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    Xanthine derivatives
    2.
    发明公开
    Xanthine derivatives 失效
    叶黄素衍。

    公开(公告)号：EP0619316A1

    公开(公告)日：1994-10-12

    申请号：EP94105380.3

    申请日：1994-04-07

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： Shimada, Junichi ,  Kuwabara, Takashi ,  Yasuzawa, Tohru ,  Magara, Hiroshi ,  Nonaka, Hiromi ,  Kusaka, Hideaki ,  Suzuki, Fumio

    IPC分类号： C07D473/04 ,  A61K31/52

    CPC分类号： C07D473/04 ,  Y10S514/869

    摘要： There is provided a novel xanthine Compound(I)

    wherein R¹ and R² are the same or different and each represent hydroxy-substituted, oxo-substituted or unsubstituted lower alkyl, Y is a single bond or alkylene, and Q is

    wherein R³ and R⁴ are the same or different and each represent hydrogen or hydroxy, n is 0 or 1; provided that when both of R³ and R⁴ are hydrogen, at least one of R¹ and R² is hydroxy-substituted or oxo-substituted lower alkyl; or a pharmaceutically acceptable salt thereof.
    The xanthine compound has adenosine A₁ receptor antagonizing activity, and thus shows diuretic effect, renal-protecting effect, bronchodilatory effect, cerebral function improving effect and anti-dementia effect.

    摘要翻译： 提供了一种新颖的黄嘌呤化合物（I）其中R 1和R 2相同或不同，各自表示羟基取代的，取代或未取代的低级烷基，Y是单键或亚烷基 且Q为，其中R 3和R 4相同或不同，各自表示氢或羟基，n为0或1; 条件是当R 3和R 4都是氢时，R 1和R 2中的至少一个是羟基取代的或氧代取代的低级烷基; 或其药学上可接受的盐。 黄嘌呤化合物具有腺苷A1受体拮抗活性，因此具有利尿作用，肾保护作用，支气管扩张作用，脑功能改善作用和抗痴呆作用。

    Xanthine compounds
    3.
    发明公开
    Xanthine compounds 失效
    XANTHINE化合物

    公开(公告)号：EP0501379A3

    公开(公告)日：1992-12-09

    申请号：EP92103067.2

    申请日：1992-02-24

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： Suzuki, Fumio ,  Shimada, Junichi

    IPC分类号： C07D473/06 ,  A61K31/52

    CPC分类号： C07D473/06

    摘要： Novel xanthine compounds represented by the following formula:

    wherein each of R 1 and R 2 independently represents allyl or propargyl; R 3 represents hydrogen or lower alkyl; each of X 1 and X 2 independently represents oxygen or sulfur; Y represents a single bond or alkylene, and n represents 0 or 1; and pharmaceutically acceptable salts thereof have a diuretic effect and a renal-protecting effect.

    Xanthine compounds
    5.
    发明公开
    Xanthine compounds 失效
    Xanthinverbindungen。

    公开(公告)号：EP0501379A2

    公开(公告)日：1992-09-02

    申请号：EP92103067.2

    申请日：1992-02-24

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： Suzuki, Fumio ,  Shimada, Junichi

    IPC分类号： C07D473/06 ,  A61K31/52

    CPC分类号： C07D473/06

    摘要： Novel xanthine compounds represented by the following formula:

    wherein each of R 1 and R 2 independently represents allyl or propargyl; R 3 represents hydrogen or lower alkyl; each of X 1 and X 2 independently represents oxygen or sulfur; Y represents a single bond or alkylene, and n represents 0 or 1; and pharmaceutically acceptable salts thereof have a diuretic effect and a renal-protecting effect.

    摘要翻译： 由下式表示的新型黄嘌呤化合物：其中R 1和R 2各自独立地表示烯丙基或炔丙基; R 3表示氢或低级烷基; X 1和X 2各自独立地表示氧或硫; Y表示单键或亚烷基，n表示0或1; 及其药学上可接受的盐具有利尿作用和肾脏保护作用。

    Xanthine derivatives
    7.
    发明公开
    Xanthine derivatives 失效
    黄嘌呤衍生物

    公开(公告)号：EP0556778A3

    公开(公告)日：1993-11-24

    申请号：EP93102412.9

    申请日：1993-02-16

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： Suzuki, Fumio ,  Shimada, Junichi ,  Ishii, Akio ,  Shiozaki, Shizuo

    IPC分类号： C07D473/04 ,  A61K31/52

    CPC分类号： C07D473/04

    摘要： A xanthine derivative of the formula (I):

    wherein R 1 represents substituted or unsubstituted lower alkyl, lower alkenyl, lower alkynyl, substituted or unsubstituted alicyclic alkyl, substituted or unsubstituted phenyl, or substituted or unsubstituted benzyl;
    R 2 represents -(CH2)m-X, wherein m is 2 or 3, and X is

    wherein a is NH, O or S, b and d are the same or different and are CH or N, and R 3 is lower alkyl, substituted or unsubstituted alicyclic alkyl, or substituted or unsubstituted phenyl, or wherein e, g and h are the same or different and are CH or N, and R 3 is the same as defined above; Q represents substituted or unsubstituted alicyclic alkyl,
    wherein R 4 and R 5 are the same or different and are substituted or unsubstituted alicyclic alkyl,
    wherein Y is single bond or alkylene; and n is 0 or 1,
    wherein K-M is -CH 2 -CH 2 - or -CH = CH-, and Y is the same as defined above, or
    wherein Y is the same as defined above; or a pharmacologically acceptable salt thereof is disclosed. This derivative has anti-dementia activity.

