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1. 发明申请

WO2011033307A1 NILOTINIB DIHYDROCHLORIDE SALT 审中-公开
标题翻译： NILOTINIB DIHYDROCHLORIDE盐
公开(公告)号：WO2011033307A1
公开(公告)日：2011-03-24
申请号：PCT/GB2010/051556
申请日：2010-09-16
申请人： GENERICS [UK] LIMITED , MYLAN INDIA PRIVATE LIMITED , GORE, Vinayak Govind , PATKAR, Laxmikant , BAGUL, Amit , PRIYESH, Vijaykar , EDAKE, Mahesh
发明人： GORE, Vinayak Govind , PATKAR, Laxmikant , BAGUL, Amit , PRIYESH, Vijaykar , EDAKE, Mahesh
IPC分类号： C07D401/14
CPC分类号： C07D401/14
摘要： The present invention relates to nilotinib dihydrochloride and its hydrates, to methods for preparing nilotinib dihydrochloride and its hydrates, pharmaceutical compositions comprising nilotinib dihydrochloride and its hydrates, and methods of treatment using the same.
摘要翻译：本发明涉及尼罗替尼二盐酸盐及其水合物，制备尼罗替尼二盐酸盐及其水合物的方法，包含尼洛替尼二盐酸盐及其水合物的药物组合物及其使用方法。

2. 发明申请

WO2011067588A1 CYCLIC SULPHINYL ESTERS OF CYTIDINE 审中-公开
标题翻译： CYTIDINE的CYCLIC SULPHINYLESTERS
公开(公告)号：WO2011067588A1
公开(公告)日：2011-06-09
申请号：PCT/GB2010/051994
申请日：2010-11-30
申请人： GENERICS [UK] LIMITED , MYLAN INDIA PRIVATE LIMITED , GORE, Vinayak Govind , PATKAR, Laxmikant , BAGUL, Amit , EDAKE, Mahesh
发明人： GORE, Vinayak Govind , PATKAR, Laxmikant , BAGUL, Amit , EDAKE, Mahesh
IPC分类号： C07H19/06
CPC分类号： C07H19/06
摘要： The present invention relates to novel intermediates and to an improved process for the preparation of N- functionalised cytidine derivatives such as capecitabine, galocitabine and sapacitabine. Said intermediates are se from a copound of formula (A- 2), (A-3), (A-6), (A-7). wherein: R 1 and R 3 arc each independendy selected from hydrogen, -F, -CI, -Br, -I, -CN, -NO 2 , -N 3 , -O-R 7 , -S-R 7 , -N(R 7 ) 2 , -N(R 7 ) 3 + or -0-Si(R 7 ) 3 ; R 4 and R 5 arc each independendy selected from hydrogen, -F, -CI, -Br and -I; R 6 is selected from an alkyl, alkenyl, alkynyl, atyl, aiylalkyl, arylalkenyl, arylalkynyl, alkylaiyl, alkenylaryl or alkynylaryl group, each of which may optionally be substituted, and each of which may optionally include one or more heteroatoms N, O or S in its carbon skeleton; and each R 7 is independendy selected from hydrogen, or an alkyl, alkenyl, alkynyl, atyl, aiylalkyl, arylalkenyl, arylalkynyl, alkylaiyl, alkenylaryl or alkynylaryl group, each of which may optionally he substituted, and each of which may optionally include one or more heteroatoms N, O or S in its carbon skeleton, and wherein any two or more R 7 groups may, together with rhe atom or atoms to which they are attached, form a cyclic alkyl, alkenyl, alkynyl, aryl, aiylalkyl, arylalkcnyl, arylalkynyl, alkylaiyl, alkenylaryl or alkynylaryl group, each of which may optionally be substituted, and each of which may optionally include one or more heteroatoms N, O or S in its carbon skeleton.
摘要翻译：本发明涉及新型中间体以及用于制备N-功能化胞苷衍生物如卡培他滨，乙酰西他滨和西他滨的改进方法。所述中间体是式（A-2），（A-3），（A-6），（A-7）的组合物。其中：R 1和R 3各自独立地选自氢，-F，-C 1，-Br，-I，-CN，-NO 2，-N 3，-O-R 7，-S-R 7，-N（R 7） -N（R 7）3+或-O-Si（R 7）3; R4和R5各自独立地选自氢，-F，-CI，-Br和-I; R 6选自烷基，烯基，炔基，芳基，芳基烷基，芳基烯基，芳基炔基，烷基亚烷基，烯基芳基或炔基芳基，其各自可任选被取代，并且其各自可以任选地包括一个或多个杂原子N，O或S 在其碳骨架; 并且每个R 7独立地选自氢或烷基，烯基，炔基，芳基，芳基烷基，芳基烯基，芳基炔基，烷基亚烷基，烯基芳基或炔基芳基，其各自可以任选地被它取代，并且它们各自可以任选地包括一个或多个杂原子N，O或S在其碳骨架中，并且其中任何两个或更多个R 7基团可以与它们所连接的转原子或原子一起形成环烷基，烯基，炔基，芳基，芳基烷基，芳基炔基，芳基炔基，烷基亚烷基，烯基芳基或炔基芳基，其各自可任选被取代，并且其各自可以任选地在其碳骨架中包含一个或多个杂原子N，O或S。

