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Generated: September 26, 2017
| Title: | Pharmacologically active thiourea and urea compounds |
| Abstract: | The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity. |
| Inventor(s): | Durant; Graham John (Welwyn Garden City, EN), Emmett; John Colin (Codicote, EN), Ganellin; Charon Robin (Welwyn Garden City, EN) |
| Assignee: | Smith Kline & French Laboratories Limited (Welwyn Garden City, EN) |
| Filing Date: | Dec 05, 1975 |
| Application Number: | 05/638,005 |
| Claims: | 1. A compound of the formula: ##STR28## wherein A is such that there is formed together with the carbon atom shown an unsaturated heterocyclic nucleus, said unsaturated heterocyclic nucleus being a pyrimidine, pyrazine or pyridazine ring; X.sub.1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, benzyl, halogen, amino or ##STR29## X.sub.2 is hydrogen or when X.sub.1 is lower alkyl, lower alkyl or halogen; k is 0 to 2 and m is 2 or 3, provided that the sum of k and m is 3 or 4; Y is oxygen, sulphur or NH; E is oxygen or sulphur; and R.sub.1 is hydrogen, lower alkyl, benzoyl or di-lower alkylamino-lower alkyl or a pharmaceutically acceptable addition salt thereof. 2. A compound of claim 1 wherein Y is oxygen or sulphur. 3. A compound of claim 1 wherein Y is NH. 4. A compound of claim 1 wherein k is 1 and m is 2. 5. A compound of claim 1 in which X.sub.1 is hydrogen, methyl, bromo, hydroxyl or amino and X.sub.2 is hydrogen; Y and E are sulphur and R.sub.1 is methyl. 6. A compound of claim 1 wherein X.sub.1 is hydrogen, lower alkyl, trifluoromethyl, benzyl, halogen or ##STR30## X.sub.2 is hydrogen or when X.sub.1 is lower alkyl, lower alkyl or halogen; k is 0 and 2 and m is 2 or 3, provided that the sum of k and m is 3 or 4; Y is oxygen or sulphur; E is oxygen or sulphur and R.sub.1 is hydrogen, lower alkyl, benzoyl or di-lower alkylamino-lower alkyl or a pharmaceutically acceptable addition salt thereof. 7. A compound of claim 1, said compound, being N-methyl N'-[-2-(2-pyrazinylmethylthio)ethyl]thiourea. 8. A compound of claim 1, said compound being N-methyl-N'-[2-(3-pyridazinylmethylthio)ethyl]thiourea. |
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