Abstract: Compounds of formula ##STR1## where R is 5-indanyl or a carboxylic acid protecting group, or an amine salt thereof, are prepared by hydrogenating an (E)-allylic ether of formula ##STR2## in the presence of a stereoselective rhodium or ruthenium biphosphine catalyst and a protic solvent.

Abstract: Macrolides of formula (I) and methods of treatment of resistance to transplantation, fungal infections and autoimmune diseases such as rheumatoid arthritis and psoriasis using said macrolides of formula (I), ##STR1## wherein n is 1 or 2; A and B are taken together and form .dbd.O or A and B are taken separately and are each OH or A is OH and B is H; R.sup.1 is a fluoroglycosyl group; R.sup.2 is OH or a fluoroglycosyloxy group; and R.sup.3 is an alkyl or allyl group.

Abstract: A method of blocking N-methyl-D-aspartic acid (NMDA) receptor sites in a mammal in need thereof with an effective NMDA blocking (neuroprotective and antiischemic) amount of prodrug esters of 2-piperidino-1-alkanol derivatives and prodrug esters of 2-azabicyclo-1-alkanol derivatives and analogs and pharmaceutically acceptable salts thereof; methods of using these compounds in the treatment of stroke, spinal cord trauma, traumatic brain injury, multiinfarct dementia, CNS degenerative diseases such as Alzheimer's disease, senile dementia of the Alzheimer's type, Huntington's disease, Parkinson's disease, epilepsy, amyotrophic lateral sclerosis, pain, AIDS dementia, psychotic conditions, drug addictions, migraine, hypoglycemia, anxiolytic conditions, urinary incontinence and an ischemic event arising from CNS surgery, open heart surgery or any procedure during which the function of the cardiovascular system is compromised.

Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sup.1 is H, C.sub.1 -C.sub.4 alkyl CN or CONR.sup.4 R.sup.5 ; R.sup.2 is C.sub.2 -C.sub.4 alkyl; R.sup.3 is SO.sub.2 NR.sup.6 R.sup.7, NO.sub.2, NH.sub.2, NHCOR.sup.8 NHSO.sub.2 R.sup.8 or N(SO.sub.2 R.sup.8).sub.2 ; R.sup.4 and R.sup.5 are each independently selected from H and C.sub.1 -C.sub.4 alkyl; R.sup.6 and R.sup.7 are each independently selected from H and C.sub.1 -C.sub.4 alkyl optionally substituted with CO.sub.2 R.sup.9, OH, pyridyl 5-isoxazolin-3-onyl, morpholino or 1-imidazolidin-2-onyl; or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino, morpholino, 1-pyrazolyl or 4-(NR.sup.10)-1-piperazinyl group wherein any of said groups may optionally be substituted with one or two substituents selected from C.sub.1 -C.sub.4 alkyl, CO.sub.2 R.sup.9, NH.sub.2 and OH; R.sup.8 is C.sub.1 -C.sub.4 alkyl or pyridyl; R.sup.9 is H or C.sub.1 -C.sub.4 alkyl; and R.sup.10 is H, C.sub.

Abstract: Two novel optically pure intermediates, (R)-4-(2-bromo-1-hydroxyethyl)-2- trifluoro(-)methylthiazole and (S)-4-oxiranyl-2-trifluoromethylthiazole, which have utility in the synthesis of a potent class of antidiabetic agents. The invention also embraces an enantioselective reduction process for their preparation.

Abstract: Macrolides of formula (I) and methods of treatment of resistance to transplantation, fungal infections and auto-immune diseases such as rheumatoid arthritis and psoriasis using said macrolides of formula (I), ##STR1## wherein n is 1 or 2; A and B are taken together and form .dbd.O or A and B are taken separately and are each H or A is OH and B is H; R.sup.1 is a desosamino group; R.sup.2 is OH or a desosaminyloxy group; and R.sup.3 is an alkyl or allyl group.

Abstract: The borane reduction of prochiral ketones to optically pure alcohols is effectively achieved by the utilization of catalytic amounts of the new and valuable oxazaborolidine catalysts of formula (I).

Abstract: This invention is directed to anthelmintic benzimidazole compounds of the formula (I), ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.6 alkylthio; R.sup.2 is C.sub.1 -C.sub.4 alkyl; and R.sup.3 is C.sub.1 -C.sub.4 alkyl.

