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US 5,852,038 AGranted
Substituted 3-aminoquinuclidines
AssigneePfizer Inc.
InventorsFumitaka Ito, Toshihide Kokura, Masami Nakane, Kunio Satake, Hiroaki Wakabayashi
Life of this patent
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Abstract
The abstract isn’t available for this document.
Claims23
A compound having the formula ##STR18## wherein X is optionally substituted CONR.sup.1 R.sup.2 or CONR.sup.1 OR.sup.2 ;
- and n is an integer from zero to six;
- Ar.sup.1, Ar.sup.2 and Ar.sup.3 are each, independently, optionally substituted aryl, wherein said aryl is selected from phenyl, naphthyl, pyridyl, quinolyl, thienyl, furyl, phenoxyphenyl, oxazolyl, tetrazolyl, thiazolyl, imidazolyl and pyrazolyl;
- R.sup.1 and R.sup.2 are independently selected from hydrogen, optionally substituted (C.sub.1 -C.sub.6)alkyl, optionally substituted (C.sub.1 -C.sub.6)alkoxy, optionally substituted (C.sub.3 -C.sub.8)cycloalkyl, optionally substituted aryl, wherein said aryl is selected from phenyl, naphthyl, pyridyl, quinolyl, thienyl, furyl, phenoxyphenyl, oxazolyl, tetrazolyl, thiazolyl, imidazolyl and pyrazolyl;
- and optionally substituted (C.sub.1 -C.sub.5)heterocyclic groups, wherein said heterocyclic groups are selected from pyrrolidino and piperidino and when X is CONR.sup.1 R.sup.2, R.sup.1 and R.sup.2 may form, together with the nitrogen to which they are attached, a morpholino or thiamorpholino group;
- and wherein the substituents on the foregoing substituted alkyl, cycloalkyl and alkoxy groups are independently selected from halo, nitro, amino, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, trifluoromethyl and trifluoromethoxy;
- and wherein the substituents on the foregoing substituted (C.sub.1 -C.sub.5) heterocyclic groups are attached to a sulfur or nitrogen atom on the ring and are independently selected from oxygen, di-oxygen and (C.sub.1 -C.sub.4)alkyl when attached to a ring sulfur atom, and are independently selected from oxygen and (C.sub.1 -C.sub.4)alkyl when attached to a ring nitrogen atom;
- and wherein the substituents on said substituted Ar.sup.1 groups are independently selected from (C.sub.1 -C.sub.6)alkyl optionally substituted with from one to three halo groups, (C.sub.1 -C.sub.6)alkoxy optionally substituted with from one to three halo groups, (C.sub.1 -C.sub.6)alkylsulfinyl, (C.sub.2 -C.sub.6)alkenyl, (C.sub.1 -C.sub.6)alkylthio, (C.sub.1 -C.sub.6)alkylsulfonyl, (C.sub.1 -C.sub.6)alkylsulfonylamino, and di-(C.sub.1 -C.sub.6)alkylamino wherein one or both of the alkyl groups may be optionally substituted with a (C.sub.1 -C.sub.6)alkylsulfonyl, or (C.sub.1 -C.sub.6)alkylsulfinyl group;
- and wherein the substituents on said substituted Ar.sup.2 and Ar.sup.3 groups are independently selected from (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkylsulfinyl, di-(C.sub.1 -C.sub.4)alkylamino, trifluoromethyl and trifluoromethoxy;
- or a pharmaceutically acceptable salt of such compound.
6 more elements
A compound of the formula:
- ##STR21## wherein R is halo, (C.sub.1 -C.sub.6) alkyl optionally substituted with from one to three halo groups, (C.sub.1 -C.sub.6)alkoxy optionally substituted with from one to three halo groups, (C.sub.2 -C.sub.6)alkenyl, (C.sub.1 -C.sub.6)alkylthio, (C.sub.1 -C.sub.6)alkylsulfinyl or (C.sub.1 -C.sub.6)alkylsulfonyl;
- n is an integer from zero to six;
- X is optionally substituted CONR.sup.1 R.sup.2 or CONR.sup.1 OR.sup.2 ;
- and each of R.sup.1 and R.sup.2 is hydrogen, optionally substituted (C.sub.1 -C.sub.6)alkyl, optionally substituted (C.sub.1 -C.sub.6)alkoxy, optionally substituted (C.sub.3 -C.sub.8) cycloalkyl, optionally substituted aryl, wherein said aryl is phenyl, naphthyl, pyridyl, quinolyl, thienyl, furyl, phenoxyphenyl, oxazolyl, tetrazolyl, thiazolyl, imidazolyl or pyrazolyl;
- or an optionally substituted (C.sub.1 -C.sub.5) heterocyclic group, wherein said heterocyclic group is pyrrolidino or piperidino.
2 more elements
Dependencies are inferred from the claim text.