Abstract: Antimicrobial dithiocarbamoyl quinolone compounds of the general formula: ##STR1## wherein (1) A.sup.1, A.sup.2, A.sup.3, R.sup.1, R.sup.3, R.sup.4, and R.sup.6 form any of a variety of quinolone and related heterocyclic structures similar to those known in the art to have antimicrobial activity; and(2) (1) R.sup.1 is X, R.sup.3 is X, or both R.sup.1 and R.sup.3 are X; and X is the dithiocarbamate containing moiety;and pharmaceutically-acceptable salts and biohydrolyzable esters thereof, and hydrates thereof.

Abstract: Compounds of the formula ##STR1## wherein X is O or S--(O).sub.t ; n is one; m is zero or one; Y is CH.sub.2, O, or S--(O).sub.t provided that Y is O or S--(O).sub.t only when m is one; and A is ##STR2## are dual inhibitors of NEP and ACE. Compounds wherein A is ##STR3## are selective ACE inhibitors. Also disclosed are methods of preparation and intermediates.

Abstract: Process for the preparation of 3-(N-aryl-amino)-propyl-2'-sulfatoethyl-sulfonyl compoundsCompounds of the formula (1)Ar--NH--(CH.sub.2).sub.3 --SO.sub.2 --(CH.sub.2).sub.2 --OSO.sub.3 M(1)are prepared by reacting a compound of the formula (2) ##STR1## with 2-mercaptoethanol to give a compound of the formula (3)Ar--NH--(CH.sub.2).sub.3 --S--(CH.sub.2).sub.2 --OH (3)at temperatures from 90.degree. to 270.degree. C. in the presence of a catalytic amount of a base, subsequently oxidizing the compound of the formula (3) to give a compound of the formula (4)Ar--NH--(CH.sub.2).sub.3 --SO.sub.2 --(CH.sub.2).sub.2 --OH(4),and finally esterifying the compound of the formula (4) with at least one molar equivalent of sulfuric acid, oleum or halosulfonic acid to give a compound of the formula (1).Compounds of the formula (1) are valuable starting compounds for the preparation of reactive dyestuffs.

Abstract: Amino acid esters of the formulas ##STR1## wherein m is zero or one and R.sub.3 is an acid protecting group are prepared. These amino acid esters are useful as intermediates in the preparation of fused bicyclic ring compounds.

Abstract: The invention relates to novel compounds of formula I ##STR1## wherein X is a direct bond, sulfur or --CHR.sub.5 --, R.sub.1 is hydrogen, C.sub.1 -C.sub.25 alkyl, unsubstituted or C.sub.1 -C.sub.4 alkyl-substituted C.sub.5 -C.sub.8 cycloalkyl; unsubstituted or C.sub.1 -C.sub.4 alkyl-substituted C.sub.5 -C.sub.8 cycloalkenyl; unsubstituted or C.sub.1 -C.sub.4 alkyl-substituted phenyl; C.sub.7 -C.sub.9 phenylalkyl or --CH.sub.2 --S--R.sub.6 ; R.sub.2 is hydrogen, C.sub.1 -C.sub.25 alkyl, C.sub.2 -C.sub.24 alkenyl, unsubstituted or C.sub.1 -C.sub.4 alkyl-substituted C.sub.5 -C.sub.8 cycloalkyl; unsubstituted or C.sub.1 -C.sub.4 alkyl-substituted C.sub.5 -C.sub.8 cycloalkenyl; unsubstituted or C.sub.1 -C.sub.4 alkyl-substituted phenyl; C.sub.7 -C.sub.9 -phenylalkyl or --CH.sub.2 S--R.sub.6 ; R.sub.3 is hydrogen or methyl; R.sub.4 is C.sub.1 -C.sub.8 alkyl, O.sup..cndot., OH, NO, --CH.sub.2 CN, C.sub.1 -C.sub.18 alkoxy, C.sub.5 -C.sub.12 cycloalkoxy, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.1 -C.

Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating vital infection.

Abstract: A series of 2-amino-6-alkyl-5-(4-substituted-1-piperazinyl)pyrimidin-4-ones that have selective cytotoxicity on human CNS tumor cells.

