公开(公告)号：US20120165320A1

公开(公告)日：2012-06-28

申请号：US13380744

申请日：2010-06-22

申请人： Rajseh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Gurmeet Kaur ,  Sandeep Kanwar ,  Nishan Singh ,  Gurmeet Kaur Nanda ,  Sitaram Kumar Magadi ,  Sudhir Kumar Sharma

发明人： Rajseh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Gurmeet Kaur ,  Sandeep Kanwar ,  Nishan Singh ,  Gurmeet Kaur Nanda ,  Sitaram Kumar Magadi ,  Sudhir Kumar Sharma

IPC分类号： A61K31/422 ,  C07D413/14 ,  A61K31/4439 ,  A61K31/5377 ,  A61P25/00 ,  A61K31/403 ,  C07D417/10 ,  A61K31/541 ,  A61K31/551 ,  A61K31/5513 ,  C07D413/10 ,  C07D403/10

CPC分类号： C07D221/22 ,  C07D209/52 ,  C07D401/10 ,  C07D409/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/08

摘要： The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.

摘要翻译： 本发明涉及式I的新化合物，其药学上可接受的衍生物，互变异构体，立体异构体，包括R和S异构体，多晶型物，前药，代谢物，盐或溶剂化物。 本发明还涉及合成式I的新化合物，其药学上可接受的衍生物，互变异构体形式，立体异构体，多晶型物，前药，代谢物，盐或溶剂合物的方法。

公开(公告)号：US20110245258A1

公开(公告)日：2011-10-06

申请号：US13130440

申请日：2009-11-18

申请人： Rajesh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Sandeep Kanwar ,  Sitaram Kumar Magadi ,  Sudhir Kumar Sharma

发明人： Rajesh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Sandeep Kanwar ,  Sitaram Kumar Magadi ,  Sudhir Kumar Sharma

IPC分类号： A61K31/4985 ,  C07D487/04 ,  A61K31/519 ,  A61P31/04 ,  A61P31/16 ,  A61P31/06

CPC分类号： C07D487/04 ,  C07D263/20 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： The present invention relates to novel phenyl oxazolidinone compounds of formula I, their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of formula I or their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of formula I and methods of using them. The compounds of the present invention are useful as antimicrobial agents, effective against a number of aerobic and/or anaerobic Gram positive and/or Gram negative pathogens such as multi drug resistant species of Staphylococcus, Streptococcus, Enterococcus, Bacterioides, Clostridia, H. influenza, Moraxella, acid-fast organisms such as Mycobacterium tuberculosis as well as Linezolid resistant species of Staphylococcus and Enterococcus.

摘要翻译： 本发明涉及式I的新型苯基恶唑烷酮化合物，其药学上可接受的类似物，互变异构形式，立体异构体，多晶型物，前药，代谢物，盐或溶剂化物。 本发明还涉及合成新型式I化合物或其药学上可接受的类似物，互变异构体形式，立体异构体，多晶型物，前药，代谢物，盐或溶剂合物的方法。 本发明还提供了包含新颖的式I化合物和使用它们的方法的药物组合物。 本发明的化合物可用作抗微生物剂，对许多需氧和/或厌氧革兰氏阳性和/或革兰氏阴性病原体有效，如葡萄球菌，链球菌，肠球菌，细菌，梭菌，流感嗜血杆菌 ，莫拉氏菌，耐酸菌，如结核分枝杆菌，以及耐盐霉菌属的霉菌和肠球菌。

公开(公告)号：US20090317464A1

公开(公告)日：2009-12-24

申请号：US12305025

申请日：2007-07-05

申请人： Amarjit Singh ,  Sarabjit Singh ,  Shivanand Puthli

发明人： Amarjit Singh ,  Sarabjit Singh ,  Shivanand Puthli

IPC分类号： A61K9/24 ,  A61K31/167 ,  A61K9/20 ,  A61P5/28

CPC分类号： A61K31/10 ,  A61K9/2018 ,  A61K9/2846 ,  A61K9/2886 ,  A61K31/167

摘要： The invention provides a method and a composition for producing an anti-androgenic effect in a mammal. The method comprises administering a modified release pharmaceutical composition of bicalutamide to a mammal, with a reduced dosing frequency, for improved patient convenience and compliance. The composition of the invention also provides for a higher bioavailability and improved pharmacokinetic profile as compared to a conventional bicalutamide composition.

