Abstract: The present invention provides class of compounds of formula I ##STR1## and their pharmaceutically acceptable salts in which R.sup.1 is hydrogen, hydroxy, alkoxy, alkoxycarbonyloxy, alkylcarbonyloxy, arylcarbonyloxy; R.sup.2 is hydrogen, hydroxy, alkoxy, alkoxycarbonyloxy, alkylcarbonyloxy, alkylsulfonyloxy, arylcarbonyloxy, Cl or Br; R.sup.3 and R.sup.4 are independently C.sub.1 -C.sub.4 alkyl, or combine with the nitrogen atom to which they are attached to form a pyrrolidino, piperidino, or hexamethyleneimino ring; X is selected from ##STR2## and Y is --CO--, --CHOH--, or --CH.sub.2 --. The compounds and pharmaceutical compositions containing the compounds, either alone or in combination with either progestin or estrogen, are useful for alleviating the symptoms of osteoporosis, cardiovascular related pathological conditions such as hyperlipidemia, and estrogen-dependent cancer.

Abstract: Oligopeptide compounds or oligopeptide analague compounds of the formula, A-B-D-E-G-J-L-M-N(R.sup.4)Arg-OH, which are ligands for the anaphylatoxin receptor and are useful in the treatment of inflammatory disease states, as well as anaphylatoxin receptor ligand compositions and a method for modulating anaphylatoxin activity.

Abstract: The present invention provides a method of inhibiting hormone-dependent breast carcinoma in a mammal comprising administering to said mammal in need of treatment an effective amount of a first component which is a compound of formula I ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl);R.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl);n is 2 or 3; andR.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;or a pharmaceutically acceptable salt thereof, and an effective amount of a second component which is a compound of formula II ##STR2## wherein either R.sup.4 is H or a lower alkyl radical and R.sup.5 is a lower alkyl radical, or R.sup.4 and R.sup.

Abstract: The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxy)benzoyl]benzo[b]thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thi ophene hydrochloride, as well as processes for their preparation.

Abstract: The present invention relates to a compound of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein W is a tricyclic heterocyclic ring system; which is an .alpha.-1 adrenergic antagonist and is useful in the treatment of BPH; also disclosed are .alpha.-1 antagonist compositions and a method for antagonizing .alpha.-1 receptors and treating BPH.

Abstract: A process for preparing a compound of the structure I ##STR1## where A is oxygen and sulfur and R.sup.1 is selected from the group consisting of hydrogen, halogen, alkyl of one to six carbon atoms, alkoxy of one to six carbon atoms, and trifluoromethyl, and R.sup.2 is alkyl of one to four carbon atoms, comprising coupling a compound of formula II: ##STR2## where X is bromine or iodine, with an N-hydroxyurea compound of formula III: ##STR3## in the presence of a palladium catalyst followed by reaction of the product thus formed with an alkali metal isocyante.The compounds of formula I are inhibitors of the enzyme 5-lipoxygenase and are thus useful as therapeutic agents for the treatment of allergic and inflammatory disease conditions.

Abstract: The present invention provides compounds of formula ##STR1## and the pharmaceutically acceptable salts thereof which are potent antagonists of PAF and are useful in the treatment of PAF-related disorders including asthma, shock, respiratory distress syndrome, acute inflammation, transplanted organ rejection, gastrointestinal ulceration, allergic skin diseases, delayed cellular immunity, parturition, fetal lung maturation, and cellular differentiation.

Abstract: Compounds of the structure ##STR1## where p and q are zero or one, but cannot both be the same, M is a pharmaceutically acceptable cation or a metabolically cleavable group, B is a valence bond or a straight or branched alkylene group, R is alkyl, cycloalkyl or --NR.sup.1 R.sup.2, where R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl or alkanoyl, and A is optionally substituted carbocyclic aryl, furyl, benzo[b]furyl, thienyl, or benzo[b]thienyl are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.

Abstract: A novel process for preparing enantiomerically-pure 3-methyl-5-(1-(C.sub.1 -C.sub.3 -alkyl)-2-pyrrolidinyl)isoxazole in high yield, wherein a protected 2-oxo-pyrrolidine starting material is reacted with a suitable organic anion and a resulting beta-keto oxime intermediate is cyclized and dehydrated.

Abstract: Straight-chain alkanoic acids, substituted at the .OMEGA.-carbon atom by a substituted phenyl, naphthyl, furyl, or thienyl group and by a substituted 1,4-benzoquinon-2-yl group are effective in the therapy or prophylaxis of conditions associated with lipid peroxide injury to vascular endothelium particularly preeclampsia and eclampsia in pregnant females.

