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US 10,239,862 B2Granted
Benzazepine compounds, conjugates, and uses thereof
AssigneeSilverback Therapeutics, Inc.
InventorsCraig Alan Coburn, Peter Robert Baum, Sean Wesley Smith
Life of this patent
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Abstract
Benzazepine compounds, conjugates, and pharmaceutical compositions for use in the treatment of disease, such as cancer, are disclosed herein. The disclosed benzazepine compounds are useful, among other things, in the treating of cancer and modulating TLR8. Additionally, benzazepine compounds incorporated into a conjugate with an antibody construct are described herein.
Claims21
A compound represented by the structure of Formula (IIA):
- or a pharmaceutically acceptable salt thereof, wherein:
- represents an optional double bond;
- L10 is selected from —C(O)— and —C(O)N(R10)—*, wherein * represents where L10 is bound to R5;
- L2 is selected from a bond and —C(O)—;
- R1 and R2 are independently selected from hydrogen, C1-10 alkyl, C2-10 alkenyl, and C2-10 alkynyl;
- R4 is selected from —OR10, —N(R10)2, —C(O)N(R10)2, —C(O)R10, —C(O)OR10, —S(O)R10, —S(O)2R10, C1-10 alkyl, C2-10 alkenyl and C2-10 alkynyl;
- R5 is selected from unsaturated C4-s carbocycle, bicyclic carbocycle, and fused 5-5, fused 5-6, and fused 6-6 bicyclic heterocycle, wherein R5 is optionally substituted and wherein substituents are independently selected at each occurrence from:
- halogen, —OR10, —SR10, —C(O)N(R10)2, —N(R10)C(O)R10, —N(R10)C(O)N(R10)2, —N(R10)2, —C(O)R10, —C(O)OR10, —OC(O)R10, —NO2, ═O, ═S, ═N(R10), and —CN;
- and
- C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, each of which is optionally substituted with one or more substituents independently selected from halogen, —OR10, —
- SR10, —C(O)N(R10)2, —N(R10)C(O)R10, —N(R10)C(O)N(R10)2, —
- N(R10)2, —C(O)R10, —C(O)OR10, —OC(O)R10, —NO2, ═O, ═S, ═N(R10), —CN, C3-12 carbocycle, and 3- to 12-membered heterocycle;
- and
- C3-12 carbocycle, and 3- to 12-membered heterocycle, wherein each C3-12 carbocycle, and 3- to 12-membered heterocycle in R5 is optionally substituted with one or more substituents independently selected from halogen, —OR10, —SR10, —C(O)N(R10)2, —N(R10)C(O)R10, —N(R10)C(O)N(R10)2, —N(R10)2, —C(O)R10, —C(O)OR10, —OC(O)R10, —NO2, ═O, ═S, ═N(R10), —CN, C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl;
- and
- R10 is independently selected at each occurrence from hydrogen, —NH2, and —C(O)OCH2C6H5;
- and C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-12 carbocycle, and 3- to 12-membered heterocycle, each of which is optionally substituted with one or more substituents independently selected from halogen, —OH, —CN, —NO2, —NH2, ═O, ═S, —C(O)OCH2C6H5, —NHC(O)OCH2C6H5, C1-10 alkyl, —C1-10 haloalkyl, —O—C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-12 carbocycle, 3- to 12-membered heterocycle, and haloalkyl.
14 more elements
Dependencies are inferred from the claim text.