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。