Abstract: Treatment of cotton plants or flowering ornamental plants with a formulation comprising an agent effective to inhibit 1-aminocyclopropane-1-carboxylic acid synthase activity accelerates the flowering of cotton plants and accelerates and extends flower longevity of flowering ornamental plants, particularly when such flowering plants are subjected to the stresses of the conditions of shipping.

Abstract: The present invention relates to a compound of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein W is a bicyclic heterocyclic ring system. The compounds are .alpha.-1 adrenergic antagonists and are useful in the treatment of BPH; also disclosed are .alpha.-1 antagonist compositions and a method for antagonizing .alpha.-1 receptors and treating BPH.

Abstract: Peptides possessing LHRH antagonistic activity, and useful for the controlling the release of LHRH in mammals are decapeptide analogues of LHRH having a lactam group at the N-terminus of the formula ##STR1## where n is 1, 2, or 3 and R.sup.1 is selected from the group consisting of hydrogen, benzyl, 4-chlorobenzyl, 2-methylnaphth-1-yl, 1-methylnaphth-2-yl, and quinolin-3-ylmethyl.

Abstract: Compounds of the structure ##STR1## where R.sup.1 is alkyl of one to four carbon atoms and R.sup.2 is selected from(a) alkenyl of one to four carbon atoms,(b) ##STR2## (c) ##STR3## and (d) ##STR4## are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.

Abstract: A novel process for preparing enantiomerically-pure 3-methyl-5-(1-(C.sub.1 -C.sub.3 -alkyl)-2-pyrrolidinyl)isoxazole in high yield, wherein a protected 2-oxo-pyrrolidine starting material is reacted with a suitable organic anion and a resulting beta-keto oxime intermediate is cyclized and dehydrated.

Abstract: Compounds having the structure ##STR1## or a pharmaceutically acceptable salt thereof have activity as inhibitors of cylooxygenase and 5-lipoxygenase, reduce the biosynthesis of leukotrienes B.sub.4, C.sub.4, D.sub.4, and E.sub.4 and cylooxygenase products such as prostaglandins and thromboxane and are useful in the treatment of inflammatory and allergic disease states. The compounds have the structure indicated above wherein A is selected from (a) optinally substituted carbocyclic aryl, (b) optinally substituted furyl, (c) optinally substituted benzo[b]furyl, (d) optinally substituted thienyl, (e) optinally substituted pyridyloxy, (f) optinally substituted pyridylalkyl, (g) optinally substituted benzo[b]thienyl, (h) optinally substituted pyridyl, (i) optinally substituted quinolyl, and (j) optinally substituted indolyl; X is selected from (a) optionally substituted alkyl, (b) optinally substituted alkenyl, and (c) optinally substituted alkynyl; R.sup.1 and R.sup.

Abstract: The present invention provides certain (substituted carbocyclic aryl)amidoalkyl- and (substituted heterocyclic aryl)amidoalkyl-N-Hydroxy urea compounds which inhibit lipoxygenase enzyme activity and are thus useful in the treatment of allergic and inflammatory disease states.

Abstract: The present invention relates to a compound of formulaW--X--Q--Y--CH(R.sup.1)--O--N.dbd.C(R.sup.2)--A--COMor a pharmaceutically acceptable salt thereof wherein W is optionally substituted aryl or heteroaryl; X is a valence bond, or methylene, divalent alkylene, alkenylene, alkynylene or alkyloxy; Q is a valence bond, or --O--, --S--, >NR.sup.4 or >NCOR.sup.5 ; Y is optionally substituted phenyl, biphenyl, naphthyl, tetrahydronaphthyl, indolyl, pyridyl, or benzo b!thienyl, thienyl, thiazolyl, or thiazolylphenyl; R.sup.1 is alkyl, cycloalkyl, alkoxyalkyl, aryl or arylalkyl, heteroaryl or heteroarylalkyl; R.sup.2 is hydrogen, alkyl or hydroxyalkyl; A is a valence bond or is selected from alkylene, alkenylene, alkynylene, cycloalkylene, phenylene, pyridylene, thienylene and furylene; and M is a pharmaceutically acceptable, metabolically cleavable group, --OR.sup.6, --NR.sup.6 R.sup.

Abstract: A class of cyclic peptides are effective inhibitors of LHRH and are useful in the treatment of disease conditions which are mediated by sex hormones including prostate cancer, endometriosis, uterine fibroids, and precocious puberty.

Abstract: Novel compounds useful in the preparation of enantiomerically-pure 3-methyl-5-(1-(C.sub.1 -C.sub.3 -alkyl)-2-pyrrolidinyl)isoxazole in high yield, namely 5(S)-(3-methyl-5-isoxazolyl)-2-pyrrolidinone, 3-methyl-5-(1-methyl-2-pyrrolidinyl)-5-hydroxy-4,5-dihydro-isoxazole, and 1-(1-methyl-2(S)-pyrrolidinyl)-1,3-butanedione-3-oxime.