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US 8,476,451 B2Granted
Tubulysin D analogues
AssigneeThe Regents of the University of California
InventorsJonathan A. Ellman, Andrew W. Patterson, Hillary Peltier
Life of this patent
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Abstract
The present invention provides novel tubulysin analogues, methods of making and methods of using such analogues and conjugates thereof. The compounds of the invention are highly potent cell-growth inhibitors have been developed that are smaller and considerably more stable than tubulysin D.
Claims24
A compound of the formula which is selected from:
- wherein
- R1 is a nitrogen containing moiety selected from an azide, a hydrazide and a hydrazone;
- R2 is selected from H, substituted alkyl and substituted or unsubstituted heteroalkyl;
- R3 is selected from H, acyl, substituted or unsubstituted alkyl, and substituted or unsubstituted heteroalkyl;
- R6 is a member selected from H, substituted or unsubstituted alkyl and substituted or unsubstituted heteroalkyl;
- R6a, R7a and R8 are independently selected from H, substituted or unsubstituted alkyl and substituted or unsubstituted heteroalkyl;
- and
- Y is a member selected from (CH2)nCOOR4a, (CH2)nOR4;
- and (CH2)nNR4R5
- wherein
- n is an integer from 0 to 10;
- R4a is selected from H, substituted or unsubstituted alkyl and substituted or unsubstituted heteroalkyl;
- and
- R4 and R5 are independently selected from H, substituted or unsubstituted alkyl and substituted or unsubstituted heteroalkyl;
- or a pharmaceutically acceptable salt or prodrug thereof.
12 more elements
A compound of the formula:
- wherein
- R2 is selected from H, substituted alkyl and substituted or unsubstituted heteroalkyl;
- R3 is selected from H, acyl, substituted or unsubstituted alkyl, or substituted or unsubstituted heteroalkyl;
- R6a is selected from H, substituted or unsubstituted alkyl and substituted or unsubstituted heteroalkyl;
- and
- Y is a member selected from (CH2)nCOOR4a, (CH2)nOR4;
- and (CH2)nNR4R5
- wherein
- n is an integer from 0 to 10;
- R4a is selected from H, substituted or unsubstituted alkyl and substituted or unsubstituted heteroalkyl;
- and
- R4 and R5 are independently selected from H, substituted or unsubstituted alkyl and substituted or unsubstituted heteroalkyl;
- or a pharmaceutically acceptable salt or prodrug thereof.
10 more elements
A compound of the formula which is selected from:
- wherein
- R1 is a nitrogen containing moiety selected from an azide, a hydrazide and a hydrazone;
- R2 is selected from H, substituted alkyl and substituted or unsubstituted heteroalkyl;
- R3 is selected from H, acyl, substituted or unsubstituted alkyl, and substituted or unsubstituted heteroalkyl;
- R6 is a member selected from H, substituted or unsubstituted alkyl and substituted or unsubstituted heteroalkyl;
- R6a, R7a and R8 are independently selected from H, substituted or unsubstituted alkyl and substituted or unsubstituted heteroalkyl;
- and
- Y is (CH2)nC(O)NR4R5
- wherein
- n is an integer from 0 to 10;
- and
- R4 and R5 are independently selected from H, unsubstituted alkyl and substituted or unsubstituted heteroalkyl;
- or a pharmaceutically acceptable salt or prodrug thereof.
10 more elements
A compound which is selected from
Dependencies are inferred from the claim text.