Abstract: A class of 3-phenylimidazo[1,2-?]pyrimidine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, and further substituted on the phenyl ring by alkyl, trifluoromethyl, alkoxy or one or two halogen atoms, especially fluoro, are selective ligands for GABAA receptors, in particular having good affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

Abstract: The present invention provides a matrix metalloproteinase inhibiting compound having structure (VIII) or a salt, an enantiomer, a diastereomer, a racemate, or a tautomer thereof. In other embodiments, the present invention provides a method of changing the conformation of a matrix metalloproteinase, a method of inhibiting a matrix metal metalloproteinase, and a method of treating osteoarthritis.

Abstract: The invention provides the use of an optionally hydroxy-protected 4-hydroxyo or hydroperoxy-3,5-dioxopyrazolidine or an equivalent wherein a pyrazolidine ring attached oxygen is replaced by a sulphur, or a physiologically acceptable salt thereof, for the manufacture of a medicament for use in therapy or prophylaxis. Additionally, the invention provides a method of combating HIV infection which comprises administering to an HIV-infected patient a T-lymphocyte growth suppressing agent, preferably a pyrazolidinol, in an amount sufficient to suppress T-lymphocyte growth in said patient for a period sufficient to reduce the T-lymphocyte concentration in lymph nodes in said patient by at least 25%, said administration being repeated at intervals of at least 3 months.

Abstract: Disclosed are novel compounds of the formula Ia and methods of using soluble epoxide hydrolase (sEH) inhibitors of the formulas I and Ia for diseases related to cardiovascular disease.

Abstract: The present invention is directed to compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof, and methods of making, methods of using and pharmaceutical compositions having compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof: In Structural Formula I, n is 2, 3, or 4; V is O or S; W is O, S, or SO2; R1 is H, a C1-C4 alkyl, phenyl or trifluoromethyl; R2 are each, independently, H, a C1-C6 alkyl, an aryl-C1-C6 alkyl, a cycloalkyl-C1-C4 alkyl, an aryl, a cycloalkyl, or together with the phenyl to which they are bound form naphthyl or 1,2,3,4-tetrahydronaphthyl; R3 are each, independently, H, a C1-C6 alkyl, an aryl-C1-C6 alkyl, a cycloalkyl-C1-C4 alkyl, an aryl, or a cycloalkyl; R4 are each, independently, H, a C1-C4 alkyl, an aryl, or benzyl; R5 are each, independently, H, a substituted or unsubstituted aryl or a heteroaryl, provided that at least one R5 is a substituted or u

Abstract: Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed.

Abstract: This invention is an aminostyrylanthracene compound represented by, for example, the following general formula [I]. This compound is produced by condensation from a corresponding aminobenzaldehyde and a phosphonic ester or phosphonium salt. [where, in the general formula [I] above, R2 represents an unsubstituted aryl group, R1 represents an aryl group which may have a variety of substituents, and R3 to R5 each represent a hydrogen atom, a cyano group, or a hydrocarbon group.

Abstract: A compound of the formula (I): in which Z, R1, R2, R8, R10, R11, R12, R13 and R14 are each as defined in the description, or a salt thereof. The object compound of the present invention has pharmacological activities such as Tachykinin antagonism, and is useful for manufacture of a medicament for treating or preventing Tachykinin-mediated diseases.

Abstract: The instant invention relates to novel tetrazole derivatives of the formula (I) wherein R1 represents halogen, methyl, ethyl, halomethyl, methoxy, ethoxy, C1-2 haloalkoxy, methylthio, ethylthio, C1-3 alkylsulfonyl, methylsulfonyloxy, ethylsulfonyloxy, nitro or cyano, R2 represents C1-6 alkyl, C3-6 cycloalkyl which may be optionally substituted with halogen or C1-3 alkyl, C1-4 haloalkyl, C2-6 alkenyl, or phenyl which may be optionally substituted with halogen, C1-3 alkyl, C1-4 haloalkyl, C2-6 alkenyl, or phenyl which may be optionally substituted with halogen, C1-3 alkyl, C1-2 haloalkyl or nitro, m represents 0, 1 or 2, two R1 s may be identical or different, in case m represents 2, n represents 1 or 2, Q represents one the cyclic groups which are mentioned in the specification, to intermediates and several processes for their preparation, to their use as herbicides and to novel compositions containing them.

