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    POLYCYCLIC ALCALOID-DERIVATIVES AS NMDA-RECEPTOR ANTAGONISTS
    1.
    发明公开
    POLYCYCLIC ALCALOID-DERIVATIVES AS NMDA-RECEPTOR ANTAGONISTS 失效
    多环生物碱衍生物作为NMDA受体拮抗剂

    公开(公告)号：EP0840731A1

    公开(公告)日：1998-05-13

    申请号：EP96922703.0

    申请日：1996-07-12

    申请人： BIOCHEM PHARMA INC.

    发明人： DIMAIO, John ,  DIXIT, Dilip, M.

    IPC分类号： A61K31 ,  A61P25 ,  A61P43 ,  C07C215 ,  C07D221 ,  C07D225 ,  C07D313 ,  C07D337

    CPC分类号： C07C215/44 ,  C07D225/08 ,  C07D313/20 ,  C07D337/16

    摘要： Polycyclic alkaloids of formula (I), wherein R1 is H, C1-6 alkyl, or C6-12 aryl optionally substituted with polar groups; R2 abd R3 are independently H, OH, C1-6 alkyl, -C(NH)-NH2, a positively charged group, or C7-13 aralkyl optionally substituted with NH2, OH, C1-6 alkyl, or halogen; or R2 and R3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R4 is H, C1-6 alkyl, OR6, SR6 or N(R6)2, wherein each R6 is independently H, C1-3 alkyl; X is O, S, SO, SO2, N-R5, or C-(R5)2, wherein each R5 is independently H, C1-6 alkyl, or C7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; m is an integer from 0 to 3; with the proviso that when X is CH2 then R1 is not CH3, R2 and R3 are not both H, R4 is not OH, m is not 3 and n is not 0. That act as antagonists at the ionotropic NMDA (N-methyl-(D)-aspartic acid) receptor.

    NOVEL HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF PAIN AND USE THEREOF
    2.
    发明授权
    NOVEL HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF PAIN AND USE THEREOF 失效
    杂环化合物疼痛治疗及其用途

    公开(公告)号：EP0850234B1

    公开(公告)日：2001-11-28

    申请号：EP96921855.1

    申请日：1996-07-12

    申请人： Shire Biochem Inc.

    发明人： DIMAIO, John ,  DIXIT, Dilip M

    IPC分类号： C07D337/16 ,  C07D313/20 ,  A61K31/38

    CPC分类号： C07C215/44 ,  C07D225/08 ,  C07D313/20 ,  C07D337/16

    摘要： Polycyclic alkaloids of formula (I), wherein R1 is H, C1-6 alkyl, or C6-12 aryl optionally substituted with polar groups; R2 and R3 are independently H, OH, C1-6 alkyl, -C(NH)-NH2, a positively charged group, or C7-13 aralkyl optionally substituted with NH2, OH, C1-6 alkyl, or halogen; or R2 and R3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R4 is H, C1-6 alkyl, OR6, SR6 or N(R6)2, wherein each R6 is independently H, C1-3 alkyl, or halogen; X is O, S, SO, SO2, N-R5, or C-(R5)2, wherein each R5 is independently H, C1-6 alkyl, or C7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; m is an integer from 0 to 3; with the proviso that when X is CH2 then R1 is not CH3, R2 and R3 are not both H, R4 is not OH, m is not 3 and n is not 0. For the treatment of pain and pharmaceutically acceptable compositions comprising those compounds. The compounds of this invention act as agonists at the opiate receptor.

    NOVEL HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF PAIN AND USE THEREOF
    4.
    发明公开
    NOVEL HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF PAIN AND USE THEREOF 失效
    杂环化合物疼痛治疗及其用途

    公开(公告)号：EP0850234A1

    公开(公告)日：1998-07-01

    申请号：EP96921855.0

    申请日：1996-07-12

    申请人： BIOCHEM PHARMA INC.

    发明人： DIMAIO, John ,  DIXIT, Dilip M

    IPC分类号： A61K31 ,  A61P25 ,  A61P43 ,  C07C215 ,  C07D221 ,  C07D225 ,  C07D313 ,  C07D337

    CPC分类号： C07C215/44 ,  C07D225/08 ,  C07D313/20 ,  C07D337/16

    摘要： Polycyclic alkaloids of formula (I), wherein R1 is H, C1-6 alkyl, or C6-12 aryl optionally substituted with polar groups; R2 and R3 are independently H, OH, C1-6 alkyl, -C(NH)-NH2, a positively charged group, or C7-13 aralkyl optionally substituted with NH2, OH, C1-6 alkyl, or halogen; or R2 and R3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R4 is H, C1-6 alkyl, OR6, SR6 or N(R6)2, wherein each R6 is independently H, C1-3 alkyl, or halogen; X is O, S, SO, SO2, N-R5, or C-(R5)2, wherein each R5 is independently H, C1-6 alkyl, or C7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; m is an integer from 0 to 3; with the proviso that when X is CH2 then R1 is not CH3, R2 and R3 are not both H, R4 is not OH, m is not 3 and n is not 0. For the treatment of pain and pharmaceutically acceptable compositions comprising those compounds. The compounds of this invention act as agonists at the opiate receptor.

    POLYCYCLIC ALCALOID-DERIVATIVES AS NMDA-RECEPTOR ANTAGONISTS
    8.
    发明授权
    POLYCYCLIC ALCALOID-DERIVATIVES AS NMDA-RECEPTOR ANTAGONISTS 失效
    多环生物碱衍生物作为NMDA受体拮抗剂

    公开(公告)号：EP0840731B1

    公开(公告)日：2001-10-10

    申请号：EP96922703.2

    申请日：1996-07-12

    申请人： Shire Biochem Inc.

    发明人： DIMAIO, John ,  DIXIT, Dilip, M.

    IPC分类号： A61K31/38

    CPC分类号： C07C215/44 ,  C07D225/08 ,  C07D313/20 ,  C07D337/16

    摘要： Polycyclic alkaloids of formula (I), wherein R1 is H, C1-6 alkyl, or C6-12 aryl optionally substituted with polar groups; R2 abd R3 are independently H, OH, C1-6 alkyl, -C(NH)-NH2, a positively charged group, or C7-13 aralkyl optionally substituted with NH2, OH, C1-6 alkyl, or halogen; or R2 and R3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R4 is H, C1-6 alkyl, OR6, SR6 or N(R6)2, wherein each R6 is independently H, C1-3 alkyl; X is O, S, SO, SO2, N-R5, or C-(R5)2, wherein each R5 is independently H, C1-6 alkyl, or C7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; m is an integer from 0 to 3; with the proviso that when X is CH2 then R1 is not CH3, R2 and R3 are not both H, R4 is not OH, m is not 3 and n is not 0. That act as antagonists at the ionotropic NMDA (N-methyl-(D)-aspartic acid) receptor.