公开(公告)号：US08759515B2

公开(公告)日：2014-06-24

申请号：US13583951

申请日：2011-03-11

Applicant: Debashish Datta ,  Siva Rama Prasad Vellanki ,  Arabinda Sahu ,  Raja Babu Balusu ,  Mastan Rao Ravi ,  Hari Babu Nandipati ,  Shankar Rama ,  Lakshmana Rao Vadali ,  Srikanth Sarat Chandra Gorantla ,  Srinivasa Rao Dasari ,  Nagaraju Mittapelly

Inventor： Debashish Datta ,  Siva Rama Prasad Vellanki ,  Arabinda Sahu ,  Raja Babu Balusu ,  Mastan Rao Ravi ,  Hari Babu Nandipati ,  Shankar Rama ,  Lakshmana Rao Vadali ,  Srikanth Sarat Chandra Gorantla ,  Srinivasa Rao Dasari ,  Nagaraju Mittapelly

IPC: C07F9/40 ,  C07D473/34

CPC classification number: C07F9/65616

Abstract: The present invention relates to an improved process for the preparation of Tenofovir Disoproxil and its pharmaceutically acceptable salts comprising the steps of: a) esterifying Tenofovir with chloromethyl isopropyl carbonate in presence of a base, phase transfer catalyst and optionally dehydrating agent, in a suitable solvent; b) optionally purifying Tenofovir Disoproxil; and c) converting of Tenofovir Disoproxil into its pharmaceutically acceptable salts. The present invention further relates to a process for the preparation of Tenofovir by reacting 1-(6-amino-purin-9-yl)-propan-2-ol with toluene-4-sulfonic acid diethoxy phosphoryl methyl ester in presence of a base in a non-polar solvent medium followed by hydrolysis.

Abstract translation: 本发明涉及一种用于制备替诺福韦替泊芬及其药学上可接受的盐的改进方法，其包括以下步骤：a）在碱，相转移催化剂和任选的脱水剂存在下，在合适的溶剂中酯化替诺福韦与氯甲基异丙基碳酸酯 ; b）任选地净化替诺福韦酯; 和c）将替诺福韦酯替代物转化为其药学上可接受的盐。 本发明还涉及通过使1-（6-氨基 - 嘌呤-9-基） - 丙-2-醇与甲苯-4-磺酸二乙氧基磷酰基甲基酯在碱的存在下反应制备替诺福韦的方法 在非极性溶剂介质中进行水解。

公开(公告)号：US20100190982A1

公开(公告)日：2010-07-29

申请号：US12733690

申请日：2008-09-01

Applicant: Janardhana Rao Vascuri ,  Ravinder Reddy Vennapureddy ,  Shankar Rama ,  Ramesh Dandala ,  Sivakumaran Meenakshisunderam

Inventor： Janardhana Rao Vascuri ,  Ravinder Reddy Vennapureddy ,  Shankar Rama ,  Ramesh Dandala ,  Sivakumaran Meenakshisunderam

IPC: C07D239/47

CPC classification number: C07D411/04

Abstract: The present invention provides a process for preparing a stable crystalline solid of Lamivudine polymorphic Form I, which does not change to Form II during storage and pharmaceutical unit operations.

Abstract translation: 本发明提供了一种制备拉米夫定多晶型I的稳定结晶固体的方法，其在储存和药物单元操作期间不改变形式II。

公开(公告)号：US20120295930A1

公开(公告)日：2012-11-22

申请号：US13577118

申请日：2011-02-01

Applicant: Shankar Rama ,  Sarat Chandra Srikanth Gorantla ,  Lakshmana Rao Vadali ,  Venkata Bala Kishore Sarma Inupakutika ,  Srinivas Rao Dasari ,  Nagaraju Mittapelly ,  Santosh Kumar Singh ,  Debashish Datta

Inventor： Shankar Rama ,  Sarat Chandra Srikanth Gorantla ,  Lakshmana Rao Vadali ,  Venkata Bala Kishore Sarma Inupakutika ,  Srinivas Rao Dasari ,  Nagaraju Mittapelly ,  Santosh Kumar Singh ,  Debashish Datta

IPC: C07D411/04 ,  A61P31/18 ,  A61P31/14 ,  C07D411/12 ,  A61K31/513

CPC classification number: C07D411/04

Abstract: The present invention relates to an improved process for the preparation of cis-nucleoside derivative of formula-1 involving chlorination of the compound of formula-2 followed by reaction with compound of formula-3 in presence of a base to get compound of formula-4, reacting the compound of formula-4 with an alkyl halide (RiX) to get a quaternary ammonium salt then with cytosine derivative of formula-5 to provide the compound of formula-6, optionally de-protecting the compound of formula-6 to the compound of formula-7, reducing compound of formula-7 with metal catalyst in presence of a buffer solution, then adding an organic acid to get the compound of formula-8, and converting the compound of formula-8 to cis-nucleoside derivative of formula-1. The present invention further relates to novel cis-nucleoside derivative of formula-8. The present invention also relates to a pharmaceutical composition comprising cis-nucleoside derivative of formula-1 with excipients.

