Tubulysin compounds with high cytotoxicity, pharmaceutical compositions thereof, and method of use thereof
US8580820B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jul 22, 2010 |
| Grant date | Nov 12, 2013 |
| Priority date | — |
| Expiry date | Jan 9, 2031 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07K5/06139
- WIPO fieldBiotechnology
- WIPO sectorChemistry
Abstract
Tubulysine compounds of formula (A) having a high cytotoxicitywherein:B is selected from CH2, CH2—CH2 or CH2—CH2—CH2,D is an aromatic linker,X1 is alkyl or alkenyl,X2 is selected from the X2a, substituted or non substituted, selected from: aryl, heteroaryl, arylalkyl, cycloalkylalkyl, heterocycloalkylalkyl, or heteroarylalkyl,X2b: alkylene-O-alkyl, wherein alkylene is C2-C10,X2c: CH2—O-alkyl,X3 is selected from H, or together with X4 forms the group ═O,X4 is selected from H, halogen, OH, SH, alkyl, alkenyl, (OR5)n—OR6, OC(O)R7, NR6R7, or together with X4 forms the group ═O,R5 is an alkylene,n is zero or an integer from 1 to 10,R6 and R7, equal to or different from each other, have the following meanings:
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.