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US 11,518,786 B2Granted
Third generation tubulysin analogues and process of preparation thereof
AssigneeIndian Institute of Technology Indore
InventorsVenkatesh Chelvam, Amit Pandit, Ramesh Reddy Baddipally, Kratika Yadav, Biswarup Pathak, Diptendu Roy
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Abstract
The present disclosure relates to a third generation tubulysin analogues and process of preparation thereof. The present disclosure also relates to a method of using these third generation tubulysin analogues for treatment of various diseases including cancer.
Claims12
A compound of Formula I
- Formula I
- and its stereo isomers thereof, wherein R is a methyl group;
- R1 is one of CH2CONHTrt, (CH2)2COOtBu, and CH2COOH•,
- R2 is CH(CH3)2,
- R3 is CH(CH3)CH2CH3, and
- R4 is-(CH2)4 or
3 more elements
A compound of Formula II
- Formula II
- and its stereoisomers thereof, wherein R is a methyl or hydrogen group;
- R1 is one of CH2COOtBu, (CH2)2COOtBu, CH2Ph, and CH2—C6H4-p-OtBu•, R2 is CH(CH3)2, R3 is CH(CH3)CH2CH3, and
- R4 is-(CH2)4 or
1 more element
A pharmaceutical composition comprising a therapeutic amount of compound of Formula I or Formula II.
Dependencies are inferred from the claim text.