    摘要翻译： 式（I）的黄嘌呤衍生物：其中R1代表取代或未取代的低级烷基，低级链烯基，低级炔基，取代或未取代的脂环族烷基，取代或未取代的苯基或取代或未取代的苄基; R2表示 - （CH2）mX，其中m为2或3，X为其中a为NH，O或S，b和d相同或不同，为CH或N，R3为低级烷基，取代或未取代的 脂环族的烷基或取代或未取代的苯基，或者e，g和h相同或不同，为CH或N，R3与上述定义相同; Q表示取代或未取代的脂环族烷基，其中R4和R5相同或不同并且是取代或未取代的脂环族烷基，其中Y是单键或亚烷基; 并且n是0或1，其中K-M是-CH 2 -CH 2 - 或-CH = CH-，并且Y与以上定义的相同，或者其中Y与以上定义的相同; 或其药理学上可接受的盐。 该衍生物具有抗痴呆活性。

    Therapeutic agents for use in the treatment of parkinson's disease
    8.
    发明公开
    Therapeutic agents for use in the treatment of parkinson's disease 失效
    Arzneimittel zur Verwendung bei der Behandlung von Parkinsonismus。

    公开(公告)号：EP0565377A1

    公开(公告)日：1993-10-13

    申请号：EP93302780.7

    申请日：1993-04-08

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： Suzuki, Fumio ,  Shimada, Junichi ,  Ishii, Akio ,  Ichikawa, Shunji

    IPC分类号： A61K31/52 ,  C07D473/06

    CPC分类号： C07D473/12 ,  A61K31/52 ,  C07D473/06 ,  C07D473/08

    摘要： Disclosed are therapeutic agents for use in the treatment of Parkinson's disease, such agents being xanthine derivatives of the Formula (I) and their pharmaceutical acceptable salts :

    where R 1 , R 2 and R 3 are each H, C 1 -C 6 alkyl or allyl ; and R 4 is cycloalkyl of 3 to 8 carbon atoms, a -(CH 2 ) n -R 5 group where n is an cycloalkyl of 3 to 8 carbon atoms, a - (CH 2 ) n -R 5 group where n is an integer of from 0-4 and R 5 is an aryl group of 6 to 10 carbon atoms or a heterocyclic group, such aryl or heterocyclic group optionally being substituted by up to 3 substituent(s) selected from C 1 -C 6 alkyl, hydroxy, C 1 -C 6 alkoxy, halogen, nitro and amino ; or
    a

    group, where Y 1 and Y 2 are each H or CH 3 and Z is a substituted or unsubstituted aryl or heterocyclic group as defined under R 5 .

    摘要翻译： 本发明公开了用于治疗帕金森病的治疗剂，所述药剂为式（I）的黄嘌呤衍生物及其药学上可接受的盐：其中R 1，R 2和R 3各自为 H，C 1 -C 6烷基或烯丙基; 且R 4为3-8个碳原子的环烷基， - （CH 2）n R 5基团，其中n为3至8个碳原子的环烷基，其中n为 0-4的整数和R 5为6至10个碳原子的芳基或杂环基，任选被至多3个选自C 1 -C 6烷基，羟基的取代基取代的芳基或杂环基 ，C 1 -C 6烷氧基，卤素，硝基和氨基; 或基团，其中Y 1和Y 2各自为H或CH 3，Z为取代或未取代的R 5所定义的芳基或杂环基。

    3-Substituted carbacephem and cephem compounds and pharmaceutical compositions
    10.
    发明公开
    3-Substituted carbacephem and cephem compounds and pharmaceutical compositions 失效
    3-取代Carbacephem-和头孢烯化合物及其药物组合物。

    公开(公告)号：EP0182301A2

    公开(公告)日：1986-05-28

    申请号：EP85114501.1

    申请日：1985-11-14

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： Mochida, Kenichi ,  Ogasa, Takehiro ,  Shimada, Junichi ,  Hirata, Tadashi ,  Sato, Kiyoshi ,  Okachi, Ryo

    IPC分类号： C07D501/59 ,  C07D471/04 ,  A61K31/545

    CPC分类号： C07D463/22 ,  Y02P20/55

    摘要： Carbacephem and cephem compounds represented by the formula:


    [Wherein X is S or CH 2 ; n is an integer of 1 to 5; R 1 is an unsubstituted or substituted heterocyclic group (where the heterocyclic group is a 5- or 6-membered heterocyclic group having 1 to 4 of O, S and N); R 2 is a group represented by the formula:
    (where R 4 is an unsubstituted or substituted phenyl or 2-amino- thiazolyl) or a group represented by the formula:

    (where R 5 is an unsubstituted or substituted lower alkyl); R 3 is hydrogen, an alkali metal, an alkaline earth metal, an organic ammonium group or an ester residue, and R 1 may be a quaternary ammonium group, where -CO 2 R 3 represents -CO 2 ] have strong antibacterial activity against Gram-positive and Gram-negative bacteria, and are useful for treating various infections.