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1. 发明申请

WO2011045807A3 A NOVEL PROCESS TO MANUFACTURE (2R,3S)-2-(2,4-DIFLUOROPHENYL)-3-(5-FLUOROPYRIMIDIN-4-YL)-1-(1H-1,2,4-TRIAZOL-1-YL)BUTAN-2-OL 审中-公开
公开(公告)号：WO2011045807A3
公开(公告)日：2011-04-21
申请号：PCT/IN2009/000752
申请日：2009-12-30
申请人： NEULAND LABORATORIES LTD. , RAMAKRISHNAN, Arul , KAPKOTI, Gobind, Singh , DEHURY, Sanjay, Kumar
发明人： RAMAKRISHNAN, Arul , KAPKOTI, Gobind, Singh , DEHURY, Sanjay, Kumar
IPC分类号： C07D403/06
摘要： The present invention relates to a novel industrially viable, cost effective process to manufacture substantially pure form of (2R,3S)-2-(2,4-difluorophenyl)-3-(5- fluoropyrimidin-4-yl)-l-(lH-l,2,4-triazol-l-yl)butan-2-ol (Voriconazole) with a chiral purity level of greater than 99.9 % and impurity level of less than 0.1 %.

2. 发明申请

WO2010106550A2 A PROCESS FOR THE PREPARATION OF N-[[TRANS-4-(1-METHYLETHYL)CYCLOHEXYL]CARBONYL]-D-PHENYLALANINE 审中-公开
标题翻译：制备N - [[反式-4-（1-甲基乙基）环丙基]羰基] -D-苯基亚胺的方法
公开(公告)号：WO2010106550A2
公开(公告)日：2010-09-23
申请号：PCT/IN2010/000131
申请日：2010-03-09
申请人： NEULAND LABORATORIES LTD. , RAMKRISHNANA, Arul , KAPKOTI, Gobind Singh , DEHURY, Sanjay Kumar
发明人： RAMKRISHNANA, Arul , KAPKOTI, Gobind Singh , DEHURY, Sanjay Kumar
IPC分类号： C07C51/08
CPC分类号： C07C303/26 , C07B2200/07 , C07C233/63 , C07C303/00 , C07C309/00 , C07C2601/14
摘要： The present invention is directed to an novel, industrially viable and cost effective process for preparation of substantially pure N-[[trans-4-(l-methylethyl) cyclohexyl] carbonyl]-D- phenylalanine commonly known as Nateglinide.
摘要翻译：本发明涉及用于制备通常称为那格列奈的基本上纯的N - [[反式-4-（1-甲基乙基）环己基]羰基] -D-苯丙氨酸的新型工业上可行且具有成本效益的方法。

3. 发明申请

WO2007060518A3 KETOLIDE DERIVATIVES AS ANTIBACTERIAL AGENTS 审中-公开
公开(公告)号：WO2007060518A3
公开(公告)日：2007-05-31
申请号：PCT/IB2006/003298
申请日：2006-11-21
申请人： RANBAXY LABORATORIES LIMITED , DAS, Biswajit , CHAKRABARTI, Anjan , KUMAR, Rajesh , VENKATARAMANAN, Ramadass , HAJARE, Atul Kashinath , BANDYOPADHYAY, Anish , KATOCH, Rita , KAPKOTI, Gobind Singh , SURASE, Yogesh Baban , SALMAN, Mohammad , UPADHYAY, Dilip J.
发明人： DAS, Biswajit , CHAKRABARTI, Anjan , KUMAR, Rajesh , VENKATARAMANAN, Ramadass , HAJARE, Atul Kashinath , BANDYOPADHYAY, Anish , KATOCH, Rita , KAPKOTI, Gobind Singh , SURASE, Yogesh Baban , SALMAN, Mohammad , UPADHYAY, Dilip J.
IPC分类号： C07H17/08 , A61K31/7052 , A61P31/04
摘要： Provided herein are ketolide derivatives, which can be used as antibacterial agents. Compounds described herein can be used for treating or preventing conditions caused by or contributed to by gram positive, gram negative or anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Moraxalla spp., Chlamydia spp., Mycoplasm, Legionella spp., Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Bacillus, Enterobactericeae, Propionibacterium acnes or any combination thereof. Also provided are processes for preparation of compounds described herein, pharmaceutical compositions thereof, and methods of treating bacterial infections.

