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US 10,208,011 B2Granted
Benzothiophene estrogen receptor modulators
AssigneeG1 Therapeutics, Inc.
InventorJay Copeland Strum
Life of this patent
Estimating the term…
Abstract
This invention is a benzothiophene estrogen receptor modulator or its pharmaceutically acceptable salt or a pharmaceutically acceptable composition thereof to treat an estrogen-related medical disorder.
Claims15
A compound selected from:
- or a pharmaceutically acceptable salt thereof;
- wherein A is:
- m is 0, 1, or 2;
- n is 1, 2, or 3;
- o is 0, 1, 2, 3, 4, or 5;
- Z is selected from —O—, —C(R3)2—, —CHR3—, —CH2—, —CHF—, —CF2—, and —S—;
- ZA and ZB are independently selected from —O—, —C(R3)2—, —CHR3—, —CH2—, —CHF—, —CF2—, and —S—;
- each R1 is independently selected from C1-C3alkyl, halogen, and C1-C3haloalkyl;
- R2 is selected from:
- a. 4-6 membered heterocycle optionally substituted with one, two, or three groups independently selected from R4;
- b. —NH2, —NH(C1-C3alkyl or C2-C3haloalkyl), and —N((independently)C1-C3alkyl or C2-C3haloalkyl)2;
- c. monocyclic 7-8 membered heterocycle optionally substituted with one, two, or three groups independently selected from R4;
- and
- d. 6-12 membered bicyclic or bridged heterocycle optionally substituted with one, two, or three groups independently selected from R4;
- R3 is independently selected from —F, —Cl, —Br, —CH3, —CH2F, —CHF2, and —CF3;
- R4 is selected from hydrogen, halogen, C1-C3alkyl, and C1-C3haloalkyl;
- and
- R5 is selected from hydrogen, halogen, C1-C3alkyl, and C1-C3haloalkyl.
15 more elements
A compound selected from:
- or a pharmaceutically acceptable salt thereof,
- wherein A is:
- Y is
- m is 0, 1, or 2;
- n is 1, 2, or 3;
- o is independently 0, 1, 2, 3, 4, or 5;
- Z is selected from —O—, —C(R3)2—, —CHR3—, —CH2—, —CHF—, —CF2—, and —S—;
- ZA and ZB are independently selected from —O—, —C(R3)2—, —CHR3—, —CH2—, —CHF—, —CF2—, and —S—;
- each R1 is independently selected from C1-C3alkyl, halogen, and C1-C3haloalkyl;
- R2 is selected from:
- a. 4-6 membered heterocycle optionally substituted with one, two, or three groups independently selected from R4;
- b. —NH2, —NH(C1-C3alkyl or C2-C3haloalkyl), and —N((independently)C1-C3alkyl or C2-C3haloalkyl)2;
- c. monocyclic 7-8 membered heterocycle optionally substituted with one, two, or three groups independently selected from R4;
- d. 6-12 membered bicyclic or bridged heterocycle optionally substituted with one, two, or three groups independently selected from R4;
- and
- e. hydroxyl, alkoxy, —NH—(CH2)n1—NH2, —NH—(CH2)n1—NH(C1-C12alkyl or C2-C12haloalkyl), —NH—(CH2)n1—N((independently)C1-C12alkyl or C2-C12haloalkyl), —NHC4-C12alkyl, and —N(C1-C12alkyl)2;
- n1 is 2, 3, 4, 5, or 6;
- R3 is independently selected from —F, —Cl, —Br, —CH3, —CH2F, —CHF2, and —CF3;
- R4 is selected from hydrogen, halogen, C1-C3alkyl, and C1-C3haloalkyl;
- or R4 is selected from hydrogen, halogen, C1-C3alkyl, C1-C3haloalkyl, —COOH, —COOC1-C12alkyl, —CONH2, —CON(H)alkyl, and —CON(alkyl)2;
- R5 is selected from hydrogen, halogen, C1-C3alkyl, and C1-C3haloalkyl;
- and
- R7 is a 4, 5, 6, 7, 8, 9, or 10 membered heterocycle optionally substituted with 1, 2, or 3 groups selected from R4.
20 more elements
Dependencies are inferred from the claim text.