公开(公告)号：US20130338193A1

公开(公告)日：2013-12-19

申请号：US13995336

申请日：2012-01-12

申请人： Dinesh Kumar Dikshit ,  Madhu Dikshit ,  Tanveer Irshad Siddiqui ,  Anil Kumar ,  Rabi Sankar Bhata ,  Girish Kumar Jain ,  Manoj Kumar Barthwal ,  Ankita Misra ,  Vivek Khanna ,  Prem Prakash ,  Manish Jain ,  Vishal Singh ,  Varsha Gupta ,  Anil Kumar Dwivedi

发明人： Dinesh Kumar Dikshit ,  Madhu Dikshit ,  Tanveer Irshad Siddiqui ,  Anil Kumar ,  Rabi Sankar Bhata ,  Girish Kumar Jain ,  Manoj Kumar Barthwal ,  Ankita Misra ,  Vivek Khanna ,  Prem Prakash ,  Manish Jain ,  Vishal Singh ,  Varsha Gupta ,  Anil Kumar Dwivedi

IPC分类号： C07D401/06

CPC分类号： A61K31/454 ,  C07B53/00 ,  C07D401/06

摘要： Chiral 1-(4-methylphenylmethyl)-5-oxo-{N-[(3-t-butoxycarbonyl-aminomethyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamides as inhibitors of collagen induced platelet activation and adhesion The present invention provides chiral (2S)-1-(4-methyl-phenylmethyl)-5-oxo-(3S)-{N-[(3-t butoxycarbonyl aminomethyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamide, and (2S)-1-(4-methylphenylmethyl)-5-oxo-(3R)-{N-[(3-t-butoxycarbonyl amino methyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamide of formula 6 and 7 respectively. The present invention also relates to use of these moieties as inhibitors of collagen induced platelet adhesion and aggregation mediated through collagen receptors. The present invention provides a process for preparation of chiral carboxamides of formula 6 and 7 using the process which has advantage to avoid any racemization at the a-carboxylic center, during N-alkylation. The reagent LiHMDS is used at low temperatures to furnish methyl N-(p methylphenylmethyl)lpyroglutamate in good chiral purity.

摘要翻译： 手性1-（4-甲基苯基甲基）-5-氧代 - {N - [（3-叔丁氧基羰基 - 氨基甲基）] - 哌啶-1-基} - 吡咯烷-2-甲酰胺作为胶原诱导的血小板活化和粘附抑制剂 本发明提供手性（2S）-1-（4-甲基 - 苯基甲基）-5-氧代 - （3S） - {N - [（3-叔丁氧基羰基氨基甲基）] - 哌啶-1-基} - 吡咯烷-2-酮 （2S）-1-（4-甲基苯基甲基）-5-氧代 - （3R） - {N - [（3-叔丁氧基羰基氨基甲基）] - 哌啶-1-基} - 吡咯烷-2-甲酰胺 分别为式6和7。 本发明还涉及这些部分作为通过胶原受体介导的胶原诱导的血小板粘附和聚集的抑制剂的用途。 本发明提供了一种制备式6和7的手性羧酰胺的方法，该方法在N-烷基化过程中有利于避免在α-羧酸中心的任何外消旋化。 在低温下使用试剂LiHMDS以提供良好的手性纯度的N-（p甲基苯基甲基）l吡咯烷酸甲酯。

公开(公告)号：US20110112042A1

公开(公告)日：2011-05-12

申请号：US12920927

申请日：2009-03-03

申请人： Rakesh Maurya ,  Preeti Rawat ,  Kunal Sharan ,  Jawed Akhtar Siddiqui ,  Gaurav Swarnkar ,  Geetanjali Mishra ,  Lakshmi Manickavasagam ,  Girish Kumar Jain ,  Kamal Ram Arya ,  Naibedya Chattopadhyay

发明人： Rakesh Maurya ,  Preeti Rawat ,  Kunal Sharan ,  Jawed Akhtar Siddiqui ,  Gaurav Swarnkar ,  Geetanjali Mishra ,  Lakshmi Manickavasagam ,  Girish Kumar Jain ,  Kamal Ram Arya ,  Naibedya Chattopadhyay

