Abstract: Methods of inhibiting HSP70 proteins, agents causing the inhibition of HSP70 proteins, and the effects of such inhibition on cell proliferation. Anti-microbial agents comprising small molecules, or pharmaceutical salts thereof, disclosed herein and further methods of use thereof are also disclosed. The disclosed small molecules, or pharmaceutical salts thereof, are effective in inhibiting microbial chaperone activity in microbes, such as homologs of HSP70. The disclosed small molecules, or pharmaceutical salts thereof, are also effective for the therapeutic treatment of cancer.

Abstract: This invention relates to multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use in, for example, the treatment of cognitive disorders.

Abstract: Bipiperidyl compounds of the formula: (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.

Abstract: There is provided a compound, which is dehydroabietylamine salt of rosuvastatin. Also provided are processes for making rosuvastatin calcium that include formation of dehydroabietylamine salt of rosuvastatin.

Abstract: The invention relates to piperidine compounds of formula (I) wherein X-R1 represents —N(H)-pyrimidinyl, wherein said pyrimidinyl is unsubstituted or mono-substituted wherein the substituent is selected from (C1-4)alkyl or halogen, or X-R1 represents —NH—C(O)-heterocyclyl, wherein the heterocyclyl is selected from benzofuranyl and imidazo[2,1-b]-thiazolyl, wherein said heterocyclyl is unsubstituted or independently mono-, di-, or tri-substituted wherein the substituents are independently selected from (C1-4)alkyl; A represents a phenyl- or thiazolyl-group, wherein the phenyl or thiazolyl is unsubstituted or mono-substituted with (C1-4)alkyl; B represents a phenyl-group, wherein the phenyl is unsubstituted or mono-, or di-substituted, wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, trifluoromethyl, cyano and halogen; to pharmaceutically acceptable salts thereof, and to the use of such compounds use as medicaments, especially as orexin receptor antagoni

Abstract: The disclosure relates to a compound of formula (I): wherein R, R2, R3, R4, R5, Z, W and D are as defined in the specification, to compositions containing them, to processes for preparing them, and to their use in the treatment or prevention of conditions capable of being modulated by the inhibition of the activity of protein kinases.

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

Abstract: The invention relates to a compound of the Formula I or salt thereof wherein Rx, Ry, Rz, R5, R6, A, B, L, n and m are as defined in the description. The invention also relates to pharmaceutical compositions of said compounds, the use of said compounds as medicaments and in the production of an anti-angiogenic effect in a warm-blooded animal. The invention also relates to processes for the preparation of said compounds.

Abstract: Disclosed are pyrimidine derivatives having interesting pharmacological properties.

Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.

Abstract: 2-Aminopyrimidine derivatives of formula (I) that are useful as modulators of the H4 receptor.

Abstract: The present invention provides a compound of formula (I): wherein the variants R1, R2, R3, R4, R5, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.

Abstract: An improved process for manufacture of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid calcium salt, which is useful for the production of a pharmaceutical useful in the treatment of, inter alia, hypercholesterolemia, hyperlipoproteinemia and atherosclerosis, is described.

Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.

Abstract: A therapeutic or prophylactic agent for multiple sclerosis is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for multiple sclerosis according to the present invention shows the excellent absorbability and in vivo stability when orally administered, and exhibits high therapeutic or prophylactic effects.

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 oxidising 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: Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.

Abstract: The present invention relates to novel pyrimidine derivatives such as compounds of the formula (I): and the use of such compounds or pharmaceutical compositions thereof in the treatment of diseases, particularly pain, which are mediated by the activity of the cannabinoid 2 receptor.

Abstract: The present invention provides organic compounds of the following structure; A-L1-B-C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.

Abstract: Provided is rosuvastatin calcium with a low salt by product content and processes for preparing such rosuvastatin calcium.

Abstract: Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.

Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.

Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, X and Y have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.

Abstract: The invention provides a compound for use as an inhibitor of Hsp90, the compound having the formula (I): or salts, tautomers, solvates or N-oxides thereof; wherein: A is N or a group CR3; R1 is a monocyclic or bicyclic carbocyclic or heterocyclic ring of 5 to 10 ring members of which up to two ring members may be heteroatoms selected from N, O and S and the remainder are carbon atoms, the carbocyclic or heterocyclic ring being optionally substituted by one or more substituent groups independently selected from R10; and R2, R3 and R10 are as defined in the claims.

Abstract: The compounds of the disclosure, for example, the compound represented by the formula: has excellent therapeutic and prophylactic effects against inflammatory bowel disease. Further, they are excellent in absorption and in vivo stability when administered orally in comparison with conventional compounds. That is, the compounds can be administered orally, and can have excellent therapeutic or prophylactic effect sustained for a longer period of time.

Abstract: The present invention relates to a process for the preparation of rosuvastatin calcium, a promising new HMG-CoA reductase inhibitor.

Abstract: N-aryl piperidine substituted biphenylcarboxamides compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.

Abstract: This invention relates to a compound of formula I, wherein R1, R2, R3, m, n, W, X and Y are as defined herein, or a physiologically tolerated salt thereof, its pharmaceutical composition and use for lowering blood glucose, treating diabetes, or increasing insulin release.

Abstract: The present invention relates to new dopamine D3 and D2 ligands of formula (I): wherein R1, R2 and Q are as described herein, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates and/or polymorphs thereof. The invention also relates to processes for preparing the same, to compositions containing the same and to their use in the treatment and/or prevention of conditions which requires modulation of dopamine receptors.

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein Ar, X, m, R1, R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I for treatment of 5-HT6-mediated diseases.

