Abstract: Novel pyrazin-2-one derivatives of formula [1] are provided, ##STR1## which are useful as active ingredients of herbicides, wherein R.sup.1 is hydrogen or alkyl; R.sup.2 is haloalkyl; R.sup.3 is optionally substituted alkyl; alkenyl, or alkynyl; and Q is optionally substituted phenyl. Also provided are their use and intermediates for their production.

Abstract: The present invention relates to therapeutically active azabicyclic compounds of formula I ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3, Ar, m and n are defined in the description, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a disease in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.

Abstract: Novel antidiabetic compounds, their tautomeric forms, their derivatives, their analogues, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them; methods for preparing the antidiabetic compounds and their uses.

Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their analogues, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel azolidinedione compounds of the general formula (I), and their analogues, their derivatives, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them.

Abstract: Aromatic keto-acid compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, arthrities, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes.

Abstract: This invention relates to compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, which are effective for inhibiting platelet aggregation and bone resorption, pharmaceutical compositions for effecting such activity, and a method for using these compounds.

Abstract: This invention relates to compounds of formula (I) ##STR1## which are useful as modulators of D.sub.3 receptors, in particular as antipsychotic agents.

Abstract: Compounds of formula I: ##STR1## as well as pharmaceutically acceptable salts thereof are disclosed. R.sup.2 is H and R.sup.3 is C1-3 alkyl, or R.sup.2 and R.sup.3 taken in combination represent C.sub.1-3 alkylidene. Pharmaceutical compositions and methods of treatment are also included. The compounds are useful against methicillin resistant staphylococci (MRSA).

Abstract: This invention relates to a compound of the following formula or a salt thereof, their production and use. ##STR1## wherein R.sup.1 and R.sup.2 independently represent hydrogen, a group bonding through a carbon atom, a group bonding through a nitrogen atom, a group bonding through an oxygen atom, or a group bonding through a sulfur atom; R.sup.3 represents hydrogen, halogen, a group bonding through a carbon atom, a group bonding through a nitrogen atom, a group bonding through an oxygen atom, or a group bonding through a sulfur atom; W represents an oxygen atom or sulfur atom; A represents a group forming a nitrogen-containing condensed ring at the 3,4- of a 1,4-thiazine ring; R.sup.1 and R.sup.2 may be combined to form a bivalent hydrocarbon group interrupted by one or more hetero atoms or an alkylene group.

Abstract: The invention relates to novel compounds of formula (I): ##STR1## where R1 is chosen from hydrogen, saturated or unsaturated linear or branched C1 to C8 alkyl groups which are optionally substituted with a substituent, and optionally substituted benzyl groups, and R2 is chosen from hydrogen, saturated or unsaturated linear or branched C1 to C24 alkyl groups which are optionally substituted with a substituent, aromatic groups which are optionally substituted with a substituent, and saturated or unsaturated heterocyclic groups; and the use of these derivatives for skincare.

Abstract: The compounds of the formula: ##STR1## wherein ring ##STR2## is a hetero ring containing nitrogen atom, optionally selected from ##STR3## n is 0-2; Y is bond or alkylene;Z is bond, alkylene or vinylene;E is(i) 4-15 membered, unsaturated, partially saturated or fully saturated, mono or bicyclic hetero ring containing as hetero atoms, 1 or 2 N atoms, 1 or 2 O atoms or 1 S atom,(ii) 4-15 membered, unsaturated or partially saturated, mono or bicyclic carbocyclic ring, or(iii) --OR.sup.4 (in which R.sup.4 is hydrogen atom, alkyl or alkyl substituted by a hydroxy group);Cyc is 5-7 membered, unsaturated, partially saturated or fully saturated, monocyclic hetero ring containing as hetero atoms, 1 or 2 N atoms or 5-7 membered, unsaturated or partially saturated, monocyclic carbocyclic ring;R.sup.1 is H or alkyl;R.sup.2 is H, alkyl, alkoxy or halogen atom;R.sup.3 is H, alkyl, alkoxy or --COOR.sup.5 (in which R.sup.