IPC分类号： A61K31/7048 ,  C07H7/06 ,  C07H1/08 ,  A61P19/08

CPC分类号： C07H7/06 ,  C07D405/04

摘要： The present invention provides a flavonol compound and a bioactive extract/fraction from Ulmus wallichiana useful for the management or prevention or treatment of bone disorders. Said extract/fraction comprising marker compounds of general formula 2, K058: R1═R2═0H K012: R1═R2═OH, 2,3 double bond K068: R1═R2═H KIOOi R1═OH, R2═H mula 2 Wherein the marker compounds K012, K058, K068, K100 ranges 6.7-12%, 1.7-4.5%, 0.6-1.2%, 1.7-4.5% respectively in alcoholic extract and a process of extraction thereof. According to another aspect of the invention provides a pharmaceutical composition comprising the said compound. The present invention further provides a method of treating bone disorders by administering the pharmaceutical composition by oral, intravenous, subcutaneous, intra-peritoneal or intramuscular route.

摘要翻译： 本发明提供了一种黄酮醇化合物和可用于治疗或预防或治疗骨骼疾病的来自榆树的生物活性提取物/部分。 所述提取物/级分包含通式2的标记化合物，K058：R1 = R2 = 0H，K012：R1 = R2 = OH，2,3双键，K068：R1 = R2 = H，KIOO，R1 = OH，R2 = H， 标记化合物K012，K058，K068，K100分别在酒精提取物中分别为6.7-12％，1.7-4.5％，0.6-1.2％，1.7-4.5％及其提取方法。 根据本发明的另一方面，提供了包含所述化合物的药物组合物。 本发明还提供了通过口服，静脉内，皮下，腹膜内或肌肉内途径施用药物组合物来治疗骨病的方法。

公开(公告)号：US20110086070A1

公开(公告)日：2011-04-14

申请号：US12934122

申请日：2008-09-26

申请人： Munish Talwar ,  Rahul Dabre ,  Ritesh Kapoor ,  Himanshu Verma ,  Nitin Jain ,  Girish Kumar Jain

发明人： Munish Talwar ,  Rahul Dabre ,  Ritesh Kapoor ,  Himanshu Verma ,  Nitin Jain ,  Girish Kumar Jain

IPC分类号： A61K31/235 ,  A61K31/192 ,  A61K9/00

CPC分类号： A61K9/0056 ,  A61K9/2054 ,  A61K9/7007 ,  A61K31/192 ,  A61K31/235

摘要： The invention relates to orally disintegrating pharmaceutical compositions comprising rhein or diacerein, or salts or esters or prodrugs thereof, and processes for preparing such compositions.

摘要翻译： 本发明涉及包含大黄酸或双醋瑞因或其盐或酯或前药的口服崩解药物组合物，以及制备该组合物的方法。

公开(公告)号：US20110070300A1

公开(公告)日：2011-03-24

申请号：US12954644

申请日：2010-11-25

申请人： Prashant Manohar MANDAOGADE ,  Venkatesh Madhavacharya Joshi ,  Saurabh Srivastava ,  Vinayak Dinkar Kadam ,  Girish Kumar Jain

发明人： Prashant Manohar MANDAOGADE ,  Venkatesh Madhavacharya Joshi ,  Saurabh Srivastava ,  Vinayak Dinkar Kadam ,  Girish Kumar Jain

IPC分类号： A61K9/48 ,  A61K9/00 ,  A61K9/20 ,  A61K9/50 ,  A61K31/435 ,  A61K31/138 ,  A61K31/554 ,  A61K31/18 ,  A61K31/196 ,  A61K31/496 ,  A61K31/137 ,  A61P43/00

CPC分类号： A61K31/138 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/2077 ,  A61K9/5047 ,  A61K9/5078

摘要： The present invention relates to extended release dosage forms of metoprolol or salts thereof comprising a water insoluble and non-swellable inert core and one or more pharmaceutically acceptable excipients. The invention also relates to processes for the preparation of an inert core and extended release dosage forms.