Abstract: Quinolinecarboxylic acid derivatives which are represented by the general formula (I) ##STR1## wherein R.sub.1 is a C.sub.1 to C.sub.6 alkyl group which may be substituted, a C.sub.2 to C.sub.6 alkenyl group which may be substituted, a C.sub.3 to C.sub.7 cycloalkyl group which my be substituted or an aryl group which may be substituted,R.sub.2 is hydrogen atom; a halogen atom; hydroxyl group which may be protected, amino group or a C.sub.1 to C.sub.6 alkylamino group each of which may be protected; a C.sub.1 to C.sub.6 dialkylamino group or a C.sub.1 to C.sub.6 alkyl group,R.sub.3 is hydrogen atom or a C.sub.1 to C.sub.6 alkyl group,A is nitrogen atom or ##STR2## wherein A' is hydrogen atom. a halogen atom, a C.sub.1 to C.sub.6 alkyl group, a C.sub.1 to C.sub.6 alkoxyl group which may be substituted, cyano group, or nitro group, and A' may form a ring with R.sub.1 ; the ring may include oxygen atom, nitrogen atom, or sulfur atom as a constituent atom; the ring may be substituted with a C.sub.1 to C.sub.

Abstract: The invention concerns pharmaceutically useful compounds of the formula I, in which R.sup.1, R.sup.2, R.sup.3, n, m and Het have any of the meanings defined herein, and their pharmaceutically-acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processess for the manufacture of the novel compounds and the use of the compounds in medical treatment.

Abstract: Certain benzoxazinones are useful in the inhibition of HIV reverse transcriptase (including its resistant varieties), the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Abstract: A quinoline compound represented by the formula (1) or a salt thereof: ##STR1## wherein the definition of each substituents are described in the specification, which have angiotensin II antagonism and hypotensive action and are useful as an agent for the prevention and treatment of cardiovascular system diseases such as hypertension, heart failure and the like.

Abstract: Compounds of the formula ##STR1## X is --O--, --NH-- and --NR.sup.8 --; Y is --CH.sub.2 --, --CHR.sup.8 -- and --C(R.sup.8).sub.2 --; R.sup.1 is camphor-10-yl, C.sub.1-5 alkoxyl, styryl, hydroxystyryl, furyl, unsubstituted or substituted thienyl, naphthyl, indolyl, tetrahydronaphthyl, unsubstituted, mono- or di-substituted pyridyl, pyrazinyl, unsubstituted or substituted cyclohexyl where the substituent is R.sup.4, and unsubstituted or substituted phenyl where the substituents on phenyl are R.sup.5, R.sup.6 and R.sup.7 ; R.sup.2 is hydrogen, C.sub.1-5 alkoxy, C.sub.1-5 alkyl, amino, C.sub.1-5 alkylcarbonylamino, nitro or halogen; R.sup.3 is hydrogen, C.sub.1-5 alkoxycarbonyl, cyano or carbamoyl; R.sup.4 is one to two of hydrogen, oxo, hydroxy, C.sub.1-5 alkoxy, C.sub.1-5 alkoxycarbonylamino-C.sub.1-5 alkyl and amino-C.sub.1-5 alkyl; R.sup.5, R.sup.6 are each independently selected from hydrogen, halogen, C.sub.1-5 alkyl, hydroxyl and C.sub.1-5 alkoxy; R.sup.7 is ##STR2## W is CO or SO.sub.

Abstract: A process for stereoselectively forming N-substituted dihydro-2,3 benzodiazepines which are useful as AMPA receptor antagonists. The process includes an opening reduction step which sets the stereochemistry of the intermediates and the final compounds to the desired enantiomer. The reduction step may be carried out by an enzymatic reduction.

Abstract: The present invention relates to new cephem compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same and anti-bacterial methods of using the same. The subject cephem compounds comprise a thiadiazine ring bonded to the cephem through an iminoacetamido chain and a pyarzolium ring bonded to the cephem through a methylene chain.

