	US 11,952,349 B2
	Anti-cancer nuclear hormone receptor-targeting compounds
Son Minh Pham, San Francisco, CA (US); Jayakanth Kankanala, Saint Paul, MN (US); Jeremy Pettigrew, Vancouver (CA); and Christopher Paul Miller, San Mateo, CA (US)
Assigned to Nuvation Bio Inc., New York, NY (US)
Filed by Nuvation Bio Inc., New York, NY (US)
Filed on Nov. 12, 2020, as Appl. No. 17/096,743.
Claims priority of provisional application 62/935,065, filed on Nov. 13, 2019.
Prior Publication US 2021/0214316 A1, Jul. 15, 2021
This patent is subject to a terminal disclaimer.
Int. Cl. C07D 237/32 (2006.01)

CPC C07D 237/32 (2013.01)

10 Claims

1. A compound of Formula A-L-B, wherein:

A is A1 or A4, wherein:

L is L1, L2, L3, L4, L5, L6, L7, L8, L9, L10, L11, L12, L13, L14, L15, L16, L17, L18, L19, L20, L21, L22, L23, L24, L25, L26, L27, L28, L29, L30, L31, L32, L33, L34, L35, L36, L37, L38, L39, L40, L41, L42, L43, L44, L45, or L46, wherein:

and;

B is B1, B2, B3, B4, B5, B6, B7, B8, B9, B10, B11, B12, B13, B14, B4-5-B16, B17, B18, or B19, wherein:

and further wherein the “*” in A1 and A4 and each L moiety denotes a covalent bond therebetween, and the wavy line in each L and B denotes a covalent bond therebetween;

wherein the compound of Formula A-L-B is selected from:


