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51. 发明申请

US20110195120A2 Sustained Release Pharmaceutical Composition Containing Metformin Hydrochloride 审中-公开
标题翻译：含有盐酸二甲双胍的缓释药物组合物
公开(公告)号：US20110195120A2
公开(公告)日：2011-08-11
申请号：US10272812
申请日：2002-10-17
申请人： Suresh GIDWANI , Purushottam Singnurkar , Prashant Tewari
发明人： Suresh GIDWANI , Purushottam Singnurkar , Prashant Tewari
IPC分类号： A61K9/22
CPC分类号： A61K9/1694 , A61K9/2013 , A61K9/2022 , A61K9/2027 , A61K9/2077 , A61K9/2095 , A61K31/155
摘要： A monolithic sustained-release pharmaceutical composition comprising a therapeutically effective dose of metformin hydrochloride as an active substance and a hydrophobic polymer and/or other hydrophobic material, wherein the metformin hydrochloride is released no more than forty percent in gastric fluid having pH 1.2 and is released no less than ninety percent eight to ten hours after administration in simulated intestinal fluid (phosphate buffer) having pH 6.8, and wherein the metformin hydrochloride displays a peak plasma concentration, a systemic bioavailability over time, and a residual plasma concentration twenty-four hours after administration of an oral dosage form of the pharmaceutical composition, so that the metformin hydrochloride concentration remains therapeutically effective and once daily administration of the pharmaceutical composition is sufficient to be therapeutically effective throughout a day.
摘要翻译：一种整体缓释药物组合物，其包含治疗有效剂量的二甲双胍盐酸盐作为活性物质和疏水性聚合物和/或其它疏水材料，其中盐酸二甲双胍在pH 1.2的胃液中释放不超过百分之四十，并释放在pH 6.8以上的模拟肠液（磷酸盐缓冲液）给药后8〜10小时不少于90％，其中盐酸二甲双胍显示峰值血药浓度，随时间推移的全身生物利用度和二十四小时后的残留血浆浓度施用药物组合物的口服剂型，使得盐酸二甲双胍浓度保持治疗有效性，并且每天一次的药物组合物给药足以在一天内具有治疗有效性。

52. 发明授权

US07964182B2 Pharmaceutical compositions comprising phosphate-binding polymer 有权
标题翻译：包含磷酸结合聚合物的药物组合物
公开(公告)号：US07964182B2
公开(公告)日：2011-06-21
申请号：US12957810
申请日：2010-12-01
申请人： Ashok Omray , Varsha Shashank Choudhary , Yogesh Sharad Bhide
发明人： Ashok Omray , Varsha Shashank Choudhary , Yogesh Sharad Bhide
IPC分类号： A61K31/77 , A61K31/765 , A61K9/50 , C08G79/02
CPC分类号： A61K9/284 , A61K9/1641 , A61K9/2045 , A61K9/2095 , A61K9/2846 , A61K9/2866 , A61K31/785 , C08F8/00 , C08F26/02
摘要： The present invention discloses pharmaceutical composition comprising phosphate binding polymers such as Sevelamer carbonate substantially free of monovalent anion other than bicarbonate anion. Particularly, monovalent anion content is less than about 0.05% (w/w). Disclosed are compositions comprising wet granulated Sevelamer carbonate free of added metal ions and/or added monovalent anion source.
摘要翻译：本发明公开了包含磷酸盐结合聚合物如基本上不含碳酸氢根阴离子以外的一价阴离子的赛维拉姆碳酸酯的药物组合物。特别地，一价阴离子含量小于约0.05％（w / w）。公开了包含不含添加的金属离子和/或添加的一价阴离子源的湿法制粒的赛维米尔碳酸盐的组合物。

53. 发明授权

US07378439B2 Process for the preparation of 4-(2-dipropylaminoethyl)-1,3-dihydro-2H-indol-2-one hydrochloride 失效
标题翻译： 4-（2-二丙基氨基乙基）-1,3-二氢-2H-吲哚-2-酮盐酸盐的制备方法
公开(公告)号：US07378439B2
公开(公告)日：2008-05-27
申请号：US10888901
申请日：2004-07-09
申请人： Venkatasubramanian Radhakrishna Tarur , Dhananjay Govind Sathe , Harish Kashinath Mondkar , Rajesh Ganpat Bhopalkar , Samadhan Daulat Patil
发明人： Venkatasubramanian Radhakrishna Tarur , Dhananjay Govind Sathe , Harish Kashinath Mondkar , Rajesh Ganpat Bhopalkar , Samadhan Daulat Patil
IPC分类号： A61K31/4015 , C07D209/34
CPC分类号： C07D209/48 , C07D209/34
摘要： The present invention discloses a novel process and novel intermediates for the Preparation of 4-[2-(di-n-propyl amino) ethyl]-1,3-dihydro-2H-indol-2-one, commonly known as Ropinirole (I) and pharmaceutical composition comprising the same. Further the present invention also discloses a method of treatment for cardiovascular disorders and Parkinson's disease.
摘要翻译：本发明公开了一种制备4- [2-（二正丙基氨基）乙基] -1,3-二氢-2H-吲哚-2-酮的新型方法和新型中间体，通常称为Ropinirole（I ）和包含其的药物组合物。此外，本发明还公开了一种治疗心血管疾病和帕金森病的方法。

