Patent number: 7754885
Abstract: The invention relates to a compound of the following general formula (tubulysin) having the following meanings for R, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, S, T, U, V, W, X, Y and Z: R=H, alkyl, aryl, OR1, NR1R2 or R1=H, C1-6alkyl or aryl R2=H, C1-6alkyl or aryl S=H, Hal, NO2 or NHR3 U=H, Hal, NO2 or NHR3 R3=H, HCO or C1-4alkyl-CO T=H or OR4 R4=H, C1-4alkyl, aryl, COR5, P(O)(OR6)2 or SO3R6 R5=C1-6alkyl, alkenyl, aryl or heteroaryl R6=H, alkyl or a metal ion V=H, OR7, Hal or (for W=O) O R7=H, C1-4alkyl or COR8 R5=C1-4alkyl, alkenyl or aryl W=H or C1-4alkyl or (for V=O) O X=H, C1-4alkyl, alkenyl or CH2OR9 R9=H, C1-4alkyl, alkenyl, aryl or COR10 R10=C1-6alkyl, alkenyl, aryl or heteroaryl Y=(for Z=CH3 or COR11) free electron pair or (for Z=CH3)O R11=C1-4alkyl, CF3 or aryl and/or Z=(for Y=O or free electron pair) CH3 or (for Y=free electron pair) COR11.
Type:
Grant
Filed:
October 20, 2003
Date of Patent:
July 13, 2010
Assignee:
Helmholtz-Zentrum fuer Infektionsforschung GmbH
Inventors:
Gerhard Hoefle, Nicole Glaser, Heinrich Steinmetz, Thomas Leibold, Florenz Sasse
Publication number: 20060128754
Abstract: The invention relates to a compound of the following general formula (tubulysin) having the following meanings for R, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, S, T, U, V, W, X, Y and Z: R=H, C1-4alkyl, aryl, OR1, NR1R2 or NH—(CH2)2-4 R1=H, C1-6alkyl or aryl R2=H, C1-6alkyl or aryl S=H, Hal, NO2 or NHR3 U=H, Hal, NO2 or NHR3 R3=H, HCO or C1-4alkyl-CO T=H or OR4 R4=H, C1-4alkyl, aryl, COR5, P(O)(OR6)2 or SO3R6 R5=C1-6alkyl, alkenyl, aryl or heteroaryl R6=H, alkyl or a metal ion V=H, OR7, Hal or (for W=O)O R7=H, C1-4alkyl or COR8 R5=C1-4alkyl, alkenyl or aryl W=H or C1-4alkyl or (for V=O) O X=H, C1-4alkyl, alkenyl or CH2OR9 R9=H, C1-4alkyl, alkenyl, aryl or COR10 R10=C1-6alkyl, alkenyl, aryl or heteroaryl Y=(for Z=CH3 or COR11) free electron pair or (for Z=CH3)O R11=C1-4alkyl, CF3 or aryl and/or Z=(for Y=O or free electron pair) CH3 or (for Y=free electron pair) COR11.
Type:
Application
Filed:
October 20, 2003
Publication date:
June 15, 2006
Inventors:
Gerhard Hoefle, Nicole Glaser, Heinrich Steinmetz, Thomas Leibold, Florenz Sasse