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    • 8. 发明授权
    • &OHgr;-amino-&agr;-hydroxycarboxylic acid derivatives having integrin &agr;&ngr;&bgr;3 antagonistic activity
    • 具有整合素α2β3拮抗活性的ω-氨基-α-羟基羧酸衍生物
    • US06750219B1
    • 2004-06-15
    • US10048914
    • 2002-02-05
    • Keiichi AjitoNaokazu YahataMinoru IshikawaDai KubotaShoichi MurakamiMikio YamamotoKazuyuki FujishimaShuichi GomiShokichi Ouchi
    • Keiichi AjitoNaokazu YahataMinoru IshikawaDai KubotaShoichi MurakamiMikio YamamotoKazuyuki FujishimaShuichi GomiShokichi Ouchi
    • C07D40304
    • C07D239/42
    • 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.
    • 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。