Abstract: A method for relaxing bronchial tissue in mammals, including humans, by use of a combination of prazosin and pirbuterol or their pharmaceutically acceptable acid addition salts.

Abstract: Laminate device for the controlled and prolonged release of at least one active agent to an ambient environment comprising at least one core sheet, said core sheet or sheets comprising said agent or agents in a polymer matrix, and, in a preferred embodiment, a porosity enhancing agent in admixture with said agent; said core sheet or sheets being alternately sandwiched or interposed between coextensive inert polymeric films substantially impermeable to said environment and to said agent or agents, said device being perforated by one or a plurality of macroholes extending through said sheets and said films. In a modification of said device the perimeter edge thereof is coated by an inert polymeric film substantially impermeable to said environment and to said agent or agents. Also included are methods for making such a device.

Abstract: N-(mono or disubstituted phenoxyalkyl)imidazoles and the pharmaceutically acceptable acid addition salts thereof are able to selectively inhibit the action of the thromboxane synthetase enzyme without significantly inhibiting the action of the prostacycline synthetase or cyclooxygenase enzymes and are thus useful in the treatment of ischaemic heart disease, stroke, transient ischaemic attack, thrombosis, migraine, and the vascular complications of diabetes.

Abstract: Bis(t-butoxycarbonyl) derivatives of phenylalanylhistidine as intermediates in the synthesis of rennin inhibiting polypeptides.

Abstract: Certain 2-substituted-2-penem-3-carboxylic acid compounds and pharmaceutically-acceptable salts thereof can be prepared from the appropriate xanthate or trithiocarbonate by desulfurization and addition of an electrophilic sulfur compound followed by halogenation and ring closure. The corresponding desulfurized and halogenated olefinic intermediates are disclosed.

Abstract: Compounds having the formula ##STR1## wherein ##STR2## R.sub.1 is hydrogen, benzyl or alkanoyl, X is C.sub.2-4 alkylene; andZ-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain and their use as CNS agents, antidiarrheals and antiemetics. Processes for their preparation and intermediates therefor are described.

Abstract: 2-Guanidino-4-(2-methyl-4-imidazolyl)thiazole and 2-(N-pentyl-N'-guanidino)-4-(2-methyl-4-imidazolyl)thiazole, histamine-H.sub.2 antagonist useful as a gastric acid antisecretory and antiulcer agents, are also useful per se in the treatment of rheumatoid arthritis.

Abstract: beta-Lactamase inhibitors which are aminoacid esters of 6-alpha- and 6-beta-(hydroxymethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof which are hydrolyzable in vivo; bis-methanediol esters thereof; or mixed methanediol esters with said beta-lactamase inhibitors and sulbactam. Pharmaceutical compositions comprising said beta-lactamase inhibitors and a conventional beta-lactam antibiotic, said compositions useful in the treatment of bacterial infections. Compounds useful as intermediates in the synthesis of said beta-lactamase inhibitors. Antibacterial mixed bis-methanediol esters of said aminoacyloxymethyl penicillanic acid 1,1-dioxides and ampicillin or amoxicillin, also useful in the treatment of bacterial infections; and intermediates therefor.

Abstract: A series of 2-guanidino-4-heteroarylthiazoles, wherein the heteroaryl substituent is selected from thiazolyl, triazolyl, imidazolyl, and 2-alkyl, 2-amino and 2-carboxamido derivatives thereof, are disclosed. The novel compounds have activity as antisecretory agents and histamine H.sub.2 antagonists and are useful for the treatment of gastric hyperacidity and peptic ulcers. Also disclosed are pharmaceutical compositions containing the novel compounds of this invention and a method of using the compounds in the treatment of gastric hyperacidity and peptic ulcers. Novel intermediates useful in the preparation of the novel antisecretory compounds are also described.

Abstract: 1,4-Dihydropyridine derivatives of the formula: ##STR1## wherein R is aryl or heteroaryl; R.sup.1 and R.sup.2 are each C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl; n is 2, 3 or 4; R.sup.3 is H, C.sub.1 -C.sub.4 alkyl, CH.sub.2 CO.sub.2 (C.sub.1 -C.sub.4 alkyl) or CH.sub.2 CN; and R.sup.4 is a group of the formula COR.sup.5, CSR.sup.5, C(.dbd.NR.sup.6)R.sup.7 or SO.sub.2 R.sup.5, wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl, NH.sub.2, NH(C.sub.1 -C.sub.4 alkyl), NH(C.sub.3 -C.sub.6 cycloalkyl), N(C.sub.1 -C.sub.4 alkyl).sub.2, NHCH.sub.2 CO.sub.2 (C.sub.1 -C.sub.4 alkyl), NHCH.sub.2 CONH.sub.2, NHCH.sub.2 CO.sub.2 H, NH(CH.sub.2).sub.2 NH.sub.2, NHNH.sub.2, NHNRCO.sub.2 (C.sub.1 -C.sub.4 alkyl), NH-aryl, NHCO-aryl or a heterocyclic, NH-heterocyclic or NHCO-heterocyclic group, or when R.sup.4 is C(.dbd.O)R.sup.5, R.sup.5 may be H or CF.sub.3 ; R.sup.6 is H, CN, CO.sub.2 (C.sub.1 -C.sub.4 alkyl), CO(C.sub.1 -C.sub.4 alkyl), SO.sub.2 (C.sub.1 -C.sub.4 alkyl), SO.sub.2 -aryl, SO.sub.2 NH.sub.2, SO.sub.2 N(C.sub.1 -C.

