Abstract: A method of treatment of a human to inhibit a steroid 5.alpha.-reductase, particularly a testosterone 5.alpha.-reductase, which comprises treating said human with an effective amount of a compound of the formula (I) ##STR1## or a pharmaceutically acceptable base salt thereof, wherein R is --CO.sub.2 H or tetrazol-5-yl;R.sup.1 is C.sub.3 -C.sub.8 alkyl optionally substituted by fluoro; andR.sup.2 is C.sub.2 -C.sub.4 alkylor with a pharmaceutically acceptable base salt or composition thereof. Conditions which are treatable by such inhibition include acne vulgaris, alopecia, seborrhoea, female hirsutism, benign prostatic hypertropy, male pattern baldness and human prostate adenocarcinomas.

Abstract: Compounds of formula (I), ##STR1## wherin X is CH.sub.2, CO, CS or SO.sub.2 ; Y is selected from: a direct link, aliphatic hydrocarbylene radicals having up to 20 carbon atoms, which radical may be mono-substituted by hydroxy, (C.sub.1 -C.sub.10)alkoxy, (C.sub.1 -C.sub.10)acyl, (C.sub.1 -C.sub.10)acyloxy, or (C.sub.6 -C.sub.10)aryl, NH, and O, provided that if X is CH.sub.2,Y is a direct link; Z is selected from the following groups: (1) H, halo, cyano, (2) hydroxy, (C.sub.1 -C.sub.10)alkoxy, (C.sub.1 -C.sub.10)a1kylthio, (C.sub.1 -C.sub.10)acyl, thiophenylcaronyl (C.sub.1 -C.sub.10)alkoxycarbonyl, (3) (C.sub.1 -C.sub.10)aklkyammo, di(C.sub.1 -C.sub.10)alylamino, (C.sub.6 -C.sub.10)aryl(C.sub.1 -C.sub.10)alkylamino, provided that Y is not O or NH, (4) unsubstituted vinyl, (C.sub.6 -C.sub.10)aryl, (C.sub.3 -C.sub.8)cycloalkyl and fused benz derivatives thereof, (C.sub.7 -C.sub.10)polycycloalkyl, (C.sub.4 -C.sub.8)cycloalkenyl, (C.sub.7 -C.sub.10)polycycloalkenyl, (5) (C.sub.6 -C.sub.10)aryloxy, (C.sub.6 -C.

Abstract: A compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein X is O, S or NH;R and R.sup.1 are each independently selected from H and C.sub.1 -C.sub.4 alkyl or taken together represent C.sub.2 -C.sub.6 alkylene;R.sup.2 is H or C.sub.1 -C.sub.4 alkyl;R.sup.3 is a 6-membered heterocyclic ring containing 2N hetero-atoms, said ring being linked to X by a ring carbon atom, optionally benzo-fused and optionally substituted, including in the benzo-fused portion, by C.sub.1 -C.sub.6 alkyl, hydroxy, --OR.sup.5, halo, --S(O).sub.m R.sup.5, oxo, amino, --NHR.sup.5, --N(R.sup.5).sub.2, cyano, --CO.sub.2 R.sup.5, --CONH.sub.2, --CONHR.sup.5 or --CON(R.sup.5).sub.2, with the proviso that R.sup.3 is not an N--(C.sub.1 -C.sub.6 alkyl)pyridonyl group;R.sup.4 is phenyl substituted by a hydroxy group and optionally further substituted by 1 or 2 substitutents each independently selected from hydroxy, C.sub.1 -C.sub.6 alkyl, --OR.sup.5, halo, cyano and nitro;R.sup.5 is C.sub.1 -C.sub.6 alkyl;R.sup.

Abstract: Devices for controlled release of active substances in the form of tablets, capsules and beads comprised of a porous substructure surrounded by one or more interfacial membranes.

Abstract: Certain 1-(benzyl or 5-benzofuranylmethyl)-1-hydroxyurea derivatives are useful as hypoglycemic and hypocholesterolemic agents.

Abstract: A method for the separation of R-(+)- and S-(-)-isomers of amlodipine (I) from mixtures thereof, which comprises the reaction of the mixture of isomers with either L- or D-tartaric acid in an organic solvent containing sufficient dimethyl sulphoxide (DMSO) for the precipitation of, respectively, a DMSO solvate of an L-tartrate salt of R-(+)-amlodipine, or a DMSO solvate of a D-tartrate salt of S-(-)-amlodipine.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is H, C.sub.1 -C.sub.3 alkyl, C.sub.3 -C.sub.5 cycloalkyl or C.sub.1 -C.sub.3 perfluoroalkyl;R.sup.2 is H, C.sub.1 -C.sub.6 alkyl optionally substituted by OH, C.sub.1 -C.sub.3 alkoxy or C.sub.3 -C.sub.6 cycloalkyl, or C.sub.1 -C.sub.3 perfluoroalkyl;R.sup.3 is H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.6 perfluoroalkyl or (C.sub.3 -C.sub.6 cycloalkyl)C.sub.1 -C.sub.6 alkyl;and Y is chloro, bromo, or fluoro.The above compounds are intermediates useful in the synthesis of certain pyrazolopyrimidinones which inhibit cyclic guanosine 3', 5'-monophosphate phosphodiesterase.

