Abstract: Pharmaceutically suitable crystalline and amorphous alkali and earth-alkali salts of 2-n-butyl-4-chloro-5-hidrox-ymethyl-1-[[2?-(1 H-tetrazole-5-yl)[1.1?-biphenyl]-4-yl]-1 Himidazole have been prepared and new manufacturing, purification and isolation procedure for said salts in high purity have been described. Stable pharmaceutical compositions containing new crystalline potassium salts of 2-n-butyl-5-chloro-5hidroxymethyl-1-[[2?-(1H-tetrazole-5-yl)[1.1?-biphenyl]-44-yl]-1H-imidazole have been prepared.

Abstract: 3-ethyl 5-methyl (+/?) 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate benzenesulfonate, containing overall impurities of significantly less than 0.3% is disclosed, as well as process for its preparation, according to which substance of 3-ethyl 5-methyl (+/?) 2-[2-(N-trialkylamino)ethoxymethyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate is converted with benzenesulfonic acid in ethanol solution, at a temperature between 20° C. and reflux temperature, followed by isolation and purification of 3-ethyl 5-methyl (+/?) 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate benzenesulfonate. Amlodipine benzenesulfonate is useful as an antiishemic and antihypertensive agent.

Abstract: The present invention relates to new processes for the preparation of gabapentin by the desilylation of a silylated gabapentin or by the silylation-desilylation of an acid addition salt of gabapentin with a silylating agent.

Abstract: Atorvastatin calcium, the substance known by the chemical name (R—(R*,R*))-2-(4-fluorophenyl)-?, ?-dihydroxy-5-(1-methylethyl)-3-phenyl-((phenylamino)carbonyl)-1H-pyrrole-1-heptanoic acid hemi calcium salt is known as HMG-CoA reductase inhibitor and is used as an antihypercholesterolemic agent. Atorvastatin in the pharmaceutical compositions available in the market, is usually prepared as its calcium salt since it enables atorvastatin to be conveniently formulated in the pharmaceutical formulations, for example, in tablets, capsules, powders and the like for oral administration. Atorvastatin calcium can exist in an amorphous form or in one of the at least four known crystalline forms (Form I, Form II, Form III and Form IV). Atorvastatin calcium is the substance which is sparingly soluble in water, with pKa 4,5, and it has been found that the crystalline forms are less soluble than the amorphous form, which may cause problems in bioavailability of atorvastatin in the body.

Abstract: This invention provides a process of preparation of novel polymorphic hemifumarate salts of 8-chloro-6,11-dihyfro-11-(4-piperidylidene)-5H-benzo[5,6]-cyclohepta[1,2-b]pyridine, hereinafter called “desloratadine”. These polymorphic salt forms show much higher solubility in water and also in protic organic solvents compare to the parent desloratadine. The process of preparing the polymorphic forms comprising: a) mixing the ethanolic solution of desloratadine and fumaric acid at a temperature of from about 55° C. to 70° C., and stirring for 30 to 45 minutes after mixing, and thereafter filtering the solid thereby prepared in hot condition; to yield the polymorphic form 2 having a DSC of 232° C.±2° C.; or b) mixing the ethanolic solution of desloratadine and fumaric acid at a temperature of form about 15° C. room temperature (25° C.) and stirring at this temperature for 30 to 45 minutes, then filtering at room temperature; to yield the polymorphic form 1 having a DSC of 224° C.±2° C.

Abstract: Azithromycin in the form of a monohydrate comprising from 4.0% to 6.5% of water, a process for its preparation and its use in pharmaceutical compositions.

Abstract: The novel intermediate compound crystalline 7-[2-(2-fomylaminothiazol-4-yl)-2 -(Z)-(methoxyimino)acetamido]-3-methoxymethyl-3-cephem-4-carboxylic acid-1 -(isopropoxy/crystallization of cefpodoxime proxetil. The crystallization process comprises dissolving or suspending the intermediate in the presence of a nitrile or a ketone or mixtures thereof; at a ratio of 1 gm of the intermediate to 2-15 ml nitrile; or at a ratio of 1 gm of the intermediate to 3-15 ml ketone; in the presence of 5-80 ml water; and thereafter isolating the intermediate in crystalline form and converting the intermediate by splitting off the formyl group from the amino group attached to the thiazolyl group, to obtain the desired product cefpodoxime proxetil, in the form of a diastereoisomeric mixture in a ratio of B/(A+B) of 0.5 to 0.6.

