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US 11,993,599 B2Granted
Therapeutic compounds
AssigneeGenentech, Inc.
InventorsElisia Villemure, Joachim Rudolph, Mingshuo Zeng
Life of this patent
Estimating the term…
Abstract
The present disclosure relates to compounds and salts thereof that are useful for modulating target polypeptides and proteins, in particular BRM. Also disclosed are pharmaceutical compositions comprising the compounds, or a salt (e.g., a pharmaceutically acceptable salt) thereof, and methods of using such compounds and salts in the treatment of various BRM-mediated and/or BRG1-mediated diseases or disorders.
Claims29
A compound of formula (II):
- or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein:
- (i) R1 is —C═C—Ra, wherein
- (a) Ra is C1-6alkyl, wherein the C1-6alkyl of Ra is optionally substituted with one or more Rb, wherein each Rb is independently 3-15 membered heterocyclyl, —O-(3-15 membered heterocyclyl), C1-6alkoxy, —OH, —CN, halo, or —N(Rx)(Ry), wherein
- the 3-15 membered heterocyclyl of Rb is optionally substituted with one or more Rc, wherein each Rc is independently —OH, —CN, halo, oxo, C1-6alkyl, C1-6alkoxy, C3-10cycloalkyl, 3-15 membered heterocyclyl, 5-20 membered heteroaryl, —C(O)-(3-15 membered heterocyclyl), —C(O)—C1-6alkoxy, —C(O)—N(Rx)(Ry), or —N(Rx)(Ry), wherein
- the C1-6alkyl of Rc is optionally substituted with one or more —OH, —CN, halo, C1-6alkoxy, or 3-15 membered heterocyclyl,
- the C3-10cycloalkyl of Rc is optionally substituted with one or more halo, and
- the 3-15 membered heterocyclyl of Rc is optionally substituted with one or more C1-6alkyl or —C(O)—C1-6alkyl, and
- the C1-6alkoxy of Rb is optionally substituted with one or more OH, or
- (b) Ra is C3-10cycloalkyl, wherein the C3-10cycloalkyl of Ra is optionally substituted with one or more Rz, or
- (c) Ra is 3-15 membered heterocyclyl, wherein the 3-15 membered heterocyclyl of Ra is optionally substituted with one or more Rz, or
- (d) Ra is 5-20 membered heteroaryl, wherein the 5-20 membered heteroaryl of Ra is optionally substituted with one or more Rz, or
- (ii) R1 is —(CH2)n—Rg, wherein
- n is an integer from 1-6, and
- Rg is —N(Rx)(Ry) or —OH, wherein
- Rz is, independently at each occurrence, —OH, —CN, halo, C1-6alkyl, C1-6alkoxy, —N(Rx)(Ry), or —C(O)—N(Rx)(Ry), and
- the Rx and Ry of —C(O)N(Rx)(Ry) and —N(Rx)(Ry) are, independently of each other and independently at each occurrence, H, —C(O)—(CH2)p—N(Rp)(Rq), 5-20 membered heteroaryl, or C1-6alkyl, wherein
- p is an integer from 1-6,
- Rp and Rq are, independently of each other and independently at each occurrence H, or C1-6alkyl, and
- the C1-6alkyl of Rx or Ry is optionally substituted with one or more —OH, 3-15 membered heterocyclyl, or —C(O)-(3-15 membered heterocyclyl).
16 more elements
Dependencies are inferred from the claim text.