公开(公告)号：EP1439175A4

公开(公告)日：2004-12-29

申请号：EP02802050

申请日：2002-10-22

申请人： EISAI CO LTD

发明人： HARADA HITOSHI ,  ASANO OSAMU ,  UEDA MASATO ,  MIYAZAWA SHUHEI ,  KOTAKE YOSHIHIKO ,  KABASAWA YASUHIRO ,  YASUDA MASAHIRO ,  YASUDA NOBUYUKI ,  IIDA DAISUKE ,  NAGAKAWA JUNICHI ,  HIROTA KAZUO ,  NAKAGAWA MAKOTO

IPC分类号： A61K31/506 ,  A61P1/00 ,  A61P1/10 ,  A61P3/04 ,  A61P3/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/02 ,  A61P19/10 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D401/04 ,  C07D405/14 ,  C07D409/14

CPC分类号： C07D405/14 ,  A61K31/506 ,  C07D401/04 ,  C07D409/14

摘要： A novel pyrimidine compound having an excellent antagonistic activity against adenosine receptors (A1, A2A, and A2B receptors). Specifically, it is a compound represented by the following formula, a salt of the compound, or a solvate of either. (I) In the formula, R1 and R2 are the same or different and each represents hydrogen, optionally substituted C1-6 alkyl, etc.; R3 represents hydrogen, halogeno, etc.; R4 represents an optionally substituted C6-14 aromatic hydrocarbon ring group, optionally substituted 5- to 14-membered nonaromatic heterocyclic group having at least one unsaturated bond, etc.; and R5 represents an optionally substituted C6-14 aromatic hydrocarbon ring group or optionally substituted 5- to 14-membered aromatic heterocyclic group.

摘要翻译： 对腺苷受体（A1，A2A和A2B受体）具有优异拮抗活性的新型嘧啶化合物。 具体地说，它是由下式表示的化合物，该化合物的盐或任一种的溶剂化物。 （I）式中，R 1和R 2相同或不同，表示氢原子，可以具有取代基的C 1-6烷基等。 R3代表氢，卤代等; R4表示任选取代的C6-14芳族烃环基团，具有至少一个不饱和键的任选取代的5-14元非芳族杂环基团等; 并且R 5表示任选取代的C 6-14芳族烃环基团或任选取代的5至14元芳族杂环基团。

公开(公告)号：EP0790228A4

公开(公告)日：1998-07-08

申请号：EP95935597

申请日：1995-10-31

申请人： EISAI CO LTD

发明人： HIBI SHIGEKI ,  KIKUCHI KOUICHI ,  YOSHIMURA HIROYUKI ,  NAGAI MITSUO ,  TAGAMI KATSUYA ,  ABE SHINYA ,  HISHINUMA IEHARU ,  NAGAKAWA JUNICHI ,  MIYAMOTO NORIMASA ,  HIDA TAKAYUKI ,  OGASAWARA AICHI ,  HIGASHI SEIKO ,  TAI KENJI ,  YAMANAKA TAKASHI ,  ASADA MAKOTO

IPC分类号： A61P19/02 ,  C07C57/03 ,  C07C229/44 ,  C07D209/08 ,  C07D213/69 ,  C07D215/12 ,  C07D215/14 ,  C07D215/18 ,  C07D223/16 ,  C07D225/06 ,  C07D231/12 ,  C07D241/38 ,  C07D241/42 ,  C07D241/46 ,  C07D261/18 ,  C07D263/32 ,  C07D265/36 ,  C07D333/76 ,  C07D405/14 ,  C07D455/04 ,  C07D487/04 ,  C07D495/04 ,  G06F17/30 ,  C07C53/00 ,  C07C229/00 ,  C07D471/06 ,  C07D521/00

CPC分类号： C07D213/69 ,  C07C57/03 ,  C07C229/44 ,  C07D209/08 ,  C07D215/12 ,  C07D215/14 ,  C07D215/18 ,  C07D223/16 ,  C07D225/06 ,  C07D231/12 ,  C07D233/16 ,  C07D241/38 ,  C07D241/42 ,  C07D241/46 ,  C07D261/18 ,  C07D263/32 ,  C07D265/36 ,  C07D333/76 ,  C07D405/14 ,  C07D455/04 ,  C07D487/04 ,  C07D495/04 ,  G06F17/30607 ,  Y02P20/55

摘要： Novel retinoid-related compounds that can substitute for retinoic acid as preventives or remedies for various diseases and compounds that are antagonistic to retinoids, i.e., heterocyclic compounds represented by the general formula (1-I): Z-(CR3=CR2)n-COOR1 or physiologically acceptable salts thereof, and compounds represented by general formula (2-I) or physiologically acceptable salts thereof. The compounds have a potent ability to combine with RARs and are efficacious in treating various diseases including various keratinization anomalies and rheumatoid arthritis.