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115 条记录 (耗时 0.067 秒)

    ALKYLIDENEIMIDAZOLE DERIVATIVE
    1.
    发明专利
    ALKYLIDENEIMIDAZOLE DERIVATIVE 失效

    公开(公告)号：JPH06279437A

    公开(公告)日：1994-10-04

    申请号：JP9091293

    申请日：1993-03-25

    申请人： YAMANOUCHI PHARMA CO LTD

    发明人： KIKUCHI KAZUMI ,  WATANABE TOSHIHIRO ,  OKAZAKI TOSHIO ,  YANAGISAWA ISAO ,  INAGAKI OSAMU

    IPC分类号： A61K31/415 ,  A61K31/44 ,  A61K31/4427 ,  A61P9/00 ,  A61P9/12 ,  A61P43/00 ,  C07D401/14 ,  C07D403/10

    摘要： PURPOSE:To produce the subject new derivative (or a salt thereof) having excellent anti-angiotensin II activity, thus useful as an angiotensin II antagonistic agent for treating hypertension and chronic cardiac insufficiency, etc. CONSTITUTION:An alkylideneimidazole derivative (or a salt thereof) of formula I [R is cycloalkyl, lower alkyl or formula A-X-R (A is single bond or lower alkylene; X is O or S; R is lower alkyl); R and R are each lower alkyl, phenyl or pyridyl; R is H or aralkyl], e.g. 2-cyclopropyl-4-isopropylidene-5-oxo-1-[[2'-(N- triphenylmethyl-1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-4,5-dihydro-1H- imidazole. The compound of the formula I can be obtained, for example, by reaction of an imidazole derivative of formula II with a biphenylmethyl halide of formula III in an appropriate solvent. The compound III is reduced or treated with an acid to obtain another version of this compound (where, R is H).

    NEW PYRAZOLOTRIAZOLE DERIVATIVE OR ITS SALT
    2.
    发明专利
    NEW PYRAZOLOTRIAZOLE DERIVATIVE OR ITS SALT 失效

    公开(公告)号：JPH06256349A

    公开(公告)日：1994-09-13

    申请号：JP6752593

    申请日：1993-03-02

    申请人： YAMANOUCHI PHARMA CO LTD

    发明人： OKAZAKI TOSHIO ,  SUGA AKIRA ,  WATANABE TOSHIHIRO ,  YANAGISAWA ISAO

    IPC分类号： A61K31/415 ,  A61P9/12 ,  C07D487/04

    摘要： PURPOSE:To obtain a new compound useful as an intermediate for pyrazolotriazole derivatives having angiotensin II antagonistic activity. CONSTITUTION:A compound of formula I (R is hydroxy lower alkyl, lower acyloxy lower alkyl or carboxyl; R is H or lower alkyl; R is H or lower alkyl), e.g. 6-acetyloxymethyl-2,7-diethyl-1H-pyrazolo[1,5-b][1,2,4]triazole. This compound of formula I can be obtained by bringing a compound of formula II (R and R are each lower alkyl; A is lower alkylene) under acidic condition followed by dealkylation using an oxidizing agent such as hydrobromic acid or by acyloxidation using e.g. acetic acid. The compound of formula I can be led to a pyrazolotriazole derivative of formula III.

    SULFAMOYLAMIDINE DERIVATIVE AND ITS PREPARATION
    5.
    发明专利
    SULFAMOYLAMIDINE DERIVATIVE AND ITS PREPARATION 失效

    公开(公告)号：JPS60197663A

    公开(公告)日：1985-10-07

    申请号：JP5389184

    申请日：1984-03-21

    申请人： YAMANOUCHI PHARMA CO LTD

    发明人： YANAGISAWA ISAO ,  OOTA MITSUAKI ,  TAKAGI TOKUICHI

    IPC分类号： C07D295/08 ,  A61K31/445 ,  A61P1/04

    摘要： NEW MATERIAL:The sulfamoylamidine derivative of formula I (R is H or lower alkyl; n is 2, 3 or 4) or its acid addition salt. EXAMPLE:4-[ m-( piperidinomethyl )phenoxy ]-N -sulfamoylbutylamidine dihydrochloride. USE:A gastric juice secretion suppressing agent based on histamine H2 receptor antagonistic activity, and free from the side effect caused by anticholine activity. PREPARATION:The compound of formula I can be prepared by reacting the imidate derivative of formula II (R' is lower alkyl) with the sulfamide derivative of formula III. When a compound of formula III wherein R is H is used as the starting material, the dimer of formula IV is also produced as a by-product, which is, however, separable easily from the compound of formula I taking advantage of the difference in the physical and chemical properties between the compound of formula I .