Abstract: Amidine compounds of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsin, anti-plasmin, anti-kallikrein and anti-thrombin agents. They are also useful as a powerful anti-complement agent.

Abstract: Amino acid ester hydrohalide is produced by reacting amino acid, alcohol, and halocarbonyl compound represented by the formula: ##STR1## in the presence of an excess of the alcohol and under substantially anhydrous conditions, wherein X.sub.1 and X.sub.2 are each independently fluoro, chloro, bromo, trichloromethoxy or tribromomethoxy.

Abstract: The invention provides a compound of the formula (I): ##STR1## or a salt, ester or amide thereof; wherein R.sub.1 is hydrogen or C.sub.1-4 alkyl and R.sub.2 is C.sub.1-4 alkyl substituted by a group R.sub.3 CO.sub.2 H or R.sub.1 and R.sub.2 taken together with the nitrogen comprise a nitrogen-containing heterocyclic ring having four to six ring members substituted by a group R.sub.3 CO.sub.2 H, wherein R.sub.3 is a C.sub.1-7 aliphatic hydrocarbon group or a single bond;R.sub.4 is hydrogen, halogen, hydroxy, cyano, C.sub.1-4 acyloxy, C.sub.1-4 alkoxy or C.sub.1-4 alkyl optionally substituted by one to three halogen atoms;X is --N.dbd. or --CH.dbd.; andA and B each represent hydrogen atoms or --CA--CB-- represents --C.dbd.C--.The invention also provides a method for the preparation of compounds of the formula (I), novel chemical intermediates in their preparation and pharmaceutical formulations. Compounds of the formula (I) have antihistaminic activity.

Abstract: Novel 3-hydroxy-4-alkyloxphenyl heterocyclic aromatic carboxylate compounds particularly well suited as sweeteners in foodstuff.

Abstract: Compounds of the formula: ##STR1## wherein R.sup.2 is --(CH.sub.2).sub.k --X--(CH.sub.2).sub.j --NHR.sup.3 ; wherein k is 0 to 3, j is 1 or 2; X is F or OH; and, R.sup.3 is hydrogen; loweralkyl or loweraralkyl which may be substituted by hydroxy, carboxy, carbamoyl, or carbalkoxy; or, acyl; and, a pharmaceutically acceptable salt thereof; are inhibitors of angiotensin I converting enzyme useful as antihypertensive agents.

Abstract: 4-Substituted proline derivatives having the formula ##STR1## can be prepared by reacting the compound having the formula ##STR2## with a compound having the formula ##STR3## to obtain a compound having the formula ##STR4## (a novel intermediate), alkylating that compound to obtain a compound having the formula ##STR5## (a novel intermediate), converting that compound to a compound having the formula ##STR6## (a novel intermediate), and oxidizing that compound to yield the desired proline having the formula ##STR7## wherein R.sub.1 is alkyl, cycloalkyl, aryl or arylalkyl, R.sub.1 ' is alkyl, cycloalkenyl, aryl or arylalkyl, R.sub.2 is alkyl, aryl, arylalkyl or cycloalkyl and R.sub.3 is hydrogen, alkyl, aryl, arylalkyl or cycloalkyl.

Abstract: The present invention provides a process for the preparation of aryl carboxylic acids by the carbonylation of diaryliodonium salts. The diaryliodonium salts are reacted with carbon monoxide in the presence of a zero-valent palladium in a hydrocarbon acid reaction medium to prepare the aromatic carboxylic acids.

Abstract: This invention relates to a process for the preparation of free L .alpha.-amino acids by the complete conversion of their D antipodes taken individually or possibly in racemic mixtures.The process according to the present invention is characterized in that the D antipodes of an ester of said .alpha.-amino acid is racemized in the presence of a chemical catalyst formed by at least one aromatic aldehyde corresponding to the general formula: ##STR1## wherein: Ar represents an aromatic ring optionally containing a heteroatom, such as nitrogen, andB represents a basic function,to produce a mixture in dynamic equilibrium of the two forms D and L of said ester, the ester which is present in the L form is hydrolyzed enzymatically and irreversibly to produce the corresponding stereostable L .alpha.-amino acid, said stages of chemical racemization and of enzymatic hydrolysis being carried out under identical reaction conditions, and the free L .alpha.-amino acid is recovered.

Abstract: Substituted phenylalkenoic acids and esters of the formula: ##STR1## having useful pharmaceutical activity are disclosed.

Abstract: Substituted phenylalkenoic acids and esters of the formula: ##STR1## having useful pharmaceutical activity are disclosed.

Abstract: Certain pyrrolecarboxylic and pyrroleacetic acid derivatives substituted on the pyrrole ring with thioether groups, acyl groups, phenyl, substituted phenyl, phenoxy, substituted phenoxy, benzyl or halo and optionally substituted on the pyrrole nitrogen with alkyl, and the pharmaceutically acceptable salts thereof, are useful in lowering the blood glucose levels of hyperglycemic animals.

Abstract: Certain pyrrolecarboxylic and pyrroleacetic acid derivatives substituted on the pyrrole ring with thioether groups, acyl groups, phenyl, substituted phenyl, phenoxy, substituted phenoxy, benzyl or halo and optionally substituted on the pyrrole nitrogen with alkyl, and the pharmaceutically acceptable salts thereof, are useful in lowering the blood glucose levels of hyperglycemic animals.

