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。

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。

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).