US4238487A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Aminoalkyl benzofuran derivatives
Assignee: Merck and Co Inc
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Filing: 1979-10-31
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Granted: 1980-12-09
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Expires: 1999-10-31
Abstract
Abstract There are disclosed novel compounds described as aminoalkyl benzofuran derivatives in which the aminoalkyl benzofuran is connected to a guanidine moiety or functional equivalent thereof through a linear connecting group. Processes for the preparation of such compounds are also disclosed. The compounds are useful for the suppression of gastric acid secretions in mammals and compositions for such uses are also disclosed.
Inventors
- 👤 John B. Bicking
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-28 23:04
CPC Classifications
C; C07; C07D; C07D307/00; C07D307/77; C07D307/78; C07D307/79; A; A61; A61P; A61P7/00; A61P7/06; C07D307/81
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
99 words
A compound having the formula: ##STR20## wherein R 1 and R 2 are independently loweralkyl of from 1 to 3 carbon atoms, and R 1 and R 2 may be joined to form, together with the nitrogen atom to which they are attached, heterocycle selected from piperidine, pyrrolidine, morpholine, piperazine, and N-methylpiperazine; X is sulfur or a methylene group; n is 2, 3, or 4; R 3 is hydrogen, lower alkyl, cycloloweralkyl, cycloloweralkyl lower alkyl, loweralkenyl, loweralkynyl, phenylloweralkyl, hydroxyloweralkyl, loweralkoxyloweralkyl, and di(loweralkyl)aminoloweralkyl; and Y is sulfur, ═CHNO 2 or ═NR 4 wherein R 4 is nitro, cyano, or loweralkylsulfonyl.
Claim 2
Dependent Claim
99 words
A compound having the formula: ##STR20## wherein R 1 and R 2 are independently loweralkyl of from 1 to 3 carbon atoms, and R 1 and R 2 may be joined to form, together with the nitrogen atom to which they are attached, heterocycle selected from piperidine, pyrrolidine, morpholine, piperazine, and N-methylpiperazine; X is sulfur or a methylene group; n is 2, 3, or 4; R 3 is hydrogen, lower alkyl, cycloloweralkyl, cycloloweralkyl lower alkyl, loweralkenyl, loweralkynyl, phenylloweralkyl, hydroxyloweralkyl, loweralkoxyloweralkyl, and di(loweralkyl)aminoloweralkyl; and Y is sulfur, ═CHNO 2 or ═NR 4 wherein R 4 is nitro, cyano, or loweralkylsulfonyl.
Claim 3
Dependent Claim
12 words
The compound of claim 1 wherein the heterocycle is piperidine or pyrrolidine.
Claim 4
Dependent Claim
44 words
The compound of claim 1 wherein: R 1 and R 2 are the same and are loweralkyl of from 1 to 3 carbon atoms; X is sulfur; n is 2; R 3 is hydrogen, loweralkyl, or loweralkynyl; and Y is ═CHNO 2 or ═N-CN.
Claim 5
Dependent Claim
34 words
The compound of claim 3 wherein: R 1 and R 2 are methyl; X is sulfur; n is 2; R 3 is hydrogen, methyl, ethyl or propargyl; and Y is ═CH-NO 2 or ═N-CN.
Claim 6
Dependent Claim
32 words
The compound of claim 4 wherein: R 1 and R 2 are methyl; X is sulfur; n is 2; R 3 is hydrogen or methyl; and R is ═CH-NO 2 or ═N-CN.
Claim 7
Dependent Claim
8 words
The compound of claim 5 which is N-cyano-N'-[2-(6-dimethylaminomethyl-2-benzofuranylmethylthio)-ethyl]-N"-methyl-guanidine.
Claim 8
Dependent Claim
8 words
The compound of claim 5 which is N-[2-(6-dimethylaminomethyl-2-benzofuranylmethylthio)ethyl]-N'-methyl-2-nitro-1,1-ethenediamine.
Claim 9
Dependent Claim
30 words
A method for the treatment of excess gastric acid secretions which comprises administering to a mammal with excess gastric acid secretions, an effective amount of a compound of claim 1.
Claim 10
Dependent Claim
26 words
A composition useful for the treatment of excess gastric acid secretions which comprises an inert carrier and an effective amount of a compound of claim 1.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1983-12-09 | 1984-06-09 | 1984-12-09 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-12-09 | 1988-06-09 | 1988-12-09 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-12-09 | 1992-06-09 | 1992-12-09 | $7700.00 | Window Closed / Lapsed |