Abstract: The invention provides compounds which inhibit reverse transcriptase (RT) and which inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The compound of the invention are phenoxyethyl-thiourea-pyridines. The invention additionally provides a method for inhibiting reverse transcriptase activity of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention. The invention additionally provides a method for inhibiting replication of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention.

Abstract: The application relates to a process for preparing a compound of Formula I This compound is an intermediate used to produce compounds that are useful as hypocholesterolemic agents in the treatment and prevention of atheroschlerosis.

Abstract: The invention provides a method for preparing a 1-benzotriazolylcarbonate ester of a water-soluble and non-peptidic polymer by reacting a terminal hydroxyl group of a water-soluble and non-peptidic polymer with di(1-benzotriazolyl)carbonate in the presence of an amine base and an organic solvent. The polymer backbone can be poly(ethylene glycol). The 1-benzotriazolylcarbonate ester can then be reacted directly with a biologically active agent to form a biologically active polymer conjugate or reacted with an amino acid, such as lysine, to form an amino acid derivative.

Abstract: The present invention is a heteroaromatic substituted amide showing antagonist activity to neurokinin 1 (NK-1, substance P) receptors.

Abstract: The present invention provides compounds of Formula (I): 1

Abstract: Novel imidazole derivatives are disclosed. These compounds have a good affinity to the NMDA (N-methyl-D-aspartate)-receptor subtype selective blockers, which have a key function in modulating neuronal activity and plasticity which makes them key players in mediating processes underlying development of CNS as well as learning and memory formation. These compounds are useful in the control or treatment of diseases mediated by this receptor.

Abstract: A compound of formula (I): compositions containing them and methods of use to control pests.

Abstract: The invention relates to novel substituted N-aryl nitrogen-containing heterocyclic compounds of the general formula (I) 1

Abstract: Aminopyrimidine and aminopyridine (I) compounds, compositions and methods useful in the treatment of inflammatory, metabolic or malignant conditions, are provided herein.

Abstract: Novel substitued triazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.

Abstract: The present invention is a heteroaromatic substituted amide showing antagonist activity to neurokinin 1 (NK-1, substance P) receptors.

Abstract: New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.

Abstract: This invention claims the process for producing two structural variants of functionalized 4-amino-3-mercapto-1,2,4-triazoles as inhibitors of nitric oxide synthase (NOS) and as inhibitors of malignant cell growth. This fundamental molecular construct operates as a heterocyclic mimic of the open-chain N-aminoarginines (or N-aminoguanidines) previously established as NOS inhibitors.

Abstract: Salts of a bicyclic, N-acylated imidazo-3-amine or an imidazo-5-amine of the formula: 1

Abstract: The present invention relates to compounds of the formula 1

Abstract: A process for preparing a compound of the formula 1

Abstract: Novel heterocyclic compounds of formula I and the salts, solvates and prodrugs thereof, wherein the meanings of the various substituents are as disclosed in the description. Said compounds are useful as anti-inflammatories.

Abstract: Embodiments of the invention relate to C2-substituted indan-1-ols and to their physiologically acceptable salts and physiologically functional derivatives.

Abstract: The present invention is a heteroaromatic substituted amide showing antagonist activity to neurokinin 1 (NK-1, substance P) receptors.

Abstract: The present application describes disubstituted pyrazolines and triazolines of formulae I and II: 1

Abstract: The instant invention provides &bgr;3 adrenergic receptor agonists of structural Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, wherein Ar, R, R1, R2, R3, R4, R5, R6, R7, R8, X, and Y, are as defined herein.

Abstract: The present invention provides a compound of the formula (I):   wherein A ring, B ring and C ring are each independently optionally substituted aromatic carbocycle or optionally substituted 5- or 6-membered heterocycle which may fuse with benzene ring, W1, W2 and/or W3 represents a bond when A ring, B ring and/or C ring is optionally substituted 5-membered heterocycle, X is —O—, —NR1— wherein R1 is hydrogen, lower alkyl etc. or the like, Y is hydrogen, lower alkyl, lower alkenyl or the like, one of V1 and V2 is a bond, and the other is a bond, —O— or the like, and a pharmaceutical composition comprising the same.

Abstract: This invention provides a method of conducting a simultaneous chemical reaction and controlled crystallization of the product employing impinging fluid jet streams containing reactants capable of producing the product with desired particle size characteristics.

Abstract: N-Heterocyclic derivatives of the formula (I): 1

Abstract: The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions containing a therapeutically effective amount of at least one of these analogues. In accordance with the present invention, the pyridoxal and pyridoxine analogues can be used in the treatment of undesired platelet aggregation, and in the treatment of symptoms thereof.

Abstract: The present invention provides compounds and pharmaceutical compositions that act as antagonists at metabotropic glutamate receptors, and that are useful for treating neurological diseases and disorders. Methods of preparing the compounds also are disclosed.

Abstract: This invention relates aryl substituted pyridines of Formula I: 1

Abstract: Novel sulphonyltriazole derivatives of the formula 1

Abstract: 2-[1′,2′,4′-Triazol-3′-yloxymethylene]anilides of the formula I where the index and the substituents have the following meanings: n is 0, 1, 2, 3 or 4; X is a direct bond, O or NRa; Ra is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl; R1 is nitro, cyano, halogen, unsubstituted or substituted alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy or alkynyloxy; R2 is hydrogen, nitro, cyano, halogen, alkyl, haloalkyl, alkoxy, alkylthio or alkoxycarbonyl; R3 is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl or heteroaryl; R4 is hydrogen, unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkylcarbonyl or alkoxycarbonyl; R5 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, processes and intermediates for their preparation and their use are described.

