Substituted cyclohexenes as central nervous system agents

C - Chemistry – Metallurgy – 07 – D

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C07D 401/14 (2006.01) A61K 31/395 (2006.01) C07D 213/74 (2006.01) C07D 401/04 (2006.01) C07D 401/08 (2006.01) C07D 409/08 (2006.01) C07D 409/12 (2006.01) C07D 409/14 (2006.01) C07D 417/12 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2031570

Substituted cyclohexenes are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperproloactinaemia-related conditions and central nervous system disorders. The general structure of compounds according to the invention are as shown in Formula I below. Image wherein R1 is aryl, 2-, 3-, or 4-pyridinyl or 2-, 3-, or 4-pyridinyl substituted by lower alkyl, lower alkoxy, or halogen, 2-, 4-, or 5-pyrimidinyl or 2-, 4-, or 5-pyrimidinyl substituted by lower alkyl, lower alkoxy, or halogen, 2-pyrazinyl or 2-pyrazinyl subsituted by lower alkyl, lower alkoxy, or halogen, 2- or 3-thienyl or 2- or 3-thienyl substituted by lower alkyl or halogen, 2- or 3-furanyl or 2- or 3-furanyl substituted by lower alkyl or halogen, 2-, 4-, or 5-thiazolyl or 2-, 4- or 5-thiazolyl substituted by lower alkyl or halogen; m is zero or an integer from one to two; R2 is Image wherein R1 is as defined above; n is zero or an integer from one to four; and corresponding optical isomers thereof; or a pharmaceutically acceptable acid additive salt thereof.

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