专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20070179315A1 Methods of amination 失效
标题翻译：胺化方法
公开(公告)号：US20070179315A1
公开(公告)日：2007-08-02
申请号：US10593212
申请日：2005-03-18
申请人： Andrew Holmes , Catherine Smith , Melanie Tsang , Theresa Early , Richard Shute
发明人： Andrew Holmes , Catherine Smith , Melanie Tsang , Theresa Early , Richard Shute
IPC分类号： C07C209/00
CPC分类号： C07C227/08 , C07C209/10 , C07C213/02 , C07D207/325 , C07D207/327 , C07C211/55 , C07C217/92 , C07C229/60
摘要： A method of synthesizing a compound of formula I: comprising the step of reacting a moiety of formula II: with a moiety of formula III: in compressed carbon dioxide in the presence of a transition metal catalyst and a base, wherein L is a labile leaving group; RN1 is optionally substituted C5-20 aryl; RN2 is selected from optionally substituted C5-20aryl, optionally substituted C3-20 heterocyclyl, optionally substituted C3-7 alkyl, and optionally substituted sulfonyl; RN3 is selected from H and optionally substituted C1-7 alkyl, C3-20 heterocyclyl and C5-20 aryl; or RN2 and RN3 together with the nitrogen atom to which they are attached form optionally substituted nitrogen-containing C3-20 heterocylyl or C5-20 heteroaryl; and R1 R2 and R3 are independently selected from optionally substituted C1-7 alkyl, C5-20 aryl, C3-20 heterocyclyl, hydroxy, halo, amino and C1-7 alkoxy, or two of R1, R2 and R3, together with the silicon atom to which they are attached, may form a silicon containing C5-7 heterocyclyl group.
摘要翻译：合成式I化合物的方法：包括使式II部分与式III部分反应的步骤：在过渡金属催化剂和碱的存在下，在压缩二氧化碳中，其中L是不稳定的离去组; R 01是任选取代的C 5-20芳基; R N2选自任选取代的C 5-20芳基，任选取代的C 3-20杂环基，任选取代的C 3-8芳基， 7烷基和任选取代的磺酰基; R N 3选自H和任选取代的C 1-7 - 烷基，C 3-20 - 杂环基和C 5-20杂环基， / SUB>芳基; 或R N2和R N3与它们所连接的氮原子一起形成任选取代的含氮C 3-20异氰酸酯或C 5-20杂芳基; R 1和R 3独立地选自任选取代的C 1-7烷基，C 1 -C 6烷基，羟基，卤素，氨基和C 1-7 - 烷氧基，或者R 1，R 2，R 2， 1，R 2和R 3与它们所连接的硅原子一起可以形成含有C 5-7的硅， / SO 2杂环基。

2. 发明申请

US20060194843A1 3,4-Disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinase and glycogen synthase kinase-3 modulators 有权
公开(公告)号：US20060194843A1
公开(公告)日：2006-08-31
申请号：US11336599
申请日：2006-01-20
申请人： Valerio Berdini , Michael O'Brien , Maria Carr , Theresa Early , Adrian Gill , Gary Trewartha , Alison Woolford , Andrew Woodhead , Paul Wyatt
发明人： Valerio Berdini , Michael O'Brien , Maria Carr , Theresa Early , Adrian Gill , Gary Trewartha , Alison Woolford , Andrew Woodhead , Paul Wyatt
IPC分类号： A61K31/454 , A61K31/416 , A61K31/4152 , C07D403/02
CPC分类号： C07D231/38 , A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/416 , A61K31/4178 , A61K31/4196 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K45/06 , C04B35/632 , C07D231/14 , C07D231/40 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D453/02 , C07D471/04
摘要： The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C═O, NRg(C═O) or O(C═O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).

3. 发明申请

US20070135477A1 Benzimidazole derivatives and their use as protein kinases inhibitors 失效
标题翻译：苯并咪唑衍生物及其作为蛋白激酶抑制剂的用途
公开(公告)号：US20070135477A1
公开(公告)日：2007-06-14
申请号：US10564166
申请日：2004-07-05
申请人： Valerio Berdini , Michael O'Brien , Maria Carr , Theresa Early , Eva Navarro , Adrian Gill , Steven Howard , Gary Trewartha , Alison Woolford , Andrew Woodhead , Paul Wyatt
发明人： Valerio Berdini , Michael O'Brien , Maria Carr , Theresa Early , Eva Navarro , Adrian Gill , Steven Howard , Gary Trewartha , Alison Woolford , Andrew Woodhead , Paul Wyatt
IPC分类号： A61K31/4745 , A61K31/4184 , C07D403/04
CPC分类号： A61K31/5377 , A61K31/00 , A61K31/4184 , A61K45/06 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D513/04
摘要： The invention provides compounds of the formula (1): The compounds have activity against cyclin depdenent kinases, glycogen synthase kinase and Auroa kinases and are therefore useful to treat cancer and viral diseases.
摘要翻译：本发明提供式（1）化合物：该化合物对细胞周期蛋白依赖性激酶，糖原合酶激酶和Auroa激酶具有活性，因此可用于治疗癌症和病毒性疾病。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式