Abstract: Hypotensive activity is exhibited by new phosphonate substituted amino or imino acids of the formula ##STR1## isomeric mixtures thereof and pharmaceutically acceptable salts thereof, wherein:X is an imino or amino acid of the formula ##STR2##

Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts and tautomeric mixtures thereof possess activity as HMg-CoA reductase inhibitors, thus making them useful as antihypercholesterolemic agents. In the above formula,Z is ##STR2## R.sup.1 and R.sup.2 are each independently fluoro or hydrogen, except that at least one of R.sup.1 and R.sup.2 is fluoro;R.sup.3 is hydrogen, alkyl, cycloalkyl, aryl or arylalkyl; andR.sup.4 is hydrogen, alkyl, ammonium, alkylammonium, or alkali metal.

Abstract: Disclosed herein is a process for preparing a novel monoester of the formula ##STR1## in which the associated novel diester ##STR2## is hydrolyzed in the presence of one or more water-soluble enzymes or microorganisms capable of selectively hydrolyzing the --O--C(O)--R.sup.1 group, wherein the treatment is carried out in a biphasic solvent system comprising an aqueous phase having the enzymes or microorganisms and an organic phase immiscible in water having the diester. Also disclosed is a process for preparing [1S-[1.alpha., 2.alpha.(Z),3.alpha.,4.alpha.]]-7-[3[[[[(1-oxoheptyl)amino]acetyl]-amino]m ethyl-7-oxabicyclo-[2.2.1]hept-2-yl]-5-heptenoic acid using this enzymatic/microbial process.

Abstract: Disclosed herein is a novel process in which novel aldehydes ##STR1## and the trans isomer thereof are hydrolyzed by treatment with an alkali metal carbonate, bicarbonate or hydroxide and water to form the cis enantiomer ##STR2## Also disclosed is a process for preparing [1S-[1.alpha., 2.alpha.(Z), 3.alpha., 4.alpha.]]-7-[3[[[[(1-oxoheptyl)amino]acetyl]-amino ]methyl-7-oxabicyclo-[2.2.1]hept-2-yl]-5-heptenoic acid using the above process.

Abstract: A process is described in which a lactone ##STR1## is reacted with an alkylester X.sup.1 --CH.sub.

Abstract: Antihypercholesterolemic activity has been discovered in compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein: Z is ##STR2## X is lower alkyl, lower alkenyl, or lower alkenyl; R.sup.1 is hydrogen, alkyl, alkenyl, aryl, alkylaryl, or substituted aryl having one or more substituents; andone of R.sup.2 and R.sup.3 is hydrogen and the other is hydrogen, alkyl, alkenyl, aryl, alkylaryl or alkenyl aryl; or R.sup.2 and R.sup.3 are both lower alkyl; or R.sup.2 and R.sup.3 together complete a substituted or unsubstituted hydrocarbon ring that is cycloalkyl or cycloalkenyl with substituents as defined in the specification.

Abstract: Antihypercholesterolemic activity is exhibited by novel compounds of the formula ##STR1## wherein: Z is ##STR2## X is lower alkyl or lower alenyl; R.sup.1 is aryl or alkyl;R.sup.2 and R.sup.3 are the same or different and are hydrogen, or lower alkyl or aryl, or R.sup.2 and R.sup.3 taken together to form a cycloalkyl group; andR.sup.4 is hydrogen, lower alkyl, or alkali metal (such as sodium, lithium, or potassium) or a radical such as ammonium.Methods of use and novel intermediates of these compounds are also provided.

Abstract: A process is disclosed for direct isolation of captopril from a substrate of the formula ##STR1## wherein R is lower alkyl or lower alkoxy. In this process, the substrate is first treated with an aqueous alkali metal hydroxide capable of forming a water-soluble salt of the substrate, wherein the alkali metal hydroxide has a concentration of 4M or greater. The substrate is then neutralized, preferably with a mineral acid. By this process, captopril may be directly crystallized from an aqueous solution, avoiding the prior art use of organic solvents and zinc treatment to reduce levels of sulfide and disulfide impurities, respectively. In an alternative embodiment, neutralization is carried out by use of a hydrogen-supplying ion exchange resin.

Abstract: Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, has been found in compounds of the formula ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected from:(1) alkyl,(2) substituted alkyl in which one or more substituents are selected from(a) halogen,(b) hydroxyl,(c) alkoxy,(d) alkoxycarbonyl,(e) acyloxy,(f) cycloalkyl,(g) phenyl,(h) substituted phenyl in which one or more substituents are X or Y,(i) alkyl-S(O).sub.n,(j) cycloalkyl-S(O).sub.n,(k) phenyl-S(O).sub.n,(l) substituted phenyl-S(O).sub.n in which one or more substituents are X or Y, and(m) oxo,(3) alkoxy,(4) alkenyl,(5) cycloalkyl,(6) substituted cycloalkyl in which one or more substituents are selected from(a) alkyl,(b) substituted alkyl in which one or more substituents are selected from(i) halogen,(ii) hydroxy,(iii) alkoxy,(iv) alkoxycarbonyl(v) acyloxy(vi) phenyl(vii) substituted phenyl in which one or more substituents are X and Y,(viii) alkyl-S(O).sub.n,(ix) cycloalkyl-S(O).sub.

