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Inhibitors of tyrosine kinases and uses thereof

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Title: Inhibitors of tyrosine kinases and uses thereof.
Abstract: Disclosed herein are compounds that inhibit the activity of particular tyrosine kinases. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of tyrosine kinase-mediated diseases or conditions or tyrosine kinase-dependent diseases or conditions are provided. ...


Browse recent Pharmacyclics, Inc. patents - Sunnyvale, CA, US
Inventors: Orion D. Jankowski, James T. Palmer, Lee Honigberg
USPTO Applicaton #: #20120083470 - Class: 514 81 (USPTO) - 04/05/12 - Class 514 
Drug, Bio-affecting And Body Treating Compositions > Designated Organic Active Ingredient Containing (doai) >Phosphorus Containing Other Than Solely As Part Of An Inorganic Ion In An Addition Salt Doai >Nitrogen Containing Hetero Ring >Polycylo Ring System Having A Ring Nitrogen In The System >Nonshared Hetero Atoms In At Least Two Rings Of The Polycyclo Ring System

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The Patent Description & Claims data below is from USPTO Patent Application 20120083470, Inhibitors of tyrosine kinases and uses thereof.

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RELATED APPLICATIONS

This application claims benefit of U.S. Provisional Application No. 60/758,617 entitled “INHIBITORS OF TYROSINE KINASES” filed Jan. 13, 2006, which is herein incorporated by reference.

FIELD OF THE INVENTION

Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.

BACKGROUND OF THE INVENTION

Bruton\'s tyrosine kinase (Btk), a member of the Tec family of non-receptor tyrosine kinases, is a key signaling enzyme expressed in all hematopoietic cells types except T lymphocytes and natural killer cells. Btk plays an essential role in the B-cell signaling pathway linking cell surface B-cell receptor (BCR) stimulation to downstream intracellular responses.

Btk is a key regulator of B-cell development, activation, signaling, and survival (Kurosaki, Curr Op Imm, 2000, 276-281; Schaeffer and Schwartzberg, Curr Op Imm 2000, 282-288). In addition, Btk plays a role in a number of other hematopoetic cell signaling pathways, e.g., Toll like receptor (TLR) and cytokine receptor-mediated TNF-α production in macrophages, IgE receptor (FcepsilonRI) signaling in Mast cells, inhibition of Fas/APO-1 apoptotic signaling in B-lineage lymphoid cells, and collagen-stimulated platelet aggregation. See, e.g., C. A. Jeffries, et al., (2003), Journal of Biological Chemistry 278:26258-26264; N. J. Horwood, et al., (2003), The Journal of Experimental Medicine 197:1603-1611; Iwaki et al. (2005), Journal of Biological Chemistry 280(48):40261-40270; Vassilev et al. (1999), Journal of Biological Chemistry 274(3):1646-1656, and Quek et al. (1998), Current Biology 8(20):1137-1140.

SUMMARY

OF THE INVENTION

Compounds, compositions and methods for inhibiting the activity of a subset of tyrosine kinases (such as Btk) are provided. In one embodiment, compounds provided herein are used to inhibit Bruton\'s tyrosine kinase (Btk), and are thus inhibitors of Btk. Processes for the preparation of compounds that inhibit the activity of certain tyrosine kinases, compositions that include the compounds, as well as methods of use thereof are provided.

Compounds provided herein include those that have a structure of Formula (Ia), Formula (Ib), Formula (Ic), Formula (II), Formula (III), Formula (IIIa), Formula (IIIb), Formula (IIIc), Formula (IV), Formula (V), and/or Formula (VI), and pharmaceutically acceptable salts, solvates, esters, acids and prodrugs thereof. In certain embodiments, isomers and chemically protected forms of compounds having a structure represented by Formula (Ia), Formula (Ib), Formula (Ic), Formula (II), Formula (III), Formula (IIIa), Formula (IIIb), Formula (IIIc), Formula (IV), Formula (V), and/or Formula (VI), are also provided.

