利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

18 条记录 (耗时 0.039 秒)

    16-membered macrolide derivatives and process for producing the same
    3.
    发明授权
    16-membered macrolide derivatives and process for producing the same 失效
    16元大环内酯衍生物及其制备方法

    公开(公告)号：US5407918A

    公开(公告)日：1995-04-18

    申请号：US143125

    申请日：1993-10-29

    申请人： Keiichi Ajito ,  Ken-ichi Kurihara ,  Akira Shimizu ,  Shuichi Gomi ,  Nobue Kikuchi ,  Minako Araake ,  Tsuneo Ishizuka ,  Aiko Miyata ,  Osamu Hara ,  Seiji Shibahara

    发明人： Keiichi Ajito ,  Ken-ichi Kurihara ,  Akira Shimizu ,  Shuichi Gomi ,  Nobue Kikuchi ,  Minako Araake ,  Tsuneo Ishizuka ,  Aiko Miyata ,  Osamu Hara ,  Seiji Shibahara

    IPC分类号： C07H17/08 ,  C12P19/62 ,  A61K31/70 ,  C12P19/60

    CPC分类号： C07H17/08

    摘要： 16-membered macrolide derivatives represented by the formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or a COR.sup.6 group, wherein R.sup.6 represents a straight-chain alkyl group having 1 to 3 carbon atoms; R.sup.2 represents a hydrogen atom or a COR.sup.6 group, wherein R.sup.6 is as defined above; R.sup.3 represents a hydrogen atom or a COR.sup.6 group, wherein R.sup.6 is as defined above; R.sup.4 represents a straight-chain alkyl group having 1 to 4 carbon atoms or a substituted or unsubstituted allyl group; and R.sup.5 represents a substituted or unsubstituted, straight-chain or branched alkyl, alkenyl or aralkyl group having 1 to 10 carbon atoms; and pharmaceutically acceptable salts thereof are disclosed. These compounds show excellent and long-acting antimicrobial activities. A novel process for producing these 16-membered macrolide derivatives is further disclosed.

    摘要翻译： 由式（I）表示的16元大环内酯衍生物：其中R 1表示氢原子或COR 6基团，其中R 6表示具有1至3个碳原子的直链烷基; R2表示氢原子或COR6基团，其中R6如上所定义; R3表示氢原子或COR6基团，其中R6如上所定义; R4表示碳原子数1〜4的直链烷基或取代或未取代的烯丙基; R 5表示具有1〜10个碳原子的取代或未取代的直链或支链烷基，烯基或芳烷基; 及其药学上可接受的盐。 这些化合物显示出优异的长效抗菌活性。 进一步公开了一种制备这些16元大环内酯衍生物的新方法。

    Phenylpiperazine derivatives as integrin &agr;v&bgr;3 antagonists
    5.
    发明授权
    Phenylpiperazine derivatives as integrin &agr;v&bgr;3 antagonists 失效
    苯基哌嗪衍生物作为整合素α2β拮抗剂

    公开(公告)号：US06451800B1

    公开(公告)日：2002-09-17

    申请号：US09601176

    申请日：2000-07-28

    申请人： Keiichi Ajito ,  Shoichi Murakami ,  Minoru Ishikawa ,  Mikio Yamamoto ,  Dai Kubota ,  Shuichi Gomi ,  Mitsugu Hachisu ,  Kiyoaki Katano

    发明人： Keiichi Ajito ,  Shoichi Murakami ,  Minoru Ishikawa ,  Mikio Yamamoto ,  Dai Kubota ,  Shuichi Gomi ,  Mitsugu Hachisu ,  Kiyoaki Katano

    IPC分类号： A61K31497

    CPC分类号： C07D239/42 ,  C07D235/30 ,  C07D239/14

    摘要： An objective of the present invention is to provide compounds having integrin &agr;v&bgr;3 antagonistic activity, GP IIb/IIIa antagonistic activity, and/or human platelet aggregation inhibitory activity, and therapeutic agents for treating integrin &agr;v&bgr;3-mediated diseases and for inhibiting platelet aggregation. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein A represents a five- to seven-membered heterocyclic ring containing two nitrogen atoms or the like; X and Z represent CH or a nitrogen atom; R4 and R5 represent alkyl, halogen or the like; Q represents >C=O, >CH2 or the like; R6 represents H, alkyl, aralkyl or the like; R7 represents H, alkynyl or the like; R8 represents H, substituted amino or the like; R9 represents H or alkyl; m is 0 to 5; n is 0 to 4; p is 2 or 3; and q is 0 or 1.

