发明名称 SUBSTITUTED 2-BENZILAMINO-2-PHENYL-ACETAMIDE COMPOUNDS
摘要 1. A compound which is a substituted 2-benzylamino-2-phenyl acetamide of formula (I) wherein: n is zero, 1, 2 or 3; X is -O-, -S-, -CH2- or -NH-; each of R, R1, R2 and R3, independently, is hydrogen, C1-C6 alkyl, halogen, hydroxy, C1-C6 alkoxy or trifluoromethyl; each of R4 and R5, independently, is hydrogen, C1-C6 alkyl or C3-C7 cycloalkyl; or a pharmaceutically acceptable salt thereof. 2. A compound according to Claim 1, wherein n is 1 or 2; X is -O-; each of R, R1, R2 and R3, independently, is hydrogen, or halogen; R4 and R5 are hydrogen. 3. A compound according to Claim 1, which is selected from: 2-[4-benzyloxybenzylamino]-2-phenylacetamide; 2-[4-(3-fluorobenzyloxy)benzylamino]-2-phenylacetamide; 2-[4-(3-chlorobenzyloxy)benzylamino]-2-phenylacetamide; 2-[4-(3-bromobenzyloxy)benzylamino]-2-phenylacetamide; 2-[4-(2-fluorobenzyloxy)benzylamino]-2-phenylacetamide; 2-[4-(3-fluorobenzyloxy)benzylamino]-2-(2-fluorophenyl)-acetamide; 2-[4-(3-fluorobenzyloxy)benzylamino]-2-(3-fluorophenyl)-acetamide; and 2-[4-(3-chlorobenzyloxy)benzylamino]-2-(3-fluorophenyl)-acetamide, if the case either as a single isomer or as a mixture thereof, or a pharmaceutically acceptable salt thereof. 4. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and, as an active agent, a compound as defined in Claim 1. 5. A compound as defined in Claim 1, for use in a method of treatment of the human or animal body by therapy. 6. A compound as claimed in Claim 5 for use in regulating a physiological condition related to sodium channel blockade. 7. A compound as claimed in Claim 5, for use in treating chronic or neuropathic pain. 8. A method of treating a mammal, including a human, in need of a sodium channel-blocking agent, said method comprising administering thereto an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof. 9. A method according to Claim 8 wherein the mammal is suffering from chronic or neuropathic pain.
申请公布号 EA003097(B1) 申请公布日期 2002.12.26
申请号 EA20000000728 申请日期 1998.12.12
申请人 NEWRON PHARMACEUTICALS S.P.A. 发明人 PEVARELLO, PAOLO;VARASI, MARIO;SALVATI, PATRICIA;POST, CLAES
分类号 A61P25/04;A61K31/16;A61K31/165;A61P25/00;A61P43/00;C07C237/20 主分类号 A61P25/04
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