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US 12,668,598 B2Granted
MK2 inhibitors and uses thereof
AssigneeBristol-Myers Squibb Company
InventorsXirui Hu, Lixin Qiao, Boris Seletsky, Matthew Patton, Min Cao, Farid van der Mei, Guobin Miao, Ivar McDonald, Carolyn Dzierba
Life of this patent
Estimating the term…
Abstract
The present invention provides compounds, compositions thereof, and methods of using the MK2 inhibitors of the Formula:
Claims13
A compound of formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- Ring A is a 5-6 membered heteroaryl ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur, provided that when Ring A is a 6-membered heteroaryl ring the 1-3 heteroatoms are each nitrogen;
- each R1 and R1′ is independently selected from -hydrogen and C1-4 aliphatic substituted with 0-3 instances of Rx, or:
- R1 and R1′ may, together with the intervening atoms to which they are attached, form an optionally substituted 3- to 6-membered saturated, or partially unsaturated, heterocyclyl, carbocycle, or aryl ring having 0-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
- Rx is —CN, —NO2, halogen, —OR, —SR, —N(R)2, —C(O)N(R)2, —C(O)OR, —C(O)R, —N(R)C(O)R, —SO2N(R)2, or —N(R)SO2;
- R2 is —CN, C2-6 aliphatic substituted with m instances of Ry, wherein the C2-6 aliphatic has at least one unit of unsaturation, or R2 is selected from the group consisting of
- each Ry is independently selected from D, halogen, —CN, —CO2R, —N(R)2, and a 3- to 6-membered saturated or partially unsaturated heterocyclic ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
- each R3 is —(CH2)r-Cy, or R3 is selected from the group consisting of
- each R4 is independently selected from hydrogen, C1-6 aliphatic, and —Cy, wherein the C1-6 aliphatic is optionally substituted with one or more substituents each independently selected from D, halogen and —OR;
- each R5 is independently selected from —OR and —Cy;
- each Cy is independently a ring selected from a 3- to 9-membered saturated or partially unsaturated monocyclic carbocyclic ring, a 3- to 9-membered saturated or partially unsaturated monocyclic heterocyclic ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur, phenyl, a 5- to 6-membered heteroaryl ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur, a 7- to 12-membered saturated or partially unsaturated fused, spirofused, or bridged bicyclic carbocyclic ring, or a 7- to 12-membered saturated or partially unsaturated fused, spirofused, or bridged bicyclic heterocyclic ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur, wherein the ring is optionally substituted with one or more substituents each independently selected from D, halogen, oxo, R, and —(CH2)q—OR;
- each R is independently hydrogen or a C1-6 aliphatic optionally substituted with one or more substituents each selected from D, halogen, —OH, and —O—(C1-6 aliphatic), or:
- two R groups on the same nitrogen are taken together with the nitrogen to form a 3-7 membered saturated or partially unsaturated heterocyclic ring having 1-3 heteroatoms selected from nitrogen, oxygen, or sulfur;
- n is 0;
- each of q, and r is independently 0-4;
- and
- tis 1-4.
14 more elements
A compound which is (R)-10-methyl-3-(5-methyl-2-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one.
A compound which is (R)-10-methyl-3-(5-methyl-2-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.