GCN2 inhibitors and uses thereof

Patent metadata

Field	Value
Publication number	US-10793563-B2
Application number	US-201916260019-A
Country	US
Kind code	B2
Filing date	Jan 28, 2019
Priority date	Jan 29, 2018
Publication date	Oct 6, 2020
Grant date	Oct 6, 2020

Abstract

The present invention provides compounds, compositions thereof, and methods of using the same.

First claim

We claim:

1. A compound of one of formula XV-a, XV-a, or XV-c:

or a pharmaceutically acceptable salt thereof, wherein:
each of R 1 is independently hydrogen, halogen, —CN, —NO 2 , —C(O)R, —C(O)OR, —C(O)NR 2 , —C(O)NRS(O) 2 R, —C(O)N═S(O)R 2 , —NR 2 , —NRC(O)R, —NRC(O)NR 2 , —NRC(O)OR, —NRS(O) 2 R, —NRS(O) 2 NR 2 , —OR, —ON(R)SO 2 R, —P(O)R 2 , —SR, —S(O)R, —S(O) 2 R, —S(O)(NH)R, —S(O) 2 N(R) 2 , —S(NH 2 ) 2 (O)OH, —N═S(O)R 2 , —CH 3 , —CH 2 OH, —CH 2 NHSO 2 CH 3 , —CD 3 , —CD 2 NRS(O) 2 R, or R; or
two R 1 groups are optionally taken together to form ═O or ═NH; or
two R 1 groups are optionally taken together to form a bivalent C 2-4 alkylene chain;

each R is independently hydrogen or an optionally substituted group selected from C 1-6 aliphatic, a 3-8 membered saturated or partially unsaturated monocyclic carbocyclic ring, phenyl, an 8-10 membered bicyclic aromatic carbocyclic ring, a 4-8 membered saturated or partially unsaturated monocyclic heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur, a 5-6 membered monocyclic heteroaromatic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an 8-10 membered bicyclic heteroaromatic ring having 1-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur; or
two R groups are optionally taken together to form a bivalent C 2-4 alkylene chain; or
two R groups are optionally taken together with their intervening atoms to form an optionally substituted 3-7 membered saturated or partially unsaturated monocyclic ring having 0-4 heteroatoms independently selected from nitrogen, oxygen or sulfur;

m is 0, 1, 2, 3, 4 or 5.

2. The compound of claim 1 , wherein m is 1, 2 or 3.

3. A compound selected from the group consisting of:

Assignees

• Merck Patent Gmbh
• Vertex Pharma

Inventors

• Bleich Matthew
• Charrier Jean-Damien
• Dong Huijun
• Durrant Steven
• Eno Meredith Suzanne
• Etxebarria I Jardi Gorka
• Everitt Simon
• Fraysse Damien
• Knegtel Ronald
• Mochalkin Igor
• North Kiri
• Porichis Filippos
• Qiu Hui
• Pullin Robert
• Storck Pierre-Henri
• Twin Heather Clare
• Xiao Yufang

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• C07D519/00

  Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00 · CPC title

• C07D471/04 Primary

  Ortho-condensed systems · CPC title

• A61P25/28

  for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia · CPC title

• A61K31/506

  not condensed and containing further heterocyclic rings · CPC title