摘要翻译： 本发明涉及美托洛尔或其盐的延长释放剂型，其包含水不溶性和不可溶胀的惰性核心和一种或多种药学上可接受的赋形剂。 本发明还涉及制备惰性核心和延长释放剂型的方法。

公开(公告)号：US07582653B2

公开(公告)日：2009-09-01

申请号：US11812251

申请日：2007-06-15

申请人： Sangita ,  Atul Kumar ,  Man Mohan Singh ,  Girish Kumar Jain ,  Puvvada Sri Ramanchandra Murthy ,  Suprabhat Ray

发明人： Sangita ,  Atul Kumar ,  Man Mohan Singh ,  Girish Kumar Jain ,  Puvvada Sri Ramanchandra Murthy ,  Suprabhat Ray

IPC分类号： A61K31/4453 ,  A61K31/40 ,  A61K31/135 ,  A61K31/12 ,  C07D295/04 ,  C07C317/14 ,  C07C321/00

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。

公开(公告)号：US20090208570A1

公开(公告)日：2009-08-20

申请号：US12225746

申请日：2007-03-28

申请人： Prashant Manohar Mandaogade ,  Venkatesh Madhavacharya Joshi ,  Saurabh Srivastava ,  Vinayak Dinkar Kadam ,  Girish Kumar Jain

发明人： Prashant Manohar Mandaogade ,  Venkatesh Madhavacharya Joshi ,  Saurabh Srivastava ,  Vinayak Dinkar Kadam ,  Girish Kumar Jain

IPC分类号： A61K9/62 ,  A61K9/58 ,  A61K9/22 ,  A61K9/16 ,  A61K31/138 ,  A61P9/00 ,  A61P9/04 ,  A61P9/12

CPC分类号： A61K31/138 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/2077 ,  A61K9/5047 ,  A61K9/5078

摘要： The present invention relates to extended release dosage forms of metoprolol or salts thereof comprising a water insoluble and non-swellable inert core and one or more pharmaceutically acceptable excipients. The invention also relates to processes for the preparation of an inert core and extended release dosage forms.

摘要翻译： 本发明涉及美托洛尔或其盐的延长释放剂型，其包含水不溶性和不可溶胀的惰性核心和一种或多种药学上可接受的赋形剂。 本发明还涉及制备惰性核心和延长释放剂型的方法。

公开(公告)号：US09119819B2

公开(公告)日：2015-09-01

申请号：US12989966

申请日：2008-09-23

申请人： Himanshu Verma ,  Rahul Dabre ,  Girish Kumar Jain

发明人： Himanshu Verma ,  Rahul Dabre ,  Girish Kumar Jain

IPC分类号： A61K31/215 ,  A61K31/192 ,  A61P19/02 ,  A61K9/00

CPC分类号： A61K31/192 ,  A61K9/0095

摘要： The invention relates to liquid pharmaceutical compositions for oral administration comprising rhein or diacerein, or salts or esters or prodrugs thereof and processes for preparing such compositions.

摘要翻译： 本发明涉及用于口服给药的液体药物组合物，其包含大黄酸或双醋瑞因，或其盐或酯或前药及其制备方法。

公开(公告)号：US20140079834A1

公开(公告)日：2014-03-20

申请号：US14113561

申请日：2012-04-25

申请人： Rakesh Maurya ,  Preety Dixit ,  Ritu Trivedi ,  Vikram Khedgikar ,  Jyoti Gautam ,  Avinash Kumar ,  Divya Singh ,  Sheelendra Pratap Singh ,  (none) Wahajuddin ,  Girish Kumar Jain ,  Naibedya Chattopadhyay

发明人： Rakesh Maurya ,  Preety Dixit ,  Ritu Trivedi ,  Vikram Khedgikar ,  Jyoti Gautam ,  Avinash Kumar ,  Divya Singh ,  Sheelendra Pratap Singh ,  (none) Wahajuddin ,  Girish Kumar Jain ,  Naibedya Chattopadhyay

IPC分类号： A61K31/7048 ,  A61K31/352 ,  A61K36/48

CPC分类号： A61K31/7048 ,  A61K31/352 ,  A61K36/48 ,  C07D311/36 ,  C07H17/07

摘要： The present invention relates to bioactive fractions and compounds from Dalbergia sissoo for the prevention or treatment of osteo-health related disorders. The present invention relates in the field of pharmaceutical composition that provides new plant extracts, their fractions and pure compound isolated from natural sources that are useful for the prevention and/or treatment of various medical indications associated with estrogen dependent or independent diseases or syndromes or disorders preferably in the prevention or treatment of estrogen dependent or independent diseases or syndromes or disorders caused in humans and animals, and achievement of peak bone mass during skeletal growth and health in humans and animals. Particularly the present invention further relates to the processes for the preparation of biologically active extracts, fractions, and isolation of pure compounds, from Dalbergia sissoo plant from the family Fabaceae their pharmaceutically acceptable salts and compositions of the principal aspect of the present invention.

