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1. 发明授权

US06326023B1 Synergistic anti-malarial formulation 失效
标题翻译：协同反疟制剂
公开(公告)号：US06326023B1
公开(公告)日：2001-12-04
申请号：US09537246
申请日：2000-03-28
申请人： Guru Prakash Dutta , Dharam Chand Jain , Ranjendra Singh Bhakuni , Sudhanshu Saxena , Sangeeta Dhawan , Suman Preet Singh Khanuja , Sushil Kumar , Renu Tripathi , Aseem Umesh , Nuzhat Kamal , Anil Kumar Dwivedi , Satyawan Singh
发明人： Guru Prakash Dutta , Dharam Chand Jain , Ranjendra Singh Bhakuni , Sudhanshu Saxena , Sangeeta Dhawan , Suman Preet Singh Khanuja , Sushil Kumar , Renu Tripathi , Aseem Umesh , Nuzhat Kamal , Anil Kumar Dwivedi , Satyawan Singh
IPC分类号： A61K902
CPC分类号： A61K45/06 , A61K9/0031 , A61K9/4858 , A61K31/357 , A61K47/44 , Y02A50/411 , Y10S514/966 , A61K2300/00
摘要： The present invention relates to a synergistic formulation comprising pharmaceutically effective amount of &agr;/&bgr; arteether and a neutralized refined vegetable oil suitable for administration by rectal route, method for the treatment of cerebral and comatose malaria and process for the preparation of the said formulation.
摘要翻译：本发明涉及包含药学有效量的α/β糖精和适于通过直肠途径给药的中和精制植物油，用于治疗脑和昏迷病疟疾的方法和制备所述制剂的方法的协同制剂。

2. 发明申请

US20110077294A1 R-(-) / S-(+)-7-[3-N SUBSTITUTED AMINO-2 HYDROXYPROPOXY] FLAVONES 审中-公开
标题翻译： R - （ - ）/ S - （+） - 7- [3-N取代的氨基-2-羟基丙氧基]
公开(公告)号：US20110077294A1
公开(公告)日：2011-03-31
申请号：US12376909
申请日：2007-08-02
申请人： Ram Pratap , Himanshu Singh , Alok Kumar Verma , Amar Bahadur Singh , Priti Priti Tiwari Tiwari , Mukesh Srivastava , Arvind Kumar Srivastava , Anil Kumar Dwivedi , Satyawan Singh , Pratima Pnahma Svivastva Srivastava , Shio Kumar Singh , Chandishwar Nath , Ram Raghubir
发明人： Ram Pratap , Himanshu Singh , Alok Kumar Verma , Amar Bahadur Singh , Priti Priti Tiwari Tiwari , Mukesh Srivastava , Arvind Kumar Srivastava , Anil Kumar Dwivedi , Satyawan Singh , Pratima Pnahma Svivastva Srivastava , Shio Kumar Singh , Chandishwar Nath , Ram Raghubir
IPC分类号： A61K31/352 , C07D311/60 , A61P3/10 , A61P3/06
CPC分类号： C07D311/30
摘要： The present invention provides an optically active compound of general formula (I) and salts thereof: wherein R′ is selected from a group consisting of t-butyl amine, n-butylamine, iso-butylamine, iso-propyl amine, 4-phenyl-piperazine-1-ylamine, 4-(2-methoxyphenyl)-piperazin-1-ylamine, and 3,4-dimethoxy phenethyl amine; wherein R1, R2 and R3 are selected from the group consisting of hydrogen, methyl or iso pentenyl; R4, R5 and R6 are selected from the group consisting of Oil, O-alkyl, O-benzyl, O-substituted phenyl or combination thereof.
摘要翻译：本发明提供通式（I）的光学活性化合物及其盐：其中R'选自叔丁胺，正丁胺，异丁胺，异丙基胺，4-苯基 - 哌嗪-1-基胺，4-（2-甲氧基苯基） - 哌嗪-1-基胺和3,4-二甲氧基苯乙胺; 其中R1，R2和R3选自氢，甲基或异戊烯基; R4，R5和R6选自油，O-烷基，O-苄基，O-取代的苯基或其组合。