Abstract: The present invention discloses compounds of the formula, or any of its enantiomers or any mixture thereof, a pharmaceutically acceptable addition salt thereof or the N-oxide thereofwhereinX and Y together forms .dbd.O, .dbd.S, .dbd.NOR.sup.2, .dbd.CR.sup.3 R.sup.4, .dbd.N--CN, .dbd.N--NR.sup.7 R.sup.8, --(CH.sub.2).sub.m --, or--W'--(CH.sub.2).sub.p --W"--, or one of X and Y is hydrogen and the other is --OR.sup.5, --SR.sup.5, or --NR.sup.5 R.sup.6Z is hydrogen, --COOR.sup.9 ;R.sup.3 and R.sup.4 are independently hydrogen, halogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, aryl, arylalkyl, or --(CH.sub.2).sub.q --COOR.sup.2 ;R.sup.2, R.sup.5 and R.sup.6 are independently hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl, or arylalkyl, --CO-alkyl, or --SO.sub.2 -alkyl;R.sup.7 and R.sup.8 are independently hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl, or arylalkyl;R.sup.9 is alkyl, alkenyl or alkynyl;R.sup.

Abstract: Pyrimidinone derivatives of the general formula: ##STR1## wherein R.sup.1 is hydrogen or alkyl; R.sup.2 is haloalkyl; R.sup.3 is nitrogen or CH; G is optionally substituted ethylene, trimethylene, or vinylene; and Q is selected from several heterocyclic-condensed phenyl groups, are useful as the active ingredients of herbicides because of their excellent herbicidal activity.

Abstract: The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a --Z--CH.sub.2 group. The naphthosultam is further substituted with various substituent groups including cationic groups. The compounds are represented by formula I: ##STR1## Pharmaceutical compositions and methods of use are also included.

Abstract: Heterocyclic derivatives of the formula (I) ##STR1## wherein each symbol is as defined in the specification, pharmaceutically acceptable salts thereof and method of producing them. Pharmaceutical compositions containing the heterocyclic derivative or a pharmaceutically acceptable salt thereof, particularly, ACAT inhibitors and lipoperoxidation inhibitors. The heterocyclic derivatives and pharmaceutically acceptable salts thereof of the present invention show superior ACAT inhibitory activity and lipoperoxidation inhibitory activity, and are useful as ACAT inhibitors and hyperlipemia inhibitors. To be specific, they are useful for the prevention and treatment of arteriosclerotic lesions of arteriosclerosis, hyperlipemia and diabetes, as well as ischemic diseases of brain, heart and the like.

Abstract: The invention concerns compounds of formula I ##STR1## wherein the substituents have various meanings, and their use in the prevention or treatment of inflammatory and proliferative skin diseases and cancer.

Abstract: The present invention provides for the reaction of optionally substituted indole-3-acetamides with optionally substituted methyl indole-3-glyoxyl reagent to prepare potent PKC inhibitors. The reaction is a very efficient and robust macrocyclization methodology.

Abstract: A compound of the formula: ##STR1## wherein X' is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; X is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value equal to 0; A, A' and A" are individually substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; Z' is a substituent other than hydrogen; j is an integer from 0 to 5; and the wavy line in the structure indicates that the compound can exist in the form of an enantiomer or a diasteromer; Z" is hydrogen or a substituent other than hydrogen; Y is C.dbd.O, C(OH)R' or C--A, where R' is hydrogen or lower alkyl is provided.

Abstract: The novel compounds of formula I: ##STR1## (R.sup.1, R.sup.2 and Hal are defined in the specification) show selective fungicidal activity, in particular against rice blast disease. The new compounds are processed with carriers, and optionally an adjuvant, to make fungicidal compositions.