发明授权
US5703115A �(benzodioxan, benzofuran or benzopyran) alkylamino! alkyl substituted
guanidines
失效
[(苯并二恶烷,苯并呋喃或苯并吡喃)烷基氨基]烷基取代的胍
- 专利标题: �(benzodioxan, benzofuran or benzopyran) alkylamino! alkyl substituted guanidines
- 专利标题(中): [(苯并二恶烷,苯并呋喃或苯并吡喃)烷基氨基]烷基取代的胍
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申请号: US632230申请日: 1996-04-15
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公开(公告)号: US5703115A公开(公告)日: 1997-12-30
- 发明人: Guy Rosalia Eugene Van Lommen , Marcel Frans Leopold De Bruyn , Walter Jacobus Joseph Janssens
- 申请人: Guy Rosalia Eugene Van Lommen , Marcel Frans Leopold De Bruyn , Walter Jacobus Joseph Janssens
- 申请人地址: BEX Beerse
- 专利权人: Janssen Pharmaceutica, N.V.
- 当前专利权人: Janssen Pharmaceutica, N.V.
- 当前专利权人地址: BEX Beerse
- 主分类号: C07D307/81
- IPC分类号: C07D307/81 ; C07D311/58 ; C07D319/20 ; C07D405/12 ; C07D405/14 ; A61K31/34 ; A61K31/35
摘要:
The present invention is concerned with vasoconstricive �benzodioxan, benzofuran or benzopyran)alkylamino!alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is a bivalent C.sub.1-3 alkanediyl radical; A is a bivalent radical of formula: ##STR2## wherein each R.sup.5 is hydrogen or C.sub.1-4 alkyl; wherein each R.sup.6 is hydrogen or C.sub.1-4 alkyl; Alk.sup.2 is C.sub.2-15 alkanediyl or C.sub.5-7 cycloalkanediyl; and each p is 0, 1 or 2; provided that �2-�(2,3-dihydro-1,4-benzodioxin-2-yl)methyl!amino!ethyl guanidine is excluded. Pharmaceuticals which are useful as vasoconstrictors. Compositions comprising said guanidine derivatives as active ingredients, processes for preparing said guanidine derivatives and novel N-cyano guanidine, intermediates; and a use as a medicine are described.
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