4. 发明申请

WO2006046112A2 KETOLIDE DERIVATIVES AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译： KETOLIDE衍生物作为抗菌剂
公开(公告)号：WO2006046112A2
公开(公告)日：2006-05-04
申请号：PCT/IB2005/003181
申请日：2005-10-25
申请人： RANBAXY LABORATORIES LIMITED , DAS, Biswajit , SALMAN, Mohammad , KURHADE, Santosh, Haribhau , VENKATARAMANAN, Ramadass , KUMAR, Rajesh , KAPKOTI, Gobind, Singh , KATOCH, Rita , BANDYOPADHYAY, Anish , RATTAN, Ashok
发明人： DAS, Biswajit , SALMAN, Mohammad , KURHADE, Santosh, Haribhau , VENKATARAMANAN, Ramadass , KUMAR, Rajesh , KAPKOTI, Gobind, Singh , KATOCH, Rita , BANDYOPADHYAY, Anish , RATTAN, Ashok
CPC分类号： C07H17/00
摘要： The present invention provides ketolide derivatives, which can be used as anti-bacterial agents. Compounds disclosed herein can be used for the treating or preventing conditions caused by or contributed to by gram positive, gram negative or anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Moraxalla spp., Chlamydia spp., Mycoplasm, Legionella spp., Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Bacillus, Enterobactericeae or any combination thereof. Also provided are processes for preparing compounds disclosed herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods of treating bacterial infections.
摘要翻译：本发明提供了可用作抗菌剂的酮内酯衍生物。本文公开的化合物可用于治疗或预防由革兰氏阳性，革兰氏阴性或厌氧菌引起的或由其引起的疾病，更特别是针对例如葡萄球菌，链球菌，肠球菌，嗜血杆菌，莫拉沙拉菌，衣原体属，支原体，军团菌属，分枝杆菌属，螺杆菌属，梭菌属，拟杆菌属，棒状杆菌属，芽孢杆菌属，肠杆菌属或其任何组合。还提供了用于制备本文公开的化合物的方法，其合成中使用的中间体，其药物组合物以及治疗细菌感染的方法。

5. 发明申请

WO2005118537A2 ADRENERGIC RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2005118537A2
公开(公告)日：2005-12-15
申请号：PCT/IB2005/001534
申请日：2005-05-31
申请人： RANBAXY LABORATORIES LIMITED , SALMAN, Mohammad , SHARMA, Somesh , YADAV, Gyan, Chand , KAPKOTI, Gobind Singh , MISHRA, Anurag , GUPTA, Praful , ANAND, Nitya , CHUGH, Anita , NANDA, Kamna
发明人： SALMAN, Mohammad , SHARMA, Somesh , YADAV, Gyan, Chand , KAPKOTI, Gobind Singh , MISHRA, Anurag , GUPTA, Praful , ANAND, Nitya , CHUGH, Anita , NANDA, Kamna
IPC分类号： C07D209/00
CPC分类号： C07D207/404 , C07D207/416 , C07D207/452 , C07D209/48 , C07D209/94 , C07D211/88 , C07D409/12 , C07D513/04
摘要： The present invention relates to α 1a and/or α 1d adrenergic receptor antagonists, which can function as α 1a and/or α 1d adrenergic receptor antagonist and can be used for the treatment of a disease or disorder mediated through α 1a and/or α 1d adrenergic receptor. Compounds disclosed herein can be used for the treatment of benign prostatic hyperplasia (BPH) and the related symptoms thereof. Further, compounds disclosed herein can be used for the treatment of lower urinary tract symptoms associated with or without BPH. Also provided are processes for preparing such compounds, pharmaceutical compositions thereof, and the methods of treating BPH or related symptoms thereof.
摘要翻译：本发明涉及α1a和/或α1肾上腺素能受体拮抗剂，其可用作α1a和/或α1肾上腺素能受体拮抗剂，并可用于治疗通过α1a和/或α1d肾上腺素能受体介导的疾病或病症。本文公开的化合物可用于治疗良性前列腺增生（BPH）及其相关症状。此外，本文公开的化合物可用于治疗与或不与BPH相关的下尿路症状。还提供了制备这种化合物的方法，其药物组合物，以及治疗BPH或其相关症状的方法。

