PGI Drug Discovery LLC.;SUNOVION PHARMACEUTICALS INC.
发明人:
Campbell John Emmerson,Campbell Una,Hanania Taleen G,Hewitt Michael Charles,Shao Liming
申请号：
NZ71180210
公开号：
NZ711802A
申请日:
2010.12.03
申请国别(地区):
NZ
年份:
2017
代理人:
摘要：
Disclosed are 7-aminoalkyl-thieno[2,3-c]pyran derivatives and analogues of formula (IVa) or a pharmaceutically acceptable salt or stereoisomer thereof, wherein (i) R1 and R3 together with the atoms to which they are attached form an optionally substituted heterocyclyl, and R4 is hydrogen or alkyl； or (ii) R3 and R4 together form a double bond and together with R1 and the atoms to which they are attached form an optionally substituted 5- to 20-membered heteroaryl； R2 is hydrogen, alkyl or absent； R5 is hydrogen or alkyl； R6 and R7 are each independently (i) hydrogen, halo, alkyl, alkoxyl, aminoalkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, or arylalkyl, each of which is optionally substituted； or (ii) -(CH2)p-R11, wherein R11 is CF3, CN, nitro, amino (-NH2), hydroxyl, cycloalkoxyl, heteroaryl, or heterocyclyl, each of which is optionally substituted； m is 0, 1, or 2； n is 0, 1, or 2； and each occurrence of p is independently 0, 1, or 2； and wherein the remaining substituents are as defined herein； wherein ‘cycloalkyl’ refers to a cyclic fully or partially saturated bridged and/or non-bridged hydrocarbon radical or ring system； and wherein ‘aminoalkyl’ refers to a stable straight or branched chain, or cyclic hydrocarbon radical, or combinations thereof having one or more N atoms. Representative compounds include 7-(R)-((2S)-pyrrolidin-2-yl)-4,6-dihydro-thieno[2,3-c]pyran, 7-(S)-((2S)-pyrrolidin-2-yl)-4,6-dihydro-thieno[2,3-c]pyran, 7-(R)-((2R)-pyrrolidin-2-yl)-4,6-dihydro-thieno[2,3-c]pyran, 7-(S)-((2R)-pyrrolidin-2-yl)-4,6-dihydro-thieno[2,3-c]pyran, 7-(S)-(imidazol-4-yl)-4,6-dihydro-thieno[2,3-c]pyran and 7-(2-methylpyrazol-3-yl)-4,6-dihydro-thieno[2,3-c]pyran. Also disclosed is a pharmaceutical composition comprising a compounds as defined above, and optionally further comprising one or more additional active agents, for treating a neurological disorder such as schizophrenia, psychotic disorders, Parkinson’s psychosis, Tourette’s syndrome, post-traumat
