Abstract: Heterobiaryl derivatives of the formulaR.sub.1 NH--X.sub.1 --X.sub.2 --X.sub.3 --Y.sub.1 --Y.sub.2 --Y.sub.3 --Y.sub.4 --E (I)whereinR.sub.1, X.sub.1 to X.sub.3 and Y.sub.1 to Y.sub.4 are as defined herein, the tautomers, stereoisomers and mixtures thereof, and the salts, particularly the physiologically acceptable salts, thereof with organic or inorganic acids or bases. The derivatives have valuable pharmacological properties, such as inhibiting cell-cell aggregation and cell-matrix interactions.

Abstract: Disclosed herein are compounds of the formula:A'--N(R.sup.1')c(O)CH.sub.2 CHR.sup.2 C(O)--Bwherein A' is HO--CR.sup.5 (R.sup.6)CH.sub.2 wherein R.sup.5 and R.sup.6 together with the carbon atom to which they are attached form a 1,1-(lower cycloalkanediyl); R.sup.1' is R.sup.7 R.sup.8 NC(O)CH.sub.2 wherein R.sup.7 hydrogen or lower alkyl and R.sup.8 is lower alkyl; R.sup.2 is, for example, 4-thiazolylmethyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state mimic, for example, [1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl]amino. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.

Abstract: Various substituted benzoxazoles and benzothiazoles, are described and disclosed, which are potent inhibitors of leukotriene synthesis in warm-blooded animals.

Abstract: Disclosed herein is a combination of an antiviral nucleoside analog and a ribonucleotide reductase inhibiting peptide derivative. The combination is useful for combatting herpes infections.

Abstract: Disclosed herein are compounds which inhibit human immunodeficiency virus (HIV) protease activity and inhibit HIV replication in human cells. Thus, the compounds are indicated for the treatment of HIV infections. The compounds can be represented by the formula ##STR1## wherein X is a terminal group, for example, an aryloxycarbonyl, an alkanoyl or an arylalkyl carbamoyl; A is absent or an amino acid or a derived amino acid; either R.sup.1 or R.sup.2 is hydrogen while the other is alkyl or R.sup.1 and R.sup.2 are joined to form a cyclohexane; Q is hydrogen, hydroxy, halo or lower alkoxy; and Y is a terminal group, for example, an alkylamino, alkoxy or an optionally substituted anilino.

Abstract: Disclosed herein are compounds of the formula:A--N(R.sup.1)C(O)CH.sub.2 CHR.sup.2 C(O)--Bwherein A is R.sup.3 R.sup.4 NC(O)CH.sub.2 wherein, for example, R.sup.3 is hydrogen or alkyl and R.sup.4 is hydrogen, alkyl or a substituted alkyl such as 2-(2-pyridinyl)ethyl, or R.sup.3 and R.sup.4 together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino, morpholino or thiomorpholino; R.sup.1 is, for example, benzyl, alkyl or a substituted alkyl such as cyclohexylmethyl; R.sup.2 is, for example, alkyl, cycloalkylmethyl, 1H-imidazol-4-ylmethyl, 4-thiazolylmethyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state analog, for example, [1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl]amino. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.

Abstract: The present invention relates to a new process for preparing enantiomerically pure diarylprolinols, especially (R)-(+)- or (S)-(-)-2-(diphenylhydroxymethyl)-pyrrolidine (R)-(+)- or (S)-(-)-.alpha.,.alpha.-diphenyl-(2-pyrrolidinyl)-methanol) starting from proline.

Abstract: Disclosed herein are compounds of the formula:A--N(R.sup.1)C(O)CH.sub.2 CHR.sup.2 C(O)--Bwherein A is various oxygen-bearing radicals; for example, HO--CH(R.sup.3)CH.sub.2 wherein R.sup.3 is, inter alia, hydrogen, lower alkyl, lower cycloalkyl or phenyl; or HO--CR.sup.5 (R.sup.6)CH.sub.2 wherein each of R.sup.5 and R.sup.6 is lower alkyl, or R.sup.5 and R.sup.6 together with the carbon atom to which they are attached form a 1,1-(lower cycloalkanediyl); R.sup.1 is, for example, benzyl, alkyl or a substituted alkyl such as cyclohexylmethyl; R.sup.2 is, for example, cyclo-alkylmethyl, 1H-imidazol-4-ylmethyl, 4-thiazolylmethyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state mimic, for example, [1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl]amino. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.

Abstract: A phenylalkyl derivative of the formula ##STR1## wherein R.sub.a to R.sub.f, A and B are substituents and n is the number 0 or 1.These phenylalkyl derivatives possess angiotensin antagonist activity.

Abstract: The invention relates to cyclic derivatives of general formula ##STR1## wherein R.sub.a, R.sub.b, X and Y are as defined in claim 1, the tautomers, the stereoisomers including the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable pharmacological properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing the compounds and processes for preparing them.

Abstract: The use of a compound of formula ##STR1## wherein the substituents are defined herein and the physiologically acceptable acid addition salts thereof for treating high blood pressure and cardiac insufficiency.