3. 发明授权

US07404962B1 Combination kit used in the treatment of malaria 失效
标题翻译：用于治疗疟疾的组合药盒
公开(公告)号：US07404962B1
公开(公告)日：2008-07-29
申请号：US10296215
申请日：2000-08-30
申请人： Francis Joseph Pinto , Swati Ajay Piramal , Ram Pratap , Amiya Prasad Bhaduri , Harsh Pati Thapliyal , Sunil Kumar Puri , Guru Prasad Dutta , Anil Kumar Dwivedi , Satyawan Singh , Pratima Srivastava , Vikash Chandra Pandey , Sudhir Srivastava , Shio Kumar Singh , Ram Chandra Gupta , Jagdishwar Sahai Srivastava , Omkar Prasad Asthana
发明人： Francis Joseph Pinto , Swati Ajay Piramal , Ram Pratap , Amiya Prasad Bhaduri , Harsh Pati Thapliyal , Sunil Kumar Puri , Guru Prasad Dutta , Anil Kumar Dwivedi , Satyawan Singh , Pratima Srivastava , Vikash Chandra Pandey , Sudhir Srivastava , Shio Kumar Singh , Ram Chandra Gupta , Jagdishwar Sahai Srivastava , Omkar Prasad Asthana
IPC分类号： A61K39/015 , C07D215/38
CPC分类号： A61K31/4706 , A61K31/47 , Y02A50/411 , A61K2300/00
摘要： A combination kit for the treatment of malaria caused by Plasmodium vivax (P. vivax) having individual doses of an anti-malarial agent, 3-[1-[[4-[(6-methoxy-8-quinolinyl)amino]pentyl]amino]ethylidene]-dihydro-2(3H)-furanone (I) in the form of capsules; individual doses of the anti-malarial agent, chloroquine in the form of tablets; and instruction material for the administration of the two anti-malarial drugs. The combination kit is particularly suited for a 6 days treatment regimen where the treatment is rendered by five tablets containing 500 mg of chloroquine phosphate (equivalent to 300 mg base), three to be taken on day one and one each on days two and three; and five capsules containing 25 mg of 3-[1-[[4-[(6-methoxy-8-quinolinyl)amino]pentyl]amino]ethylidene]-dihydro-2(3H)-furanone (I), one each to be taken on days two to six.
摘要翻译：用于治疗由间日疟原虫（间日疟原虫）引起的疟疾的组合试剂盒，其具有单个剂量的抗疟剂，3- [1 - [[4 - [（6-甲氧基-8-喹啉基）氨基]戊基] 氨基]亚乙基] - 二氢-2（3H） - 呋喃酮（I）单剂量的抗疟剂，片剂形式的氯喹; 以及两种抗疟药物的管理指导材料。组合试剂盒特别适用于6天的治疗方案，其中使用含有500mg磷酸氯喹（相当于300mg碱）的五片，第三天服用三次，第二天和第三次服用一次; 和5粒含有25mg 3- [1 - [[4 - [（6-甲氧基-8-喹啉基）氨基]戊基]氨基]亚乙基] - 二氢-2（3H） - 呋喃酮（I）的胶囊，在二至六天内服用。

