Back to results
US 11,691,982 B2Granted
Thailanstatin analogs
AssigneepH Pharma Co., Ltd.
InventorsVasu Jammalamadaka, Sanjeev Satyal, Hoyoung Huh
Life of this patent
Estimating the term…
Abstract
The invention provides novel cytotoxic compounds and cytotoxic conjugates comprising these cytotoxic compounds and cell-binding agents. More specifically, this invention relates to novel thailanstatin A analogs, useful as cytotoxic small molecule toxins in antibody-drug conjugates (ADCs). The present invention further relates to compositions including these cytotoxic compounds and ADCs, and methods for using these toxins and ADCs to treat pathological conditions including cancer.
Claims9
A compound of Formula (II):
- or a pharmaceutically acceptable salt thereof, wherein:
- L is a linker;
- R is selected from the group consisting of:
- —(CH2)n—R1;
- -5 to 6 membered heteroaryl, where heteroaryl is optionally substituted with one or more of halogen, —CF3, —C1-6alkyl, and —O—C1-6alkyl;
- —C(R2)═N—R3;
- —CH(CF3)NH(CH2)mCH3;
- —C(RaRb)NH(CH2)mCH3;
- —C(halogen)=CH(CH2)mCH3;
- —SO2—NH(CH2)mCH3;
- —O(CO)-aryl;
- —O(CO)-heteroaryl;
- —NRaRb;
- and —NH-heteroaryl;
- wherein R1 is —O—CRaRb(CH2)mCH3 or —N—CRaRb(CH2)mCH3;
- wherein Ra and Rb, together with the atoms to which they are joined, form a C3-10 heterocyclyl ring;
- R2 is —CN or —NH(CH2)mCH3;
- R3 is —(CH2)mCH3 or —O—(CH2)mCH3;
- each n is independently 1, 2, or 3;
- and
- each m is independently 0, 1, 2, or 3.
18 more elements
A compound of Formula (II):
- or a pharmaceutically acceptable salt thereof, wherein:
- L is a linker;
- and
- R is selected from the group consisting of
1 more element
Dependencies are inferred from the claim text.