6. 发明申请

WO2006051374A2 ADRENERGIC RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2006051374A2
公开(公告)日：2006-05-18
申请号：PCT/IB2005/003295
申请日：2005-11-04
申请人： RANBAXY LABORATORIES LIMITED , SALMAN, Mohammad , ANAND, Nitya , YADAV, Gyan, Chand , SHARMA, Somesh , KAPKOTI, Gobind, Singh , CHUGH, Anita , NANDA, Kamna
发明人： SALMAN, Mohammad , ANAND, Nitya , YADAV, Gyan, Chand , SHARMA, Somesh , KAPKOTI, Gobind, Singh , CHUGH, Anita , NANDA, Kamna
IPC分类号： A61K31/4355 , C07D491/04 , C07D401/12 , C07D209/76
CPC分类号： C07D209/48 , C07D209/76 , C07D491/04
摘要： The present invention relates to α 1a and/or α 1d adrenergic receptor antagonists, which can be used to treat a disease or disorder mediated through α 1a and/or α 1d adrenergic receptors. Compounds and pharmaceutical compositions disclosed herein can be used to treat benign prostatic hyperplasia (BPH) and related symptoms thereof. Further, such compounds can be used to treat lower urinary tract symptoms that may or may not be associated with BPH. The present invention also relates to processes to prepare the disclosed compounds, pharmaceutical compositions thereof, and methods of treating BPH or related symptoms thereof.
摘要翻译：本发明涉及可用于治疗通过1a介导的疾病或病症的<！ - SIPO - >1α1α和/或1β1肾上腺素能受体拮抗剂。 >和/或<1d>肾上腺素能受体。本文公开的化合物和药物组合物可用于治疗良性前列腺增生（BPH）及其相关症状。此外，这些化合物可用于治疗可能与也可能不伴有BPH的下尿路症状。本发明还涉及制备所公开的化合物的方法，其药物组合物，以及治疗BPH或其相关症状的方法。

