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    M-substituted benzoic acid derivatives having integrin alpha v beta 3 antagonistic activity
    3.
    发明申请
    M-substituted benzoic acid derivatives having integrin alpha v beta 3 antagonistic activity 审中-公开
    具有整合素αvβ3拮抗活性的M取代苯甲酸衍生物

    公开(公告)号：US20050059669A1

    公开(公告)日：2005-03-17

    申请号：US10944712

    申请日：2004-09-21

    申请人： Keiichi Ajito ,  Minoru Ishikawa ,  Dai Kubota ,  Shoichi Murakami ,  Mikio Yamamoto ,  Naokazu Yahata ,  Kazuyuki Fujishima ,  Makoto Oyama

    发明人： Keiichi Ajito ,  Minoru Ishikawa ,  Dai Kubota ,  Shoichi Murakami ,  Mikio Yamamoto ,  Naokazu Yahata ,  Kazuyuki Fujishima ,  Makoto Oyama

    IPC分类号： C07C229/54 ,  C07C229/60 ,  C07D239/14 ,  C07D239/42 ,  C07D401/12 ,  A61K31/496 ,  A61K31/454 ,  C07D43/02

    CPC分类号： C04B35/632 ,  C07C229/54 ,  C07C229/60 ,  C07D239/14 ,  C07D239/42 ,  C07D401/12

    摘要： An object of the present invention is to provide m-substituted benzoic acid derivatives having integrin αvβ3 antagonistic activity. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof, which are useful for the treatment or prevention of cardiovascular diseases, angiogenesis-related diseases, cerebrovascular diseases, cancers and metastasis thereof, immunological diseases, osteopathy and other diseases: wherein A represents an optionally substituted heterocyclic group containing two nitrogen atoms, a bicylic group or the like; D represents a bond, >NR4, >CR5R6, O, S, or —NR4—CR5R6—; X represents CH or N; R7 and R8 represent hydroxyl, alkyl or the like; Q represents >C═O or the like; R9 represents hydrogen, alkyl or the like; J represents a bond or alkylene; R10 represents optionally substituted hydroxyl, amino or the like; R11 represents hydrogen, alkyl or the like; m is 0 to 5; n is 0 to 4; and p and q are each 0 to 3.

    摘要翻译： 本发明的目的是提供具有整合素α噬菌体拮抗活性的m取代苯甲酸衍生物。 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，其可用于治疗或预防心血管疾病，血管生成相关疾病，脑血管疾病，癌症及其转移，免疫疾病 ，骨病和其他疾病：其中A表示任选取代的含有两个氮原子的杂环基团，二等基团等; D表示键，NR 4，CR 5 R 6，O，S或-NR 4 -CR 5 R 6 - 。 X表示CH或N; R 7和R 8代表羟基，烷基等; Q表示> C = O等; R 9表示氢，烷基等; J表示键或亚烷基; R 10表示任选取代的羟基，氨基等; R 11表示氢，烷基等; m为0〜5; n为0〜4; p和q各自为0〜3。

    &OHgr;-amino-&agr;-hydroxycarboxylic acid derivatives having integrin &agr;&ngr;&bgr;3 antagonistic activity
    4.
    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。

    Phenylpiperazine derivatives as integrin &agr;v&bgr;3 antagonists
    6.
    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。