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US 2020/0048250 A1Published application
Selective estrogen receptor degraders and uses thereof
AssigneeInventisbio Co., Ltd.
InventorsXing DAI, Yaolin WANG
Life of this patent
Estimating the term…
Abstract
The present disclosure provides compounds of Formula (I) and Formula (II). The compounds described herein may be useful in treating proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.
Claims31
A compound of Formula (I):
- or a pharmaceutically acceptable salt thereof,
- wherein:
- A is —CRA═ or —N═, as valency permits;
- W is —NH—, —O—, or —S—;
- a is 1, 2, or 3;
- n is 1, 2, 3, or 4;
- each instance of R1 is independently hydrogen, halogen, substituted or unsubstituted alkyl, —ORA, or —CN;
- R2 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl;
- R3 is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, —ORA, or —N(RB)2;
- R4 is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, —ORA or —N(RB)2;
- R5 is hydrogen, halogen, substituted or unsubstituted alkyl;
- R6 is hydrogen, halogen, substituted or unsubstituted alkyl;
- R7 is hydrogen, halogen, substituted or unsubstituted alkyl, —ORA or —N(RB)2;
- RA is hydrogen or substituted or unsubstituted alkyl, or oxygen protecting group;
- and
- RB is hydrogen or substituted or unsubstituted alkyl, nitrogen protecting group, or optionally two RB are taken together with the intervening atoms to form substituted or unsubstituted heterocyclyl or substituted or unsubstituted heteroaryl.
13 more elements
2-23. (canceled)
A compound of Formula (II):
- or a pharmaceutically acceptable salt thereof,
- wherein:
- A is —CRA═ or —N═, as valency permits;
- W is —NH—, —O—, or —S—;
- a is 1, 2, or 3;
- each instance of R1 is independently hydrogen, halogen, substituted or unsubstituted alkyl, —ORA, or —CN;
- R2 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl;
- R3 is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, —ORA or —N(RB)2;
- R4 is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, —ORA or —N(RB)2, or R3 and R4 are taken together with the intervening atoms to form substituted or unsubstituted carbocyclyl or substituted or unsubstituted heterocyclyl;
- R8 is hydrogen, halogen, or methyl;
- RA1 is substituted or unsubstituted alkyl, chlorine, or fluorine;
- RA2 is substituted or unsubstituted alkyl, chlorine, or fluorine, wherein:
- (i) either RA1 or RA2 is chlorine;
- or (ii) one of RA1 and RA2 is fluorine, and the other one of RA1 and RA2 is selected from the group consisting of substituted or unsubstituted alkyl, chlorine, and fluorine;
- RA is hydrogen or substituted or unsubstituted alkyl, or oxygen protecting group;
- and
- RB is hydrogen or substituted or unsubstituted alkyl, nitrogen protecting group, or optionally two RB are taken together with the intervening atoms to form substituted or unsubstituted heterocyclyl or substituted or unsubstituted heteroaryl;
- wherein when both RA1 and RA are fluorine, the compound further satisfies at least one of the following conditions:
- W is O or S:
- at least one of R1 is not hydrogen;
- R2 is not hydrogen or methyl;
- A is —N═;
- R3 and R4 are taken together with the intervening atoms to form substituted or unsubstituted carbocyclyl or substituted or unsubstituted heterocyclyl;
- or
- at least two of R3, R4, and R8 are each independently halogen.
22 more elements
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45-46. (canceled)
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Dependencies are inferred from the claim text.