Abstract: 6-alpha/beta-[(C.sub.1 -C.sub.4)Alkoxyaminomethyl and benzyloxyaminomethyl]penicillanic acid 1,1-dioxides, pharmaceutically acceptable salts thereof and conventional esters thereof hydrolyzable under physiological conditions, all of which are useful in medicine as beta-lactamase inhibitors; intermediates and processes therefor; and a process for the conversion of the present compounds to 6-alpha- and 6-beta-(aminomethyl)penicillanic acid 1,1-dioxides and derivatives.

Abstract: Racemic endo- and exo-1-methoxybicyclo[2.2.2]oct-5-ene-2-carboxylic acids are starting materials for a novel and efficient synthesis of chiral 3R-[2-hydroxy-4-(1,1-dimethylheptyl)phenyl]-4R-(3-hydroxypropyl)-1R-cycloh exanol, a compound having valuable central nervous system (CNS) activity, particularly as an analgesic and as an antiemetic.

Abstract: Triazole antifungal agents of the formula: ##STR1## and their O-esters and O-ethers, where R is a phenyl group optionally substituted by 1 to 3 substituents each independently selected from halo, CF.sub.3, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy;R.sup.1 is selected from (a) ##STR2## (b) --SO.sub.2 (C.sub.1 -C.sub.4 alkyl), (C) --SO.sub.2 NR.sup.2 R.sup.3 where either R.sup.2 and R.sup.3 are both C.sub.1 -C.sub.4 alkyl, or R.sup.2 and R.sup.3 together with the N atom to which they are attached represent piperidino, (d) --NHSO.sub.2 (C.sub.1 -C.sub.4 alkyl) and (e) --CONR.sup.4 R.sup.5 where either R.sup.4 is H or C.sub.1 -C.sub.4 alkyl and R.sup.5 is C.sub.1 -C.sub.4 alkyl, or R.sup.4 and R.sup.5 together with the N atom to which they are attached represent piperidino;and n is 1 or 2 with the proviso that n is 2 when R.sup.1 is --NHSO.sub.2 (C.sub.1 -C.sub.4 alkyl);and their pharmaceutically acceptable salts. The compounds are useful as human and agricultural fungicides.

Abstract: New antibacterial agents from a neutral macrolide wherein the keto group of the beta-D-4,6-dideoxy-3-ketoallose unit is converted to the corresponding hydroxy, amino, methylamino and dimethylamino functions.

Abstract: A fungicidal agent of the formula: ##STR1## or a pharmaceutically or agriculturally acceptable salt thereof, wherein R is 5-chloropyrid-2-yl or a phenyl group optionally substituted by 1 to 3 substituents each independently selected from F, Cl, Br, I, CF.sub.3, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy;and ##STR2## where n is 0, 1, 2 or 3 and R.sup.2 is H or C.sub.1 -C.sub.4 alkyl.

Abstract: 2-(2-Amino-2-thiazolin-4-yl)acetic acid or a pharmaceutically acceptable acid addition or cationic salt thereof useful in removal of excessive levels of certain metal ions from animals, including humans, and in protection of said animals from exposure to radioactivity.

Abstract: The use of trimazosin or a pharmaceutically acceptable acid addition salt thereof as an agent for retarding the development of atherosclerosis in a mammal, especially for retarding and reducing the development of fibrous plaques associated with atherosclerosis.

Abstract: Fermentation of a culture of Nocardia sp. ATCC 39043 produces an antibiotic complex comprising erythromycin D, 3",4"-di-O-acetylerythromycin D, 3"-O-acetyl-4"-O-propionylerythromycin D and 4"-O-acetylerythromycin D. The components are separated and are each useful in vitro and in vivo as antibacterial agents. If erythromycin D is the desired product, the esters can be hydrolyzed prior to the separation of the erythromycin D.

Abstract: An improved antiinflammatory composition and method of treating inflammation which employs a combination of antiinflammatory piroxicam, or a pharmaceutically acceptable salt thereof, with analgesic acetaminophen, antidepressant doxepin, bronchodilator pirbuterol, minor tranquilizer diazepam, or antihypertensive trimazosin.

Abstract: Tricyclic benzo fused compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, wherein n is zero, 1 or 2, and t is 1 or 2; M is CH or N, R.sub.1 is H or certain acyl groups; Q is CO.sub.2 R.sub.4, COR.sub.5, C(OR.sub.7)R.sub.5 R.sub.6, CN, CONR.sub.9 R.sub.10, CH.sub.2 NR.sub.9 R.sub.10, CH.sub.2 NHCOR.sub.11, CH.sub.2 NHSO.sub.2 R.sub.12, 5-tetrazolyl or when n is 1, Q and OR.sub.1 together form a lactone or certain reduced derivatives thereof; and Z is certain alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl groups, are valuable central nervous system active agents, methods for their use, pharmaceutical compositions containing them and certain intermediates therefor.