7. 发明申请

WO2005113498A1 ADRENERGIC RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2005113498A1
公开(公告)日：2005-12-01
申请号：PCT/IB2004/001641
申请日：2004-05-19
申请人： RANBAXY LABORATORIES LIMITED , SALMAN, Mohammad , SHARMA, Somesh , KAPKOTI, Gobind, Singh , ANAND, Nitya , CHUGH, Anita
发明人： SALMAN, Mohammad , SHARMA, Somesh , KAPKOTI, Gobind, Singh , ANAND, Nitya , CHUGH, Anita
IPC分类号： C07D207/40
CPC分类号： C07D207/408 , C07D207/448 , C07D209/48
摘要： This invention relates to α 1a and/or α 1d adrenergic receptor antagonists. Compounds disclosed herein can function as α 1a and/or α 1d adrenergic receptor antagonist and can be used for the treatment of diseases or disorder mediated through α 1a and/or α 1d adrenergic receptors. Compounds disclosed herein can be used for the treatment of benign prostatic hyperplasia and the related symptoms thereof. Compounds disclosed herein can be used for the treatment of lower urinary tract symptoms associated with or without benign prostatic hyperplasia. Processes for the preparation of compounds disclosed herein, pharmaceutical compositions containing the compounds disclosed herein, and methods of treating benign prostatic hyperplasia or related symptoms thereof are also provided. Formula (I) Its pharmaceutically acceptable acid addition salts,pharmaceutically acceptable solvates, enantiomers, diastereomers, N-oxides, polymorphs or metabolites,wherein; A represents a Formula (F.a or ,F.b or F.c wherein) N represents 1 or 2; Y represents cycloalkyl (C 5- C 7 ) group; optionally substituted with halogen atom(s) or lower alkyl (C 1- C 4 ) group; and R is selected from optionally substituted non_aromatic or aromatic monocyclic or bicyclic ring system having 0 to 4 heteroatom(s),the substituent(s) may be selected from the group consisting of halogen, lower alkyl (C 1- C 4 ),halogenated lower alkyl (C 1- c 4 ),cyano, hydroxy, lower alkoxy (C 1- C 4 ),cycloalkoxy (C 3- C 6 ),amino,lower alkylamino (C 1- C 4 ) and lower alkylamino (C 1- C 4 ) carbonyl group.
摘要翻译：本发明涉及α1a和/或α1d肾上腺素能受体拮抗剂。本文公开的化合物可用作α1a和/或α1肾上腺素能受体拮抗剂，并且可用于治疗通过α1a和/或α1肾上腺素能受体介导的疾病或病症。本文公开的化合物可用于治疗良性前列腺增生及其相关症状。本文公开的化合物可用于治疗与或不伴有良性前列腺增生相关的下尿路症状。还提供了制备本文公开的化合物的方法，含有本文公开的化合物的药物组合物，以及治疗良性前列腺增生或其相关症状的方法。式（I）其药学上可接受的酸加成盐，药学上可接受的溶剂合物，对映异构体，非对映异构体，N-氧化物，多晶型物或代谢物，其中; A表示式（F.a或F.b或F.c，其中N表示1或2; Y代表环烷基（C5-C7）基团; 任选被卤素原子或低级烷基（C 1 -C 4）基团取代; 并且R选自具有0至4个杂原子的任选取代的非芳族或芳族单环或双环体系，所述取代基可以选自卤素，低级烷基（C 1 -C 4），卤代低级烷基（C1-C4），氰基，羟基，低级烷氧基（C1-C4），环烷氧基（C3-C6），氨基，低级烷基氨基（C1-C4）和低级烷基氨基（C1-C4）羰基。

8. 发明申请

WO2005037282A1 1-ALKYLPIPERAZINYL-PYRROLIDIN-2,5-DIONE DERIVATIVES AS ADRENERGIC RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为ADRENERGIC受体拮抗剂的1-烷基哌嗪 - 吡咯烷-2,5-二酮衍生物
公开(公告)号：WO2005037282A1
公开(公告)日：2005-04-28
申请号：PCT/IB2004/003362
申请日：2004-10-14
申请人： RANBAXY LABORATORIES LIMITED , ANAND, Nitya , SALMAN, Mohammad , SHARMA, Somesh , KAPKOTI, Gobind, Singh , GUPTA, Praful , MISHRA, Anurag , CHUGH, Anita , TIWARI, Atul
发明人： ANAND, Nitya , SALMAN, Mohammad , SHARMA, Somesh , KAPKOTI, Gobind, Singh , GUPTA, Praful , MISHRA, Anurag , CHUGH, Anita , TIWARI, Atul
IPC分类号： A61K31/496
CPC分类号： C07D207/40 , C07D207/408 , C07D207/416 , C07D209/48
摘要： This invention relates to α 1a and/or α 1d adrenergic receptor antagonists of formula 1 Compounds disclosed herein can function as α 1a and/or α 1d adrenergic receptor antagonists and can be used for the treatment of diseases or disorders mediated through α 1a and/or α 1d adrenergic receptors. Compounds disclosed herein can be used for the treatment of benign prostatic hyperplasia and related symptoms thereof. Compounds disclosed herein can also be used for the treatment of lower urinary tract symptoms associated with or without benign prostatic hyperplasia. The invention also relates to a process for the preparation of compounds disclosed herein, pharmaceutical compositions containing these compounds and the methods of treating diseases or disorders mediated through α 1a and/or α 1d receptors.
摘要翻译：本发明涉及式1的α1a和/或α1d肾上腺素能受体拮抗剂。本文公开的化合物可用作α1a和/或α1肾上腺素能受体拮抗剂，并且可用于治疗通过α1a和/或α1d肾上腺素能受体介导的疾病或病症。本文公开的化合物可用于治疗良性前列腺增生及其相关症状。本文公开的化合物也可用于治疗与或不伴有良性前列腺增生相关的下尿路症状。本发明还涉及制备本文公开的化合物的方法，含有这些化合物的药物组合物和治疗通过α1a和/或α1受体介导的疾病或病症的方法。

