Claims
- 1. A compound of the formula (I): ##STR13## or a pharmaceutically acceptable salt thereof, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are selected from the group consisting of:
- (1) R.sup.1 and R.sup.2 together represent --(CH.sub.2).sub.q --wherein q is an integer from 4 to 6, to form together with the nitrogen atom to which they are attached a 5-7 membered saturated ring, optionally substituted by C.sub.1-6 alkyl; and
- R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached form a benzene ring optionally substitued by C.sub.1-6 alkyl;
- (2) R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-6 alkyl, phenyl (C.sub.1-6)alkyl, furanyl (C.sub.1-6)alkyl, thienyl(C.sub.1-6)-alkyl, C.sub.3-10 -cycloalkyl, hydroxy(C.sub.2-6)alkyl or halo(C.sub.2-6)alkyl, (wherein said hydroxy and halo groups are not substituted on the carbon atom adjacent to the nitrogen atom); and
- R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached form a benzene ring optionally substituted by C.sub.1-6 alkyl; and
- (3) R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-6 alkyl, phenyl(C.sub.1-6)alkyl, furanyl(C.sub.1-6)alkyl, thienyl(C.sub.1-6)alkyl, C.sub.3-10 -cycloalkyl, hydroxy(C.sub.2-6)alkyl or halo(C.sub.2-6)alkyl, (wherein said hydroxy and halo groups are not substituted on the carbon atoms adjacent to the nitrogen atom);
- R.sup.3 is hydrogen, C.sub.1-6 alkyl or aryl (C.sub.1-6)alkyl and R.sup.4 is hydrogen or C.sub.1-6 alkyl;
- n is an integer from 1 to 6;
- Z is 1,3-phenylene, 1,4-phenylene, 2,4-pyridyl (wherein the R.sup.1 R.sup.2 N(CH.sub.2).sub.n group is in the 4-position);
- m is an integer from zero to one;
- Y is ozygen sulfur or methylene; and
- p is an integer from two to four.
- 2. A compound according to claim 1 wherein R.sup.1 R.sup.2 N(CH.sub.2).sub.n --is piperidinomethyl.
- 3. A compound according to claim 1 wherein Z is 1,3-phenylene.
- 4. A compound according to any one of claims 1 to 3 wherein m is zero and Y is oxygen.
- 5. A compound according to claim 1 which is 2-[3-[3-(piperidinomethyl)phenoxy]propylamino]-4-quinolone or a pharmaceutically acceptable salt thereof.
- 6. A pharmaceutical composition having histamine H.sub.2 -receptor blocking activity which comprises in an effective but non-toxic amount to block said receptors a compound according to claim 1 and a pharmaceutically acceptable carrier.
- 7. A pharmaceutical composition having histamine H.sub.2 -receptor blocking activity which comprises in an effective but non-toxic amount to block said receptors a compound according to claim 8 and a pharmaceutically acceptable carrier.
- 8. A method of blocking histamine H.sub.2 -receptors which comprises administering to an animal an effective amount to block said receptors of a compound of claim 1.
- 9. A method of blocking histamine H.sub.2 -receptors which comprises administering to an animal an effective amount to block said receptors of a compound of claim 8.
- 10. A compound of the formula: ##STR14## wherein: R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-6 alkyl, phenyl(C.sub.1-6)alkyl, furanyl (C.sub.1-6)alkyl, thienyl (C.sub.1-6)alkyl, C.sub.3-10 cycloalkyl, hydroxy(C.sub.2-6)alkyl or halo(C.sub.2-6)alkyl, (wherein said hydroxy and halo groups are not substituted on the carbon atoms adjacent to the nitrogen atom); or
- R.sup.1 and R.sup.2 together represent --(CH.sub.2).sub.q --wherein q is an integer from 4 to 6, to form together with the nitrogen atom to which they are attached a 5-7 membered saturated ring, optionally substituted by C.sub.1-6 alkyl;
- n is an integer from 1 to 6;
- Z is 1,3-phenylene, 1,4-phenylene, 2,4-pyridyl (wherein the R.sup.1 R.sup.2 N(CH.sub.2).sub.n group is in the 4-position);
- m is an integer from zero to one;
- Y is oxygen, sulphur or methylene;
- p is an integer from two to four;
- R.sup.3 is hydrogen, C.sub.1-6 alkyl or aryl (C.sub.1-6)alkyl and R.sup.4 is hydrogen or C.sub.1-6 alkyl; or R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached form a benezene ring optionally substituted by C.sub.1-6 alkyl;
- z is an integer from zero to 1; and
- R.sup.a is hydrogen or R, except if z is zero, R.sup.a cannot be hydrogen, R is C.sub.1-6 alkyl, benzyl, substituted benzyl, allyl, 2,2,2-trichloroethyl or methoxyethyl.
Priority Claims (1)
Number |
Date |
Country |
Kind |
83-32091 |
Dec 1983 |
GBX |
|
Parent Case Info
This is a division of application Ser. No. 675,661 filed Nov. 28, 1984, now U.S. Pat. No. 4,608,380.
US Referenced Citations (5)
Divisions (1)
|
Number |
Date |
Country |
Parent |
675661 |
Nov 1984 |
|