Abstract translation: 本发明涉及一种制备式-1的顺式 - 核苷衍生物的改进方法，其涉及氯化式-2化合物，然后在碱存在下与式-3化合物反应得到式-4的化合物 ，使式-4的化合物与烷基卤化物（R 1 X）反应，得到季铵盐，然后与式-5的胞嘧啶衍生物反应，得到式-6的化合物，任选地将式-6的化合物去保护 在缓冲液存在下，将式7的化合物，式VII的还原化合物与金属催化剂反应，然后加入有机酸得到式-8的化合物，并将式-8的化合物转化为顺式 - 公式1。 本发明还涉及式-8的新型顺式 - 核苷衍生物。 本发明还涉及包含式-1的顺式核苷衍生物与赋形剂的药物组合物。

公开(公告)号：US20130005969A1

公开(公告)日：2013-01-03

申请号：US13583951

申请日：2011-03-11

Applicant: Debashish Datta ,  Siva Rama Prasad Vellanki ,  Arabinda Sahu ,  Raja Babu Balusu ,  Mastan Rao Ravi ,  Hari Babu Nandipati ,  Shankar Rama ,  Lakshmana Rao Vadali ,  Srikanth Sarat Chandra Gorantla ,  Srinivasa Rao Dasari ,  Nagaraju Mittapelly

Inventor： Debashish Datta ,  Siva Rama Prasad Vellanki ,  Arabinda Sahu ,  Raja Babu Balusu ,  Mastan Rao Ravi ,  Hari Babu Nandipati ,  Shankar Rama ,  Lakshmana Rao Vadali ,  Srikanth Sarat Chandra Gorantla ,  Srinivasa Rao Dasari ,  Nagaraju Mittapelly

IPC: C07F9/6561

CPC classification number: C07F9/65616

Abstract: The present invention relates to an improved process for the preparation of Tenofovir Disoproxil and its pharmaceutically acceptable salts comprising the steps of: a) esterifying Tenofovir with chloromethyl isopropyl carbonate in presence of a base, phase transfer catalyst and optionally dehydrating agent, in a suitable solvent; b) optionally purifying Tenofovir Disoproxil; and c) converting of Tenofovir Disoproxil into its pharmaceutically acceptable salts. The present invention further relates to a process for the preparation of Tenofovir by reacting 1-(6-amino-purin-9-yl)-propan-2-ol with toluene-4-sulfonic acid diethoxy phosphoryl methyl ester in presence of a base in a non-polar solvent medium followed by hydrolysis.

Abstract translation: 本发明涉及一种用于制备替诺福韦替泊芬及其药学上可接受的盐的改进方法，其包括以下步骤：a）在碱，相转移催化剂和任选的脱水剂存在下，在合适的溶剂中酯化替诺福韦与氯甲基异丙基碳酸酯 ; b）任选地净化替诺福韦酯; 和c）将替诺福韦酯替代物转化为其药学上可接受的盐。 本发明还涉及通过使1-（6-氨基 - 嘌呤-9-基） - 丙-2-醇与甲苯-4-磺酸二乙氧基磷酰基甲基酯在碱的存在下反应制备替诺福韦的方法 在非极性溶剂介质中进行水解。

公开(公告)号：US09090537B2

公开(公告)日：2015-07-28

申请号：US14379467

申请日：2013-02-15

Applicant: Shankar Rama ,  Seshadri Rao Manukonda ,  Srinivasa Rao Dasari ,  Ramesh Dandala ,  Lakshmana Rao Vadali

Inventor： Shankar Rama ,  Seshadri Rao Manukonda ,  Srinivasa Rao Dasari ,  Ramesh Dandala ,  Lakshmana Rao Vadali

IPC: C07C233/00 ,  C07C231/12 ,  C07C231/22

CPC classification number: C07C231/12 ,  C07C231/22 ,  C07C233/11

Abstract: The present invention relates to an improved process for the preparation of pure compound of Formula-II, which is an intermediate in the preparation of Aliskiren and further conversion of compound of Formula-II into Aliskiren or its pharmaceutically acceptable salts.

Abstract translation: 本发明涉及一种制备式II纯化合物的改进方法，其为制备阿利吉仑的中间体，并进一步将式II化合物转化成阿利吉仑或其药学上可接受的盐。

公开(公告)号：US20100137592A1

公开(公告)日：2010-06-03

申请号：US12452196

申请日：2008-06-02

Applicant: Asif Parvez Sayyed ,  Murali Krishna Ankaraju ,  Ravinder Reddy Vennapureddy ,  Shankar Rama ,  Ramesh Dandala ,  Sivakumaran Meenakshisunderam

Inventor： Asif Parvez Sayyed ,  Murali Krishna Ankaraju ,  Ravinder Reddy Vennapureddy ,  Shankar Rama ,  Ramesh Dandala ,  Sivakumaran Meenakshisunderam

IPC: C07D473/32 ,  C07D239/50 ,  C07C255/37 ,  C07C217/48 ,  C07C213/02 ,  C07C213/08

CPC classification number: C07D239/50 ,  C07C213/02 ,  C07C255/15 ,  C07D473/32

Abstract: A process for the preparation of famciclovir a compound of Formula (I) and its intermediates.

Abstract translation: 泛昔洛韦制备式（I）化合物及其中间体的方法。