Piperazino derivatives as neurokinin antagonists
First Claim
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1. A compound of the formula:
- ##STR263## wherein u is 0 to 2;
m is 1, and y is 1 to 3;
or m is 2, and y is 0;
Ra and Rb are independently selected from the group consisting of H, ##STR264## and allyl;
or when Ra and Rb are attached to the same nitrogen, then Ra and Rb, together with the nitrogen to which they are attached, form a 4 to 7 member ring;
R1 and R2 are independently selected from the group consisting of H, ##STR265## or when R1 and R2 are on adjacent carbons on a ring, they can form ##STR266## wherein n'"'"' is 1 or 2;
R3 is independently selected from the group consisting of H, C1 -C6 alkyl, --CF3, --C2 F5, Cl, Br, I, F, --ORa, --OCF3, phenyl, ##STR267## Ar1 is ##STR268## Ar2 is ##STR269## Z is ##STR270## m1 and m2 are independently 0 or 1;
n6 is 0 to 2;
##STR271## X4 is --O-- or X5a and X5d are (H, H);
G is ##STR272## n3 is 0 to 4;
Rg is ##STR273## Rh is H, C1 -C6 alkyl, --C(O)Ra or --C(O)ORa ;
n7 is 0 to 4;
Re and Rf are independently selected from the group consisting of H, ##STR274## and allyl;
R5 is H or C1 -C6 alkyl;
R6 is R1 -pyridyl or an N-oxide thereof, R1 -thienyl, R1 -oxazolyl, ##STR275## provided that when X4 isX5a is (H, H) ##STR276## G is not or any enantiomer or diastereomer thereof,or a pharmaceutically acceptable salt thereof.
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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.
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Citations
8 Claims
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1. A compound of the formula:
- ##STR263## wherein u is 0 to 2;
m is 1, and y is 1 to 3;
or m is 2, and y is 0;Ra and Rb are independently selected from the group consisting of H, ##STR264## and allyl;
or when Ra and Rb are attached to the same nitrogen, then Ra and Rb, together with the nitrogen to which they are attached, form a 4 to 7 member ring;R1 and R2 are independently selected from the group consisting of H, ##STR265## or when R1 and R2 are on adjacent carbons on a ring, they can form ##STR266## wherein n'"'"' is 1 or 2;
R3 is independently selected from the group consisting of H, C1 -C6 alkyl, --CF3, --C2 F5, Cl, Br, I, F, --ORa, --OCF3, phenyl, ##STR267## Ar1 is ##STR268## Ar2 is ##STR269## Z is ##STR270## m1 and m2 are independently 0 or 1;
n6 is 0 to 2;
##STR271## X4 is --O-- or X5a and X5d are (H, H);G is ##STR272## n3 is 0 to 4;
Rg is ##STR273## Rh is H, C1 -C6 alkyl, --C(O)Ra or --C(O)ORa ;
n7 is 0 to 4;Re and Rf are independently selected from the group consisting of H, ##STR274## and allyl;
R5 is H or C1 -C6 alkyl;R6 is R1 -pyridyl or an N-oxide thereof, R1 -thienyl, R1 -oxazolyl, ##STR275## provided that when X4 is X5a is (H, H) ##STR276## G is not or any enantiomer or diastereomer thereof, or a pharmaceutically acceptable salt thereof. - View Dependent Claims (2, 3, 4, 5, 7, 8)
- ##STR263## wherein u is 0 to 2;
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6. A compound selected from the group consisting of compounds represented by the formula wherein Gc is selected from the group consisting of ##STR279##
Specification
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Current AssigneeSchering Corporation (Merck & Co., Inc.)
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Original AssigneeSchering Corporation (Merck & Co., Inc.)
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InventorsFriary, Richard J., Shih, Neng-Yang, Chen, Xiao, McCormick, Kevin D., Blythin, David J., Shue, Ho-Jane, Piwinski, John J.
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Primary Examiner(s)BERNHARDT, EMILY A
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Application NumberUS09/313,150Time in Patent Office337 DaysField of Search544/362, 544/364, 544/367, 544/373, 514/253, 514/216, 540/585US Class Current514/253.04CPC Class CodesC07D 241/04 having no double bonds betw...C07D 401/12 linked by a chain containin...C07D 403/12 linked by a chain containin...C07D 453/06 containing isoquinuclidine ...C07D 487/08 Bridged systems