Abstract: Novel thromboxane receptor antagonists are disclosed, having the formula ##STR1## wherein: A is aryl, optionally substituted withhalogen,lower alkoxy,carboalkoxy,lower alkyl,alkylamino, orphenyl;X is --CH.sub.2 or --NH;R.sub.1 is COOH, COO-alkali metal (such as Na, K, or Li), COO-lower alkyl, CONHSO.sub.2 R.sub.2, or 5-tetrazolyl;R.sub.2 is lower alkyl or aryl;m is 0, 1, or 2; andp is 2, 3, 4 or 5.Also disclosed are novel intermediates of formula I compounds.

Abstract: A process has now been discovered by which an intermediate in preparation of antibiotics ##STR1## may be directly derived from the substrate ##STR2## by treatment with aqueous solutions of MHCO.sub.3 and MOH, wherein: R.sup.1, R.sup.2 and R.sup.3 are each independently alkyl, alkenyl, alkynyl, substituted alkyl, substituted alkenyl, substituted alkynyl, aryl, or substituted aryl;M is alkali metal (such as Na, Li, or K); andX is halogen.

Abstract: This process enables preparation of the preferred (+)-threo enantiomer by resolution of its racemic mixture of a compound of the formula ##STR1## wherein Y.sup.1 and Y.sup.2 are each independently lower alkyl and R.sup.1 is hydrogen or lower alkyl. The compound is treated with a chiral acid (tartaric aicd preferred) in an organic solvent (ethanol preferred) to yield the (+)-threo enantiomer, which is then recovered from the reaction mixture. This enantiomer may then be used to produce the preferred (+)-cis enantiomer of certain benzothiazepine cardiovascular agents.

Abstract: Vasodilating activity is exhibited by compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein X is --CH.sub.2 -- or --S--;R.sub.1 is ##STR2## or --O--Y.sub.3 ; R.sub.2 is heterocyclo or heteroaryl;R.sub.3 and R.sub.4 are each independently hydrogen, halogen, alkyl, alkoxy, aryloxy, arylalkoxy, arylalkyl, cyano, hydroxy, alkanoyloxy, ##STR3## fluoro-substituted alkoxy, fluoro-substituted alkyl, (cycloalkyl)alkoxy, --NO.sub.2, --NY.sub.10 Y.sub.11, --S(O).sub.k alkyl, --S(O).sub.k aryl ##STR4## n is 0, 1, 2 or 3; m is 0, 1, 2 or 3;k is 0, 1 or 2;Y.sub.1 and Y.sub.2 are each independently hydrogen or alkyl; or Y.sub.1 is hydrogen and Y.sub.2 is alkenyl, alkynyl, aryl, heteroaryl, or cycloalkyl; or Y.sub.1 and Y.sub.2, together with the carbon atom to which they are attached, are cycloalkyl;Y.sub.3 is hydrogen, alkyl, alkanoyl, alkenyl, arylcarbonyl, heteroarylcarbonyl, or ##STR5## Y.sub.8 and Y.sub.9 are each independently hydrogen, alkyl, aryl, or heteroaryl; or Y.sub.

Abstract: The crystalline anhydrous form of [3S-[3.alpha.(Z), 4.beta.]]-3-[[(2-amino-4-thiazolyl) [(1-carboxy-1-methylethoxy)imino]acetyl]amino]-4-methyl-2-oxo-1-azetidines ulfonic acid is prepared.

Abstract: A process is provided for inverting a hydroxy function of a L-trans-hydroxy proline derivative to the corresponding L-cis-hydroxy proline sulfonate by a Modified Mitsunobu reaction process.

Abstract: 4-Diazo-3-methoxy-2,5-cyclohexandien-1-one, and pharmaceutically acceptable salts thereof, are antibiotics having antibacterial activity against a variety of gram positive and gram negative bacteria, particularly against anaerobic bacteria. The compound can be prepared by culturing aerobically Penicillium funiculosum A.T.C.C. No. 20783 in a culture medium containing assimilable sources of carbohydrates and nitrogen.

Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.4 is aryl are disclosed. These novel compounds are useful, for example, as cardiovascular agents.

Abstract: Zofenopril, and pharmaceutically acceptable salts thereof, can be used for the treatment of rheumatoid arthritis.

Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is oxygen or sulfur;R is hydrogen, alkyl, cycloalkyl, aryl, or arylalkyl and R.sub.1 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, ##STR2## or halo substituted alkyl, or R and R.sub.1 taken together with the nitrogen atom to which they are attached are 1-pyrrolidinyl, 1-piperidinyl, 1-azepinyl, 4-morpholinyl, 4-thiamorpholinyl, 1-piperazinyl, 4-alkyl-1-piperazinyl, 4-arylalkyl-1-piperazinyl, 4-diarylalkyl-1-piperazinyl or 1-pyrrolidinyl, 1-piperidinyl, or 1-azeipinyl substituted with alkyl, alkoxy, alkylthio, halo, trifluoromethyl or hydroxy;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, ##STR3## or halo substituted alkyl; R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, ##STR4## or halo substituted alkyl; R.sub.4 is aryl or heterocyclo;R.sub.5 and R.sub.6 are each independently hydrogen, alkyl, --(CH.sub.2).sub.q --aryl or --(CH.sub.2).sub.