Unbridged bis-aryl carbinol derivatives compositions and methods of use
AssigneeSchering Corporation
InventorsRichard Friary, John J. Piwinski, Jesse K. Wong
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Abstract
Disclosed is a compound of Formula 1.0: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: AR.sup.1 represents ##STR2## AR.sup.2 represents ##STR3## or a five-membered heterocyclic aromatic group selected from the group consisting of Formulas I to XII, wherein the substitutable carbon atoms of the five-membered heterocyclic group can optionally be substituted with a group R.sup.1. Also disclosed are pharmaceutical compositions containing compounds of Formula 1.0. Further disclosed is a method for treating asthma, allergy and inflammation by administering an anti-asthmatic, anti-allergic or anti-inflammatory, respectively, effective amount of a compound of Formula 1.0.
Claims22
A method of treating inflammation or allergy comprising administering to a mammal in need of such treatment an antiinflammatory or anti-allergic effective amount of a compound of Formula 1.0 ##STR98## or a pharmaceutically acceptable salt or solvate thereof, wherein:
- AR.sup.1 represents ##STR99## AR.sup.2 represents ##STR100## or a five-membered heterocyclic aromatic group selected from the group consisting of Formulas I to XII:
- ##STR101## wherein X represents O, S, or NR.sup.10 wherein R.sup.10 is as defined below, said five-membered heterocyclic aromatic group can optionally be substituted with a group R.sup.1 as defined below;
- one of a, b and c represents N or N.sup.+ O.sup.- and the remaining a, b, and c represent C, or all of a, b and c represent C;
- one of d, e and f represents N or N.sup.+ O.sup.- and the remaining d, e, and f represent C, or all of d, e and f represents C;
- L represents N.sup.+ O.sup.- ;
- R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are each independently selected from the group consisting of:
- H, halo, --CF.sub.3, --OR.sup.11, --C(O)R.sup.11, SR.sup.11, --S(O).sub.q R.sup.12 wherein q is 1 or 2, --N(R.sup.11).sub.2, --NO.sub.2, --OC(O)R.sup.11, --CO.sub.2 R.sup.11, --OCO.sub.2 R.sup.12, --CON(R.sup.11).sub.2, --NR.sup.11 C(.dbd.O)R.sup.11, --CN, alkyl, aryl, alkenyl and alkynyl, said alkyl group is optionally substituted with --OR.sup.11, --SR.sup.11, --N(R.sup.11).sub.2 or --CO.sub.2 R.sup.11, and said alkenyl group is optionally substituted with halo, --OR.sup.12 or --CO.sub.2 R.sub.11 ;
- R.sup.5 and R.sup.6 are each independently selected from the group consisting of:
- H, alkyl and aryl;
- or R.sup.5 can be taken together with R.sup.6 to represent .dbd.O or .dbd.S;
- R.sup.7, R.sup.8 and R.sup.9 are each independently selected from the group consisting of:
- H, halo, --CF.sub.3, --OR.sup.11, --C(O)R.sup.11, --SR.sup.11, --S(O).sub.e R.sup.12 wherein e is 1 or 2, --N(R.sup.11).sub.2, --NO.sub.2, CN, --CO.sub.2 R.sup.11, --OCO.sub.2 R.sup.12, --OC(O)R.sup.11, --CON(R.sup.11).sub.2, --NR.sup.11 C(O)R.sup.11, alkyl, aryl, alkenyl and alkynyl, said alkyl group is optionally substituted with --OR.sup.11, --SR.sup.11, --N(R.sup.11).sub.2, or --CO.sub.2 R.sup.11, and said alkenyl group is optionally substituted with halo, --OR.sup.12 or --CO.sub.2 R.sup.11 ;
- R.sup.10 is selected from the group consisting of:
- H and alkyl;
- R.sup.11 is selected from the group consisting of:
- H, alkyl and aryl;
- R.sup.12 is selected from the group consisting of:
- alkyl and aryl;
- and
- Z is selected from the group consisting of:
- O and S, or Z optionally represents H and R.sup.10 ;
- wherein said alkyl contains from one to twenty carbon atoms, said alkenyl contains from 2 to 12 carbon atoms, said alkynyl contains from 2 to 12 carbon atoms, and said aryl contains from 6 to 14 carbon atoms.
Dependencies are inferred from the claim text.