Kenneth G Rice

US Patent:

6562854, May 13, 2003

Filed:

Jun 4, 2001

Appl. No.:

09/874412

Inventors:

Timothy J. Church - Redwood City CA
Neil Scott Cutshall - San Mateo CA
Anthony R. Gangloff - Pacifica CA
Thomas E. Jenkins - La Honda CA
Martin S. Linsell - Foster City CA
Joane Litvak - Oakland CA
Kenneth D. Rice - Sausalito CA
Jeffrey R. Spencer - San Mateo CA
Vivian R. Wang - Redwood City CA

Assignee:

Axys Pharmaceuticals, Inc. - South San Francisco CA

International Classification:

A61K 314184

US Classification:

514394, 5483057

Abstract:

Novel compounds, compositions and methods effective for the prevention and treatment of mast-cell mediated inflammatory disorders are described. The compounds, compositions and methods are effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis, as well as other types of immunomediated inflammatory disorders, such as rheumatoid arthritis, conjunctivitis and inflammatory bowel disease, various dermatological conditions, as well as certain viral conditions. The compounds comprise potent and selective inhibitors of the mast cell protease tryptase. The compositions for treating these conditions include oral, inhalant, topical and parenteral preparations as well as devices comprising such preparations.

US Patent:

7576074, Aug 18, 2009

Filed:

Jul 14, 2003

Appl. No.:

10/522004

Inventors:

Kenneth D. Rice - Mill Valley CA, US
Neel K. Anand - Burlingame CA, US
Joerg Bussenius - Foster City CA, US
Abigail R. Kennedy - San Leandro CA, US
Angie I. Kim - San Mateo CA, US
Csaba J. Peto - Alameda CA, US
Tsze H. Tsang - El Cerrito CA, US

International Classification:

A01N 43/00
A61K 31/33
A01N 43/54
A61K 31/517
C07D 401/00
C07D 403/00
C07D 413/00
C07D 417/00
C07D 419/00
C07D 239/72

US Classification:

514183, 5142662, 5142663, 5142664, 544284, 544287, 544293

Abstract:

The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i. e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.

US Patent:

7704995, Apr 27, 2010

Filed:

May 2, 2003

Appl. No.:

10/513081

Inventors:

Chris A. Buhr - Redwood City CA, US
Sunghoon Ma - Foster City CA, US
Zerom Tesfai - Castro Valley CA, US
Longcheng Wang - Palo Alto CA, US
Erick Wang Co - Redwood City CA, US
Sergey Epshteyn - Fremont CA, US
Abigail R Kennedy - San Leandro CA, US
Baili Chen - Palo Alto CA, US
Larisa Dubenko - San Francisco CA, US
Neel Kumar Anand - San Mateo CA, US
Tsze H. Tsang - El Cerrito CA, US
John M. Nuss - Danville CA, US
Csaba J Peto - Alameda CA, US
Kenneth D. Rice - Mill Valley CA, US
Mohamed Abdulkader Ibrahim - Mountain View CA, US
Kevin Luke Schnepp - Elk Grove CA, US
Xian Shi - San Francisco CA, US
James William Leahy - San Leandro CA, US
Jeff Chen - San Francisco CA, US
Lisa Esther Dalrymple - San Francisco CA, US
Timothy Patrick Forsyth - San Mateo CA, US
Tai Phat Huynh - Oakland CA, US
Grace Mann - Brisbane CA, US
Larry Wayne Mann - Redwood City CA, US
Craig Stacy Takeuchi - Burlingame CA, US
Peter Lamb - Oakland CA, US
David J. Matthews - San Francisco CA, US
Nicole Miller - San Francisco CA, US

Assignee:

Exelixis, Inc. - South San Francisco CA

International Classification:

C07D 279/16
C07D 279/12
C07D 417/12
C07D 265/36
C07D 413/12
C07D 403/12
C07D 401/12
C07D 405/12
C07D 409/12
C07D 411/12
C07D 419/12
C07D 241/18
C07D 241/20
A61K 31/55
A61K 31/497
A61K 31/5355
A61K 31/541
C07D 305/12
C07D 307/79
A61K 31/44
A61P 35/00

US Classification:

51421705, 51425211, 51425213, 51425505, 51425506, 5142358, 5142278, 5142305, 514352, 544405, 544407, 544295, 544120, 544 586, 544 60, 544105, 540598, 549310, 546309, 546311

Abstract:

This invention relates to compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion, and to pharmaceutical compositions containing such compounds. Even more specifically, the invention relates to compounds that inhibit, regulate and/or modulate kinases, particularly Checkpoint Kinases, even more particularly Checkpoint Kinase 1, or Chk1. Methods of therapeutically or prophylactically using the compounds and compositions to treat kinase-dependent diseases and conditions are also an aspect of the invention, and include methods of treating cancer, as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, by administering effective amounts of such compounds.

US Patent:

7803839, Sep 28, 2010

Filed:

Oct 5, 2006

Appl. No.:

11/995928

Inventors:

Naing Aay - San Mateo CA, US
Neel Kumar Anand - Burlingame CA, US
Charles M. Blazey - San Francisco CA, US
Owen Joseph Bowles - Pacifica CA, US
Joerg Bussenius - Foster City CA, US
Simona Costanzo - Los Altos CA, US
Jeffry Kimo Curtis - San Anselmo CA, US
Steven Charles DeFina - Burlingame CA, US
Larisa Dubenko - San Francisco CA, US
Anagha Abhijit Joshi - Fremont CA, US
Abigail R. Kennedy - Oakland CA, US
Angie Inyoung Kim - San Mateo CA, US
Elena S. Koltun - Foster City CA, US
Jean-Claire Limun Manalo - Daly City CA, US
Csaba J. Peto - Alameda CA, US
Kenneth D. Rice - San Rafael CA, US
Tsze H. Tsang - El Cerrito CA, US

Assignee:

Exelixis, Inc. - South San Francisco CA

International Classification:

A61K 31/27
C07D 205/00

US Classification:

514477, 548950

Abstract:

Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.

US Patent:

7846959, Dec 7, 2010

Filed:

Mar 25, 2005

Appl. No.:

11/568789

Inventors:

Neel Kumar Anand - Burlingame CA, US
Charles M. Blazey - San Francisco CA, US
Owen Joseph Bowles - Pacifica CA, US
Joerg Bussenius - Foster City CA, US
Simona Costanzo - Los Altos CA, US
Jeffry Kimo Curtis - San Anselmo CA, US
Larisa Dubenko - San Francisco CA, US
Abigail R. Kennedy - Oakland CA, US
Steven Charles Defina - Burlingame CA, US
Angie I. Kim - San Mateo CA, US
Jean-Claire L. Manalo - Daly City CA, US
Csaba J. Peto - Alameda CA, US
Kenneth D. Rice - San Rafael CA, US
Tsze H. Tsang - El Cerrito CA, US
Anagha Abhijit Joshi - Fremont CA, US

Assignee:

Exelixis, Inc. - South San Francisco CA

International Classification:

C07D 231/02

US Classification:

514405, 514403, 548356, 5483601, 5483611

Abstract:

The present invention relates to compounds of the Formula I, wherein G, A, X1, X2, X3, Z, E, Y, and X are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Raf. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.

