Abstract: Novel 1,2,4-thiadiazole compounds are provided, which are effective as inhibitors of cysteine activity-dependent enzymes and in particular of cysteine proteases. The compounds are useful in treating acne by inhibition of transglutaminase, common cold by inhibition of human rhinovirus 3C protease and inflammatory joint disease by inhibition of cathepsins. The compounds of the present invention are 3,5-disubstituted 1,2,4-thiadazole of the general formula (I): ##STR1## where Z is a nitrogen containing group with recognition sequence for the enzyme and Y is a substituent that tunes the reactivity of the inhibitor towards the thiol group of the cysteine activity-dependent enzyme. The Y group may also serve in recognition.

Abstract: Leukotriene-B.sub.4 derivatives of general formula (I), in which R.sub.1 represents H, CF.sub.3, CH.sub.2 OH, and R.sub.2 represents H or an organic acid radical; R.sup.3 symbolizes H, C.sub.1 -C.sub.14 alkyl, C.sub.3 -C.sub.10 cycloalkyl, or a 5- to 6-membered aromatic heterocyclic ring with at least 1 heteroatom; R.sub.4 means hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.10 cycloalkyl; A symbolizes a trans, trans--CH.dbd.CH--CH.dbd.CH, a --CH.sub.2 CH.sub.2 --CH.dbd.CH-- or a tetramethylene group; B symbolizes a C.sub.1 -C.sub.10 -- straight-chain or branched-chain alkylene group or group (a) or (b); D can mean a direct bond, oxygen, sulfur, --C.tbd.C--, --CH.dbd.CR.sub.7, or together with B can also mean a direct bond; R.sub.5 and R.sub.6 are the same or different and represent H or C.sub.1 -C.sub.4 alkyl, or R.sub.6 represents H and R.sub.5 represents C.sub.1 -C.sub.15 alkanoyl or R.sub.8 represents SO.sub.2 ; R.sub.7 means H, C.sub.1 -C.sub.5 alkyl, chlorine, bromine; R.sub.

Abstract: Novel isoxazolidinedione derivatives of the formula (I) ##STR1## wherein R is an optionally substituted aromatic hydrocarbon, an optionally substituted alicyclic hydrocarbon, an optionally substituted heterocyclic group, an optionally substituted condensed heterocyclic group or a group of the formula ##STR2## R.sub.4 is a hydrogen atom, a lower alkyl or a hydroxy; R.sub.5 is a lower alkyl optionally substituted by hydroxy; and P and Q are each a hydrogen atom or P and Q together form a bond, and pharmaceutically acceptable salts thereof. Said novel isoxazolidinedione derivatives and pharmaceutically acceptable salts thereof have superior hypoglycemic and hypolipidemic actions and are useful for the treatment of diabetes and the complications thereof, as well as therapeutic agents for related diseases such as hyperlipidemia.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salt thereof are useful as histamine H.sub.3 receptor ligands. R.sup.1 is an optional substituent such as C.sub.1 to C.sub.6 alkyl. The moiety (1) replaces any available hydrogen atom on a carbon or nitrogen atom in the ring which includes X. R.sup.2 is C.sub.1 to C.sub.8 hydrocarbylene (in which one or more hydrogen atoms may be replaced by halogen atoms, and up to 2 carbon atoms may be replaced by oxygen, nitrogen or sulfur atoms); R.sup.3 replaces any available hydrogen atom on a carbon or nitrogen atom in the ring which includes X, and is hydrogen or C.sub.1 to C.sub.15 hydrocarbyl (in which one or more hydrogen atoms may be replaced by halogen atoms, and up to 3 carbon atoms may be replaced by oxygen, nitrogen or sulfur atoms); the (or each) R.sup.4 group is independently selected from H, non-aromatic C.sub.1 to C.sub.6 hydrocarbyl, and aryl (C.sub.1 to C.sub.3 alkyl); X is --SO-- or --SO.sub.2 --; Y and Z are each hydrogen, or together represent .

Abstract: A process is disclosed for the preparation of N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)amino)carbonyl)-amino acid derivatives.

Abstract: The present invention presents novel 1,3,4-thiadiazole derivatives of formula I ##STR1## which have useful antiviral activity against herpes virus, cytomegalovirus (CMV).

Abstract: The present invention relates to an oxidation which converts a primary or secondary alcohol of Formula II: ##STR1## to an acid or ketone of Formula I: ##STR2## with periodic acid and a catalytic amount of a chromium reagent.