Abstract: There is disclosed a chiral phosphine compound of formula (1): wherein R1, R2, and Ar are as defined in the specification. The chiral phosphine compound is suitably used to produce a transition metal complex that is useful as an asymmetric reaction catalyst.

Abstract: The invention provides for a non-steroidal compound having the formula wherein Re and ′Re are OH, optionally independently etherified or esterified; Z is —CH2— or —CH2CH2—; R1 is H, halogen, CF3, or (1C-4C)alkyl; R2, R3 and R4 are independently H, halogen, —CF3, —OCF3, (1C-8C)Alkyl, hydroxy, (1C-8C)alkyloxy, aryloxy, aryl(1C-8C)alkyl, halo(1C-8C)alkyl, —O(CH2)mX, wherein X is halogen or phenyl and m=2-4; —O(CH2)mNRaRb, —S(CH2)mNRaRb or —(CH2)mNRaRb, wherein m=2-4 and Ra, Rb are independently (1C-8C)alkyl, (2C-8C)alkenyl, (2C-8C)alkynyl, or aryl, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, —OH, (1C-8C)alkoxy, aryloxy, carboxyl, (1C-8C)alkylthio, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl, halo(1C-8C)alkyl or Ra and Rb form a 3-8 membered ring structure, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, hydroxy, hydroxy(1C-4C)a

Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.

Abstract: The invention provides compounds of formula 1 wherein R1, R2, R3, and R4 are as defined, and their pharmaceutically acceptable salts. Compounds of formula 1 are indicated to have activity inhibiting cdk5, cdk2, and GSK-3. Pharmaceutical compositions and methods comprising compounds of formula 1 for treating and preventing diseases and conditions comprising abnormal cell growth, such as cancer, and neurodegenerative diseases and conditions and those affected by dopamine neurotransmission.

Abstract: The invention features methods for decreasing necrosis. The invention also features methods for treating a subject with a condition in which necrosis occurs. The invention further features chemical compounds used to decrease necrosis.

Abstract: The invention pertains to novel cyclin dependent kinase inhibitors (cdks) and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. As described herein, the inhibitors of this invention are capable of inhibiting the cell-cycle machinery and consequently may be useful in modulating cell-cycle progression, ultimately controlling cell growth and differentiation. Such compounds would be useful for treating subjects having disorders associated with excessive cell proliferation.

Abstract: A polymerizable molten salt monomer represented by the following general formula (I): wherein Q represents a nitrogen-containing aromatic heterocyclic atomic group which can form a cation; Y1 represents a divalent interlocking group or a bonding hand; Y2 represents a substituted or unsubstituted alkyl group; n represents an integer of from 2 to 20; m represents an integer of 2 or more; X− represents an anion; plural Y1's and plural Y2's may be the same or different, respectively, with the proviso that at least one of Y2's has a polymerizable substituent group; and a plurality of the compounds of the general formula (I) may be connected to each other at Q or Y2 to form a dimer, trimer or tetramer. Also disclosed are an electrolyte composition containing a polymer compound obtained by the polymerization of the molten salt monomer, and a cell containing the electrolyte composition.

Abstract: This invention relates to a novel process of preparing selected 5-substituted pyrazoles useful as p38 kinase and COX-2 inhibitors.

Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.

Abstract: Compounds of formula I are provided as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R3 and n have the significance given in the specification can be used to treat non-insulin dependent diabetes mellitus.

Abstract: New compounds have the formula: wherein R, R1, X and Y have the meanings described herein. Methods are set forth for synthesizing these compounds and using these compounds to treat diseases associated with amyloidosis, such as Alzheimer's disease, maturity onset diabetes mellitus, familial amyloid polyneuropathy, scrapie, and Kreuzfeld-Jacob disease.