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21. 发明授权

US07002018B2 Process for the preparation of amorphous form of torsemide 失效
标题翻译：制备无定形形式的托塞米的方法
公开(公告)号：US07002018B2
公开(公告)日：2006-02-21
申请号：US10485590
申请日：2002-08-02
申请人： Yatendra Kumar , Om Dutt Tyagi , Nitin Maheshwari
发明人： Yatendra Kumar , Om Dutt Tyagi , Nitin Maheshwari
IPC分类号： C07D211/72
CPC分类号： C07D213/74
摘要： The present invention relates to a simple and efficient process for the preparation of amorphous form of torsemide. The process includes recovering amorphous torsemide from a solution thereof in a suitable solvent comprising alcohols, ketones, chlorinated hydrocarbons, esters, nitriles, cyclic ethers, and mixtures thereof, by spray drying.
摘要翻译：本发明涉及制备无定形形式的托塞米姆的简单有效的方法。该方法包括通过喷雾干燥从包含醇，酮，氯代烃，酯，腈，环醚及其混合物的合适溶剂中的溶液中回收无定形托塞米。

22. 发明授权

US06384213B1 Process for preparing a pure, pharmacopoeial grade amorphous form of cefuroxime axetil 失效
标题翻译：制备纯的，药典级无定形形式的头孢呋辛酯的方法
公开(公告)号：US06384213B1
公开(公告)日：2002-05-07
申请号：US09574311
申请日：2000-05-19
申请人： Vijay Kumar Handa , Om Dutt Tyagi , Uttam Kumar Ray
发明人： Vijay Kumar Handa , Om Dutt Tyagi , Uttam Kumar Ray
IPC分类号： C07D50134
CPC分类号： C07D501/00
摘要： There is described a process for the preparation of a pure amorphous form of cefuroxime axetil which involves dissolving crystalline cefuroxime axetil in acetic acid including at least 5% v/v water and recovering said amorphous form of cefuroxime axetil from the solution by the addition of additional water, the solution being added all at once to the additional water being present in a volume which is sufficient to precipitate said amorphous cefuroxime axetil.
摘要翻译：描述了一种制备纯无定形形式的头孢呋辛酯的方法，该方法包括将结晶头孢呋辛酯溶解在包含至少5％v / v水的乙酸中，并通过加入额外的溶液从溶液中回收所述无定形形式的头孢呋辛酯水，溶液一次全部添加到足以沉淀所述无定形头孢呋辛酯的体积中的另外的水。

23. 发明授权

US6060599A Process for the preparation of cefuroxime axetil in an amorphous form 失效
标题翻译：以无定形形式制备头孢呋辛酯的方法
公开(公告)号：US6060599A
公开(公告)日：2000-05-09
申请号：US98513
申请日：1998-06-17
申请人： Jitendra Krishan Somani , Sanjeev Sethi , Om Dutt Tyagi
发明人： Jitendra Krishan Somani , Sanjeev Sethi , Om Dutt Tyagi
IPC分类号： C07D501/00 , C07D501/02 , C07D501/12
CPC分类号： C07D501/00
摘要： A process for preparing cefuroxime axetil in substantially amorphous form comprises forming a mixture of crystalline cefuroxime axetil and at least one pharmaceutically acceptable excipient, and subjecting the mixture to milling for a period of time sufficient to convert the crystalline cefuroxime axetil to substantially amorphous form, i.e., the crystallinity is less than 5%. The amorphous cefuroxime axetil has a chemical purity of at least 95%. Desirably, the particles of the milled material are reduced to a size of less than 2 .mu.m. The amorphous cefuroxime axetil prepared by this method may consist of R isomer, S isomer, or a racemic mixture of the R and S isomers.
摘要翻译：制备基本无定形形式的头孢呋辛酯的方法包括形成结晶头孢呋辛酯和至少一种药学上可接受的赋形剂的混合物，并使混合物磨碎一段时间以足以将结晶头孢呋辛酯转变为基本上无定形的形式，即，结晶度小于5％。无定形头孢呋辛酯的化学纯度至少为95％。理想地，研磨材料的颗粒被还原成小于2μm的尺寸。通过该方法制备的无定形头孢呋辛酯可以由R异构体，S异构体或R和S异构体的外消旋混合物组成。

