US2020216431A1PendingUtilityA1

Compositions and methods for inhibition of the jak pathway

Assignee: RIGEL PHARMACEUTICALS INCPriority: Jan 23, 2009Filed: Jan 3, 2020Published: Jul 9, 2020
Est. expiryJan 23, 2029(~2.5 yrs left)· nominal 20-yr term from priority
A61K 31/54A61K 31/155C07D 498/04C07D 419/14A61K 31/635A61K 31/541C07D 403/12C07D 491/08A61P 27/02A61P 27/14C07D 413/04C07D 471/08C07D 471/04A61K 31/506C07D 413/12A61K 31/538C07D 401/14A61K 31/5377A61K 31/5415C07D 487/08A61K 31/551C07D 413/14C07D 487/10C07D 451/02A61K 31/675C07D 487/04A61K 45/06A61P 27/00A61K 31/5383A61K 31/55A61P 11/06A61P 29/00C07F 9/65583A61P 27/06A61P 37/00A61P 35/00A61P 37/06A61P 9/00A61P 43/00A61P 13/12A61P 1/16
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Claims

Abstract

Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.

Claims

exact text as granted — not AI-modified
1 . A pharmaceutical composition comprising an inhibitory means for inhibiting JAK in a subject and a pharmaceutically acceptable carrier. 
     
     
         2 . The pharmaceutical composition according to  claim 1 , wherein the inhibitory means is a pyrimidine diamine means. 
     
     
         3 . The pharmaceutical composition according to  claim 2 , wherein the pyrimidine diamine means is a 5-halogenpyrimidine diamine means or a 5-alkylpyrimidine diamine means. 
     
     
         4 . The pharmaceutical composition according to  claim 2 , wherein the pyrimidine diamine means is a 5-fluoropyrimidine diamine means or a 5-methylpyrimidine diamine means. 
     
     
         5 . The pharmaceutical composition according to  claim 2 , wherein the pyrimidine diamine means is a 2,4-diaminopyrimidine means. 
     
     
         6 . The pharmaceutical composition according to  claim 5 , wherein the 2,4-diaminopyrimidine means comprises a C 6-10 aryl or a 5-10 membered heteroaryl on the 2-amino moiety. 
     
     
         7 . The pharmaceutical composition according to  claim 6 , wherein the C 6-10 aryl or 5-10 membered heteroaryl is a bicyclic ring moiety. 
     
     
         8 . The pharmaceutical composition according to  claim 6 , wherein the C 6-10 aryl or 5-10 membered heteroaryl is an optionally substituted phenyl, optionally substituted pyridinyl, or optionally substituted isoindolinyl moiety. 
     
     
         9 . The pharmaceutical composition according to  claim 1 , wherein the inhibitory means is an aminobenzoxazolone means. 
     
     
         10 . The pharmaceutical composition according to  claim 1 , wherein the inhibitory means is an (aminopyrimidin-4-yl)amino)benzo [d]oxazol-2(3H)-one means. 
     
     
         11 . The pharmaceutical composition according to  claim 1 , wherein the inhibitory means is a salt. 
     
     
         12 . The pharmaceutical composition according to  claim 1 , wherein the inhibitory means comprises a pyrimidinediamine moiety, a benzoxazolone moiety and a phenyl moiety. 
     
     
         13 . The pharmaceutical composition according to  claim 1 , wherein the inhibitory means comprises a pyrimidinediamine moiety, a benzoxazolone moiety and a pyridinyl moiety. 
     
     
         14 . The pharmaceutical composition according to  claim 1 , wherein the inhibitory means comprises a pyrimidinediamine moiety, a benzoxazolone moiety and a bicyclic ring moiety. 
     
     
         15 . The pharmaceutical composition according to  claim 14 , wherein the bicyclic ring moiety comprises a phenyl ring and a 5-membered partially saturated ring optionally comprising one or more heteroatoms. 
     
     
         16 . A method of inhibiting an activity of a JAK kinase, comprising contacting the JAK kinase with an amount of an inhibitory means for inhibiting the JAK kinase, the amount being effective to inhibit an activity of the JAK kinase. 
     
     
         17 . A method, comprising administering to a subject a pyrimidine diamine means for inhibiting a JAK kinase. 
     
     
         18 . A method of treating a JAK kinase-mediated disease, comprising administering to a subject an amount of the pharmaceutical composition of  claim 1  effective to treat or prevent the JAK kinase-mediated disease. 
     
     
         19 . A method of treating a T-cell mediated autoimmune disease, comprising administering to a patient suffering from such an autoimmune disease an amount of the pharmaceutical composition of  claim 1  effective to treat the autoimmune disease. 
     
     
         20 . A method of treating a disease and/or disorder of the eye, comprising administering to a subject an amount of the pharmaceutical composition of  claim 1  effective to treat the disease and/or disorder of the eye.

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