Serving 500+ biopharmaceutical companies globally:
Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing
Serving 500+ biopharmaceutical companies globally:
Generated: June 24, 2017
| Title: | Inhibitors of H-2 histamine receptors |
| Abstract: | The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity. |
| Inventor(s): | Durant; Graham J. (Welwyn Garden City, GB2), Emmett; John C. (Codicote, GB2), Ganellin; Charon R. (Welwyn Garden City, GB2) |
| Assignee: | Smith Kline & French Laboratories Limited (Welwyn Garden City, GB2) |
| Filing Date: | Mar 17, 1980 |
| Application Number: | 06/130,760 |
| Claims: | 1. A method of inhibiting H-2 histamine receptors which comprises administering to an animal in need of inhibition of said receptors in an effective amount to inhibit said receptors a heterocyclic 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 5,6,7,8-tetrahydroimidazo[1,5-a]pyridine 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 pharmaceutical composition to inhibit H-2 histamine receptors comprising a pharmaceutical carrier and in an effective amount to inhibit said receptors a heterocyclic compound of the formula: ##STR30## wherein A is such that there is formed together with the carbon atom shown an unsaturated heterocyclic nucleus, said unsaturated heterocyclic nucleus being a 5,6,7,8-tetrahydroimidazo[1,5-a]pyridine ring; X.sub.1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, benzyl halogen, amino or ##STR31## 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. 3. A pharmaceutical composition of claim 2 in which the heterocyclic compound is N-methyl-N'-[2-(3-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridyl)methylthio)ethy l]thiourea. 4. A pharmaceutical composition of claim 2 in which the pharmaceutical composition is in the form of a tablet or capsule. 5. A pharmaceutical composition of claim 2 in which the heterocyclic compound is present in an amount of from about 50 mg. to about 250 mg. 6. A method of claim 1 in which the heterocyclic compound is N-methyl-N'-[2-(3-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridyl)methylthioethyl ]thiourea. 7. A method of claim 1 in which the heterocyclic compound is administered orally. 8. A method of claim 1 in which the heterocyclic compound is administered in a daily dosage regimen of from about 150 mg. to about 1000 mg. 9. A method of inhibiting gastric acid secretion which comprises administering to an animal in need thereof in an effective amount to inhibit gastric acid secretion a heterocyclic compound of the formula: ##STR32## wherein A is such that there is formed together with the carbon atom shown an unsaturated heterocyclic nucleus, said unsaturated heterocyclic nucleus being a 5,6,7,8-tetrahydroimidazo[1,5-a]pyridine ring; X.sub.1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, benzyl, halogen, amino or ##STR33## 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. |
Serving 500+ biopharmaceutical companies globally:
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.
Copyright 2002-2017 thinkBiotech LLC
ISSN: 2162-2639
Follow DrugPatentWatch:
Join the 21,683 other biopharmaceutical professionals who get our Drug Patent Expiration Alerts:
