Piperazino derivatives as neurokinin antagonists
First Claim
Patent Images
1. A compound of the formula:
- ##STR181## wherein u is 0 to 2;
m is 1, and y is 1 to 3;
or m is 2, and y is 0;
and with the further proviso that no more than one Rc is other than H in the ##STR182## moiety;
each Rc is independently selected from the group consisting of H and C1 -C6 alkyl;
each Ra and Rb is independently selected from the group consisting of H, C1 -C6 alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl and allyl;
or Ra and Rb together are C3 -C6 alkylene and are attached to the same nitrogen, so that Ra and Rb together with the nitrogen to which they are attached, form a 4 to 7 member ring;
each R1 and R2 is independently selected from the group consisting of H, C1 -C6 alkyl, CF3, C2 F5, Cl, Br, I, F, NO2, ORa, CN, NRa Rb, ##STR183## and where Ra is not H in ##STR184## or when R1 and R2 are on adjacent carbons on a ring, they can form ##STR185## wherein n'"'"' is 1 or 2;
each R3 is independently selected from the group consisting of H, C1 -C6 alkyl, CF3, C2 F5, ##STR186## Cl, Br, I, F, ORa, OCF3, and phenyl;
Ar1 is ##STR187## Ar2 is ##STR188## Z is ##STR189## n is independently 0-2;
m2 =1-2;
n3 is 0-4;
each Re and Rf is independently selected from the group consisting of H, C1 -C6 alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl and allyl;
or Re and Rf taken together with the carbon to which they are attached can also form a carbonyl group with the proviso that no more than one carbonyl group is in the ##STR190## moiety;
n5 is 1;
R5 is H or C1 -C6 alkyl;
R6 is H, C1 -C6 alkyl, C3 -C6 cycloalkyl, thienyl, pyridyl, isoxazoyl, ##STR191## or when Re,Rf taken together with the carbon atom to which they are attached form a carbonyl group and n3 is 1, R6 can also be --ORa wherein Ra is not H;
and wherein substituted means 1 to 3 substituents independently selected from the group consisting of H, C1 -C6 alkyl, CF3, C2 F5, OH, OC1 -C6 alkyl, Cl, Br, I and F;
or any enantiomer thereof,or a pharmaceutically acceptable salt thereof.
1 Assignment
0 Petitions
Accused Products
Abstract
The invention relates to compounds of the formula ##STR1## wherein Z, Rc, y, m, u, Ar2, n, X, Rc'"'"', I and Ar2 are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
-
Citations
6 Claims
-
1. A compound of the formula:
- ##STR181## wherein u is 0 to 2;
m is 1, and y is 1 to 3;
or m is 2, and y is 0;and with the further proviso that no more than one Rc is other than H in the ##STR182## moiety;
each Rc is independently selected from the group consisting of H and C1 -C6 alkyl;each Ra and Rb is independently selected from the group consisting of H, C1 -C6 alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl and allyl;
or Ra and Rb together are C3 -C6 alkylene and are attached to the same nitrogen, so that Ra and Rb together with the nitrogen to which they are attached, form a 4 to 7 member ring;each R1 and R2 is independently selected from the group consisting of H, C1 -C6 alkyl, CF3, C2 F5, Cl, Br, I, F, NO2, ORa, CN, NRa Rb, ##STR183## and where Ra is not H in ##STR184## or when R1 and R2 are on adjacent carbons on a ring, they can form ##STR185## wherein n'"'"' is 1 or 2;
each R3 is independently selected from the group consisting of H, C1 -C6 alkyl, CF3, C2 F5, ##STR186## Cl, Br, I, F, ORa, OCF3, and phenyl;
Ar1 is ##STR187## Ar2 is ##STR188## Z is ##STR189## n is independently 0-2;
m2 =1-2;
n3 is 0-4;each Re and Rf is independently selected from the group consisting of H, C1 -C6 alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl and allyl;
or Re and Rf taken together with the carbon to which they are attached can also form a carbonyl group with the proviso that no more than one carbonyl group is in the ##STR190## moiety;
n5 is 1;R5 is H or C1 -C6 alkyl; R6 is H, C1 -C6 alkyl, C3 -C6 cycloalkyl, thienyl, pyridyl, isoxazoyl, ##STR191## or when Re,Rf taken together with the carbon atom to which they are attached form a carbonyl group and n3 is 1, R6 can also be --ORa wherein Ra is not H; and wherein substituted means 1 to 3 substituents independently selected from the group consisting of H, C1 -C6 alkyl, CF3, C2 F5, OH, OC1 -C6 alkyl, Cl, Br, I and F; or any enantiomer thereof, or a pharmaceutically acceptable salt thereof. - View Dependent Claims (2, 3, 5, 6)
- ##STR181## wherein u is 0 to 2;
-
4. A compound selected from the group consisting of ##STR196## or any enantiomer thereof, or a pharmaceutically acceptable salt thereof.
Specification