公开(公告)号：US06664267B1

公开(公告)日：2003-12-16

申请号：US10156685

申请日：2002-05-28

申请人： Noel J. de Souza ,  Prasad K Deshpande ,  Milind C. Shukla ,  Siddiqui M Jaweed Mukarram ,  Dilip Ganesh Kulkarni ,  Ansari Azizur Rahman ,  Ravindra D Yeole ,  Mahesh V Patel ,  Shrikant V Gupte

发明人： Noel J. de Souza ,  Prasad K Deshpande ,  Milind C. Shukla ,  Siddiqui M Jaweed Mukarram ,  Dilip Ganesh Kulkarni ,  Ansari Azizur Rahman ,  Ravindra D Yeole ,  Mahesh V Patel ,  Shrikant V Gupte

IPC分类号： C07D45504

CPC分类号： C07D455/04

摘要： The invention relates to the new arginine salt forms of RS-(±)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, R-(+)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating microbial infections.

摘要翻译： 本发明涉及新的精氨酸盐形式的RS-（±）-9-氟-6,7-二氢-8-（4-羟基哌啶-1-基）-5-甲基-1-氧代-1H，5H- 苯并[i，j]喹嗪-2羧酸，S - （ - ） - 9-氟-6,7-二氢-8-（4-羟基哌啶-1-基）-5-甲基-1-氧代-1H- ，5H-苯并[i，j]喹嗪-2-羧酸，R - （+） - 9-氟-6,7-二氢-8-（4-羟基哌啶-1-基）-5-甲基-1- 氧代-1H，5H-苯并[i，j]喹嗪-2-羧酸，其制备方法和包含这些精氨酸盐形式的药物制剂作为其用于治疗微生物感染的活性成分。

公开(公告)号：US06514986B2

公开(公告)日：2003-02-04

申请号：US09802793

申请日：2001-03-09

申请人： Noel J. de Souza ,  Shivkumar Agarwal ,  Mahesh V. Patel ,  Satish B. Bhawsar ,  Rupinder K. Beri ,  Ravindra D. Yeole ,  Nitin Shetty

发明人： Noel J. de Souza ,  Shivkumar Agarwal ,  Mahesh V. Patel ,  Satish B. Bhawsar ,  Rupinder K. Beri ,  Ravindra D. Yeole ,  Nitin Shetty

IPC分类号： C07D45506

CPC分类号： C07D215/233 ,  A61K31/4745 ,  A61K45/06 ,  C07B2200/07 ,  C07C279/14 ,  C07D401/04 ,  C07D401/14 ,  C07D455/04 ,  C07D471/04 ,  C07D471/08

摘要： The invention relates to the new arginine salt forms of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating antimicrobial infections.

公开(公告)号：US07405228B2

公开(公告)日：2008-07-29

申请号：US10616888

申请日：2003-07-10

申请人： Mahesh V Patel ,  Prasad K Deshpande ,  Milind D Sindkhedkar ,  Shrikant V Gupte ,  Yati Chugh ,  Nitin Shetty ,  Milind C Shukla ,  Ravindra D Yeole ,  Noel J De Souza

发明人： Mahesh V Patel ,  Prasad K Deshpande ,  Milind D Sindkhedkar ,  Shrikant V Gupte ,  Yati Chugh ,  Nitin Shetty ,  Milind C Shukla ,  Ravindra D Yeole ,  Noel J De Souza

IPC分类号： A61K31/421 ,  A61K31/454 ,  C07D413/10 ,  C07D401/10

CPC分类号： C07D413/10 ,  C07D413/14 ,  C07D417/14

摘要： The present invention provides agents having high antimicrobial activity for preventing and treating infectious diseases. Thus, the present invention provides novel cyano-(substituted)-methylenepiperidinophenyl oxazolidinone derivatives, processes for making the compounds, as well as antimicrobial compositions containing said derivatives as active ingredients and methods of treating bacterial infections with the said derivatives.