54. 发明授权

US07846425B2 Process for the preparation of sevelamer hydrochloride and formulation thereof 有权
标题翻译：盐酸司维拉姆及其制剂的制备方法
公开(公告)号：US07846425B2
公开(公告)日：2010-12-07
申请号：US12620931
申请日：2009-11-18
申请人： Deepak Anant Hegde , Varsha Shashank Choudhary , Yogesh Sharad Bhide
发明人： Deepak Anant Hegde , Varsha Shashank Choudhary , Yogesh Sharad Bhide
IPC分类号： A61K31/785 , A61P13/12 , C08G61/02
CPC分类号： A61K31/785 , A61K9/284 , A61K9/2846 , A61K9/2866 , C08F8/02 , C08F8/08 , C08F126/02
摘要： Disclosed herein is an improved process for preparation of Sevelamer hydrochloride having phosphate binding capacity of 4.7 to 6.4 mmol/g. Further, the invention discloses Sevelamer hydrochloride compositions and a novel process for preparation of said compositions comprising high shear non-aqueous granulation.
摘要翻译：本文公开了一种改进的具有4.7至6.4mmol / g的磷酸盐结合能力的盐酸司维拉姆的制备方法。此外，本发明公开了盐酸司维拉姆组合物和用于制备包含高剪切非水性造粒物的所述组合物的新方法。

55. 发明授权

US07446200B2 Rapid resolution process of clopidogrel base and a process for preparation of clopidogrel bisulfate polymorph-form I 失效
标题翻译：氯吡格雷碱的快速分离过程和硫酸氢氯吡格雷多晶型I的制备方法
公开(公告)号：US07446200B2
公开(公告)日：2008-11-04
申请号：US11149646
申请日：2005-06-10
申请人： Manoj Madhukarrao Deshpande , V. R. Tarur , Dhananjay Govind Sathe , Harish Kashniath Mondkar , Kamlesh Digambar Sawant , Tushar Anil Naik
发明人： Manoj Madhukarrao Deshpande , V. R. Tarur , Dhananjay Govind Sathe , Harish Kashniath Mondkar , Kamlesh Digambar Sawant , Tushar Anil Naik
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The present invention discloses a rapid resolution process of racemic clopidogrel base followed by conversion of the resolved (S) isomer to crystalline Clopidogrel bisulfate Form I. The invention also discloses novel racemization process of the unwanted (R) isomer of clopidogrel base. The invention further discloses an improved process for preparation of acid addition salts of clopidogrel.
摘要翻译：本发明公开了外消旋氯吡格雷碱的快速拆分方法，然后将分解的（S）异构体转化为结晶氯吡格雷硫酸氢盐形式I.本发明还公开了氯吡格雷碱的不需要的（R）异构体的新型外消旋化方法。本发明还公开了一种制备氯吡格雷的酸加成盐的改进方法。

56. 发明授权

US07439365B2 Pharmaceutical salt of (1-benzyl-4-[(5,6-dimethoxy-1-indanone)-2-yl] methyl piperidine (Donepezil) 失效
标题翻译：（1-苄基-4 - [（5,6-二甲氧基-1-二氢茚酮）-2-基]甲基哌啶（多奈哌齐）
公开(公告)号：US07439365B2
公开(公告)日：2008-10-21
申请号：US10879816
申请日：2004-06-29
申请人： Venkatasubramanian Radhakrishnan Tarur , Dhananjay Govind Sathe , Avinash Venkatraman Naidu , Umesh Parashram Aher
发明人： Venkatasubramanian Radhakrishnan Tarur , Dhananjay Govind Sathe , Avinash Venkatraman Naidu , Umesh Parashram Aher
IPC分类号： C07D211/02
CPC分类号： C07D211/32 , C07D211/22
摘要： The present invention relates to the oxalate salt of 1-benzyl-4-[(5,6-dimethoxy-1-indanone)-2-yl]methyl piperidine, commonly known as Donepezil, and its method of preparation.
摘要翻译：本发明涉及通常称为多奈哌齐的1-苄基-4 - [（5,6-二甲氧基-1-二氢茚酮）-2-基]甲基哌啶的草酸盐及其制备方法。

