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US 12,577,245 B2Granted
Sulfonyl benzamide derivatives as Bcl-2 inhibitors
AssigneesAscentage Pharma (Suzhou) Co., Ltd., Ascentage Pharma Group Corp Limited
InventorsDongbo Li, Jianyong Chen, Fang Liu, Hao Chen, Xianchan Zha
Life of this patent
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Abstract
The present disclosure provides compounds having Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein variables are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a disease, disorder, or condition responsive to Bcl-2 protein inhibition, particularly Bcl-2 WT and/or Bcl-2 G101V.
Claims21
A compound of Formula (I):
- or a pharmaceutically acceptable salt or solvate thereof, wherein:
- Ring X is a 5- or 6-membered ring, containing one or more additional degrees of unsaturation;
- each R1 independently is selected from the group consisting of C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and halogen;
- p is 0, 1, or 2;
- Ring Y is a 5- to 9-membered mono- or fused-ring system, including at least one S, and optionally containing one or more additional heteroatom selected from the group consisting of O, N, or S, and containing one or more degrees of unsaturation;
- each R2 independently is selected from the group consisting of (CH2)t—R4, CONH—R4, NHC(O)—R4, NHR4, and (C≡C)—R4;
- each R4 independently is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-10 cycloalkyl, aryl, C3-10 heterocyclyl, heteroaryl;
- each R4 may be substituted with one or more of the group consisting of C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, halogen, C3-6 cycloalkyl, C3-6 heterocyclyl, OSO2CH3, NH2, NHC1-6 alkyl, N(C1-6 alkyl), C1-6 alkoxy, OH, C1-6 alkyl-OH, C2-6 alkyl (OH) (C3-46cycloalkyl), C1-6 haloalkyl-OH, C3-6 cycloalkyl-OH, C1-6 alkyl-COOH, C1-6 alkyl-O—C1-6 alkyl, CN, C1-6 alkyl-CN, C1-6 alkyl-NHC(O)—C1-6 alkyl, and C1-6 alkyl-C(O) NH—C1-6 alkyl;
- q is 1 or 2;
- each t is 0, 1, 2, 3, 4, 5, or 6;
- Ring Z is a saturated 6-membered ring, optionally containing one or more O;
- each R3 is selected from the group consisting of one or more of C1-6 alkyl, C1-6 alkoxy, and OH;
- and
- r is 0, 1, or 2.
11 more elements
A compound, or a pharmaceutically acceptable salt thereof, selected from the group consisting of:
Dependencies are inferred from the claim text.