Abstract: Urazole compounds having the formula (I), 1

Abstract: A compound of formula (I): 1

Abstract: A class of N-arylheteroarylalkyl imidazol-2-one compounds is described for use in treatment of arteriosclerosis.

Abstract: N-Heterocyclic derivatives of the formula (I): 1

Abstract: A novel bicyclic imidazo-5-yl-amine derivative of Formula I, 1

Abstract: Triazolone derivatives represented by the formula wherein R1 represents optionally substituted C1-10 alkyl, A1—L1—, A1—ON═CA2, etc.; R2 represents hydrogen, C1-6 alkyl, etc.; R3 represents C1-6 alkoxy, etc.; one of T, U, and V represents CR4, another represents CH or nitrogen, and the remaining one represents CR5 or nitrogen; and W represents CR6 or nitrogen.

Abstract: There are described benzoylcyclohexanediones of the formula I, their preparation, and their use as herbicides and plant growth regulators.

Abstract: N-Heterocyclic derivatives of the formula (I): 1

Abstract: A heterocyclic compound has the following formula (I) wherein Y represents a substituted or unsubstituted ethylene group or a trimethylene group, W represents the group —SO2R1, X represents an oxygen atom or sulfur atom or the group —NR2 or —CHR3, R represents a hydrogen atom or a methyl group and Z represents a pyridyl group.

Abstract: The use is described of 3,5-diphenyl-1,2,4-triazoles of the formula I in which R1-R5 are as defined in the description. The compounds have useful pharmaceutical properties and are particularly active as iron chelators. They can be used for the treatment of iron overload in warm-blooded animals.

Abstract: The invention relates to certain heterocyclic compounds useful for the treatment of cancer and other diseases, having the Formula (I): 1

Abstract: A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):

Abstract: Compounds of formula I wherein: R1 is pyridyl optionally substituted with halogen, C1-4 alkyl, C1-4 alkenyl, CN, Me2N, CO2Me, OMe, aryl, heterocyclyl, or R4; R2 is CF3; halogen; CN; branched or unbranched C1-8 alkyl; branched or unbranched C1-8 alkenyl; C3-8 cycloalkyl optionally substituted with OH, CN, or methoxy; C1-8 alkoxy; C1-4 alkyloxyalkyl; C1-8 alkylthio; C1-4 alkylthioalkyl; C1-8 dialkylamino; C1-4 dialkylaminoalkyl; CO2R4; or aryl connected to the triazole in any position that makes a stable bond and wherein the aryl thereof is optionally substituted with halogen, C1-4 alkyl, C1-4 alkenyl, CN, Me2N, CO2Me, OMe, aryl, heterocyclyl, or R4; L is —NHC(O)—; —NHC(O)O—; —NHC(O)C(O)—; —NHC(S)—; —NH—; —NHC(O)NH—; —NHC(S)NH—; —NHCH2—; —NHCH(R5)—, wherein R5 is H, CN, C1-6 alkyl, C1-6 alkyloxyalkyl, C1-6 alkylthioalkyl, C1-6 alkylsulfinylalkyl, C1-6 alkylsulfonylalkyl, C3-6 cycloalk

Abstract: There is disclosed a 1H-pyrrolo-[1,2-b] [1,2,4]triazole compound represented by formula (I): 1

Abstract: The present invention provides of method of preparing phenyl-substituted azoles. This method uses an efficient ligand-accelerated Ullmann coupling reaction of anilines with azoles. The coupling products are useful for preparing factor Xa inhibitors.

Abstract: The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions containing a therapeutically effective amount of at least one of these analogues. In accordance with the present invention, the pyridoxal and pyridoxine analogues can be used in the treatment of cardiovascular or related diseases and in the treatment of symptoms thereof.

Abstract: 3-(Substituted aryl)-5-{substituted aryl-(alkynyl-aryl)}-[1,2,4]- triazole compounds are useful as insecticides and acaricides. New synthetic procedures and intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects and mites using the compounds are also provided.

Abstract: Compounds of the formula wherein one of X and Y is lower alkyl, haloalkyl, lower alkenyl, lower alkynyl, or alkoxyalkyl; and the other of X and Y is optionally substituted phenyl, pyridyl, thienyl, cyclopropyl, or thiazolyl; and Z is subtituted pyridyl are useful as insecticides and acaricides. New synthetic procedures and intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects and mites using the compounds are also provided.

Abstract: N-Benzoyl arylsulfonamides having the formula 1

Abstract: Compounds of the formula I  in which A is ═N— or R1 is hydrogen, fluorine, chlorine, bromine or methyl; R2 is C1-C4alkyl, C1-C4haloalkyl, halogen, R6O—, nitro, amino or cyano; W is a group  or  and R3, R6, R14 to R24 and X3 to X9 have the meanings given in claim 1 and the agrochemically tolerated salts and stereoisomers of these compounds of the formula I are suitable for use as herbicides.

Abstract: The invention provides a method for preparing a 1-benzotriazolylcarbonate ester of a water-soluble and non-peptidic polymer by reacting a terminal hydroxyl group of a water-soluble and non-peptidic polymer with di(1-benzotriazolyl) carbonate in the presence of an amine base and an organic solvent. The polymer backbone can be poly(ethylene glycol). The 1-benzotriazolylcarbonate ester can then be reacted directly with a biologically active agent to form a biologically active polymer conjugate or reacted with an amino acid, such as lysine, to form an amino acid derivative.