发明公开
- 专利标题： Guanidine derivatives, processes for their manufacture and pharmaceutical compositions containing them
- 专利标题（中）： 胍衍生物，其制备方法和含有它们的药物组合物。
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申请号： EP80304023.7申请日： 1980-11-11
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公开(公告)号： EP0030092A1公开(公告)日： 1981-06-10
- 发明人: Yellin, Tobias Oregon , Edwards, Philip Neil , Large, Michael Stewart
- 申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI AMERICAS INC.
- 申请人地址： Imperial Chemical House, Millbank London SW1P 3JF GB
- 专利权人： IMPERIAL CHEMICAL INDUSTRIES PLC,ICI AMERICAS INC.
- 当前专利权人： IMPERIAL CHEMICAL INDUSTRIES PLC,ICI AMERICAS INC.
- 当前专利权人地址： Imperial Chemical House, Millbank London SW1P 3JF GB
- 代理机构： Brown, Ivor James Stewart
- 优先权： GB7939232 19791113; GB8012789 19800418; GB8026420 19800813
- 主分类号： C07D277/48
- IPC分类号： C07D277/48 ; C07D213/75 ; C07D231/40 ; C07D239/42 ; C07D239/47 ; C07D239/48 ; C07D241/20 ; C07D251/18 ; C07D285/08 ; C07D403/12 ; C07D417/12
摘要：
The invention relates to a guanidine of the formula:-
in which R 1 and R 2 are H, Ci-io alkyl, C 3-8 cycloalkyl or cycloalkylalkyl in which the alkyl part is C 1-6 and the cycloalkyl part is C 3-8 , each of the alkyl, cycloalkyl and cycloalkylal- kyls being optionally substituted by one or more halogens selected from F, Cl and Br, provided that at least one of R' and R' is a halogen substituted alkyl, cycloalkyl or cycloalkyl-alkyl and provided that there is no halogen substituent on the carbon directly attached to the nitrogen;
ring X is phenyl carrying 1 or 2 optional substitutents or a 5- or 6-membered heterocyclic aromatic ring containing 1, 2 or 3 hetero atoms selected from 0, N and S, which heterocyclic ring may, carry a single optional substituent selected from F, Cl, Br, I, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkylthio, trifluoromethyl, hydroxy and amino;
Y is 0, S, a direct bond, methylene, vinylene, SO or NR 4 in which R 4 is H or C 1-6 alkyl;
m is 0 to 4 and n is 1 to 5, provided that when Y is 0, SO or NR 4 , n is 2 to 5;
R 3 has various significances; and the pharmaceutically-acceptable acid-addition salts thereof.
Manufacturing processes and pharmaceutical compositions are also described.
in which R 1 and R 2 are H, Ci-io alkyl, C 3-8 cycloalkyl or cycloalkylalkyl in which the alkyl part is C 1-6 and the cycloalkyl part is C 3-8 , each of the alkyl, cycloalkyl and cycloalkylal- kyls being optionally substituted by one or more halogens selected from F, Cl and Br, provided that at least one of R' and R' is a halogen substituted alkyl, cycloalkyl or cycloalkyl-alkyl and provided that there is no halogen substituent on the carbon directly attached to the nitrogen;
ring X is phenyl carrying 1 or 2 optional substitutents or a 5- or 6-membered heterocyclic aromatic ring containing 1, 2 or 3 hetero atoms selected from 0, N and S, which heterocyclic ring may, carry a single optional substituent selected from F, Cl, Br, I, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkylthio, trifluoromethyl, hydroxy and amino;
Y is 0, S, a direct bond, methylene, vinylene, SO or NR 4 in which R 4 is H or C 1-6 alkyl;
m is 0 to 4 and n is 1 to 5, provided that when Y is 0, SO or NR 4 , n is 2 to 5;
R 3 has various significances; and the pharmaceutically-acceptable acid-addition salts thereof.
Manufacturing processes and pharmaceutical compositions are also described.
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