57. 发明授权

US07820409B2 Chimeric human growth hormone derived from the placenta and pituitary isoform and processes for obtaining said chimera 失效
标题翻译：衍生自胎盘和垂体同种型的嵌合人生长激素和获得所述嵌合体的方法
公开(公告)号：US07820409B2
公开(公告)日：2010-10-26
申请号：US11464251
申请日：2004-06-23
申请人： Dipanwita Maiti , Shrikant Misiira , Laxmi Srinivas Rao , Milind Prabhakar Nipiiadkar , Ahmed Monsur Borbiiuiya , Ganesh Aruna Khare
发明人： Dipanwita Maiti , Shrikant Misiira , Laxmi Srinivas Rao , Milind Prabhakar Nipiiadkar , Ahmed Monsur Borbiiuiya , Ganesh Aruna Khare
IPC分类号： C12N15/18 , C12N15/63 , C12N1/21 , C12N5/00
CPC分类号： C07K14/61
摘要： A way to increase the production of recombinant polypeptides by combining pieces of several different isoforms of a given gene to make a chimeric isoform of the gene (using a chimeric gene can increase the production of polypeptide over 25%), or by inserting several copies of the coding region in tandem into a transformation vector (e.g., plasmids carrying multiple copies of the chimera of SEQ ID NO: 3 increased production 107%).
摘要翻译：通过组合给定基因的几种不同同种型的片段来增加重组多肽的产生的方法以制备基因的嵌合同种型（使用嵌合基因可以增加多肽的产生超过25％），或通过插入几个拷贝的将编码区串联成转化载体（例如携带SEQ ID NO：3的嵌合体的多个拷贝的质粒增加产量107％）。

58. 发明授权

US08377891B2 Process for synthesis of cyclic octapeptide 有权
标题翻译：合成八肽的方法
公开(公告)号：US08377891B2
公开(公告)日：2013-02-19
申请号：US13123623
申请日：2009-05-04
申请人： Divya Lal Saksena , Digamber Shripati Pawar , Nikhil Umesh Mohe , Nilesh Dagdu Patil , Chandrakesan Muralidharan , Lester Lobo , Radhakrishnan Venkatasubramanian Tarur
发明人： Divya Lal Saksena , Digamber Shripati Pawar , Nikhil Umesh Mohe , Nilesh Dagdu Patil , Chandrakesan Muralidharan , Lester Lobo , Radhakrishnan Venkatasubramanian Tarur
IPC分类号： A61K38/08
CPC分类号： C07K14/6555 , A61K38/00
摘要： This invention relates a process for preparing octreotide and derivatives thereof. The starting material, Cys(Trt)-2-Chlorotrityl resin is coupled with various amino acids to obtain a protected heptapeptide of formula (2): Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-2-Chlorotrityl resin. The linear protected peptide of formula (2) is cleaved from the support using TFA5TIS and water to yield linear protected peptide of formula (3) Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-OH Linear protected heptapeptide of formula (3) is deprotected to yield heptapeptide of formula (6): D-Phe-Cys-Phe-D-Tip-Lys-Thr-Cys-OH; which is cyclized using hydrogen peroxide and to the cyclic peptide of formula (7) D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-OH; threoninol is coupled at C terminal to yield octreotide. Alternatively threoninol is coupled to the heptapeptide of formula (3) to yield protected octapeptide of formula (4) Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-Thr-OL which is subsequently deprotected to yield linear octapeptide of formula (5) D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-OL and cyclized with hydrogen peroxide to yield cyclic octreotide with a yield of >95%.
摘要翻译：本发明涉及制备奥曲肽及其衍生物的方法。将起始物质Cys（Trt）-2-氯三苯甲基树脂与各种氨基酸偶联得到式（2）的保护的七肽：Boc-D-Phe-Cys（Trt）-Phe-D-Trp-Lys（Boc ）-Thr（OBut）-Cys（Trt）-2-氯三苯甲基树脂。使用TFA5TIS和水从支持物上切割式（2）的线性保护肽，得到式（3）的线性保护肽Boc-D-Phe-Cys（Trt）-Phe-D-Trp-Lys（Boc） - Thr（OBut）-Cys（Trt）-OH将式（3）的线性保护的七肽脱保护得到式（6）的七肽：D-Phe-Cys-Phe-D-Tip-Lys-Thr-Cys-OH; 其使用过氧化氢和式（7）D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-OH的环肽环化; 苏氨酚在C末端偶联以产生奥曲肽。或者，苏糖醇与式（3）的七肽偶联以得到式（4）的保护的八肽Boc-D-Phe-Cys（Trt）-Phe-D-Trp-Lys（Boc）-Thr（OBut）-Cys Trt）-Thr-OL，随后脱保护得到式（5）D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-OL的直链八肽，并用过氧化氢环化，得到环状奥曲肽，产量> 95％。

