公开(公告)号：EP1382603A4

公开(公告)日：2004-12-29

申请号：EP02722791

申请日：2002-04-25

申请人： EISAI CO LTD

发明人： YOSHIDA ICHIRO ,  YONEDA NAOKI ,  OHASHI YOSHIAKI ,  SUZUKI SHUICHI ,  MIYAMOTO MITSUAKI ,  MIYAZAKI FUTOSHI ,  SESHIMO HIDENORI ,  KAMATA JUNICHI ,  TAKASE YASUTAKA ,  SHIRATO MANABU ,  SHIMOKUBO DAIYA ,  SAKUMA YOSHINORI ,  YOKOHAMA HIROMITSU

IPC分类号： A61K31/4155 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5415 ,  A61K31/551 ,  A61P1/04 ,  A61P3/04 ,  A61P11/00 ,  A61P17/00 ,  A61P31/04 ,  A61P31/12 ,  A61P31/18 ,  A61P33/00 ,  A61P35/00 ,  A61P35/02 ,  A61P37/02 ,  A61P37/08 ,  A61P43/00 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D493/04 ,  C07F5/02 ,  A61P29/00

CPC分类号： C07D401/04 ,  A61K31/4155 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5415 ,  A61K31/551 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D493/04 ,  C07F5/025 ,  Y02P20/55

摘要： A compound having excellent inhibitory activity against STAT 6. It is a compound represented by the following general formula (I), a salt thereof, or a hydrate of either. (I) In the formula, X represents a nitrogenous fused aromatic heterocyclic group, e.g., imidazo[1,2-a]pyridine, and has (R4)n as a substituent; Y represents C3-8 cycloalkyl, etc.; n in (Z)n is an integer of 0 to 3 and Z's each independently represents (1) hydrogen, (2) amino, etc.; R1 represents (1) hydrogen, (2) halogeno, etc.; R2 represents hydrogen or a protective group; and R3 represents hydrogen, halogeno, etc.

摘要翻译： 对STAT6具有优异抑制活性的化合物。它是由下列通式（I）表示的化合物，其盐或任一种的水合物。 （I）式中，X表示含氮稠合芳香族杂环基，例如咪唑并[1,2-a]吡啶，并且具有（R4）n作为取代基; Y代表C 3-8环烷基等; （Z）中的n为0〜3的整数，Z各自独立地表示（1）氢，（2）氨基等。 R1代表（1）氢，（2）卤代等; R2代表氢或保护基团; 和R3代表氢，卤代等

公开(公告)号：EP1101495A4

公开(公告)日：2003-05-07

申请号：EP00929921

申请日：2000-05-30

申请人： EISAI CO LTD

发明人： YAMAUCHI TOSHIHIKO ,  YOKOHAMA HIROMITSU ,  KOBAYASHI SEIICHI ,  SETO TOSHIO

IPC分类号： A61P7/04 ,  C07K16/28 ,  A61K45/00 ,  A61K39/395

CPC分类号： C07K16/2875 ,  A61K2039/505

摘要： Preventives for idiopathic thrombocytopenic purpura (ITP) which contain as the active ingredient a drug inhibiting the interaction between a receptor gp39 mediating the contact-dependent helper effector function on T cell surface and CD40 on antigen presenting cell surface.

公开(公告)号：EP1666606A4

公开(公告)日：2006-11-29

申请号：EP04772285

申请日：2004-08-20

申请人： LOCOMOGENE INC ,  EISAI CO LTD

发明人： NAKAJIMA TOSHIHIRO ,  AMANO TETSUYA ,  ZHANG LEI ,  IKEDA RIE ,  YAMASAKI SATOSHI ,  YAGISHITA NAOKO ,  YOKOHAMA HIROMITSU ,  KOGUSHI MOTOJI

IPC分类号： C12Q1/25 ,  A61K38/00 ,  A61K38/16 ,  A61P29/00 ,  C12Q1/26

CPC分类号： A61K38/16 ,  A61K38/005 ,  C12Q1/25 ,  C12Q1/26 ,  G01N2333/90245 ,  G01N2500/00

摘要： It is intended to provide a method for evaluating an effect of controlling the activity of proline 4-hydroxyolase; a screening method with the use of the above evaluation method; and a method of screening a compound which is useful in treating or preventing fibrosis or rheumatoid arthritis. A method for detecting an effect of controlling the ubiquitination activity of proline 4-hydroxyolase alpha subunit (P4HA1) by synoviolin; and a method of screening a substance having an effect of controlling the ubiquitination activity of P4HA1 of synoviolin based on the above method. A compound found out by this screening is useful in treating or preventing diseases caused by disorders in the activity of proline 4-hydroxylase such as fibrosis and rheumatoid arthritis.

公开(公告)号：EP1262194A4

公开(公告)日：2003-05-07

申请号：EP01908214

申请日：2001-03-01

申请人： EISAI CO LTD

发明人： YAMAUCHI TOSHIHIKO ,  YOKOHAMA HIROMITSU ,  KOBAYASHI SEIICHI ,  SETO TOSHIO

IPC分类号： A61P7/02 ,  A61P15/08 ,  A61P43/00 ,  C07K16/28 ,  A61K45/00 ,  A61K38/17 ,  A61K39/395

CPC分类号： C07K16/2875 ,  A61K2039/505

摘要： Remedies and preventives for antiphospholipid antibody syndrome (APS) containing, as the active ingredient, a drug inhibiting the interaction between a receptor gp39, which mediates contact-dependent helper effecter function on T cell surface, and CD40 on antigen presenting cell surface.