发明授权
- 专利标题: Pyrimidone derivatives
- 专利标题(中): 嘧啶衍生物
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申请号: US58256申请日: 1979-07-17
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公开(公告)号: US4524071A公开(公告)日: 1985-06-18
- 发明人: Barry J. Price , John W. Clitherow , John Bradshaw , Michael Martin-Smith , Duncan B. Judd , Roger Hayes
- 申请人: Barry J. Price , John W. Clitherow , John Bradshaw , Michael Martin-Smith , Duncan B. Judd , Roger Hayes
- 申请人地址: GB2 London
- 专利权人: Glaxo Group Limited
- 当前专利权人: Glaxo Group Limited
- 当前专利权人地址: GB2 London
- 优先权: GBX31153/78 19780726
- 主分类号: A61K31/505
- IPC分类号: A61K31/505 ; A61P27/16 ; A61P29/00 ; A61P37/08 ; C07D213/65 ; C07D215/12 ; C07D239/46 ; C07D239/47 ; C07D239/56 ; C07D307/52 ; C07D401/06 ; C07D401/12 ; C07D403/06 ; C07D405/12 ; C07D405/14 ; C07D409/14
摘要:
Compounds of the formula (I) ##STR1## in which R.sub.1 and R.sub.2 each may represent hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, or alkyl, substituted by hydroxy, C.sub.1-3 alkoxy, amino, C.sub.1-3 alkylamino or di-C.sub.1-3 alkylamino or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form an alicyclic heterocyclic ring which may be unsubstituted or may be substituted by one or more C.sub.1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom are described.Alk is a straight lower alkylene chain,Q is a furan or thiophen ring, the furan ring optionally bearing a further substituent R.sub.5 adjacent to the group R.sub.1 R.sub.2 NAlk-- or Q represents a benzene ring.R.sub.5 represents halogen or C.sub.1-3 alkyl which may be substituted by a hydroxy or C.sub.1-3 alkoxy group;X represents --CH.sub.2 --, --O-- or --S--;n represents zero or 1;m represents 2, 3 or 4;Y represents .dbd.O or .dbd.S;R.sub.3 represents hydrogen in which case R.sub.4 represents methyl or R.sub.3 represents --(CH.sub.2).sub.p V(CH.sub.2).sub.q Ar, phenyl, or alkyl in which case R.sub.4 represents hydrogen;V represents --CH.sub.2 --, --O--, or --S--;p represents zero, 1, 2 or 3;q represents zero, 1, 2 or 3;the sum of p+q being 3 or less;Ar represents an aromatic carbocyclic or heterocyclic ring being optionally substituted by at least one C.sub.1-3 alkyl, C.sub.1-3 alkoxy C.sub.1-3 alkyl, hydroxy, C.sub.1-3 alkoxy, methylenedioxy, halogen, trifluoromethyl or di-C.sub.1-3 alkylamino group;except that when n is zero and X is oxygen then Q represents a benzene or thiophen ring. The compounds of formula (I) have pharmacological activity as selective histamine H.sub.2 -antagonists.