24. 发明授权

US08318930B2 Process for preparing polymorphic forms of (S)-6-chloro-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one 有权
标题翻译：（S）-6-氯 - （环丙基乙炔基）-1,4-二氢-4-（三氟甲基）-2H-3,1-苯并恶嗪-2-酮的多晶形式的制备方法
公开(公告)号：US08318930B2
公开(公告)日：2012-11-27
申请号：US12810288
申请日：2008-12-24
申请人： Om Dutt Tyagi , Ramakoteswara Rao Jetti , B. A. Ramireddy
发明人： Om Dutt Tyagi , Ramakoteswara Rao Jetti , B. A. Ramireddy
IPC分类号： C07D265/18
CPC分类号： C07D265/18
摘要： Disclosed herein is a novel process for preparing polymorphic Forms of (S)-6-chloro-(cyclopropylethynyl)-1,4-di-hydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one referred as M1, I, II, β, and ω.
摘要翻译：本文公开了一种制备（S）-6-氯 - （环丙基乙炔基）-1,4-二氢-4-（三氟甲基）-2H-3,1-苯并恶嗪-2-酮的多晶形式的新方法，称为 M1，I，II，＆bgr，和ω。

25. 发明授权

US08247568B2 Process for the preparation of pure rabeprazole 有权
标题翻译：制备纯雷贝拉唑的方法
公开(公告)号：US08247568B2
公开(公告)日：2012-08-21
申请号：US12665851
申请日：2008-06-19
申请人： Om Dutt Tyagi , Purna Chandra Ray , Madhuresh Kumar Sethi , Bhausaheb Chavhan
发明人： Om Dutt Tyagi , Purna Chandra Ray , Madhuresh Kumar Sethi , Bhausaheb Chavhan
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： The present invention relates to a process for the preparation of pure Rabeprazole sulfoxide using the solvent mixture for the extraction steps and this invention further relates to the process for the preparation of amorphous Rabeprazole sodium using pure rabeprazole base in presence of aqueous NaOH and water miscible solvent and adding an anti-solvent.
摘要翻译：本发明涉及一种使用溶剂混合物制备纯拉贝拉唑亚砜的方法，本发明还涉及在NaOH水溶液和水混溶性溶剂存在下，使用纯雷贝拉唑碱制备无定形雷贝拉唑钠的方法并加入抗溶剂。

26. 发明申请

US20100274007A1 PROCESS FOR PREPARING POLYMORPHIC FORMS OF (S)-6-CHLORO-(CYCLOPROPYLETHYNYL)-1,4-DIHYDRO-4-(TRIFLUOROMETHYL)-2H-3,1-BENZOXAZIN-2-ONE 有权
标题翻译：制备（S）-6-氯 - （环丙基乙基）-1,4-二氢-4-（三氟甲基）-2H-3,1-苯并恶嗪-2-酮的多晶型的方法
公开(公告)号：US20100274007A1
公开(公告)日：2010-10-28
申请号：US12810288
申请日：2008-12-24
申请人： Om Dutt Tyagi , Ram K. R. Jetti , B. A. Ramireddy
发明人： Om Dutt Tyagi , Ram K. R. Jetti , B. A. Ramireddy
IPC分类号： C07D265/18
CPC分类号： C07D265/18
摘要： Disclosed herein is a novel process for preparing polymorphic Forms of (S)-6-chloro-(cyclopropylethynyl)-1,4-di-hydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one referred as M1, I, II, β, and ω.
摘要翻译：本文公开了一种制备（S）-6-氯 - （环丙基乙炔基）-1,4-二氢-4-（三氟甲基）-2H-3,1-苯并恶嗪-2-酮的多晶形式的新方法，称为 M1，I，II，＆bgr，和ω。

