Piperazino derivatives as neurokinn antagonists
First Claim
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1. A compound of the formula:
- ##STR209## u is 0 to 2;
y is 1 to 3;
with the proviso that no more than one Rc is other than H in the ##STR210## moiety;
each Rc is independently H, C1 -C6 alkyl, hydroxy(C1 -C6)alkyl, carboxy(C1 -C6)alkyl or H2 NC(O)-(C1 C6)alkyl;
each R1 and R2 is independently H, C1 -C6 alkyl, CF3, C2 F5, Cl, Br, I, ##STR211## or when R1 and R2 are on adjacent carbons on a ring, they can form ##STR212## wherein n'"'"' is 1 or 2;
each R3 is independently H, C1 -C6 alkyl, CF3, C2 F5, ##STR213## Cl, Br, I, or F, ORa, OCF3 or phenyl;
each Ra and Rb is independently selected from the group consisting of H, C1 -C6 alkyl, phenyl, benzyl, allyl, ##STR214## or Ra and Rb together are C2 -C6 alkylene and are attached to the same nitrogen, so that Ra and Rb, together with the nitrogen to which they are attached, join to form a 4 to 7 membered ring;
Ar1 is ##STR215## m1 =0 to 1;
n3 is 0 to 4;
each Re and Rf is independently selected from the group consisting of H, C1 -C6 alkyl, phenyl, benzyl, allyl, ##STR216## 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 ##STR217## moiety;
R6 is H, C3 -C6 cycloalkyl, ##STR218## heteroaryl, substituted heteroaryl, or, provided that Re,Rf taken together with the carbon atom to which they are attached form a carbonyl group and n3 is R1, R6 is ORa wherein Ra is not H;
wherein heteroaryl is selected from the group consisting of imidazolyl, oxadiazolyl, thiadiazolyl, benzimidazolyl, indolyl, thiazolyl, thienyl, pyrrolyl, furyl, pyridyl, isoxazolyl, pyrimidyl and quinolyl; and
wherein substituted heteroaryl are heteroaryl rings substituted with R1, R2 and R3 ;
or a pharmaceutically acceptable salt thereof.
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Abstract
The invention relates to compounds of the formula ##STR1## 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:
- ##STR209## u is 0 to 2;
y is 1 to 3;with the proviso that no more than one Rc is other than H in the ##STR210## moiety;
each Rc is independently H, C1 -C6 alkyl, hydroxy(C1 -C6)alkyl, carboxy(C1 -C6)alkyl or H2 NC(O)-(C1 C6)alkyl;each R1 and R2 is independently H, C1 -C6 alkyl, CF3, C2 F5, Cl, Br, I, ##STR211## or when R1 and R2 are on adjacent carbons on a ring, they can form ##STR212## wherein n'"'"' is 1 or 2;
each R3 is independently H, C1 -C6 alkyl, CF3, C2 F5, ##STR213## Cl, Br, I, or F, ORa, OCF3 or phenyl;
each Ra and Rb is independently selected from the group consisting of H, C1 -C6 alkyl, phenyl, benzyl, allyl, ##STR214## or Ra and Rb together are C2 -C6 alkylene and are attached to the same nitrogen, so that Ra and Rb, together with the nitrogen to which they are attached, join to form a 4 to 7 membered ring;Ar1 is ##STR215## m1 =0 to 1;
n3 is 0 to 4;each Re and Rf is independently selected from the group consisting of H, C1 -C6 alkyl, phenyl, benzyl, allyl, ##STR216## 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 ##STR217## moiety;
R6 is H, C3 -C6 cycloalkyl, ##STR218## heteroaryl, substituted heteroaryl, or, provided that Re,Rf taken together with the carbon atom to which they are attached form a carbonyl group and n3 is R1, R6 is ORa wherein Ra is not H;wherein heteroaryl is selected from the group consisting of imidazolyl, oxadiazolyl, thiadiazolyl, benzimidazolyl, indolyl, thiazolyl, thienyl, pyrrolyl, furyl, pyridyl, isoxazolyl, pyrimidyl and quinolyl; and
wherein substituted heteroaryl are heteroaryl rings substituted with R1, R2 and R3 ;or a pharmaceutically acceptable salt thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8)
- ##STR209## u is 0 to 2;
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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InventorsShih, Neng-Yang, Chen, Xiao, Tom, Wing C., 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 NumberUS08/663,880Time in Patent Office795 DaysField of Search544/349, 544/373, 544/295, 544/362, 544/363, 544/367, 544/369, 544/370, 544/372, 514/253, 514/212, 540/598, 540/599US Class Current514/254.08CPC Class CodesC07D 241/04 having no double bonds betw...C07D 401/12 linked by a chain containin...C07D 401/14 containing three or more he...C07D 405/14 containing three or more he...C07D 409/14 containing three or more he...C07D 453/02 containing not further cond...C07D 487/04 Ortho-condensed systemsC07D 487/10 Spiro-condensed systems
