Abstract: Bis-(amidine phenyl)cyclohexanecarboxylic acid ketones are provided having the structure ##STR1## wherein R is hydrogen, lower alkyl or aryl and n is 0, 1 or 2, and acid-addition salts thereof. In addition, pharmaceutical compositions containing the above compounds and a method of using same to treat inflammatory conditions in mammalian species are also provided.

Abstract: A method is provided for preparing compounds of the formulae ##STR1## wherein A may be --C.dbd.C-- or --C.tbd.C--, by reducing an epoxy lactone of the structure ##STR2## to form the corresponding epoxy hemiacetal, reacting the epoxy hemiacetal with a silyl compound to form an epoxy silyl acetal, reacting the epoxy silyl acetal with an acetylenic derivative to form a silyl acetal, removing the silyl protecting group to form a hemiacetal, reacting the hemiacetal compound with an appropriate Wittig reagent to form a protected difluoro PGF.sub.2.alpha. type compound, removing the protecting group, reacting the difluoro PGF.sub.2.alpha. with an iodine compound to form an iodoether and reacting the iodoether with a base to form the desired compounds.Novel intermediates produced in the above method are also provided.

Abstract: Cultivation of a strain of the microorganism Nocardia sp. 11,340, which has been deposited in the American Type Culture Collection as A.T.C.C. No. 31531, yields a novel antibiotic substance EM 4940, having activity against a range of gram-positive and gram-negative bacteria, yeasts, fungi, acholeplasma, and the protozoan Trichomonas vaginalis.

Abstract: Compounds for alleviating or reducing angiotensin related hypertension in hypertensive mammals comprising angiotensin converting enzyme inhibitors selected from a group of mercaptoacyl aminoacids.

Abstract: Compounds having the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently hydrogen, halogen, trifluoromethyl, aminosulfonyl, nitro, alkyl or alkoxy;R.sub.3 is hydrogen, alkyl, or phenylmethyl;R.sub.4 is hydrogen, alkyl, or phenyl, and R.sub.15 is alkyl, phenyl or phenylmethyl, or R.sub.4 and R.sub.15 together are --(CH.sub.2).sub.m -- wherein m is 1 or 2;R.sub.5,R.sub.6,R.sub.7,R.sub.8,R.sub.9,R.sub.10,R.sub.11,R.sub.12,R.sub.13 and R.sub.14 are each independently hydrogen, halogen, alkyl or phenyl;n.sub.1,n.sub.2,n.sub.3,n.sub.4 and n.sub.5 are each independently 0 or 1;with the proviso that if R.sub.4 and R.sub.15 together are --(CH.sub.2).sub.m -- the sum of n.sub.1, n.sub.2, n.sub.3, n.sub.4, n.sub.5 and m is 2 or 3;have diuretic activity.

Abstract: Esters of phosphinylalkanoyl prolines and phosphinylalkanoyl substituted prolines are inhibitors of angiotensin converting enzyme and are useful in the treatment of hypertension.

Abstract: Antibacterial activity is exhibited by .beta.-lactams having a sulfate substituent in the 1-position and an acylamino substituent in the 3-position.

Abstract: Compounds are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, alkyl of 1-3 carbons, phenyl optionally substituted by R.sup.4 ; R.sup.2 is cyano; ##STR2## (wherein Z is a single bond or ##STR3## X is O or S); ##STR4## (wherein R.sup.9 is hydrogen or alkyl, Q is CH or N); ##STR5## wherein R.sup.6 is amino, alkylamino, dialkylamino, haloalkyl or ##STR6## and R.sup.4 and R.sup.5 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, alkanoyloxy, benzyloxy, substituted benzyloxy, hydroxy, halogen (Cl, Br and F), nitro and trifluoromethyl; and R.sup.7, R.sup.8, m and n are as defined hereinafter. The above compounds are useful as anti-allergy agents.

Abstract: An apparatus for holding a syringe and filling ampules is described. The apparatus is comprised of a housing having a base and a vertical support member. A syringe holder is affixed to the vertical support member in a manner which permits the syringe holder to slide up and down between two limits on the vertical support member.The apparatus operates by first lowering the syringe holder downward to place the needle of the syringe (in the holder) into an ampule, in response to the downward movement on the device's handle. Further downward movement of the handle causes material from the syringe, such as a viscous liquid, to be dispensed into the ampule.

Abstract: A method of purifying by separation of mercaptoacyl amino acid from mercaptoacyl amino acid dimer comprising,providing a first solution of impure mercaptoacyl amino acid in a fluid container means,contacting said first solution with a metal whereby said mercaptoacyl amino acid precipitates yielding a second solution and a purified mercaptoacyl amino acid precipitate,separating said purified mercaptoacyl amino acid precipitate from said second solution.

Abstract: Carbinolamine esters of 1,2,4-triazoles are provided having the structure ##STR1## wherein R, R.sup.1, R.sup.2 and R.sup.3 are as defined herein. These compounds are useful as antiinflammatory agents.

