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91. 发明申请

WO2006048890A1 IMATINIB MESYLATE CRYSTAL FORM AND PROCESS FOR PREPARATION THEREOF 审中-公开
标题翻译： IMATINIB MESYLATE晶体形式及其制备方法
公开(公告)号：WO2006048890A1
公开(公告)日：2006-05-11
申请号：PCT/IN2005/000340
申请日：2005-10-20
申请人： SUN PHARMACEUTICAL INDUSTRIES LIMITED , PATEL, Hetalkumar, Virendrabhai , JANI, Raja, Jyotir , THENNATI, Rajamannar
发明人： PATEL, Hetalkumar, Virendrabhai , JANI, Raja, Jyotir , THENNATI, Rajamannar
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： The present invention provides crystalline imatinib mesylate in a non-needle shaped a-crystalline form. In one aspect the present invention provides crystalline form of imatinib mesylate, characterized in that the difference between the tapped and untapped density is less than 0.15 gm/ml. The present invention also provides a novel, simple viable process for preparation of crystalline imatinib mesylate of the present invention.
摘要翻译：本发明提供非针状a晶体形式的结晶伊马替尼甲磺酸盐。在一个方面，本发明提供甲磺酸伊马替尼的结晶形式，其特征在于，轻敲和未开发密度之间的差异小于0.15gm / ml。本发明还提供了制备本发明的结晶伊马替尼甲磺酸盐的新型简单可行的方法。

92. 发明申请

WO2005122698A2 NOVEL STABLE POLYMORPHIC FORMS OF AN ANTICONVULSANT 审中-公开
标题翻译：新的稳定的多形态的抗生素
公开(公告)号：WO2005122698A2
公开(公告)日：2005-12-29
申请号：PCT/IN2004/000447
申请日：2004-12-24
申请人： SUN PHARMACEUTICAL INDUSTRIES LIMITED , NATARAJAN, Muthukumaran , PATEL, Nileshkumar, Sureshbhai , BHATT, Mehul, Chandrakatbhai , KILARU, Srinivasu , THENNATI, Rajamannar
发明人： NATARAJAN, Muthukumaran , PATEL, Nileshkumar, Sureshbhai , BHATT, Mehul, Chandrakatbhai , KILARU, Srinivasu , THENNATI, Rajamannar
CPC分类号： C07D409/06
摘要： Stable polymorphic forms III, IV and substantially amorphous forms of an anticonvulsant, tiagabine hydrochloride.
摘要翻译：稳定的多晶型III，IV和基本无定形形式的抗惊厥药，盐酸噻加滨。

93. 发明申请

WO2005101982A2 A STABLE OPHTHALMIC COMPOSITION 审中-公开
标题翻译：稳定的眼科组合物
公开(公告)号：WO2005101982A2
公开(公告)日：2005-11-03
申请号：PCT/IN2005/000090
申请日：2005-03-24
申请人： SUN PHARMACEUTICAL INDUSTRIES LIMITED , BHOWMICK, Subhas, Balaram , SHAH, Shrenik, Popatlal , KHOPADE, Ajay
发明人： BHOWMICK, Subhas, Balaram , SHAH, Shrenik, Popatlal , KHOPADE, Ajay
IPC分类号： A61K31/407 , A61K47/38
CPC分类号： A61K31/407 , A61K9/0048 , A61K47/38
摘要： The present invention provides a stable ophthalmic composition comprising ketorolac or its pharmaceutically acceptable salts and one or more pharmaceutically acceptable excipient(s), wherein the said pharmaceutically acceptable excipient(s) is not tocophersolan, and the said ophthalmic composition is nonirritating to the eye.
摘要翻译：本发明提供一种稳定的眼用组合物，其包含酮咯酸或其药学上可接受的盐和一种或多种药学上可接受的赋形剂，其中所述药学上可接受的赋形剂不是生育酚，并且所述眼科组合物对眼睛无刺激。

94. 发明申请

WO2005074387A3 NOVEL CRYSTAL FORMS OF 4-[2-DI-N-PROPYLAMINO)ETHYL]-2 (3H)- INDOLONE HYDROCHLORIDE 审中-公开
公开(公告)号：WO2005074387A3
公开(公告)日：2005-08-18
申请号：PCT/IN2004/000439
申请日：2004-12-30
申请人： SUN PHARMACEUTICAL INDUSTRIES LIMITED , PATEL, Hetalkumar, Virendrabhai , DIPCHANDANI, Jitendra, Gopaldas , JANI, Raja, Jyotir , THENNATI, Rajamannar
发明人： PATEL, Hetalkumar, Virendrabhai , DIPCHANDANI, Jitendra, Gopaldas , JANI, Raja, Jyotir , THENNATI, Rajamannar
IPC分类号： C07D209/34
摘要： Crystal forms I and II of 4-[2-(di-n-propylamino)ethyl]2(3H)-indolone hydrochloride and the process for their preparation.

