| 摘要 |
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to substituted quinoxaline-type piperidine compounds of formulaor to a pharmaceutically acceptable derivative thereof, wherein: Yrepresents O; Q is specified in condensed benzo or pyridino; each Ris independently specified in: (a) -halogen or -CN; (b) -(C-C)alkyl; a is an integer specified in 0, 1 or 2; a dash line in a 6-member ring containing a nitrogen atom which is condensed with Q group means the presence or absence of a bond, and when the dash line means the absence of the bond, then R, and one Rare absent; Ris specified in: (a) -H; each Ris independently specified in: (a) -H; or (b) - halogen or CN; or (c) -X, -(C-C)alkyl-X, -(5- or 6-member)heterocyclyl-X or -(5- or 6-member)heterocyclyl-(C-C)alkyl-X; or (d) -C(=Y)X, -C(=Y)T, -C(=Y)YX, - C(=Y)YT, -C(-Y)N(T)(T), -C(=Y)N(R)CN, -C(=Y)N(R)X, -C(=Y)N(R)YH, -C(=Y)N(R)YX, -C(=Y)N(R)YCHX, -C(-Y)N(R)YCHCHX or -C(=Y)N(R)S(K))T; or (e) -N(R)X, -N(R)-CHX, -N(R)-CHCHX, -N(R)CHN(R)C(=N(R))N(R), -N(R)-CHCHN(R)C(=N(R))N(R), -N(T)(T), -N(T)C(=Y)T, -N(T)C(=Y)YT, -N(T)C(=Y)N(T)(T), -N(T)S(=O)Tor -N(T)S(=O)N(T)(T); X represents: (a) -H, -( C-C)alkyl, -(C-C)alkenyl, -(C-C)alkoxy, -(C-C)cycloalkyl, -(5- or 6-member)heterocycle or -(7-10-member)bicycloheterocycle each of which is unsubstituted or substituted with 1, 2 or 3 of optionally substituted Rgroups; or (b) -phenyl, -naphthalenyl, or -(5- or 6-member)heteroaryl each of which is unsubstituted or substituted with 1 or 2 of independently specified in Rgroups; each Y is independently specified in O; A and B are independently specified in: (a) -H; or (c) A-B together can form a (C-C)bridge each can optionally contain -HC=CH- or -O- in a (C-C)bridge; wherein the 6-member ring containing a nitrogen atom which is condensed with Q group can be found in the endo- or exo- configuration in relation to the A-B bridge; or (d) A-B together can form the -CH-N(R)-CH- bridge wherein the 6-member ring containing a nitrogen atom is condensed with Q group, and can be found in the endo- or exo- configuration in relation to the A-B bridge; Ris specified in -H or -(C-C)alkyl; Z represents -[(C-C)alkyl optionally substituted with R]-, wherein h is equal to 0 or 1; each Ris independently specified in: (b) -(C-C)alkyl, -(C-C)alkenyl, -(C-C)alkynyl-(C-C)cycloalkoxy, -(C-C)bicycloalkyl, -(CC)tricycloalkyl, -(C-C)cycloalkenyl, -(C-C)bicycloalkenyl, -(3-7-member)heterocyclyl each of which is unsubtituted or substituted with 1, 2 or 3 of independently specified in Rgroups;oror (d) -phenyl, -naphthalenyl each of which is unsubstituted or substituted with Rgroup; each Ris optionally specified in -H; each Ris independently specified in -(C-C)alkyl, -OR, -C(halogen), -CH(halogen), -CH(halogen), -CN, -halogen, -N(R), -C(=O)OR; each Ris independently specified in -(C-Calkyl, tetrzolyl, imidazolyl, furanyl, -(C-C)alkylCOOR, -OR, -SR, -C(halogen), -CH(halogen), -CH(halogen), -CN, =O, -halogen, -N(R)(C-C)alkylCOOR, -N(R), -N(R)S(=O)R, -N(R)C(=O)R, -N(R)C(=O)OR, -C(=O)R, -C(=O)N(T)(T), -C(=O)OR, -OC(=O)R, or -S(=O)R; each Ris independently specified in -H, -(C-C)alkyl, -(C-C)cycloalkyl, -phenyl, -benzyl, -(5- to 6-member)heterocycle, -C(halogen); -CH(halogen)or -CH(halogen); if h is equal to O, then Rcan be specified in -H, -C(=O)ORor -C(=O)N(R)or Rcan be -(C-C)alkyl; if h is equal to 1, then Rcan be specified in -H; each Ris independently specified in -H or -(C-C)alkyl; m is equal to an integer specified in 3, 4, 5, 6, 7, 8 or 9; each e and f is equal to an integer independently specified in 0 or 1, provided 2?(e+f)?5; each j and k is equal to an integer independently specified in 0 or 1, provided 1?(j+k)?4; each p is equal to an integer independently specified in 0 or 1; each T, T, and Tis independently specified in -H or -(C-C)alkyl which is unsubstituted or substituted with 1, 2 or 3 from independently specified Rgroups, or Tand Ttogether can form 5- to 8-member ring wherein the number of ring atoms contains a nitrogen atom wherein Tand Tare bound; the above 5- to 8-member ring is unsubstituted or substituted with 1, 2 or 3 from independently specified Rgroups and optionally any carbon atom in the above 5- to 8-member ring is independently substituted with O or N(R); each halogen is independently specified in -F, -CI, -Br or -I.EFFECT: invention refers to the intermediate compounds of formula,,for preparing the above compounds of formula (II), compositions containing the above compounds and to a method of treating or preventing a diseased state, such as a pain.36 cl, 58 ex, 2 tbl |