4. 发明申请

US20120003273A1 SUBSTITUTED BENZFUROCHROMENES AND RELATED COMPOUNDS FOR THE PREVENTION AND TREATMENT OF BONE RELATED DISORDERS 有权
标题翻译：用于预防和治疗骨髓相关疾病的替代苯唑西林和相关化合物
公开(公告)号：US20120003273A1
公开(公告)日：2012-01-05
申请号：US13127913
申请日：2009-05-14
申请人： Atul Goel , Amit Kumar , Sumit Chaurasia , Divya Singh , Abnish Kumar Gautam , Rashmi Pandey , Ritu Trivedi , Man Mohan Singh , Naibedya Chattopadhyay , Lakshmi Manickavasagam , Girish Kumar Jain , Anil Kumar Dwivedi
发明人： Atul Goel , Amit Kumar , Sumit Chaurasia , Divya Singh , Abnish Kumar Gautam , Rashmi Pandey , Ritu Trivedi , Man Mohan Singh , Naibedya Chattopadhyay , Lakshmi Manickavasagam , Girish Kumar Jain , Anil Kumar Dwivedi
IPC分类号： A61K31/352 , C07D311/36 , A61P19/08 , A61K31/4453 , A61P19/10 , C07D493/04 , A61K9/00
CPC分类号： C07D493/04 , C07D311/36
摘要： The present invention relates to novel substituted benzfurochromenes and related compounds having the general formula (I), salts and chiral, achiral derivatives thereof; wherein R1, R2, R3, R4, R5, R6, R7, R8 are independently selected from the groups consisting of hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkylthio, optionally substituted amino, optionally substituted acylamino, optionally substituted arylamino, optionally substituted acylthio, optionally substituted acyl, optionally substituted aroyl, optionally substituted acyloxy, optionally substituted thioamido, halogens, nitriles, esters, hydroxy, mercapto, carbontrifluoride, nitro but not limited to this; wherein R1R2 or R2R3 or R6R7 may be connected and form either a five membered ring or a six membered ring such as optionally substituted furan, optionally substituted dihydrofuran, optionally substituted pyran; or may be connected through a methylenedeoxy moiety; wherein X is selected from the units consisting of optionally a ketone group, optionally a methylene group, optionally substituted methylene group, optionally substituted alkene; wherein Y and Z is selected from the units consisting of CH, C—OH, C-Me, C—OMe with the proviso that bond between Y and Z is a single bond; Wherein Y and Z may be a carbon atom with the proviso that bond between Y and Z is a double bond. The compounds of the general formula is useful for the prevention and treatment of bone related disorders.
摘要翻译：本发明涉及具有通式（I）的新型取代的苯并呋喃和其相关化合物，其盐和手性的非手性衍生物; 其中R1，R2，R3，R4，R5，R6，R7，R8独立地选自氢，任选取代的烷基，任选取代的烯基，任选取代的烷氧基，任选取代的芳基，任选取代的杂芳基，任选取代的烷硫基，任选取代的氨基，任选取代的酰基氨基，任选取代的芳基氨基，任选取代的酰基硫基，任选取代的酰基，任选取代的芳酰基，任选取代的酰氧基，任选取代的硫代酰氨基，卤素，腈，酯，羟基，巯基，三氟化碳，硝基，但不限于此 ; 其中R1R2或R2R3或R6R7可以连接并形成五元环或六元环，例如任选取代的呋喃，任选取代的二氢呋喃，任选取代的吡喃; 或可以通过亚甲二氧基部分连接; 其中X选自由任选的酮基，任选的亚甲基，任选取代的亚甲基，任选取代的烯烃组成的单元; 其中Y和Z选自由CH，C-OH，C-Me，C-OMe组成的单元，条件是Y和Z之间的键是单键; 其中Y和Z可以是碳原子，条件是Y和Z之间的键是双键。通式的化合物可用于预防和治疗骨相关疾病。

5. 发明申请

US20110305754A1 CONTROLLED RELEASE MICRO-CAPSULE FOR OSTEOGENIC ACTION 有权
标题翻译：控制释放微胶囊用于卵泡作用
公开(公告)号：US20110305754A1
公开(公告)日：2011-12-15
申请号：US13203603
申请日：2010-02-26
申请人： Prabhat Ranjan Mishra , Ritu Trivedi , Girish Kumar Gupta , Avinash Kumar , Varsha Gupta , Srikanta Kumar Rath , Kamini Srivastava , Naibedya Chattopadhyay , Anil Kumar Dwivedi
发明人： Prabhat Ranjan Mishra , Ritu Trivedi , Girish Kumar Gupta , Avinash Kumar , Varsha Gupta , Srikanta Kumar Rath , Kamini Srivastava , Naibedya Chattopadhyay , Anil Kumar Dwivedi
IPC分类号： A61K9/52 , A61K9/50 , A61P19/10 , A61P19/00 , A61K31/352 , A61K31/7048
CPC分类号： A61K9/1641 , A61K9/1611 , A61K9/1652 , A61K9/1658 , A61K9/5031 , A61K9/5052 , A61K9/5073
摘要： The present invention relates to a microcapsule for controlled release of flavanoid compound and a process for preparation thereof. The microcapsule comprising a core particle consisting of a calcium salt, Pluronic F68 [poly (ethylene oxide-co-polypropylene co-polypropylene oxide), block poly oxyethylene-polypropylene block copolymer], loaded with a flavanoid compound, the resulting core particle having a plurality of alternate layers of cationic and anionic polyelectrolytes adsorbed thereon and an outer layer formed by a bile salt, wherein the flavanoid is ranging between 10 to 96% by weight.
摘要翻译：本发明涉及一种用于控制释放类黄酮化合物的微胶囊及其制备方法。该微胶囊包含由钙盐，Pluronic F68 [聚（环氧乙烷 - 共聚 - 丙烯共聚 - 丙烯氧化物），嵌段聚氧乙烯 - 聚丙烯嵌段共聚物]组成的核心颗粒，负载有类黄酮化合物，所得核心颗粒具有吸附在其上的多个阳离子和阴离子聚电解质的交替层和由胆汁盐形成的外层，其中所述类黄酮的范围在10至96重量％之间。

