Abstract: A method for the systematic and efficient synthetic preparation and identification of metabolites of a pharmaceutical product in order to study possible toxic and/or otherwise biologically-active metabolites of such pharmaceutical products as early and conveniently as possible in the very expensive drug development process, comprising adding samples of the pharmaceutical product to a series of combinations of a synthetic metalloporphyrin (SMP) with a synthetic metalloporphyrin-co-oxidizing reagent in the presence of a suitable solvent, under specified conditions, in a manner such that each sample of pharmaceutical product is reacted with a different combination of synthetic metalloporphyrin, SMP-co-oxidizing reagent and solvent, followed by separation and isolation of the resulting oxidative products, then confirmation of the identity of metabolites from the pre-identified oxidative products by appropriate animal model studies, and subjecting the actual metabolites prepared in larger quantities by the above m

Abstract: A process for the crystallization of an iron-dextran complex in readily-filterable form comprising adding slowly, with stirring, an acidified aqueous iron-dextran solution to a vessel containing a water miscible organic solvent such as methanol, as well as crystalline iron-dextran complexes so prepared.

Abstract: The present invention relates to a process for the selective alkylation of intermediates of betaxolol.

Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.

Abstract: A process of synthesizing a peptide using an alkylene oxide as an acid scavenger is provided. A process of the present invention can be used in a solid phase or solution phase synthetic process where peptide synthesis occurs by the sequential addition of N-.alpha.-amino-Boc-protected residues followed by acid deprotection of that N-.alpha.-amino protecting group and scavenging of the acid.

Abstract: The invention relates to a mutant of Bacillus thuringiensis which produces a larger amount of crystal delta-endotoxin with a greater pesticidal activity as compared to the corresponding parental strain. The mutant may also have a larger crystal size as compared to the corresponding parental strain. The crystal delta-endotoxin produced by the mutant Bacillus thuringiensis will have an activity directed towards the same pest(s) as its parental Bacillus thuringiensis crystal delta-endotoxin. The invention further relates to a method for producing such a mutant, compositions comprising such a mutant as well as methods for controlling a pest(s) using these compositions.

Abstract: The present invention provides a process for the preparation of BPD 1,4-diene diester A-ring comprising reacting hematoporphyrin IX dimethyl ester with dimethyl acetylenedicarboxylate followed by purification of the product by a series of fractional crystallizations.

Abstract: A process of producing atracurium besylate that substantially reduces the level of impurities in the final product and avoids the repeated use of ether is provided. In accordance with such a process, N, N'-4,10-dioxa-3,11-dioxotridecylene-1,13-bis-tetrahydropapaverine (Compound 1), methyl benzenesulfonate and a catalytic amount of an insoluble base in a solvent are combined to form a reaction mixture that is maintained for a period of time sufficient for atracurium besylate formation. The reaction mixture is then filtered to remove the insoluble base and the atracuriurn besylate is precipitated.

Abstract: The present invention relates to the production of pemoline and its intermediates.

Abstract: The present invention relates to devices and methods for enhancing the rate and efficacy of permeation of a drug into and through skin and into the circulatory system utilizing ultrasound.

Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.

Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.

Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed wherein the terms R.sub.1, R.sub.2, R.sub.5, R.sub.6, Y, Y', m and n are herein defined.

Abstract: The invention relates to a mutant of Bacillus thuringiensis which produces a larger amount of crystal delta-endotoxin with a greater pesticidal activity as compared to the corresponding parental strain. The mutant may also have a larger crystal size as compared to the corresponding parental strain. The crystal delta-endotoxin produced by the mutant Bacillus thuringiensis will have an activity directed towards the same pest(s) as its parental Bacillus thuringiensis crystal delta-endotoxin. The invention further relates to a method for producing such a mutant, compositions comprising such a mutant as well as methods for controlling a pest(s) using these compositions.

Abstract: A process for the manufacture of vancomycin which does not require preparation of a phosphate intermediate. The process consists of passing a vancomycin broth through a suitable adsorbent, followed by passing the vancomycin through a second adsorbent, producing a purified vancomycin. Purified vancomycin is then crystallized from the solution by adding a base solution that imparts a pH of above about 9.0 to about 9.5 to the purified vancomycin. The crystallized vancomycin is separated from the solution, dissolved in solution and recrystallized by adding a base solution which imparts a pH of above about 9.0 to about 9.5 to the dissolved solution. The recrystallized vancomycin is dissolved and titrated with hydrochloric acid. Vancomycin. HCl is then precipitated from the solution using an organic solvent.

Abstract: A method for the separation of gibberellins from mixtures thereof by selective silylation or desilylation, as well as substantially pure gibberellins prepared thereby.

Abstract: A needle guard assembly for a prefilled emergency syringe includes a cylindrical sidewall which extends coaxially with the syringe needle. The sidewall is joined to the syringe housing by spin welding or sonic welding an annular fusible portion that extends axially rearward from an annular flange on the base of the sidewall to contact the front wall of the housing. The sidewall is joined to the housing so that an annular clearance space for the hood is maintained between the hub and the sidewall guard.

Abstract: A pharmaceutical tablet composition comprising a compound of the formula (II): ##STR1## wherein R.sub.1 is 4-piperazinyl, 1-methyl-4-piperazinyl, 1-methyl-1-oxo-4-piperazinyl, 2-oxo-4-piperazinyl, 4-morpholinyl, 4-thiomorpholinyl or 1-methyl-4-homopiperazinyl;R.sub.2 is benzyl, p-methoxybenzyl, 2-phenylethyl, 1-naphthylmethyl or 2-naphthylmethyl;R.sub.3 is 4-thiazolyl, 2-amino-4-thiazolyl, 2-thiazolyl, 5-thiazolyl, 1-pyrazolyl, 3-pyrazolyl, 1-imidazolyl, n-propyl, isopropyl, CH.sub.3 S-- or CH.sub.3 SCH.sub.2 --;R.sub.4 is loweralkyl or cyclopropyl;R.sub.5 is hydrogen or loweralkyl; andX is CH.sub.2 or NH;or a pharmaceutically acceptable salt, ester or prodrug thereof, and a pharmaceutically acceptable organic polycarboxylic acid. In addition, the tablet composition can further comprise one or more pharmaceutically acceptable non-ionic surfactants.