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1. 发明申请

US20120094910A1 IMPROVED PROCESS FOR THE PREPARATION OF DESMOPRESSIN OR ITS PHARMACEUTICALLY ACCEPTABLE SALTS 审中-公开
标题翻译：改进去甲伐他汀或其药学上可接受的盐的方法
公开(公告)号：US20120094910A1
公开(公告)日：2012-04-19
申请号：US13263123
申请日：2010-04-05
申请人： Ananda Kuppanna , Mallikarjuna Sarma Dokka , Bulliraju Kamana , Sreelatha Vanjivaka , Debashish Datta
发明人： Ananda Kuppanna , Mallikarjuna Sarma Dokka , Bulliraju Kamana , Sreelatha Vanjivaka , Debashish Datta
IPC分类号： A61K38/11 , C07K7/16
CPC分类号： C07K7/16
摘要： The present invention relates to a novel and improved process for the preparation of 1-deamino-8-D-arginine vasopressin (Desmopressin) or its pharmaceutically acceptable salts thereof and also relates to an improved process for the purification of Desmopressin or its pharmaceutically acceptable salts. Further, the present invention also relates to pharmaceutical composition of Desmopressin or its pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及一种制备1-脱氨基-8-D-精氨酸加压素（去氨加压素）或其药学上可接受的盐的新颖和改进的方法，还涉及一种改进的去氨加压素或其药学上可接受的盐的纯化方法。此外，本发明还涉及去氨加压素或其药学上可接受的盐的药物组合物。

2. 发明申请

US20130060004A1 Novel Process For The Preparation Of Leuprolide And Its Pharmaceutically Acceptable Salts Thereof 审中-公开
标题翻译：用于制备亮丙瑞林及其药学上可接受的盐的新方法
公开(公告)号：US20130060004A1
公开(公告)日：2013-03-07
申请号：US13696656
申请日：2011-05-04
申请人： Ananda Kuppanna , Bulli Raju Kamana , Sreelatha Vanjivaka , Debashish Datta
发明人： Ananda Kuppanna , Bulli Raju Kamana , Sreelatha Vanjivaka , Debashish Datta
IPC分类号： C07K1/10 , C07K1/14 , C07K7/08
CPC分类号： C07K7/23
摘要： The present invention relates to a novel process for the preparation of Leuprolide or its pharmaceutically acceptable salts thereof by solid and solution phase peptide synthesis (Hybrid approach). The present invention also relates to a process for the preparation of Leuprolide or its pharmaceutically acceptable salts thereof by synthesizing the peptide fragments by solid phase (7 and 5 amino acids fragment) and solution phase (2 and 4 amino acids fragment) respectively. The final solution phase condensation of these peptide fragments (7+2 and 5+4) led to a nonapeptide Leuprolide in the protected form. The present invention further relates to novel peptide fragements—Pyr-His(Trt)-Trp(Boc)-Ser(tBu)-Tyr(tBu)-DLeu-Leu-OH (Fragment-11); H-Arg(Pbf)-Pro-NHEt (Fragment-I11); Pyr-His(Trt)-Trp(Boc)-Ser(tBu)-Tyr(tBu)-DLeu-Leu-Arg(Pbf)-Pro-NHEt (Protected Leuprolide) (Fragment-IV); Pyr-His(Trt)-Trp(Boc)-Ser(tBu)-Tyr(tBu)-OH (Fragment-V); H-DLeu-Leu-Arg(Pbf)-Pro-NHEt (Fragment-VI) and process for the preparation thereof.
摘要翻译：本发明涉及通过固相和溶液相肽合成制备亮丙瑞林或其药学上可接受的盐的新方法（Hybrid approach）。本发明还涉及通过分别通过固相（7和5个氨基酸片段）和溶液相（2和4个氨基酸片段）合成肽片段来制备亮丙瑞林或其药学上可接受的盐的方法。这些肽片段（7 + 2和5 + 4）的最终溶液相缩合导致了受保护形式的一种单肽亮丙瑞林。本发明还涉及新颖的肽片段 - Pyr-His（Trt）-Trp（Boc）-Ser（tBu）-Tyr（tBu）-DLeu-Leu-OH（片段-11）; H-Arg（Pbf）-Pro-NHEt（Fragment-I11）; Pyr-His（Trt）-Trp（Boc）-Ser（tBu）-Tyr（tBu）-DLeu-Leu-Arg（Pbf）-Pro-NHEt（受保护的亮丙瑞林）（片段-IV） Pyr-His（Trt）-Trp（Boc）-Ser（tBu）-Tyr（tBu）-OH（片段-V）; H-DLeu-Leu-Arg（Pbf）-Pro-NHEt（片段-VI）及其制备方法。