摘要翻译： 本发明提供了用于预防和治疗感染性疾病的高抗微生物活性的试剂。 因此，本发明提供新的氰基 - （取代） - 亚甲基哌啶基苯基恶唑烷酮衍生物，制备该化合物的方法，以及含有所述衍生物作为活性成分的抗微生物组合物以及用所述衍生物治疗细菌感染的方法。

公开(公告)号：US07164023B2

公开(公告)日：2007-01-16

申请号：US10749932

申请日：2003-12-31

申请人： Prasad K. Deshpande ,  Vijaya N. Desai ,  Ravindra D. Yeole ,  Shrikant V. Gupte ,  Mahesh V. Patel ,  Noel J. de Souza

发明人： Prasad K. Deshpande ,  Vijaya N. Desai ,  Ravindra D. Yeole ,  Shrikant V. Gupte ,  Mahesh V. Patel ,  Noel J. de Souza

IPC分类号： C07D401/04 ,  C07D401/14

CPC分类号： C07D471/06

摘要： The invention relates to crystalline S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid L-arginine salt tetrahydrate, a process for its preparation and pharmaceutical formulations incorporating it as the active ingredient for use in treating microbial infections.

公开(公告)号：US07132541B2

公开(公告)日：2006-11-07

申请号：US10671040

申请日：2003-09-25

申请人： Noel J. de Souza ,  Prasad K Deshpande ,  Milind C. Shukla ,  Siddiqui M Jaweed Mukarram ,  Dilip Ganesh Kulkarni ,  Ansari Azizur Rahman ,  Ravindra D Yeole ,  Mahesh V Patel ,  Shrikant V Gupte

发明人： Noel J. de Souza ,  Prasad K Deshpande ,  Milind C. Shukla ,  Siddiqui M Jaweed Mukarram ,  Dilip Ganesh Kulkarni ,  Ansari Azizur Rahman ,  Ravindra D Yeole ,  Mahesh V Patel ,  Shrikant V Gupte

IPC分类号： C07D451/00 ,  C07D453/00 ,  C07D455/00

CPC分类号： C07D455/04

摘要： The invention relates to the new arginine salt forms of RS-(±)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, R-(+)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating microbial infections.

公开(公告)号：US06987167B2

公开(公告)日：2006-01-17

申请号：US10153555

申请日：2002-05-22

申请人： Nishith C. Chaturvedi ,  Suresh Beri ,  Ravindra D. Yeole ,  Noel J. De Souza

发明人： Nishith C. Chaturvedi ,  Suresh Beri ,  Ravindra D. Yeole ,  Noel J. De Souza

IPC分类号： A61K38/04 ,  C07K16/00 ,  C07K17/00 ,  C07K5/00 ,  C07K7/00

CPC分类号： C07K5/0821 ,  C07K5/0812 ,  C07K14/6555

摘要： The present invention relates to a process for commercial production of octreotide using solution peptide chemistry and inexpensive amino acid derivatives. Thus the hexapeptide (Boc) D-Phe-Cys(Acm)-Phe-D-Trp-Lys(Boc)-Thr-OMe is synthesized by condensation of two tripeptide fragments, saponified and condensed with Cys(Acm)-Thr-OL to give the linear octapeptide alcohol. The linear peptide alcohol is treated with iodine, after removal of Boc groups, to give the cyclic peptide octreotide. The linear octapeptide alcohol can alternately be made by condensation of the protected hexapeptide acid with the dipeptide Cys(Acm)-Thr-OMe, followed by reduction with sodium borohydride.