59. 发明授权

US07897724B2 Solid phase Fmoc chemistry process to prepare peptides 失效
标题翻译：固相Fmoc化学过程制备肽
公开(公告)号：US07897724B2
公开(公告)日：2011-03-01
申请号：US11729047
申请日：2007-03-27
申请人： Divya Lal Saksena , Shrikant Mishra , Chandrakesan Muralidharan , Nilesh Patil , Nikhil Umesh Mohe , Mandar Ravindra Maduskar
发明人： Divya Lal Saksena , Shrikant Mishra , Chandrakesan Muralidharan , Nilesh Patil , Nikhil Umesh Mohe , Mandar Ravindra Maduskar
IPC分类号： C07K1/06
CPC分类号： C07K14/75 , C07K14/78 , Y02P20/582
摘要： The present invention relates to an improved process for the preparation of N6-(aminoiminomethyl)-N2-(3-mercapto-1-oxopropyl)-L-lysylglycyl-L-α-aspartyl-L-tryptophyl-L-prolyl-L-cysteinamide, cyclic(1→6)-disulfide of formula (1), which involves assembling a peptide chain comprising of six amino acids and a thioalkyl carboxylic acid in a required sequence on a solid support to obtain a peptide bound resin of formula (2), capping the free amino groups after each coupling, cleaving Dde group in the peptide of formula (2) from the solid support to obtain peptide-solid support of formula (3), guanylating the peptide of formula (3) at ε-lysine-NH2 in an organic solvent to obtain peptide-solid support of formula (4), cleaving and deprotecting all groups in the peptide of formula (4) from the solid support to obtain peptide-amide formula (5), oxidizing the SH-peptide of formula (5) with an appropriate oxidizing agent to obtain the crude peptide-amide of formula (1) and purifying the crude peptide-amide of formula (1) by chromatographic technique. The solid support is either resin or a cellulose support like cotton, gauze, fabric, paper and perloza beads. The described process is simple, easy, environment friendly, takes lesser time and more cost effective.
摘要翻译：本发明涉及一种制备N6-（氨基亚氨基甲基）-N2-（3-巯基-1-氧代丙基）-L-赖氨酰甘氨酰-L-α-天冬氨酰-L-色氨酰-L-脯氨酰基-L- 半胱氨酰胺，式（1）的环状（1→6） - 二硫化物，其包括在固体支持物上以所需的顺序将包含六个氨基酸的肽链和硫代烷基羧酸组装以获得式（2）的肽结合树脂），在每次偶联后封端游离氨基，从固体支持物切割式（2）的肽中的Dde基团以获得式（3）的肽 - 固体支持物，在式（3）的肽上进行脒化，赖氨酸-NH 2在有机溶剂中得到式（4）的肽固体支持物，从固体支持物中切割和脱保护基团中所有基团的肽，得到肽 - 酰胺式（5），氧化SH- 式（5）的肽与适当的氧化剂反应，得到式（1）的粗肽 - 酰胺并纯化粗蛋白 e通过色谱技术制备式（1）的肽 - 酰胺。固体支持物是树脂或纤维素载体，如棉，纱布，织物，纸和perloza珠。描述的过程简单，容易，环保，花费更少的时间和更具成本效益。

60. 发明授权

US07186842B2 Polymorph of (1-benzyl-4-[(5,6-dimethoxy-1-indanone)-2-y1] methyl piperidine hydrochloride (Donepezil hydrochloride) and a process for producing thereof 失效
标题翻译：（1-苄基-4 - [（5,6-二甲氧基-1-二氢茚酮）-2-y1]甲基哌啶盐酸盐（盐酸多奈哌齐）的多晶型物及其制备方法
公开(公告)号：US07186842B2
公开(公告)日：2007-03-06
申请号：US11145202
申请日：2005-06-03
申请人： Umesh P. Aher , Venkatasubramanian R. Tarur , Dhananjay Govind Sathe , Avinash Venkataraman Naidu , Kamlesh Digambar Sawant
发明人： Umesh P. Aher , Venkatasubramanian R. Tarur , Dhananjay Govind Sathe , Avinash Venkataraman Naidu , Kamlesh Digambar Sawant
IPC分类号： C07D211/32 , A61K31/445
CPC分类号： C07D211/06
摘要： The present invention discloses a novel, stable polymorph of 1-benzyl-4-[(5,6-dimethoxy-1-indanone)-2-yl] methyl piperidine hydrochloride commonly known as Donepezil hydrochloride. Further the present invention discloses a process for producing Donepezil HCl amorphous and its polymorph Form (VI).
摘要翻译：本发明公开了通常称为盐酸多奈哌齐的1-苄基-4 - [（5,6-二甲氧基-1-茚满酮）-2-基]甲基哌啶盐酸盐的新型稳定多晶型物。此外，本发明公开了一种生产多奈哌齐HCl无定形物及其多晶型物（VI）的方法。

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