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:
NZ62606810
公开号:
NZ626068A
申请日:
2010.12.03
申请国别(地区):
NZ
年份:
2016
代理人:
摘要:
Disclosed are thieno[3,2-c]pyran derivatives as represented by the general formula (IIa) or a pharmaceutically acceptable salt or stereoisomer thereof, wherein: R1 and R2 are each independently hydrogen, alkyl, or cycloalkyl, each of which is optionally substituted, or R1 and R2 together with the nitrogen atom to which they are attached form an optionally substituted heterocyclyl or heteroaryl, wherein at least one of R1 and R2 is not hydrogen; R3 and R4 are each independently (i) hydrogen or optionally substituted alkyl; or (ii) R3 and R4 together with the carbon atom to which they are attached form an optionally substituted cycloalkyl or heterocyclyl ring; or (iii) R3 and R1 together with the atoms to which they are attached form an optionally substituted heterocyclyl, and R4 is hydrogen; or (iv) R3 and R4 are combined together to form a double bond and together with R1 and/or R2 and the atoms to which they are attached form an optionally substituted heteroaryl; R5 is hydrogen or optionally substituted alkyl; R6 and R7 are each independently (i) hydrogen, halo, alkyl, alkoxyl, aminoalkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, or aralkyl, each of which is optionally substituted; or (ii) –(CH2)p–R11, wherein R11 is heteroaryl; m is 0; n is 1; and each occurrence of p is 0; wherein the substituents and terms such as hydrogen, alkyl, alkenyl, cycloalkyl, alkoxyl, aminoalkyl etc. are as defined herein. Representative compounds include N,N-dimethyl-6,7-dihydro-4H-thieno[3,2-c]pyran-4-methanamine, N-methyl-6,7-dihydro-4H-thieno[3,2-c]pyran-4-methanamine, N-methyl-2-(pyridin-4-yl)-6,7-dihydro-4H-thieno[3,2-c]pyran-4-methanamine, 2-methyl-4-(pyrrolidin-1-ylmethyl)-6,7-dihydro-4H-thieno[3,2-c]pyran, 4-(pyrrolidin-2-yl)-6,7-dihydro-4H-thieno[3,2-c]pyran and N-methyl-1-(6,7-dihydro-4H-thieno[3,2-c]pyran-4-yl)cyclopropylamine. Also disclosed is a pharmaceutical composition comprising a compound as defined above, or a pharmaceutically acceptable salt