摘要翻译： 本发明提供了一种用于在哺乳动物中产生抗雄激素作用的方法和组合物。 该方法包括向哺乳动物施用改性释放的药物组合物，其具有降低的给药频率，以改善患者的便利性和依从性。 与常规比卡鲁胺组合物相比，本发明的组合物还提供更高的生物利用度和改善的药代动力学特征。

公开(公告)号：US20090258896A1

公开(公告)日：2009-10-15

申请号：US12299317

申请日：2007-05-09

申请人： Rajesh Jain ,  Kour Chand Jindal

发明人： Rajesh Jain ,  Kour Chand Jindal

IPC分类号： A61K31/437 ,  A61K31/405 ,  A61P3/10

CPC分类号： A61K36/48 ,  A61K31/045 ,  A61K36/82 ,  A61K2300/00

摘要： Novel compositions comprising a combination of at least one higher primary aliphatic alcohol preferably selected from those having 18 to 40 carbon atoms or mixtures thereof, at least one source of 5-hydroxytryptophan (5-HTP) optionally additionally comprising a source of caffeine and/or catechin-polyphenol and/or epigallocatechin gallate as active agents, either alone or in combination with other active agent(s), optionally with one or more excipient(s) are provided. Particularly, the invention relates to compositions and process for preparation of such compositions and method of use thereof for the management of obesity and associated disorders.

摘要翻译： 包含至少一种优选选自具有18-40个碳原子的高级伯脂肪醇或其混合物的至少一种5-羟基色氨酸（5-HTP）的组合的新型组合物任选地另外包含咖啡因和/或 儿茶素多酚和/或表没食子儿茶素没食子酸酯作为活性剂，单独或与其它活性剂，任选地与一种或多种赋形剂组合使用。 特别地，本发明涉及用于制备这种组合物的组合物和方法及其用于治疗肥胖症和相关疾病的方法。

公开(公告)号：US20080247962A1

公开(公告)日：2008-10-09

申请号：US10586545

申请日：2005-01-19

申请人： Rajesh Jain ,  Kour Chand Jindal ,  Sukhjeet Singh

发明人： Rajesh Jain ,  Kour Chand Jindal ,  Sukhjeet Singh

IPC分类号： A61K9/12 ,  A61K31/045 ,  A61K31/40 ,  A61P3/00 ,  A61K31/351

CPC分类号： A61K31/366 ,  A61K31/045 ,  A61K31/40 ,  A61K45/06 ,  A61K2300/00

摘要： A novel pharmaceutical composition comprising a mixture of higher primary aliphatic alcohols from (24) to (39) carbon atoms; at least one another component selected from resins and pigments, hydrocarbons, esters, ketones and aldehydes, and phenolic compounds, and HMG CoA reductase inhibitor, its salts, analogs or derivatives thereof, preferably statins, optionally with pharmaceutically acceptable excipients, and process of preparation of such composition is provided. Also provided are method of treatment and use of such composition for reducing abnormal lipid parameters associated with hyperlipidemia.

摘要翻译： 一种新型药物组合物，其包含来自（24）至（39）个碳原子的较高级脂族醇的混合物; 选自树脂和颜料，烃，酯，酮和醛中的至少一种组分和酚类化合物，和HMG CoA还原酶抑制剂，其盐，类似物或衍生物，优选他汀类，任选地具有药学上可接受的赋形剂，以及制备方法 提供了这种组合物。 还提供了治疗和使用这种组合物以减少与高脂血症相关的异常脂质参数的方法。

公开(公告)号：US20070219175A1

公开(公告)日：2007-09-20

申请号：US10551058

申请日：2005-01-05

申请人： Rajesh Jain ,  Kour Jindal ,  Sukhjeet Singh

发明人： Rajesh Jain ,  Kour Jindal ,  Sukhjeet Singh

IPC分类号： A61K31/43

CPC分类号： A61K9/2095 ,  A61K9/1635 ,  A61K9/2081 ,  A61K9/5026 ,  A61K9/5036 ,  A61K9/5042 ,  A61K31/43 ,  A61K45/06 ,  A61K2300/00

