Abstract: Fused heterocyclic compounds are disclosed that have formula 1: where A, B, L, N, R1, R3, R4?, Y and Z are as defined herein. The compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.

Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R2 and R3 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.

Abstract: The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, esters, and tautomers thereof, wherein: Q is selected from the group consisting of: and L is selected from the group consisting of: pharmaceutically compositions comprising one or more compounds of formula (I), and methods of using the compounds of formula (I).

Abstract: Tocopherol derivatives having the general formula: wherein n is an integer of 6 to 13, R1 is hydrogen, a silyl ether or acetate, R2 is an optionally substituted nitrogen-containing heterocycle or a polycyclic nitrogen-containing heterocycle; and pharmaceutically acceptable salts thereof are provided. A method for synthesizing the compounds is also provided. The tocopherol derivatives are capable of inhibiting the primary enzyme responsible for the metabolism of the tocopherols and tocotrienols compounds of vitamin E, namely tocopherol-?-hydroxylase, and thus increase the amount and prolong the availability of these compounds in plasma and tissue.

Abstract: This invention relates to the methanesulfonic acid addition salts of Imatinib and to the synthesis thereof. In particular, this invention relates to the synthesis of crystalline ?-form of Imatinib methanesulfonate. Furthermore, the invention is directed to a novel acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-[(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]benzamide with two molecules of methanesulfonic acid and to the polymorphic forms thereof, as well as to their pharmaceutical compositions.

Abstract: The present invention is directed to fused [d]pyridazin-7-ones. The invention is also directed to methods for making and using the fused [d]pyridazin-7-ones. In particular, the compounds of the present invention may be effective in the treatment of diseases or disease states related to the activity of VEGFR2, MLK1 and CDK5 enzymes, including, for example, angiogenic disorders and neurodegenerative diseases.

Abstract: Pyridazinyl compounds, compositions and related methods of use.

Abstract: Crystal forms of (6R)-L-erythro-tetrahydrobiopterin dihydrochloride, hydrates and solvates and processes for their preparation are provided. These crystal forms are either intermediates for the preparation of stable polymorphic form B or are suitable for solid formulations.

Abstract: The present invention relates to kinase inhibitor compounds and derivatives thereof as well as compositions comprising them consisting of the structure of formula I: Wherein R1, R2, A, B, D and E are defined herein. These 4-benzimidazol-2-ylpyridazin-3-ones and their derivatives and compositions comprising them are useful in the treatment of neurological disorders such as Alzheimers' disease, Parkinsons' disease, obesity, hypertension and the like. These pyridazinone derivatives particularly inhibit the metabolic activity of glycogen synthase kinase-3 ? (GSK-3?) which is believed to cause the neurodegeneration that results in these diseases.

Abstract: Disclosed are hydrates and polymorphs of 4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]Amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide: processes for preparing them and their use as pharmaceutical compositions with antiproliferative activity.

Abstract: Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.

Abstract: Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract: The present invention concerns a process for preparing crystalline 3-(2-chloro-ethyl)-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one substantially free of 2-acetylbutyrolactone.

Abstract: The invention relates to compounds of formula wherein Het, A1, A2, A3, A4, D, W, T, Q, Y, X1, X2, R1, R2, R3, R4, k and m are as defined hereinabove, and, where applicable, to possible E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form, to a process for the preparation of and to the use of those compounds, E/Z isomers, mixtures of E/Z isomers and/or tautomers, to pesticidal compositions in which the active ingredient has been selected from those compounds, E/Z isomers, mixtures of E/Z isomers and/or tautomers, in each case in free form or in agrochemically usable salt form, to a process for the preparation of and to the use of those compositions, to plant propagation material treated with those compositions, to a method of controlling pests, to intermediates and, where applicable, to possible E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form, for the preparation of those compounds, E/Z isomers, m

Abstract: A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, wherein: Q is selected from the group consisting of: and L is selected from the group consisting of: or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, are useful in treating diseases, disorders, or conditions such as metabolic syndrome and dyslipidemia.

Abstract: The present invention provides compounds of the class of thienopyrimidines, processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, type II diabetes, Metabolic syndrome and neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea, Alzheimer's disease, and pain related disorders, and to pharmaceutical compositions containing them.

Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, M, L, E, G, and J are as defined in the description and claims. The invention also relates to a process for the manufacture of such compounds, pharmaceutical compositions containing them, and methods for treating CNS disorders.

Abstract: The invention relates to new pteridine compounds of formula 1 wherein R1, R2 , R3 and R4 have the meanings given herein, which are useful for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system, or cancers. The invention further relates to pharmaceutical compositions which contain these compounds.

Abstract: The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A1, A2, A3 or A4 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.

Abstract: The present invention provides bipyrimidinyl diphosphine compounds of the formula wherein R is optionally substituted alkyl, cycloalkyl, aryl or heteroaryl; R? and R? are independently optionally substituted alkyl, cycloalkyl, aryl or heteroaryl; or an enantiomer thereof; or an enantiomeric mixture thereof. The compounds of the formula (I) are chiral atropisomeric bipyrimidinyl diphosphine compounds and, thus, may be employed as ligands to generate chiral transition metal catalysts which may be applied in a variety of asymmetric reactions, e.g., in palladium catalyzed asymmetric allylic substitution reactions. The compounds of the present invention are easily accessible in high enantiomeric purity according to the methods disclosed herein.