Abstract: 2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula ##STR1## wherein Q is S or CH.dbd.CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y.sup.1 are taken together and are arylmethylene or aralkylmethylene (or a corresponding epoxy derivative) or Y and Y.sup.1 are taken separately and Y is hydrogen or OH, and Y.sup.1 is aryl, aralkyl, arylthio, or aryloxy; and structurally related 2-(piperidino) alkanols; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.

Abstract: This invention is directed to certain 2-(alkoxycarbonylamino)- and 2-(alkoxycarbonylimino)benzlmidazole derivatives which are useful in the topical, oral or parenteral treatment of animals suffering from helminth infections.

Abstract: A process for the stereoselective preparation of intermediates in the preparation of potent, chiral thiazolidine-2,4-dione hypoglycemics.

Abstract: Macrolides of the FK-506 type and methods of treatment of resistance to transplantation, fungal infections, and autoimmune diseases such as rheumatoid arthritis and psoriasis using said macrolides.

Abstract: Compounds of the formulae ##STR1## where R is cycloalkyl or aryl; R.sub.1 is alkyl, X is O or C.dbd.O; A is O or S; and B is N or CH are useful as hypoglycemic agents.

Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Actinomadura sp. ATCC 55080. This novel antibiotic is useful as an anticoccidial in poultry, in the prevention and treatment of swine dysentery and as a growth promotant in cattle and swine.

Abstract: Compounds of formula: ##STR1## and pharmaceutically acceptable salts thereof whereinR.sup.1 is H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or CONR.sup.5 R.sup.6 ;R.sup.2 is H or- C.sub.1 -C.sub.4 alkyl;R.sup.3 is C.sub.2 -C.sub.4 alkyl;R.sup.4 is H, C.sub.2 -C.sub.4 alkanoyl optionally substituted with NR.sup.7 R.sup.8, (hydroxy)C.sub.2 -C.sub.4 alkyl optionally substituted with NR.sup.7 R.sup.8, CH.dbd.CHCO.sub.2 R.sup.9, CH.dbd.CHCONR.sup.7 R.sup.8, CH.sub.2 CH.sub.2 CO.sub.2 R.sup.9, CH.sub.2 CH.sub.2 CONR.sup.7 R.sup.8, SO.sub.2 NR.sup.7 R.sup.8, SO.sub.2 NH(CH.sub.2).sub.n NR.sup.7 R.sup.8 or imidazolyl;R.sup.5 and R.sup.6 are each independently H or C.sub.1 -C.sub.4 alkyl;R.sup.7 and R.sup.8 are each independently H or C.sub.1 -C.sub.4 alkyl, or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino, morpholino or 4-(NR.sup.10)-1-piperazinyl group wherein any of said groups is optionally substituted with CONR.sup.5 R.sup.6 ;R.sup.9 is H or C.sub.1 -C.sub.

Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Actinomadura sp. ATCC 53764. This novel antibiotic is useful as an anticoccidial in chickens, in the prevention or treatment of swine dysentery, and as a growth promotant in cattle and swine.

Abstract: This invention is directed to anthelmintic benzimidazole compounds of formula (IA) or (IB) ##STR1## or non-toxic salts thereof, wherein R, which in the compounds (IA) is in the 5- or 6- position, is H, benzoyl, styryl, phenyloxy, phenylthio, phenylsulfinyl, phenylsulfonyl, phenylsulfonyloxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulfinyl, C.sub.1 -C.sub.6 alkylsulfonyl or (C.sub.3 -C.sub.7 cycloalkyl) carbonyl, said phenyl groups, and the phenyl portion of said benzoyl group, optionally having 1 to 3 substituents each independently selected from halo, C.sub.1 -C.sub.4 alkyl, halo-(C.sub.1 -C.sub.4 alkyl), C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.2 -C.sub.4 alkanoyl, nitro, isothiocyanato, and cyano; and either (a) R.sup.1 is a 1- (C.sub.2 -C.sub.6 alkanoyloxy) (C.sub.1 -C.sub.4 alkyl) group and R.sup.2 is H, C.sub.1 -C.sub.4 alkyl or a 1-(C.sub.1 -C.sub.

Abstract: Certain 3-(phenyl, chroman-2-yl, benzofuran-5-yl or benzoxazol-5-yl)-2-(hydroxy or mercapto)propionic acid derivatives and analogs are useful as hypoglycemic and hypocholesterolemic agents.

Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof are selective cGMP PDE inhibitors which are useful in the treatment of such diseases and adverse conditions as angina, hypertension, congestive heart failure, reduced blood vessel patency, peripheral vascular disease, stroke, bronchitis, chronic asthma, allergic asthma, allergic rhinitis, glaucoma, and diseases characterized by disorders of gut motility.