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    PROCESS FOR PRODUCING CYCLIC COMPOUND
    4.
    发明申请
    PROCESS FOR PRODUCING CYCLIC COMPOUND 审中-公开
    生产环化合物的方法

    公开(公告)号：WO01060768A1

    公开(公告)日：2001-08-23

    申请号：PCT/JP2001/001190

    申请日：2001-02-20

    IPC: C07D225/06 ,  C07D313/08 ,  C07D313/20 ,  C07B37/10

    CPC classification number: C07D225/06 ,  C07D313/08 ,  C07D313/20

    Abstract: A process suitable for safely mass-producing, through a short step, cyclic compounds useful in medicines, agricultural chemicals, foods, cosmetics, and chemical products or as intermediates therefor. The process, which is for producing a compound represented by the formula (I) or a salt thereof: {wherein Z represents an electron-attracting group; W represents optionally substituted ethylene or optionally substituted vinylene; R represents hydrogen or an optionally substituted hydrocarbon group; and X represents a divalent group [provided that when W represents optionally substituted vinylene, then -X-CH2-Z is not -X -X -CH2-Z (wherein X represents sulfur or optionally substituted nitrogen and X represents optionally substituted ethylene)]}, is characterized by subjecting a compound represented by the formula (II) or a salt thereof: (wherein the symbols have the same meanings as the above) to a ring closure reaction in a solvent containing a carbonic diester.

    Abstract translation: 一种适用于通过短步安全批量生产用于药物，农药，食品，化妆品和化学产品的环状化合物或其中间体的方法。 该方法用于制备由式（I）表示的化合物或其盐：其中Z表示吸电子基团; W表示任选取代的乙烯或任选取代的亚乙烯基; R 3表示氢或任选取代的烃基; 并且X表示二价基团[条件是当W表示任选取代的亚乙烯基时，则-X-CH 2 -Z不是-X 1 -X 2 -CH 2 -Z（其中X 1表示硫或任选取代的 氮和X 2表示任选取代的乙烯）]}的特征在于使式（II）表示的化合物或其盐：（其中符号具有与上述相同的含义）进行闭环反应 含有碳酸二酯的溶剂。

    NOVEL HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF PAIN AND USE THEREOF
    7.
    发明申请
    NOVEL HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF PAIN AND USE THEREOF 审中-公开
    用于治疗疼痛和用途的新型杂环化合物

    公开(公告)号：WO1997003978A1

    公开(公告)日：1997-02-06

    申请号：PCT/CA1996000467

    申请日：1996-07-12

    Applicant: BIOCHEM PHARMA INC. ,  DIMAIO, John

    Inventor： BIOCHEM PHARMA INC.

    IPC: C07D337/16

    CPC classification number: C07C215/44 ,  C07D225/08 ,  C07D313/20 ,  C07D337/16

    Abstract: 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.

    Abstract translation: 式（I）的多环生物碱，其中R 1为H，C 1-6烷基或任选被极性基团取代的C 6-12芳基; R2和R3独立地是H，OH，C1-6烷基，-C（NH）-NH2，带正电荷的基团或任选被NH 2，OH，C 1-6烷基或卤素取代的C 7-13芳烷基; 或R 2和R 3一起形成任选地加入杂原子的5至6元环; R4是H，C1-6烷基，OR6，SR6或N（R6）2，其中每个R6独立地是H，C1-3烷基或卤素; X是O，S，SO，SO 2，N-R 5或C（R 5）2，其中每个R 5独立地是H，C 1-6烷基或任选被一个或多个杂原子中断的C 7-13芳烷基; n为0〜2的整数; m是0至3的整数; 条件是当X是CH 2时，R 1不是CH 3，R 2和R 3不同时为H，R 4不为OH，m不为3且n不为0.对于用于治疗包含那些化合物的疼痛和药学上可接受的组合物。 本发明化合物作为鸦片剂受体的激动剂。

    POLYCYCLIC ALCALOID-DERIVATIVES AS NMDA-RECEPTOR ANTAGONISTS
    10.
    发明申请
    POLYCYCLIC ALCALOID-DERIVATIVES AS NMDA-RECEPTOR ANTAGONISTS 审中-公开
    作为NMDA受体拮抗剂的多环类衍生物衍生物

    公开(公告)号：WO1997003979A1

    公开(公告)日：1997-02-06

    申请号：PCT/CA1996000468

    申请日：1996-07-12

    Applicant: BIOCHEM PHARMA INC. ,  DIMAIO, John ,  DIXIT, Dilip, M.

    Inventor： BIOCHEM PHARMA INC.

    IPC: C07D337/16

    CPC classification number: C07C215/44 ,  C07D225/08 ,  C07D313/20 ,  C07D337/16

    Abstract: 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.

    Abstract translation: 式（I）的多环生物碱，其中R 1为H，C 1-6烷基或任选被极性基团取代的C 6-12芳基; R2 abd R3独立地为H，OH，C1-6烷基，-C（NH）-NH2，带正电荷的基团或任选被NH 2，OH，C 1-6烷基或卤素取代的C 7-13芳烷基; 或R 2和R 3一起形成任选地加入杂原子的5至6元环; R4是H，C1-6烷基，OR6，SR6或N（R6）2，其中每个R6独立地是H，C1-3烷基; X是O，S，SO，SO 2，N-R 5或C（R 5）2，其中每个R 5独立地是H，C 1-6烷基或任选被一个或多个杂原子中断的C 7-13芳烷基; n为0〜2的整数; m是0至3的整数; 条件是当X是CH 2时，R 1不是CH 3，R 2和R 3不都是H，R 4不是OH，m不是3且n不是0。作为离子型NMDA（N-甲基 - （D）天冬氨酸）受体。

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