US4450168A
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Pharmaceutical compositions containing compounds having action on histamine receptors
Assignee: Glaxo Group Ltd
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Filing: 1983-07-14
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Granted: 1984-05-22
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Expires: 2003-07-14
Abstract
Abstract Compounds of general formula (I) ##STR1## and physiologically acceptable salts and hydrates thereof in which R 1 and R 2 each represent methyl groups or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino or hexamethylenimino group; R 3 represents hydrogen or methyl; Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms; R 4 represents a hydrogen atom and R 5 represents a C 1-4 alkyl group; or R 4 and R 5 together with the atoms to which they are attached form a tetrahydropyranyl ring; and either n is zero, X is oxygen, m is 3 or 4, and Q is a benzene ring linked through the 1- and 3- positions; or n is 1, X is sulphur, m is 2, and Q is a furan ring linked through the 2- and 5- positions with optionally a methyl substituent on the carbon atom adjacent to the group R 1 R 2 NCH 2 , or Q is a thiophene ring linked through the 2- and 4- positions with the group R 1 R 2 NCH 2 in the 2- position; with the proviso that when Q is other than a benzene ring, R 1 and R 2 are methyl groups, are disclosed as having action as histamine H 2 -antagonists.
Inventors
- 👤 David E. Bays
- 👤 Roger Hayes
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 07:05
CPC Classifications
C; C07; C07D; C07D405/00; C07D405/02; C07D405/12; A; A61; A61P; A61P43/00; C07D249/00; C07D249/02; C07D249/08; C07D249/10; C07D249/14
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
244 words
A pharmaceutical composition for the treatment of conditions mediated through histamine H 2 -receptors, comprising an effective amount for the treatment of the said condition of a compound of formula (I) ##STR6## or a physiologically acceptable salt or hydrate thereof in which R 1 and R 2 each represent methyl groups or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino or hexamethylenimino group; R 3 represents hydrogen or methyl; Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms; R 4 represents a hydrogen atom and R 5 represents a C 1-4 alkyl group; or R 4 and R 5 together with the atoms to which they are attached form a tetrahydropyranyl ring; and either n is zero, X is oxygen, m is 3 or 4, and Q is a benzene ring linked through the 1- and 3-positions; or n is 1, X is sulphur, m is 2, and Q is a furan ring linked through the 2- and 5-positions with optionally a methyl substituent on the carbon atom adjacent to the group R 1 R 2 NCH 2 , or Q is a thiophene ring linked through the 2- and 4-positions with the group R 1 R 2 NCH 2 in the 2-position; with the proviso that when Q is other than a benzene ring R 1 and R 2 are methyl groups, together with at least one pharmaceutically acceptable carrier or diluent.
Claim 2
Dependent Claim
244 words
A pharmaceutical composition for the treatment of conditions mediated through histamine H 2 -receptors, comprising an effective amount for the treatment of the said condition of a compound of formula (I) ##STR6## or a physiologically acceptable salt or hydrate thereof in which R 1 and R 2 each represent methyl groups or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino or hexamethylenimino group; R 3 represents hydrogen or methyl; Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms; R 4 represents a hydrogen atom and R 5 represents a C 1-4 alkyl group; or R 4 and R 5 together with the atoms to which they are attached form a tetrahydropyranyl ring; and either n is zero, X is oxygen, m is 3 or 4, and Q is a benzene ring linked through the 1- and 3-positions; or n is 1, X is sulphur, m is 2, and Q is a furan ring linked through the 2- and 5-positions with optionally a methyl substituent on the carbon atom adjacent to the group R 1 R 2 NCH 2 , or Q is a thiophene ring linked through the 2- and 4-positions with the group R 1 R 2 NCH 2 in the 2-position; with the proviso that when Q is other than a benzene ring R 1 and R 2 are methyl groups, together with at least one pharmaceutically acceptable carrier or diluent.
Claim 3
Dependent Claim
114 words
A pharmaceutical composition for the treatment of conditions mediated through histamine H 2 -receptors, comprising an effective amount for the treatment of the said condition of a compound of formula (II) ##STR7## or a physiologically acceptable salt or hydrate thereof, in which R 1 R 2 N is a pyrrolidino, piperidino or hexamethylenimino ring; m is 3 or 4; R 3 represents hydrogen or methyl; Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms; and R 4 represents a hydrogen atom and R 5 represents a C 1-4 alkyl group; or R 4 and R 5 together with the atoms to which they are attached form a tetrahydropyranyl ring.
Claim 4
Dependent Claim
114 words
A pharmaceutical composition for the treatment of conditions mediated through histamine H 2 -receptors, comprising an effective amount for the treatment of the said condition of a compound of formula (II) ##STR7## or a physiologically acceptable salt or hydrate thereof, in which R 1 R 2 N is a pyrrolidino, piperidino or hexamethylenimino ring; m is 3 or 4; R 3 represents hydrogen or methyl; Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms; and R 4 represents a hydrogen atom and R 5 represents a C 1-4 alkyl group; or R 4 and R 5 together with the atoms to which they are attached form a tetrahydropyranyl ring.
