Title:
チューブライシン、その製造方法、及び、チューブライシン製剤
Document Type and Number:
Japanese Patent JP4620467
Kind Code:
B2
Abstract:
New tubulysin compounds (I) comprise functionally modified derivatives of known tubulysins, i.e. the peptidic thiazole compounds tubulysin A to tubulysin F described in J. Antibiot., 2000, 53, 579-558and . Tubulysin compounds of formula (I) are new. [Image] R : H, alkyl, aryl, OR 1>, NR 1>R 2>or -NH-(CH 2) n-maleimido; n : 2-4; R 1>, R 2>H, alkyl or aryl; U, U' : H, halo, NO 2or NHR 3>; R 3>H, CHO or alkylcarbonyl; T : H or OR 4>; R 4>H, alkyl, aryl, COR 5>, P(O)(OR 6>) 2or SO 3R 6>; R 5>= alkyl, alkenyl, aryl or heteroaryl; R 6>H, alkyl or metal ion; V : H, OR 7>or halo; W : H or alkyl; or V + W : O; R 7>H, alkyl or COR 8>; R 8>alkyl, alkenyl or aryl; X : H, alkyl, alkenyl or CH 2OR 9>; R 9>H, alkyl, alkenyl, aryl or COR 1>0>; Z 1Me or COR 1>1>; R 1>1>alkyl, CF 3or aryl; Y : free electron pair (i.e. is absent), or may also be O if Z = Me. An independent claim is also included for the preparation of (I). ACTIVITY : Cytostatic. MECHANISM OF ACTION : None given in the source material.
Inventors:
Horfur, gerhard
Glacier, Nicole
Steinmetz, Heinrich
Reybold, Thomas
Sachet, florentz
Glacier, Nicole
Steinmetz, Heinrich
Reybold, Thomas
Sachet, florentz
Application Number:
JP2004552485A
Publication Date:
January 26, 2011
Filing Date:
October 20, 2003
Export Citation:
Assignee:
Helmholtz-Zentrum Fuer Inffects Forcing Game Bha
International Classes:
C07D417/12; C07D277/56; C07D417/14; C07K5/02; A61K31/454; A61K38/00; A61P35/00
Other References:
THE JOURNAL OF ANTIBIOTICS,2000年,53,9,879-885
Attorney, Agent or Firm:
Kiyoshi Fujino
Kiyonori Fujino
Kyoko Yoshimi
Yoshio Ishii
Sanae Goto
Kiyonori Fujino
Kyoko Yoshimi
Yoshio Ishii
Sanae Goto