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

Abstract: Novel benzamide compounds of Formula (I), Formula (II) and Formula (III, salts, water soluble salts, analogs and radiolabeled counterparts thereof as sigma-2 receptor radiotracers for imaging the proliferative status of solid tumors. A method for diagnosing a mammal for the presence of a mammalian tumor therein comprises administering to the mammal a diagnostic imaging detectable effective amount of a benzamide compound having a structure illustrated in Formula (I), Formula (II) and Formula (III) and detecting binding of the compound to a tumor in the mammal. A method for diagnostic imaging of a mammalian tissue having cell surface sigma-2 receptors comprising administering to a mammal a diagnostic imaging amount of a compound having a structure illustrated in Formula (I) Formula (II) and Formula (III) and detecting an image of a tissue having an ample cells with sigma-2 receptors.

Abstract: The present invention discloses compounds of formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of formula (I): which are useful in the treatment of metabolic disorders related to insulin resistance or hyperglycemia. These compounds include inhibitors of protein tyrosine phosphatase (PTP-1B) that are useful in the treatment of diabetes and other PTP-1B mediated diseases, such as cancer, neurodegenerative diseases and the like. The compounds of the invention are also useful in pharmaceutical compositions and methods of treating the aforementioned conditions.

Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: Histone deacetylase inhibitors and uses thereof are provided that have the general formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, M and L have the definitions as described herein.

Abstract: Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents.

Abstract: Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents as inhibitors of phosphodiesterase 5 cardiovascular disorders

Abstract: A chemical genus of 2-(aminomethyl)arylamides, which are useful as analgesics, is disclosed.

Abstract: Tetrahydroquinoline derivatives of general formula (I) or salts thereof, having a specific and strong binding affinity for AR and exhibiting AR agonism or antagonism; and pharmaceutical compositions containing the derivatives or the salts.

Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents.

Abstract: Beta-carboline hydroxamic acid compounds represented by formula (I) are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the activity of HIV integrase enzyme and to treat HIV integrase-mediated diseases and conditions.

Abstract: Compounds of the formula (I) are disclosed and are useful in the treatment bacterial infections: wherein: R1 is Ar or Het; R2 is C1-6alkyl, (R?)2N—(CH2)m— or Ar—C0-6alkyl; X is H, C1-4alkyl, OR?, SR?, C1-4alkylsulfonyl, C1-4alkylsulfoxyl, CN, N(R?)2, CH2N(R?)2, NO2, CF3, CO2R?, CON(R?)2, COR?, NR?C(O)R?, F, Cl, Br, I, or CF3S(O)r—; R? is H, C1-6alkyl or Ar—C0-6alkyl; each R? independently is H, C1-6alkyl or Ar—C0-6alkyl; m is 1 or 2; n is 0, 1 or 2; and r is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.

Abstract: Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment bacterial infections: wherein: R1 is Ar or Het; R2 is H, C1-6alkyl or Ar-C0-6alkyl; X is H, C1-4alkyl, OR?, SR?, C1-4alkylsulfonyl, C1-4alkylsulfoxyl, CN, N(R?)2, CH2N(R?) 2, NO2, CF3, CO2R?, CON(R?)2, COR?, NR?C(O)R?, F, Cl, Br, I, or CF3S(O)r—; R? is H, C1-6alkyl or Ar-C0-6alkyl; and r is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.

Abstract: This invention provides compounds which are useful as inhibitors of protein tyrosine phosphatases (PTPases). As inhibitors of PTPases, the compounds of the invention are useful for the management, treatment, control and adjunct treatment of diseases mediated by PTPase activity. Such diseases include type I diabetes, type II diabetes, immune dysfunction, AIDS, autoimmunity, glucose intolerance, obesity, cancer, psoriasis, allergic diseases, infectious diseases, inflammatory diseases, diseases involving the modulated synthesis of growth hormone or the modulated synthesis of growth factors or cytokines which affect the production of growth hormone, or Alzheimer's disease.

Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which ?7 is known to be involved.

Abstract: Cycloalkano-indole and -azaindole derivatives are prepared by reaction of appropriately substituted carboxylic acids with amines. The cycloalkano-indole and -azaindole derivatives are suitable as active compounds for medicaments, preferably antiatherosclerotic medicaments.

Abstract: The invention provides novel lavendamycin analogs having the following general formula: and quinoline-5,8-diones having the following formula: Methods of making and using and compositions containing these compounds are also disclosed.

Abstract: Compounds of the formula (I) wherein m, n, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.

Abstract: A composition includes a substituted dihydro- or tetrahydro-&bgr;-carboline of formula (II) or (III), wherein the aromatic ring of the carboline may include one or more substituents selected from the group consisting of hydroxy, C1-6 alkoxy, benzyloxy, C1-6 acyloxy, amino, C1-6 alkyl, C1-6 dialkylamino, halogen, and carboxy, and the C-1 position of the carboline may include a substitutent selected from the group consisting of a carbocyclic group and a heterocyclic group. The composition may include a salt or a prodrug of the substituted dihydro- or tetrahydro-&bgr;-carboline. The composition may further includes a pharmaceutically acceptable carrier, diluent, or excipient.

