Back to results
US 10,479,786 B2Granted
Protein kinase inhibitors
AssigneePrinceton Drug Discovery Inc
InventorKan He
Life of this patent
Estimating the term…
Abstract
The present invention concerns novel deuterated and non-deuterated cyclic chemical compounds and their corresponding salts thereof active on protein kinases in general, and in particular as inhibitors of protein kinases. Additionally, methods of treating mammals with protein kinase-mediated diseases or conditions by administering a therapeutically effective amount of the novel deuterated or non-deuterated cyclic chemical compound and their corresponding salts thereof.
Claims30
A compound of formula I:
- and/or a salt, an enantiomer or an enantiomeric mixture thereof;
- wherein
- W1, W2, and W3 are independently hydrogen or deuterium;
- Y is C—H or nitrogen;
- R1 is
- -Q-A
- wherein
- Q is a single bond directly attaching A to a ring carbon atom, or a methylene or ethylene group connecting A to a ring carbon atom;
- and
- A is
- wherein
- Y1 is C—H or nitrogen and Y2 is carbon and wherein A is a five or six membered ring;
- Z1 and Z2 are independently hydrogen, —(CH2)n—OR5, or [—NR7R6], where n is an integer number from 0 to 4, and R5 R6 are independently hydrogen, lower alkyl, or lower alkenyl;
- T1 and T2 are independently an integer number from 0 to 4 with the provisos that when T1 or T2 is 0, —(CH2)T1 or —(CH2)T2 is a single bond;
- R2 and R3 are independently hydrogen;
- halogen;
- alkoxyl;
- lower alkyl or lower alkenyl, wherein the lower alkyl or lower alkenyl is optionally substituted with one or more substituents selected from —OH and alkoxyl, wherein alkoxyl is methoxy, ethoxy, propyloxy, or tert-butoxy;
- or optionally substituted heterocyclo, wherein optionally substituted includes [—NR7R6], wherein R6 and R7 are independently hydrogen, lower alkyl, or lower alkenyl;
- and wherein the positions of R1, R2 and R3 are exchangeable.
17 more elements
A compound of formula II:
- and/or a salt, an enantiomer or an enantiomeric mixture thereof:
- wherein W1, W2, and W3 are independently hydrogen or deuterium;
- wherein Y is C—H or nitrogen;
- wherein R2, R3, and R4 are independently hydrogen;
- halogen;
- alkoxyl;
- lower alkyl or lower alkenyl, wherein the lower alkyl or lower alkenyl is optionally substituted with one or more substituents selected from —OH and alkoxyl, wherein alkoxyl is methoxy, ethoxy, propyloxy, or tert-butoxy;
- or optionally substituted heterocyclo, wherein optionally substituted includes [—NR7R6], wherein R6 and R7 are independently hydrogen, lower alkyl, or lower alkenyl;
- and
- wherein X is independently hydrogen, —(CH2)n—OR5, or [—NR7R6], wherein n is an integer number from 0 to 4 and R5 R6 are independently hydrogen, lower alkyl, or lower alkenyl.
7 more elements
A compound of formula III:
- and/or a salt, an enantiomer or an enantiomeric mixture thereof:
- wherein W1, W2, and W3 are independently hydrogen or deuterium;
- wherein Y is C—H or nitrogen;
- wherein R2, R3, and R4 are independently H;
- halogen;
- alkoxyl;
- lower alkyl or lower alkenyl, wherein the lower alkyl or lower alkenyl is optionally substituted with one or more substituents selected from —OH and alkoxyl, wherein alkoxyl is methoxy, ethoxy, propyloxy, or tert-butoxy;
- or optionally substituted heterocyclo, wherein optionally substituted includes [NR7R6], wherein R6 are independently hydrogen, lower alkyl, or lower alkenyl.
5 more elements
A pharmaceutical composition comprising a compound of formula 1
- and/or a salt, an enantiomer or an enantiomeric mixture thereof;
- wherein
- W1, W2, and W3 are independently hydrogen or deuterium;
- Y is C—H or nitrogen;
- R1 is
- -Q-A
- wherein
- Q is a single bond directly attaching A to a ring carbon atom, or a methylene or ethylene group connecting A to a ring carbon atom;
- and
- A is
- wherein
- Y1 is C—H or nitrogen and Y2 is carbon and wherein A is a five or six membered ring;
- Z1 and Z2 are independently hydrogen, —(CH2)n—OR5, or [—NR7R6], where n is an integer number from 0 to 4, and R5 R6 are independently hydrogen, lower alkyl, or lower alkenyl;
- T1 and T2 are independently an integer number from 0 to 4 with the provisos that when T1 or T2 is 0, —(CH2)T1 or —(CH2)T2 is a single bond;
- R2 and R3 are independently hydrogen;
- halogen;
- alkoxyl;
- lower alkyl or lower alkenyl, wherein the lower alkyl or lower alkenyl is optionally substituted with one or more substituents selected from —OH and alkoxyl, wherein alkoxyl is methoxy, ethoxy, propyloxy, or tert-butoxy;
- or optionally substituted heterocyclo, wherein optionally substituted includes [—NR7R6], wherein R6 and R7 are independently hydrogen, lower alkyl, or lower alkenyl;
- and wherein the positions of R1, R2 and R3 are exchangeable;
- and a pharmaceutically acceptable excipient or carrier.
18 more elements
Dependencies are inferred from the claim text.