Abstract:
PROBLEM TO BE SOLVED: To provide a novel metalloprotease inhibitor that is useful for treating rheumatoid arthritis and the like, a method of producing the same and medicinal composition containing the same. SOLUTION: This invention relates to a novel compound represented by formula (I) [wherein R1 is H or the like; X is O or the like; A represents the compound represented by formula A (wherein Ra is H or the like) or the like], an isomer thereof, an N-oxide thereof and a pharmaceutically acceptable adduct salt.
Abstract:
PROBLEM TO BE SOLVED: To provide a compound having a specific structure, selectively inhibiting FTase with respect to GGTase and useful for the treatment of diseases relating to the intracellular signal transduction through Ras protein, etc., and the investigation of pathology relating to angiogenetic amplification. SOLUTION: The objective compound is expressed by formula (I) [X is a bond, an alkylene, S(O)n or the like; Y is an aryl, a heteroaryl or the like; R1 to R4 are each independently H, an aryl or the like or together form a bond, a condensed benzene ring or the like; T is CH(R5 ) (R5 is H or the like) or the like; V is H, a substituted aryl or the like; A2 is [C(R6 ) (R'6 )] (R6 and R'6 are each H or the like; and (p) is 0-4); and R7 and R8 are each H or the like]. The invention further relates to its isomer, diastereomer, pharmacologically permissible acid or base and its addition salt.
Abstract:
Compounds of formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 80 , R 90 , R 81 , R 91 , AIk and G are such as defined in the description, can be used for drugs.
Abstract:
A compound having formula (I), wherein X denotes an alkylene group or chain, CO, S(O)n, -S(O)n-A1-, -CO-A1-, -A1-S(O)n-A'1, or A1-CO-A'1-; Y denotes a substituted or non-substituted aryl, heteroaryl, cycloalkyl or heterocyclalkyl group; W denotes a CO or CH2 group; T denotes a N(R1)- or N(R1)CO- group; V denotes a hydrogen atom or a substituted or non-substituted aryl or heteroaryl group; A2 denotes a [C(R2)(R'2)]p group; R1 and R2 are as defined in the description. Medicaments.
Abstract:
The invention concerns a compound of formula (I), wherein: (a) represents a single or double bond; (b) represents a cycle selected among (i), (ii), (iii), (iv) and (v); R9a, R9b, R9c, X and Y are such as defined in the description; R1 represents a group selected among hydrogen, aryl, heteroaryl, cycloalkyl, alkyl optionally substituted, and COR11, wherein R11 is such as defined in the description; R2 to R8 represent each a group selected among hydrogen, halogen, hydroxy, polyhalogenoalkyl, nitro, alkyl optionally substituted, amino optionally substituted, alkoxy optionally substituted, -OPO(OH)2 and (II), wherein m represents an integer such that 1
Abstract translation:本发明涉及式(I)化合物,其中:(a)表示单键或双键; (b)表示选自(i),(ii),(iii),(iv)和(v)中的循环; R9a,R9b,R9c,X和Y如描述中所定义; R 1表示选自氢,芳基,杂芳基,环烷基,任选取代的烷基和COR 11中的基团,其中R 11如说明书中所定义; R 2至R 8表示选自氢,卤素,羟基,多卤代烷基,硝基,任选取代的烷基,任选取代的氨基,任选取代的烷氧基,-OPO(OH)2和(II)中的基团,其中m表示1 R 3或具有R 4的R 3或具有R 5的R 4一起与含有任选含有1或2个杂原子并任选取代的单环或双环基团的碳原子一起形成; R 16表示氢原子或烷基; (c)表示芳基,杂芳基或芳基烷基; 以及其光学异构体,其与药学上可接受的酸或碱的加成盐以及其水合物和溶剂合物。 本发明可用于制备药物。
Abstract:
Compounds of formula (I): X R4 N RS I ( ) wherein: * m and n represent 1 or 2, * A represents a pyrrolyl group, * X represents a C(O), S(O) or SO 2 group, + R and R2 represent an alkyl group or, together with the nitrogen atom carrying them, form a heterocyclic group, + R3 and R4, together with the atoms carrying them, form a heterocyclic group, + R5 represents a hydrogen atom or an alkyl group, + R represents a hydrogen atom or a halogen atom. The compounds are used in pharmaceutical compositions and in the preparation of medicaments for use in the treatment of cancer.
Abstract:
Compounds of formula (I), wherein R1, R2, R3, R4, R5, R80, R81, R90, R91, Alk, Alk1, X, X1 and G are such as defined in the description, method for its production, pharmaceutical compositions on its base and use thereof for preparation of medicaments for treating cancer.