Abstract: Isothiazolo-quinoline derivatives are described which are cytotoxic for various tumor cell lines and are useful in the treatment of neoplastic diseases.

Abstract: Compounds of the formula: ##STR1## wherein A is CH.sub.2 ; n is 0 or 1; R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, alkyl, alkenyl, aralkyl and cycloalkyl; Z is the residue from a non-steroidal anti-inflammatory carboxylic acid compound; and M is a pharmaceutically acceptable cation or a metabolically cleavable group; and the pharmaceutically acceptable salts thereof; and a non toxic pharmaceutically acceptable carrier.These compounds are useful as inhibitors of 5-lipoxygenase.

Abstract: A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 wherein R.sub.2 is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, (alpha, alpha)-dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, 1-bezyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R.sub.3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)loweralkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R.sub.4 is substituted hydroxyalkylamino.

Abstract: Substituted 8-alkoxy-1,2,3,3a,8,8a-hexahydroindeno-[1,2-c]pyrroles; 5-alkoxy-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-c]pyridines; and 9-alkoxy-2,3,3a,4,5,9a-hexahydro-1H-benz[e]isoindoles are selective 5-HT receptor agents and are thus useful in the treatment of anxiety, depression, and hypertension.

Abstract: Certain carbocyclic aryl- and heterocyclic aryl-substituted cyclopropyl N-hydroxyureas, N-hydoroxycarboxamides, and N-acyl-N-hydroxyamides inhibit 5- and/or 12-lipoxygenase and are useful in the treatment of inflammatory disease states.

Abstract: A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula: ##STR1## where A is a substituent; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 wherein R.sub.2 is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is Ch.sub.2 ; R.sub.1 is loweralkyl, cycloalkyl methyl, benzyl, (alpha, alpha)-dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, 1-bezyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R.sub.3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)loweralkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R.sub.4 is substituted hydroxyalkyamino.

Abstract: Compounds of the formulae: ##STR1## and pharmaceutically acceptable salts, esters and prodrugs thereof, wherein M and R.sub.1 are independently selected from among optionally substituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, arylalkenyl, reduced heteroaryl and reduced heteroarylalkyl groups, andZ is the residue of a compound selected from the class of compounds known as non-steroidal antiinflammatory grugs containing a carboxylic acid group, of the general form Z-COOH.

Abstract: A process for lyophilizing bulk solutions of products in which liquid product is poured into bottomless trays, frozen and dried.

Abstract: New trichothecene compositions are disclosed along with their use in methods of inhibiting nematode infection of plants.

Abstract: Compounds having 5- and 12-lipoxygenase inhibitory activity have the structure ##STR1## where A is straight or branched divalent alkylene of from one to four carbon atoms, R.sub.1 is methyl, amino, or alkylamino of from one to six carbon atoms and the substituent group R.sub.2 is C.sub.1 -C.sub.2 alkyl.The group R.sub.3 is one or more substituents selected from hydrogen, alkyl of from one to six carbon atoms, alkoxy of from one to six carbon atoms, thioalkoxy of from one to six carbon atoms, halogen, cyano, and trihalomethyl, and R.sub.4 is one or more substituents selected from hydrogen, alkyl of from one to six carbon atoms, alkoxy of from one to six carbon atoms, thioalkoxy of from one to six carbon atoms, hydroxy, halogen, cyano, and trihalomethyl, with the proviso that when R.sub.1 is amino and A is >CHCH.sub.3, R.sub.3 and R.sub.4 may not both be hydrogen.The group designated M is hydrogen, a pharmaceutically acceptable cation, or a metabolically cleavable group.

Abstract: A pharmaceutical granule comprising a core of active pharmaceutical agent and a coating of a polymer/microcrystalline cellulose is provided. These granules permit superior tableting of pharmaceutical agents whose physical properties in granule form render them unsuitable for conventional tableting.

Abstract: An improved pharmaceutical preparation uses tromethamine and dibasic potassium phosphate or calcium carbonate to enhance stability.

