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: 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: 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: A series of novel derivatives of penicillanic acid 1,1-dioxide, having a disubstituted methyl group of the formula X--CH--Y at the 6-position, and the pharmaceutically-acceptable salts thereof and the pharmaceutically-acceptable esters thereof readily hydrolyzable in vivo, wherein X is hydroxy, acylated hydroxy or amino and Y is carboxy or esterified carboxy. The compounds of the invention are inhibitors of bacterial beta-lactamases, and they will protect certain beta-lactamase-susceptible beta-lactam antibiotics, e.g. ampicillin, against inactivation by beta-lactamases. Co-administration of a compound of the invention with a beta-lactam antibiotic such as ampicillin to a mammalian subject increases the effectiveness of the beta-lactam antibiotic against infections caused by beta-lactamase-producing bacteria.

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: A femoral hip prosthesis comprises a stem component generally divided into a proximal portion and a substantially longer distal portion. The stem has a slight posterior bow along its length. The proximal portion includes a slight twist of from about 5.degree. to 15.degree., the twist extending in a direction from the anterior to the posterior face of the stem through the medial face thereof. The characteristics of the stem provide a glove fit when inserted into a prepared intermedullary canal in the femur.

Abstract: A novel series of carboxy-substituted naphthalenes and carboxy-substituted benzo-fused heterocycles, such as carboxy-substituted derivatives of indole, benzofuran and benzothiophene, has been prepared, including their pharmaceutically acceptable salts. These particular compounds are useful in therapy for the treatment of thrombosis, ischaemic heart disease, stroke, transient ischaemic attack, migraine, peripheral vascular disease, the vascular complications of diabetes and endotoxic shock. Preferred member compounds include 2-(1-imidazolylmethyl)-3-methylbenzo[b]thiophene-5-carboxylic acid and 3-methyl-2-(3-pyridylmethyl)benzo[b]thiophene-5-carboxylic acid, respectively. Methods for preparing these compounds from known starting materials are provided.

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: 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: 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: 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 series of novel antibacterially active derivatives of indolmycin as well as some prodrug forms of indolmycin is disclosed. A novel process for the production of these compounds is also disclosed.

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: A rasp handle has an elongate body portion with a pistol-type grip extending therefrom and rasp retaining structure at its front end. Such structure includes a fixed jaw and a slide jaw constructed and arranged for sliding movement relative to the fixed jaw between a forward closed locking position where a rasp is locked between the jaws and a rearward open rasp receiving and releasing position. A lever is connected to shift the slide jaw between its closed and open positions. A pivot interconnects the lever and the slide jaw so that the lever is free to move between a locked position adjacent the body portion and an unlocked jaw manipulating position away from the body portion.

Abstract: Herbicidal compositions containing salinomycin for the control of weeds are disclosed.

Abstract: A novel crystalline form of the monoethanolamine salt of N-(2-pyridyl)-2-methyl-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide has been prepared. This novel crystalline form is designated as polymorph I and is useful in therapy as a non-steroidal anti-arthritic agent. Methods for preparing this polymorph from readily available materials are provided.

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.