Abstract: The compounds of the following structural formula (I) ##STR1## are 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) synthase inhibitors and useful as antihypercholesterolemic agents for the treatmet of disease in which the inhibition of cholesterol biosynthesis would be useful, such as arteriosclerosis, hyperlipidemia and familial hypercholesterolemia.

Abstract: There are disclosed derivatives of avermectin compounds with a .DELTA.26,27-alkyl chain of 4, 5 or 6 members at the 25-position. The compounds are prepared from the known .DELTA.26,27-compounds by the appropriate synthetic procedures at the 5-, 8-, 9-, 13- , 22- and 23-positions. The compounds are potent antiparasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.

Abstract: Thieno[2,3-b]thiophene-2-sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and glaucoma.

Abstract: Certain amino-2-hydroxypropyloximinoheterocycles are .beta.-adrenoceptor antagonists useful in the treatment of elevated intraocular pressure, hypertension, angina and arrhythmia.

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: Thieno[2,3-b]furan-2-sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and glaucoma.

Abstract: Process and compositions for lowering blood pressure in diabetic by employing a cyclopeptide compound is described.

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

Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.

Abstract: A multilaminate transdermal drug delivery system containing only dissolved drug in the drug reservoir is described. The delivery system comprises a backing layer, a reservoir layer and a membrane layer, wherein the drug in the reservoir is completely dissolved and the control of delivery is effected by the joint action of reservoir and membrane.

Abstract: .beta.-Lactam derivatives and analogs are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.

Abstract: A device is disclosed for the controlled delivery of a beneficial agent. The agent is delivered to the environment surrounding the device at a substantially constant rate for a specified period with a reduced dependence on the environmental pH. The device is comprised of a core compartment containing (1) a charged, water insoluble, non-diffusible component and (2) at least one diffusable water soluble ionizable beneficial agent. The core is surrounded by a water insoluble wall containing leachable pore forming additive(s) dispersed throughout said wall, with said wall impermeable to core components (1) and permeable to beneficial agent(s) (2). In operation the insoluble charged component (often polymeric resins) and water soluble ionizable beneficial agent have the same electro-static charge and do not form an ion exchange complex.

Abstract: There is disclosed a series of macrolides isolated from the fermentation broth of a microorganism identified as MA-5920. This novel microorganism is formed by the protoplast fusion of strains of Streptomyces avermitilis and Streptomyces hygroscopicus. The structure of the novel compounds isolated from the microorganism is presented based upon analytical studies. The compounds are highly potent antiparasitic, insecticidal, and anthelmintic agents. Compositions for such uses are also disclosed.

Abstract: Novel 2-sulfamoylbenzo[b]thiopenes and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in compositions including ophthalmic drops and inserts.

Abstract: Novel cyclized N-substituted tetrahydropyridine compounds are disclosed. The compounds have the property of inhibiting calcium induced contraction of the smooth muscle and are adaptable to being employed in the chemotherapeutic treatment of cardiovascular diseases.

Abstract: The 1-aryloxy-3-(substituted alkylamino)-2-propanols of this invention and their pharmaceutically acceptable salts exhibit cardioselective .beta.-adrenergic blocking activity, and are useful as antihypertensive, cardioprotective, antiarrhythmic and, antianginal agents.

Abstract: Certain fungistats when employed in combination have been found to exhibit synergistic antifungal properties and further exhibit fungicidal properties.

Abstract: N-Alkenyl-2-hydroxybenzo[b]thiophene-3-carboxamide derivatives are prepared via treatment of the corresponding unsubstituted carboxamide with appropriate agents, such as aldehydes, ketones, enol ethers, epoxides, acetals or ketals.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: A process for the preparation of 1,4-dihydropyridine compounds, especially N-substituted 1,4-dihydropyridine compounds, is disclosed. The compounds are useful as cardiovascular agents and also as starting materials for the preparation of certain cyclized compounds which have properties as calcium entry blockers.

Abstract: The invention relates to the use of carboxylic acids incorporated as a catalyst in poly(orthoester)s and other acid labile polymers such that upon exposure to aqueous environments the acid catalyzes the erosion of the polymer matrix. The rate of release of a drug substance incorporated into or surrounded by the poly(orthoester) or other acid labile polymer can be controlled in that the drug is released as the polymer is eroded in response to the catalytic action of the acid incorporated therein.