6. 发明授权

US06740639B1 Inclusion complees of a high potent opioid peptide, pharmaceutical compositions and method of treatment 失效
标题翻译：包含的高效阿片样物质肽，药物组合物和治疗方法
公开(公告)号：US06740639B1
公开(公告)日：2004-05-25
申请号：US09537088
申请日：2000-03-29
申请人： Anil Kumar Dwivedi , Madhu Khanna , Wahajul Haq , Ram Raghubir , Sudhir Srivastava , Puvvada Sri Ramchandra Murthy , Onkar Prasad Asthana , Jagdishwar Sahay Srivastava , Satyawan Singh
发明人： Anil Kumar Dwivedi , Madhu Khanna , Wahajul Haq , Ram Raghubir , Sudhir Srivastava , Puvvada Sri Ramchandra Murthy , Onkar Prasad Asthana , Jagdishwar Sahay Srivastava , Satyawan Singh
IPC分类号： A61K3808
CPC分类号： B82Y5/00 , A61K9/2018 , A61K9/7023 , A61K38/08 , A61K47/6949
摘要： The invention provides novel inclusion complexes of highly potent opioid peptide of L-Tyrosyl-D-alanyl-glycyl-N-methylphenylalanyl-glycyl-isopropylamide with cyclodextrin, pharmaceutical preparations containing these inclusion complexes of L-Tyrosyl-D-alanyl-glycyl-N-methylphenylalanyl-glycyl-isopropylamide with cyclodextrin derivatives, the complexes being better soluble in water and having improved biopharmaceutical properties such as lesser toxicity, better analgesic action and non-addiction properties.
摘要翻译：本发明提供L-赖氨酸-D-丙氨酰 - 甘氨酰-N-甲基苯丙氨酰 - 甘氨酰 - 异丙基酰胺与环糊精的高效阿片样物质的新型包合物，其含有L-酪氨酰-D-丙氨酰 - 甘氨酰-N - 甲基苯丙氨酰 - 甘氨酰 - 异丙基酰胺与环糊精衍生物，该配合物更好地溶于水，并具有改善的生物药物性质，例如毒性较小，更好的镇痛作用和非成瘾性质。

7. 发明申请

US20130338193A1 CHIRAL 1-(4-METHYLPHENYLMETHYL)-5-OXO--PYRROLIDINE-2-CARBOXAMIDES AS INHIBITORS OF COLLAGEN INDUCED PLATELET ACTIVATION AND ADHESION 有权
标题翻译： CHIRAL 1-（4-甲基苯基甲基）-5-氧代 - 吡咯烷-2-羧酸酰胺作为胶原诱导的板激活和粘附的抑制剂
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。

8. 发明授权

US09206155B2 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 有权
标题翻译：手性1-（4-甲基苯基甲基）-5-氧代-N- {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
公开(公告)号：US09206155B2
公开(公告)日：2015-12-08
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 Bhatta , 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 Bhatta , 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 , C07B53/00
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-酮分别为式6和7的甲酰胺。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。

