Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.

Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.

Abstract: Disclosed are 1,4-disubstituted benzo-fused urea compounds of formula (I): 1

Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.

Abstract: Aminotetralin derivatives and pharmacological analogs thereof which contain an N-propynyl group exhibit differential dopaminergenic receptor activity. The subject compounds are useful in affecting dopamine receptor activity, particularly in exhibiting differing activity among the various dopamine receptor subtypes. The compounds are useful in treating CNS disorders in mammals in general, and humans in particular.

Abstract: The present invention provides novel N-alkyl-N-phenylhydroxylamine derivatives containing metal chelating groups, a process for preparing the same, the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species (ROS) and/or excess Zn ions, in particular stroke, Parkinson's disease and Alzheimer's disease. The compounds of the invention possess similar or superior LPO inhibition activity to the reference compounds of Trolox and Ebselen. While showing lower toxicity, they also effectively inhibit the cerebral neuronal cell death caused by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.

Abstract: Compounds that are dual aP2/k-FABP inhibitors are provided having the formula 1

Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.

Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.

Abstract: This invention relates to novel substituted succinic acid metallo-&bgr;-lactamase inhibitors which are useful potentiators of &bgr;-lactam antibiotics.

Abstract: This invention relates to novel potent PPAR-alpha-activating compounds which are useful in the treatment of diseases such as coronary heart disease. The invention also relates to methods of preparation of PPAR-alpha-activating compounds.

Abstract: The present invention relates to the compounds of formula: 1

Abstract: Use in sex dysfunctions of one or more of the following classes of drugs selected from the following: B) Salified and not salified, nitric oxide-donor drugs, of formula A—X1—N(O)z, C) Organic or inorganic salts of compounds inhibiting phospho-diesterases.

Abstract: The invention relates to a pharmaceutical composition for administering the dopamine agonist N-0923 in depot form. The invention makes available for the first time a depot form of N-0923, which achieves a therapeutically significant plasma level over a period of at least 24 hours after administration to a patient. As a result of poor oral bio-availability and the short plasma half-life, N-0923 was previously administered either by an intravenous drip or by transdermal systems. Preferred embodiments of said invention are oily suspensions, containing the active ingredient N-0923 in a solid phase, in addition to anhydrous pharmaceutical preparations of N-0923.

Abstract: The present invention provides methods of stimulating tissue growth, including islet cell growth, by administering GABA or a GABA agonist to act on GABAB receptors and GABAB-like receptors to activate cell replication.

Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs.

Abstract: The invention relates a pharmaceutical composition comprising a combination of:

Abstract: Polysubstituted indan-1-ol compounds of formula I, its physiologically acceptable salts and physiologically functional derivatives are disclosed 1

Abstract: Disclosed are methods of treating certain cytokine mediated diseases or conditions using novel aromatic heterocyclic compounds of the formula(I) wherein Ar1,Ar2,L,Q and X are described herein.

Abstract: Novel CycloHexenyl-Ethyl-Thiourea (CHET) compounds as inhibitors of reverse transcriptase and effective agents for the treatment of HIV infection, including mutant, drug-sensitive, drug-resistant, and multi-drug resistant strains of HIV.

Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-heteroaryl-N-phenyl aminoalcohols.

Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

Abstract: The present invention is directed to a series of novel substituted aminoalkylamide derivatives, pharmaceutical compositions containing them and their use in the treatment of reproductive disorders and affective conditions. Further, the compounds of the invention are antagonists of follicle stimulating hormone, a hormone associated with the human reproductive system.

Abstract: Tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.

Abstract: Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the “good” cholesterol and as such may be useful for treating diseases such as atherosclerosis.

