公开(公告)号：EP1727782A1

公开(公告)日：2006-12-06

申请号：EP05727512.5

申请日：2005-03-25

申请人： OTSUKA PHARMACEUTICAL CO., LTD.

发明人： KIYOKAWA, Hiroshi ,  AKI, Shinji

IPC分类号： C07C213/02 ,  C07D295/08 ,  C07D211/46 ,  C07C215/82 ,  C07C215/76

CPC分类号： C07D295/096 ,  C07C213/02 ,  C07C215/76 ,  C07C215/82

摘要： The present invention provides an industrially advantageous method of producing aminophenol compounds represented by the formula (1) by a simple and easy procedure at a high yield and a high purity. The present invention provides a method of producing an aminophenol compound represented by the formula (1): (wherein each of R1 and R2, which may be the same or different, is a hydrogen atom, a substituted or unsubstituted lower alkyl group or the like; R1 and R2, taken together with the adjacent nitrogen atom, may form a 5- or 6-membered heterocycle with or without other intervening heteroatoms; the heterocycle may be substituted by 1 to 3 substituents selected from the group consisting of a hydroxyl group, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aryloxy group and the like; and the hydroxyl group in the formula (1) is substituted on the 2- or 4-position to the amino group on the phenyl ring), which comprises allowing a cyclohexanedione compound represented by the formula (2) to react with an amine compound represented by the formula (3) (wherein R1 and R2 are as defined above), under a neutral or basic condition.

公开(公告)号：EP1727782B1

公开(公告)日：2012-08-22

申请号：EP05727512.5

申请日：2005-03-25

申请人： OTSUKA PHARMACEUTICAL CO., LTD.

发明人： KIYOKAWA, Hiroshi ,  AKI, Shinji

IPC分类号： C07C213/02 ,  C07D295/08 ,  C07D211/46 ,  C07C215/82 ,  C07C215/76

CPC分类号： C07D295/096 ,  C07C213/02 ,  C07C215/76 ,  C07C215/82

摘要： The present invention provides an industrially advantageous method of producing aminophenol compounds represented by the formula (1) by a simple and easy procedure at a high yield and a high purity. The present invention provides a method of producing an aminophenol compound represented by the formula (1): (wherein each of R1 and R2, which may be the same or different, is a hydrogen atom, a substituted or unsubstituted lower alkyl group or the like; R1 and R2, taken together with the adjacent nitrogen atom, may form a 5- or 6-membered heterocycle with or without other intervening heteroatoms; the heterocycle may be substituted by 1 to 3 substituents selected from the group consisting of a hydroxyl group, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aryloxy group and the like; and the hydroxyl group in the formula (1) is substituted on the 2- or 4-position to the amino group on the phenyl ring), which comprises allowing a cyclohexanedione compound represented by the formula (2) to react with an amine compound represented by the formula (3) (wherein R1 and R2 are as defined above), under a neutral or basic condition.

公开(公告)号：EP0503099A1

公开(公告)日：1992-09-16

申请号：EP91917341.9

申请日：1991-10-07

申请人： OTSUKA PHARMACEUTICAL CO., LTD.

发明人： KIYOKAWA, Hiroshi ,  YAMADA, Satoshi ,  MIYAJIMA, Keisuke ,  HASHIMOTO, Kinji ,  INAI, Masatoshi ,  INOUE, Makoto ,  TATSUMI, Kunihiko ,  YAMAUCHI, Takeshi ,  KURISU, Kazunobu ,  CHONE, Yoshifumi

IPC分类号： C07D487/04 ,  A61K31/505 ,  A61K31/53

CPC分类号： C07D487/04

摘要： A pyrimidine derivative represented by general formula (I), a pharmaceutically acceptable salt thereof, and an androgen inhibitor comprising the same having an excellent effect of treating prostatic hyperplasia, female hypertrichosis, and male baldness or pimple: wherein R¹ represents hydrogen or hydroxyl; R² represents hydrogen, lower alkoxycarbonyl, lower alkoxy, halogen, lower alkyl, C₃ to C₈ cycloalkyl, lower alkoxycarbonyl lower alkyl, carboxyl, carboxylated lower alkyl, CONHR, cyano, phenyl, phenylated lower alkyl, lower alkanoyloxy lower alkyl, benzoyl, lower alkanoyl or hydroxylated lower alkyl; R³ represents hydrogen, hydroxy, lower alkyl, C₃ to C₈ cycloalkyl, halogenated lower alkyl or phenyl; R⁴ represents hydrogen, lower alkyl or lower alkoxy, R⁵ represents hydrogen, lower alkyl, lower alkoxy lower alkyl or halogenated lower alkyl.

摘要翻译： 由通式（I）表示的嘧啶衍生物，其药学上可接受的盐和包含其的雄激素抑制剂具有优异的治疗前列腺增生，女性肥大症和男性秃发或疙瘩的效果：其中R 1表示氢或 羟; R 2表示氢，低级烷氧基羰基，低级烷氧基，卤素，低级烷基，C3至C8环烷基，低级烷氧基羰基低级烷基，羧基，羧基低级烷基，CONHR，氰基，苯基，苯基低级烷基，低级烷酰氧基低级烷基，苯甲酰基 ，低级烷酰基或羟基化低级烷基; R 3表示氢，羟基，低级烷基，C 3至C 8环烷基，卤代低级烷基或苯基; R 4表示氢，低级烷基或低级烷氧基，R 5表示氢，低级烷基，低级烷氧基低级烷基或卤代低级烷基。