Abstract:
Apparatus for catalysis in multiphase reaction systems is provided in which catalysts are confined within various membranes without the use of covalent coupling. Confinement of the catalysts is achieved by a combination of a small-pore skin on one side of the membrane and the use of a solvent in which the catalysts are not appreciably soluble on the other. Methods are also provided for the preparation of such apparatus and for their regeneration by incorporation of fresh catalyst.
Abstract:
This invention relates to a method for the production of (2R,3S)-3-(4-methoxyphenyl)glycidic acids and esters thereof, which are synthetic intermediate for the production of the calcium antagonist diltiazem. The method involves the stereoselective enzymatic ester hydrolysis of racemic trans-3-(4-methoxyphenyl)glycidic acid ester to yield the resolved (2R,3S) compound as the ester. Membrane reactor methods and apparatus for the conduct of this enzymatic resolution process are also disclosed herein, as is the use of bisulfite anion in the aqueous reaction phase as a means of minimizing the inhibitory effect of an aldehyde reaction by-product on the reaction's progress. The benefits of selected solvent systems from which may be obtained highly resolved ester product are also disclosed. These enriched organic solutions may be used in subsequent transformations. Alternatively, optically pure product may be obtained directly therefrom.
Abstract:
This invention relates to the resolution of racemic mixtures of optically active compounds, including but not limited to the stereochemical purification of chiral organic esters, amides, carboxylic acids, alcohols, and amines. Novel methods utilizing multiphase and extractive enzyme membrane bioreactors are disclosed that selectively produce pure or substantially purified optically active compounds from achiral precursors or mixtures of isomers in which one or several of those isomers are biologically inactive or otherwise lack desirable characteristics. The invention involves the use of fluids immiscible with one another on the opposite sides of the enzyme membrane.
Abstract:
A method for treating urinary incontinence, such as incontinence resulting from bladder detrusor muscle instability, using enantiomerically enriched (S,R)-glycopyrrolate. The method comprises administering a therapeutically effective amount of enantiomerically enriched (S,R)-glycopyrrolate, or a pharmaceutically acceptable salt thereof, substantially free of the (R,S)-glycopyrrolate enantiomer. Pharmaceutical compositions for the treatment of urinary incontinence comprising enantiomerically enriched (S,R)-glycopyrrolate, or a pharmaceutically acceptable salt thereof, and an acceptable carrier are also disclosed.
Abstract:
A method for preventing dental caries by administering fluoride and, at the same time controlling periodontal bone loss precipitated by the fluoride, by providing a combination of fluoride and NSAID is disclosed. Topical medicament compositions including NSAIDS and fluoride are also disclosed.
Abstract:
A process for the preparation of taxol and derivatives of taxol (I) is disclosed. The process involves reacting a beta -alkoxycarbonylamino-phenylpropionic acid with a 13-hydroxy taxane to produce an ester of the taxane at C-13; and then deprotecting the beta -alkoxycarbonylamino-phenylpropionic ester to produce a beta -amino- alpha -hydroxybenzenepropanoic ester of the taxane. Intermediates useful in the process are also disclosed.
Abstract:
A method for the enantioselective reduction of prochiral ketones using catalytic amounts of tetrahydroindeno[1,2-d][1,3,2]oxazaboroles of formula (II) is disclosed. The oxazaboroles can be generated in situ from the corresponding cis-1-amino-2-indanols or imino indanols (III). Novel compounds of formulas (II) and (III) are also disclosed.
Abstract:
Methods and compositions are disclosed utilizing optically pure (-)-fadrozole for the treatment of estrogen-dependent breast cancer, gynecomastia, systemic lupus erythematosus and premature labor while substantially reducing the concomitant liability of adverse effects associated with the racemic mixture of fadrozole. (-)-Fadrozole is an inhibitor of aromatase and is therefore useful in the treatment of other conditions supported by estrogen or caused by elevated estrogen levels.
Abstract:
Methods and compositions are disclosed utilizing optically pure R-(-)-casodex for the treatment of androgen-dependent prostate cancer, while substantially reducing the concomitant liability of adverse effects associated with the central antiandrogen activity of the racemic mixture of casodex. R-(-)-casodex is a peripherally selective antiandrogen and is therefore useful in the treatment of other conditions supported by androgen or caused by elevated androgen levels. Such conditions include benign prostatic hypertrophy or hyperplasia, acne and hirsutism.
Abstract:
Methods and compositions are disclosed utilizing the optically pure (2R,4S) isomer of itraconazole. This compound is a potent drug for the treatment of local and systemic fungal, yeast, and dermatophyte infections, while avoiding the concomitant liability of adverse effects associated with the racemic mixture of itraconazole.