Abstract: Compounds of formula (I) where R2, each X, L, Y, Cy, Lp, D and n are as defined in the specification, are serine protease inhibitors useful as antithrombotic agents.

Abstract: Novel anthelmintic compositions containing thiophene derivatives as active ingredients are disclosed.

Abstract: The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.

Abstract: It is an object of the invention to provide a method which makes it possible to manufacture the desired sulfonium salts directly without using a metathesis process and without using acids in large excess amounts. An aryl compound (A) in which a hydrogen atom is bonded to at least one of the carbon atoms of the aryl group, and a sulfoxide compound (B) which can be expressed by the formula: R1 SO R2 (where R1 and R2 indicate hydrocarbon groups or heterocyclic groups which may be substituted, and which may be the same or different) are reacted in the presence of a strong acid (C) which can be expressed by the formula: HMXmYn (where M indicates an element of group IIIa or group Va of the periodic table, X indicates a halogen atom, Y indicates a hydroxyl group, m and n are integers which are such that m+n=4 and n=0 to 3 in cases where M is an element of group IIIa, and m and n are integers which are such that m+n=6 and n=0 to 2 in cases where M is an element of group Va).

Abstract: The present invention provides compounds of the formula: wherein X=CH2 or S or pharmaceutical acceptable salts thereof useful for treating conditions mediated by DPIV or DPIV-like enzymes, such as arthritis, obesity, immune and autoimmune disorders, allograft transplantation, cancer, neuronal disorders and dermal diseases.

Abstract: A photochromic material having a ring opening quantum yield of 10?3 or lower which does not fade under ambient light is provided. The material comprises a compound belonging to the diheteroarylethene class. The compound has alkoxy group and aryl group on the heteroaryl group.

Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R1-4, Q, and T are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.

Abstract: The present invention relates to reduced FK228 of the formula (I) wherein R1 and R2 are the same or different and each is a hydrogen atom or a thiol-protecting group, or a salt thereof, and a histone deacetylase inhibitor containing this compound, an expression potentiator and a reactivation promoter of a transgene, and pharmaceutical agents containing them as active ingredients. The reduced FK228 or a salt thereof has a strong histone deacetylase inhibitory activity and this compound can be used for the prophylaxis or treatment of various diseases, in which histone deacetylation is involved, and for the gene therapy of such diseases.

Abstract: The present invention provides compositions for inhibiting proteases, methods for synthesizing the compositions, and methods of using the disclosed protease inhibitors. Aspects of the invention include aza-peptide epoxide compositions that inhibit proteases, for example cysteine proteases, either in vivo or in vitro. The disclosed compounds, pharmaceutically acceptable salts, pharmaceutically acceptable derivatives, prodrugs, or combinations thereof can be used to treat disease or pathological conditions related to the activity of proteases associated with a specific disease or condition. Such treatable conditions include viral infections, stroke, neurodegenerative disease, and inflammatory disease, among others.

Abstract: A pyrrolesulfonamide derivative having the following formula (I): wherein the ring P represented by is a pyrrole ring having the following structure: wherein R represents alkyl, cycloalkyl, cycloalkyl-alkyl or aralkyl; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 represents H but, when the bond is absent, Z1 represents H and Z2 represents OH or Z1 and Z2 are combined together to represent O or a group NOR1, in which R1 represents H, or alkyl, aralkyl or aryl; l stands for 0 or 1; A represents alkylene, alkenylene or alkynylene; and Y represents a group in which W represents CH, C? or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is C?; B represents a specific divalent group; E1 and E2 each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group.

Abstract: An N-aminoimidazole or N-aminoimidazolethione derivative, a pharmaceutically acceptable salt, a tautomer, an isomer, an ester or glycosylation product thereof, said derivative being represented by general formula (I): wherein m=zero or 1, n=zero or 1, R1 is selected from hydrogen, methyl or ethyl, R2 is selected from hydrogen, SH or —SR0 wherein R0 is methyl, benzyl or glucose residue; Q is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring, wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isopropyl; L is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isopropyl.

Abstract: The present invention provides novel aryl hydroxyethyl amides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, R7 and A are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said aryl hydroxyethyl amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.

Abstract: Depsipeptides and congeners thereof are disclosed having the following structure: wherein m, n, p, q, X, R1, R2 and R3 are as defined herein. These compounds, including FR901228, have activity as, for example, immunosuppressants, as well as for the prevention or treatment of patients suffering or at risk of suffering from inflammatory, autoimmune or immune system-related diseases including graft-versus-host disease and enhancement of graft/tissue survival following transplant. Also provided are methods for inhibiting lymphocyte activation, proliferation, and/or suppression of IL-2 secretion.

Abstract: This invention provides a low cost technique for synthesizing cyclic trithiocarbonates by a simple one step process from epoxides that can be conducted under atmospheric pressure. This synthesis can be depicted as follows: wherein R represents a moiety selected from the group consisting of alkyl groups and aryl groups, wherein R? represents a moiety selected from the group consisting of alkyl groups, aryl groups, and hydrogen atoms, and wherein R? represents a moiety selected from the group consisting of alkyl groups, aryl groups, and hydrogen atoms, wherein the R moiety and the R? moiety can be bonded together to form a cyclic structure, with the proviso that R? represents a hydrogen atom if R? represents an alkyl group or an aryl group. In this process carbon disulfide and a thiocyanate salt, such as potassium thiocyanate, are reacted with the epoxide in an ionic liquid, such as 1-butyl-3-methylimidazolium hexafluorophosphate ([Bmim] PF6) in the presence of water to produce the cyclic trithiocarbonate.

Abstract: Disclosed is a compound represented by the Structural Formula (I): Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C?Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R5–R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2–C6 substituted or unsubstituted alkylene group. Z is ?0 or ?S.

Abstract: There are provided by the present invention certain pyrazole based CCK-1 receptor modulators.

Abstract: Compounds are described that bind to tubulin causing tubulin depolymerization and inhibiting tubulin polymerization. The compounds of the invention are therapeutically effective to inhibit cellular proliferation, for example, as effective anti-cancer agents. The compounds can also induce cytotoxicity in cells such as leukemia cells. The chemical structure of the compounds includes a furan, thiophene, thiazole, oxazole, or imidazole group at one end of the molecule (head) and a hydrophobic, aliphatic chain at the other end of the molecule (tail).

Abstract: Fused bicyclic carboxamide derivatives are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed.

Abstract: The invention relates to new modifications of the trometamol salt of R-thioctic acid of the formula I, processes for their production, pharmaceutical preparations containing these modifications, and their medical application.

Abstract: The process for obtaining 4-(N-alkylamino)-5,6-dihydro-4H-thien-(2,3-b)-thiopyran-2-sulfonamide-7,7-dioxides (I) wherein R1 is H or C1-5 alkyl, and R2 is C1-5 alkyl, starts from the corresponding 4-(N-alkylamino)-5,6-dihydro-4H-thien-(2,3-b)-thiopyran-7,7-dioxides, and comprises protecting the alkylamine group, introducing a sulfonamide group and eliminating protecting group.