US2015290200A1PendingUtilityA1

Intracellular kinase inhibitors

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Assignee: PHARMACYCLICS INCPriority: May 18, 2006Filed: Apr 24, 2015Published: Oct 15, 2015
Est. expiryMay 18, 2026(expired)· nominal 20-yr term from priority
Inventors:Gary A. FlynnSandra LeeMary FarisDavid BrandtSubrata Chakravarty
A61P 7/02A61P 35/02A61P 7/06A61P 37/02A61P 43/00A61P 3/10A61P 37/06A61P 37/00A61P 35/00A61P 7/04A61P 7/00A61P 29/00A61P 25/02A61P 25/00C07D 317/54C07D 209/44C07D 319/18A61K 31/40A61K 31/137C07D 207/14C07D 211/30A61P 11/06A61K 31/538C07D 295/215C07D 333/56A61P 1/02A61K 31/5377C07D 207/08A61K 31/445C07D 211/10A61P 17/00C07D 295/185A61K 31/4035A61K 31/5375C07D 295/108C07D 217/04A61K 31/495C07D 307/80A61P 21/00C07D 401/04A61K 31/47A61P 1/04A61P 1/16C07D 307/52C07D 295/192A61K 31/33C07D 211/26A61P 13/12A61P 19/02C07D 401/06C07D 265/36
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Claims

Abstract

Intracellular kinase inhibitors and their therapeutic uses for patients with T cell malignancies, B cell malignancies, autoimmune disorders, and transplanted organs.

Claims

exact text as granted — not AI-modified
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         14 . A method of inhibiting the activity of a human interleukin-2 inducible tyrosine kinase in a biological sample, wherein said human interleukin-2 inducible tyrosine kinase has a cysteine at position 442, said method comprising:
 (a) Contacting the biological sample with an effective inhibitory amount of an ITK inhibitor, and   (b) Covalently binding said ITK inhibitor to the sulfur atom of Cys442 of the human interleukin-2 inducible tyrosine kinase (ITK) present in said biological sample, said covalent binding taking place at and within the active site of said kinase;   whereby the activity of said human interleukin-2 inducible tyrosine kinase (ITK) is inhibited.   
     
     
         15 . The method of  claim 1  wherein said human interleukin-2 inducible tyrosine kinase comprises SEQ ID NO: 1. 
     
     
         16 . A method of inhibiting the activity of a human Brutons's tyrosine kinase in a biological sample, wherein said human Bruton's tyrosine kinase has a cysteine at position 481, said method comprising:
 (a) Contacting the biological sample with an effective inhibitory amount of an ITK inhibitor, and   (b) Covalently binding said ITK inhibitor to the sulfur atom of Cys481 of the human Bruton's tyrosine kinase (BTK) present in said biological sample, said covalent binding taking place at and within the active site of said kinase;   whereby the activity of said human Bruton's tyrosine kinase is inhibited.   
     
     
         17 . The method of  claim 3  wherein said human Bruton's tyrosine kinase comprises SEQ ID NO:2.

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