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US 6,635,658 B2Granted
Amino-tetralin derivatives as muscarinic receptor antagonists
AssigneeSyntex (U.S.A.) Inc.
InventorsAnn Marie Madera, Robert James Weikert
Life of this patent
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Abstract
This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein R1, R2, R3 and R4 are as defined in the specification, or individual isomers, racemic or non-racemic mixtures of isomers, or acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use and preparation as therapeutic drugs.
Claims45
Compounds of Formula I:
- wherein:
- R1 is (C1-6)alkyl;
- R2 is halogen or —OR′;
- R3 is hydrogen or —OR′;
- R′ is hydrogen, (C1-6)alkyl, or SO2R″;
- R″ is (C1-6)alkyl, haloalkyl, aryl or heteroaryl, wherein said aryl or heteroaryl groups are optionally substituted with a group selected from (C16)alkyl, halo, haloalkyl, cyano, nitro, alkylsulfonyl, and alkylsulfonylamino;
- R4 is (i) (C1-6)alkyl, (ii) aryl, heterocyclyl, or heteroaryl, wherein said aryl, heterocyclyl or heteroaryl groups are optionally substituted with a group selected from (C1-6)alkyl, halo, haloalkyl, (C1-6)alkoxy, cyano, amino, mono- or di alkylamino, nitro, alkylsulfonyl, alkylcarbonyl, urea, alkylcarbonylamino, alkylsulfonylamino, alkylaminosulfonyl, alkoxycarbonyl, heterocyclyl and heteroaryl, or (iii) —NR5R6;
- and
- R5 and R6 are independently of each other hydrogen, (C1-6)alkyl, aryl or heterocyclyl;
- wherein said aryl or heterocyclyl groups are optionally substituted with (C1-6)alkyl, halo, haloalkyl, cyano, (C1-6)alkoxy, and alkylsulfonyl;
- or an individual isomer, a racemic or non-racemic mixture of isomers, or an acceptable salt or solvate thereof.
8 more elements
Dependencies are inferred from the claim text.