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US 9,957,276 B2Granted
CDK inhibitors
AssigneeGI Therapeutics, Inc.
InventorsFrancis X. Tavares, Jay C. Strum
Life of this patent
Estimating the term…
Abstract
Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.
Claims57
A compound of formula:
- or a pharmaceutically acceptable salt thereof, wherein:
- Z is —(CH2)x— wherein x is 2 or 3;
- each X is independently CH or N;
- each R1 is independently aryl, alkyl, or cycloalkyl, wherein two R1s on adjacent ring atoms or on the same ring atom together with the ring atom(s) to which they are attached optionally form a 3-8-membered cycle;
- y is 0, 1, 2, or 3;
- R2 is -(alkylene)m-heterocyclo, -(alkylene)m-heteroaryl, -(alkylene)m-NR3R4, -(alkylene)m-C(O)—NR3R4, -(alkylene)m-C(O)—O-alkyl, -(alkylene)m-O—R5, -(alkylene)m-S(O)n—R5, or -(alkylene)m-S(O)n—NR3R4 any of which may be optionally independently substituted with one or more Rx groups as allowed by valence;
- m is 0 or 1;
- n is 1 or 2;
- R3 and R4 at each occurrence are independently:
- (i) hydrogen or
- (ii) alkyl, cycloalkyl, heterocyclo, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkyl, arylalkyl, or heteroarylalkyl, or R3 and R4 together with the nitrogen atom to which they are attached may combine to form a heterocyclo ring;
- R5 is:
- (i) hydrogen or
- (ii) alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclo, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkyl, arylalkyl, or heteroarylalkyl;
- Rx at each occurrence is independently, halo, cyano, nitro, alkyl, haloalkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclo, aryl, heteroaryl, arylalkyl, heteroarylalkyl, cycloalkylalkyl, or heterocycloalkyl;
- and
- R6 is a lower alkyl or absent.
14 more elements
A compound of formula:
- or a pharmaceutically acceptable salt thereof, wherein:
- Z is —(CH2)x— wherein x is 2 or 3;
- each X is independently CH or N;
- each R1 is independently aryl, alkyl, or cycloalkyl, wherein two R1s on adjacent ring atoms or on the same ring atom together with the ring atom(s) to which they are attached optionally form a 3-8-membered cycle;
- y is 0, 1, 2, or 3;
- R6 is a lower alkyl or absent;
- R2 is
- R2* is a bond, alkylene, -(alkylene)m-O-(alkylene)m-, -(alkylene)m-C(O)-(alkylene)m-, -(alkylene)m-S(O)2-(alkylene)m- or -(alkylene)m-NH-(alkylene)m-;
- P is a 4- to 8-membered mono- or bicyclic saturated heterocyclyl group;
- each Rx1 is independently —(C(O))—O-alkyl, -(alkylene)m-cycloalkyl, —N(RN)-cycloalkyl, —C(O)-cycloalkyl, -(alkylene)m-heterocyclyl, —N(RN)-heterocyclyl, —C(O)-heterocyclyl, or —S(O)2-(alkylene)m;
- RN is H, C1 to C4 alkyl or C1 to C6 heteroalkyl;
- m is 0 or 1;
- and
- t is 0, 1 or 2.
11 more elements
A compound of formula:
- or a pharmaceutically acceptable salt thereof, wherein:
- Z is —(CH2)x— wherein x is 2 or 3;
- each X is independently CH or N;
- each R1 is independently aryl, alkyl, or cycloalkyl, wherein two R1s on adjacent ring atoms or on the same ring atom together with the ring atom(s) to which they are attached optionally form a 3-8-membered cycle;
- y is 0, 1, 2, or 3;
- R6 is a lower alkyl or absent;
- R2 is
- R2* is a bond, alkylene, -(alkylene)m-O-(alkylene)m-, -(alkylene)m-C(O)-(alkylene)m-, -(alkylene)m-S(O)2-(alkylene)m- or -(alkylene)m-NH-(alkylene)m-;
- P is a 4- to 8-membered mono- or bicyclic saturated heterocyclyl group;
- P1 is a 4- to 6-membered monocyclic saturated heterocyclyl group;
- each Rx2 is independently hydrogen or alkyl;
- m is 0 or 1;
- and
- s is 0, 1 or 2.
11 more elements
Dependencies are inferred from the claim text.