9. 发明授权

US08686028B2 Substituted benzfurochromenes and related compounds for the prevention and treatment of bone related disorders 有权
标题翻译：用于预防和治疗骨相关疾病的取代苯并呋喃并烯和相关化合物
公开(公告)号：US08686028B2
公开(公告)日：2014-04-01
申请号：US13127913
申请日：2009-05-14
申请人： Atul Goel , Amit Kumar , Sumit Chaurasia , Divya Singh , Abnish Kumar Gautam , Rashmi Pandey , Ritu Trivedi , Man Mohan Singh , Naibedya Chattopadhyay , Lakshmi Manickavasagam , Girish Kumar Jain , Anil Kumar Dwivedi
发明人： Atul Goel , Amit Kumar , Sumit Chaurasia , Divya Singh , Abnish Kumar Gautam , Rashmi Pandey , Ritu Trivedi , Man Mohan Singh , Naibedya Chattopadhyay , Lakshmi Manickavasagam , Girish Kumar Jain , Anil Kumar Dwivedi
IPC分类号： A61K31/352 , A61K31/4453 , C07D311/36 , C07D493/04
CPC分类号： C07D493/04 , C07D311/36
摘要： The present invention relates to novel substituted benzfurochromenes and related compounds having the general formula (I), salts and chiral, achiral derivatives thereof; wherein R1, R2, R3, R4, R5, R6, R7, R8 are independently selected from the groups consisting of hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkylthio, optionally substituted amino, optionally substituted acylamino, optionally substituted arylamino, optionally substituted acylthio, optionally substituted acyl, optionally substituted aroyl, optionally substituted acyloxy, optionally substituted thioamido, halogens, nitriles, esters, hydroxy, mercapto, carbontrifluoride, nitro but not limited to this; wherein R1R2 or R2R3 or R6R7 may be connected and form either a five membered ring or a six membered ring such as optionally substituted furan, optionally substituted dihydrofuran, optionally substituted pyran; or may be connected through a methylenedeoxy moiety; wherein X is selected from the units consisting of optionally a ketone group, optionally a methylene group, optionally substituted methylene group, optionally substituted alkene; wherein Y and Z is selected from the units consisting of CH, C—OH, C-Me, C—OMe with the proviso that bond between Y and Z is a single bond; Wherein Y and Z may be a carbon atom with the proviso that bond between Y and Z is a double bond. The compounds of the general formula is useful for the prevention and treatment of bone related disorders.
摘要翻译：本发明涉及具有通式（I）的新型取代的苯并呋喃和其相关化合物，其盐和手性的非手性衍生物; 其中R1，R2，R3，R4，R5，R6，R7，R8独立地选自氢，任选取代的烷基，任选取代的烯基，任选取代的烷氧基，任选取代的芳基，任选取代的杂芳基，任选取代的烷硫基，任选取代的氨基，任选取代的酰基氨基，任选取代的芳基氨基，任选取代的酰基硫基，任选取代的酰基，任选取代的芳酰基，任选取代的酰氧基，任选取代的硫代酰氨基，卤素，腈，酯，羟基，巯基，三氟化碳，硝基，但不限于此 ; 其中R1R2或R2R3或R6R7可以连接并形成五元环或六元环，例如任选取代的呋喃，任选取代的二氢呋喃，任选取代的吡喃; 或可以通过亚甲二氧基部分连接; 其中X选自由任选的酮基，任选的亚甲基，任选取代的亚甲基，任选取代的烯烃组成的单元; 其中Y和Z选自由CH，C-OH，C-Me，C-OMe组成的单元，条件是Y和Z之间的键是单键; 其中Y和Z可以是碳原子，条件是Y和Z之间的键是双键。通式的化合物可用于预防和治疗骨相关疾病。

10. 发明授权

US08496964B2 Controlled release micro-capsule for osteogenic action 有权
标题翻译：用于成骨作用的控释微胶囊
公开(公告)号：US08496964B2
公开(公告)日：2013-07-30
申请号：US13203603
申请日：2010-02-26
申请人： Prabhat Ranjan Mishra , Ritu Trivedi , Girish Kumar Gupta , Avinash Kumar , Varsha Gupta , Srikanta Kumar Rath , Kamini Srivastava , Naibedya Chattopadhyay , Anil Kumar Dwivedi
发明人： Prabhat Ranjan Mishra , Ritu Trivedi , Girish Kumar Gupta , Avinash Kumar , Varsha Gupta , Srikanta Kumar Rath , Kamini Srivastava , Naibedya Chattopadhyay , Anil Kumar Dwivedi
IPC分类号： A61K9/52 , A61K9/50 , A61K31/70 , B01J13/00 , B05D3/00 , A01N43/04
CPC分类号： A61K9/1641 , A61K9/1611 , A61K9/1652 , A61K9/1658 , A61K9/5031 , A61K9/5052 , A61K9/5073
摘要： The present invention relates to a microcapsule for controlled release of flavanoid compound and a process for preparation thereof. The microcapsule comprising a core particle consisting of a calcium salt, Pluronic F68 [poly (ethylene oxide-co-polypropylene oxide), block poly oxyethylene-polypropylene block copolymer], loaded with a flavanoid compound, the resulting core particle having a plurality of alternate layers of cationic and anionic polyelectrolytes adsorbed thereon and an outer layer formed by a bile salt, wherein the flavanoid is ranging between 10 to 96% by weight.
摘要翻译：本发明涉及一种用于控制释放类黄酮化合物的微胶囊及其制备方法。所述微胶囊包含由钙盐，Pluronic F68 [聚（环氧乙烷 - 共聚 - 丙烯氧化物），嵌段聚氧乙烯 - 聚丙烯嵌段共聚物]组成的核心颗粒，负载有类黄酮化合物，所得核心颗粒具有多个交替吸附在其上的阳离子和阴离子聚电解质层以及由胆汁盐形成的外层，其中类黄酮的范围在10至96重量％之间。

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