摘要翻译： 本发明涉及用于预防或治疗与骨骼健康相关的疾病的生物活性级分和来自枸杞子的化合物。 本发明涉及药物组合物领域，其提供新的植物提取物，其级分和从天然来源分离的纯化合物，其可用于预防和/或治疗与雌激素依赖性或独立疾病或综合征或病症相关的各种医学适应症 优选地在预防或治疗在人和动物中引起的雌激素依赖性或独立性疾病或综合征或障碍，以及在人和动物的骨骼生长和健康期间达到峰值骨量。 特别地，本发明还涉及从家蚕豆科的Dalbergia sissoo植物制备生物活性提取物，级分和分离纯化合物的方法，它们的药学上可接受的盐和本发明主要方面的组合物。

公开(公告)号：US20130059062A1

公开(公告)日：2013-03-07

申请号：US13582452

申请日：2011-03-07

申请人： Ramakant Kashinath Gundu ,  Rahul Sudhakar Dabre ,  Girish Kumar Jain

发明人： Ramakant Kashinath Gundu ,  Rahul Sudhakar Dabre ,  Girish Kumar Jain

IPC分类号： B28B7/18 ,  A61K9/28

CPC分类号： B30B15/065 ,  A61K9/2072

摘要： This invention is related to a device for the manufacture of a dosage form with a hole and method of manufacture. The dosage form may be a modified release dosage form comprising a core coated with a polymeric coat comprising one or more rate controlling polymers, said dosage form having a hole extending through the dosage form resulting in an inner radial surface and an outer radial surface, said core comprising at least one therapeutically active ingredient, characterized in that the inner radial surface is partially coated with said polymeric coat.

摘要翻译： 本发明涉及一种用于制造具有孔的剂型和制造方法的装置。 剂型可以是包含涂覆有包含一种或多种速率控制聚合物的聚合物涂层的芯的调释剂型，所述剂型具有延伸穿过剂型的孔，产生内径向表面和外径向表面，所述孔 芯包含至少一种治疗活性成分，其特征在于，所述内部径向表面部分地涂覆有所述聚合物涂层。

公开(公告)号：US20110229566A1

公开(公告)日：2011-09-22

申请号：US13060180

申请日：2009-08-22

申请人： Yatendra Kumar Gupta ,  Girish Kumar Jain ,  Munish Talwar ,  Manoj Mashalkar

发明人： Yatendra Kumar Gupta ,  Girish Kumar Jain ,  Munish Talwar ,  Manoj Mashalkar

IPC分类号： A61K9/52 ,  A61K31/277 ,  A61P25/16 ,  A61K9/24

CPC分类号： A61K45/06 ,  A61K9/2059 ,  A61K9/209 ,  A61K31/198 ,  A61K31/277 ,  A61K2300/00

摘要： There is provided a single unit oral dose pharmaceutical composition comprising a) levodopa or salts thereof from about 50 mg to about 300 mg in extended release form, b) carbidopa or salts thereof from about 10 mg to about 100 mg in extended release and c) entacapone or salts thereof from about 100 mg to about 1000 mg in immediate release form, optionally with other pharmaceutically acceptable excipients. The invention also relates to process of preparation of such compositions.

摘要翻译： 提供单一口服剂量的单一药物组合物，其包含a）左旋多巴或其盐，其以延长释放形式约50mg至约300mg，b）卡比多巴或其盐在约10mg至约100mg的延长释放中，c） 恩他卡朋或其盐以约100mg至约1000mg的速释形式，任选地与其它药学上可接受的赋形剂。 本发明还涉及这种组合物的制备方法。