Abstract: &agr;, &bgr;-Unsaturated sulfones of the following formulae are provided, which are useful as antiproliferative agents, including, for example, anticancer agents:

Abstract: Chemical structures have been identified which allosterically modify pyrvate kinase and inhibit enzymatic activity. These compounds can be used as pharmaceuticals in the treatment of a wide variety of diseases and disorders where influencing metabolic processes is beneficial, such as the glycolytic pathway, all pathways which use ATP as an energy source, and all pathways which involve 2,3-diphosphoglycerate related to the delivery of oxygen by modifying hemoglobin's oxygen affinity, treatments of tumor and cancer and Alzheimer's disease (AD).

Abstract: The present invention provides certain N-substituted sulfonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.

Abstract: The invention relates to novel amino- and amido-diphenyl ethers, processes for their preparation and their use in pharmaceuticals, in particular for the indications of arteriosclerosis and hypercholesterolaemia.

Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.

Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:

Abstract: A composition comprising a combination of a compound of formula I 1

Abstract: The presently disclosed invention relates to compounds of general formula I: 1

Abstract: Methods for inhibiting and/or reversing tau filament formation or polymerization are provided. These methods can be used for treating certain neurological disorders in vivo by administering pharmaceutical compositions which inhibit and/or reverse tau filament formation or polymerization. An especially preferred pharmaceutical composition contains an inhibitor of the general formula I wherein R1 is an aliphatic radical having one to six carbon atoms and wherein R2 and R3 independently are a second aliphatic radical having one to six carbon atoms, a hydroxyl-substituted aliphatic radical having one to six carbon atoms, or a pheny radical or a pharmaceutically acceptable salt of the inhibitor.

Abstract: Compounds represented by structural formula I 1

Abstract: Compounds having the structure shown below wherein A, B, N1, N2, X, Y, Q, R2, R5 and R6 are as defined herein are useful to inhibit serine protease enzymes, such as TF/factor VIIa factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.

Abstract: The invention provides fungicidal compounds of formula I and salts thereof: 1

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

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.

Abstract: The present invention is directed to compounds, compositions and methods of inhibiting and treating HIV and related viruses, and methods for cocrystallizing reverse transcriptase in vitro, inhibition of the replication of HIV and related viruses thereof.

Abstract: The invention relates to heteroaromatic carboxamides of formula (I), 1

Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases other than cancer and proteolytic enzyme mediated diseases other than cancer, and pharmaceutical compositions for use in such therapy.

Abstract: Compounds which are 3-aminocarbonyl-2-carboxamido-thiophene derivatives of formula (I): wherein R1 and R2 are, independently from each other, hydrogen, halogen or an optionally substituted group selected from aryl, straight or branched C1-C6 alkyl or aryl C1-C6 alkyl; or, taken together with the thiophene bond to which they are linked, R1 and R2 form a —(CH2)m—(NR4)n—(CH2)p— group wherein m and p are, each independently, an integer form 1 to 3, n is 0 or 1 and m+n+p is an integer from 3 to 5; and R4 is hydrogen or an optionally substituted straight or branched C1-C6 alkyl group; R3 is a group, optionally further substituted, selected from: i) straight or branched C1-C8 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C2-C6 alkylcarbonyl; ii) aryl; iii) 3 to 7 membered carbocycle; iv) 5 to 7 membered heterocycle with from 1 to 3 heteroatoms selected from nitrogen, oxygen and sulphur; or a pharmaceutically acceptable salt thereof; are useful in the treatment of diseases

Abstract: The present invention relates to a fungicidal composition obtained by mixing a 1,2,3-thiadiazole derivative of general formula (I) useful as a plant disease controller with at least one fungicide selected from the compounds having a fungicidal activity against plant diseases, and to a method for using the same: wherein R1 is hydrogen, alkyl or cycloalkyl and R2 is CO—Y—R3, wherein Y is O, S, NR4 or the like and R3 is hydrogen, alkyl, phenyl, 5- or 6-membered heterocycle or the like.

Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:

Abstract: Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I 1

Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.

Abstract: The present invention relates to novel 3-(cycloalkano-heteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.