Abstract: Compounds according to the formula A—Z—W as herein described, wherein A is selected from the groups consisting of: A′—(CH2)n—, A′—(CH2)nSO2—, and A′—(CH2)nCO—, where n is 0 to 4; and A′ is selected from (a) (C6-C10)aryl-, or (b) (C1-C9)heteroaryl-; which groups may be optionally substituted; and pharmaceutically acceptable salts, solvates or hydrates thereof; pharmaceutical compositions thereof; and methods useful to facilitate secretion of growth hormone(GH) in mammals.

Abstract: Compounds of the formula (I) are disclosed and are useful in the treatment bacterial infections: 1

Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective &bgr;3 receptor agonists useful in the treatment of Type II diabetes and obesity.

Abstract: The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein R1 is (a) C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20 alkynyl, carbocyclic groups, heterocyclic groups or the like; R2 is CONH2 or CONHNH2; one of R3 and R4 is —(L2)-(acidic group) wherein L2 is a group connecting with an acid group and the length of the connecting groups 1 to 5 atoms, and the other is a hydrogen atom; its prodrug, their pharmaceutically acceptable salt, or solvate thereof.

Abstract: Disclosed are compounds of the formula: wherein Ar is optionally substituted aryl or heteroaryl R1 is hydrogen or alkyl; R7 is hydrogen or alkyl; R2 is hydrogen, halogen, alkyl or alkoxy; or R1 and R2 taken together with the ring to which they are attached form a 5-9 membered saturated or aromatic ring optionally having a hetero atom selected from oxygen, sulfur or nitrogen; R3 and R4 are independently hydrogen, alkyl, cycloalkyl, aryl or heteroaryl groups; or R3 and R4 together with the nitrogen atom to which they are attached form a 5-8 membered ring; and R5 is hydrogen, halogen, straight or branched chain lower alkyl having 1-6 carbon atoms, or straight or branched chain lower alkoxy or thioalkoxy having 1-6 carbon atoms, which compounds are highly selective partial agonists or antagonists at human Corticotropin-Releasing Factor 1 (CRF1) receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as wel

Abstract: This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydrates, prodrugs, polymorphs and pseudopolymorphs thereof, to their preparation, to their compositions and to their use.

Abstract: Imidazonaphthydrine compounds that have an aryl containing substituent at the 1-position induce the biosynthesis of cytokines such as interferon and tumor necrosis factor. The compounds exhibit antiviral and antitumor properties. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.

Abstract: Compound of formula (I) wherein: R1 is hydrogen or C1-C6-alkyl optionally substituted by C3-C6-cycloylalkyl; R2 and R3 together with the nitrogen form a saturated or unsaturated 5- or 6-membered heterocyclic ring optionally containing nitrogen or oxygen as an additional heteroatom, wherein the heterocyclic ring thereof is substituted by a group selected from phenyl, benzyl, and diphenylmethyl, each optionally mono- or di-substituted by one or two groups selected from CF3, C1-C4-alkyl, C1-C4-alkoxy, phenyl, benzyl, halogen, and OH, or R2 and R3 together with the nitrogen form a saturated or unsaturated 5- or 6-membered heterocyclic ring optionally containing nitrogen or oxygen as an additional heteroatom, the heterocyclic ring thereof linked via a single bond, a methylene-bridge, or spiro-connected to another saturated or unsaturated heterocyclic group containing one or two heteroatoms selected from oxygen and nitrogen, the heterocyclic group being optionally mono- or di-substituted by a g

Abstract: Compounds of the formula (I) are disclosed which are FabI inhibitors and are useful in the treatment bacterial infections: wherein: R1 is Ar or Het; R2 is H, C1-6alkyl or Ar—C0-6alkyl; X is H, C1-4alkyl, OR′, SR′, C1-4alkylsulfonyl, C1-4alkylsulfoxyl, CN, N(R′)2, CH2N(R′)2, NO2, CF3, CO2R′, CON(R′)2, COR′, NR′C(O)R′, F, Cl, Br, I, or CF3S(O)r—; R′ is H, C1-6alkyl or Ar—C0-6alkyl; and r is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.

Abstract: A method is provided for the preparation of alpha-aryl-propionic acids such as ibuprofen by carbonylating the corresponding 1-arylethyl halide in an acidic aqueous medium containing a palladium catalyst. In the preparation of ibuprofen, 1-(4′-isobutylphenyl)ethyl halide is reacted with carbon monoxide in an acidic aqueous medium containing a palladium catalyst.

Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain urea, thiourea, acylurea, or sulfonylurea functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.

Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein n, R1, R2, R3, W, Q, and X are defined herein, which compounds bind with high selectivity and high affinity to the benzodiazepine site of the GABAA receptors and are therefore useful in the treatment of certain central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples.

Abstract: Imidazonaphthyridine compounds that are unsubstituted at the 2-position induce the biosynthesis of cytokines such as interferon and tumor necrosis factor. The compounds exhibit antiviral and antitumor properties. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.

Abstract: A method is disclosed for the prevention and treatment of Alzheimer's disease by administering to a human in need thereof an effective amount of a substituted tricyclic sPLA2 inhibitor.

Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.

Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: Substituted [1,2,4]triazolo[1,5a]pyridine derivatives and pharmaceutically active salts thereof with activity as adenosine receptor ligands are disclosed. These compounds are useful for treatment of diseases responsive to modulation of the adenosine receptor.

Abstract: The present invention relates to novel &bgr;-carboline derivatives of the general formula wherein all the variables are as described within the specification, useful as phosphodiesterase inhibitors. The present invention further relates to use of the described derivatives for the treatment of diseases and conditions related to PDE, for example male erectile dysfunction.

Abstract: The design, synthesis and antiviral activity of certain antiviral compounds are disclosed examples of which are shown below. These compounds inhibit the reverse transcriptase enzymes of several retroviruses, including human immunodeficiency virus.

Abstract: Cycloalcanoindole and -azaindole derivatives are prepared by reaction of appropriately substituted carboxylic acids with anmines. The cycloahloanindole and -azaindole derivatives are suitable as active compounds for medicaments, preferably antiatherosclerotic medicaments.

Abstract: Disclosed are compounds of the formula: wherein Ar, R1, W, X and m are substituents as defined herein.

Abstract: Non-peptide compounds that act as antagonists of the intestinal hormone glucagons-like peptide 1 (GLP-1) have a 9H-b-carboline central motif. The compounds exhibit advantageous physical, chemical and biological properties and inhibit GLP-1 peptide binding to the GLP-1 receptor and/or prevent activation of the receptor by bound GLP-1. The invention further relates to a method of inhibiting the binding of GLP-1 to the GLP-1 receptor and a method of inhibiting the activation of the GLP-1 receptor. Intermediate compounds useful for making non-peptide GLP-1 receptor antagonists are also described.

Abstract: The subject matter of the present invention is directed to novel substituted beta-carbolines, and specifically compounds of the formula I, 1

Abstract: This invention relates to sulfamides of formula (I) that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Abstract: Disclosed are compounds of the formula: wherein Ar, R1, W and X are substituents as defined herein, which compounds are (1) antagonists at CRF1 receptors and are, therefore, useful in the diagnosis and treatment of stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety; and (2) are neuropeptide Y1, receptor antagonists, and are therefore useful in the treatment of a variety of clinical conditions which are characterized by the presence of an excess of neuropeptide Y.

Abstract: Disclosed are compounds of the formula: wherein Ar is optionally substituted aryl or heteroaryl R1 is hydrogen or alkyl; R7 is hydrogen or alkyl; R2 is hydrogen, halogen, alkyl or alkoxy; or R1 and R2 taken together with the ring to which they are attached form a 5-9 membered saturated or aromatic ring optionally having a hetero atom selected from oxygen, sulfur or nitrogen; R3 and R4 are independently hydrogen, alkyl, cycloalkyl, aryl or heteroaryl groups; or R3 and R4 together with the nitrogen atom to which they are attached form a 5-8 membered ring; and R5 is hydrogen, halogen, straight or branched chain lower alkyl having 1-6 carbon atoms, or straight or branched chain lower alkoxy or thioalkoxy having 1-6 carbon atoms, which compounds are highly selective partial agonists or antagonists at human Corticotropin-Releasing Factor 1 (CRF1) receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as wel

Abstract: A compound selected from those of formula (I): wherein: represents single or double bond, R1 represents hydrogen, alkyl, —R6-aryl, —R6-cycloalkyl, —R6-heterocycle, —CO2R7—, —COR8, or —CONHR8, wherein R6, R7, and R8 are as defined in the description, R2 represents cyano, mono- or di-alkylaminoalkylaminocarbonyl, —CO2R8, —CONHR8, —NR8R9, —NHCO2R7, or —COR8 wherein R7, R8, and R9 are as defined in the description, R3 and R4 together form (C3-C10)cycloalkyl, R5 represents hydrogen, alkyl, or arylalkyl, Ra, Rb, Rc, Rd, which may be identical or different, represent a group as defined in the description, its isomers, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of CNS disorders.

Abstract: The invention provides asymmetric cyanine dye compounds having the general formula: including substituted forms thereof, which are non-fluorescent quencher molecules. The invention further provides reporter-quencher dye pairs, wherein the asymmetric cyanine dyes are the quenchers, polynucleotides incorporating the asymmetric cyanine dyes, and nucleic acid hybridization detection methods utilizing the dye-labeled polynucleotides.