摘要:
The present invention provides a pharmaceutical agent having cholesteryl ester transfer protein inhibitory action and useful as a blood lipid lowering agent and the like. The present invention relates to a compound represented by the formula 1 wherein Ar1 is an aromatic ring group optionally having substituents, Ar2 is an aromatic ring group having substituents, ORnull is an optionally protected hydroxyl group, R is an acyl group, Rnull is a hydrogen atom or a hydrocarbon group optionally having substituents, or a salt thereof, and a pharmaceutical composition containing a compound of the formula (I) or a salt thereof or a prodrug thereof.
摘要:
The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
摘要:
The compounds of formula (I) are substituted glycine derivatives useful in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, arthritis, neuropathological disorders, sleep disorders, visceral pain disorders and gastrointestinal disorders. Processes for the preparation of the final products and intermediates useful in the process are included. Pharmaceutical compositions containing one or more of the compounds are also included. 1 wherein R1 is hydroxycarbonyl, a carboxylic acid biostere or prodrug thereof; R3, R3a, R2 and R2a are independently selected from H, C1-C6 alkyl, and C1-C6 alkoxy C1-C6 alkyl; Z is; (i) a C-linked, 5 membered heterocycloalky or heteroaryl substituted with C1-C6 alkyl or fused with C3-C8 cycloalkyl, 4-8 membered heterocycloalkyl, phenyl, or monocyclic heteroaryl, wherein the fused ring is optionally substituted with one or two substituents selected from the group consisting of halogen, C1-C6 alkyl, C1-C6 alkoxy, perfluoro C1-C6 alkyl, perfluoro C1-C6 alkoxy, cyano, C1-C6 alkyl amino, C1-C6 alkyl thio, C3-C8 cycloalkyl, 4-8 membered heterocycloalkyl, phenyl, and monocyclic heteroaryl; or (ii) the group; 2 wherein R4 and R4a are independently H, C1-C6 alkyl, C1-C6 alkoxy or C1-C6 alkoxy C1-C6 alkyl; R5 is C1-C6 alkyl, C3-C12 cycloalkyl, 4-12 membered heterocycloalkyl, aryl or heteroaryl and R5 is optionally substituted with one or two substituents selected from the group consisting of halogen, C1-C6 alkyl, C1-C6 alkoxy, perfluoro C1-C6 alkyl, perfluoro C1-C6 alkoxy, cyano, C1-C6 alkyl amino, di-C1-C6 alkyl amino, amino C1-C6 alkyl, C1-C6 alkyl amino C1-C6 alkyl, di-C1-C6 alkyl amino C1-C6 alkyl, C1-C6 alkyl thio, C3-C8 cycloalkyl, 4-8 membered heterocycloalkyl, phenyl and monocyclic heteroaryl; nulland either; (i) Y is S, O, NH or CH2 and X is a direct link or C1-C2 alkyl optionally substituted with C1-C6 alkyl or di-C1-C6 alkyl or 1-4 fluorine atoms; or (ii) X is S, O, CH2 or NH and Y is C1-C2 alkyl optionally substituted with C1-C6 alkyl or di-C1-C6 alkyl or 1-4 fluorine atoms.
摘要:
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-benzyl-N-phenyl aminoalcohols. A preferred specific N-benzyl-N-phenyl aminoalcohol is the compound:
摘要:
The present invention relates to a process for the preparation of scratch-resistant coatings by dual cure of compositions comprising surface active benzoyl compounds wherein at least one non-polar fluorinated alkyl group is present. The invention also relates to a process for concentrating these surface-active photoinitiators in the surface of coatings, to novel surface active benzoyl compounds wherein at least one non-polar fluorinated alkyl group is present, to compositions wherein the novel surface active fluorinated photoinitiators are present, and to a method for improving the flow of a curable composition on substrates.
摘要:
The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(nnull1)-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-(nnull1)-Alkanol compounds are substituted (R)-Chiral fused heterocyclic amino compounds. A preferred specific (R)-Chiral fused heterocyclic amino compound is: 1
摘要:
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,N-disubstituted fused-heterocyclo amines. A preferred specific N,N-disubstituted fused-heterocyclo amine is the compound:
摘要:
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 N,N-bis-benzyl aminoalcohols. A preferred specific (R)-Chiral N,N-bis-benzyl aminoalcohol is the compound:
摘要:
The present invention relates to a compound formula nullInull: 1 wherein 2 Y is bond, nullOnull(CH2)nnull (in which n is 1, 2, 3 or 4), etc., Z is cyano, tetrazolyl, etc., R1 is hydrogen, lower alkyl, etc., R2 is hydrogen or an amino protective group, R3 is hydrogen or lower alkyl, R4 is hydrogen or lower alkyl, R5 and R8 are each independently hydrogen, halogen, hydroxy, lower alkyl, etc., R6 is hydrogen, lower alkyl, etc., R9 is hydrogen or lower alkyl, and i is 1 or 2, or a salt thereof. The compound nullInull of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.
摘要:
Substituted 3-amino-2-benzyl-1-phenlypropane derivatives, methods for preparing them, pharmaceutical compositions containing them, and methods of using them to treat various medical conditions.