5-(Hydroxypyridylalkyl)-4-pyrimidones
First Claim
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1. A pyrimidone of Structure (1):
- ##STR5## in which Het is a 2- or 4-imidazolyl group optionally substituted by lower alkyl, halogen, trifluoromethyl or hydroxymethyl, a 2-pyridyl group optionally substituted by one or more lower alkyl, lower alkoxy, halogen, amino or hydroxy groups, a 2-thiazolyl group, a 3-isothiazolyl group optionally substituted by chlorine or bromine, a 3-(1,2,5)-thiadiazolyl group optionally substituted by chlorine or bromine, or a 2-(5-amino-1,3,4-thiadiazolyl) group;
Y is sulphur or methylene;
Z is hydrogen or lower alkyl;
A is C1 -C5 alkylene; and
Het1 is 4-hydroxy-2-pyridyl, 6-hydroxy-3-pyridyl, 2-hydroxy-4-pyridyl, 4-hydroxy-5-methyl-2-pyridyl, 6-hydroxy-5-methyl-3-pyridyl, 2-hydroxy-6-methyl-4-pyridyl or 6-hydroxy-5-methoxy-3-pyridyl, in the form of the free base or a pharmaceutically acceptable acid addition salt thereof.
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Abstract
The compounds are substituted 2-amino-4-pyrimidones with a 5-(hydroxypyridylalkyl) substituent which are histamine H2 -antagonists. Two specific compounds are 2-[2-(3-bromo-2-pyridylmethylthio)ethylamino]-5-(2-hydroxy-4-pyridylmethyl)-4-pyrimidone and 2-[4-(3-methoxy-2-pyridyl)butylamino]-5-(2-hydroxy-4-pyridylmethyl)-4-pyrimidone.
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Citations
13 Claims
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1. A pyrimidone of Structure (1):
- ##STR5## in which Het is a 2- or 4-imidazolyl group optionally substituted by lower alkyl, halogen, trifluoromethyl or hydroxymethyl, a 2-pyridyl group optionally substituted by one or more lower alkyl, lower alkoxy, halogen, amino or hydroxy groups, a 2-thiazolyl group, a 3-isothiazolyl group optionally substituted by chlorine or bromine, a 3-(1,2,5)-thiadiazolyl group optionally substituted by chlorine or bromine, or a 2-(5-amino-1,3,4-thiadiazolyl) group;
Y is sulphur or methylene;
Z is hydrogen or lower alkyl;
A is C1 -C5 alkylene; and
Het1 is 4-hydroxy-2-pyridyl, 6-hydroxy-3-pyridyl, 2-hydroxy-4-pyridyl, 4-hydroxy-5-methyl-2-pyridyl, 6-hydroxy-5-methyl-3-pyridyl, 2-hydroxy-6-methyl-4-pyridyl or 6-hydroxy-5-methoxy-3-pyridyl, in the form of the free base or a pharmaceutically acceptable acid addition salt thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13)
- ##STR5## in which Het is a 2- or 4-imidazolyl group optionally substituted by lower alkyl, halogen, trifluoromethyl or hydroxymethyl, a 2-pyridyl group optionally substituted by one or more lower alkyl, lower alkoxy, halogen, amino or hydroxy groups, a 2-thiazolyl group, a 3-isothiazolyl group optionally substituted by chlorine or bromine, a 3-(1,2,5)-thiadiazolyl group optionally substituted by chlorine or bromine, or a 2-(5-amino-1,3,4-thiadiazolyl) group;
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Current AssigneeSmith Kline & French Laboratories Limited (GSK plc)
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Original AssigneeSmith Kline & French Laboratories Limited (GSK plc)
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InventorsDurant, Graham J., Ganellin, Charon R., Brown, Thomas H.
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Primary Examiner(s)Daus, Donald G.
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Assistant Examiner(s)Turnipseed, James H.
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Application NumberUS06/032,979Time in Patent Office686 DaysField of Search544/320, 424/251US Class Current514/272CPC Class CodesC07D 401/14 containing three or more he...C07D 417/14 containing three or more he...
