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    Novel carboxylate derivatives exhibiting phospholipase A2 inhibitory activity
    3.
    发明公开
    Novel carboxylate derivatives exhibiting phospholipase A2 inhibitory activity 失效
    磷脂酶A2 hemmendenAktivität。

    公开(公告)号：EP0646569A1

    公开(公告)日：1995-04-05

    申请号：EP94307136.5

    申请日：1994-09-29

    申请人： SHIONOGI & CO., LTD.

    发明人： Ohtani, Mitsuaki ,  Kato, Toshiyuki ,  Hori, Yozo

    IPC分类号： C07C69/92 ,  C07C323/19 ,  C07C317/22 ,  C07C65/01 ,  C07C217/22 ,  C07C311/17 ,  C07C233/18 ,  C07D209/48 ,  C07D275/06 ,  C07D211/70 ,  C07D295/084

    CPC分类号： C07D209/48 ,  C07C69/92 ,  C07C217/22 ,  C07C233/69 ,  C07C233/92 ,  C07C235/46 ,  C07C235/60 ,  C07C311/17 ,  C07C311/48 ,  C07C317/18 ,  C07C323/03 ,  C07D211/70 ,  C07D275/06 ,  C07D295/088

    摘要： Novel carboxylate derivatives exhibiting phospholipase A₂ inhibitory activity are disclosed. Specifically, the following compounds of the formula and pharmaceutically acceptable salts thereof are disclosed:

    wherein A is hydroxy, amino, or lower alkylamino; R¹ to R¹² are independently hydrogen, methyl, methoxy, or hydroxy, provided that all of R¹ to R¹² are not hydrogen; G¹ is a single bond, or a group of -(CH₂) x O(CH₂) y - wherein x and y are independently 0-5; G² is a single bond, oxygen, sulfur, carbonyl, etc.; G³ is alkyl, aryl, or a group of the formula:

    wherein R¹³ and R¹⁴ are independently hydrogen, alkyl, aryl, etc.; or R¹³ and R¹⁴ may be taken together with the adjacent nitrogen atom to form a heterocyclic group or a group of the formula:

    wherein Z is a carbon atom or a nitrogen atom,
       J, K ,and L are independently hydrogen or aryl, etc.; p and q are independently 0, 1, or 2; and n is an integer of 1 to 8.

    摘要翻译： 公开了显示磷脂酶A2抑制活性的新型羧酸衍生物。 具体地，公开了下列式及其药学上可接受的盐的化合物：其中A是羟基，氨基或低级烷基氨基; R 1至R 1独立地为氢，甲基，甲氧基或羟基，条件是R 1至R 12全部不为氢; G 1是单键或 - （CH 2）x O（CH 2）y - ，其中x和y独立地为0-5; G 2是单键，氧，硫，羰基等; G 3是烷基，芳基或下式的基团：其中R 1，3和R 4独立地是氢，烷基，芳基等; 或R 1'和R 1'可以与相邻的氮原子一起形成杂环基团或下式的基团：其中Z是碳原子或氮原子 ，J，K和L独立地为氢或芳基等; p和q独立地为0,1或2; n为1〜8的整数。

    Monoesters of arylacetic acid, their production and use
    4.
    发明公开
    Monoesters of arylacetic acid, their production and use 失效
    单烯酸单酯，其生产和使用

    公开(公告)号：EP0373931A3

    公开(公告)日：1991-05-15

    申请号：EP89313075.7

    申请日：1989-12-14

    申请人： SHIONOGI SEIYAKU KABUSHIKI KAISHA trading under the name of SHIONOGI & CO. LTD.

