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US 6,720,316 B2Granted
Therapeutic 5-HT ligand compounds
AssigneePharmacia & Upjohn Company
InventorWilliam W. McWhorter, Jr.
Life of this patent
Estimating the term…
Abstract
The present invention provides compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8 and Z have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands, and are useful for treating diseases whereas modulation of 5-HT activity is desired.
Claims40
A compound of Formula (I):
- wherein Z is —O— or —S—;
- l is 1 or 2;
- m is 0, 1 or 2;
- n is 1;
- R1 and R2 are each independently hydrogen, C1-6alkyl, C3-6cycloalkyl, or (C3-6cycloalkyl)C1-6alkyl;
- provided that R1 and R2 are not both hydrogen;
- R3 is hydrogen or C1-6alkyl;
- R4 and R5 are independently hydrogen, C1-6alkyl or arylC1-6alkylene;
- R6, R7, and R8 are independently hydrogen, fluoro, chloro, bromo, CF3, —OCF3, —N(R10)2, C1-6alkyl, C1-6alkoxy, heteroaryl or aryl;
- each R10 is independently hydrogen, or —C1-6alkyl;
- wherein any C1-6alkyl, C1-6alkylene, or C1-6alkoxy of R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 is optionally partially unsaturated;
- wherein any heteroaryl or aryl is optionally substituted with one or two substituents independently selected from halo, —CF3, —OCF3, C1-6alkoxy, —N(R10)2, and C1-6alkyl;
- or a pharmaceutically acceptable salt thereof.
10 more elements
A compound of Formula (II):
- wherein Z is —O— or —S—;
- l is 1 or 2;
- m is 0, 1 or 2;
- n is 1 ;
- R1 and R2 are each independently hydrogen, C1-6alkyl, C3-6cycloalkyl, or (C3-6cycloalkyl)C1-6alkyl;
- provided that R1 and R2 are not both hydrogen;
- R3 is —C(O)-aryl, —C(O)-heteroaryl, —C(O)—C1-6alkyl, —C(O)—C1-6haloalkyl, —C(O)O—C1-6alkyl, or —C(O)O—C1-6haloalkyl, where aryl or heteroaryl is optionally substituted with one or two halo, —CF3, —OCF3, C1-6alkoxy, —N(R10)2, or —C1-6alkyl;
- R4 and R5 are independently hydrogen, C1-6alkyl or arylC1-6alkylene;
- R6, R7, and R8 are independently hydrogen, fluoro, chloro, bromo, CF3, —OCF3, —N(R10)2, C1-6alkyl, C1-6alkoxy, heteroaryl or aryl;
- each R10 is independently hydrogen, or —C1-6alkyl;
- wherein any C1-6alkyl, C1-6alkylene, or C1-6alkoxy of R1, R2, R3, R4, R5, R6, R7, R8, and R10 is optionally partially unsaturated;
- wherein any heteroaryl or aryl is optionally substituted with one or two substituents independently selected from halo, —CF3, —OCF3, C1-6alkoxy, —N(R10)2, and C1-6alkyl.
9 more elements
Dependencies are inferred from the claim text.