Abstract: Novel compounds of Formula (I): ##STR1## or pharmaceutically acceptable salts, esters and amides thereof, wherein A is O, C, CH or CH.sub.2, n is 0 or 1, and the dotted line is a single bond when A is O or CH.sub.2 and a double bond when A is CH or when n=0, A is C andR.sub.6 and A taken together form a nitrogen-containing heterocycle;R is hydrogen, lower alkyl or a readily cleavable group;R.sub.1 is selected from hydrogen, halogen, lower alkyl, haloalkyl and lower alkoxy;R.sub.2 is selected from hydrogen, halogen, lower alkyl and haloalkyl or, taken together with R.sub.8, forms a fused ring;R.sub.3 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl or arylalkyl or, taken together with R.sub.4, forms a spirocycloalkyl or, taken together with R.sub.5, forms a fused cycloalkyl;R.sub.4 is hydrogen or alkyl or, taken together with R.sub.3, forms a spirocycloalkyl;R.sub.5 is hydrogen or alkyl or, taken together with R.sub.3, forms a fused cycloalkyl;R.sub.

Abstract: This invention concerns certain diethyl- or dipropylacetic acid salts of sodium valproate which have physiological properties similar to those of valproic acid or sodium valproate but show highly superior stability characteristics.

Abstract: The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is hydrogen; loweralkyl; arylalkyl; OR.sub.8 or SR.sub.8 wherein R.sub.8 is hydrogen, loweralkyl or aminoalkyl; NR.sub.9 R.sub.10 wherein R.sub.9 and R.sub.10 are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; ##STR2## wherein B is NH, alkylamino, S, O, CH.sub.2 or CHOH and R.sub.11 is loweralkyl, cycloalkyl, aryl, arylalkyl, alkoxy, alkenyloxy, hydroxyalkoxy, dihydroxyalkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, (hydroxyalkyl)(alkyl)amino, (dihydroxyalkyl)(alkyl)amino, carboxylic acid-substituted alkyl, alkoxycarbonylalkyl, aminoalkyl, N-protected aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, (N-protected)-(alkyl)aminoalkyl, (heterocyclic)alkyl or a substituted or unsubstituted heterocyclic; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, .alpha.-methylbenzyl, .alpha., .alpha.

Abstract: A compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are substituents; R.sub.6 is hydrogen, loweralkyl, cycloalkyl, loweralkenyl, arylalkyl, (substituted aryl)alkyl, or (heterocyclic)alkyl; B is a bond, an alkylene group, an alkenylene group, an alkadienylene group or a heteroatom containing linking group; D is a substituted acyl group or tetrazolyl; Z is CO, C(S) or S(O).sub.2 ; Ar is a heterocyclic group; and n is 1 to 3.Also disclosed are a composition and a method for antagonizing CCK, a composition and method for treating or preventing gastrointestinal, central nervous, appetite regulating and pain regulating systems, a composition and method for treating or preventing hyperinsulinemia, methods of making the compounds and intermediates useful in making the compounds.

Abstract: Pyridazinone, triazinone and oxapyridazinone compounds which are useful in inhibiting lipoxygenase enzymes, particularly 5-lipoxygenase.

Abstract: Novel compounds which are selective dopamine agonists are useful for treating disorders characterized by abnormal dopamine levels, such as Parkinson's Disease, as well as cardiovascular disorders.

Abstract: Compounds of the formula: ##STR1## wherein n=1 or 2; R.sub.1 is lower alkoxy, lower alkyl, halo, ester, carbamate, or substituted amino; and R.sub.2 is thienyl or furyl; or R.sub.2 is ##STR2## wherein R.sub.3 and R.sub.4 are independently selected from hydrogen, halo, hydroxy, methoxy, thioalkoxy, substituted amino and lower alkyl; and pharmaceutically acceptable salts thereof.These compounds are useful as inhibitors of alpha-2-adrenergic receptors and for the treatment of glaucoma and/or controlling intraocular pressure.

Abstract: Compounds of the formula: ##STR1## wherein A is selected from NR.sub.1 R.sub.2 and N(OR.sub.6)R.sub.2 ; and B and C are chloro when A is N(OR.sub.6)R.sub.2 or are independently selected from NHR.sub.3 and NR.sub.4 R.sub.5 where R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are independently selected from the group consisting of alkyl, cycloalkyl and alkylaryl each of which may be unsubstituted or substituted with one or more substituents selected from the group consisting of hydroxy, OR, NRR, OCOR, OCONRR, NRCOR and NRCONRR where R is selected from the group consisting of hydrogen, alkyl, aryl, alkylaryl, alkoxy and hydroxy or R.sub.1 and R.sub.2 or R.sub.4 and R.sub.5 together can form a heteroaryl group and R.sub.6 is a member selected from the group consisting of hydrogen, alkyl, alkylaryl and trialkylsilyl; and the pharmaceutically acceptable salts thereof.These compounds are useful as inhibitors of lipoxygenase enzymes.