    发明人： Ohtani, Mitsuaki ,  Matsuura, Takaharu ,  Konoike, Toshiro ,  Araki, Yoshitaka

    IPC分类号： C07C69/753 ,  C07C67/08

    CPC分类号： C07C69/753 ,  Y02P20/55

    摘要： The invention provides optically active esters of arylacetic acid of the formula:
    wherein R¹ is hydrogen or optionally substituted C₁-C₂ alkyl or phenyl or when both taken together form C₂-C₆ alkylene, C₂ or C₄-C₆ alkenylene, or a bicyclic-ring; R² is hydrogen or methyl; X is a single bond or CH₂, C=O, N-R⁴, O, S, CHNHR⁴, CHCH₃, CH-Ar, or CHOR⁵ (provided that when X is single bond or CH₂, C=O, N-R⁴, O, or S, R¹ and R² are not simultaneously hydrogen or methyl); R³ is hydrogen, optionally substituted alkyl, or optionally substituted aralkyl; R⁴ is hydrogen or an amino protecting group; R⁵ is hydrogen or a hydroxy protecting group; and Ar is optionally substituted aryl. These esters may be prepared by the reaction of a σ symmetric acid anhydride with an (R)- or (S)-arylacetic acid derivative in high optical purity, and are useful as intermediates for various optically active natural products and medicines.

    Mono esters of dicarboxylic acids, their preparation and use
    7.
    发明公开
    Mono esters of dicarboxylic acids, their preparation and use 失效
    Monoester vonDicarbonsäuren，ihre Herstellung und Verwendung。

    公开(公告)号：EP0373949A1

    公开(公告)日：1990-06-20

    申请号：EP89313122.7

    申请日：1989-12-14

    申请人： SHIONOGI SEIYAKU KABUSHIKI KAISHA trading under the name of SHIONOGI & CO. LTD.

    发明人： Ohtani, Mitsuaki ,  Matsuura, Takaharu

    IPC分类号： C07C69/753 ,  C07D491/08 ,  C07C67/08

    CPC分类号： C07D493/08

    摘要： Optically active mono-esters of dicarboxylic acids of the formula III :
    wherein R¹ is optionally substituted alkyl, menthyl optionally substituted alkenyl, optionally substituted aralkyl; -X- is -0-, -S-, -0-0, -(CH₂)m-,
    in which m is an integer of from 0 to 4, R² is hydrogen, methyl, or ethyl, and R³ is hydrogen, methyl, benzyloxycarbonyl or formyl;
    -Y- is -(CH₂)n-,
    in which n is an integer of from 0 to 3, R² is the same as defined above, and R⁴ is hydrogen, methyl, or ethyl; and Z is hydrogen, lower alkyl, or phenyl; provided that m and n are not both zero, are useful as intermediates for preparing optically active natural products or medicines. The invention includes an asymmetric synthesis process for the preparation thereof characterised by the reaction of an acid anhydride with an (R)- or (S)-arylacetic acid derivative.

    摘要翻译： 式III的二羧酸的光学活性单酯：其中R 1是任选取代的烷基，任选被取代的烯基的任选取代的烯基，任选取代的芳烷基; -X-为-O - ， - S - ， - O - ， - （CH 2）m - ，，其中m为0-4的整数，R 2为氢，甲基或乙基 R 3为氢，甲基，苄氧羰基或甲酰基; -Y-是 - （CH2）n-，其中n是0-3的整数，R 2与上述定义相同，R 4是氢，甲基或乙基; Z是氢，低级烷基或苯基; 只要m和n不为零，可用作制备光学活性天然产物或药物的中间体。 本发明包括其制备方法的不对称合成方法，其特征在于酸酐与（R） - 或（S） - 芳基乙酸衍生物的反应。

    Epimerization of malonic acid esters
    8.
    发明公开
    Epimerization of malonic acid esters 失效
    丙二酸差向异构化。

    公开(公告)号：EP0098545A1

    公开(公告)日：1984-01-18

    申请号：EP83106437.3

    申请日：1983-07-01

    申请人： SHIONOGI & CO., LTD.

    发明人： Narisada, Masayuki ,  Onoue, Hiroshi ,  Ohtani, Mitsuaki ,  Watanabe, Fumihiko

    IPC分类号： C07D498/04

    CPC分类号： C07D505/00 ,  Y02P20/55

    摘要： A compound represented by the formula (II) epimerizes by the action of a base and the product is precipitated for shift-
    wherein Ar is an optionally substituted aryl or heterocyclic group; Tet is an optionally substituted tetrazolyl group and B 1 and B 2 each is ing the equilibrium to yield the corresponding epimer represented by the formula (I):
    an ester forming group in the field of penicillin or cephalosporin chemistry.