Centrally acting substituted phenylazacycloalkanes
Patent 5462947 Issued on October 31, 1995. Estimated Expiration Date: 
October 12, 2013. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
October 12, 2013. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.Patent ReferencesNew phenylazacycloalkanes Method for using m-trifluoromethylphenyl-piperidines 3-[2,4-(Disubstituted)-phenyl]azacycloalkanones as analgesics Fungicidal N-substituted 3-arylpyrrolidine derivatives Fungicidal N-substituted 3-alkyl-4-arylpyrrolidine derivatives Patent #: 5068246 Inventors
AssigneeApplicationNo. 133606 filed on 10/12/1993US Classes:514/317, Additional ring containing514/331, Nitrogen attached indirectly to the piperidine ring by nonionic bonding546/192, Additional ring containing546/229, Nitrogen attached indirectly to the piperidine ring by nonionic bonding546/230, Cyano attached indirectly to the piperidine ring by nonionic bonding546/237, The chalcogen, X, is in a -C(=X)- group546/238, The -C(=X)- is part of a -C(=X)X- group, wherein the X's are the same or diverse chalcogens546/240The chalcogen is in an -OH or -OM group (M is Group IA or Group IIA light metal)ExaminersPrimary: Chang, CeilaAttorney, Agent or FirmForeign Patent References
International ClassesA61K 031/445C07D 211/18 AbstractA compound of Formula I ##STR1## or a pharmaceutically acceptable salt thereof wherein n is 1 or 2; R1 and R2 are independently H (provided only one is H at the same time), --OH, CN, CH2 CN, 2-- or 4--CF3, CH2 CF3, CH2 CHF2, CH=CF2, (CH2)2 CF3, ethenyl, 2-propenyl, OSO2 CH3, OSO2 CF3, SSO2 CF3, COR, COOR, CON(R)2, SOx CH3 (where, x is 0-2), SOx CF3, O(CH2)x CF3, SO2 N(R)2, CH=NOR, COCOOR, COCOON(R)2, C1-8 alkyls, C3-8 cycloalkyls, CH2 OR, CH2 (R)2, NRSO2 CF3, NO2, halogen, a phenyl at positions 2, 3 or 4, thienyl, furyl, pyrrole, oxazole, thiazole, N-pyrroline, triazole, tetrazole or pyridine; R3 is hydrogen, CF3, CH2 CF3, C1 -C8 alkyl, C3 -C8 cycloalkyl, C4 -C9 cycloalkyl-methyl, C.sub. 2 -C8 alkenyl, C2 -C8 alkynyl, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, --(CH2)m --R5 (where m is 1-8), CH2 SCH3 or a C4 -C8 alkylene bonded to said nitrogen and one of its adjacent carbon atoms inclusive whereby a heterocyclic structure is formed; R4 and R are independently selected from hydrogen, CF3, CH2 CF3, C1 -C8 alkyl, C3 -C8 cycloalkyl, C4 -C9 cycloalkyl-methyl, C2 -C8 alkenyl, C2 -C8 alkynyl, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, --(CH2)m --R5 where m is 1-8; R5 is phenyl, phenyl (substituted with a CN, CF3, CH2 CF3, C1 -C8 alkyl, C3 -C8 cycloalkyl, C4 -C9 cycloalkyl-methyl, C2 -C8 alkenyl, C2 -C8 alkynyl), 2-thiophenyl, 3-thiophenyl, --NR6 CONR6 R7, or --CONR6 R7 ; R6 and R7 are independently hydrogen, C1 -C8 alkyl, C3 -C8 cycloalkyl, C4 -C9 cycloalkylmethyl, C2 -C8 alkenyl or C2 -C8 alkynyl; and with the proviso that when R1 is CN, R2 and R4 are H, R3 is n-Pr and n is 1, then such compound is a pure enantiomer, and when R1 or R2 is OH, halogen, CONH2 or alkyl, then R4 is not hydrogen. The Formula I compounds possess selective pharmacological properties and are useful in treating central nervous system disorders related to dopamine receptor activity including depression symptoms, geriatric disorders in the improvement of mental and motor functions, schizophrenia, narcolepsy, MBD, obesitas, and disturbances of sexual functions and impotence.Other References
Field of SearchAdditional ring containingNitrogen attached indirectly to the piperidine ring by nonionic bonding Cyano attached indirectly to the piperidine ring by nonionic bonding The chalcogen, X, is in a -C(=X)- group The -C(=X)- is part of a -C(=X)X- group, wherein the X's are the same or diverse chalcogens The chalcogen is in an -OH or -OM group (M is Group IA or Group IIA light metal) Additional ring containing Nitrogen attached indirectly to the piperidine ring by nonionic bonding |
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