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21. 发明申请

WO2011061545A1 HPLC METHOD FOR ANALYZING VORINOSTAT 审中-公开
标题翻译：用于分析VORINOSTAT的HPLC方法
公开(公告)号：WO2011061545A1
公开(公告)日：2011-05-26
申请号：PCT/GB2010/051931
申请日：2010-11-20
申请人： GENERICS [UK] LIMITED , MYLAN INDIA PRIVATE LIMITED , VIJAYAKUMAR, Erra, Koteswara, Satya , VELE, Vinayak , SINGH, Manish , VISHE, Sachin
发明人： VIJAYAKUMAR, Erra, Koteswara, Satya , VELE, Vinayak , SINGH, Manish , VISHE, Sachin
IPC分类号： G01N30/34 , G01N30/36 , A61K31/19
CPC分类号： G01N30/36 , A61K31/19 , G01N30/34
摘要： The current invention relates to new HPLC methods for the analysis of the drug substance vorinostat and related substances. In a first method the mobile phase comprises two or more liquids and the relative concentration of the liquids is varied to a predetermined gradient. In a second method the mobile phase comprises an alcohol. In a third method the mobile phase comprises a phosphate salt, a phosphoric acid or an anhydride thereof. The current invention also relates to a method for analysing a substance, comprising the detection and optional quantification of one or more specific impurities. The current invention further relates to the use of specific substances as reference standards and markers, and to vorinostat and associated pharmaceutical compositions that have been analysed by the methods of the current invention and/or are substantially free of specific impurities.
摘要翻译：本发明涉及用于分析药物物质伏立诺他胺及相关物质的新型HPLC方法。在第一种方法中，流动相包含两种或更多种液体，液体的相对浓度变化到预定的梯度。在第二种方法中，流动相包含醇。在第三种方法中，流动相包含磷酸盐，磷酸或其酸酐。本发明还涉及用于分析物质的方法，包括检测和任选地定量一种或多种特定杂质。本发明还涉及特定物质作为参考标准物和标记物的用途，以及通过本发明的方法分析和/或基本上不含特定杂质的伏立诺他胺和相关药物组合物。

22. 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。

23. 发明申请

WO2011004200A1 NOVEL PYRROLE DERIVATIVES 审中-公开
标题翻译：新颖的红宝石衍生物
公开(公告)号：WO2011004200A1
公开(公告)日：2011-01-13
申请号：PCT/GB2010/051134
申请日：2010-07-09
申请人： GENERICS [UK] LIMITED , MYLAN INDIA PRIVATE LIMITED , GORE, Vinayak, Govind , PATKAR, Laxmikant , HUBLIKAR, Mahesh, Gorakhnath , MANDE, Hemant , POKHARKAR, Kiran, Shivaji , BANSODE, Prakash
发明人： GORE, Vinayak, Govind , PATKAR, Laxmikant , HUBLIKAR, Mahesh, Gorakhnath , MANDE, Hemant , POKHARKAR, Kiran, Shivaji , BANSODE, Prakash
IPC分类号： C07D207/34 , C07D403/06
CPC分类号： C07D403/06 , C07D207/34
摘要： The present invention relates to novel salts of pyrrole derivatives, their preparation and their use in the preparation of sunitinib salts, in particular sunitinib malate (IIa), and sunitinib base. The invention also relates to compositions comprising sunitinib salts or sunitinib base and the use of these compositions in the treatment of cancer.
摘要翻译：本发明涉及吡咯衍生物的新型盐，其制备方法及其在制备舒尼替尼盐，特别是苹果酸舒尼替尼（IIa）和舒尼替尼碱中的用途。本发明还涉及包含舒尼替尼盐或舒尼替尼碱的组合物以及这些组合物在治疗癌症中的用途。

24. 发明申请

WO2010131035A8 NOVEL CRYSTALLINE POLYMORPH OF SITAGLIPTIN DIHYDROGEN PHOSPHATE 审中-公开
公开(公告)号：WO2010131035A8
公开(公告)日：2010-11-18
申请号：PCT/GB2010/050772
申请日：2010-05-11
申请人： GENERICS [UK] LIMITED , MYLAN INDIA PRIVATE LIMITED , GORE, Vinayak Govind , GADAKAR, Maheshkumar , BHOSLE, Priyanka , SHINDE, Suresh , YADAV, Prashant
发明人： GORE, Vinayak Govind , GADAKAR, Maheshkumar , BHOSLE, Priyanka , SHINDE, Suresh , YADAV, Prashant
IPC分类号： C07D487/04 , A61K31/4985 , A61P3/10
摘要： The present invention relates to a novel anhydrous crystalline form of sitagliptin dihydrogenphosphate (I), to processes for its preparation and to its use in pharmaceutical compositions.

25. 发明申请

WO2009122215A1 NOVEL PROCESS 审中-公开
标题翻译：新进程
公开(公告)号：WO2009122215A1
公开(公告)日：2009-10-08
申请号：PCT/GB2009/050326
申请日：2009-04-02
申请人： GENERICS [UK] LIMITED , MYLAN INDIA PRIVATE LIMITED , GORE, Vinayak , DATTA, Debashish , GADAKAR, Maheshkumar , POKHARKAR, Kiran , MANKAR, Viraj , WAVHAL, Sneha
发明人： GORE, Vinayak , DATTA, Debashish , GADAKAR, Maheshkumar , POKHARKAR, Kiran , MANKAR, Viraj , WAVHAL, Sneha
IPC分类号： C07C227/34 , C07C229/08
CPC分类号： C07C227/34 , C07C229/08
摘要： The present invention relates to a novel process of preparing an enantiomerically enriched γ-amino acid, such as enantiomerically enriched (S)-pregabalin.
摘要翻译：本发明涉及制备对映异构体富集的β-氨基酸的新方法，例如对映体富集（S） - 普瑞巴林。

26. 发明申请

WO2011104540A1 ONE STEP PROCESS FOR THE PREPARATION OF CAPECITABINE 审中-公开
标题翻译：一步法制备CAPECITABINE
公开(公告)号：WO2011104540A1
公开(公告)日：2011-09-01
申请号：PCT/GB2011/050351
申请日：2011-02-23
申请人： GENERICS [UK] LIMITED , MYLAN INDIA PRIVATE LIMITED , GORE, Vinayak Govind , PATKAR, Laxmikant Narahari , BHALERAO, Rahul , HUBLIKAR, Mahesh Gorakhnath , POKHARKAR, Kiran Shivaji
发明人： GORE, Vinayak Govind , PATKAR, Laxmikant Narahari , BHALERAO, Rahul , HUBLIKAR, Mahesh Gorakhnath , POKHARKAR, Kiran Shivaji
IPC分类号： C07H19/067
CPC分类号： C07H19/067
摘要： The present invention relates a one step process for the preparation of capecitabine and analogues thereof, such as galocitabine, sapacitabine, 5'-deoxy-5-fiuoro-N- [(cyclohexyloxy)carbonyl]cytidine, and N-[(heptyloxy)carbonyl]cytarabine.
摘要翻译：本发明涉及一种制备卡培他滨及其类似物的方法，例如，依莫沙星，西他滨，5'-脱氧-5-氟-N - [（环己基氧基）羰基]胞苷和N - [（庚氧基）羰基 ]阿糖胞苷。

27. 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。

28. 发明申请

WO2011064574A1 HPLC METHOD FOR DETECTING LENALIDOMIDE 审中-公开
标题翻译：用于检测百里香糖苷的HPLC方法
公开(公告)号：WO2011064574A1
公开(公告)日：2011-06-03
申请号：PCT/GB2010/051951
申请日：2010-11-23
申请人： VIJAYAKUMAR, Erra Koteswara Satya , TAKALE, Santosh , SINGH, Manish , GENERICS [UK] LIMITED , MYLAN INDIA PRIVATE LIMITED
发明人： VIJAYAKUMAR, Erra Koteswara Satya , TAKALE, Santosh , SINGH, Manish
IPC分类号： G01N30/36 , G01N30/34 , G01N30/96 , A61K31/00 , A61K31/40 , A61K31/4035 , A61K31/445
CPC分类号： G01N30/96 , A61K31/00 , A61K31/40 , A61K31/4035 , A61K31/445 , G01N30/34 , G01N30/36
摘要： The present invention relates to new HPLC methods for the analysis of the drug substance lenaliclomide and related substances. In a first method the mobile phase comprises two or mote liquids and the relative concentration of the liquids is varied to a predetermined gradient. In a second method the mobile phase comprises formic acid, a formate salt or a mixture thereof. The current invention also relates to lenalidomide and associated pharmaceutical compositions that have been analysed by the methods of the current invention and/or are substantially free of specific impurities.
摘要翻译：本发明涉及用于分析药物物质lenaliclomide和相关物质的新的HPLC方法。在第一种方法中，流动相包括两种或多种液体，液体的相对浓度变化到预定的梯度。在第二种方法中，流动相包括甲酸，甲酸盐或其混合物。本发明还涉及已经通过本发明的方法分析和/或基本上不含特定杂质的来那度塞和相关的药物组合物。

29. 发明申请

WO2011015883A1 DICHLOROMETHANE SOLVATE OF TIOTROPIUM BROMIDE AND ITS USE 审中-公开
标题翻译：二氯甲烷溶解二氧化氯及其用途
公开(公告)号：WO2011015883A1
公开(公告)日：2011-02-10
申请号：PCT/GB2010/051311
申请日：2010-08-06
申请人： GENERICS [UK] LIMITED , MYLAN INDIA PRIVATE LIMITED , GORE, Vinayak Govind , MANOJKUMAR, Bindu , SHINDE, Dattatraya , KOKANE, Dattatrey
发明人： GORE, Vinayak Govind , MANOJKUMAR, Bindu , SHINDE, Dattatraya , KOKANE, Dattatrey
IPC分类号： C07D451/10 , A61K31/46 , A61P11/06
CPC分类号： C07D451/10
摘要： The present invention relates to a novel solvate of tiotropiumbromide, a process to prepare this solvate and the use of this and other solvates in processes for the preparation of anhydrous tiotropium bromide. The present invention also relates to pharmaceutical compositions comprising anhydrous tiotropium bromide and uses of the compositions.
摘要翻译：本发明涉及噻托溴铵的新型溶剂化物，制备该溶剂化物的方法以及该制备无水噻托溴铵的方法中该溶剂化物和其它溶剂化物的用途。本发明还涉及包含无水噻托溴铵和组合物的用途的药物组合物。

30. 发明申请

WO2010013048A1 POLYMORPHIC FORM OF RASAGILINE MESYLATE 审中-公开
标题翻译：硅藻土的多晶型
公开(公告)号：WO2010013048A1
公开(公告)日：2010-02-04
申请号：PCT/GB2009/050941
申请日：2009-07-29
申请人： GENERICS [UK] LIMITED , MYLAN INDIA PRIVATE LIMITED , GORE, Vinayak , MANOJKUMAR, Bindu , SONAWANE, Sandeep , KOKANE, Dattatrey , TANK, Sinderpal
发明人： GORE, Vinayak , MANOJKUMAR, Bindu , SONAWANE, Sandeep , KOKANE, Dattatrey , TANK, Sinderpal
IPC分类号： C07C211/42 , C07C309/04 , A61P25/16 , A61K31/135
CPC分类号： C07C211/42 , C07B2200/13 , C07C309/04 , C07C2602/08
摘要： The present invention relates to a novel crystalline form of rasagiline mesylate and a pure form of rasagiline mesylate and processes for their preparation. Further, the invention relates to pharmaceutical compositions comprising said forms and use of said compositions in the treatment of patients suffering from Parkinson's Disease, dementia, Alzheimer's Disease, depression, hyperactive syndrome, stroke, brain ischemia, neurotrauma, schizophrenia and multiple sclerosis.
摘要翻译：本发明涉及甲磺酸雷沙吉兰和纯甲磺酸雷沙吉兰的新型结晶形式及其制备方法。此外，本发明涉及包含所述形式的所述形式的药物组合物和所述组合物在治疗患有帕金森病，痴呆，阿尔茨海默氏病，抑郁症，多动症综合征，中风，脑缺血，神经营养不良，精神分裂症和多发性硬化症的患者中的用途。

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