Abstract: A method is provided for making substituted prolines of the structure ##STR1## wherein X is lower alkyl or aryl, R is H, lower alkyl or an alkali metal and Z is an N-protecting group, which method includes the step of reacting a compound of the structure ##STR2## wherein Z and R are as defined above and Q is Br. tosyloxy or mesylate, with an organic copper lithium compound of the structureXYCuLiwherein X is as defined above and Y is lower alkyl, aryl or CN.Where X is phenyl, the corresponding 4-cyclohexyl compound may be produced by conventional hydrogenation techniques.The compounds produced are useful as intermediates in the preparation of phosphinic acid derivatives useful in the treatment of hypertension.

Abstract: Compounds of the formula ##STR1## are useful as intermediates in the preparation of various hypotensive agents.

Abstract: The (5-R-2-oxo-1,3-dioxolen-4-yl)methyl moiety: ##STR1## wherein R is loweralkyl of 1-6 carbon atoms, especially methyl or t-butyl; when utilized as an ester on a pharmaceutical having a carboxylic acid functionality, enhances oral absorption of the pharmaceutical. This effect is applicable to a broad range of pharmaceutically active substances, including antibiotics, and antihypertensives as well as other classes of therapeutic agents.

Abstract: The invention is directed to optically active proline derivative of the general formula: ##STR1## in which X is a hydrogen atom or a hydroxyl group and R is a hydrogen atom, an unsubstituted or alkyl group substituted phenyl group or a straight chain or branched alkyl group having 1 to 20 carbon atoms and a process for its production by reacting an enantiomerically pure proline or 4-hydroxy-proline as a solution in an alkanol having 1 to 4 carbon atoms with 0.9 to 2 times the molar amount of an alkali metal alcoholate corresponding to the alkanol and 1 to 3 times the molar amount of an epoxide of the general formula ##STR2## in which R is as defined above. The optically active proline derivative of general formula (I) can be used in the form of metal ion chelate complexes as the chiral stationary phase in the separation of enantiomers by means of liquid chromatography.

Abstract: Compounds of the formula ##STR1## are useful as intermediates in the preparation of various hypotensive agents.

Abstract: Tetra- and hexa-hydropyrrolo[1,2-a]quinoxaline and azaquinoxaline derivatives of the formula: ##STR1## in which X is O or H.sub.2 ;Y is CH or N;R is hydrogen, alkyl, dialkylaminoalkyl, arylalkyl, phenoxyalkyl, benzoyl, pyridylalkyl or variations thereof; andR.sup.1 is hydrogen, alkyl, alkoxy, nitro, halo, trifluoromethyl, amino, alkylamino or dialkylamino;or pharmaceutically acceptable salts thereof; are anti-hypertensive agents.

Abstract: Chiral Schiff bases according to the general formula: ##STR1## and transition metal complexes thereof, wherein C.sup.* is an asymmetric carbon atom, R.sup.1 and R.sup.2, which may be the same or different are alkyl, aralkyl, aryl or alkaryl, R.sup.3 is hydrogen, alkyl, aralkyl, aryl or alkaryl, R.sup.4 and R.sup.5, which may be the same or different, are hydrogen or lower alkyl or, where n is 1, may with the cyclic ring to which CR.sup.4 R.sup.

Abstract: This disclosure described novel (monosubstituted-amino)heteroaryl carboxylic acids and analogs which are useful as hypolipidemic and antiatherosclerotic agents.

Abstract: This invention relates to a method of using compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, alkyl or alkenyl; R.sup.2 is hydrogen, alkyl, cycloalkyl or mononuclear aryl or R.sup.1 and R.sup.2, taken together with the carbon atom to which they are attached, form a cycloalkyl or cycloalkoxyalkyl; R.sup.3 is hydroxy, alkyl, alkoxycarbonyl, hydroxy lower alkyl or a radical of the formula: --C(.dbd.Y)NR.sup.4 R.sup.5 wherein R.sup.4 is hydrogen, alkyl, alkenyl, R.sup.5 is alkyl, alkenyl, alkoxyalkyl, carbalkoxy, mononuclear aryl, or R.sup.4 and R.sup.5 may be joined together with the nitrogen atom to which they are attached to form a 5 to 7 membered heterocyclic ring having from 1 to 3 hetero atoms; Y is O or S; X is alkyl, alkoxycarbonylalkyl or cyano; m is an integer of 0 to 2 and n and n' are integers each having a value of 1 to 2 and the dotted line indicates an optional double bond anywhere in the ring, compositions containing said compounds as insect repellents and to novel compounds.

Abstract: A compound of formula (II) or a pharmaceutically acceptable acid addition salt thereof ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and each represents C.sub.1-6 alkyl; R.sup.5 represents hydrogen or C.sub.1-6 alkyl; R.sup.6 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl, and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or R.sup.5 and R.sup.6 together represent the remaining members of a 5- or 6-membered ring optionally containing an oxygen, sulphur or additional nitrogen atom and being optionally substituted with C.sub.1-6 alkyl, carboxy or C.sub.1-6 alkoxycarbonyl; and R.sup.7 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.