.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 8,703,780

« Back to Dashboard

Claims for Patent: 8,703,780

Title:Inhibitors of Bruton's tyrosine kinase
Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
Inventor(s): Honigberg; Lee (San Francisco, CA), Verner; Erik (Belmont, CA), Pan; Zhengying (Austin, TX)
Assignee: Pharmacyclics, Inc. (Sunnyvale, CA)
Application Number:13/526,161
Patent Claims: 1. A method of treating a leukemia in a subject comprising administering to a subject in need thereof an irreversible inhibitor of Bruton's tyrosine kinase (Btk), having the structure of Formula (A): ##STR00056## wherein: A is N; R.sub.1 is phenyl-O-phenyl or phenyl-5-phenyl; R.sub.2 and R.sub.3 are independently H; R.sub.4 is L.sub.3-X-L.sub.4-G, wherein, L.sub.3 is optional, and when present is an optionally substituted or unsubstituted alkylene, optionally substituted or unsubstituted cycloalkylene, optionally substituted or unsubstituted alkenylene, or optionally substituted or unsubstituted alkynylene; X is optional, and when present is O, --C(.dbd.O), S, --S(.dbd.O), --S(.dbd.O).sub.2, --NH, --NR.sub.9, --NHC(O), --C(O)NH, --NR.sub.9C(O), --C(O)NR.sub.9, --S(.dbd.O).sub.2NH, --NHS(.dbd.O).sub.2, --S(.dbd.O).sub.2NR.sub.9-- --NR.sub.9S(.dbd.O).sub.2, OC(O)NH--, --NHC(O)O--, --OC(O)NR.sub.9-- --NR.sub.9C(O)O--, --CH.dbd.NO--, --ON.dbd.CH--, --NR.sub.10C(O)NR.sub.10--, heteroarylene, arylene, --NR.sub.10C(.dbd.NR.sub.11)NR.sub.10--, --NR.sub.10C(.dbd.NR.sub.11)--, --C(.dbd.NR.sub.11)NR.sub.10--, --OC(.dbd.NR.sub.11)--, or --C(.dbd.NR.sub.11)O--; L.sub.4 is optional, and when present is a substituted or unsubstituted alkylene, substituted or unsubstituted cycloalkylene, substituted or unsubstituted alkenylene, substituted or unsubstituted alkynylene, substituted or unsubstituted arylene, substituted or unsubstituted heteroarylene, or substituted or unsubstituted heterocyclene; or L.sub.3, X and L.sub.4 taken together form a nitrogen containing heterocyclic ring; G is ##STR00057## wherein, R.sub.6, R.sub.7 and R.sub.8 are independently selected from among H, lower alkyl or substituted lower alkyl, lower heteroalkyl or substituted lower heteroalkyl, substituted or unsubstituted lower cycloalkyl, and substituted or unsubstituted lower heterocycloalkyl; R.sub.9 is selected from among H, substituted or unsubstituted lower alkyl, and substituted or unsubstituted lower cycloalkyl; each R.sub.10 is independently H, substituted or unsubstituted lower alkyl, or substituted or unsubstituted lower cycloalkyl; or two R.sub.10 groups can together form a 5-, 6-, 7-, or 8-membered heterocyclic ring; or R.sub.10 and R.sub.11 can together form a 5-, 6-, 7-, or 8-membered heterocyclic ring; and R.sub.11 is selected from H, --S(.dbd.O).sub.2R.sub.8, --S(.dbd.O).sub.2NH.sub.2, --C(O)R.sub.8, --CN, --NO.sub.2, heteroaryl, or heteroalkyl; or a pharmaceutically acceptable salt thereof.

2. The method of claim 1, wherein the leukemia is Burkitt leukemia.

3. The method of claim 1, wherein the irreversible Btk inhibitor is administered orally.

4. The method of claim 1, wherein the irreversible Btk inhibitor has the structure: ##STR00058##

5. The method of claim 1 wherein L.sub.3, X and L.sub.4 taken together form a nitrogen containing heterocyclic ring.

6. The method of claim 5 wherein G is ##STR00059##

7. The method of claim 5 wherein R.sub.6, R.sub.7, and R.sub.8 are each independently H.

8. A method of treating a leukemia in a subject comprising administering to a subject in need thereof an irreversible inhibitor of Bruton's tyrosine kinase (Btk), having the structure of ##STR00060## or a pharmaceutically acceptable salt thereof.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc