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1. 发明授权

US5948440A Modified release matrix formulation of cefaclor and cephalexin 失效
标题翻译：头孢克洛和头孢氨苄的改性释放基质配方
公开(公告)号：US5948440A
公开(公告)日：1999-09-07
申请号：US992151
申请日：1997-12-17
申请人： Jagdish Arora , Girish Jain , Himadri Sen
发明人： Jagdish Arora , Girish Jain , Himadri Sen
IPC分类号： A61K9/20 , A61K9/22 , A61K9/28 , A61K9/30 , A61K31/545 , A61K47/38
CPC分类号： A61K31/545 , A61K9/2054 , A61K9/2866 , Y10S514/964
摘要： A pharmaceutical composition in the form of a tablet for controlled release of an active ingredient comprises cefaclor, cephalexin, or their pharmaceutically acceptable hydrates, salts, or esters as active ingredient, and a mixture of hydrophilic polymers of different viscosity grades selected from the group consisting of at least one hydroxypropyl methylcellulose and at least one hydroxypropylcellulose. The composition optionally also contains one or more of a water soluble or water dispersible diluent. The quantities of the hydrophilic polymers and water soluble or water dispersible diluent are such that the therapeutically effective active ingredient is released at a rate suitable for twice daily administration of the pharmaceutical composition to human subjects. The tablets may also be coated with a rapidly dissolving water soluble polymeric film coat. In a preferred embodiment, the composition comprises about 50% to about 90% by weight of cefaclor, cephalexin, or their pharmaceutically acceptable hydrates, salts, or esters, and about 5% to about 35% of a mixture of hydrophilic polymers of different grades, wherein the hydrophilic polymers comprise about 0.1% to about 20% by weight of hydroxypropyl methylcellulose and about 0.1% to about 20% by weight of hydroxypropyl cellulose.
摘要翻译：用于控制释放活性成分的片剂形式的药物组合物包括头孢克洛，头孢氨苄或其药学上可接受的水合物，盐或酯作为活性成分，以及不同粘度等级的亲水聚合物的混合物，其选自的至少一种羟丙基甲基纤维素和至少一种羟丙基纤维素。组合物任选地还含有一种或多种水溶性或水分散性稀释剂。亲水性聚合物和水溶性或水分散性稀释剂的量使得治疗有效的活性成分以适合于每天两次向药物组合物施用给人类受试者的速率释放。片剂也可以用快速溶解的水溶性聚合物膜包衣包衣。在优选的实施方案中，组合物包含约50％至约90％重量的头孢克洛，头孢氨苄或其药学上可接受的水合物，盐或酯，以及约5％至约35％的不同等级的亲水性聚合物的混合物，其中所述亲水性聚合物包含约0.1重量％至约20重量％的羟丙基甲基纤维素和约0.1重量％至约20重量％的羟丙基纤维素。

2. 发明申请

US20070053983A1 Extended release compositions of metoprolol succinate 审中-公开
标题翻译：美托洛尔琥珀酸酯的缓释组合物
公开(公告)号：US20070053983A1
公开(公告)日：2007-03-08
申请号：US11339676
申请日：2006-01-26
申请人： Girish Jain , Mohan Kondapaturu , Utathya Bhadra
发明人： Girish Jain , Mohan Kondapaturu , Utathya Bhadra
IPC分类号： A61K31/205 , A61K9/14
CPC分类号： A61K9/2054 , A61K9/205 , A61K31/205
摘要： The present invention relates to sustained release solid pharmaceutical composition comprising antihypertensives, in particular, Metoprolol succinate or pharmaceutically acceptable derivatives thereof and a process for preparing such a formulation. The present invention is a composition comprising Metoprolol succinate or its pharmaceutically acceptable derivatives thereof and the composition releases the drug over 24 hours. The composition further comprises hydrophilic polymer matrix based tablets. The present invention describes a sustained release tablet comprising sustained release matrix comprising of gelling agents comprising at least one hydrophilic polymer with one or more gum and gum derivatives.
摘要翻译：本发明涉及包含抗高血压药，特别是琥珀酸美托洛尔或其药学上可接受的衍生物的持续释放固体药物组合物和制备该制剂的方法。本发明是包含琥珀酸美托洛尔或其药学上可接受的衍生物的组合物，组合物在24小时内释放药物。组合物还包含基于亲水性聚合物基质的片剂。本发明描述了一种持续释放片剂，其包含由包含至少一种亲水性聚合物与一种或多种胶和胶衍生物的胶凝剂组成的缓释基质。

3. 发明申请

US20060257482A1 Modified release, multiple unit drug delivery systems 审中-公开
标题翻译：改良释放，多单位药物输送系统
公开(公告)号：US20060257482A1
公开(公告)日：2006-11-16
申请号：US10517101
申请日：2003-06-09
申请人： Patrik Kumar , Girish Jain , Ashok Rampal , Ravikumar Nithyanandam , Rajeev Raghuvanshi
发明人： Patrik Kumar , Girish Jain , Ashok Rampal , Ravikumar Nithyanandam , Rajeev Raghuvanshi
IPC分类号： A61K31/553 , A61K31/554 , A61K31/522 , A61K31/496 , A61K31/366 , A61K31/22 , A61K31/137 , A61K9/26
CPC分类号： A61K9/5078 , A61K9/209 , A61K9/5031 , A61K31/137 , A61K31/64
摘要： The invention relates to novel modified release multiple unit systems, and methods of preparing these systems, which can be easily compressed into tablets or filled into capsules or sachets without affecting the desired release characteristics of the pharmaceutical active ingredients incorporated within the systems. The multiple unit tablet includes multiple units. Each unit includes at least one core having an outer surface, a first coating layer surrounding at least a portion of the outer surface of the core and having an outer surface, one or more rate controlling polymers, and one or more one active pharmaceutical ingredients. The coating layer includes one or both of the one or more active pharmaceutical ingredients and the one or more rate controlling polymers. The tablet may further include an outer layer on the outer surface of the unit which includes a material that is one or both of elastic and compressible. The material may be a wax materials, such as polyethylene glycol's (PEGS).
摘要翻译：本发明涉及新型改性释放多单位体系，以及制备这些系统的方法，其可以容易地压制成片剂或填充到胶囊或小药囊中，而不影响并入系统内的药物活性成分的所需释放特征。多单元平板电脑包括多个单元。每个单元包括至少一个具有外表面的芯，围绕芯的外表面的至少一部分并具有外表面，一个或多个速率控制聚合物和一种或多种活性药物成分的第一涂层。涂层包括一种或多种活性药物成分和一种或多种速率控制聚合物中的一种或两种。片剂还可以包括在单元的外表面上的外层，其包括弹性和可压缩之一或两者的材料。该材料可以是蜡材料，例如聚乙二醇（PEGS）。

4. 发明申请

US20060159752A1 Extended release matrix tablets 审中-公开
标题翻译：延长释放矩阵片
公开(公告)号：US20060159752A1
公开(公告)日：2006-07-20
申请号：US10524461
申请日：2003-08-12
申请人： Girish Jain , Orn Anand , Ashok Rampal
发明人： Girish Jain , Orn Anand , Ashok Rampal
IPC分类号： A61K31/736 , A61K31/717 , A61K9/22
CPC分类号： A61K9/2027 , A61K9/205 , A61K9/2054
摘要： The present invention relates to extended release matrix tablets for oral administration that include a cationic polymer, a water-swellable polymer, and an alginic acid derivative to cause the release rate of the active ingredient of the tablets to be independent of pH and gastric residence time. The active pharmaceutical ingredient may be one or more of antibiotics, sympathomimetics, sympatholytic agents, cholinergic agents, antimuscarinics, gastro-intestinal drugs, gentio-urinary smooth muscle relaxants, cardiac drugs, anticonvulsants, tranquilizers and sedatives, and in particular may be an antibiotic, such as cefaclor, or may be a sympatholytic agent, such as carvedilol.
摘要翻译：本发明涉及用于口服给药的延长释放基质片剂，其包括阳离子聚合物，水溶胀性聚合物和藻酸衍生物，以使片剂的活性成分的释放速率与pH和胃停留时间无关。活性药物成分可以是抗生素，拟交感神经，交感神经药，胆碱能药，抗毒蕈碱，胃肠药，龙胆平喘肌松弛剂，心脏药物，抗惊厥药，镇静剂和镇静剂中的一种或多种，特别是抗生素，例如头孢克洛，或者可以是交替溶解剂，例如卡维地洛。

5. 发明申请

US20070244161A1 Novel mercaptophenyl naphthyl methane compounds and synthesis thereof 有权
标题翻译：新型巯基苯基萘甲烷化合物及其合成
公开(公告)号：US20070244161A1
公开(公告)日：2007-10-18
申请号：US11812251
申请日：2007-06-15
申请人： Sangita , Atul Kumar , Man Singh , Girish Jain , Puvvada Sri Ramanchandra Murthy , Suprabhat Ray
发明人： Sangita , Atul Kumar , Man Singh , Girish Jain , Puvvada Sri Ramanchandra Murthy , Suprabhat Ray
IPC分类号： A61K31/12 , A61K31/38 , A61K31/40 , A61K31/44 , A61P19/08 , A61P25/28 , A61P35/00
CPC分类号： C07D295/088 , C07C317/22 , C07C317/24 , C07C323/19 , C07C323/22 , C07C323/25
摘要： Novel mercaptophenyl naphthyl methane compounds, their pharmaceutically acceptable salts and compositions comprised thereof are useful for the prevention or treatment of various medical indications associated with estrogen dependent diseases or syndromes related to osteoporosis, bone loss, bone formation, cardiovascular disorders, neurodegenerative disorders, menopausal disorders, physiological disorders, diabetes disorders, prostatic carcinoma, cancer of breast, cancer of uterus, cancer of the cervix and cancer of the colon, threatened or habitual abortion, obesity, ovarian development or function, post-partum lactation and depression.
摘要翻译：新的巯基苯基萘基甲烷化合物，其药学上可接受的盐和组合物可用于预防或治疗与与雌激素依赖性疾病或与骨质疏松症，骨丢失，骨形成，心血管疾病，神经变性疾病，绝经障碍相关的综合征相关的各种医学适应症，生理障碍，糖尿病，前列腺癌，乳腺癌，子宫癌，宫颈癌和结肠癌，威胁或习惯性流产，肥胖，卵巢发育或功能，产后泌乳和抑郁症。

6. 发明申请

US20050282863A1 Novel-N substituted dihydrobenzothiepino, dihydrobenzoxepino and tetrahydro benzocyclohepta indoles as selective estrogen receptor modulators 审中-公开
标题翻译：新型N取代的二氢苯并硫代磷酸二氢苯并恶磷和四氢苯并环庚烷吲哚作为选择性雌激素受体调节剂
公开(公告)号：US20050282863A1
公开(公告)日：2005-12-22
申请号：US11089907
申请日：2005-03-25
申请人： Kanchan Hajela , Ashok Jha , Man Singh , Girish Jain , Anil Balapure , Anila Dwivedy , Bharat Agarwal , Puvvada Murthy
发明人： Kanchan Hajela , Ashok Jha , Man Singh , Girish Jain , Anil Balapure , Anila Dwivedy , Bharat Agarwal , Puvvada Murthy
IPC分类号： A61K31/407 , A61K31/454 , C07D209/94 , C07D491/04 , C07D495/04 , C07D498/02
CPC分类号： C07D495/04 , C07D209/94 , C07D491/04
摘要： The invention provides a novel class of N-substituted dihydrobenzothiepino, dihydrobenzoxepino and tetrahydro benzocyclohepta indoles and their pharmaceutically acceptable salts, and methods for of synthesizing these compounds. The invention further comprises pharmaceutical compositions and methods of use for these compounds for the treatment of estrogen related diseases or disorders.
摘要翻译：本发明提供了一类新型的N-取代的二氢苯并硫代，二氢苯并氧杂吖啉和四氢苯并环庚烯吲哚及其药学上可接受的盐，以及合成这些化合物的方法。本发明还包括用于这些化合物用于治疗雌激素相关疾病或病症的药物组合物和方法。

