公开(公告)号：EP0873123B1

公开(公告)日：2003-04-09

申请号：EP96938647.3

申请日：1996-11-05

申请人： UNIVERSITY OF PITTSBURGH

发明人： SEBTI, Said, M. ,  HAMILTON, Andrew, D. ,  ROSENBERG, Saul, H. ,  AUGERI, David, J. ,  BARR, Kenneth, J. ,  DONNER, Bernard, G. ,  FAKHHOURY, Stephen, A. ,  JANOWICK, David, A. ,  KALVIN, Douglas, M. ,  LARSEN, John, J. ,  LIU, Gang ,  O'CONNOR, Stephen, J. ,  SHEN, Wang ,  SWENSON, Rolf, E. ,  SORENSON, Bryan, K. ,  SULLIVAN, Gerard, M. ,  SZCZEPANKIEWICZ, Bruce ,  TASKER, Andrew, S. ,  WASICAK, James, T. ,  WINN, Martin

IPC分类号： A61K31/415 ,  A61K31/44 ,  C07D213/34 ,  C07D213/30 ,  C07D213/62 ,  C07D213/72 ,  C07D233/70 ,  C07D233/84 ,  C07D233/88 ,  C07D213/82 ,  C07D213/56 ,  C07D233/54 ,  C07D233/90 ,  C07D405/12 ,  C07D405/04 ,  C07D417/12 ,  C07D401/12

CPC分类号： C07D213/30 ,  C07D213/32 ,  C07D213/34 ,  C07D213/36 ,  C07D213/56 ,  C07D213/64 ,  C07D213/70 ,  C07D213/71 ,  C07D213/74 ,  C07D213/75 ,  C07D213/82 ,  C07D213/89 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D233/90 ,  C07D249/08 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

摘要： Compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R1 is selected from: (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halogen, (g) haloalkyl, (h) aryl-L2 - and (i) heterocyclic - L3; R2 is selected from the group consisting of: (a) formula (II), (b) -C(O)NH-CH(R14)-C(O)OR15, (c) formula (III), (d) -C(O)NH-CH(R14)-C(O)NHSO2R16, (e) -C(O)NH-CH(R14)-tetrazolyl, (f) -C(O)NH-heterocyclic, and (g) -C(O)NH-CH(R14)-C(O)NR17R18; R3 is pyridyl, substituted pyridyl, imidazolyl, or substituted imidazolyl; R4 is selected from hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, and (heterocyclic)alkyl; and L1 is absent or is selected from (a) -L4-N(R4)-L5-, (b) -L4-O-L5-, (c) -L4-S(O)n-L5-, (d) -L4-L6-C(W)-N(R5)-L5-, (e) -L4-L6-S(O)m-N(R7)-L5-, (f) -L4-N(R7)-C(W)-L7-L5-, (g) -L4-N(R7)-S(O)p-L7-L5-, (h) C2-C4-alkylene optionally substituted with 1 or 2 hydroxy groups, (i) C2-to-C4-alkenylene, and (j) C2-to-C4-alkynylene, are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.

公开(公告)号：EP0873123A1

公开(公告)日：1998-10-28

申请号：EP96938647.0

申请日：1996-11-05

申请人： UNIVERSITY OF PITTSBURGH

发明人： SEBTI, Said, M. ,  HAMILTON, Andrew, D. ,  ROSENBERG, Saul, H. ,  AUGERI, David, J. ,  BARR, Kenneth, J. ,  DONNER, Bernard, G. ,  FAKHHOURY, Stephen, A. ,  JANOWICK, David, A. ,  KALVIN, Douglas, M. ,  LARSEN, John, J. ,  LIU, Gang ,  O'CONNOR, Stephen, J. ,  SHEN, Wang ,  SWENSON, Rolf, E. ,  SORENSON, Bryan, K. ,  SULLIVAN, Gerard, M. ,  SZCZEPANKIEWICZ, Bruce ,  TASKER, Andrew, S. ,  WASICAK, James, T. ,  WINN, Martin

IPC分类号： C07D233 ,  A61K31 ,  A61P9 ,  A61P35 ,  A61P43 ,  C07D213 ,  C07D401 ,  C07D405 ,  C07D409 ,  C07D413 ,  C07D417 ,  C07D471 ,  C07D493 ,  C07D521 ,  C07F7

CPC分类号： C07D213/30 ,  C07D213/32 ,  C07D213/34 ,  C07D213/36 ,  C07D213/56 ,  C07D213/64 ,  C07D213/70 ,  C07D213/71 ,  C07D213/74 ,  C07D213/75 ,  C07D213/82 ,  C07D213/89 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D233/90 ,  C07D249/08 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

摘要： Compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R1 is selected from: (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halogen, (g) haloalkyl, (h) aryl-L2 - and (i) heterocyclic - L3; R2 is selected from the group consisting of: (a) formula (II), (b) -C(O)NH-CH(R14)-C(O)OR15, (c) formula (III), (d) -C(O)NH-CH(R14)-C(O)NHSO2R16, (e) -C(O)NH-CH(R14)-tetrazolyl, (f) -C(O)NH-heterocyclic, and (g) -C(O)NH-CH(R14)-C(O)NR17R18; R3 is pyridyl, substituted pyridyl, imidazolyl, or substituted imidazolyl; R4 is selected from hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, and (heterocyclic)alkyl; and L1 is absent or is selected from (a) -L4-N(R4)-L5-, (b) -L4-O-L5-, (c) -L4-S(O)n-L5-, (d) -L4-L6-C(W)-N(R5)-L5-, (e) -L4-L6-S(O)m-N(R7)-L5-, (f) -L4-N(R7)-C(W)-L7-L5-, (g) -L4-N(R7)-S(O)p-L7-L5-, (h) C2-C4-alkylene optionally substituted with 1 or 2 hydroxy groups, (i) C2-to-C4-alkenylene, and (j) C2-to-C4-alkynylene, are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.