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US 2006/0189596 A1Published application
Bridged bicyclic amine derivatives useful as CCR-3 receptor antagonists
OwnerLeyi Gonginventor
Life of this patent
Estimating the term…
Abstract
Compounds having the formula (1), are useful as CCR-3 receptor antagonists, wherein T is a bridged heterocyclyl group having one N atom and a bridge of one to two bridgehead carbon atoms; Ar and Ar1 are aryl or heteroaryl; F is alkylene, alkenylene, or a bond; E is —C(═O)N(R10)—, —SO2N(R10)—, —N(R11)C(═O)N(R10)—, —N(R11)SO2N(R10)—, —N(R11)C(═S)N(R10)—, —N(R11)C(═O)—, —N(R11)SO2—, —N(R12)C(═O)CH(R13)—, or CH(R13)C(═O)N(R12)—; Q is —C(═O)— or C1-2alkylene; and R3, R4, R5, R9, R10, R11, R12, and R13 are defined as set forth in the specification.
Claims17
A compound having the formula:
- wherein
- T is
- where R6 is taken together with one of R7 and R8 to form a bridge of one to two carbon atoms, and the other of R7 and R8 is selected from hydrogen and R9;
- Ar and Ar1 are, independently of each other, aryl or heteroaryl, with the proviso that Ar and Ar1 are not simultaneously phenyl;
- F is alkylene, alkenylene, or a bond;
- E is selected from —C(═O)N(R10)—, —SO2N(R10)—, —N(R11)C(═O)N(R10)—, —N(R11)SO2N(R10)—, —N(R11)C(═S)N(R10)—, —N(R11)C(═O)—, —N(R11)SO2—, —N(R12)C(═O)CH(R13)—, and CH(R13)C(═O)N(R12)—, where:
- R10, R11, R12, and R13 are, independently of each other, hydrogen, alkyl, acyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkenyl, heteroaryl, heteroaralkyl, heterocycloalkyl, heteroalkyl, or -(alkylene)-C(═O)-Z, where Z is alkyl, haloalkyl, alkoxy, haloalkyloxy, hydroxy, amino, mono- or disubstituted amino, aryl, aralkyl, aryloxy, aralkyloxy, heteroaryl, heteroaryloxy, or heteroaralkyloxy;
- or alternatively, R12 and R13 may be taken together with the nitrogen and carbon atoms to which they are attached, respectively, to form a heterocyclyl or heteroaryl ring optionally substituted with up to two groups selected from R14;
- R3 and R4 are, independently of each other, hydrogen, alkyl, alkenyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl, heterocyclylalkyl, heteroalkyl, -(alkylene)-C(═O)-Z1, or -(alkylene)-C(O)2Z1, where Z1 is alkyl, haloalkyl, alkoxy, haloalkyloxy, hydroxy, amino, mono- or disubstituted amino, aryl, aralkyl, aryloxy, aralkyloxy, heteroaryl, heteroaryloxy, or heteroaralkyloxy;
- R5 is hydrogen or alkyl;
- Q is —C(═O)— or C1-2alkylene;
- R9 is attached to any available carbon atom of ring T and is selected from lower alkyl, hydroxy, lower alkoxy, halo, cyano, trifluoromethyl, trifluoromethoxy, or a lower alkyl substituted with one of hydroxy, lower alkoxy, halo, cyano, trifluoromethyl, or trifluoromethoxy;
- R14 is selected from lower alkyl, hydroxy, lower alkoxy, halo, cyano, trifluoromethyl, trifluoromethoxy, and a lower alkyl substituted with one of hydroxy, lower alkoxy, halo, cyano, trifluoromethyl, or trifluoromethoxy;
- m is 0 or 1;
- and
- n is 0 to 4;
- and
- or a pharmaceutically acceptable salt thereof.
15 more elements
15-17. (canceled)
19-20. (canceled)
Dependencies are inferred from the claim text.