7. 发明申请

US20050070597A1 (3R, 4R)-trans-3, 4-diarylchroman derivatives and a method for the prevention and/or treatment of estrogen dependent diseases 失效
标题翻译：（3R，4R） - 反-3,4-二芳基苯并二氢吡喃衍生物和预防和/或治疗雌激素依赖性疾病的方法
公开(公告)号：US20050070597A1
公开(公告)日：2005-03-31
申请号：US10677116
申请日：2003-09-30
申请人： Sangita , Atul Kumar , Man Singh , Suprabhat Ray , Girish Jain
发明人： Sangita , Atul Kumar , Man Singh , Suprabhat Ray , Girish Jain
IPC分类号： C07D311/58 , A61K31/541 , A61K31/353 , A61K31/452 , A61K31/496 , A61K31/5377 , C07D45/02
CPC分类号： C07D311/58
摘要： The present invention relates to compounds of the formula I in which substituents R2 and R3 are arranged in trans-configuration: wherein: R1 is H or C1-C6 alkyl; C3-C7 cycloalkyl; R2 is phenyl, optionally substituted with 1 to 5 substituents independently selected from the group comprising OH, C1-C6-alkyl, halogen, nitro, cyano, SH, SR4, trihalo-C1-C6-alkyl, C1-C6-alkoxy and phenyl, wherein R4 is C1-C6 alkyl; R3 is phenyl substituted with OR5 wherein R5 has the formula (II), (III) or (IV) wherein Y is chosen from NHR4, NR42, NHCOR4, NHSO2R4, CONHR4, CONR4, CONR42, COOH, COOR4, SO2R4, SOR4, SONHR4, SONR42, a C3-C7 heterocyclic ring, saturated or unsaturated, containing one or two heteroatoms independently selected from the group consisting of O, S and N, optionally being substituted with 1 to 3 substituents independently selected from the group comprising H, OH, halogen, nitro, cyano, SH, SR4, trihalo-C1-C6-alkyl, C1-C6-alkyl and C1-C6-alkoxy, preferably NHR4, NR24, or a nitrogen heterocycle, wherein R4 is as defined above, and the esters, ethers, and salts of the compounds of formula I, optionally along pharmaceutically acceptable excipients, a process for the preparation of the same, and a method of preventing and/or treating estrogen-related disease conditions in a subject using compounds of formula 1, or its salts, optionally along with pharmaceutically acceptable excipients.
摘要翻译：本发明涉及式I化合物，其中取代基R 2和R 3以反式构型排列：其中：R 1是H或C 1 -C 6烷基; C3-C7环烷基; R 2是苯基，任选地被1至5个独立地选自OH，C 1 -C 6 - 烷基，卤素，硝基，氰基，SH，SR 4， - 3卤代-C 1 -C 6烷基，C 1 C 1-6 - 烷氧基和苯基，其中R 4是C 1 -C 6烷基; R 3是被OR 5取代的苯基，其中R 5具有式（II），（III）或（IV），其中Y选自NHR 4，NR 4，NHCOR 4 >，NHSO 2 R 4，CONHR 4，CONR 4，CONR 4，COOH，COOR 4，SO 2 R 4，SOR 4，SONHR 4，SONR 4 饱和或不饱和的C3-C7杂环，其含有一个或两个独立地选自O，S和N的杂原子，任选被1至3个独立地选自H，OH，卤素，硝基，氰基，SH，SR 4，三卤代-C 1 -C 6烷基，C 1 -C 6烷基和C 1 -C 6烷氧基，优选NH 4，NR 2 4或氮杂环， 4>如上所定义，并且式I化合物的酯，醚和盐，任选地沿着药学上可接受的赋形剂，其制备方法，以及预防和/或治疗雌激素相关疾病的方法使用式1化合物的受试者的条件，或其盐，任选地与药物 lly可接受的赋形剂。

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