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
Patent number: 7235669
Abstract: The invention concerns compounds which can be obtained by fermenting DSM 6773, especially epothilones A1, A2, A8, A9, B10, C1, C2, C3, C4, C5, C6, C7, C8, C9, D1, D2, D5, G1, G2, H1, H2, I1, I2, I3, I4, I5, I6 and K and trans-epothilones C1 and C2.
Type:
Grant
Filed:
February 15, 2006
Date of Patent:
June 26, 2007
Assignee:
Helmholtz-Zentrum fur Infektionsforschung, GmbH
Inventors:
Gerhard Hoefle, Hans Reichenbach, Klaus Gerth, Ingo Hardt, Florenz Sasse, Heinrich Steinmetz
Publication number: 20060142584
Abstract: The invention concerns compounds which can be obtained by fermenting DSM 6773, especially epothilones A1, A2, A8, A9, B10, C1, C2, C3, C4, C5, C6, C7, C8, C9, D1, D2, D5, G1, G2, H1, H2, I1, I2, I3, I4, I5, I6 and K and trans-epothilones C1 and C2.
Type:
Application
Filed:
February 15, 2006
Publication date:
June 29, 2006
Inventors:
Gerhard Hoefle, Hans Reichenbach, Klaus Garth, Ingo Hardt, Florenz Sasse, Heinrich Steinmetz
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
