US4144338A
Expired / Lapsed
US
⏱️ 0.0 years remaining
N-pyrimidinyl-N-dialkylaminoalkyl ureas
Assignee: Merck and Co Inc
•
Filing: 1977-02-17
•
Granted: 1979-03-13
•
Expires: 1997-02-17
Abstract
Abstract Organic chemical compounds based upon the urea molecule are disclosed which have potent gastric secretion inhibitory properties. The urea is substituted with a 6 membered heterocyclic substituent containing 2 or 3 heteroatoms, and also with a substituted amino alkyl group. Further substitution is also possible. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.
Inventors
- 👤 William A. Bolhofer
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 14:39
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/46; C07D239/47; A; A61; A61P; A61P1/00; A61P1/04; C07D239/32; C07D239/42; C07D239/48; C07D241/00; C07D241/02; C07D241/10; C07D241/14; C07D241/20; C07D251/00; C07D251/02; C07D251/12; C07D251/14; C07D251/22
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
88 words
A compound having the formula: ##STR12## wherein R is pyrimidinyl which may be optionally substituted with from 1 to 3 of loweralkyl, halo, hydroxy, amino, mono or di-loweralkylamino, loweralkoxy or phenylloweralkoxy; R 1 and R 2 are independently loweralkyl; R 3 and R 4 are independently hydrogen or loweralkyl; X is oxygen or sulfur; and n is an integer of from 2 to 6, such that the direct linkage between the nitrogen atoms is either two or three carbon atoms, and the pharmaceutically acceptable acid addition salts thereof.
Claim 2
Dependent Claim
88 words
A compound having the formula: ##STR12## wherein R is pyrimidinyl which may be optionally substituted with from 1 to 3 of loweralkyl, halo, hydroxy, amino, mono or di-loweralkylamino, loweralkoxy or phenylloweralkoxy; R 1 and R 2 are independently loweralkyl; R 3 and R 4 are independently hydrogen or loweralkyl; X is oxygen or sulfur; and n is an integer of from 2 to 6, such that the direct linkage between the nitrogen atoms is either two or three carbon atoms, and the pharmaceutically acceptable acid addition salts thereof.
Claim 3
Dependent Claim
44 words
The compound of claim 1 wherein R is pyrimidinyl, optionally substituted with 1 to 3 of methyl, chloro or dimethylamino; R 1 , r 2 , r 3 and R 4 are independently methyl, ethyl or isopropyl; n is 2; and X is oxygen.
Claim 4
Dependent Claim
38 words
The compound of claim 2 wherein R is pyrimidinyl substituted with 1 or 2 methyl groups or a chloro and 2 methyl groups; R 1 and R 2 are isopropyl; and R 3 and R 4 are methyl.
Claim 5
Dependent Claim
8 words
The compound of claim 1 which is N,N-dimethyl-N'-(2-dimethylaminoethyl)-N'-(2-pyrimidinyl)urea.
Claim 6
Dependent Claim
9 words
The compound of claim 1 which is N,N-dimethyl-N'-(2-dimethylaminoethyl) N'(4,6-dimethyl-2-pyrimidinyl)urea.
Claim 7
Dependent Claim
8 words
The compound of claim 1 which is N,N-dimethyl-N'-(2-diisopropylaminoethyl)-N'-(4,6-dimethyl-2-pyrimidinyl)urea.
Claim 8
Dependent Claim
8 words
The compound of claim 1 which is N,N-dimethyl-N'-(2-diisopropylaminoethyl)-N'-(4,6-dimethyl-5-chloro-2-pyrimidinyl)urea.
Claim 9
Dependent Claim
8 words
The compound of claim 1 which is N-(2-diisopropylaminoethyl)-N-(4,6-dimethyl-2-pyrimidinyl)urea.
Claim 10
Dependent Claim
101 words
A composition for the inhibition of gastric acid secretion which comprises an inert carrier and a compound having the formula: ##STR13## wherein R is pyrimidinyl which may be optionally substituted with from 1 to 3 of loweralkyl, halo, hydroxy, amino, mono or di-loweralkylamino, loweralkoxy, or phenyl loweralkoxy: and R 1 and R 2 , are independently loweralkyl; R 3 and R 4 are independently hydrogen or loweralkyl; and n is an integer of from 2 to 6, such that the direct linkage between the nitrogen atoms is either two or three carbon atoms, and the pharmaceutically acceptable acid addition salt thereof.
Claim 11
Dependent Claim
101 words
A composition for the inhibition of gastric acid secretion which comprises an inert carrier and a compound having the formula: ##STR13## wherein R is pyrimidinyl which may be optionally substituted with from 1 to 3 of loweralkyl, halo, hydroxy, amino, mono or di-loweralkylamino, loweralkoxy, or phenyl loweralkoxy: and R 1 and R 2 , are independently loweralkyl; R 3 and R 4 are independently hydrogen or loweralkyl; and n is an integer of from 2 to 6, such that the direct linkage between the nitrogen atoms is either two or three carbon atoms, and the pharmaceutically acceptable acid addition salt thereof.
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) | 1982-03-12 | 1982-09-11 | 1983-03-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-03-12 | 1986-09-11 | 1987-03-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-03-12 | 1990-09-11 | 1991-03-13 | $7700.00 | Window Closed / Lapsed |