Abstract: Compounds having the formula ##STR1## wherein: R.sub.1 is hydrogen, alkyl, aryl or arylalkyl;R.sub.2 is hydrogen and R.sub.3 is hydrogen, hydroxy, alkoxy or halogen, or together R.sub.2 and R.sub.3 can be .dbd.Q or --X--(CH.sub.2).sub.t --X-- wherein X is oxygen or sulfur and t is 2 or 3;R.sub.4 is hydrogen or alkyl;R.sub.5 is hydrogen, alkyl or trifluoromethyl;R.sub.6 is alkyl of 1 to 20 carbon atoms, aryl, arylalkyl or a 5- or 6-membered heterocyclic group having 1 to 2 nitrogen, sulfur or oxygen atoms in the ring;R.sub.7 is aryl;m is 0, 1 or 2; andn is 1 or 2have useful hypotensive activity.

Abstract: This invention is directed to compounds of the formula ##STR1## which are useful in the treatment of hypertension.

Abstract: A process is provided for preparing pyrazolo[1,5-c]quinazoline derivatives of the structure ##STR1## wherein X is O or S; R.sup.1 is hydrogen, lower alkyl, hydroxymethyl, phenyl-lower alkyl, phenyl or phenyl substituted with halogen, lower alkyl, lower alkoxy, or trifluoromethyl; R.sup.2 is lower alkoxy, phenyl-lower alkoxy, phenoxy, or phenoxy substituted with lower alkyl or lower alkoxy; and R.sup.3 and R.sup.4 are the same or different and are selected from the group consisting of hydrogen, alkyl of 1 to 4 carbons, alkoxy of 1 to 4 carbons, lower alkanoyloxy of 1 to 4 carbons, nitro, benzyloxy, benzyloxy having a single mono-lower alkoxy substituent, halogen, hydroxy, and trifluoromethyl, wherein quinolone compounds of the structure ##STR2## which are new intermediates, are reacted with a hydrazine compound to form a 5-(2-aminophenyl)pyrazole which is then cyclized to the product.In addition, the above product may be reacted with a halogen acid to form the corresponding hydroxymethyl compound.

Abstract: Phenylguanidine derivatives are provided having the structure ##STR1## wherein R.sup.1 is lower alkyl, cycloalkylalkyl, or phenylalkyl; R.sup.2 is lower alkyl, phenyl or benzyl; and R.sup.3 is lower alkyl, cycloalkylalkyl, lower alkenylalkyl, dihalovinylalkyl, dihalobutadienyl or phenylalkyl; and n is 1 to 5. These compounds are useful as anthelmintic agents.

Abstract: New bendroflumethiazide formulations in solid form are provided which are characterized by excellent disintegration and dissolution capabilities even after long periods of storage. The new bendroflumethiazide formulations, for example, in the form of tablets, are formed of one or more excipients and a dry granulation containing one or more fillers, such as lactose and starch, and a preformed partial coprecipitate of bendroflumethiazide and a wetting agent therefor, such as polyvinyl pyrrolidone which converts the bendroflumethiazide into a more hydrophilic form.

Abstract: Mammalian collagenase is inhibited by compounds having the formula ##STR1## or a salt thereof, wherein R.sub.1 is hydrogen, alkanoyl of 2 to 10 carbon atoms, or arylcarbonyl; ##STR2## wherein R.sub.4 is hydrogen, alkyl or aryl; R.sub.3 is alkyl of 3 to 8 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, aryl or arylalkyl; andn is an integer of 1 to 20.

Abstract: This invention is directed to compounds of the formula ##STR1## wherein A and A.sub.1 are amino acid residues, X is an .alpha.-imino acid residue, and R.sub.1 is hydrogen, lower alkyl, or halo substituted lower alkyl. These compounds are useful as hypotensive agents.

Abstract: A method is provided for preparing the optically active isomer [2R-[2.alpha.,3.alpha.,5(R*)]]-2,2'-[[5-[3-[(1,1-dimethylethyl)amino]-2-hy droxypropoxy]-1,2,3,4-tetrahydro-2,3-naphthalenediyl]bis(oxy)]bis-[N,N-dipr opylacetamide] having the structure ##STR1## which is useful as an antiarrhythmic agent.

Abstract: Benzimidazolederivatives are provided having the structure ##STR1## wherein R.sup.1 is lower alkyl, phenyl-lower alkyl, halo-lower alkyl, mono-lower alkylaminoalkyl, di-lower alkylaminoalkyl, and alkyl pyridinium halide, R.sup.2 and R.sup.3 may be the same or different and are hydrogen or lower alkyl, R.sup.4 is cycloalkyl or cycloalkenyl, and m is 0 to 3, n is 0 to 3, m+n being .ltoreq.5. These compounds are useful as anthelmintic agents.