Abstract: Disclosed are novel chalcone derivatives having the formula (I). These compounds possess antiproliferative activity, and are useful for the manufacture of a medicament for the treatment or prevention of neoplasms, particularly those located in the uterus, ovary or breast. The compounds of the invention may also be useful in the manufacture of a medicament for the treatment or prevention of menopausal disorders and osteoporosis.

Abstract: The present invention relates to novel compounds of the formula (I) in which A, B, W, G and Het are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.

Abstract: The present invention relates to a novel 3,4-dihydro-1H-naphthalene derivative having a structure of formula 1 or formula 2, its pharmaceutically acceptable salts and their geometric isomers as a highly selective cyclooxygenase-2 inhibitor. Wherein R1, R2, X, A and Q are defined in this specification respectively.

Abstract: The invention is directed to physiologically active compounds of general formula (I): wherein: R1 represents aryl, heteroaryl or a group R3—L2—Ar1—L3—; R2 represents hydrogen or lower alkyl; R3 represents aryl or heteroaryl; and Ar1 represents an optionally substituted saturated, partially saturated or fully unsaturated 8 to 10 membered bicyclic ring system containing at least one heteroatom selected from O, S or N; Y is carboxy or an acid bioisostere; and their corresponding N-oxides or prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their corresponding N-oxides or prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (&agr;4&bgr;1).

Abstract: The present invention is directed to new compounds for the inhibition of blood clotting proteins and factor Xa activity, and more particularly, to arylalkanoyl derivatives of the formula (I): wherein R(1), R(2), R(3), R(4), R(5), R(6a), and R(6b) have the meanings indicated in the claims. The invention also relates to processes for the preparation of the compounds of formula (I), to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to the use of the compounds of formula (I) in the treatment and prophylaxis of diseases whcih can be treated or prevented by the inhibition of factor Xa activity, such as cardiovascular or thromboembolic diseases, and to the use of the compounds of formula (I) in the preparation of medicaments to be applied in such diseases.

Abstract: The invention is a compound of Formula (I): wherein R is —OH, R1 is —OH, R2 is —H, n is 2 or 3 and X is sulfur, or a pharmaceutically acceptable salt of a compound having Formula (1), or a pharmaceutical composition comprising a compound having Formula (1) or a pharmaceutically acceptable salt thereof, or methods of treating bone loss, breast cancer or prostate cancer comprising administering an effective amount of the compound having Formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.

Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.

Abstract: The novel compound 3-amidinobenzoyl-D-phenylglycine-3-phenylanilide is useful as a serine protease inhibitor.

Abstract: Compounds useful as reactive coalescents and methods of improving the stability of reactive coalescents are disclosed. A process for the preparation of low molecular weight polymers which are also useful as reactive coalescents is also disclosed.

Abstract: Compounds of the formula I in which R1 and R2, independently of one another, each denote H, A, OA, SA or HaI, R3 denotes H or A, R4 denotes A or NH2, R5 denotes H, NH2, NHA or NA2, A denotes alkyl having 1 to 10 carbon atoms, alkenyl, cycloalkyl or alkylenecycloalkyl, Hal denotes F, Cl, Br or I, and their physiologically acceptable salts and/or solvates, as phosphodiesterase VII inhibitors.

Abstract: A compound of formula (1) wherein R1 is hydrogen, halo or methoxy, R2 is hydrogen, halo, methyl, ethyl or methoxy; R3 is carboxy, tetrazolyl, or —CONHSO2R4 where R4 is methyl, ethyl, phenyl, 2,5-dimethylisoxazolyl or trifluoromethyl; T is —CH2— or —SO2—; and ring A is 3-chlorophenyl, 4-chlorophenyl, 3-trifluoromethylphenyl, 3,4-dichlorophenyl, 3,4-difluorophenyl, 3-fluoro-4-chlorophenyl, 3-chloro-4-fluorophenyl or 2,3-dichloropyrid-5-yl; or a pharmaceutically acceptable salt or prodrug thereof, as well as pharmaceutical compositions containing them are described and claimed. These compounds and compositions are useful in the treatment of disease mediated by monocyte chemoattractant protein-1 or RANTES (Regulated Upon Activation, Normal T-cell Expressed and Secreted), such as inflammatory disease.

Abstract: A catalyst comprising a promoted mixed metal oxide is useful for the vapor phase oxidation of an alkane or a mixture of an alkane and an alkene to an unsaturated carboxylic acid and for the vapor phase ammoxidation of an alkane or a mixture of an alkane and an alkene to an unsaturated nitrile.

Abstract: The present invention relates to a catalyst and to a process for preparing color-reduced polyisocyanates containing isocyanurate groups.

Abstract: This invention relates to novel compounds of the following formula and a process for the preparation thereof. wherein X is Cl, Br or I.

Abstract: Compounds of formula (I) and (II) are disclosed wherein, R1, R2, R3, R4, X, A, B, D and Q are as disclosed in the specification, and the compounds are FabI inhibitors useful in the treatment of bacterial infections.

Abstract: This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therepeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.

Abstract: A method of synthesizing a compound having the formula: from a compound having the formula: wherein R1 is hydrogen, fluorine, chlorine or SiR5R6R7, wherein R5, R6, and R7 are independently the same or different an alkyl group or an aryl group, R2 is an alkyl group, R3 is a protecting group, R4 is an alkyl group, an allyl group, a propargyl group —CO2H, or a benzyl group, R8 is —CO2R10, wherein R10 is an alkyl group or an aryl group, X1 is OH and X2 is H, includes the step of exposing compound (III) to at least one of an organic acid or an inorganic acid. A compound has the general formula (III).

Abstract: The present invention relates to compounds of the formula I, wherein Z1, Z2, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurological and gastrointestinal disorders.

Abstract: Compounds of structure (1) are obtained by reduction of compounds of the structures: Compounds of structure (1), especially where Z is a hydrogen atom or a 3,4-methylenedioxyphenyl group, are important intermediates for inter alia paroxetine.