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US 10,519,136 B2Granted
Dual inhibitors of PARP1 and CDK
AssigneeAccutar Biotechnology Inc.
InventorsJie Fan, Ke Liu
Life of this patent
Estimating the term…
Abstract
Disclosed herein, in various embodiments, are compounds having dual activity as PARP1 and CDK inhibitors, and pharmaceutical compositions comprising the same. In some embodiments, the present disclosure provides for methods of treating diseases or conditions in a subject in need thereof, comprising administering one or more compounds disclosed herein. In some embodiment, the disease is cancer, including breast cancer.
Claims31
A compound having a structure according to Formula I,
- or a pharmaceutically acceptable salt, or tautomer, thereof,
- wherein:
- M is a bond, —NH—, or —C(O)—;
- L is a aryl, arylalkyl, or heteroarylalkyl comprising a 5- to 20-membered heteroaryl having one to six heteroatoms selected from the group consisting of N, O, or S, each of which is optionally substituted with one or more halogen, aryl, 5- to 20-membered heteroaryl comprising one to six heteroatoms selected from the group consisting of N, O, or S, arylalkyl, or heteroarylalkyl comprising a 5- to 20 membered heteroaryl having one to six heteroatoms selected from the group consisting of N, O, or S, wherein the aryl, heteroaryl, arylalkyl, or heteroarylalkyl is optionally substituted with one or more substituents selected from the group consisting of halogen, nitro, hydroxyl, SH, oxo, alkyl, alkenyl, alkynyl, aryl, 3- to 20-membered heterocyclyl comprising one to six heteroatoms selected from the group consisting of N, O, or S, NRgRh, NRgC(═O)Rh, NRgC(═O)NRgRh, NRgC(═O)ORh, NRgSO2Rh, OC(═O)NRgRh, ORg, SRg, SORg, SO2Rg, OSO2Rg, SO2ORg, ═NSO2Rg, and SO2NRgRh, C(═O)Rg, C(═O)ORg, —C(O)NRgRh, CH2SO2Rg, and CH2SO2NRgRh, wherein each of Rg and Rh are independently hydrogen, alkyl, alkenyl, or alkynyl;
- Q is CH2, O, S, or a bond;
- W and Y are independently CH or N, provided that at least one of W or Y is N, and when W is CH, Q is O or S;
- R1 and R2 are independently selected from hydrogen, halogen, alkyl, and 3- to 20-membered heterocyclyl comprising one to six heteroatoms selected from the group consisting of N, O, or S, each of which is optionally substituted with one or more halogen or alkyl;
- or R1 and R2 together with the atoms are to which they are attached form a C3-C20 carbocyclyl or 3- to 20-membered heterocyclyl comprising one to six heteroatoms selected from the group consisting of N, O, or S, each of which is optionally substituted with one or more halogen, alkyl, carbocyclyl comprising from 3 to 20 carbon atoms, oxo, —C(O)Rg, wherein Rg is alkyl, and —C(O)NRaRb, wherein each of Ra and Rb are independently selected from H or alkyl;
- and
- R9 is hydrogen, halogen, or alkyl.
7 more elements
Dependencies are inferred from the claim text.