In one aspect, provided herein are compounds of Formula (III):

wherein: Ra and Rb are each independently selected from among H, halogen, CN, NO2, C1-C4alkyl, C1-C4haloalkyl, and C1-C4alkoxy; T is 1,6-dimethyl-9-oxo-8,9-dihydro-1H-imidazo[4,5-h]isoquinolin-2,7-ylene, or 1,7-dimethyl-9-oxo-8,9-dihydro-1H-imidazo[4,5-h]isoquinolin-2,6-ylene; L is —X250a—Y250— or —Y250—X250a—, wherein, X250a is a substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6haloalkyl, substituted or unsubstituted C3-C8cycloalkyl, substituted or unsubstituted C5-C8cycloalkenyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C2-C6haloalkenyl, substituted or unsubstituted C2-C6alkynyl, or substituted or unsubstituted C2-C6haloalkynyl; Y250 is a bond, —O—, —S(═O)—, —S(═O)2—, —C(═O)—, —NR45—, —NH—, —NHC(═O)—, —NR45C(═O)—, —NR45C(═O)NR45—, —C(═O)NH—, —C(═O)NR45—, —OC(═O)—, —C(═O)O—, —NHSO2—, —NR45SO2—, —SO2NH—, —SO2NR45—, —C(R45)═NO—, —CH═NO—, —ON═CH—, heteroaryl, aryl, —NHC(═O)O—, —OC(═O)NH—, —NR45C(═O)O—, or —OC(═O)NR45—; where each R45 is independently selected from among hydrogen, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C3-C8cycloalkyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C2-C6alkynyl; M is N or CH; W is

E is oxygen or sulfur; R100 is halogen, —OH, or an optionally substituted group selected from among C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, phenyl, C1-C4alkyl(phenyl), C3-C8cycloalkyl, C1-C4alkyl(C3-C8cycloalkyl), C2-C8heterocycloalkyl, C1-C4alkyl(C2-C8heterocycloalkyl), heteroaryl, C1-C4alkyl(heteroaryl), C1-C6alkoxy, C1-C6alkenyloxy, C1-C6alkynyloxy, or —NR102aR102b; R102a and R102b are independently hydrogen, or an optionally substituted group selected from among C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, aryl, aralkyl, heteroaryl, heteroaralkyl, C3-C8cycloalkyl, C1-C4alkyl(C3-C8cycloalkyl), C2-C8heterocycloalkyl, and C1-C4alkyl(C2-C8heterocycloalkyl); R200 is an optionally substituted group selected from among C2-C10acyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, C1-C4alkyl(C3-C6cycloalkyl), aryl, heteroaryl, heteroaralkyl, C1-C6alkylsulfonyl, C2-C6alkenylsulfonyl, arylsulfonyl, heteroarylsulfonyl, C1-C10alkoxycarbonyl, aminosulfonyl, C1-C6alkylaminosulfonyl, di(C1-C6alkyl)aminosulfonyl, and C1-C6alkylsulfonylamino; R350a is hydrogen, a substituted or unsubstituted C1-C6alkyl, a substituted or unsubstituted C2-C6alkenyl, a substituted or unsubstituted C2-C6alkynyl, a substituted or unsubstituted C1-C6haloalkyl, a substituted or unsubstituted C2-C6haloalkenyl, or a substituted or unsubstituted C2-C6haloalkynyl; n is 0, 1, or 2; and pharmaceutically active metabolites, pharmaceutically acceptable solvates, pharmaceutically acceptable salts, or pharmaceutically acceptable prodrugs thereof.

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stats Patent Info
Application #
US 20120083470 A1
Publish Date
04/05/2012
Document #
13253861
File Date
10/05/2011
USPTO Class
514 81
Other USPTO Classes
51425303, 51425218
International Class
/
Drawings
0



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