摘要： Rapidly disintegrating oral controlled release pharmaceutical compositions and process for preparation of such compositions are provided. The compositions preferably comprise antibiotic(s) as active ingredient, more preferably amoxicillin either alone or in combination with other antibiotic(s). The controlled release compositions comprise at least one active ingredient, and a polymer system comprising of at least two polymers which retard the release of the active ingredient in the stomach while providing rapid release of the said active ingredient in the alkaline contents of small intestine, optionally with other pharmaceutically acceptable excipients. The compositions provide therapeutically effective levels of the active ingredient for extended periods of time, and possess bioadhesive properties.

摘要翻译： 提供快速崩解的口服释药药物组合物和制备这些组合物的方法。 组合物优选包含抗生素作为活性成分，更优选单独或与其它抗生素组合使用阿莫西林。 控释组合物包含至少一种活性成分和包含至少两种聚合物的聚合物体系，所述聚合物延缓了胃中活性成分的释放，同时提供所述活性成分在小肠的碱性成分中的快速释放，任选地 与其它药学上可接受的赋形剂。 该组合物延长时间段提供治疗有效水平的活性成分，并且具有生物粘合性质。

公开(公告)号：US2159383A

公开(公告)日：1939-05-23

申请号：US13666337

申请日：1937-04-13

申请人： UNITED CARR FASTENER CORP

发明人： JONES WALTER I

IPC分类号： A47C31/02

CPC分类号： A47C31/02 ,  Y10T24/3499 ,  Y10T24/4727 ,  Y10T24/497

公开(公告)号：US08841306B2

公开(公告)日：2014-09-23

申请号：US13130440

申请日：2009-11-18

申请人： Rajesh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Sandeep Kanwar ,  Sitaram Kumar Magadi ,  Sudhir Kumar Sharma

发明人： Rajesh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Sandeep Kanwar ,  Sitaram Kumar Magadi ,  Sudhir Kumar Sharma

IPC分类号： A61K31/33 ,  C07D413/14 ,  C07D417/12 ,  C07D487/04 ,  C07D413/12 ,  C07D263/20

CPC分类号： C07D487/04 ,  C07D263/20 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： The present invention relates to novel phenyl oxazolidinone compounds of formula I, their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of formula I or their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of formula I and methods of using them. The compounds of the present invention are useful as antimicrobial agents, effective against a number of aerobic and/or anaerobic Gram positive and/or Gram negative pathogens such as multi drug resistant species of Staphylococcus, Streptococcus, Enterococcus, Bacterioides, Clostridia, H. influenza, Moraxella, acid-fast organisms such as Mycobacterium tuberculosis as well as Linezolid resistant species of Staphylococcus and Enterococcus.

摘要翻译： 本发明涉及式I的新型苯基恶唑烷酮化合物，其药学上可接受的类似物，互变异构形式，立体异构体，多晶型物，前药，代谢物，盐或溶剂化物。 本发明还涉及合成新型式I化合物或其药学上可接受的类似物，互变异构体形式，立体异构体，多晶型物，前药，代谢物，盐或溶剂合物的方法。 本发明还提供了包含新颖的式I化合物和使用它们的方法的药物组合物。 本发明的化合物可用作抗微生物剂，对许多需氧和/或厌氧革兰氏阳性和/或革兰氏阴性病原体有效，如葡萄球菌，链球菌，肠球菌，细菌，梭菌，流感嗜血杆菌 ，莫拉氏菌，耐酸菌，如结核分枝杆菌，以及耐盐霉菌属的霉菌和肠球菌。

公开(公告)号：US20110130434A1

公开(公告)日：2011-06-02

申请号：US13055778

申请日：2009-07-28

申请人： Rajesh Jain ,  Sarabjit Singh

发明人： Rajesh Jain ,  Sarabjit Singh

IPC分类号： A61K31/403 ,  A61P9/12

CPC分类号： A61K9/4808 ,  A61K9/2009 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/2846 ,  A61K31/403

摘要： The invention relates to a modified release pharmaceutical composition comprising ramipril or pharmaceutically acceptable salts thereof and pharmaceutically acceptable excipient(s) wherein pharmaceutical composition is bioequivalent to conventional immediate release formulation of ramipril administered twice daily. The invention further relates to a modified release pharmaceutical composition comprising: an immediate release component comprising ramipril or pharmaceutically acceptable salts thereof and a modified release component comprising ramipril or pharmaceutically acceptable salts thereof. The invention further relates to the process for the preparation of modified release pharmaceutical composition of ramipril.