Claim 5
Dependent Claim
30 words
A pharmaceutical composition according to claim 2 in which, in formula (II), R 1 R 2 N is a piper idino ring, m is 3 and R 3 is methyl.
Claim 6
Dependent Claim
48 words
A pharmaceutical composition according to claim 1 in which, in formula (I); Alk represents methylene or ethylene and R 4 and R 5 together with the atoms to which they are attached form a tetrahydropyranyl ring or R 4 represents hydrogen and R 5 represents methyl or ethyl.
Claim 7
Dependent Claim
40 words
A pharmaceutical composition for the treatment of conditions mediated through histamine H 2 -receptors comprising an effective amount of a compound selected from 1-methyl-N-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]-3-[(tetrahydro-2-pyranyl)oxymethyl]-1H-1,2,4-triazole-5-amine; 3-[(ethoxymethoxy)methyl]-1-methyl-N-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]-1H-1,2,4-triazole-5-amine; and physiologically acceptable salts thereof, together with at least one pharmaceutically acceptable carrier or diluent.
Claim 8
Dependent Claim
40 words
A pharmaceutical composition for the treatment of conditions mediated through histamine H 2 -receptors comprising an effective amount of a compound selected from 1-methyl-N-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]-3-[(tetrahydro-2-pyranyl)oxymethyl]-1H-1,2,4-triazole-5-amine; 3-[(ethoxymethoxy)methyl]-1-methyl-N-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]-1H-1,2,4-triazole-5-amine; and physiologically acceptable salts thereof, together with at least one pharmaceutically acceptable carrier or diluent.
Claim 9
Dependent Claim
14 words
A pharmaceutical composition according to claim 1 in a form adapted for oral administration.
Claim 10
Dependent Claim
89 words
A compound of the formula (II) ##STR8## or a physiologically acceptable salt or hydrate therof in which R 1 R 2 N is a pyrrolidino, piperidino or hexamethylenimino ring; m is 3 or 4; R 3 represents hydrogen or methyl; Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms; and R 4 represents a hydrogen atom and R 5 represents a C 1-4 alkyl group; or R 4 and R 5 together with the atoms to which they are attached form a tetrahydropyranyl ring.
Claim 11
Dependent Claim
89 words
A compound of the formula (II) ##STR8## or a physiologically acceptable salt or hydrate therof in which R 1 R 2 N is a pyrrolidino, piperidino or hexamethylenimino ring; m is 3 or 4; R 3 represents hydrogen or methyl; Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms; and R 4 represents a hydrogen atom and R 5 represents a C 1-4 alkyl group; or R 4 and R 5 together with the atoms to which they are attached form a tetrahydropyranyl ring.
Claim 12
Dependent Claim
25 words
A compound according to claim 7 in which R 1 R 2 N is a piperidino ring, m is 3 and R 3 is methyl.
Claim 13
Dependent Claim
44 words
A compound according to claim 7 in which Alk represents methylene or ethylene and R 4 and R 5 together with the atoms to which they are attached form a tetrahydropyranyl ring or R 4 represents hydrogen and R 5 represents methyl or ethyl.
Claim 14
Dependent Claim
10 words
1-Methyl-N-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]-3-[(tetrahydro 2-pyranyl)oxymethyl]-1H-1,2,4-triazole-5-amine; or 3-[(ethoxymethoxy)methyl]-1-methyl-N-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]-1H-1,2,4-triazole-5-amine; or a physiologically acceptable salt thereof.
Claim 15
Dependent Claim
10 words
1-Methyl-N-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]-3-[(tetrahydro 2-pyranyl)oxymethyl]-1H-1,2,4-triazole-5-amine; or 3-[(ethoxymethoxy)methyl]-1-methyl-N-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]-1H-1,2,4-triazole-5-amine; or a physiologically acceptable salt thereof.
Claim 16
Dependent Claim
38 words
A method for the treatment of a condition mediated through histamine H 2 -receptors which comprises administering to a patient an effective amount to alleviate said condition of a compound of formula (I) as defined in claim 1.
Claim 17
Dependent Claim
35 words
A method for the treatment of a condition mediated through histamine H 2 -receptors which comprises administering to a patient an effective amount to alleviate said condition of a compound as claimed in claim 7.
References Cited (Backward Citations)
GB2063253A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-05-22 | 1987-11-21 | 1988-05-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-05-22 | 1991-11-21 | 1992-05-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-05-22 | 1995-11-21 | 1996-05-22 | $7700.00 | Window Closed / Lapsed |