Abstract: Peripherally administered analogs and derivatives of Brefeldin A are used to enhance learning and reverse memory dysfunction through induced long term potentiation in hippocampal tissues.

Abstract: Metal chelates capable of exhibiting an immobilized relativity between about 60 and 200 mM−1s−1/metal atom are useful as magnetic resonance imaging agents. Additionally, a compound which is useful as a metal-chelating ligand has the following formula: wherein Q is a 4- to an 8-membered carbocyclic ring which may be fully or partially saturated; t is an integer from 2 to 16; each R group is independently hydrogen, —OH, —CH2—A, —OCH2CH(OH)CH2—A or a functional group capable of forming a conjugate with a biomolecule, provided that at least two of the R groups are selected from —CH2—A or —OCH2CH(OH)CH2—A; and A is a moiety capable of chelating a metal atom.

Abstract: Resolved enantiomers of the formula (IA) and (IB) wherein B is a purine or pyrimidine base or aza and/or deaza analogs thereof are useful in antiviral pharmaceutical compositions to treat retroviral infections.

Abstract: A process for the manufacture of 3,5-diamino-6-substituted-1,2,4-triazines is disclosed which comprises the steps of: (a) reacting a compound of formula (II):  with aminoguanidine salts, (b) dehydrating the compound obtained to form a compound of formula IV,  and (c) cyclization of the compound of formula IV into a 3,5-diamino-6-substituted-1,2,4-triazine compound of formula I or into a hydrated form thereof.

Abstract: The present invention relates to a method for preparing 5- and 6-halomethyl quinoxalines. The method comprises contacting a 5- or 6-methyl quinoxaline with a halogenating agent in the presence of a radical initiator in a solvent selected from the group consisting of fluorobenzene, difluorobenzenes, trifluorobenzenes, chlorobenzene, dichlorobenzenes, trichlorobenzenes, &agr;, &agr;, &agr;-trifluorotoluene and &agr;, &agr;, &agr;-trichlorotoluene. The invention also relates to preparing 6-bromomethyl quinoxaline with N-bromosuccinimide in the presence of a radical initiator in 1,2-dichloroethane. The method for halogenating benzylic methyl groups may also be employed to halogenate a wide variety of halomethyl heterocyclic compounds.

Abstract: A compound of formula (I): which is useful as a TXA2 and 5-HT2 receptor and pharmaceutical compositions containing the same.

Abstract: Described herein is a compound of the formula wherein Ar′ is a mono or bicyclic aromatic or heteroaromatic radical substituted with one to three substituents selected from the group consisting of hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; R1 is hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio; R2 is phenyl, naphthyl or (C3-C12)cycloalkyl substituted with one or two substituents selected from the group consisting of hydrogen (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; R3 is selected from the group consisting of hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; X is —(C═O)—; or a pharmaceutically acceptable salt racemate, optical isomer or solvat

Abstract: The present invention provides processes for the preparation of 1, 2, 3, 4, 8, 9, 10, 10a-octahydro-7bH-cyclopenta[b][1, 4]diazepino[6, 7, 1-hi]indole derivatives of the general formula: wherein: R is H, alkyl, acyl, or aroyl; R1, R2, R4 and R5 are H, OH, alkyl, cycloalkyl, alkoxy s, halogen, fluorinated alkyl, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino s, dialkylamino, fluorinated alkoxy, acyl, aryl, or aroyl; R3 is H, alkyl, cycloalkyl, alkoxy, fluorinated alkyl, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, aryl, or aroyl; or a pharmaceutically acceptable salt thereof, which are useful in the treatment of central nervous system disorders.