Abstract: The invention provides novel pyrimidine derivatives of formula (I) and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-IR) or analplastic lymphoma kinase (ALK).

Abstract: The present invention relates to substituted heterocyclic compounds of Formula I: or pharmaceutically acceptable salts or N-oxides or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are histamine H4 receptor inhibitors/antagonists useful in the treatment of histamine H4 receptor-associated conditions or diseases or disorders including, for example, inflammatory diseases or disorders, pruritus, and pain.

Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I) or pharmaceutically acceptable salts thereof, wherein X, Y1, Y2, Z, R1, R2 and R3 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.

Abstract: The invention relates to new sulfonamide Nav1.7 inhibitors and pharmaceutically acceptable salts thereof, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.

Abstract: The present invention provides an improved process for preparing HMG-CoA reductase inhibitors such as rosuvastatin calcium, fluvastatin sodium, and pitavastatin calcium under a mild condition, using a novel amide-bond-containing compound having R2—N—O—R1 moiety as a key intermediate. And also, the present invention provides the novel compound, an intermediate useful for the preparation thereof, and a process for the preparation thereof.

Abstract: The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.

Abstract: Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof.

Abstract: The present invention provides an improved process for the preparation of (E)-N-(4-(4-fluorophenyl)-6-isopropyl-5-(3-oxoprop-1-enyl)pyrimidin-2-yl)-N-methyl methanesulfon-amide, which is a useful intermediate for the preparation of (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl methylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxy hept-6-enoic acid, commonly known as Rosuvastatin.

Abstract: The present invention relates to an improved process for preparing (2E)-3-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyrimidin-5-yl]-propenal of formula (I), which is an useful intermediate in the preparation of Rosuvastatin.

Abstract: The invention relates to methods of using certain compounds of formula (I), (II) and (III) in the synthesis of an insecticide intermediate of formula (IV), wherein the substituents are as defined in claim 1, to processes for preparing these compounds, to processes which use these compounds to prepare insecticide intermediates, and to certain novel compounds of formula (II?) and (III?).

Abstract: This invention relates generally to N-benzylamino cyclic thioureas, pharmaceutical compositions containing them, and their use as antagonists of melanin-concentrating hormone receptor (MCH receptor).

Abstract: The invention relates to chemical compounds, or pharmaceutically acceptable salts thereof of the formula (I): which penetrate the blood-brain barrier, inhibit the formation and accumulation of beta-amyloid, and are useful in the treatment of neurodegenerative diseases, particularly Alzheimer's disease. Further, the compounds of the present invention inhibit certain kinases, thereby being useful for the treatment of cancers of the central nervous system.

Abstract: Disclosed are an assay to identify modulators of the PD-1:PD-L pathway and PD-1:PD-L pathway modulators, e.g., compounds and pharmaceutical compositions thereof. Methods for treating diseases influenced by modulation of the PD-1:PD-L pathway such as, for example, autoimmune diseases, inflammatory disorders, allergies, transplant rejection, cancer, immune deficiency, and other immune system-related disorders, are also disclosed.

Abstract: The present invention relates in general to the field of organic chemistry and in particular to a process for the preparation of 5-((E)-2-((2S,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-methanesulfonylamino)pyrimidine (RSVL) as well as a process for preparing crystalline 5-((E)-2-((2S,4R)-4-(tert-butyldimethylsilyloxy)-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethanesulfonylamino)pyrimidine (RSVLTBS) useful as key intermediates for the preparation of rosuvastatin or pharmaceutically acceptable salts thereof.

Abstract: The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

Abstract: The present application relates to novel dipyridyl-dihydropyrazolones, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.

Abstract: The present invention relates to an improved process for the preparation of amide intermediates useful in the preparation of cholesterol reducing agents.

Abstract: The present invention relates to an improved process for preparing Rosuvastatin calcium of Formula I.

Abstract: The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

Abstract: Process for the preparation of enantiomerically pure methyl ester of rosuvastatin has been developed, wherein the crude methyl ester ester is first purified by preparative chromatography, followed by crystallization.

Abstract: The present invention pertains to plant additives containing a molecule selected in a family of compounds, wherein said molecule can modulate some molecular markers and physiological modifications observed in cases of phosphate deficiency. The family of compounds comprises the molecule MC2 of formula (I) as well as analogues thereof.

Abstract: This invention relates to compounds of Formulas I, II, and III, and their use as inhibitors of phosphatidylcholine transfer protein (PC-TP). The invention further relates to pharmaceutical compositions and methods of treatment of disorders related to the inhibition of PC-TP using the compounds of Formulas I, II, and III. Such disorders include obesity and disorders associated with obesity.

Abstract: Pyrimidine deriviatives are ubiquination inhibitors that inhibit the ubiquitin ligase activity, particularly of POSH polypeptides, are useful for the treatment of viral infections and neurological disorders.

Abstract: A process for the preparation of a compound of Formula (1) and intermediates useful therein are provided. The process comprises reacting a compound of formula R1—CO—CH2-E with a compound of formula R2—CHX1X2 in the presence of a compound of formula R3R4N—C(?NH)NH2 and a catalyst, thereby to form a dihydropyrimidine; and oxidizing the dihydropyrimidine to form the compound of Formula (I). R1 is H or an alkyl group; R2 is H, an alkyl or aryl group; R3 and R4 are each independently H, alkyl or aryl, or R3 and R4 are linked to form, together with the nitrogen to which they are attached to form a 5 to 7 membered heterocyclic ring; E is H, an unsubstituted alkyl group, an aryl group or an electron withdrawing group; and X1 and X2 are each independently leaving groups, or X1 and X2 together represent ?O.

Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a compound. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal patched pathway or agonizing smoothened or hedgehog activity.

Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: The present invention concerns a compound of formula (I) or a salt, suitably a pharmaceutically acceptable salt, or solvate thereof, wherein the groups R1, R2, Ar?, A and B are defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.

Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.

Abstract: The invention provides compounds and methods for inhibition of kinases, more specifically IGF 1 R kinases. The invention also provides compounds and methods for inhibition of wildtype Abl. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, or prodrug thereof, wherein, V is NR1R1a, or O—R1, wherein X is H, halo, C1-C6 alkyl, NO2, mono-, di-, or tri-halo substituted methyl, NR13R,14.

Abstract: The present invention relates to novel intermediate compounds used in preparing Rosuvastatin or the pharmaceutically acceptable salts thereof, to a method for preparing same, and to a method for preparing Rosuvastatin or the pharmaceutically acceptable salts thereof from the intermediates. The preparation method of the present invention has the effect of providing Rosuvastatin hemi-calcium salts with an excellent yield rate.

Abstract: The process for the synthesis of statins featuring the use of an early intermediate (4R,6S)-6-(dialkoxymethyl)tetrahydro-2H-pyran-2,4-diol which already possesses the desired stereochemistry corresponding to the final statin.

Abstract: Provided are certain chemical entities, pharmaceutical compositions, and methods of treatment of a member of the flaviviradae family of viruses such as hepacivirus (Hepatitis C or HCV).

Abstract: Disclosed are compounds of formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, U, W, X, R1, R2, R6, R7, R30 and R31 are as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.

Abstract: The present invention is directed to 2-cycloalkylamino-4-arylamino-benzamide compounds of formula I pharmaceutically acceptable salts thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as cardiovascular disease, inflammatory disease, autoimmune disease and cell proliferative disorder.

Abstract: Two polymorphic forms of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt, processes for making them and their use as HMG Co-A reductase inhibitors are described.

Abstract: The present invention relates in general to the field of organic chemistry and in particular to the preparation of N-(4-(4-fluorophenyl)-6-isopropyl-5-methylpyrimidin-2-yl)-N-methylmethanesulfonamide (I), N-(4-(4-fluorophenyl)-5-(bromomethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (II) and N-(4-(4-fluorophenyl)-5-(hydroxymethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (III), key intermediates in preparation of Rosuvastatin.

Abstract: The present invention provides imidazopyridine compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.

Abstract: This invention relates to the discovery of novel rosuvastatin analogues. More specifically, the invention relates to novel rosuvastatin analogues which have utility in treating conditions treatable by the inhibition of HMG-CoA reductase.

Abstract: This invention relates to the discovery of novel rosuvastatin and atorvastatin analogues.

Abstract: A process for the manufacture of the calcium salt of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid, useful as an HMGCoA reductase inhibitor, from a compound of the formula (7) wherein A is an acetal or ketal protecting group and R is alkyl, via isolated crystalline compounds of the formula (8) or of formula (10) is described. Crystalline intermediates of formulae 7, 8 and 10 are also described.

Abstract: The present invention relates to a process for preparing pyrimidine derivatives of the formula V, in particular as intermediates useful for preparing pyrimidine derivatives of a class that is effective at inhibiting the biosynthesis of cholesterol in humans, such as HMG-CoA reductase inhibitors, e.g. rosuvastatin.

Abstract: Small molecule inhibitors of bacterial nicotinamide adenine dinucleotide synthetase (NADs), bacterial nicotinic acid mononucleotide adenylyltransferase (NaMNAT), and human nicotinamide mononucleotide adenylyltransferase (NMNAT) are provided, as well as methods of making and using the inhibitors.

Abstract: A method for preparing a compound of formula k or a salt or solvate thereof, wherein R1 is as defined herein, the method comprising treating a compound of formula j or a salt or solvate thereof, with ammonia, to form the compound of formula k.

Abstract: The present invention publicly discloses a synthetic method and intermediates of rosuvastatin calcium and synthetic methods of the intermediates. The synthetic method uses 4-4?-fluorophenyl-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyridine-5-formaldehyde as the raw material, includes 4-4?-fluorophenyl-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyridine-5-acrylonitrile (intermediate I) from a nitrilized reaction, and 4-4?-fluorophenyl-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyridine-5-acraldehyde (intermediate II) from an aldehydized reaction of the intermediate I, and further goes through such unit processes as side-chain extension, ketone-group reduction, ethyl-group hydrolysis and neutralization reaction or decomposition reaction to obtain rosuvastatin calcium. The nitrilized reagent can be phosphate diethylacetonitrile, acetonitrile, etc.; the aldehyde reductant can be diisobutyl aluminum hydride, red aluminum, etc.

Abstract: [Problem] The present invention provides a 4,6-diaminonicotinamide compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for treating diseases caused by undesirable and/or abnormal cytokine signal transduction. [Means for Solution] The present inventors have extensively studied compounds having a JAK3 inhibitory action, and as a result, they have found that a 4,6-diaminonicotinamide compound which is the compound of the present invention has an excellent JAK3 inhibitory action and is useful as an agent for preventing or treating diseases caused by undesirable and/or abnormal cytokine signal transduction, thereby completing the present invention.

Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.

Abstract: Embodiments of the present invention provide adamantyl benzamide derivtives and pharmaceutical compositions comprising adamantyl benzamide derivatives. Methods of use of such compounds and compositions to modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) in a subject are also provided.

Abstract: The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds.

Abstract: The present invention relates to acid addition salts of the pharmaceutically active compound (3,5-Bistrifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide(I): The invention also relates to processes for the preparation these acid addition salts and to their use as anti tumor agent in humans.