Abstract: Compounds of the formula ##STR1## where W is ##STR2## n is 0, 1, or 2; m is 0, 1, 2, or 3; Y and G are each independently oxygen or sulfur; Z is --O--, --S--, --NH, or --CH.sub.2 ; R.sub.1 is hydrogen, C.sub.1 to C.sub.8 alkyl, substituted C.sub.1 to C.sub.8 alkyl substituted with one hydroxy, C.sub.3 to C.sub.8 alkenyl, C.sub.3 to C.sub.8 alkynyl, aryl, C.sub.1 to C.sub.3 alkylaryl, C.sub.1 to C.sub.3 alkylheteroaryl, or --Q--R.sub.4 ; R.sub.2 and R.sub.3 are each independently hydrogen, C.sub.1 to C.sub.6 alkyl, aryl, C.sub.1 to C.sub.3 alkylaryl, or C.sub.1 to C.sub.3 alkylheteroaryl; R.sub.4 is cyano, trifluoromethyl, --COR.sub.9, --CO.sub.2 R.sub.9, --CONR.sub.9 R.sub.10, --OR.sub.9, --SO.sub.2 NR.sub.9 R.sub.10, or --S(O).sub.q R.sub.9 ; R.sub.9 and R.sub.10 are each independently hydrogen, C.sub.1 to C.sub.8 alkyl, C.sub.1 to C.sub.3 alkylaryl, aryl, or R.sub.9 and R.sub.

Abstract: Compounds of formula (I) and their possible isomers and isomer mixtures, in which (Z) is a group (a), (b), (c) or (d) and in which the other substituents are as defined herein.

Abstract: N-protected/N-substituted alpha-amino aldehydes, which are useful as pharmaceuticals and pharmaceutical intermediates, can be stored and shipped in a more stable form as N-protected/N-substituted-beta-amino hydroxy sulfonates which can be readily converted back into the aldehyde under mild conditions. The present invention relates to N-protected/N-substituted-beta-amino hydroxy sulfonates and their preparation and use.

Abstract: Compounds related to lactacystin and lactacystin .beta.-lactone, pharmaceutical compositions containing the compounds, and methods of use.

Abstract: A compound represented by the formula (I): ##STR1## wherein, for example, R.sup.1 is optionally substituted aralkyl, Z is nitrogen atom which optionally substituted with alkyl, X.sup.1 is --CH.sub.2 NHCO--, X.sup.2 is phenylene, X.sup.3 is a bond, Y.sup.2 is optionally substituted aryl, B is oxygen atom, its pharmaceutically acceptable salt, or hydrate thereof and a pharmaceutical composition which contains them as an active ingredient.

Abstract: There are described processes for the preparation of a compound of formula I ##STR1## and novel intermediates in the preparative process.

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein A is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, arylC.sub.1-6 alkyl, aryl, S(O).sub.p R.sup.1, OR.sup.1 or NR.sup.1 R.sup.12 ;B is optionally substituted 5- or 6-membered heteroaromatic ring or C(O)NR.sup.10 R.sup.11 ;R.sup.1 is hydrogen, optionally substituted C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl or C.sub.3-6 cycloalkenyl, optionally substituted aryl, arylC.sub.1-6 alkyl, arylC.sub.2-6 alkenyl or arylC.sub.2-6 alkynyl or an optionally substituted 5- or 6-membered heteroaromatic ring;R.sup.2 and R.sup.3 are hydrogen or C.sub.1-6 alkyl;R.sup.4 is hydrogen, C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, aryl or CH.sub.2 (CO).sub.m NR.sup.8 R.sup.9 ;R.sup.5 is NR.sup.6 R.sup.7, C.sub.1-6 alkyl or C.sub.1-6 alkoxy;R.sup.6 is independently as defined for R.sup.4 ;R.sup.

Abstract: The present invention relates to organic molecules capable of inhibiting protein tyrosine phosphatase activity. The invention further relates to the use of such molecules to modulate or regulate signal transduction by inhibiting protein tyrosine phosphatase activity. Finally, the invention relates to the use of such molecules to treat various disease states including diabetes mellitus.

Abstract: This invention relates to neurotrophic N-glyoxylprolyl ester compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity.

Abstract: Compounds of the formula: ##STR1##

Abstract: 1,3-diazolino and 1,3-diazolidino heterocycle derivatives useful as nitric oxide synthase inhibitors.

Abstract: This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.

Abstract: Novel sulphonyloxadiazolones of the formula ##STR1## in which A represents oxygen, sulphur, --SO--, --SO.sub.2 -- or ##STR2## where R.sup.3 represents hydrogen or alkyl,R.sup.1 represents optionally substituted cycloalkyl, optionally substituted cycloalkenyl or optionally substituted aryl andR.sup.2 represents optionally substituted heterocyclyl,a process for preparing these substances and their use as microbicides in crop protection and in the protection of materials.