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Alkylthiopyrimidines as CRTH2 antagonists
- 专利权人:
- ACTIMIS PHARMACEUTICALS; INC.
- 发明人:
- LY, TAI,RAAUM, ERIK,TRAN, MARIE
- 申请号:
- ES08833849
- 公开号:
- ES2383249T3
- 申请日:
- 2008.09.24
- 申请国别(地区):
- ES
- 年份:
- 2012
- 代理人:
- 摘要:
- A compound having the formula I: ** Formula ** or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer or tautomer thereof, where W is a single bond, - (CH2) m-, -O-, -S (O ) n, -NR7-, -C (O) -, -C (O) O-, -C (O) NR7--, NR7C (O) NR7, or -NR7C (O) O-; R1 is -CO2R9 -C (O) NR8aR8b, nitrile or tetrazolyl; R2 is (a) hydrogen; (b) halogen; (c) (C1-C6) alkyl; (d) (C1-C6) alkyl substituted by aryl, hydroxy, carboxyl, alkoxy, carbamoyl, (C1-C6) alkyl carbamoyl, dialkyl (C1-C6) carbamoyl, cycloalkyl (C3-C7) carbamoyl or heterocyclyl (C3-C7) carbamoyl; (e) (C1-C6) alkyl substituted with mono-, di- or tri-halogen; (t) cycloalkyl (C3-C7); (g) -NR8aR8b, (h) -SR3; or (i) (C1-C6) alkoxy optionally substituted with mono-, di- or tri-halogen, each R3 is independently (a) hydrogen; (b) (C1-C6) alkyl optionally substituted with mono-, di-, or trihalogen; (c) cycloalkyl (C3-C7) or (d) -C (O) R9; R4a and R4b are each independently selected from hydrogen or (C1-C6) alkyl; each R5 is independently (a) hydrogen; (b) halogen; (c) cyano; (d) nitro; (e) hydroxy; (f) phenyl; (g) phenyloxy; (h) benzyl; (i) benzyloxy; (j) guanidino; (k) heterocyclyl; (I) -NR8aR8b; (m) sulfamoyl; (n) (C1-C6) alkylsulfonyl; (o) (C1-C6) alkyl aminosulfonyl; (p) dialkyl (C1-C6) aminosulfonyl; (q) -C (O) R9; (r) -C (O) OR9; (s) -C (O) NR8aR8b; (t) -OC (O) NR8aR8b; (u) -NR7C (O) OR9; (v) -NR7COR9; (w) alkenylol (C2-C6); (x) (C1-C6) alkyl optionally substituted with mono-, di- or tri-halogen; (y) (C1-C6) alkoxy optionally substituted with mono-, di- or trihalogen; or (z) alkylthio (C1-C6) optionally substituted with mono-, di- or tri-halogen; R6 is (a) hydrogen; (b) (C1-C6) alkyl; (c) C2-C6 alkenyl; (d) (C2-C6) alkynyl; (e) cycloalkyl (C3-C7); (f) (C1-C6) alkyl substituted with aryl or heteroaryl; (g) (C2-C4) alkenyl substituted with aryl or heteroaryl; (h) (C1-C6) alkyl substituted with mono-, di- or tri-halogen; (i) (C1-C6) alkyl substituted with -C (O) R6a; (j) (C1-C6) alkoxysubstituted with mono-, di-
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