95. 发明申请

WO2005069742A2 CRYSTAL FORM II OF MEMANTINE HYDROCHLORIDE 审中-公开
标题翻译：盐酸氢氯化物的晶体形式II
公开(公告)号：WO2005069742A2
公开(公告)日：2005-08-04
申请号：PCT/IN2004/000386
申请日：2004-12-10
申请人： SUN PHARMACEUTICAL INDUSTRIES LIMITED , BORASE, Ashok, Punju , PERIYANDI, Nagarajan , KILARU, Srinivasu , THENNATI, Rajamannar
发明人： BORASE, Ashok, Punju , PERIYANDI, Nagarajan , KILARU, Srinivasu , THENNATI, Rajamannar
CPC分类号： C07C211/38 , C07C2603/74
摘要： Crystalline memantine hydrochloride with improved properties.
摘要翻译：结晶美金刚盐酸盐具有改善的性能。

96. 发明申请

WO2005039481A2 ORAL DRUG DELIVERY SYSTEM 审中-公开
标题翻译：口服药物递送系统
公开(公告)号：WO2005039481A2
公开(公告)日：2005-05-06
申请号：PCT/IN2004/000192
申请日：2004-06-30
申请人： SUN PHARMACEUTICAL INDUSTRIES LIMITED , DHARMADHIKARI, Nitin, Bhalachandra , ZALA, Yashoraj, Rupsinh , SINGH, Amarjit
发明人： DHARMADHIKARI, Nitin, Bhalachandra , ZALA, Yashoraj, Rupsinh , SINGH, Amarjit
IPC分类号： A61K
CPC分类号： A61K9/2072
摘要： The present invention provides an oral drug delivery system comprising - (a). a core comprising an active ingredient composition comprising at least one active ingredient and a pharmaceutically acceptable excipient, and (b). a coating surrounding the core, wherein the drug delivery system is designed in a manner such that the coating is reliably removed fully or partially from one or more preselected surfaces of the system upon contact with an aqueous environment, provided further that the coating is not removed from at least one of the surfaces.
摘要翻译：本发明提供一种口服药物递送系统，其包含 - （a）。核心，其包含包含至少一种活性成分和药学上可接受的赋形剂的活性成分组合物，和（b）。围绕芯的涂层，其中药物递送系统被设计成使得当与水性环境接触时，涂层被完全或部分地从系统的一个或多个预选表面被可靠地移除，进一步地，涂层不被去除从至少一个表面。

97. 发明申请

WO2004113296A1 A PROCESS FOR PREPARATION OF 1-[9H-CARBAZOL-4-YLOXY]- 3-[{2-(2-(-(METHOXY)PHENOXY)-ETHYL}-AMINO]-PROPAN-2-OL 审中-公开
标题翻译：制备1- [9H-二氧杂环戊烯-4-基] -3 - [{2-（2 - （ - （甲氧基）苯氧基） - 乙基} - 氨基]丙-2-醇的方法
公开(公告)号：WO2004113296A1
公开(公告)日：2004-12-29
申请号：PCT/IN2004/000052
申请日：2004-03-04
申请人： SUN PHARMACEUTICAL INDUSTRIES LIMITED , CHHABADA, Vijay, Chhangamal , REHANI, Rajeev, Budhdev , THENNATI, Rajamannar
发明人： CHHABADA, Vijay, Chhangamal , REHANI, Rajeev, Budhdev , THENNATI, Rajamannar
IPC分类号： C07D209/88
CPC分类号： C07D405/12 , C07D209/88
摘要： The present invention provides a process for preparation of 1-[9 H -carbazol-4-yloxy]-3-[{2-(2-(methoxy)phenoxy)-ethyl}-amino]-propan-2-ol, a compound of formula 1 in racemic form or in the form of optically active R or S enantiomer or its pharmaceutically acceptable salt, comprising, reacting 4-(oxiranylmethoxy)-9 H -carbazole, a compound of formula (2) or the R or S enantiomer thereof with a compound of formula (5), wherein R 1 is benzyl or substituted benzyl group, in an aprotic organic solvent in presence of a catalyst to obtain a compound of formula (6), or the R or S enantiomer thereof, wherein R 1 is as defined above. The resultant compound of formula (6) is subjected to debenzylation reaction by catalytic hydrogenation to obtain the compound of formula (1), if desired converting the resultant compound of formula (1) to a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了制备1- [9H-咔唑-4-基氧基] -3 - [{2-（2-（甲氧基）苯氧基） - 乙基} - 氨基] - 丙-2-醇的方法，包括使4-（环氧乙烷基甲氧基）-9H-咔唑，式（2）的化合物或R或S（R 1）的化合物与式（1）的外消旋形式或以光学活性的R或S对映体或其药学上可接受的盐的形式反应，对映异构体与式（5）化合物反应，其中R1是苄基或取代的苄基，在非质子有机溶剂中，在催化剂存在下，得到式（6）化合物或其R或S对映异构体，其中R 1 如上所述。所得到的式（6）化合物通过催化氢化进行脱苄基化反应，得到式（1）化合物，如果需要将所得式（1）化合物转化为其药学上可接受的盐。