    摘要翻译： 本发明的目的是提供具有整合素α2拮抗活性，GP IIb / IIIa拮抗活性和/或人血小板聚集抑制活性的化合物，以及用于治疗整合素α1β介导的疾病和抑制血小板聚集的治疗剂。 根据本发明的衍生物是由式（I）表示的化合物或其药学上可接受的盐或溶剂化物：其中A表示含有两个氮原子等的5-至7-元杂环; X和Z表示CH或氮原子; R4和R5代表烷基，卤素等; Q表示> C = O，> CH2等; R6表示H，烷基，芳烷基等; R 7表示H，炔基等; R8表示H，取代的氨基等; R9代表H或烷基; m为0〜5; n为0〜4; p为2或3; q为0或1。

    &OHgr;-amino-&agr;-hydroxycarboxylic acid derivatives having integrin &agr;&ngr;&bgr;3 antagonistic activity
    6.
    发明授权
    &OHgr;-amino-&agr;-hydroxycarboxylic acid derivatives having integrin &agr;&ngr;&bgr;3 antagonistic activity 失效
    具有整合素α2β3拮抗活性的ω-氨基-α-羟基羧酸衍生物

    公开(公告)号：US06750219B1

    公开(公告)日：2004-06-15

    申请号：US10048914

    申请日：2002-02-05

    申请人： Keiichi Ajito ,  Naokazu Yahata ,  Minoru Ishikawa ,  Dai Kubota ,  Shoichi Murakami ,  Mikio Yamamoto ,  Kazuyuki Fujishima ,  Shuichi Gomi ,  Shokichi Ouchi

    发明人： Keiichi Ajito ,  Naokazu Yahata ,  Minoru Ishikawa ,  Dai Kubota ,  Shoichi Murakami ,  Mikio Yamamoto ,  Kazuyuki Fujishima ,  Shuichi Gomi ,  Shokichi Ouchi

    IPC分类号： C07D40304

    CPC分类号： C07D239/42

    摘要： An objective of the present invention is to provide highly water-soluble compounds having integrin &agr;v&bgr;3 antagonistic activity. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts or solvates thereof: wherein A represents a two nitrogen atom-containing optionally substituted saturated or unsaturated five- to seven-membered heterocyclic group, which is optionally condensed with another carbocyclic ring or heterocyclic ring to form a bicyclic group, or —C(—NR1R2)(═NR3) wherein R1, R2, and R3 represent hydrogen, alkyl or the like; D represents a bond, >NR4, wherein R4 represents hydrogen or optionally substituted alkyl, —O—, or —S—; X and Z represent either CH or N; R7 and R8 represent C1-6 alkyl, halogen, oxygen or the like; Q represents >C═O, >CHR13 or >CHOR13 wherein R13 represents hydrogen or alkyl; R9 represents hydrogen, alkyl or the like; J represents a bond or alkylene having 1 to 3 carbon atoms; R10 and R11 represent hydrogen, alkyl or the like; m is an integer of 0 to 5; n is an integer of 0 to 4; and p and q are an integer of 1 to 3.

    摘要翻译： 本发明的目的是提供具有整合素α2拮抗活性的高水溶性化合物。 根据本发明的化合物是由式（I）表示的化合物及其药学上可接受的盐或溶剂化物：其中A表示两个含有氮原子的任选取代的饱和或不饱和的五至七元杂环基，其任选地稠合 与另一个碳环或杂环形成双环基团，或-C（-NR 1 R 2）（= NR 3）（其中R 1，R 2和R 3） 代表氢，烷基等; D表示键，NR 4，其中R 4表示氢或任选取代的烷基，-O-或-S-; X和Z表示CH或N; R 7和R 8表示C 1-6烷基，卤素，氧等; Q表示C = O，> CHR 13或CHOR 13，其中R 13表示氢或烷基; R 9表示氢，烷基等; J表示碳原子数1〜3的键或亚烷基。 R 10和R 11代表氢，烷基等; m为0〜5的整数。 n为0〜4的整数。 p和q为1〜3的整数。