27. 发明申请

US20100191015A1 PROCESS FOR THE PREPARATION OF O-DESMETHYLVENLAFAXINE SUCCINATE POLYMORPHIC FORMS 有权
标题翻译：制备邻苯二酚脂肪酸多糖形式的方法
公开(公告)号：US20100191015A1
公开(公告)日：2010-07-29
申请号：US12669487
申请日：2008-07-15
申请人： Ramakoteswara Rao Jetti , Purandhar Koilkonda , Jagan Mohana Chary Tummanapally , Mohana Vamsi, Krishna Vadlamudi , Prasanth Kumar Barik , Om Dutt Tyagi
发明人： Ramakoteswara Rao Jetti , Purandhar Koilkonda , Jagan Mohana Chary Tummanapally , Mohana Vamsi, Krishna Vadlamudi , Prasanth Kumar Barik , Om Dutt Tyagi
IPC分类号： C07C215/42
CPC分类号： C07C213/10 , C07B2200/13 , C07C2601/14 , C07C215/64
摘要： The present invention relates to process for the preparation of novel crystalline Desmethylvenlafaxine succinate polymorphic Forms-A, B. The present invention also relates to novel processes for the preparation of 0-Desmethylvenlafaxine succinate polymorphic Forms-(I), (II), (III) and amorphous.
摘要翻译：本发明涉及制备新的结晶Desmetvenlafaxine琥珀酸多晶型A，B的方法。本发明还涉及制备O-去甲基文拉法辛琥珀酸多晶型的新方法 - （I），（II），（III ）和无定形。

28. 发明申请

US20100056785A1 Preparation Of Zopiclone And Its Enantiomerically Enriched Isomer 有权
标题翻译：佐匹克隆及其对映体富集异构体的制备
公开(公告)号：US20100056785A1
公开(公告)日：2010-03-04
申请号：US12595663
申请日：2008-04-10
申请人： Om Dutt Tyagi , Tushar Kumar Srivastava , Vellanki Siva Ram Prasad , Dnyandev Ragho Rane , Bandi Naga Durga Rao , Daggula Srinivas Reddy
发明人： Om Dutt Tyagi , Tushar Kumar Srivastava , Vellanki Siva Ram Prasad , Dnyandev Ragho Rane , Bandi Naga Durga Rao , Daggula Srinivas Reddy
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Present invention relates to an improved process for the preparation of Zopiclone and its enantiomerically enriched isomer (Eszopiclone). 6-(5-Chloropyridin-2-yl)-5-hydroxy-7-oxo-5,6-dihydropyrrolo[3,4-b]pyrazine is reacted with 1-chloro-carbonyl-4-methylpiperazine in the presence of alkali earth metal carbonates, hydroxides or oxides in a solvent medium to give Zopiclone. It is reacted with optically active acid in a mixture of water and water miscible organic solvent followed by work up to give Eszopiclone. The present invention also relates to process for the conversion of (R) or (S) Zopiclone to 6-(5-chloropyrid-2-yl)-5-hydroxy-7-oxo-5,6-dihydro-pyrrolo-[3,4-b]-pyrazine of the intermediate which can be converted to racemic Zopiclone.
摘要翻译：本发明涉及一种改良的佐匹克隆及其对映体富集异构体（依佐替普）的制备方法。 6-（5-氯吡啶-2-基）-5-羟基-7-氧代-5,6-二氢吡咯并[3,4-b]吡嗪在碱存在下与1-氯 - 羰基-4-甲基哌嗪反应土壤金属碳酸盐，氢氧化物或氧化物在溶剂介质中给予佐匹克隆。将其与光学活性酸在水和水混溶性有机溶剂的混合物中反应，随后加工得到依佐替普。本发明还涉及将（R）或（S）佐匹克隆转化为6-（5-氯吡啶-2-基）-5-羟基-7-氧代-5,6-二氢 - 吡咯并[3 ，4-b] - 吡嗪，其可以转化为外消旋佐匹克隆。

