Abstract: The invention encompasses a series cyclic bicyclic heterocyclic compounds of Formula I which are inhibitors of HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS.

Abstract: The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS.

Abstract: The invention relates to triazolopyrimidines of formula (I), in which the substituents are defined as follows: L1 represents cyano, S(?O)nA1 or C(?O)A2, wherein A1 stands for hydrogen, hydroxy, alkyl, alkylamino or dialkylamino; A2 stands for C1–C8 alkoxy, C1–C6 haloalkoxy or one of the groups named in A1; and n stands for 0, 1 or 2; L2, L3 represent hydrogen or halogen; L4, L5 represent hydrogen, halogen or alkyl; X represents halogen, cyano, alkyl, haloalkyl, alkoxy or haloalkoxy; R1 represents alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, alkadienyl, haloalkenyl, cycloalkenyl, alkynyl, haloalkynyl or cycloalkynyl, phenyl, naphthyl, or a five to ten-membered saturated, partially unsaturated or aromatic heterocyclus containing between one and four heteroatoms from the group containing O, N or S; R2 represents hydrogen or R1; R1 and R2 can form, together with the nitrogen atom to which they are bonded, a five or six-membered ring, which can be interrupted and/or substituted by an atom from the group

Abstract: The use of a compound of formula (I): wherein R1 is selected from H, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, halogen, CN, NR5R6, NR4CONR5, NR4CONR5R6,NR4CO2R7 and NR4SO2R7; R2 is selected from aryl attached via an unsaturated carbon; R3 is selected from H, alkyl, COR5, CO2R7, CONR5R6, CONR4NR5R6 and SO2R7; R4, R5 and R6 are independently selected from H, alkyl and aryl or where R5 and R6 are in an NR5R6 group, R5 and R6 may be linked to form a heterocyclic group, or where R4, R5 and R6 are in a (CONR4NR5R6) group, R4 and R5 may be linked to form a heterocyclic group; and R7 is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, in the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2A receptors, may be beneficial, particularly wherein said disorder is a movement disorder such as Parkinson's disease or said disorder is depression, cognitive or memory impairment, acute

Abstract: The present invention provides a method of treating Alzheimer's disease using a compound of Formula (I). Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of the Formula (I) and a method of imaging amyloid deposits, as well as new compounds of Formula (I).

Abstract: This invention relates to novel compounds of Formula (I) for use as vascular damaging agents: wherein: X is selected from: —O—, —S—, —S(O)—, —S(O2)—, —N(R4)— or —N(R4)CH2C(O)—; R1 is independently selected from: amino, halo, hydroxy, —OPO3H2, C1-4alkyl, C1-4alkoxy, N-C1-4alkylamino, N,N-di-C1-4alkanoylamino or C1-4alkylthio wherein the amino group is optionally substituted by an amino acid residue and the hydroxy group is optionally esterified; R2 is selected from: hydrogen or C1-4alkyl; R3 is selected from: hydrogen or C1-4alkyl; R4 is selected from: hydrogen or C1-4alkyl; n is 0, 1 or 2; and p is 0, 1, 2 or 3; or a salt, pro-drug or solvate thereof. The invention also relates to methods for preparing compounds of Formula (I), to their use as medicaments (including methods for the treatment of angiogenesis or disease states associated with angiogenesis) and to pharmaceutical compositions containing compounds of Formula (I).

Abstract: The present invention provides isotopically labeled oxazinocarbazole derivatives having a ring connecting position 8 (C-8) and position 9 (N-9), and more specifically, provides compounds of formula (I) wherein R1, R2, R3 and R4 are described herein. These compounds are useful in the diagnostic analysis of diseases wherein modulation of 5-HT activity is desired.

Abstract: Carbamoyl tetrahydropyridine derivatives represented by the formula: [in the formula, R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C5 alkyl group, or the like; Y1—Y2 represents (R4)C?C(R5), (R6)C?N, N?N, (R7) N—CO, or N?C(R8); X1, X2, and X3 are identical or different, and each represents a hydrogen atom, a halogen atom, or the like; R3, R4, R5, and R6 are identical or different, and each represents a hydrogen atom or an alkyl group; R7 represents a hydrogen atom, a C1-C5 alkyl group, or the like; and R8 represents a hydrogen atom or a carbamoyl group] or a pharmaceutically acceptable salt thereof, and intermediates for the preparation thereof are provided. The derivatives described above are effective for diseases which are believed to involve CRF.

Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof wherein A is a structure i, ii, iii, or iv X is CR7; Y is —S(?O)n—, —S(?NR8)—, or —S(?NR8)(?O)—; Z is —NHC(?O)R1, —NHC(?S)R1, —NR-het1, —O-het1, —S-het1, or -het2; and n is independently 0, 1, or 2. The compounds of formula I are useful as antimicrobials against a number of human and veterinary pathogens.

Abstract: The present invention comprises 6-9-Disubstituted 2-[trans-(4-aminocyclohexyl]aminopurines that are useful in inhibiting cyclin dependent kinases, particularly cdk-2. The present invention also provides a method of preventing apoptosis in neuronal cells and a method of inhibiting the development of neoplasms.

