发明申请
- 专利标题: SELECTIVE NEUROKININ ANTAGONISTS
- 专利标题(中): 选择性神经营养因子拮抗剂
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申请号: PCT/US2000/033831申请日: 2000-12-14
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公开(公告)号: WO01044200A2公开(公告)日: 2001-06-21
- 主分类号: A61K31/4164
- IPC分类号: A61K31/4164 ; A61K31/4178 ; A61K31/421 ; A61K31/433 ; A61K31/454 ; A61K31/505 ; A61K31/506 ; A61K31/5377 ; A61P1/04 ; A61P1/08 ; A61P1/14 ; A61P3/04 ; A61P3/10 ; A61P9/10 ; A61P11/00 ; A61P11/06 ; A61P13/10 ; A61P15/00 ; A61P17/06 ; A61P19/02 ; A61P25/00 ; A61P25/06 ; A61P25/08 ; A61P25/18 ; A61P25/22 ; A61P25/28 ; A61P29/00 ; A61P31/04 ; A61P37/08 ; C07C45/71 ; C07C217/46 ; C07C217/48 ; C07D211/58 ; C07D233/14 ; C07D233/16 ; C07D233/22 ; C07D233/30 ; C07D233/32 ; C07D233/34 ; C07D233/40 ; C07D233/42 ; C07D233/46 ; C07D233/48 ; C07D233/78 ; C07D239/10 ; C07D263/24 ; C07D285/10 ; C07D401/04 ; C07D401/12 ; C07D403/12 ; C07D405/04 ; C07D409/06 ; C07D413/04 ; C07D413/06 ; C07D413/10 ; C07F9/6506 ; A61K31/4166 ; A61K31/513 ; A61K31/66 ; C07D233/26 ; C07D233/38 ; C07D233/52 ; C07D285/06 ; C07D403/04 ; C07D521/00 ; C07F9/22
摘要:
Compound represented by structural formula (I) or a pharmaceutically acceptable salt thereof, wherein Ar and Ar are optionally substituted heteroaryl or optionally substituted phenyl; X is -O-, -S-, -SO-, -SO2-, -NR -, -NCOR - or -NR SO2R ; (a) is selected from the group consisting of (b), (c), (d) and (e); X is -O-, -S- or -NR -; Y is =O, =S or =NR ; Y is H, C1-C6 alkyl, -NR R , -SCH3, R -aryl(CH2)n6-, R -heteroaryl-(CH2)n6-, -(CH2)n6-heterocycloalkyl, -(C1-C3)alkyl-NH-C(O)O(C1-C6)alkyl or -NHC(O)R ; R is H or -(CH2)n1-G, wherein n1 is 0-5 G is H, -CF3, -CHF2, -CH2F, -OH, -O-(C1-C6 alkyl), -SO2R , -O-(C3-C8 cycloalkyl), -NR R , -SO2NR R , -NR SO2R , -NR COR , -NR (CONR R ), -CONR R , -COOR , C3-C8 cycloalkyl, R -aryl, R -heteroaryl, and provided when n1=0, G is not H; R , R , R and R are H, alkyl, cycloalkyl, -CHF2, -CH2F or -CF3; or R and R , together with the carbon to which they are attached, form an alkylene ring; or R and R together are =O; R is R or -OH; and the remaining variables are as defined in the specifiation, methods of treating diseases susceptible to treatment with neurokinin antagonists with said compounds, and pharmaceutical compositions comprising said compounds are disclosed. Also disclosed are pharmaceutical compositions comprising an effective amount of a compound of claim 1, at least one pharmaceutically acceptable carrier, and in combination with an effective amount of a selective serotonin reuptake inhibitor.