9. 发明申请

WO2010106550A3 A PROCESS FOR THE PREPARATION OF N-[[TRANS-4-(1-METHYLETHYL)CYCLOHEXYL]CARBONYL]-D-PHENYLALANINE 审中-公开
标题翻译：制备N - [[反式-4-（1-甲基乙基）环丙基]羰基] -D-苯基亚胺的方法
公开(公告)号：WO2010106550A3
公开(公告)日：2012-09-27
申请号：PCT/IN2010000131
申请日：2010-03-09
申请人： NEULAND LAB LTD , RAMKRISHNANA ARUL , KAPKOTI GOBIND SINGH , DEHURY SANJAY KUMAR
发明人： RAMKRISHNANA ARUL , KAPKOTI GOBIND SINGH , DEHURY SANJAY KUMAR
IPC分类号： C07C233/63 , C07C231/14 , C07C309/74
CPC分类号： C07C303/26 , C07B2200/07 , C07C233/63 , C07C303/00 , C07C309/00 , C07C2601/14
摘要： The present invention is directed to an novel, industrially viable and cost effective process for preparation of substantially pure N-[[trans-4-(l-methylethyl) cyclohexyl] carbonyl]-D- phenylalanine commonly known as Nateglinide.
摘要翻译：本发明涉及用于制备通常称为那格列奈的基本上纯的N - [[反式-4-（1-甲基乙基）环己基]羰基] -D-苯丙氨酸的新型工业上可行且具有成本效益的方法。

10. 发明申请

WO2011045807A2 A NOVEL PROCESS TO MANUFACTURE (2R,3S)-2-(2,4-DIFLUOROPHENYL)-3-(5-FLUOROPYRIMIDIN-4-YL)-1-(1H-1,2,4-TRIAZOL-1-YL)BUTAN-2-OL 审中-公开
标题翻译：制备（2R，3S）-2-（2,4-二氟苯基）-3-（5-氟吡啶-4-基）-1-（1H-1,2,4-三唑-1-基） 2-丁酮OL
公开(公告)号：WO2011045807A2
公开(公告)日：2011-04-21
申请号：PCT/IN2009000752
申请日：2009-12-30
申请人： NEULAND LAB LTD , RAMAKRISHNAN ARUL , KAPKOTI GOBIND SINGH , DEHURY SANJAY KUMAR
发明人： RAMAKRISHNAN ARUL , KAPKOTI GOBIND SINGH , DEHURY SANJAY KUMAR
IPC分类号： C07D403/06
CPC分类号： C07D403/06
摘要： The present invention relates to a novel industrially viable, cost effective process to manufacture substantially pure form of (2R,3S)-2-(2,4-difluorophenyl)-3-(5- fluoropyrimidin-4-yl)-l-(lH-l,2,4-triazol-l-yl)butan-2-ol (Voriconazole) with a chiral purity level of greater than 99.9 % and impurity level of less than 0.1 %.
摘要翻译：本发明涉及一种新型工业上可行的，具有成本效益的制备基本上纯的形式的（2R，3S）-2-（2,4-二氟苯基）-3-（5-氟嘧啶-4-基）-1-（ 1H-1,2,4-三唑-1-基）丁-2-醇（伏立康唑），手性纯度水平大于99.9％，杂质含量低于0.1％。

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