-噻吩基)-4-甲基-1,3-噻唑-2-基]乙酰 胺; |
12 | N-(5-{5-[(烯丙氨基)磺酰基]-2-噻吩基}-4-甲基-1,3-噻唑-2-基)乙酰胺; |
13 | N-{4-甲基-5-[5-(吗啉-4-基-磺酰基)-2-噻吩基]-1,3-噻唑-2-基}乙酰胺; |
14 | N-(5-{5-[(E)-(羟基亚氨基)甲基]-2-噻吩基}-4-甲基-1,3-噻唑-2-基)乙酰 胺; |
15 | N-[5-(5-氰基-2-噻吩基)-4-甲基-1,3-噻唑-2-基]乙酰胺; |
16 | 5-[2-(乙酰氨基)-4-甲基-1,3-噻唑-5-基]噻吩-2-羧酸甲酯; |
17 | N-{5-[5-(氨基磺酰基)-2-噻吩基]-4-甲基-1,3-噻唑-2-基}乙酰胺; |
18 | N-{5-[5-(1,4-二氧杂-8-氮杂螺[4.5]癸烷-8-基-磺酰基)-2-噻吩基]-4-甲基- 1,3-噻唑-2-基}乙酰胺; |
19 | N-[4-甲基-5-(3-噻吩基)-1,3-噻唑-2-基]乙酰胺。 |
实施例序号 | PI3K IC50(μM) |
1 | 0.215 |
3 | 0.219 |
5 | 0.249 |
8 | 1.098 |
实施例实施例序号 | 细胞实验(P-Akt,Elisa) IC50[nM] |
12 | 322 |
实施例序号 | 抑制百分比% |
12 | 38 |
Claims (13)
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP05104418.8 | 2005-05-24 | ||
EP05104418 | 2005-05-24 | ||
US68626605P | 2005-06-01 | 2005-06-01 | |
US60/686,266 | 2005-06-01 | ||
PCT/EP2006/062602 WO2006125807A1 (en) | 2005-05-24 | 2006-05-24 | Thiazole derivatives and use thereof |
Publications (2)
Publication Number | Publication Date |
---|---|
CN101258149A CN101258149A (zh) | 2008-09-03 |
CN101258149B true CN101258149B (zh) | 2012-09-19 |
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Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN2006800270292A Active CN101304995B (zh) | 2005-05-24 | 2006-05-24 | 噻唑衍生物及其应用 |
CN2006800270305A Expired - Fee Related CN101258149B (zh) | 2005-05-24 | 2006-05-24 | 噻唑衍生物及其应用 |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN2006800270292A Active CN101304995B (zh) | 2005-05-24 | 2006-05-24 | 噻唑衍生物及其应用 |
Country Status (19)
Country | Link |
---|---|
US (4) | US7879888B2 (zh) |
EP (2) | EP1885716B1 (zh) |
JP (2) | JP5203937B2 (zh) |
KR (2) | KR20080015114A (zh) |
CN (2) | CN101304995B (zh) |
AU (2) | AU2006251161B2 (zh) |
BR (2) | BRPI0611176A2 (zh) |
CA (2) | CA2608153C (zh) |
DK (1) | DK1885716T3 (zh) |
EA (2) | EA014350B1 (zh) |
ES (1) | ES2399101T3 (zh) |
HK (1) | HK1121161A1 (zh) |
IL (2) | IL187391A (zh) |
MX (2) | MX2007014884A (zh) |
NO (2) | NO20076558L (zh) |
PT (1) | PT1885716E (zh) |
UA (2) | UA92489C2 (zh) |
WO (2) | WO2006125807A1 (zh) |
ZA (2) | ZA200710104B (zh) |
Families Citing this family (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TW200519106A (en) | 2003-05-02 | 2005-06-16 | Novartis Ag | Organic compounds |
JP5290751B2 (ja) | 2005-05-24 | 2013-09-18 | メルク セローノ ソシエテ アノニム | チアゾール誘導体及びそれらの使用 |
JP5203937B2 (ja) | 2005-05-24 | 2013-06-05 | メルク セローノ ソシエテ アノニム | チアゾール誘導体及びその使用 |
JP2009524677A (ja) * | 2006-01-25 | 2009-07-02 | シンタ ファーマシューティカルズ コーポレーション | 炎症および免疫関連使用用のチアゾールおよびチアジアゾール化合物 |
AR069798A1 (es) | 2007-12-20 | 2010-02-17 | Novartis Ag | Derivados de 1, 3-tiazol, metodos para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la manufactura de medicamentos para el tratamiento de enfermedades mediadas por la fosfatidilinositol 3-cinasa. |
UA104147C2 (uk) | 2008-09-10 | 2014-01-10 | Новартис Аг | Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань |
EP2440556A1 (en) * | 2009-06-10 | 2012-04-18 | Vertex Pharmaceuticals Incorporated | Inhibitors of phosphatidylinositol 3-kinase |
US8293753B2 (en) | 2009-07-02 | 2012-10-23 | Novartis Ag | Substituted 2-carboxamide cycloamino ureas |
