Azaindoles useful as inhibitors of JAK and other protein kinases
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Abstract
The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
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Citations
90 Claims
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1-66. -66. (canceled)
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67. A compound of formula (IB)
or pharmaceutically acceptable salts thereof, wherein: -
R1 is T-R′
or is —
Si(R′
)3;R2, R3, and R4 are each independently halogen, CN, NO2, or V—
R′
;x is 1, 2 or 3; each occurrence of R5 is independently halogen, CN, NO2, or U—
R′
, wherein at least one R5 is —
N(R′
)2, —
NR′
CH(CH2OH)R′
, —
NR′
CH(CH2CH2OH)R′
, —
NR′
(CH2)R′
, —
NR′
(CH2)2R′
, NR′
(CH2)N(R′
)2, —
NR′
(CH2)2N(R′
)2, —
OR′
, —
NR′
COR′
, —
NR′
COCH2R′
, or —
NR′
CO(CH2)2R′
;T, V, and U are each independently a bond or an optionally substituted C1-C6 alkylidene chain, wherein up to two methylene units of the chain are optionally and independently replaced by —
NR′
—
, —
S—
, —
O—
, —
CS—
, —
CO2—
, —
OCO—
, —
CO—
, —
COCO—
, —
CONR′
—
, —
NR′
CO—
, —
NR′
CO2—
, —
SO2NR′
—
, —
NR′
SO2—
, —
CONR′
NR′
—
, —
NR′
CONR′
—
, —
OCONR′
—
, —
NR′
NR′
—
, —
NR′
SO2NR′
—
, —
SO—
, —
SO2—
, —
PO—
, —
PO2—
, or —
POR′
—
; andeach occurrence of R′
is independently hydrogen or an optionally substituted group selected from a C1-C6 aliphatic group, a 3-8-membered saturated, partially unsaturated, or fully unsaturated monocyclic ring having 0-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an 8-12 membered saturated, partially unsaturated, or fully unsaturated bicyclic ring system having 0-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur;
or two occurrences of R′
, are taken together with the atom(s) to which they are bound to form an optionally substituted 3-12 membered saturated, partially unsaturated, or fully unsaturated monocyclic or bicyclic ring having 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, provided that;a) if R2, R3 and R4 are simultaneously H, then R′
is not Si(R′
)3; andb) if R1, R2 and R4 are simultaneously H then R3 is not phenyl or phenyl substituted with O-phenyl or N(Me)2. - View Dependent Claims (68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 89, 90)
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88. A compound selected from:
Specification