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US 8,709,431 B2Granted
Enediyne compounds, conjugates thereof, and uses and methods therefor
AssigneeBristol-Myers Squibb Company
InventorsNaidu S. Chowdari, Sanjeev Gangwar, Bilal Sufi
Life of this patent
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Abstract
Enediyne compounds having a structure according to formula (I), where R0, R2, R3, R4, R5, R6, and R7 are defined herein, can be used in chemotherapeutic drugs, especially in conjugates, for the treatment of diseases such as cancer.
Claims16
A compound having a structure represented by formula (Ia):
- wherein
- R1a is H, C1-C6 alkyl, (CH2)nNH2, C(═O)(CH2)nNH2, C(═O)CHR8NH2, or C(═O)R9NH2;
- R8 is the side chain residue of an α-amino acid selected from the group consisting of alanine, arginine, asparagine, aspartic acid, γ-carboxyglutamic acid, citrulline, cysteine, glutamic acid, glutamine, glycine, histidine, isoleucine, leucine, lysine, methionine, norleucine, norvaline, ornithine, phenylalanine, serine, threonine, tryptophan, tyrosine, and valine;
- R9 is unsubstituted or substituted arylene, unsubstituted or substituted heteroarylene, unsubstituted or substituted alkylarylene, unsubstituted or substituted cycloalkylene or unsubstituted or substituted heterocycloalkylene;
- and
- n is 2, 3, 4, 5, or 6;
- or a pharmaceutically acceptable salt thereof.
4 more elements
A conjugate having a structure represented by formula (III)
- [D(XD)aC(XZ)b]mZ (III)
- wherein
- Z is a targeting moiety that specifically or preferentially binds to a chemical entity on a target cell;
- XD is a first spacer moiety;
- Xz is a second spacer moiety;
- C is a cleavable group;
- subscripts a and b are independently 0 or 1;
- subscript m is 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10;
- and
- D is selected from the group consisting of
7 more elements
A composition having a structure according to formula (IV)
- D-(XD)aC(XZ)b—R31 (IV)
- wherein
- R31 is a reactive functional group;
- XD is a first spacer moiety;
- Xz is a second spacer moiety;
- C is a cleavable group;
- subscripts a and b are independently 0 or 1;
- subscript m is 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10;
- and
- D is selected from the group consisting of
7 more elements
Dependencies are inferred from the claim text.