Abstract: A unique process for preparing certain (2R-trans)hexahydroaroquinolizines, especially (2R-trans)-N-[2-(1,3,4,6,7,12b-hexahydro-2'-oxospiro[aro-[2,3-a]-quinolizi ne-2,4'-imidazolidin]-3'-yl)ethyl)-methanesulfonamide from (2R-trans)-N-[2-[(2-cyano-(1,3,4,6,7,12b-hexahydro-aro-[2,3-a]quinolizin-2 -yl)amino]ethyl]methanesulfonamide is described.

Abstract: Pyrolysis of substituted salicylate O(N,N-dialkyl)thiocarbamates yielded the corresponding N,N-dialkyl-2-(methylthio)benzamide. Similarly, substituted 6-azasalicylate O(N,N-dialkyl)thiocarbamates yielded the corresponding N,N-dialkyl-2-(methylthio)-6-aza-benzamide.

Abstract: Novel fused polycyclic and bridged compounds are disclosed which are useful as calcium entry blockers.

Abstract: 3-Hydroxybenzo[b]thiophene-2-carboxamide derivatives have been prepared by:(1) treating a substituted 2-halobenzoate with a thioacetamide.(2) treating a substituted thiosalicylate with an appropriately substituted haloacetamide; and(3) further synthetic modification of compounds prepared above.These compounds have been found to be effective inhibitors of both cyclooxygenase and lipoxygenase and thereby useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases, cardiovascular disorders, psoriasis, inflammatory bowel disease, glaucoma or other prostaglandins and/or leukotriene mediated diseases.

Abstract: New cyclosporin analogs with modified "C-9 amino acids" have been made and are found to be effective immunosuppressive agents.

Abstract: Substituted cinnamyl-2,3-dihydrobenzofurans and analogs were prepared from the nucleophlic substitution of a cinnamylhalide with a 2,3-dihydrobenzofuran anion or an analog thereof. These compounds were found to be potent topical anti-inflammatory agents.

Abstract: Compounds having somatostatin-like activity have been found to be useful as local anti-inflammatory agents in the treatment of such conditions as, for example, psoriasis, eczema, seborrhea, and other localized inflammatory and allergic conditions. Particularly useful are cyclic and bridged somatostatin analogs.

Abstract: The addition of organolithium to dimethylhydrazones of certain ethers of a-hydroxyaldehydes results in the synthesis of threo- or erythro- intermediates readily convertible to threo- or erythro-2-amino alcohols.

Abstract: Novel substituted 4-heteroaryl-1,4-dihydropyridine compounds useful as calcium channel blockers, pharmaceutical compositions therof, and methods of treatment are disclosed.

Abstract: There are disclosed bicyclic lactams and derivatives thereof which are useful as converting enzyme inhibitors and as antihypertensives.

Abstract: The invention in its broad aspects relates to caprolactam derivatives which are useful as angiotensin converting enxyme inhibitors and as antihypertensives.

Abstract: There are disclosed novel diazapines and derivatives thereof which are useful in the treatment of cardiovascular disorders.

Abstract: Pharmaceutical compositions of specific substituted pyrimidines and methods of treatment of certain cardiovascular disorders are disclosed. Also disclosed are novel substituted acrylated pyrimidines which are useful as calcium channel blockers.

Abstract: Crystalline salts of (R,S)-pivaloyloxyethyl esters of (S)-3-(3,4-dihydroxyphenyl)-2-methylalanine and processes for their preparation are disclosed.

Abstract: Hydroxyalkyl-phenoxy-propan-2-olamines and novel esters thereof are oculoselective .beta.-blockers useful in the treatment of elevated intraocular pressure with little or no effect on the pulmonary or cardiovascular system.

Abstract: Indene derivatives have been found to have potent and specific PAF (Platelet-Activating-Factor) antagonistic activities and are thereby useful in the treatment of various diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, and adult respiratory distress syndrome.

Abstract: Novel 5-amino or substituted amino 1,2,3-triazoles are disclosed as having anticoccidial activity. The compounds are useful for controlling coccidiosis when administered in minor quantities to animals, in particular to poultry, usually in admixture with animal sustenance.

Abstract: There are disclosed novel avermectin 8,9-cyclopropyl compounds (also referred to as 8,9-dihydro-8,9-methano avermectin compounds). The 8,9-cyclopropyl compounds are prepared by treating an avermectin compound with an iodohalomethane compound in the presence of an activated form of zinc. The avermectin 8,9-cyclopropyl compounds have utility as anti-parasitic agents and compositions for that use are also disclosed. The compounds are also highly potent insecticides against agricultural pests.

Abstract: There are disclosed novel avermectin and milbemycin compounds wherein the 13-position is oxidized to a keto function. The 13-keto derivatives are prepared from the 13-hydroxy compounds by oxidizing the 13-position with a suitable oxidizing agent. The avermectin and milbemycin 13-keto derivatives are active in their own right and also serve as intermediates in the preparation of 13-imino and 13-amino derivatives. The 13-keto, imino and amino compounds have utility as anti-parasitic agents and compositions for that use are also disclosed. The compounds are also highly potent insecticides against agricultural pests.

Abstract: Hydroxybenzylamino derivatives have been prepared from an appropriate hydroxybenzaldehyde and an amine followed by reduction. These compounds are found to be active topical anti-inflammatory agents.