Follow us on Twitter
twitter icon@FreshPatents

Browse patents:
Next
Prev

Inhibitors of tyrosine kinases and uses thereof / Pharmacyclics, Inc.




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


USPTO Applicaton #: #20120083470
Inventors: Orion D. Jankowski, James T. Palmer, Lee Honigberg


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

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

- Top of Page


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

- Top of Page


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

- Top of Page


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




← Previous       Next →
Advertise on FreshPatents.com - Rates & Info


You can also Monitor Keywords and Search for tracking patents relating to this Inhibitors of tyrosine kinases and uses thereof patent application.

###


Browse recent Pharmacyclics, Inc. patents

Keyword Monitor How KEYWORD MONITOR works... a FREE service from FreshPatents
1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored.
3. Each week you receive an email with patent applications related to your keywords.  
Start now! - Receive info on patent apps like Inhibitors of tyrosine kinases and uses thereof or other areas of interest.
###


Previous Patent Application:
Inhibitors of arginase and their therapeutic applications
Next Patent Application:
Novel compounds, pharmaceutical compositions containing same, methods of use for same, and methods for preparing same
Industry Class:
Drug, bio-affecting and body treating compositions
Thank you for viewing the Inhibitors of tyrosine kinases and uses thereof patent info.
- - -

Results in 0.19309 seconds


Other interesting Freshpatents.com categories:
Novartis , Apple , Philips , Toyota ,

###

Data source: patent applications published in the public domain by the United States Patent and Trademark Office (USPTO). Information published here is for research/educational purposes only. FreshPatents is not affiliated with the USPTO, assignee companies, inventors, law firms or other assignees. Patent applications, documents and images may contain trademarks of the respective companies/authors. FreshPatents is not responsible for the accuracy, validity or otherwise contents of these public document patent application filings. When possible a complete PDF is provided, however, in some cases the presented document/images is an abstract or sampling of the full patent application for display purposes. FreshPatents.com Terms/Support
-g2-0.183

66.232.115.224
Browse patents:
Next
Prev

stats Patent Info
Application #
US 20120083470 A1
Publish Date
04/05/2012
Document #
File Date
12/31/1969
USPTO Class
Other USPTO Classes
International Class
/
Drawings
0




Follow us on Twitter
twitter icon@FreshPatents

Pharmacyclics, Inc.


Browse recent Pharmacyclics, Inc. patents



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  

Browse patents:
Next
Prev
20120405|20120083470|inhibitors of tyrosine kinases and uses thereof|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 |Pharmacyclics-Inc
';