Abstract: The present invention relates to novel compounds of formula (I): wherein Z represents a 5 or 6 membered cycloalkyl, aryl, substituted cycloalkyl, or substituted aryl, said cycloalkyl, aryl, substituted cycloalkyl or substituted aryl optionally containing one or more heteroatoms selected from 0, N or S; k represents 0 or 1; n represents an integer of 1 to 50; X represents —O—, —N(H)—, —N(C1-6alkyl)-, —N(C3-8cycloalkyl)-, —N(C1-8alkyl)(C3-8 cycloalkyl), —N[(CH2CH2O)m(C1-12 alkyl, aryl, or aralkyl)]-, —CH2O—, —CH2NH—, —CH2N(C1-6alkyl)-, —CH2N(C3-8cycloalkyl)-, or —C1-12alkyl-; Q represents (—CH2)p, (—CH═CH—)p, (—C≡C—)p, (—(O)p1CH2—)p or (—CH2(O)p1)p R6 and R7 independently represent O or S; and all other variables are as defined herein; processes for their preparation, pharmaceutical formulations containing them, and their use in me

Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.

Abstract: This invention discloses pyrimidine derivatives, and pharmaceutically acceptable salts and prodrugs thereof, of the following formula: wherein L and M are selected from the group consisting of carbon and CH, the chemical bond between L and M is selected from the group consisting of a single bond and a double bond, wherein Z4 and Z5 are different and are selected from the group consisting of R14 and  where Z4 is R14 when Z5 is  and Z4 is  when Z5 is R14; wherein A1 is CH; wherein B1 is CH; wherein R17 is selected from the group consisting of aryl, diaryl, triaryl, mono-, di- or tri-substituted aryl, mono-, di- or tri-substituted diaryl, mono-, di- or tri- substituted triaryl, a substituted or unsubstituted heteroaryl and p-aroyl-L-glutamate; wherein R18 is a lower akyl group; and said compound capable of inhibiting dihydrofolate reductase and thymidylate synthase.

Abstract: Oxadiazole derivatives represented by formula (I): (wherein R1 represents a hydrogen atom or an amino-protective group; R2, R3, and R4 each independently represents an alkyl group, a cycloalkyl group, a phenyl group which may be substituted, or a 3,4-methylenedioxyphenyl group, or R3 and R4 are taken together to represent a C2-6 alkylene group), a process of producing the same, and a process for producing oxadiazole derivatives represented by formula (II): (wherein all symbols have the same meanings as described above) using the above derivative. According to the invention, the compound represented by formula (II) is produced through fewer steps in a high yield.

Abstract: Aryl substituted phosphoryl derivatives of the formula In which Ar is phenyl, naphthyl, or pyridyl, Y is O or S, X1 is O, NR3, S, CR3R4, CR3W1 or CW1W2, X2 and X6 are a bond or X6 is CH2 and X2 is O, NR3, S, CR3R4, CR3W1 or CW1W2, R3 and R4 are H, alkyl or phenyl, groups, W1 and W2 are heteroatoms, X3 is alkylene, X4 is oxygen or CH2, X5 is a bond or CH2, Z is O, NR5, S, alkyl or phenyl, R5 is H, alkyl or phenyl, J is H, alkyl, phenyl, or a heterocyclic or polycyclic group, Q is O, NR6, S, CR6R7, CR6W3 or CW3W4, R6 and R7 are H, alkyl, or phenyl, and W3 and W4 are hetero atoms, T1 and T2 are H or CH2R8, R8 is H, OH or F, or T1 and T2 together are —CH═CH— or —C(R9)(R10)C(R11)(R12)—, R9 is H, halogeno, CN, NH2, CO-alkyl, or alkyl, R10, R11, and R12 are H, N3, halogen, CN, NH2, CO-alkyl, or alkyl, and B is a purine or pyrimidine base, have antiviral activity, as for example against HIV.

Abstract: A compound useful as an anti-bacterial agent, having the formula wherein R2 together with the nitrogen atom to which it is attached forms a cyclic aminoguanidine group or derivative thereof as defined

Abstract: The present invention relates to novel 9-N-bicyclic nucleoside agents which are useful as selective inhibitors of proinflammatory cytokines.

Abstract: The present invention provides a compound of formula I: wherein X is O or S(O)n; n is zero, 1 or 2; and Y is CR7R8, CHOR9, C(OR9)2, C═NOR10 or C═NNR20R21. Compounds of formula I are useful as herbicidal agents, particularly as agents for the control of undesirable plant species in the presence of a cereal crop.

Abstract: The invention provides new fluorinated cephalosporin antibiotics of Formula I wherein Ra, Rb, Rc, Rd and Re, independently, are H, F or a C1-C6 alkyl-(Z)n— group having at least one fluorine substituent; X is O or S; Y is S, O, or —CH2—; Z is O, S, —SO—, or —SO2—; m and n independently are 0 or 1; and R1 is H, C1-C6-alkyl, phenyl or benzyl, each of which may optionally have up to three substituents selected from halo, C1-C4-alkoxy, phenyl, NO2, C1-C6-alkanoyl, benzoyl, or C1-C6-alkanoyloxy; or a physiologically acceptable salt thereof; and methods of preventing or treating or treating infection, particularly mastitis in ruminants, using these antibiotics.

Abstract: A C-nitroso compound having a molecular weight ranging from about 225 to about 1,000 (from about 225 to about 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to about 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. The compound is preferably water-soluble and preferably contains a carbon alpha to the nitrosylated carbon which is part of a ketone group.