公开(公告)号：JPH09208466A

公开(公告)日：1997-08-12

申请号：JP2832596

申请日：1996-02-15

申请人： EISAI CO LTD

发明人： SUGUMI HIROYUKI ,  NIIJIMA ATSUSHI ,  KOTAKE YOSHIHIKO ,  OKADA TOSHIMI ,  KAMATA JUNICHI ,  YOSHIMATSU KENTARO ,  NAGASU TAKESHI ,  NAKAMURA KATSUJI ,  KAMINAKA TOSHIMITSU ,  IIJIMA ATSUYOSHI ,  YOSHINO HIROSHI ,  KOYANAGI NOZOMI ,  KITO KYOSUKE

IPC分类号： C07D487/06 ,  A61K31/505 ,  A61K31/535 ,  A61K31/54 ,  A61P35/00 ,  C07D471/06 ,  C07D471/16 ,  C07D491/16 ,  C07D495/14 ,  C07D498/06 ,  C07D513/06

摘要： PROBLEM TO BE SOLVED: To obtain the subject new compound having excellent antitumor activity with low toxicity and useful as an antitumor agent. SOLUTION: This condensed polycyclic heterocycle derivative is a compound expressed by formula I or its pharmacologically allowable salt [cycle A is a monocyclic aromatic ring or a dicyclic condensed ring having aromatic ring in at least one cycle; cycle B is pyrrole or 4H-1,4-oxazine, etc.; cycle C is a monocyclic or condensed dicyclic aromatic ring; Y is a group of formula -(e)-(f) ((e) is a lower alkylene; (f) is amidino or guanidino, etc.; excepting a case that both of the cycles A and C are each a monocyclic aromatic ring] and e.g. 5-[2-(dimethylamino)ethyl]-4H-benzo[C]pyrimido[5,6,1-(jk)]carbazole-4, 6(5H)-dione is exemplified. The compound of the formula I is obtained by reacting a compound of formula II (cycle Aa and cycle Ca are each protectable cycle A or cycle C; cycle Ba is pyrrole, etc.; (fa) is a protectable (f)) with a compound of formula III (D and E are each a leaving group).

公开(公告)号：JPH09194481A

公开(公告)日：1997-07-29

申请号：JP275696

申请日：1996-01-11

申请人： EISAI CO LTD

发明人： SUGUMI HIROYUKI ,  NIIJIMA ATSUSHI ,  KOTAKE YOSHIHIKO ,  OKADA TOSHIMI ,  KAMATA JUNICHI ,  YOSHIMATSU KENTARO ,  NAGASU TAKESHI ,  NAKAMURA KATSUJI ,  KAMINAKA TOSHIMITSU ,  IIJIMA ATSUYOSHI ,  YOSHINO HIROSHI ,  KOYANAGI NOZOMI ,  KITO KYOSUKE

IPC分类号： C07D487/04 ,  A61K31/505 ,  A61K31/535 ,  A61K31/54 ,  A61K31/55 ,  A61P35/00 ,  C07D498/04 ,  C07D498/14 ,  C07D513/04

摘要： PROBLEM TO BE SOLVED: To obtain the subject new compound derivative which is a specific condensed tetra- and heterocyclic derivative, having a cyclic imide part in the molecule, excellent antitumor activities and low toxicity and useful as an active ingredient, etc., of an antitumor agent. SOLUTION: This new tetra- and heterocyclic derivative (salt) is represented by formula I rings A and B are each a (substituted)monocyclic aromatic ring; X is a bond, O, S or CH=CH; Y is a group represented by the formula e-f [(e) is a lower alkylene; (f) is an amino group which may be substituted with a lower alkyl group]}, has excellent antitumor activities and low toxicity and is useful as an active ingredient, etc., of an antitumor agent. The compound is obtained by reacting a compound represented by formula II [ring Aa is a (protected)ring A; G is O or S] with a compound represented by formula III [ring Ba is a (protected)ring B; K and L are each an eliminable group; R is a lower alkyl], then amidating the resultant compound, providing a condensed tricyclic compound represented by formula IV and further carrying out the cyclizing reaction of the resultant condensed tricyclic compound represented by formula IV with a compound represented by formula V (D and E are each an eliminable group).

公开(公告)号：JP2002053491A

公开(公告)日：2002-02-19

申请号：JP2000240791

申请日：2000-08-09

申请人： EISAI CO LTD

发明人： KAMINAKA TOSHIMITSU ,  IWATA MASAO ,  NAKAMURA KATSUJI ,  ARAI TORU

IPC分类号： G01N33/50 ,  A61K38/00 ,  A61K45/00 ,  A61K48/00 ,  A61P35/00 ,  C12N15/09 ,  C12Q1/06 ,  G01N33/15 ,  G01N33/566 ,  G01N33/68

摘要： PROBLEM TO BE SOLVED: To construct a foundation of development of a new medicine by inhibiting an interaction between SH3 domain and its ligand. SOLUTION: An inhibition of an interaction between SH3 domain and its ligand bonded in high affinity by transducing a vector to express an eugenic negative mutant of c-Src SH3 domain to a cell and using a peptide to inhibit the interaction is shown to exhibit a foundation of development of a new medicine.