		A1-L1-B1
		A1-L1-B2
		A1-L1-B3
		A1-L1-B4
		A1-L1-B5
		A1-L1-B6
		A1-L1-B7
		A1-L1-B8
		A1-L1-B9
		A1-L1-B10
		A1-L1-B11
		A1-L1-B12
		A1-L1-B13
		A1-L2-B1
		A1-L2-B2
		A1-L2-B3
		A1-L2-B4
		A1-L2-B5
		A1-L2-B6
		A1-L2-B7
		A1-L2-B8
		A1-L2-B9
		A1-L2-B10
		A1-L2-B11
		A1-L2-B12
		A1-L2-B13
		A1-L3-B1
		A1-L3-B2
		A1-L3-B3
		A1-L3-B4
		A1-L3-B5
		A1-L3-B6
		A1-L3-B7
		A1-L3-B8
		A1-L3-B9
		A1-L3-B10
		A1-L3-B11
		A1-L3-B12
		A1-L3-B13
		A1-L4-B1
		A1-L4-B2
		A1-L4-B3
		A1-L4-B4
		A1-L4-B5
		A1-L4-B6
		A1-L4-B7
		A1-L4-B8
		A1-L4-B9
		A1-L4-B10
		A1-L4-B11
		A1-L4-B12
		A1-L4-B13
		A1-L5-B1
		A1-L5-B2
		A1-L5-B3
		A1-L5-B4
		A1-L5-B5
		A1-L5-B6
		A1-L5-B7
		A1-L5-B8
		A1-L5-B9
		A1-L5-B10
		A1-L5-B11
		A1-L5-B12
		A1-L5-B13
		A1-L6-B1
		A1-L6-B2
		A1-L6-B3
		A1-L6-B4
		A1-L6-B5
		A1-L6-B6
		A1-L6-B7
		A1-L6-B8
		A1-L6-B9
		A1-L6-B10
		A1-L6-B11
		A1-L6-B12
		A1-L6-B13
		A1-L7-B1
		A1-L7-B2
		A1-L7-B3
		A1-L7-B4
		A1-L7-B5
		A1-L7-B6
		A1-L7-B7
		A1-L7-B8
		A1-L7-B9
		A1-L7-B10
		A1-L7-B11
		A1-L7-B12
		A1-L7-B13
		A1-L8-B1
		A1-L8-B2
		A1-L8-B3
		A1-L8-B4
		A1-L8-B5
		A1-L8-B6
		A1-L8-B7
		A1-L8-B8
		A1-L8-B9
		A1-L8-B10
		A1-L8-B11
		A1-L8-B12
		A1-L8-B13
		A1-L9-B1
		A1-L9-B2
		A1-L9-B3
		A1-L9-B7
		A1-L9-B8
		A1-L9-B9
		A1-L9-B11
		A1-L9-B13
		A1-L20-B1
		A1-L20-B2
		A1-L20-B3
		A1-L20-B4
		A1-L20-B5
		A1-L20-B6
		A1-L20-B7
		A1-L20-B8
		A1-L20-B9
		A1-L20-B10
		A1-L20-B11
		A1-L20-B12
		A1-L20-B13
		A1-L21-B1
		A1-L21-B2
		A1-L21-B3
		A1-L21-B4
		A1-L21-B5
		A1-L21-B6
		A1-L21-B7
		A1-L21-B8
		A1-L21-B9
		A1-L21-B10
		A1-L21-B11
		A1-L21-B12
		A1-L21-B13
		A1-L22-B1
		A1-L22-B2
		A1-L22-B3
		A1-L22-B4
		A1-L22-B5
		A1-L22-B6
		A1-L22-B7
		A1-L22-B8
		A1-L22-B9
		A1-L22-B10
		A1-L22-B11
		A1-L22-B12
		A1-L22-B13
		A1-L23-B1
		A1-L23-B2
		A1-L23-B3
		A1-L23-B4
		A1-L23-B5
		A1-L23-B6
		A1-L23-B7
		A1-L23-B8
		A1-L23-B9
		A1-L23-B10
		A1-L23-B11
		A1-L23-B12
		A1-L23-B13
		A1-L24-B1
		A1-L24-B2
		A1-L24-B3
		A1-L24-B4
		A1-L24-B5
		A1-L24-B6
		A1-L24-B7
		A1-L24-B8
		A1-L24-B9
		A1-L24-B10
		A1-L24-B11
		A1-L24-B12
		A1-L24-B13
		A1-L30-B1
		A1-L30-B2
		A1-L30-B3
		A1-L30-B4
		A1-L30-B5
		A1-L30-B6
		A1-L30-B7
		A1-L30-B8
		A1-L30-B9
		A1-L30-B10
		A1-L30-B11
		A1-L30-B12
		A1-L30-B13
		A1-L31-B1
		A1-L31-B2
		A1-L31-B3
		A1-L31-B4
		A1-L31-B5
		A1-L31-B6
		A1-L31-B7
		A1-L31-B8
		A1-L31-B9
		A1-L31-B10
		A1-L31-B11
		A1-L31-B12
		A1-L31-B13
		A1-L32-B1
		A1-L32-B2
		A1-L32-B3
		A1-L32-B7
		A1-L32-B8
		A1-L32-B9
		A1-L32-B11
		A1-L32-B13
		A1-L39-B1
		A1-L39-B2
		A1-L39-B3
		A1-L39-B4
		A1-L39-B5
		A1-L39-B6
		A1-L39-B7
		A1-L39-B8
		A1-L39-B9
		A1-L39-B10
		A1-L39-B11
		A1-L39-B12
		A1-L39-B13
		A1-L40-B1
		A1-L40-B2
		A1-L40-B3
		A1-L40-B4
		A1-L40-B5
		A1-L40-B6
		A1-L40-B7
		A1-L40-B8
		A1-L40-B9
		A1-L40-B10
		A1-L40-B11
		A1-L40-B12
		A1-L40-B13
		A1-L41-B1
		A1-L41-B2
		A1-L41-B3
		A1-L41-B4
		A1-L41-B5
		A1-L41-B6
		A1-L41-B7
		A1-L41-B8
		A1-L41-B9
		A1-L41-B10
		A1-L41-B11
		A1-L41-B12
		A1-L41-B13
		A1-L42-B1
		A1-L42-B2
		A1-L42-B3
		A1-L42-B4
		A1-L42-B5
		A1-L42-B6
		A1-L42-B7
		A1-L42-B8
		A1-L42-B9
		A1-L42-B10
		A1-L42-B11
		A1-L42-B12
		A1-L42-B13
		A1-L43-B1
		A1-L43-B2
		A1-L43-B3
		A1-L43-B4
		A1-L43-B5
		A1-L43-B6
		A1-L43-B7
		A1-L43-B8
		A1-L43-B9
		A1-L43-B10
		A1-L43-B11
		A1-L43-B12
		A1-L43-B13
		A1-L44-B1
		A1-L44-B2
		A1-L44-B3
		A1-L44-B7
		A1-L44-B8
		A1-L44-B9
		A1-L44-B11
		A1-L44-B13
		A1-L20-B14
		A1-L21-B14
		A1-L22-B14
		A1-L23-B14
		A1-L24-B14
		A1-L2-B14
		A1-L3-B14
		A1-L45-B14
		A1-L20-B16
		A1-L21-B16
		A1-L22-B16
		A1-L23-B16
		A1-L24-B16
		A1-L2-B16
		A1-L3-B16
		A1-L45-B16
		A1-L20-B17
		A1-L21-B17
		A1-L22-B17
		A1-L23-B17
		A1-L24-B17
		A1-L2-B17
		A1-L3-B17
		A1-L45-B17
		A1-L20-B18
		A1-L21-B18
		A1-L22-B18
		A1-L23-B18
		A1-L24-B18
		A1-L2-B18
		A1-L3-B18
		A1-L45-B18
		A1-L20-B19
		A1-L21-B19
		A1-L22-B19
		A1-L23-B19
		A1-L24-B19
		A1-L2-B19
		A1-L3-B19
		A1-L45-B19
		A4-L46-B10
		A4-L18-B10
		A4-L19-B10
		A4-L46-B16
		A4-L18-B16
		A4-L19-B16
		A4-L46-B6
		A4-L18-B6
		A4-L19-B6 and
		A1-L45-B10

or a stereoisomer, mixture of stereoisomers, hydrate, solvate, isotopically enriched analog or pharmaceutically acceptable salt thereof.