Abstract: Intermediates and synthetic processes for the preparation of substituted phenylalanine-based compounds (e.g.

Abstract: An improved process for manufacture of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl)(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid calcium salt, which is useful for the production of a pharmaceutical useful in the treatment of, inter alia, hypercholesterolemia, hyperlipoproteinemia and atherosclerosis, is described.

Abstract: A compound represented by the following general formula (I), wherein R1, R2, R3, R4 and R5 represent hydrogen atom, a halo(lower alkyl) group, cyano group and the like, R6 represents an alkyl group, a cycloalkyl group and the like, R7, R8, R9 and R10 represent hydrogen atom, a halogen atom, a lower alkyl group, a halo(lower alkyl) group and the like, R11 and R12 represent hydrogen atom, a lower alkyl group, a (lower cycloalkyl) (lower alkyl) group and the like, and R13 represents hydrogen atom, a halogen atom, a lower alkoxy group and the like, which has potent inhibitory activity on cholesterol ester transfer protein (CETP).

Abstract: Provided are processes and intermediates for preparation of rosuvastatin.

Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.

Abstract: The present invention is directed to certain hexahydrpyrrolidinone compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

Abstract: The present invention provides a compound of formula I: or a pharmaceutically acceptable derivative thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK3, Aurora2, and Syk mammalian protein kinases. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.

Abstract: The present invention relates to salts of HMG CoA reductase inhibitors, and in particular, rosuvastatin amine salts and their use as intermediates in the preparation of rosuvastatin calcium.

Abstract: This invention relates to a process for making spirolactone compounds analogous to formula I.

Abstract: Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.

Abstract: The present invention relates to a compound of the formula [I]: wherein G1 is an alkyl which is substituted by a halogen atom or an alkoxy, or a group of the formula: wherein ring B is benzene ring which may be substituted, etc., Q1 and Q2 maybe the same or different, and each is hydrogen atom, a halogen atom or an alkyl, n is 0, 1, 2, 3 or 4, R1 is hydrogen atom, an alkyl which may be substituted, a cycloalkyl which may be substituted, a phenyl which may be substituted, etc., Z1, Z2, Z3 and Z4 may be the same or different, and each is CH or N, provided that 3 or more of Z1, Z2, Z3 and Z4 should not be N at the same time, G2 is hydrogen atom, —NR3R4, —OR5, etc., where R3 to R8 each is independently hydrogen atom, an alkyl which may be substituted, an alkenyl, an alkynyl, etc., or a pharmaceutically acceptable salt thereof.

Abstract: The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula (I) wherein ring A, X, Y, Z, R1, R2, R3, R4, m and n are as defined herein.

Abstract: This invention provides potassium channel modulators which are compounds of formula I where at least one of W and Z is N; where the moiety is one of Groups A or B below A where Ar is a 1,2-fused, six membered ring aromatic group, bearing substituents R1 and R2 as defined below, and containing zero or one ring nitrogen atom; and where other substituents are defined herein. The invention also provides a composition comprising a pharmaceutically acceptable carrier and at least one of the following: i) a pharmaceutically effective amount of a compound of formula I and ii) a pharmaceutically acceptable salt, ester, or prodrug thereof. The invention also provides a method of preventing or treating a disease or disorder which is affected by activities of potassium channels, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula I or a salt, ester, or prodrug thereof.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.

Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.

Abstract: There is provided a process for the preparation of a compound of formula (7): formula (7) wherein R1 represents an alkyl group; R2 represents an aryl group; R3 represents hydrogen, a protecting group or an alkyl group; and R4 represents hydrogen, a protecting group or a SO2R5 group where R5 is an alkyl group, which comprises a) hydroxylating a compound of formula (1): formula (1) wherein Y represents a halo group; P1 represents hydrogen or a protecting group, and W represents ?O or —OP2, in which P2 represents hydrogen or a protecting group, to give a compound of formula (2): formula (2) b) oxidising the compound of formula (2) to give a compound of formula (3): formula (3) c) coupling the compound of formula (3) with a compound of formula (4): formula (4) wherein R3 represents a protecting group or an alkyl group; R4 represents a protecting group or a SO2R5 group where R5 is an alkyl group; and R6 represents (PR7R8)+X? or P(?O)R7R8 in which X is an anion and R7 and R8 each independently is an alkyl, aryl, al

Abstract: The present invention relates to one or more crystalline forms and polymorphs of compounds of formula I: in the form of pharmaceutically acceptable salts. The present invention is directed to crystalline polymorphs and forms of specific anilino-pyrimidine benzenesulfonamide compounds of formula I as pharmaceutically acceptable salts.

Abstract: There is provided compounds of Formula (I) and salts, solvates, and physiologically functional derivatives thereof: wherein R1 is hydrogen or C1-6alkyl; n is 1, 2, 3 or 4; R2 is aryl, optionally substituted by one or two groups selected from the group consisting of halogen, hydroxy, cyano, C1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkyl, haloC1-4alkoxy, aryl, aryloxy, C1-4alkoxycarbonyl, C1-4alkylsulfonyl and a group R3R4NSO2 (wherein R3 and R4 are independently hydrogen or C1-4alkyl) and a 5- or 6-membered heteroaryl group; or n is 0 and R1 and R2, together with the nitrogen atom to which they are joined, form a 5- or 6-membered monocyclic heterocyclic ring or a 9- or 10-membered bicyclic heterocyclic ring wherein at least the ring which contains the nitrogen atom to which R1 and R2 are joined is non-aromatic, and wherein the 5- or 6-membered monocyclic heterocyclic ring or the 9- or 10-membered bicyclic heterocyclic ring is optionally substituted by one or two groups selected from the group consistin

Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.