US5864045A
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Heterocyclic substituted piperazinone derivatives
Assignee: Aventis Pharmaceuticals Inc
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Filing: 1998-04-27
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Granted: 1999-01-26
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Expires: 2018-04-27
Abstract
Abstract The present invention relates to substituted piperazinone derivatives of formula (1) or stereoisomers, or pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions disclosed herein including: asthma, cough, and bronchitis. The present invention also relates to intermediates useful in the preparation of compounds of formula (1).
Inventors
- 👤 Timothy P. Burkholder
- 👤 Elizabeth M. Kudlacz
- 👤 Tieu-Binh Le
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 12:53
CPC Classifications
C; C07; C07D; C07D403/00; C07D403/02; C07D403/06; A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K31/50; A61P; A61P11/00; A61P11/06; A61P11/08; A61P11/14; A61P43/00; C07D209/00; C07D209/02; C07D209/04; C07D209/10; C07D209/18; C07D209/20; C07D403/14
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
146 words
A compound of the formula ##STR31## wherein Ar 1 is a radical chosen from the group: ##STR32## wherein Z 1 is from 1 to 3 substituents each independently chosen from the group consisting of hydrogen, halogen, benzyloxy, hydroxy, CF 3 , C 1 -C 4 alkyl, and C 1 -C 4 alkoxy; R 2 is hydrogen, C 1 -C 4 alkyl, or --CHO; R 3 is hydrogen or a radical chosen from the group ##STR33## wherein Z 3 is from 1 to 3 substituents each independently chosen from the group consisting of hydrogen, halogen, benzyloxy, hydroxy, CF 3 , C 1 -C 4 alkyl, and C 1 -C 4 alkoxy; R 5 is hydrogen, benzyl, or C 1 -C 4 alkyl; R 6 is hydrogen or --C(O)OR 7 wherein R 7 is benzyl or C 1 -C 4 alkyl; or stereoisomers, or pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
146 words
A compound of the formula ##STR31## wherein Ar 1 is a radical chosen from the group: ##STR32## wherein Z 1 is from 1 to 3 substituents each independently chosen from the group consisting of hydrogen, halogen, benzyloxy, hydroxy, CF 3 , C 1 -C 4 alkyl, and C 1 -C 4 alkoxy; R 2 is hydrogen, C 1 -C 4 alkyl, or --CHO; R 3 is hydrogen or a radical chosen from the group ##STR33## wherein Z 3 is from 1 to 3 substituents each independently chosen from the group consisting of hydrogen, halogen, benzyloxy, hydroxy, CF 3 , C 1 -C 4 alkyl, and C 1 -C 4 alkoxy; R 5 is hydrogen, benzyl, or C 1 -C 4 alkyl; R 6 is hydrogen or --C(O)OR 7 wherein R 7 is benzyl or C 1 -C 4 alkyl; or stereoisomers, or pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
12 words
A compound of claim 1 wherein R 6 is --C(O)OR 7 .
Claim 4
Dependent Claim
10 words
A compound of claim 1 wherein R 6 is hydrogen.
Claim 5
Dependent Claim
10 words
A compound of claim 1 wherein R 5 is methyl.
Claim 6
Dependent Claim
11 words
A compound of claim 1 wherein the compound is 2- (R)-2-(1H-Indol-3-yl)-1-carboxymethyl-ethylamino!-N-(t-butoxycarbonyl)-N-(2-phenyl-ethyl)-ethylamine.
Claim 7
Dependent Claim
11 words
A compound of claim 1 wherein the compound is 2- (R)-2-(1H-Indol-3-yl)-1-carboxymethyl-ethylamino!-N-(2-phenyl-ethyl)-ethylamine.
Claim 8
Dependent Claim
11 words
A compound of claim 1 wherein the compound is 2- (S)-2-(1H-Indol-3-yl)-1-carboxymethyl-ethylamino!-N-(t-butoxycarbonyl)-N-(2-phenyl-ethyl)-ethylamine.
Claim 9
Dependent Claim
11 words
A compound of claim 1 wherein the compound is 2- (S)-2-(1H-Indol-3-yl)-1-carboxymethyl-ethylamino!-N-(2-phenyl-ethyl)-ethylamine.
Claim 10
Dependent Claim
13 words
A compound of claim 1 wherein the compound is 2- (R)-2-(1H-Indol-3-yl)-1-carboxymethyl-ethylamino!-N-(t-butoxycarbonyl)-N- 2- (4-benzyloxy)phenyl-ethyl!!-ethylamine.
Claim 11
Dependent Claim
13 words
A compound of claim 1 wherein the compound is 2- (R)-2-(1H-Indol-3-yl)-1-carboxymethyl-ethylamino!-N- 2- (4-benzyloxy)phenyl-ethyl!!-ethylamine.
Claim 12
Dependent Claim
13 words
A compound of claim 1 wherein the compound is 2- (S)-2-(1H-Indol-3-yl)-1-carboxymethyl-ethylamino!-N-(t-butoxycarbonyl)-N- 2- (4-benzyloxy)phenyl-ethyl!!-ethylamine.
Claim 13
Dependent Claim
13 words
A compound of claim 1 wherein the compound is 2- (S)-2-(1H-Indol-3-yl)-1-carboxymethyl-ethylamino!-N- 2- (4-benzyloxy)phenyl-ethyl!!-ethylamine.
Claim 14
Dependent Claim
11 words
A compound of claim 1 wherein the compound is 2- (R)-2-(1H-Indol-3-yl)-1-carboxymethyl-ethylamino!-N-(t-butoxycarbonyl)-N-(2,2-bis-phenyl-ethyl)!-ethylamine.
Claim 15
Dependent Claim
11 words
A compound of claim 2 wherein the compound is 2- (R)-2-(1H-Indol-3-yl)-1-carboxymethyl-ethylamino!-N-(2,2-bis-phenyl-ethyl)!-ethylamine.
References Cited (Backward Citations)
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