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    • 3. 发明申请
    • A CO-PRECIPITATED CEFEPIME COMPOSITION AND PROCESS FOR PREPARATION THEREOF
    • 共沉淀的头峰组合物及其制备方法
    • WO2005094800A3
    • 2005-11-24
    • PCT/IN2005000095
    • 2005-03-30
    • LUPIN LTDTYAGI OM DUTTCHAUHAN YOGENDRA KUMARSRIVASTAVA TUSHAR KUMAR
    • TYAGI OM DUTTCHAUHAN YOGENDRA KUMARSRIVASTAVA TUSHAR KUMAR
    • A61K31/546C07D501/00
    • A61K31/546
    • The present invention provides a stable and sterile composition of Cefepime with a pharmaceutically acceptable non-toxic organic and inorganic base in high purity which exhibits good thermal stability which is obtained by co precipitation of composition containing non-sterile Cefepime and non-sterile pharmaceutically acceptable base. The method of preparing the co-precipitated composition of Cefepime with pharmaceutically acceptable non-toxic base comprises of, i) dissolving a composition containing mixture of non sterile Cefepime and a non sterile pharmaceutically acceptable non-toxic organic or inorganic base in water to obtain a clear aqueous solution having a pH in the range of 3.5-7 and ii) filtration of aqueous solution through 0.2 micron membrane filter and then adding the clear aqueous solution to a suitable an organic solvent followed by stirring, filtration and drying.
    • 本发明提供了具有高纯度的药学上可接受的无毒有机和无机碱的稳定且无菌的头孢吡肟组合物,其显示出良好的热稳定性,其通过共沉淀包含非无菌头孢吡肟和非无菌药学上可接受的碱 。 制备头孢吡肟与药学上可接受的无毒碱的共沉淀组合物的方法包括:i)将含有非无菌头孢吡肟和非无菌药学上可接受的无毒有机或无机碱的混合物的组合物溶解于水中以获得 澄清的pH值为3.5-7的水溶液,和ii)通过0.2微米膜过滤器过滤水溶液,然后将澄清的水溶液加入合适的有机溶剂中,随后搅拌,过滤并干燥。
    • 9. 发明专利
    • Preparation of (2-methyl-5-phenyl-3-(piperazin-1-ylmethyl)) pyrrole derivatives
    • AU2006233943A1
    • 2006-10-19
    • AU2006233943
    • 2006-04-05
    • LUPIN LTD
    • NALAM VASANTHCHAUHAN YOGENDRA KUMARUPADHAYAYA RAM SHANKARSINHA NEELIMAJAIN SANJAYTYAGI OM DUTTARORA SUDERSHAN KUMAR
    • A61K31/4025A61P31/06C07D207/50
    • 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.