摘要翻译： 本发明涉及包含雷米普立或其药学上可接受的盐和药学上可接受的赋形剂的改性释放药物组合物，其中药物组合物与常规立即释放的雷米普利制剂每天两次生物等效。 本发明还涉及一种调释释放药物组合物，其包含：包含雷米普立或其药学上可接受的盐的速释组分和包含雷米普利或其药学上可接受的盐的缓释组分。 本发明还涉及制备雷米普里缓释药物组合物的方法。

公开(公告)号：US20110091536A1

公开(公告)日：2011-04-21

申请号：US12995436

申请日：2009-05-28

申请人： Rajesh Jain ,  Sukhjeet Singh ,  Shilpa Bhasin

发明人： Rajesh Jain ,  Sukhjeet Singh ,  Shilpa Bhasin

IPC分类号： A61K36/47 ,  A61K9/14 ,  A61K9/28 ,  A61K9/20 ,  A61K9/48 ,  A61K9/50 ,  A61P1/00 ,  A61P29/00

CPC分类号： A61K36/47 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/284 ,  A61K9/2886 ,  A61K9/4858 ,  A61K9/4866

摘要： Oral pharmaceutical compositions comprising dry extract of Euphorbia prostrata from about 0.1% to about 99% by weight wherein the effective average particle size of the dry extract of Euphorbia prostrata is not more than about 500 microns with pharmaceutically acceptable excipient(s) and process(s) for the preparation of such compositions useful for the treatment of anorectal disease and colonic diseases such as hemorrhoids, fissures, cracks, fistulas, abscesses, inflammatory bowel disease and the like are provided. Further, the pharmaceutical compositions of the present invention provides for the administration of a therapeutically and/or prophylactically effective amount of the Euphorbia prostrata wherein the compositions possess properties to control inflammation, prevent capillary bleeding and fragility in mammalians, particularly human beings. Furthermore, the compositions preferably provides a release of not less than about 50% of the dry extract of Euphorbia prostrata in first 15 minutes and not less than about 80% of dry extract of Euphorbia prostrata after total dissolution study of about 60 minutes when tested in accordance with the dissolution method described herein employing physiological pH range of about 2 to about 7.5 optionally with surfactant(s). Preferably the compositions of the present invention are in the form of tablets, minitablets, powders, capsules, pellets, granules, beads, compacts and the like. The present invention also provides and prophylactic and/or therapeutic methods of using such compositions for the treatment of anorectal diseases including hemorrhoids and colonic diseases.

摘要翻译： 包含约0.1％至约99％重量的大戟草干提取物的口服药物组合物，其中大戟属干提取物的有效平均粒度不超过约500微米，其药学上可接受的赋形剂和方法 ）用于制备用于治疗肛门直肠疾病和结肠疾病如痔疮，裂隙，裂缝，瘘，脓肿，炎性肠病等的组合物。 此外，本发明的药物组合物提供治疗和/或预防有效量的大戟蒿的施用，其中所述组合物具有控制哺乳动物，特别是人类的炎症，防止毛细血管出血和脆性的性质。 此外，组合物优选提供在前15分钟内不少于约50％的大戟干提取物的释放，并且在大约60分钟的总溶出度研究后，在大约60分钟的时间内测试时，不少于约80％的大戟草干提取物的释放 根据本文所述的溶解方法，其使用任选具有表面活性剂的约2至约7.5的生理pH范围。 优选地，本发明的组合物是片剂，微型药物，粉剂，胶囊，丸剂，颗粒剂，珠粒，压块等的形式。 本发明还提供了使用这些组合物治疗包括痔疮和结肠疾病在内的肛门疾病的预防和/或治疗方法。