29. 发明申请

US20090118509A1 PREPARATION OF [2-METHYL-5-PHENYL-3-(PIPERAZIN-1-YLMETHYL)] PYRROLE DERIVATIVES 审中-公开
公开(公告)号：US20090118509A1
公开(公告)日：2009-05-07
申请号：US11911272
申请日：2006-04-05
申请人： Sudershan Kumar Arora , Neelima Sinha , Sanjay Jain , Ram Shankar Upadhayaya , Om Dutt Tyagi , Vasanth Nalam , Yogendra Kumar Chauhan
发明人： Sudershan Kumar Arora , Neelima Sinha , Sanjay Jain , Ram Shankar Upadhayaya , Om Dutt Tyagi , Vasanth Nalam , Yogendra Kumar Chauhan
IPC分类号： C07D401/14
CPC分类号： C07D207/50 , C07D207/335 , C07D401/04 , C07D401/12
摘要： A process for the preparation of compounds of Formula I and their pharmaceutically acceptable acid addition salt wherein, R1 is phenyl or substituted phenyl R2 is selected from a group consisting of phenyl which is unsubstituted or substituted with 1 or 2 substituents, each independently selected from Cl, F, or pyridine, or naphthalene, or NHCOR4 wherein R4 is aryl, unsubstituted or substituted heteroaryl, unsubstituted or substituted heterocyclyl. R3 is selected from a group of formula wherein R5 is phenyl which is unsubstituted or substituted with 1 or 2 substituents each independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, nitro, amino, haloalkyl, haloalkoxy etc.; unsubstituted or substituted benzyl; unsubstituted or substituted heteroaryl; unsubstituted or substituted heteroaroyl; unsubstituted or substituted diphenylmethyl, n=0-2 and X═—NCH3, CH2, S, SO, or SO2 Such that when R2 is phenyl, which is unsubstituted or substituted with 1 or 2 substituents, each independently selected from Cl, F; R5 is not C1-C4 alkyl, or X is not —NCH3, CH2, S, SO, or SO2, when n=1, or X is not —CH2 when n=0; comprising the steps of (a) reacting compound of Formula II with a chlorinating agent in the presence or absence of catalytic amount of N,N-dimethylformamide to yield the compound of Formula III, (b) reacting the compound of Formula III with a compound of Formula R1H (R1 is as defined above), in presence of a Lewis acid to obtain the compound of Formula IV, (c) reacting the compound of Formula IV with a compound of Formula R2NH2 (R2 is as defined above) in presence of catalytic amounts of an aryl or alkyl sulphonic acid in an organic solvent to obtain the compound of Formula V, (d) reacting the compound of Formula V with various secondary amines of the Formula R3H (R3 is as defined above) in the presence of formaldehyde and acetic acid in acetonitrile followed by crystallization yield the compound of Formula I, (e) purifying the compound of Formula I by crystallization, (f) converting the purified compound of Formula I to a pharmaceutically acceptable acid addition salt.

30. 发明授权

US06534494B1 Process for the preparation of cefuroxime axetil in an amorphous form 失效
标题翻译：以无定形形式制备头孢呋辛酯的方法
公开(公告)号：US06534494B1
公开(公告)日：2003-03-18
申请号：US09673929
申请日：2000-12-18
申请人： Jitendra Krishan Somani , Sanjeev Sethi , Om Dutt Tyagi
发明人： Jitendra Krishan Somani , Sanjeev Sethi , Om Dutt Tyagi
IPC分类号： C07D50102
CPC分类号： C07D501/00
摘要： A process for preparing cefuroxime axetil in substantially amorphous form comprises forming a mixture of crystalline cefuroxime axetil and at least one pharmaceutically acceptable excipient, and subjecting the mixture to milling for a period of time sufficient to convert the crystalline cefuroxime axetil to substantially amorphous form, i.e., the crystallinity is less than 5%. The amorphous cefuroxime axetil has a chemical purity of at least 95%. Desirably, the particles of the milled material are reduced to a size of less than 2.
摘要翻译：制备基本无定形形式的头孢呋辛酯的方法包括形成结晶头孢呋辛酯和至少一种药学上可接受的赋形剂的混合物，并使混合物磨碎一段时间以足以将结晶头孢呋辛酯转变为基本上无定形的形式，即，结晶度小于5％。无定形头孢呋辛酯的化学纯度至少为95％。理想地，研磨材料的颗粒被还原成小于2的尺寸。

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