3. 发明申请

WO2010139981A3 PROCESSES FOR PREPARING CRYSTALLINE FORMS OF DASATINIB 审中-公开
公开(公告)号：WO2010139981A3
公开(公告)日：2010-12-09
申请号：PCT/GB2010/050894
申请日：2010-05-28
申请人： GENERICS [UK] LIMITED , MYLAN INDIA PRIVATE LIMITED , GORE, Vinayak Govind , PATKAR, Laxmikant , BAGUL, Amit , VIJAYKAR, Priyesh Surendra , EDAKE, Mahesh
发明人： GORE, Vinayak Govind , PATKAR, Laxmikant , BAGUL, Amit , VIJAYKAR, Priyesh Surendra , EDAKE, Mahesh
IPC分类号： C07D417/12 , A61K31/506 , A61P35/00
摘要： The present invention relates to processes for the preparation of dasatinib and to crystalline monohydrate and anhydrous polymorphic forms of dasatinib. The invention further relates to pure polymorphs, to pharmaceutical compositions comprising said polymorphs and to uses thereof.

4. 发明申请

WO2010139980A1 PROCESS FOR PREPARING CRYSTALLINE DASATINIB MONOHYDRATE 审中-公开
标题翻译：用于制备结晶DASATINIB MONOHTHDRATE的方法
公开(公告)号：WO2010139980A1
公开(公告)日：2010-12-09
申请号：PCT/GB2010/050893
申请日：2010-05-28
申请人： GENERICS [UK] LIMITED , MYLAN INDIA PRIVATE LIMITED , GORE, Vinayak Govind , PATKAR, Laxmikant , BAGUL, Amit , VIJAYKAR, Priyesh Surendra , EDAKE, Mahesh
发明人： GORE, Vinayak Govind , PATKAR, Laxmikant , BAGUL, Amit , VIJAYKAR, Priyesh Surendra , EDAKE, Mahesh
IPC分类号： C07D417/12 , A61K31/506 , A61P35/00
CPC分类号： C07D417/12
摘要： The present invention relates to processes for the preparation of crystalline N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5- thiazolecarboxamide (dasatinib) monohydrate. The invention further relates to pure polymorphs, to pharmaceutical compositions comprising said polymorphs and to uses thereof.
摘要翻译：本发明涉及制备结晶的N-（2-氯-6-甲基苯基）-2 - [[6- [4-（2-羟乙基）-1-哌嗪基] -2-甲基-4-嘧啶基 ]氨基] -5-噻唑烷酰胺（达沙替尼）一水合物。本发明还涉及纯多晶型物，包含所述多晶型物的药物组合物及其用途。

5. 发明申请

WO2010139979A3 PROCESSES FOR PREPARING CRYSTALLINE FORMS OF DASATINIB 审中-公开
公开(公告)号：WO2010139979A3
公开(公告)日：2010-12-09
申请号：PCT/GB2010/050892
申请日：2010-05-28
申请人： GENERICS [UK] LIMITED , MYLAN INDIA PRIVATE LIMITED , GORE, Vinayak Govind , PATKAR, Laxmikant , BAGUL, Amit , VIJAYKAR, Priyesh Surendra , EDAKE, Mahesh
发明人： GORE, Vinayak Govind , PATKAR, Laxmikant , BAGUL, Amit , VIJAYKAR, Priyesh Surendra , EDAKE, Mahesh
IPC分类号： C07D417/12 , A61K31/506 , A61P35/00
摘要： The present invention relates to intermediates and their preparation, for use in the manufacture of pure dasatinib, in particularly dasatinib monohydrate and anhydrous dasatinib. The invention also relates to pharmaceutical compositions comprising pure dasatinib and their use in the treatment of cancer.

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