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 , R 8 and R 9 are independently hydrogen; alkyl, alkoxy, or the like; R 10 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,R 8和R 9独立地是氢; 烷基,烷氧基等; R 10是任选取代的芳环,等等; 或其药学上可接受的盐,其对胆固醇酯转移蛋白(CETP)具有抑制活性。
Abstract:
The present invention relates to a compound of the formula [I] wherein G 1 is an alkyl which is substituted by a halogen atom or an alkoxy, or a group of the formula [II] wherein ring B is benzene ring which may be substituted, etc., Q 1 and Q 2 may be the same or different, and each is hydrogen atom, a halogen atom or an alkyl, n is 0, 1, 2, 3 or 4, R 1 is hydrogen atom, an alkyl which may be substituted, a cycloalkyl which may be substituted, a phenyl which may be substituted, etc., Z 1 , Z 2 , Z 3 and Z 4 may be the same or different, and each is CH or N, provided that 3 or more of Z 1 , Z 2 , Z 3 and Z 4 should not be N at the same time, G 2 is hydrogen atom, -NR 3 R 4 , -OR 5 , etc., where R 3 to R 8 each is independently hydrogen atom, an alkyl which may be substituted, an alkenyl, an alkynyl, etc., or a pharmaceutically acceptable salt thereof.
Abstract:
The present invention provides a novel pyrazolopyrimidine compound of the formula [I]: wherein R' is (A) a substituted aryl group, (B) an optionally substituted nitrogen-containing aliphatic heteromonocyclic group, (C) a substituted cyclo-lower alkyl group, (D) an optionally substituted amino group, or (E) a substituted heteroaryl group, R 2 is (a) an optionally substituted heteroaryl group or (b) an optionally substituted aryl group, Y is a single bond, a lower alkylene group or a lower alkenylene group, Z is a group of the formula: -CO-, -CH2-, -S02- or a group of the formula[II]: Q is a lower alkylene group, and q is an integer of 0 or 1 or a pharmaceutically acceptable sait thereof, which has a small conductance potassium channel (SK channel) blocking activity and is useful as a medicament and a process for preparing the same.
Abstract:
There are disclosed a large conductance calcium-activated K channel opener comprising a compound of the formula (I): wherein ring A is a 5-membered heterocyclic ring containing any one of O, N or S, which ring may be substituted by R 4 , R 1 is aryl, heterocyclic or heterocycle-substituted carbonyl; R 2 is hydrogen, halogen, carboxy, amino, alkyl, alkoxycarbonyl, alkenyl or cycloalkyl; R 3 is aryl, heterocyclic or alkyl; and R 4 is hydrogen or alkyl, each of substituents may be substituted, or a pharmaceutically acceptable salt thereof as an active ingredient.
Abstract translation:公开了一种包含式(I)化合物的大电导钙激活K通道开放剂:其中环A是含有O,N或S中任何一个的5元杂环,该环可以被R> 4,R 1是芳基,杂环或杂环取代的羰基; R 2是氢,卤素,羧基,氨基,烷基,烷氧基羰基,烯基或环烷基; R 3是芳基,杂环或烷基; R 4是氢或烷基,各取代基可以被取代,或其药学上可接受的盐作为活性成分。
Abstract:
A process for preparing 9-hydroxyellipticine, or salt thereof, which comprises treating acetal compound (I): wherein R is alkyl or aryl, R is lower alkyl or aryl, R and R are the same or different and each are substituted or unsubstituted lower alkyl, or both may combine each other at their termini to form substituted or unsubstituted lower alkylene, or a corresponding aldehyde thereof, with an acid, to give 9-hydroxyellipticine in a single step, and if necessary, converting the resulting 9-hydroxyellipticine into a salt thereof. These compounds are useful as an antitumor agent or an intermediate for preparing other medicaments.
Abstract:
A 2-oxoindoline derivative represented by general formula (I) and a pharmacologically acceptable salt thereof, wherein ring A represents (un)substituted benzene; R represents hydrogen, cycloalkyl, aryl, nitrogenous heterocycle, oxygenous heterocycle, sulfurous heterocycle, heterocycle containing nitrogen and oxygen, heterocycle containing nitrogen and sulfur, lower alkoxy, carboxy, cyano, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, oxiranyl, or 2-(lower alkylthio)-1-hydroxyethyl; R represents aryl, a group represented by formula (a), (un)substituted nitrogenous heteromonocycle, (un)substituted nitrogenous heterobicycle, a group represented by formula (b), (wherein n represnts 1 or 2), oxygenous heterocycle, sulfurous heterocycle, heterocyle containing nitrogen and oxygen or heterocycle containing nitrogen and sulfur; R represents (un)substituted lower alkyl; Q represents a single bond or lower alkylene; and Y represents a single bond, lower alkylene or lower alkinylene.
Abstract translation:由通式(I)表示的2-氧代二氢吲哚衍生物及其药理学上可接受的盐,其中环A表示(未)取代的苯; R 1表示氢,环烷基,芳基,含氮杂环,含氧杂环,亚硫杂环,含氮和氧的杂环,含氮和硫的杂环,低级烷氧基,羧基,氰基,低级烷硫基,低级烷基亚磺酰基,低级烷基磺酰基,环氧乙烷基, 或2-(低级烷硫基)-1-羟乙基; R 2表示芳基,由式(a)表示的基团,(un)取代的含氮异单环,(un)取代的含氮异双环,由式(b)表示的基团,(其中n表示1或2),氧杂环 ,亚硫杂环,含有氮和氧的杂环,或含有氮和硫的杂环; R 3表示(un)取代的低级烷基; Q表示单键或低级亚烷基; Y表示单键,低级亚烷基或低级亚烷基。
Abstract:
The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: wherein R 1 and R 2 are the same or different and an optionally substituted aryl group etc., R 3 is an alkyl group etc., E is one of the following groups of the formula (i) to (iv): Q 1 is a single bond, an alkylene group or a group of the formula: -N(R 7 )-, R 7 is a hydrogen atom or an alkyl group, Q 2 is a single bond, an oxygen atom or an alkylene group, R 4 is a cycloalkyl group, a group of the formula: -N(R 5 )(R 6 ) etc., one of R 5 and R 6 is a hydrogen atom or an alkyl group and the other is an alkyl group, a group of the formula: -N(R 8 )(R 9 ) etc., D is an oxygen atom etc., R A1 is an amino group etc., R A2 is an optionally substituted aliphatic heterocyclic group, R is an alkyl group optionally substituted by one to three halogen atom(s) etc., one of R 8 and R 9 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., or a pharmaceutically acceptable salt thereof.
Abstract:
The present invention relates to a novel pyrazolo[1,5-a]pyrimidine compound of the formula [I]: wherein Ring A is a substituted pyrazole ring fused to the adjacent pyrimidine ring having the following formula (A), (B) or (C), or a pharmaceutically acceptable salt thereof.
Abstract:
Indole derivatives of formula (I) or a pharmaceutically acceptable salt thereof: wherein R 1 is halogen, or alkyl, R 2 is hydrogen, or halogen, Ar is phenyl, or thienyl, which may be substituted with halogen, alkyl, alkoxy, alkylthio, etc.