3. 发明授权

US07632864B2 Gabapentin analogues and process thereof 失效
标题翻译：加巴喷丁类似物及其过程
公开(公告)号：US07632864B2
公开(公告)日：2009-12-15
申请号：US11583953
申请日：2006-10-20
申请人： Nagarajan Kuppuswamy , Sivaramakrishnan Hariharan , Venkatachalam Sankar Iyer , Suresh Babu Balakrishnan , Gopalakrishnan Krishnamurthi , Ananda Kuppanna , Muruga Poopati Raja Karuppiah , Balaram Padmanabhan , Aravinda Subrayashastry , Gouriamma Vasudev Prema , Shamala Narayanaswamy
发明人： Nagarajan Kuppuswamy , Sivaramakrishnan Hariharan , Venkatachalam Sankar Iyer , Suresh Babu Balakrishnan , Gopalakrishnan Krishnamurthi , Ananda Kuppanna , Muruga Poopati Raja Karuppiah , Balaram Padmanabhan , Aravinda Subrayashastry , Gouriamma Vasudev Prema , Shamala Narayanaswamy
IPC分类号： A61K31/195 , C07C229/00
CPC分类号： C07C229/28 , C07C233/08 , C07C2601/14
摘要： The present invention relates to compounds trans (E) and cis (Z) stereoisomers of 4-t-butyl gabapentin of formula (11) and (12) and a process for the preparation of the said stereoisomers.
摘要翻译：本发明涉及式（11）和（12）的4-叔丁基加巴喷丁的反式（E）和顺式（Z）立体异构体的制备方法和所述立体异构体的制备方法。

4. 发明申请

US20050209332A1 Gabapentin analogues and process thereof 审中-公开
标题翻译：加巴喷丁类似物及其过程
公开(公告)号：US20050209332A1
公开(公告)日：2005-09-22
申请号：US11079481
申请日：2005-03-15
申请人： Nagarajan Kuppuswamy , Sivaramakrishnan Hariharan , Venkatachalam Iyer , Suresh Balakrishnan , Gopalakrishnan Krishnamurthi , Ananda Kuppanna , Muruga Karuppiah , Balaram Padmanabhan , Aravinda Subrayashastry , Gouriamma Prema , Shamala Narayanaswamy
发明人： Nagarajan Kuppuswamy , Sivaramakrishnan Hariharan , Venkatachalam Iyer , Suresh Balakrishnan , Gopalakrishnan Krishnamurthi , Ananda Kuppanna , Muruga Karuppiah , Balaram Padmanabhan , Aravinda Subrayashastry , Gouriamma Prema , Shamala Narayanaswamy
IPC分类号： A61K31/195
CPC分类号： C07C229/28 , C07C233/08 , C07C2601/14
摘要： The present invention relates to compounds cis (Z) and trans (E) stereoisomers of 4-t-butylgabapentin of formula (11) and (12) and a process for the preparation of the said stereoisomers.
摘要翻译：本发明涉及式（11）和（12）的4-叔丁基加巴喷丁的顺式（Z）和反（E）立体异构体的化合物和制备所述立体异构体的方法。

5. 发明申请

US20070123591A1 Gabapentin analogues and process thereof 失效
标题翻译：加巴喷丁类似物及其过程
公开(公告)号：US20070123591A1
公开(公告)日：2007-05-31
申请号：US11583953
申请日：2006-10-20
申请人： Nagarajan Kuppuswamy , Sivaramakrishnan Hariharan , Venkatachalam Sankar Iyer , Suresh Babu Balakrishnan , Gopalakrishnan Krishnamurthi , Ananda Kuppanna , Muruga Poopati Raja Karuppiah , Balaram Padmanabhan , Aravinda Subrayashastry , Gouriamma Vasudev Prema , Shamala Narayanaswamy
发明人： Nagarajan Kuppuswamy , Sivaramakrishnan Hariharan , Venkatachalam Sankar Iyer , Suresh Babu Balakrishnan , Gopalakrishnan Krishnamurthi , Ananda Kuppanna , Muruga Poopati Raja Karuppiah , Balaram Padmanabhan , Aravinda Subrayashastry , Gouriamma Vasudev Prema , Shamala Narayanaswamy
IPC分类号： A61K31/195 , C07C229/12
CPC分类号： C07C229/28 , C07C233/08 , C07C2601/14
摘要： The present invention relates to compounds trans (E) and cis (Z) stereoisomers of 4-t-butyl gabapentin of formula (11) and (12) and a process for the preparation of the said stereoisomers.
摘要翻译：本发明涉及式（11）和（12）的4-叔丁基加巴喷丁的反式（E）和顺式（Z）立体异构体的制备方法和所述立体异构体的制备方法。

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