	US 11,993,599 B2
	Therapeutic compounds
Elisia Villemure, South San Francisco, CA (US); Joachim Rudolph, South San Francisco, CA (US); and Mingshuo Zeng, South San Francisco, CA (US)
Assigned to GENENTECH, INC., South San Francisco, CA (US)
Filed by Genentech, Inc., South San Francisco, CA (US)
Filed on Aug. 8, 2022, as Appl. No. 17/883,004.
Claims priority of provisional application 63/231,219, filed on Aug. 9, 2021.
Claims priority of provisional application 63/231,220, filed on Aug. 9, 2021.
Prior Publication US 2023/0112485 A1, Apr. 13, 2023
Int. Cl. C07D 471/14 (2006.01); A61K 31/501 (2006.01); C07D 471/08 (2006.01); C07D 471/10 (2006.01); C07D 487/14 (2006.01)

CPC C07D 471/08 (2013.01) [C07D 471/10 (2013.01); C07D 487/14 (2013.01)]

29 Claims

1. A compound of formula (II):

or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein:

(i) R¹is —C═C—R^a, wherein

(a) R^ais C_1-6alkyl, wherein the C_1-6alkyl of R^ais optionally substituted with one or more R^b, wherein each R^bis independently 3-15 membered heterocyclyl, —O-(3-15 membered heterocyclyl), C_1-6alkoxy, —OH, —CN, halo, or —N(R^x)(R^y), wherein

the 3-15 membered heterocyclyl of R^bis optionally substituted with one or more R^c, wherein each R^cis independently —OH, —CN, halo, oxo, C_1-6alkyl, C_1-6alkoxy, C_3-10cycloalkyl, 3-15 membered heterocyclyl, 5-20 membered heteroaryl, —C(O)-(3-15 membered heterocyclyl), —C(O)—C_1-6alkoxy, —C(O)—N(R^x)(R^y), or —N(R^x)(R^y), wherein

the C_1-6alkyl of R^cis optionally substituted with one or more —OH, —CN, halo, C_1-6alkoxy, or 3-15 membered heterocyclyl,

the C_3-10cycloalkyl of R^cis optionally substituted with one or more halo, and

the 3-15 membered heterocyclyl of R^cis optionally substituted with one or more C_1-6alkyl or —C(O)—C_1-6alkyl, and

the C_1-6alkoxy of R^bis optionally substituted with one or more OH, or

(b) R^ais C_3-10cycloalkyl, wherein the C_3-10cycloalkyl of R^ais optionally substituted with one or more R^z, or

(c) R^ais 3-15 membered heterocyclyl, wherein the 3-15 membered heterocyclyl of R^ais optionally substituted with one or more R^z, or

(d) R^ais 5-20 membered heteroaryl, wherein the 5-20 membered heteroaryl of R^ais optionally substituted with one or more R^z, or

(ii) R¹is —(CH₂)_n—R^g, wherein

n is an integer from 1-6, and

R^gis —N(R^x)(R^y) or —OH, wherein

R^zis, independently at each occurrence, —OH, —CN, halo, C_1-6alkyl, C_1-6alkoxy, —N(R^x)(R^y), or —C(O)—N(R^x)(R^y), and

the R^xand R^yof —C(O)N(R^x)(R^y) and —N(R^x)(R^y) are, independently of each other and independently at each occurrence, H, —C(O)—(CH₂)_p—N(R^p)(R^q), 5-20 membered heteroaryl, or C_1-6alkyl, wherein

p is an integer from 1-6,

R^pand R^qare, independently of each other and independently at each occurrence H, or C_1-6alkyl, and

the C_1-6alkyl of R^xor R^yis optionally substituted with one or more —OH, 3-15 membered heterocyclyl, or —C(O)-(3-15 membered heterocyclyl).