摘要翻译： 本发明涉及使用溶液肽化学和便宜的氨基酸衍生物商业生产奥曲肽的方法。 因此，通过两个三肽片段的缩合合成六肽（Boc）D-Phe-Cys（Acm）-Phe-D-Trp-Lys（Boc）-Thr-OMe），皂化并与Cys（Acm）-Thr-OL 得到线性八肽醇。 线性肽醇用碘处理后除去Boc基团，得到环肽奥曲肽。 线性八肽醇可以交替地通过保护的六肽酸与二肽Cys（Acm）-Thr-OMe的缩合，然后用硼氢化钠还原来制备。

公开(公告)号：US06964966B2

公开(公告)日：2005-11-15

申请号：US10128996

申请日：2002-04-23

申请人： Noel John De Souza ,  Mahesh Vithalbhai Patel ,  Prasad Keshav Deshpande ,  Shiv Kumar Agarwal ,  Shrikant V. Gupte ,  Dilip J. Upadhyay ,  Satish B. Bhawsar ,  Rupinder K. Beri ,  Kandepu Sreenivas ,  Sheela Chandrasekharan Nair ,  Milind Chintaman Shukla ,  Yati Chugh ,  Nitin Shetty ,  Ravindra D. Yeole ,  M. Madhav Reddy

发明人： Noel John De Souza ,  Mahesh Vithalbhai Patel ,  Prasad Keshav Deshpande ,  Shiv Kumar Agarwal ,  Shrikant V. Gupte ,  Dilip J. Upadhyay ,  Satish B. Bhawsar ,  Rupinder K. Beri ,  Kandepu Sreenivas ,  Sheela Chandrasekharan Nair ,  Milind Chintaman Shukla ,  Yati Chugh ,  Nitin Shetty ,  Ravindra D. Yeole ,  M. Madhav Reddy

IPC分类号： A61K31/095 ,  A61K31/191 ,  A61K31/47 ,  A61K31/4709 ,  A61K45/06 ,  A61P3/04 ,  A61P11/00 ,  A61P13/10 ,  A61P13/12 ,  A61P19/02 ,  A61P27/16 ,  A61P29/00 ,  A61P31/00 ,  A61P31/04 ,  C07D215/22 ,  C07D215/233 ,  C07D401/04 ,  C07D401/14 ,  C07D413/12 ,  C07D455/04 ,  C07D471/04 ,  C07D471/08 ,  C07D519/00 ,  A61K31/497 ,  C07D215/36 ,  C07D279/12 ,  C07D401/00 ,  C07F5/02

CPC分类号： C07D215/233 ,  A61K31/47 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D413/12 ,  C07D455/04 ,  C07D471/04 ,  C07D471/08

摘要： This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydrates, prodrugs, polymorphs and pseudopolymorphs thereof, to their preparation, to their compositions and to their use.

摘要翻译： 本发明涉及新一代三靶向，手性，广谱抗微生物7-取代的哌啶子基 - 喹诺酮羧酸衍生物，其旋光异构体，非对映异构体或对映异构体，以及其药学上可接受的盐，水合物，前药，多晶型物和假多晶型物 ，准备，组合和使用。

公开(公告)号：US06753333B2

公开(公告)日：2004-06-22

申请号：US10303692

申请日：2002-11-22

申请人： Noel J. De Souza ,  Shivkumar Agarwal ,  Mahesh V. Patel ,  Satish B. Bhawsar ,  Rupinder K. Beri ,  Ravindra D. Yeole ,  Nitin Shetty

发明人： Noel J. De Souza ,  Shivkumar Agarwal ,  Mahesh V. Patel ,  Satish B. Bhawsar ,  Rupinder K. Beri ,  Ravindra D. Yeole ,  Nitin Shetty

IPC分类号： A61K314375

CPC分类号： C07D215/233 ,  A61K31/4745 ,  A61K45/06 ,  C07B2200/07 ,  C07C279/14 ,  C07D401/04 ,  C07D401/14 ,  C07D455/04 ,  C07D471/04 ,  C07D471/08

摘要： The invention relates to the new arginine salt forms of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating antimicrobial infections.

摘要翻译： 本发明涉及新的精氨酸盐形式的S - （ - ） - 9-氟-6,7-二氢-8-（4-羟基哌啶-1-基）-5-甲基-1-氧代-1H，5H- 苯并[i，j]喹嗪-2-羧酸，其制备方法和药物制剂，其包含这些精氨酸盐形式作为其用于治疗抗微生物感染的活性成分。