US Patent:

7872014, Jan 18, 2011

Filed:

Jul 23, 2004

Appl. No.:

10/565657

Inventors:

Neel Kumar Anand - Burlingame CA, US
Charles M. Blazey - San Francisco CA, US
Owen Joseph Bowles - Pacifica CA, US
Joerg Bussenius - Foster City CA, US
Simona Costanzo - Los Altos CA, US
Jeffry Kimo Curtis - San Anselmo CA, US
Larisa Dubenko - San Francisco CA, US
Abigail R. Kennedy - Oakland CA, US
Richard G. Khoury - Redwood City CA, US
Angie I. Kim - San Mateo CA, US
Jean-Claire L. Manalo - Daly City CA, US
Csaba J. Peto - Alameda CA, US
Kenneth D. Rice - San Rafael CA, US
Tsze H. Tsang - El Cerrito CA, US

Assignee:

Exelixis, Inc. - South San Francisco CA

International Classification:

C07D 471/02
A61K 31/4745

US Classification:

514291, 514292, 546 82

Abstract:

The present invention comprises compounds and pharmaceutical compositions comprising the compounds that are inhibitors of ALK. The invention also comprises methods of using the compounds and compositions to treat diseases mediated by ALK, including diseases such as cancer, immunological disorders, cardiovascular diseases, and other degenerative disorders.

US Patent:

7915250, Mar 29, 2011

Filed:

May 5, 2010

Appl. No.:

12/774544

Inventors:

Naing Aay - San Mateo CA, US
Neel Kumar Anand - Burlingame CA, US
Charles M. Blazey - San Francisco CA, US
Owen Joseph Bowles - Pacifica CA, US
Joerg Bussenius - Foster City CA, US
Simona Costanzo - Los Altos CA, US
Jeffry Kimo Curtis - San Anselmo CA, US
Steven Charles DeFina - Burlingame CA, US
Larisa Dubenko - San Francisco CA, US
Anagha Abhijit Joshi - Fremont CA, US
Abigail R. Kennedy - Oakland CA, US
Angie Inyoung Kim - San Mateo CA, US
Elena S. Koltun - Foster City CA, US
Jean-Claire Limun Manalo - Daly City CA, US
Csaba J. Peto - Alameda CA, US
Kenneth D. Rice - San Rafael CA, US
Tsze H. Tsang - El Cerrito CA, US

Assignee:

Exelixis, Inc. - South San Francisco CA

International Classification:

A61K 31/397
A61K 31/50
A61K 31/505
A61K 31/4523
A61K 31/4178

US Classification:

51421018, 514248, 51425203, 51425205, 514256, 514318, 514403, 544235, 544242, 544333, 544405, 546208, 546210, 5462681, 5462684, 5462754

Abstract:

Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.

US Patent:

8012956, Sep 6, 2011

Filed:

Oct 27, 2008

Appl. No.:

12/290159

Inventors:

Kenneth D. Rice - San Rafael CA, US
Naing Aay - San Mateo CA, US
Neel Kumar Anand - Burlingame CA, US
Arlyn Arcalas - South San Francisco CA, US
Charles M. Blazey - San Francisco CA, US
Owen Joseph Bowles - Pacifica CA, US
Chris A. Buhr - Redwood City CA, US
Joerg Bussenius - Foster City CA, US
Simona Costanzo - Los Altos CA, US
Jeffrey Kimo Curtis - San Anselmo CA, US
Steven Charles Defina - Burlingame CA, US
Larisa Dubenko - San Francisco CA, US
Abigail R. Kennedy - Oakland CA, US
Angie Inyoung Kim - San Mateo CA, US
Katherine Lara - San Mateo CA, US
Sunghoon Ma - Foster City CA, US
Jean-Claire Limun Manalo - Daly City CA, US
Csaba J. Peto - Alameda CA, US
Tsze H. Tsang - El Cerrito CA, US
Longcheng Wang - Palo Alto CA, US

Assignee:

Exelixis, Inc. - South San Francisco CA

International Classification:

A61K 31/46
A61K 31/5377
A61K 31/496
A61K 31/497
C07D 451/04

US Classification:

51421021, 5142332, 51425304, 51425505, 514304, 546124, 546125, 544127, 544362, 544405

Abstract:

A compound according to Formula I or II:.