Abstract: The present invention relates to a process for the recombinant production of a desired heterologous polypeptide with a clearly defined homogenous N-terminus in a bacteria host cell. A fusion comprising a peptide with the autoproteolytic activity of an autoprotease Npro of a pestivirus and the heterologous polypeptide is initially expressed in the form of cytoplasmic inclusion bodies in the host cell, the inclusion bodies are isolated and subsequently treated so that the desired heterologous polypeptide is cleaved autoproteolytically by the Npro activity of the fusion protein.

Abstract: A pharmaceutical composition comprising as an active ingredient an HMG-CoA reductase inhibitor and an aminosugar.

Abstract: A stable pharmaceutical composition comprising about 1 wt. % to about 80 wt. % of an ACE inhibitor or a pharmaceutical acceptable salt thereof, about 1 wt. % to about 70 wt. % of an alkali or alkaline earth metal carbonate, and about 1 wt. % to about 80 wt. % of hydroxypropyl cellulose, wherein the ACE inhibitor is selected from the group consisting of quinapril, enalapril, spirapril, ramipril, perindopril, indolapril, lisinopril, alacepril, trandolapril, benazapril, libenzapril, delapril, cilazapril and combinations thereof; wherein the formation of an internal cyclization product, and/or ester hydrolysis product, and/or oxidation product, has been reduced or eliminated, and the weight percents are based on the total weight of the pharmaceutical composition.

Abstract: A method for preparing an alkali metal salt comprising: (a) condensing a disilyloxydiene with an aldehyde in the presence of a titanium (IV) catalyst in an inert solvent to form a 5(S)-hydroxy-3-ketoester; (b) reducing the 5(S)-hydroxy-3-ketoester to a 3(R),5(S)-dihydroxyester in the presence of a di(lower alkyl)methoxyborane; and (c) hydrolyzing the 3(R),5(S)-dihydroxyester in the presence of an aqueous base to form an alkali metal salt.

Abstract: Processes for the depletion of 7-ADCA in mixtures of vinyl-ACA with 7-ADCA via novel salts of vinyl-ACA or via chromatography.

Abstract: A process for the purification of cefixime via a novel tert-octylamine salt of a cefixime intermediate of formula V which may be crystalline and which may be produced in a one-pot reaction from 7-amino-3-vinyl-ceph-3-em-4-carboxylic acid.

Abstract: A process which comprises (i) acylating a compound of formula II with a compound of formula IV to obtain a compound of formula I and (ii) deformylating said compound of formula I to obtain a compound of formula III

Abstract: A compound of formula (I) wherein R2 is arylene or heterocyclene; or R and R2 together with the nitrogen atom to which they are attached form non-aromatic heterocyclene; and the other residues have various meanings, useful as pharmaceuticals, e.g. antimicrobials.

Abstract: A process for the production of a compound of formula comprising i) silylating a compound of formula then reacting a resulting with a compound of formula R′BS—X′  IVB wherein R′B is hydrogen or trialkysilyl and X′ is as defined above, in the presence of a compound of formula wherein R2, R3 and R4 independently of each another are aryl or alkyl, and R5 is alkyl, perfluorinated alkyl, or aryl; and isolating the desired product.

Abstract: This invention provides composition comprising a cyclosporin and a carrier medium.

Abstract: A compound selected from 14—O—[(cycloalkyl-sulfanyl)acetyl]mutilins; 14—O—[(cycloalkyl-alkyl-sulfanyl)acetyl] mutilins; 14—O—[(cycloalkoxy)acetyl] mutilins; and 14—O—[(cycloalkyl-alkoxy)acetyl] mutilins and its use as a pharmaceutical.

Abstract: A low temperature process for preparing an aromatic acid having formula (I), said process comprising reacting an aromatic aldehyde having formula (II) with a gas having an oxygen content of 1 to 100 weight percent, based on the total weight of the gas, at a temperature of about 20° C. to less than 100° C. in the presence of a supported Group VIII metal catalyst, and a solvent having a flash point greater than 95° C. and/or a melting point less than 55° C., provided that the flash point of the solvent is greater than the reaction temperature, wherein R1 and R2 are independently selected from the group consisting of hydrogen and a C1-C8 linear, branched or cyclic alkyl group. The process of the invention yields an aromatic acid in excellent yield, and (i) does not involve the use of deleterious oxidizing agents; (ii) is essentially free of by-products; and (iii) is accomplished at a temperature of less than 100° C.

Abstract: Use of the 2-amino-2,4,4-trimethylpentane salt of clavulanic acid as an intermediate in the production of pharmaceutically acceptable salts of clavulanic acid.