Abstract: Certain benzocycloheptapyridine compounds with fluorine substitution across the exocyclic double bond are prepared and they are useful as antihistaminic agents.

Abstract: Tricyclic pyrrolo naphthyridinone compounds and tricyclic pyrrolo pyrido pyrazines are disclosed, which are useful as antiinflammatory and anti-hyperproliferative agents.

Abstract: Certain substituted sulfonamide quinolines and isoquinolines are disclosed having anti-allergic activity. A preferred use is for the treatment of chronic obstructive lung disease, and in particular, asthma.

Abstract: An insoluble zinc-protamine alpha interferon complex useful as an injectable sustained release dosage form for administering alpha interferon is disclosed.

Abstract: Novel phosphorous containing compounds and compositions containing said compounds inhibit the actions of enkephalinases in mammals. Methods for preparing said compounds and compositions and methods for their use to elicit analgesia and treat mental disorders are described.Useful intermediates for preparing the compounds are also described.

Abstract: Stable oleaginous gels comprising water-in-oil emulsions in gels are disclosed. Sustained release injectable pharmaceutical formulations comprising such oleaginous gels are also disclosed, in particular such formulations comprising interferon.

Abstract: Substituted 2,3-dihydro-6-substituted-pyrimido[2,1-f]purine-4,8(1H, 9H)-diones, their tautomers and salts, are disclosed for use as antihyperproliferative skin disease agents.Methods for their preparation and use are described.

Abstract: The present invention relates to ophthalmological pharmaceutical compositions comprising (benzothiadiazine, benzamide and benzenesulfonyl)phenyl-substituted carboxyalkyl dipeptide compounds and to methods for using said composition in reducing intraocular pressure, e.g., in the treatment of glaucoma.

Abstract: Compositions for the transdermal delivery of azatadine and the use of such compositions in the treatment of allergic reactions are disclosed.

Abstract: Antihistamines of the formula ##STR1## wherein ##STR2## is a 5 or 6 membered ring which is phenyl or heterocyclic ##STR3## is a six membered ring which is 2,3, or 4 pyridyl or is phenyl or substituted phenyl, with the proviso that is ##STR4## is a nitrogen containing ring ##STR5## must be phenyl; Z is an alkylene chain having 0 to 2 carbon atoms in the chain, said 2 carbon chain optionally having one double bond, said chain optionally having either a carbonyl oxygen, or a hydroxy group as a substituent; W is defined hereinbelow.

Abstract: This invention relates to a novel process for preparing 3-amino-2-methylbenzotrifluoride from benzotrifluoride. The process comprises nitrating benzotrifluoride to form 3-nitrobenzotrifluoride, reacting this compound with trimethyl sulphoxonium halide to form 3-nitro-2-methylbenzotrifluoride and reducing the nitro group to an amino group.

Abstract: A high yielding process for converting 3,2',6'-tri-N-acetyl sisomicin to netilmicin comprising the step of silylating the starting material at the 5,2' positions, and optionally at the 4' position, converting the 1-amino substituent to a 1-N-imino substituent, converting the imino to an ethylamino, deprotecting the compound and recovering netilmicin. Also disclosed are novel intermediate compounds.

Abstract: Derivatives of 6,11-dihydro-11-(4-piperidylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine, and pharmaceutically acceptable salts and solvates thereof are disclosed, which possess anti-allergic and anti-inflammatory activity. Methods for preparing and using the compounds are also described.

Abstract: A method of enhancing transdermal delivery of a pharmaceutically active drug from a transdermal delivery system as well as a transdermal delivery system capable of providing a desirable flow interface between the delivery system and the skin surface are disclosed. The method involves pre-treating an area of skin with an anticholinergic agent in an amount sufficient to have a local antisecretory effect on the area treated, such amount being insufficient to cause systemic effects; and applying the transdermal delivery system to the pre-treated area. The delivery system of the present invention is comprised of a carrier means, a pharmaceutically active drug and an anticholinergic agent. With both the method and the delivery system, the anticholinergic agent is preferably a quaternary ammonium salt which is itself transdermally delivered to the area beneath the delivery system in an amount sufficient to suppress perspiration in that area.

Abstract: The present invention relates to carboxyalkyl dipeptides which are inhibitors of angiotensin-converting enzyme and are useful as antihypertensive agents and in the treatment of congestive heart failure.The compounds of the present invention are compounds of the formulae ##STR1## and the pharmaceutically acceptable salts thereof, wherein R and R.sup.6 are the same or different and are hydroxy or lower alkoxy;R.sup.1 is benzyloxylower alkyl or benzylthiolower alkyl;R.sup.2 is benzylthiomethyl, 2-phyenylethylthiomethyl, napthylmethylthiomethyl, methylbenzylthiomethyl, 2-(carboxyphenyl)ethyl or 2-(alkoxycarbonylphenyl)ethyl) andR.sup.3 is hydrogen, lower alkyl or aminolower alkyl.

Abstract: A method of inducing anorexia or nasal decongestion comprising transdermally administering an enantiomer of phenylpropanolamine is disclosed.

Abstract: Substituted 2,3-dihydro-6-substituted-pyrimido[2,1-f]purine-4,8(1H,9H)-diones, their tautomers and salts, are disclosed for use as antihyperproliferative skin disease agents.Methods for their preparation and use are described.

Abstract: Novel polycyclic quinoline, naphthyridine and pyrazinopyridine derivatives are disclosed which are useful for treating allergic reactions, inflammation, peptic ulcers, hypertension, and hyperproliferative skin diseases and for suppressing the immune response in mammals. Methods for preparing said compounds are also disclosed.

Abstract: The present invention relates to carboxyalkyl dipeptides which are inhibitors of angiotensin-converting enzyme and are useful as antihypertensive agents and in the treatment of congestive heart failure.The compounds of the present invention are compounds of the formulae ##STR1## and the pharmaceutically acceptable salts thereof, wherein R and R.sup.6 are the same or different and are hydroxy or lower alkoxy;R.sup.1 is benzyloxylower alkyl or benzylthiolower alkyl;R.sup.2 is benzylthiomethyl, 2-phenylethylthiomethyl, naphthylmethylthiomethyl, methylbenzylthiomethyl; 2-(carboxyphenyl)ethyl or 2-(alkoxycarbonylphenyl)ethyl; andR.sup.3 is hydrogen, lower alkyl or aminolower alkyl.

Abstract: Derivatives of 6,11-dihydro-11-(4-piperidylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine, and pharmaceutically acceptable salts and solvates thereof are disclosed, which possess anti-allergic activity, making them effective as anti-allergic compounds. Methods for preparing and using the compounds are also described.