Abstract: The present invention relates to compounds useful as tyrosine kinase inhibitors, having the following general formula (I) ##STR1## wherein one of the groups X.sup.1, X.sup.2, X.sup.3, X.sup.4 is N and the others are CH; R is a group of formula (a), (b), (c) or (d) ##STR2## each of R.sup.1 and R.sup.3 independently is hydrogen, amino, carboxy, cyano, --SO.sub.3 R.sup.4, --SO.sub.2 NHR.sup.5, ##STR3## --COOR.sup.6, --CONH(CH.sub.2).sub.o Ph, --CONHCH.sub.2 (CHOH).sub.n CH.sub.2 OH, ##STR4## --N (CH.sub.2 CH.sub.2 OH).sub.2, --NHCH.sub.2 (CHOH).sub.n CH.sub.2 OH, --NHCONH.sub.2, --NHC(NH.sub.2).dbd.NH, --NHCO(CHOH).sub.n CH.sub.2 OH, ##STR5## --NHSO.sub.2 R.sup.7, --OCH.sub.2 (CHOH).sub.n CH.sub.2 OH, --OOC(CHOH).sub.n CH.sub.2 OH, --OPO(OH).sub.2, --OCH.sub.2 SO.sub.2 NH.sub.2, --CH.sub.2 NH.sub.2, --C(NH.sub.2).dbd.NH, --CH.sub.2 NHC(NH.sub.2).dbd.NH, ##STR6## --CH.sub.2 OH, --CH.sub.2 OOC(CHOH).sub.n C.sub.2 OH, --CH.sub.2 OPO(OH).sub.2, --PO(OH).sub.2 ;R.sup.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.

Abstract: Novel 1-dethia-2-thia-cephalosporanic acid derivatives of the formula ##STR1## wherein R is selected from the group consisting of ##STR2## Ra is an organic radical, R.sub.i and R.sub.j are individually selected from the group consisting of hydrogen, aliphatic, aromatic and heterocycle or taken together with the nitrogen atom to which they are attached form an optionally substituted cycle or R.sub.b NH--, R.sub.b is optionally substituted carbocyclic or heterocyclic aryl, R.sub.1 and --COM are as defined in the specification, R.sub.4 is hydrogen or methoxy, n.sub.2 is 0, 1 or 2 and their non-toxic, pharmaceutically acceptable acid addition salts in racemic or optically active form having antibiotic activity and their preparation and novel intermediates.

Abstract: A process for the synthesis of compounds of formula I ##STR1## wherein Ar.sub.1, Ar.sub.2, A.sub.1, A.sub.2, R and X are as defined in the description, exhibit valuable pharmaceutical properties and are effective especially against diseases responsive to the inhibition of protein kinases, for example tumors.

Abstract: A class of cysteine protease inhibitors which inactivate a cysteine protease by covalently bonding to the protease and releasing a heterocyclic leaving group is presented. The cysteine protease inhibitors of the present invention comprise a first portion which targets a desired cysteine protease and positions the inhibitor near the thiolate anion portion of the active site of the protease, and a second portion which covalently bonds to the cysteine protease and irreversibly deactivates that protease by providing a carbonyl or carbonyl-equivalent which is attacked by the thiolate anion of the active site of the cysteine protease to sequentially cleave a heterocyclic leaving group. The heterocyclic leaving group of the protease inhibitor is of the formula: --O--Het, where Het is a heterocycle having 4-7 atoms in the ring, with at least one of the heterocycle atoms being N, O or S.

Abstract: The present invention relates to imidazoquinazoline derivatives represented by the general formula (I): ##STR1## or pharmacologically acceptable salts thereof. The compounds of the present invention have strong and selective cGMP-specific PDE inhibitory activity and are useful for treating or ameliorating cardiovascular diseases such as thrombosis, angina pectoris, hypertension, arterial sclerosis and the like, as well as asthma and the like.

Abstract: The present invention relates to 1-arylpyrimidine derivatives represented by general formula (I): ##STR1## wherein R.sub.1 is H, alkyl or aralkyl;Ar is 1-naphthyl, or a substituted or unsubstituted phenyl group;R.sub.4 is a substituted phenyl, a substituted styryl, 1-methylcyclohexyl, 4-methylcyclohexyl, 4-oxo-4H-pyran-2-yl or 2-oxo-2H-pyran-5-yl group;R.sub.5 and R.sub.6 are each independently H or alkyl;R.sub.3 is H, and R.sub.7 and R.sub.8 are combined together to be oxo, or else R.sub.3 and R.sub.7 are combined together to be another direct bond, and R.sub.5 and R.sub.8 are combined together to be a direct bond,or pharmaceutically acceptable salts thereof; and methods for treating allergic diseases with such compounds.