Publication number: 20060046997
Abstract: This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula (I) in which R1a, R1b, R2a, R3a, R3b, R4, R5, R6, R7, A, Y, D, E, G, Y and Z have the meanings that are indicated in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and thus find use in treating diseases or conditions associated with the need for cell growth, division and/or proliferation. Thus the compounds are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanoma, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (such as psoriasis, arthritis). Methods of use and preparation of the compounds are also described.
Type:
Application
Filed:
August 31, 2005
Publication date:
March 2, 2006
Inventors:
Ulrich Klar, Wolfgang Schwede, Werner Skuballa, Bernd Buchmann, Jens Hoffmann, Rosemarie Lichtner
Publication number: 20050113429
Abstract: This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula (I) in which R1a, R1b, R2b, R3a, R3b, R4, R5, R6, R7, A, Y, D, E, G, Y and Z have the meanings that are indicated in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and thus find use in treating diseases or conditions associated with the need for cell growth, division and/or proliferation. Thus the compounds are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanoma, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (such as psoriasis, arthritis). Methods of use and preparation of the compounds are also described.
Type:
Application
Filed:
October 18, 2004
Publication date:
May 26, 2005
Inventors:
Ulrich Klar, Wolfgang Schwede, Werner Skuballa, Bernd Buchmann, Jens Hoffmann, Rosemarie Lichtner
Publication number: 20050080060
Abstract: This invention describes the new 17?-fluoroalkyl steroids of general formula I in which R1 stands for a methyl or ethyl group, R2 stands for a radical of formula CnFmHo, whereby n is 2, 3, 4, 5 or 6, m>1 and m+o=2n+1, R3 stands for a free, etherified or esterified hydroxy group, R4 and R5 each stand for a hydrogen atom, or together for an additional bond or a methylene group, St stands for a steroidal ABC-ring system of partial formula A, B or C in which R6 means a hydrogen atom, a straight-chain C1-C4 alkyl group or branched C3-C4 alkyl group or a halogen atom, R7 means a hydrogen atom, a straight-chain C1-C4 alkyl group or a branched C3-C4 alkyl group, or if St stands for a steroidal ABC-ring system A or B, in addition R6 and R7 together can mean an additional bond, X means an oxygen atom, a hydroxyimino grouping ?N—OH or two hydrogen atoms, R8 means a radical Y or an aryl radical that is optionally substituted in several places with a group Y, whereby Y is a hydrogen atom, a halogen at
Type:
Application
Filed:
September 24, 2004
Publication date:
April 14, 2005
Inventors:
Wolfgang Schwede, Arwed Cleve, Ulrich Klar, Gunter Neef, Kristof Chwalisz, Martin Schneider, Ulrike Fuhrmann, Holger Heb-Stumpp