Abstract: The present invention relates to a class of compounds represented by the Formula I: or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the ?V?3 and/or the ?V?5 integrin.

Abstract: The invention provides compounds of Formula (I): wherein: R1-R4, A, L, and X have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use, and methods and intermediates useful for preparing them.

Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein G1 is selected from the group consisting of a, b1 and b2, and A and G2 are as defined in the specification; or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

Abstract: A serine protease inhibitor having the formula (I), in which J is H, R1, R1—O—C(O)—, R1—C(O—, R1—SO2—, R3OOC—(CHR2)p—, (R2a,R2b)N—CO—(CHR2)p— or Het-CO—(CHR2)p—; W is an amino-acid of the formula —NH—CHR1—C(O)—, —NR4—CH((CH2)qC(O)OR1)—C(O)—, —NR4—CH((CH2)qC(O)N(R2a,R2b))—C(O)—, —NR4—CH((CH2)qC(O)Het)-C(O)—, D-1-Tiq, D-3-Tiq, D-Atc, Aic, D-1-Piq, D-3 Piq, glutanyl or a (C1-C6) alkylester thereof; E is —NR2—CH2— or the fragment ?which is unsubstituted or substituted with (1-6C)alkyl, (1-6C)alkoxy or benzyloxy; R1 is selected form (1-12C)alkyl, (2-12C)alkenyl, (2-12C)alkynyl, (3-12C)cycloalkyl and (3-12C)cycloalkyl(1-6C)alkylene, which groups are unsubstituted or substituted with (3-12C)cycloalkyl, (1-6C)alkoxy, oxo, OH, CF3 or halogen, and from (6-14C)aryl, (7-15C)aralkyl, (8-16C)aralkenyl and (14-20C)(bisary)alkyl, wherein the aryl groups are unsubstituted or substituted with (1-6C)alkyl, (3-12C)cycloalkyl, (1-6C)alkoxy, OH, CF3 or halogen; R2, R2a and R2b are each independently selected from H, (1-

Abstract: The present invention relates to pyrazinoylguanidine compounds represented by formula (I): where at least one of R3 and R4 is a group represented by formula (A): where the other structural groups are defined herein. The present invention also includes a variety of methods of treatment using these sodium channel blockers.

Abstract: New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1), wherein X N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R1 is OSO2CF3, OSO2CH3, SOR3, SO2R3, COR3, NO2, or CONHR3 and when X is CH or C R1 may also be CF3, CN, F, Cl, Br, or I; R2 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4,-trifluorobutyl, or —(CH2)—R4; R3 is a C1-C3 alkyl CF3, or N(R2)2; R4 is a C3-C6 cycloalkyl, 2-tetrahydrofurane or 3-tetra-hydrofurane, as well as pharmaceutically acceptable salts thereof are disclosed.

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, antherosclerosis. AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: The invention provides compounds of formula (I) wherein R1, R2, R3, R6, Z, Q, m, n, X1, X2, X3, X4 and T are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy, especially for the treatment of chemokine receptor related diseases and conditions

Abstract: The invention relates to new piperazinyl-substituted pyridylalkane, alkene, and alkine acid amides substituted with saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group according to the general formula (I) as well as methods for the production of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.

Abstract: This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)-amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each C1-12alkyl may optionally be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C16alkyloxy-carbonyl,; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is —X1—R6 or —X2-Alk-R7 wherein R6 and R7

Abstract: Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovascular disorders.

Abstract: This invention relates to compounds which are generally alpha-1A/B adrenoceptor antagonists and which are represented by Formula I: wherein Z is —C(O)— or —S(O)2—, X is carbon or nitrogen, Y is carbon, and X—Y considered together are two adjoining atoms of the ring A, said ring being a fused aromatic ring of five to six atoms per ring optionally incorporating one to two heteroatoms per ring, chosen from N, O, or S; and the other substituents are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds induce mitotic arrest thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases which can be treated by inducing mitotic arrest.

Abstract: This invention relates to compounds of the formula wherein A, B, D, E, K, T, G, R3 and R5 are defined as in the specification, and to the pharmaceutically acceptable salts of such compounds.

Abstract: The present invention relates to a class of compounds represented by the Formula I Wherein A1 is a pyridinyl of the formula optionally substituted by one or more Rk selected from the group consisting of hydroxy, alkyl, alkoxy, alkoxyalkyl, thioalkyl, haloalkyl, cyano, amino alkylamino, halogen, acylamino, sulfonamide and —COR; and R is hydroxy, alkoxy, alkyl or amino; and pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the ?v?3 and/or ?v?5 integrin.

Abstract: The invention relates to chiral ionic liquids of the general formula [A]n+[Y]n?, whereby n=1 or 2, the anion [Y]n? is the anion of an organic or inorganic proton acid and the cation [A]+ an optically active organic ammonium cation with up to 50 carbon atoms, at least one chirality center and at least one functional group that can produce a coordination by forming hydrogen bridges or by providing free electron pairs. At least one chirality center is provided with a distance of up to 5 atomic bonds from the functional group. The invention also relates to a method for producing said chiral ionic liquids and to the use thereof in methods for the asymmetric synthesis, the asymmetric catalysis and for separating racemates.

Abstract: There are provided novel compounds of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.

Abstract: The present invention relates to certain novel substituted dihydroimidazo[2,1-b]thiazole and dihydro-5H-thiazolo[3,2-a]pyrimidine compounds including pharmaceutically acceptable salts thereof which have an affinity for 5-HT1A receptors and which inhibit neuronal reuptake of 5-hydroxytryptamine and/or noradrenaline, to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of depression, anxiety, psychoses including schizophrenia, tardive dyskinesia, obesity, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders such as bulimia, anorexia, snaking and binge eating, non-insulin dependent diabetes mellitus, hyperglycaemia, hyperlipidaemia, stress, as an aid to smoking cessation and in the treatment and/or prophylaxis of seizures, neurological disorders such as epilepsy and/or in which there is neurological damage such as stroke, brain trauma, cerebral ischaemia

Abstract: The invention relates to a compound of the formula I: or a salt thereof with a physiologically tolerated acid, or stereoisomers thereof, wherein R1, R2, A, B, C and D have the meanings described in the specification.

Abstract: The invention is directed to physiologically active compounds of general formula (I): and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.