Centrally actig substituted phenylazacycloalkanes
Patent 5594024 Issued on January 14, 1997. Estimated Expiration Date: 
May 31, 2015. 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.
May 31, 2015. 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 1-aminomethyl-1,2,3,4-tetrahydronaphthalenes Process for preparing cyclic amines and intermediate products thereof Arylcycloalkanepolyalkylamine ligands Patent #: 5223530 Inventors
AssigneeApplicationNo. 455474 filed on 05/31/1995US Classes:514/429, Carbocyclic ring bonded directly to the five-membered hetero ring514/422, Additional hetero ring546/218, The chalcogen, X, is part of a -C(=X)X- group, wherein the X's are the same or diverse chalcogens548/146, 1,3-thiazoles (including hydrogenated)548/215, 1,3-oxazoles (including hydrogenated)548/250, Tetrazoles (including hydrogenated)548/517, Additional hetero ring, which is attached directly or indirectly to the five-membered hetero ring by nonionic bonding548/518, The additional hetero ring also contains nitrogen548/577Benzene ring bonded directly to the five-membered hetero ringExaminersPrimary: Chang, CeilaAttorney, Agent or FirmForeign Patent References
International ClassesA61K 031/40C07D 207/04 AbstractA compound or 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, C2 -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 SearchBenzene ring bonded directly to the five-membered hetero ring1,3-thiazoles (including hydrogenated) Additional hetero ring, which is attached directly or indirectly to the five-membered hetero ring by nonionic bonding 1,3-oxazoles (including hydrogenated) The additional hetero ring also contains nitrogen Tetrazoles (including hydrogenated) The chalcogen, X, is part of a -C(=X)X- group, wherein the X's are the same or diverse chalcogens Additional hetero ring Carbocyclic ring bonded directly to the five-membered hetero ring The additional hetero ring consists of one nitrogen and four carbons (e.g., nicotine, etc.) |
| ||||||||||||||
