Abstract: The invention relates to new hydroxyindoles of the Formula, 1

Abstract: The present invention provides compounds of formula (I): 1

Abstract: This invention relates to substituted imidazoles of Formula I 1

Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: The present invention relates to 3-guanidinocarbonyl-1-heteroaryl-indole derivatives, pharmaceutical compositions comprising such derivatives, methods of treatment comprising administering such derivatives, and processes for their preparation.

Abstract: This invention describes novel pyrazole compounds of formula IIIc: 1

Abstract: The invention relates generally to naphthyridine derivatives of the formula 1

Abstract: Novel 2,4-diaminothiazole derivatives of the general formula (I) which inhibit GSK-3 (glycogen synthase kinase-3), use of these compounds as medicaments, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful for the treatment of disorders, syndromes, diseases and conditions, wherein an inhibition of GSK-3 (glycogen synthase kinase-3) is beneficial, especially IGT (impaired glucose tolerance), type 1 diabetes, type 2 diabetes, obesity, Alzheimer's disease and bipolar disorder.

Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.

Abstract: The present application describes novel hydantoin derivatives of formula (I): 1

Abstract: This invention relates to a method for producing compounds of the formula (I) or their salts: wherein each of R1 and R2 is hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted alkynyl, unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, OR3, SR3, COR3, COOR3 or cyano; R1 and R2 may combine together with the adjacent carbon atom of ═CR1R2 to form an unsubstituted or substituted cyclic ring; each of R4 and R5 is hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted alkynyl, unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, NR6R7, OR8 or SR9; R4 and R5 may combine together with the adjacent skeleton of C/N bond to form a heterocyclic ring; which comprises rearranging compounds of the formula (II) or their salts: wherein R1, R2, R4 and R5 are as defined above.

Abstract: The present invention relates to 5-sulfonamido substituted indolinones that modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

Abstract: The present invention is directed to a compound of formula I, 1

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

Abstract: This invention features a compound of formula (I): 1

Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain sulfonamide or sulfonamide 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: Disclosed are compounds of the formula: wherein R8 represents a cyclic moiety to which is bound an imodazolylalkyl group; R9 represents a carbamate, urea, amide or sulfonamide group; and the remaining substituents are as defined herein. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.

Abstract: The present invention provides a compound of formula (I): 1

Abstract: The present invention provides a compound of formula I: 1

Abstract: Compounds of formula (I) 1

Abstract: N-Benzoyl arylsulfonamides having the formula 1

Abstract: The present invention relates to novel substituted pyrrole compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel substituted pyrrole compounds of the general formula (I), their analogs, their derivatives, their polymorphs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them.

Abstract: The present invention relates to a new crystalline modification of 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1&lgr;6-thiomorpholin-4-yl)-4-(4-fluoro-2-methyl-phenyl)-pyridin-3-yl]-N-methyl-isobutyramide characterized by the following X-ray diffraction pattern obtained with a CuK&agr;, radiation at 2&thgr; (2Theta)=4.5, 6.4, 7.5, 7.7, 8.0, 8.2, 10.0, 10.2, 10.9, 11.1, 12.9, 13.4, 14.0, 14.5, 15.1, 15.6, 16.2, 16.5, 17.3, 17.5, 18.0, 18.9, 19.3, 19.5, 19.9, 20.1, 20.6, 21.0, 21.4, 22.7, 23.1 and 23.6 and an infrared spectrum having sharp bands at 2925, 2854, 1637, 1604, 1484, 1395, 1375, 1285, 1230, 1172, 1125, 1082, 999, 943, 893, 868, 860, 782, 705, 684 cm−1, and wherein the extrapolated melting point (DSC) is 137.2° C.

Abstract: The present invention provides compounds having formula (I): 1

Abstract: The present invention relates to piperazine and piperidine derivatives, which are especially useful for treating or preventing neuronal damage, particularly damage associated with neurological diseases. These compounds are also useful for stimulating nerve growth. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage or for stimulating nerve growth.

Abstract: This invention provides a compound of the formula (I): 1

Abstract: This invention relates to compounds of formula (I) wherein R2 to R10, —X—Y—, A, —W—, n and p have the values defined in claim 1, their preparation and use as pharmaceuticals.

Abstract: Indole derivatives represented by formula (I): 1

Abstract: Compounds which are oxazolyl-pyrazole derivatives, as defined in the specification, and pharmaceutically acceptable salts thereof; are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, viral infections, autoimmune diseases and neurodegenerative disorders.

Abstract: The present invention is directed to novel compounds represented by structural Formula (I): 1

Abstract: This invention relates aryl substituted thiazolidinones of Formula I: 1

Abstract: The purpose is to provide selective PDE IV inhibitors which have a potent anti-asthmatic profile with excellent safety.

Abstract: The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomeruloscierosis.

Abstract: Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-&bgr; signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.

Abstract: 1-Amino 1H-imidazoquinoline compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.

Abstract: The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity.

Abstract: Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3, A1 and A2 have the significance given in claim 1, can be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.