98. 发明申请

WO2004108732A1 PROCESS FOR THE PREPARATION OF 2,3:4,5-BIS-O(1-METHYLETHYLIDENE)-ß-D-FRUCTOPYRANOSE SULFAMATE 审中-公开
标题翻译：制备2,3：4,5-BIS-O（1-甲基乙基）-β-D-吡喃木糖磺酸盐的方法
公开(公告)号：WO2004108732A1
公开(公告)日：2004-12-16
申请号：PCT/IN2004/000131
申请日：2004-05-12
申请人： SUN PHARMACEUTICAL INDUSTRIES LIMITED , BHATT, Mehul, Chandrakant , KILARU, Srinivasu , THENNATI, Rajamannar
发明人： BHATT, Mehul, Chandrakant , KILARU, Srinivasu , THENNATI, Rajamannar
IPC分类号： C07D493/14
CPC分类号： C07D493/14
摘要： A process for the preparation of 2,3:4,5-bis-O(1-methylethylidene)-ß-D-fructopyranose sulfamate, compound of formula (I), comprising reacting 2,3:4,5-bis-O(1-methylethylidene)-ß-D-fructopyranose sulfonyl chloride, compound of formula (II) with an amine RNH2, wherein R is selected from hydrogen and C1 to C4 alkyl, in a solvent selected from the group consisting of ketones, nitriles, esters and their mixtures to yield the compound of formula (I).
摘要翻译：制备2,3,4,5-二-O-（1-甲基亚乙基）-β-D-吡喃葡萄糖氨基磺酸盐的方法，式（I）化合物，包括使2,3：4,5-双-O- （1-methylethylidene）-β-D-吡喃葡萄糖磺酰氯，式（Ⅱ）化合物与胺RNH2，其中R选自氢和C1至C4烷基，选自酮，腈，酯及其混合物，得到式（I）化合物。

99. 发明申请

WO2003101917A3 A PROCESS FOR THE PREPARATION OF PHENYLCARBAMATES 审中-公开
公开(公告)号：WO2003101917A3
公开(公告)日：2003-12-11
申请号：PCT/IN2003/000210
申请日：2003-06-02
申请人： SUN PHARMACEUTICAL INDUSTRIES LIMITED , PATEL, Hetalkumar, Virendrabhai , THENNATI, Rajamannar
发明人： THENNATI, Rajamannar
IPC分类号： C07C269/00
摘要： A process for the preparation of compound of formula (I); wherein R 1 is hydrogen, linear, branched or cyclic lower alkyl, cyclohexyl, allyl, propargyl or benzyl; R 2 is hydrogen, methyl, ethyl or propyl; or R 1 and R 2 together with the nitrogen to which they are attached form a cyclic moiety of three to eight-membered ring, with or without a hetero atom like nitrogen or oxygen; R 3 is hydrogen or lower alkyl; R 4 and R 5 are the same or different and each is a lower alkyl; comprising reacting compound of formula (II); wherein R 3 , R 4 and R 5 are as defined above, with compound of formula (III); wherein R 1 and R 2 are as defined above, in the presence of a base, and further resolving the compound of formula (I) to obtain (S)-isomer of compound of formula (I), substantially free of R-isomer.

100. 发明申请

WO2003101917A2 A PROCESS FOR THE PREPARATION OF PHENYLCARBAMATES 审中-公开
标题翻译：一种制备苯甲酸酯的方法
公开(公告)号：WO2003101917A2
公开(公告)日：2003-12-11
申请号：PCT/IN2003/000210
申请日：2003-06-02
申请人： SUN PHARMACEUTICAL INDUSTRIES LIMITED , PATEL, Hetalkumar, Virendrabhai , THENNATI, Rajamannar
发明人： THENNATI, Rajamannar
IPC分类号： C07C
CPC分类号： C07C269/06 , C07C271/44
摘要： A process for the preparation of compound of formula (I); wherein R 1 is hydrogen, linear, branched or cyclic lower alkyl, cyclohexyl, allyl, propargyl or benzyl; R 2 is hydrogen, methyl, ethyl or propyl; or R 1 and R 2 together with the nitrogen to which they are attached form a cyclic moiety of three to eight-membered ring, with or without a hetero atom like nitrogen or oxygen; R 3 is hydrogen or lower alkyl; R 4 and R 5 are the same or different and each is a lower alkyl; comprising reacting compound of formula (II); wherein R 3 , R 4 and R 5 are as defined above, with compound of formula (III); wherein R 1 and R 2 are as defined above, in the presence of a base, and further resolving the compound of formula (I) to obtain (S)-isomer of compound of formula (I), substantially free of R-isomer.
摘要翻译：制备式（I）化合物的方法; 其中R 1是氢，直链，支链或环状低级烷基，环己基，烯丙基，炔丙基或苄基; R 2是氢，甲基，乙基或丙基; 或R 1和R 2与它们所连接的氮一起形成三至八元环的环状部分，具有或不具有诸如氮或氧的杂原子; R 3是氢或低级烷基; R 4和R 5相同或不同，各自为低级烷基; 包括使式（II）化合物反应; 其中R 3，R 4和R 5如上定义，与式（III）化合物反应; 其中R 1和R 2如上所定义，在碱的存在下，进一步拆分式（I）化合物，得到基本上不含有式（I）的化合物的（S） - 异构体， R-异构体。

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