Abstract:
A novel compound of the formula (I): wherein R 1 is alkoxycarbonyl or the like, R 2 is alkyl or the like; R 3 is hydrogen or the like; R 4 is alkylene or the like; R 5 is optionally substituted heterocyclic group; R 6 , R 7 , and R 8 are independently hydrogen; alkyl, alkoxy, or the like; R10 is optionally substituted aromatic ring, or the like; or a pharmaceutically acceptable salt thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP).
Abstract translation:式(I)的新化合物:其中R 1是烷氧基羰基等,R 2是烷基等; R 3是氢等; R 4是亚烷基等; R 5是任选取代的杂环基; R 6,R 7和R 8独立地是氢; 烷基,烷氧基等; R10是任选取代的芳环,等等; 或其药学上可接受的盐,其具有对胆固醇酯转移蛋白(CETP)的抑制活性。
Abstract:
An agent for improving depression-like symptoms comprising D-ribose, which may improve and alleviate various symptoms such as hypobulia, general fatigue, sluggishness, enervation, deterioration in concentration, memory impairment, abnormal sensation/obtundation such as impaired sight, decline in thinking power, indefinite complaint, drop in operation efficiency, or feeling of malaise, etc.
Abstract:
The present invention relates to novel compounds of formula (I), processes for their preparation, compositions comprising them and their use in the treatment or prevention of diseases capable of being modulated by the inhibition of cell adhesion.
Abstract:
The present invention provides a large conductance calcium-activated K channel opener comprising a compound of the formula (I): wherein R 1 and R 3 are each sulfonamide, carbamoyl, acyl, amino, and the like, m and n are each 0 to 2, R 2 and R 4 are each cyano, nitro, hydroxyl, an alkoxy, a halogen, or an alkyl, Ring A is benzene or a heterocyclic ring, Ring B is benzene, a heterocyclic ring, a cycloalkane etc, and Ring Q is pyrazole or isoxazole, or a pharmaceutically acceptable salt thereof as an active ingredient.
Abstract:
A crystal of a dipeptidyl peptidase IV; a three-dimensional structural coordinate of the dipeptidyl peptidase IV; a method for obtaining a three-dimensional coordinate of a homolog protein of the dipeptidyl peptidase IV; a method for obtaining a three-dimensional structural coordinate of a crystal of a complex of the dipeptidyl peptidase IV and a effector of the dipeptidyl peptidase IV; a method for identifying pharmacophore of the effector of the dipeptidyl peptidase IV; a method for designing, identifying, evaluating or searching; the effector; and a program and a medium therefor for use of the three-dimensional structural coordinate.
Abstract:
The present invention relates to a stable liquid preparation comprising a camptothecin derivative which is prepared by binding a compound of the formula [I]:wherein R 1 is a substituted or unsubstituted lower alkyl group, X 1 is a group of the formula: -NHR 2 (R 2 is a hydrogen atom or a lower alkyl group) or a hydroxy group and Alk is a straight or branched chain alkylene group optionally interrupted by an oxygen atom, and a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof, which is adjusted to pH 5-8, or a stable pharmaceutical composition produced by lyophilizing said liquid preparation.
Abstract:
Benzenesulfonate and benzoate of (S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butanoic acid of formula (1) (wherein * represents an asymmetric carbon atom) which are excellent in antihistaminic and antiallergic activities, and a process for producing them.
Abstract:
The present invention describes cyclic peptide compounds which modulate integrin mediated adhesion. These compounds can inhibit both beta 1 and beta 2 mediated adhesion. The invention further relates to therapeutic uses for these compounds in the treatment of adhesion related pathologies.
Abstract:
Cyclized integrin receptor antagonists useful in modulating cell adhesion, including adhesion related to fibronectin, as well as leukocyte adhesion to endothelial cells, are disclosed. Methods for synthesizing, testing, formulating, and using the compounds as therapeutic agents are also disclosed.
Abstract:
The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted heterocyclic group, and the like; R 1 is an optionally substituted alkyl group, wherein the alkyl group further may optionally be substituted by an optionally substituted homocyclic group, and the like; and R 2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.
Abstract translation:本发明涉及通式(1)的化合物:其中Y为亚甲基等; A是任选取代的杂环基等; B是任选取代的杂环基等; R 1是任选取代的烷基,其中烷基进一步可以任选地被任选取代的杂环基取代,等等; 和R 2是任选取代的氨基等; 或其药学上可接受的衍生物,其对胆固醇酯转移蛋白(CETP)具有抑制活性,因此可用于预防和/或治疗动脉硬化性疾病,高脂血症或血脂异常等。