EP2492269A4 (en) | 2009-10-19 | 2013-08-07 | Taisho Pharmaceutical Co Ltd | aminothiazole |
JP6236481B2 (ja) * | 2016-02-17 | 2017-11-22 | 東京エレクトロン株式会社 | パターン形成方法 |
RU2618622C1 (ru) * | 2016-03-22 | 2017-05-04 | Федеральное государственное бюджетное образовательное учреждение высшего профессионального образования "Курский государственный университет" | Способ фармакологической коррекции экспериментальной ишемии скелетной мышцы варденафилом и пентоксифиллином в условиях комбинированной терапии |
RU2618621C1 (ru) * | 2016-03-22 | 2017-05-04 | Федеральное государственное бюджетное образовательное учреждение высшего профессионального образования "Курский государственный университет" | Способ фармакологической коррекции экспериментальной ишемии скелетной мышцы силденафилом и пентоксифиллином в условиях комбинированной терапии |
RU2717104C1 (ru) * | 2019-06-26 | 2020-03-18 | Общество с ограниченной ответственностью "Иван-поле" | Способ получения алкил- и ацил-замещенных тиазолов |
Family Cites Families (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2008A (en) * | 1841-03-18 | Gas-lamp eok conducting gas pkom ah elevated buhner to one below it | ||
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US2009A (en) * | 1841-03-18 | Improvement in machines for boring war-rockets | ||
US4649146A (en) | 1983-01-31 | 1987-03-10 | Fujisawa Pharmaceutical Co., Ltd. | Thiazole derivatives and pharmaceutical composition comprising the same |
UA71971C2 (en) | 1999-06-04 | 2005-01-17 | Agoron Pharmaceuticals Inc | Diaminothiazoles, composition based thereon, a method for modulation of protein kinases activity, a method for the treatment of diseases mediated by protein kinases |
JP3892296B2 (ja) * | 1999-09-10 | 2007-03-14 | メルク エンド カムパニー インコーポレーテッド | チロシンキナーゼ阻害薬 |
WO2003048140A1 (fr) * | 2001-12-03 | 2003-06-12 | Japan Tobacco Inc. | Compose azole et utilisation medicinale de celui-ci |
US20030158199A1 (en) * | 2002-01-25 | 2003-08-21 | Kylix, B.V. | Novel compounds for inhibition of Tie-2 |
MY156407A (en) | 2002-02-28 | 2016-02-26 | Novartis Ag | 5-phenylthiazole derivatives and use as p13 kinase inhibitors |
WO2004033439A1 (en) * | 2002-10-09 | 2004-04-22 | Pfizer Products Inc. | Thiazole compounds for the treatment of neurodegenerative disorders |
US7262199B2 (en) * | 2002-12-11 | 2007-08-28 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
GB0305152D0 (en) * | 2003-03-06 | 2003-04-09 | Novartis Ag | Organic compounds |
TW200519106A (en) * | 2003-05-02 | 2005-06-16 | Novartis Ag | Organic compounds |
GB0320197D0 (en) * | 2003-08-28 | 2003-10-01 | Novartis Ag | Organic compounds |
GB0326601D0 (en) * | 2003-11-14 | 2003-12-17 | Novartis Ag | Organic compounds |
NZ548197A (en) * | 2004-01-12 | 2010-06-25 | Serono Lab | Thiazole derivatives and use thereof |
SE0402735D0 (sv) | 2004-11-09 | 2004-11-09 | Astrazeneca Ab | Novel compounds |
JP5203937B2 (ja) * | 2005-05-24 | 2013-06-05 | メルク セローノ ソシエテ アノニム | チアゾール誘導体及びその使用 |
JP5290751B2 (ja) * | 2005-05-24 | 2013-09-18 | メルク セローノ ソシエテ アノニム | チアゾール誘導体及びそれらの使用 |
EP1979346A1 (en) * | 2006-01-23 | 2008-10-15 | Laboratoires Serono S.A. | Thiazole derivatives and use thereof |
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