US4018928A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Pyridyl substituted aminoalkyl-thioureas and ureas
Assignee: Smith Kline & French Laboratories Ltd
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Filing: 1975-10-29
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Granted: 1977-04-19
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Expires: 1995-10-29
Abstract
Abstract The compounds are pyridyl substituted aminoalkylthioureas and ureas which are inhibitors of H-2 histamine receptors. A compound of this invention is N-methyl-N'-[2-(2-pyridylmethylamino)ethyl]thiourea.
Inventors
- 👤 Graham John Durant
- 👤 John Colin Emmett
- 👤 Charon Robin Ganellin
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 15:03
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/62; C07D213/70; C07D213/24; C07D213/28; C07D213/32; C07D213/36; C07D213/38; C07D213/63; C07D213/65; C07D213/72; C07D213/74; C07D231/00; C07D231/02; C07D231/10; C07D231/12; C07D233/00; C07D233/54; C07D233/66; C07D233/84; C07D233/90; C07D235/00; C07D235/02; C07D235/04; C07D235/06; C07D249/00; C07D249/02; C07D249/08; C07D249/10; C07D249/12; C07D261/00; C07D261/02; C07D261/06; C07D261/08; C07D263/00; C07D263/02; C07D263/30; C07D263/34; C07D263/46; C07D275/00; C07D275/02; C07D275/03; C07D277/00; C07D277/02; C07D277/20; C07D277/22; C07D277/26; C07D285/00; C07D285/01; C07D285/02; C07D285/04; C07D285/12; C07D285/125; C07D285/135; C07D471/00; C07D471/02; C07D471/04
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
127 words
A pharmaceutical composition to inhibit H-2 histamine receptors, said composition being suitable for oral or parenteral administration, comprising a pharmaceutical carrier and in an effective amount to inhibit said receptors a pyridyl compound of the formula: ##STR8## wherein A is such that there is formed together with the carbon atom shown a pyridine ring; X 1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, halogen, amino or ##STR9## X 2 is hydrogen or when X 1 is lower alkyl, lower alkyl or halogen; k is 1 or 2 and m is 2 or 3, provided that the sum of k and m is 3 or 4; Y is NH; E is oxygen or sulphur; R 1 is hydrogen, lower alkyl, or dimethylaminoethyl or a pharmaceutically acceptable addition salt thereof.
Claim 2
Dependent Claim
127 words
A pharmaceutical composition to inhibit H-2 histamine receptors, said composition being suitable for oral or parenteral administration, comprising a pharmaceutical carrier and in an effective amount to inhibit said receptors a pyridyl compound of the formula: ##STR8## wherein A is such that there is formed together with the carbon atom shown a pyridine ring; X 1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, halogen, amino or ##STR9## X 2 is hydrogen or when X 1 is lower alkyl, lower alkyl or halogen; k is 1 or 2 and m is 2 or 3, provided that the sum of k and m is 3 or 4; Y is NH; E is oxygen or sulphur; R 1 is hydrogen, lower alkyl, or dimethylaminoethyl or a pharmaceutically acceptable addition salt thereof.
Claim 3
Dependent Claim
13 words
A pharmaceutical composition of claim 1 in which the pyridyl compound is N-methyl-N'-[3-(2-pyridyl-amino)-propyl]thiourea.
Claim 4
Dependent Claim
14 words
A pharmaceutical composition of claim 1 wherein k is 1 and m is 2.
Claim 5
Dependent Claim
29 words
A pharmaceutical composition of claim 3 wherein X 1 is hydrogen, methyl, bromo, hydroxyl or amino and X 2 is hydrogen; E is sulphur and R 1 is methyl.
Claim 6
Dependent Claim
13 words
A pharmaceutical composition of claim 1 in which the pyridyl compound is N-methyl-N'-[2-(2-pyridylmethylamino)-ethyl]thiourea.
Claim 7
Dependent Claim
25 words
A pharmaceutical composition of claim 1 in which the pyridyl compound is present in an amount of from about 50 mg. to about 250 mg.
Claim 8
Independent Claim
125 words
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 pyridyl compound of the formula: ##STR10## wherein A is such that there is formed together with the carbon atom shown a pyridine ring; X 1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, halogen, amino or ##STR11## X 2 is hydrogen or when X 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 NH; E is oxygen or sulphur; R 1 is hydrogen, lower alkyl, or dimethylaminoethyl or a pharmaceutically acceptable addition salt thereof.
Claim 9
Independent Claim
125 words
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 pyridyl compound of the formula: ##STR10## wherein A is such that there is formed together with the carbon atom shown a pyridine ring; X 1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, halogen, amino or ##STR11## X 2 is hydrogen or when X 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 NH; E is oxygen or sulphur; R 1 is hydrogen, lower alkyl, or dimethylaminoethyl or a pharmaceutically acceptable addition salt thereof.
Claim 10
Dependent Claim
12 words
A method of claim 7 in which the pyridyl compound is N-methyl-N'-[3-(2-pyridylamino)propyl]thiourea.
Claim 11
Dependent Claim
12 words
A method of claim 7 in which the pyridyl compound is N-methyl-N'-[2-(2-pyridylmethylamino)ethyl]thiourea.
Claim 12
Dependent Claim
25 words
A method of claim 7 in which the pyridyl compound is administered in a daily dosage of from about 150 mg. to about 750 mg.
Claim 13
Independent Claim
128 words
A method of inhibiting gastric acid secretion which comprises administering internally to an animal in need of inhibition of gastric acid secretion in an effective amount to inhibit gastric acid secretion a pyridyl compound of the formula: ##STR12## wherein A is such that there is formed together with the carbon atom shown a pyridine ring; X 1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, halogen, amino or ##STR13## X 2 is hydrogen or when X 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 NH; E is oxygen or sulphur; R 1 is hydrogen, lower alkyl, or dimethylaminoethyl or a pharmaceutically acceptable addition salt thereof.
Claim 14
Independent Claim
128 words
A method of inhibiting gastric acid secretion which comprises administering internally to an animal in need of inhibition of gastric acid secretion in an effective amount to inhibit gastric acid secretion a pyridyl compound of the formula: ##STR12## wherein A is such that there is formed together with the carbon atom shown a pyridine ring; X 1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, halogen, amino or ##STR13## X 2 is hydrogen or when X 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 NH; E is oxygen or sulphur; R 1 is hydrogen, lower alkyl, or dimethylaminoethyl or a pharmaceutically acceptable addition salt thereof.
References Cited (Backward Citations)
US3535328A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1980-04-18 | 1980-10-18 | 1981-04-19 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-04-18 | 1984-10-18 | 1985-04-19 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-04-18 | 1988-10-18 | 1989-04-19 | $7700.00 | Window Closed / Lapsed |