Abstract: The invention relates to compounds of the formula wherein R1 is lower alkyl, lower alkoxy, pyridinyl, pyrimidinyl, phenyl, —S-lower alkyl, —S(O)2-lower alkyl, —N(R)—(CH2)n—N(R)2, —O—(CH2)n—N(R)2, —N(R)2, or a cyclic tertiary amine of the group which may contain one additional heteroatom, selected from N, O or S, and wherein this group may be connected with the pyrimidine ring via the linker —O(CH2)n—; R2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R3/R3′ is, independently from each other, hydrogen or lower alkyl; R4 is independently from each other halogen, trifluoromethyl or lower alkoxy; R5 is hydrogen or lower alkyl; R is, independently from each other, hydrogen or lower alkyl; X is —C(O)N(R)— or —N(R)C(O)—; Y is —O—, —S—, —SO2—, - or —N(R)—; n is 1,2,3 or 4; and m is 0,1 or 2; or a pharmaceutic

Abstract: A compound of the formula: [wherein R1 is a hydrocarbon group which may be substituted; R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; R3 is halogen atoms, a carbamoyl group which may be substituted, a sulfamoyl group which may be substituted, an acyl group derived from sulfonic acid, a C1-4 alkyl group which may be substituted, a C1-4 alkoxy group which may be substituted, an amino group which may be substituted, a nitro group or a cyano group; R4 is hydrogen atoms or a hydroxy group; n is 0 or 1; and p is 0 or 1 to 4]; or a salt thereof, has potent CCR5 antagonistic activity and can be advantageously used as a medicament for inhibition of HIV infection to human peripheral blood mononuclear cells, especially for the treatment or prevention of AIDS.

Abstract: Compounds of general formula (I) 1

Abstract: 17-beta-hydroxysteroid dehydrogenase-II inhibitors having the structural formula wherein the phenyl group labeled A and the group —C(R4)(R6)Y are oriented cis to each other; W represents O or S; R1 represents —H or optionally substituted —(C1-C4)alkyl; n represents 0 or an integer of 1-3; and R2 represents any of a variety of substituents on ring A. R4 generally represents —H but may be a bond terminating at the ortho position of ring A. Y represents fluorine, —OR5, or —SR5, and R5 represents —H, optionally substituted —(C1-C4)alkyl, optionally substituted -phenyl, optionally substituted —(C1-C4)alkyl-phenyl, or optionally substituted —(C1-C4)acyl. R6 represents any of a variety of groups as defined in the specification and claims, including heteroaryl, arylalkyl, heteroarylalkyl, arylalkenyl, heteroarylalkenyl, alkynyl, arylalkynyl, heteroarylalkynyl, aryl, and indolyl.

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: The present invention relates to compounds of formula (I) 1

Abstract: This invention provides compound of formulae I or II having the structure 1

Abstract: Substituted 6-(2-methoxy-phenyl)-triazolopyrimidines of formula I 1

Abstract: Substituted 6-(2-tolyl)-triazolopyrimidines of formula (I) in which R1 and R2 independently denote hydrogen or alkyl, alkenyl, alkynyl, or alkadienyl, haloalkyl, haloalkenyl, cycloalkyl, phenyl, naphthyl, or 5- or 6-membered heterocyclyl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or 5- or 6-membered heteroaryl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or where R1 and R2 radicals may be unsubstituted or substituted as defined in the description, or R1 and R2 together with the interjacent nitrogen atom represent a 5- or 6-membered heterocyclic ring, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, which may be substituted; R3 is halogen, cyano, alkyl, alkoxy, haloalkyl, or C(═O)A, wherein A is hydrogen, hydroxy, alkyl, amino, or mono- or dialkyl-amino; n is an integer from 1 to 4; and X is halogen, cyano, alkyl, alkoxy, haloalkoxy or alkenyl

Abstract: The invention relates to the use of compounds of formula (I) as medicaments, to the novel compounds of formula (I) themselves, and to a method for the production thereof.

Abstract: 6-(2,6-Difluoro-phenyl)-triazolopyrimidines of formula (I), in which R1 and R2 independently denote hydrogen or Alkyl, Alkyl, Alkenyl, Alkynyl, or alkadienyl, cycloalkyl, phenyl, naphthyl, or 5- or 6-membered heterocyclyl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulphur or oxygen atom. Or 5- or 6-membered heteroaryl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulphur or xygen atom where R1 and R2 radicals may be unsubstituted or substituted as defined in the description, or R1 and R2 together with the interjacent nitrogen atom represent a 5- or 6-membered hetericyclic ring, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulphur or oxygen atom, which may be substituted; X is halogen, cyano, alkoxy, haloalkoxy or alkenyloxy; Processes for their preparation, compositions containing them and to their use for combating phytopathogenic fungi.

Abstract: The present invention relates to a compound of formula I and a process for making: or a pharmaceutical acid addition salt thereof; which are useful for activating 5-HT1F receptors and inhibiting neuronal protein extravasation in a mammal.

Abstract: Novel compounds of general formula I: including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivative having activity against mammalian factor Xa is described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.