Abstract: Disclosed are novel alkylarylketocarboxylic acids and 5-substituted tetrazoles represented by the formula ##STR1## wherein Z is aryl or an alkyl of the structure ##STR2## W is a carboxyl moiety or a tetrazole moiety bound to Z at the 5-position of the tetrazole;R.sub.1 is C.sub.4 -C.sub.12 alkyl where Z is aryl and X is oxygen or is C.sub.5 -C.sub.12 alkyl where Z is alkyl and where Z is aryl and X is a bond;R.sub.2 and R.sub.3 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl, hydroxy, C.sub.1 -C.sub.4 alkoxy, halogen, trihalomethyl, nitro, cyano or C.sub.1 -C.sub.4 acyl;R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are each independently hydrogen or C.sub.1 -C.sub.4 alkyl or R.sub.4 and R.sub.6 or R.sub.5 and R.sub.7 can combine to form a carbocyclic ring;X is oxygen, or a bond at the ortho or para position;m is 0, 1 or 2; andn is 0 or 1, and nontoxic, pharmaceutically acceptable addition salts and carboxylic acid esters thereof.

Abstract: Disclosed herein are pentapeptide derivatives of the formula X--NR.sup.1 --CH(R.sup.2)--C(W)--NH--CR.sup.3 (R.sup.4)--C(W.sup.2)--NR.sup.5 --CH CH.sub.2 C(O)--Y!--C(W.sup.3)--NH--CR.sup.6 -- CR.sup.7 (R.sup.8)--COOH!--C(W.sup.4)--NH--CR.sup.9 (R.sup.10)--Z wherein X is a terminal group, for example, alkanoyl or phenylalkanoyl radicals, R.sup.1 is hydrogen, alkyl or phenylalkyl, R.sup.2, R.sup.4 and R.sup.10 are selected from amino acid or derived amino acid residues, R.sup.3, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are hydrogen or alkyl or R.sup.7 and R.sup.8 are joined to form a cycloalkyl, W.sup.1, W.sup.2, W.sup.3 and W.sup.4 are oxo or thioxo, Y is, for example, an alkoxy or a mono or disubstituted amino, and Z is a terminal group, for example, COOH or CH.sub.2 OH. The derivatives are useful for treating herpes infections.

Abstract: Racemates are obtained from non-racemic 3-oxocyclopentane or 3-oxocyclohexane carboxylic acids or their esters by esterification and ketalization of the non-racemic acid with orthoformic acid ester in an alocohol, racemization and hydrolysis of the product obtained with an alcoholate and isolation of the racemate.

Abstract: Described herein are peptide derivatives of the formula R.sup.1 NH--CO--Q--C(O)--NR.sup.2 --CH[CH.sub.2 C(O)--Y]--C(O)--NH--CH[CR.sup.3 (R.sup.4)--COOH]--C(W)--NH--CHR.sup.5 --Z wherein R.sup.1 is an optionally substituted alkyl or optionally substituted phenylalkyl, R.sup.2 is hydrogen or alkyl, R.sup.3 and R.sup.4 each independently is hydrogen or alkyl, or R.sup.3 and R.sup.4 are joined to form a cycloalkyl. R.sup.5 is alkyl, cycloalkyl or (cycloalkyl)alkyl, Q is a divalent radical, for example, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or 1,2-cyclohexanediyl, which serves as a two carbon spacer. W is oxo or thioxo, Y is, for example, an alkoxy or a monosubstituted or disubsdtuted ammo, and Z is a terminal unit, for example, hydrogen, COOH or CH.sub.2 OH. The derivatives are useful for treating herpes infections.

Abstract: This invention relates to pyridyl derivatives of the formula ##STR1## wherein X, Y, A, n and R.sub.3 to R.sub.8 are defined hereinbelow, the enantiomers thereof, the cis- and trans-isomers thereof, which have antithrombotic pharmaceutical activity.

Abstract: In order to control and optimize the amount of inhalable active substance released when drugs are administered as inhalation powders, the invention calls for the use of auxiliaries consisting of mixtures of coarser particles (average particle size>20 .mu.m) and finer particles (average particle size<10 .mu.m).

Abstract: The invention relates to cyclic urea derivatives of general formula ##STR1## wherein R.sub.a, R.sub.b, X and Y are as defined herein, pharmaceutical compositions containing the derivatives and processes for preparing them.

Abstract: Peptide derivatives are of the formula A--B--D--NHCH{CH.sub.2 C(O)R.sup.1 }C(O)--NHCH{CR.sup.2 (R.sup.3)--COOH}C(O)--E wherein A is a lower alkanoyl bearing two substituents, each substituent selected independently from phenyl or a monosubstituted phenyl wherein the monosubstituent is alkyl, halo, hydroxy or alkoxy; B is a N-methyl amino acid residue; D is an amino acid residue; R.sup.1 is alkyl, cycloalkyl, a monosubstituted amino or a disubstituted amino; R.sup.2 is hydrogen or alkyl and R.sup.3 is alkyl, or R.sup.2 and R.sup.3 are joined to form a cycloalkyl; and E is a terminal unit, for example, an alkylamino or a monovalent amino acid radical such as NHCH(alkyl)C(O)OH. The derivatives are useful for treating herpes infections.

Abstract: A viral agent that will mimic "mystery swine" disease has been isolated and described, together with a method of growing the viral agent in vitro, and a method of attenuating the virus for vaccine preparation.