Abstract: Compounds of the formula ##STR1## wherein R is an optionally substituted heteroaryl group such as 2-chromanyl, 2-pyridyl or 5-fluoro-2-benzothiazoyl;X is O, S or (CH.sub.2).sub.m ;R.sup.1 is phenyl or pyridyl, optionally substituted by one or more (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, carboxy or ?(C.sub.1 -C.sub.3)alkoxy!carbonyl groups;n is 0, 1 or 2;m is 1 or 2;Y and Y.sup.1 are taken together and are oxygen, or Y and Y.sup.1 are taken separately, Y is hydrogen and Y.sup.1 is hydroxy or an in vivo hydrolyzable acyloxy group;Z is CH.sub.2, NR.sup.2, O or S; andR.sup.2 is hydrogen or (C.sub.1 -C.sub.3)alkyl;are useful in the treatment of asthma, arthritis and related diseases mediated by leukotrienes.

Abstract: Compounds of formula (I) ##STR1## and the pharmaceutically acceptable base salts thereof, wherein R is --CO.sub.2 H or tetrazol-5 yl; R.sup.1 is C.sub.3 -C.sub.8 alkyl optionally substituted by fluoro; and R.sup.2 is C.sub.2 -C.sub.4 alkyl, together with compositions containing, uses of, process for the preparation of, and intermediates used in the preparation of, such compounds. The compounds have steroid 5.alpha.-reductase inhibitory activity and are useful for treating a disease such as benign prostatic hypertrophy.

Abstract: A compound having formula (III). Also, a process of making azithromycin comprising reducing the compound of formula (III) and N-methylating the reduced product.

Abstract: The present invention relates to compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein the dashed line represents an optional covalent bond; X is O, NH, S or a direct link; R.sup.3 is hydroxy when the dashed line does not represent a covalent bond and R.sup.3 is absent when the dashed line represents a covalent bond; R.sup.4 is (a), when X is O, a group of formula (i), (b), when X is O, NH or S, optionally substituted hydroxyphenyl, (c) an optionally substituted 4- to 7-membered heterocyclic ring, or (d), when X is NH, a group of formula (ii). The compounds are useful for the treatment of disease associated with the altered tone or motility of smooth muscle.

Abstract: 4-Chloro-2-thiophenecarboxylic acid is made by forming a compound of formula (Ia), disclosed herein, wherein R.sup.3 is (C.sub.1 -C.sub.6) alkyl, phenyl, or benzyl; converting the compound to a compound of formula (IVa), disclosed herein, and removing the silyl group R.sub.3 Si--. The product is useful as an intermediate in making pharmaceutical products.

Abstract: Process for the preparation of a dialkyl trans-piperidine-2,5-dicarboxylate from a corresponding dialkyl cis-piperidine-2,5-dicarboxylate via a trans-substituted pyridine derivative of the formula ##STR1## wherein R is a (C.sub.1 -C.sub.3)alkyl group.

Abstract: A solid phase coupling reagent for amide formation, comprising insoluble polymer bearing pendant side chains, said side chains each comprising a terminal portion having the formula ##STR1## wherein Y.sup.- is a counteranion and n is independently an integer from 2 to 6; and a method of making amides employing the coupling reagent.

Abstract: An oral dosage form of azithromycin which does not exhibit an adverse food effect; Specific azithromycin oral dosage forms including tablets, powders for oral suspensions and unit dose packets; Methods of treating microbial infections with the dosage forms; And therapeutic packages containing the dosage forms.

Abstract: Aminobenzosultam derivatives, which are inhibitors of lipoxygenase, having the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein Ar is cycloalkyl having five to seven carbon atoms, tetrahydropyranyl, pyridyl, oxazolyl, phenyl or substituted phenyl wherein said substituent is methyl, methoxy, fluoro, chloro or trifluoromethyl; n is an integer of 1 to 3; X is hydrogen, methyl, methoxy, fluoro, chloro or trifluoromethyl; Z is --NH--, --O--, or --CH.sub.2 --; and R.sup.1 is hydrogen or alkyl having one to three carbon atoms.

Abstract: Process for the preparation of a dialkyl trans-piperidine-2,5-dicarboxylate from a corresponding dialkyl cis-piperidine-2,5-dicarboxylate via a trans-substituted pyridine derivative of the formula ##STR1## wherein R is a (C.sub.1 -C.sub.3)alkyl group.

Abstract: Compounds of formula I ##STR1## or salts thereof, where R is alkyl, phenyl, phenoxy or substituted phenyl and phenoxy; X is S or O; n is an integer of 1 or 2; A is --CH.sub.2 -- or --CH(CH.sub.3)--; and B is hydrogen or methyl, useful as antiallergy and antiinflammatory agents.

Abstract: Certain 1-(benzyl or 5-benzofuranylmethyl)-1-hydroxyurea derivatives are useful as hypoglycemic and hypocholesterolemic agents.