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DERIVATIVES OF PIRROLIDINE AND PIPERIDINE AS ANTAGONISTS OF NK1.
专利权人:
OPKO HEALTH; INC.
发明人:
PALIWAL, SUNIL,REICHARD, GREGORY A.,WANG, CHENG,XIAO, DONG,TSUI, HON-CHUNG,SHIH, NENG-YANG,ARREDONDO, JUAN D.,WROBLESKI, MICHELLE LACI,PALANI, ANANDAN
申请号:
ES07118674
公开号:
ES2372871T3
申请日:
2002.12.17
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
A compound having the formula (I): or a pharmaceutically acceptable salt thereof, in which Ar1 and Ar2 are each X1 is -O-, -S-, -SO-, -SO2-, -NR34-, - N (COR12) - or -N (SO2R15) -; when X1 is -SO-, -SO2-, -N (COR12) - or -N (SO2R15) -, then: R1 and R2 are each independently selected from the group consisting of H, C1-C6 alkyl, hydroxy ( C1-C3 alkyl), C3-C8 cycloalkyl, -CH2F, -CHF2 and -CF3; or R1 and R2, together with the carbon atom to which both are attached, form a C3 to C6 alkylene ring; or when X1 is -O-, -S- or -NR34-, then: R1 and R2 are each independently selected from the group consisting of H, C1-C6 alkyl, hydroxy (C1-C3 alkyl), C3 cycloalkyl- C8, -CH2F, -CHF2 and -CF3; or R1 and R2, together with the carbon atom to which both are attached, form a C3 to C6 alkylene anyl; or R1 and R2, next to each other and the carbon atom to which they are attached, form a group C = O; R3 is selected from the group consisting of H C1-C6 alkyl, hydroxy- (C1-C3 alkyl), C3-C8 cycloalkyl, -CH2F, -CHF2 and -CF3; each R6 is independently selected from the group consisting of H, C1-C6 alkyl and -OH; each R7 is independently selected from the group consisting of H and C1-C6 alkyl; n2 is 1 to 4; R4 is selected from the group consisting of - (CR28R29) n1-G; in which n1 is 0 to 5; and G is H, -CF3, -CHF2-, -CH2F, -O- (C1-C6 alkyl), -OCH2F, -OCHF2, -OCF3, -OCH2CF3, -O- (C3-C8 cycloalkyl), -Oalkyl ( C1-C6) - (C3-C8 cycloalkyl), -NR13R14, -SO2NR13R14, -NR12SO2R13, -NR12C (O) R14, -NR12C (O) OR13, -NR12 (C (O) NR13R14), -C (O) NR13R14, -C (O) OR13, C3-C8 cycloalkyl, (R19) -aryl, (R18) -heteroaryl, -OC (O) R14, -OC (O) NR13R14, -C (= NOR14) (R13), -C (O) R13, -C (OR12) (R13) (R14), heterocycloalkenyl optionally substituted with 1 to 4 substituents independently selected from the group consisting of R30 and R31, R5 is selected from the group consisting of - ( CR28R29) n1-G, in which n1 is 0 to 5; and G is -CF3, -CHF2-, -CH2F, -O- (C1-C6 alkyl), -OCH2F, -OCHF2, -OCF3, -OCH2CF3, -5 O- (C3-C
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