NOVEL 5-PYRROLYL-2-PYRIDYLMETHYLSULFINYL BENZIMIDAZOLE DERIVATIVES
    2.
    发明申请
    NOVEL 5-PYRROLYL-2-PYRIDYLMETHYLSULFINYL BENZIMIDAZOLE DERIVATIVES 审中-公开
    新型5-苯基-2-吡啶基甲基苯乙烯苯并咪唑衍生物

    公开(公告)号:WO1995023140A1

    公开(公告)日:1995-08-31

    申请号:PCT/KR1994000098

    申请日:1994-07-22

    CPC classification number: C07D401/14

    Abstract: The present invention relates to a novel compound 5-pyrrolyl-2-pyridylmethylsulfinylbenzimidazole derivative having general formula (I) and its salt, in which X represents S, SO or SO2, R1 and R2 independently from each other represent hydrogen or alkyl, R3 represents hydrogen, C1-C8 alkyl, -SR6, -N(R7)2, 1-piperidinyl, 4-morpholinyl, 4-methylpiperazin-1-yl, 1-pyrrolidinyl, -OR6, or -O(CH2)m-Z, wherein R6 represents C1-C4 alkyl, C2-C4 alkenyl, C3-C10 cycloalkyl, C2-C5 fluoroalkyl, or phenyl or benzyl, each of which independently substituted with one or more halogen or C1-C4 alkyl or alkoxy optionally substituted with halogen, R7 represents hydrogen or C1-C5 alkyl, Z represents a group -O(CH2)p-OR8, -O(CH2)q-R9 or -O(CH2)rO(CH2)s-OR10, wherein p and q independently from each other denote an integer of 1 to 3, r and s independently from each other denote an integer of 1 to 5, R8 represents hydrogen, lower alkyl, aryl or aralkyl, R9 represents hydrogen, alkoxycarbonyl, aryl or heteroaryl, and R10 represents hydrogen or lower alkyl, m represents an integer of 2 to 10, and R4 and R5 independently from each other represent hydrogen or C1-C5 alkyl, or when R4 and R5 together with the carbon atoms adjacent with pyridine ring form a ring, R4 and R3 or R3 and R5 represent -CH=CH-CH=CH-, -O(CH2)n-, -O(CH2)nO-, -CH2(CH2)n- or -OCH=CH-, wherein n denotes an integer of 1 to 4. The present invention also relates to a process for preparation of the compound of formula (I), as defined above, and its use as an anti-ulcer agent.

    Abstract translation: 本发明涉及具有通式(I)的新化合物5-吡咯基-2-吡啶基甲基亚磺酰基苯并咪唑衍生物及其盐,其中X表示S,SO或SO 2,R 1和R 2彼此独立地表示氢或烷基,R 3表示 氢,C1-C8烷基,-SR6,-N(R7)2,1-哌啶基,4-吗啉基,4-甲基哌嗪-1-基,1-吡咯烷基,-OR6或-O(CH2)mZ,其中R6 表示C1-C4烷基,C2-C4烯基,C3-C10环烷基,C2-C5氟代烷基或苯基或苄基,其各自独立地被一个或多个卤素或任选被卤素取代的C 1 -C 4烷基或烷氧基取代,R 7表示 氢或C 1 -C 5烷基,Z表示基团-O(CH 2)p -OR 8,-O(CH 2)q -R 9或-O(CH 2)r O(CH 2)s-OR 10,其中p和q彼此独立地 表示1〜3的整数,r和s彼此独立地表示1〜5的整数,R8表示氢,低级烷基,芳基或芳烷基,R9表示氢,烷氧基羰基,芳基或杂芳基, R 10表示氢或低级烷基,m表示2〜10的整数,R4和R5彼此独立地表示氢或C1-C5烷基,或当R4和R5与与吡啶环相邻的碳原子形成环时 ,R 4和R 3或R 3和R 5表示-CH = CH-CH = CH-,-O(CH 2)n - , - O(CH 2)n O-,-CH 2(CH 2)n - 或-OCH = CH-,其中 n表示1〜4的整数。本发明还涉及如上定义的式(I)化合物的制备方法及其作为抗溃疡剂的用途。

Patent Agency Ranking