Michael W Su

US Patent:

6423840, Jul 23, 2002

Filed:

Jan 31, 2001

Appl. No.:

09/773477

Inventors:

Mark James Batchelor - Cumnor Hill, GB
David Bebbington - Pewsey, GB
Guy W. Bemis - Arlington MA
Wolf Herman Fridman - Paris, FR
Roger John Gillespie - Malmesbury, GB
Julian M. C. Golec - Swindon, GB
Yong Gu - Brookline MA
David J. Lauffer - Stow MA
David J. Livingston - Newtonville MA
Saroop Singh Matharu - Cricklade, GB
Michael D. Mullican - Needham MA
Mark A. Murcko - Holliston MA
Robert Murdoch - Highworth, GB
Philip Nyce - Milbury MA
Andrea L. C. Robidoux - Andover MA
Michael Su - Newton MA
M. Woods Wannamaker - Stow MA
Keith P. Wilson - Hopkinton MA
Robert E. Zelle - Stow MA

Assignee:

Vertex Pharmaceuticals Incorporated - Cambridge MA

International Classification:

C07D47104

US Classification:

540460, 540461, 540490, 540500, 540521, 540523

Abstract:

The present invention relates to novel classes of compounds which are inhibitors of interleukin-1 converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN--mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN--mediated diseases and decreasing IGIF and IFN- production using the compounds and compositions of this invention. This invention also relates to methods for preparing N-acylamino compounds.

US Patent:

6608060, Aug 19, 2003

Filed:

Jun 14, 1999

Appl. No.:

09/336266

Inventors:

Guy W. Bemis - Arlington MA
Francesco Gerald Salituro - Marlborough MA
John Patrick Duffy - Westborough MA
John E. Cochran - Lowell MA
Edmund Martin Harrington - Cambridge MA
Mark A. Murko - Holliston MA
Keith P. Wilson - Hopkinton MA
Michael Su - Newton MA
Vincent P. Galullo - Watertown MA

Assignee:

Vertex Pharmaceuticals Incorporated - Cambridge MA

International Classification:

C07D48704

US Classification:

5142355, 5142372, 51425312, 51425313, 514338, 514347, 514349, 514350, 514351, 514352, 514353, 514354, 514357, 544124, 544360, 544365, 546261, 546262, 546263, 546264, 5462764, 5462804, 5462837, 5462811, 5462841, 546297, 546298, 546300, 546301, 546333, 546334, 546335, 546336

Abstract:

The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

US Patent:

6849716, Feb 1, 2005

Filed:

Aug 18, 2000

Appl. No.:

09/642749

Inventors:

Michael Shin-San Su - Newton MA, US
Ted Fox - Maynard MA, US
Keith Philip Wilson - Boston MA, US
Ursula A. Germann - Newton MA, US

Assignee:

Vertex Pharmaceuticals Incorporated - Cambridge MA

International Classification:

C12P 2104

US Classification:

530350, 530300, 435 691, 435 711

Abstract:

The invention relates to methods for designing inhibitors of serine/threonine kinases and tyrosine kinases, particularly MAP kinases, through the use of ATP-binding site mutants of those kinases. The methods of this invention take advantage of the fact that the mutant kinases are capable of binding inhibitory compounds of other kinases with greater affinity than the corresponding wild-type kinase. The invention further relates to the mutant kinases themselves and crystallizable co-complexes of the mutant kinase and the inhibitory compound.

US Patent:

7205305, Apr 17, 2007

Filed:

Jul 17, 2003

Appl. No.:

10/622320

Inventors:

Guy W Bemis - Arlington MA, US
Francesco G Salituro - Marlborough MA, US
John P Duffy - Northborough MA, US
John E Cochran - North Andover MA, US
Edmund M Harrington - South Boston MA, US
Mark A Murcko - Holliston MA, US
Keith P Wilson - Hopkinton MA, US
Michael Su - Newton MA, US
Vincent P Galullo - Watertown MA, US

Assignee:

Vertex Pharmaceuticals Incorporated - Cambridge MA

International Classification:

C07D 213/02
C07D 213/89
A61K 31/44

US Classification:

51425301, 514336, 514337, 514338, 514343, 514357, 544360, 5462764, 5462804, 5462811, 5462834, 5462837, 5462841, 546333

Abstract:

The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

US Patent:

7365072, Apr 29, 2008

Filed:

Dec 8, 2005

Appl. No.:

11/298324

Inventors:

Guy W Bemis - Arlington MA, US
Francesco G Salituro - Marlborough MA, US
John P Duffy - Northborough MA, US
John E Cochran - North Andover MA, US
Edmund M Harrington - South Boston MA, US
Mark A Murcko - Holliston MA, US
Keith P Wilson - Hopkinton MA, US
Michael Su - Newton MA, US
Vincent P Galullo - Watertown MA, US

Assignee:

Vertex Pharmaceuticals Incorporated - Cambridge MA

International Classification:

C07D 487/04
A61K 31/5025

US Classification:

514248, 544236

Abstract:

The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

US Patent:

7383135, Jun 3, 2008

Filed:

Nov 3, 2000

Appl. No.:

09/706128

Inventors:

Xiaoling Xie - Cambridge MA, US
Yong Gu - Brookline MA, US
William Markland - Milford MA, US
Michael S Su - Newton MA, US
Paul R Caron - Malden MA, US
Edward Fox - Maynard MA, US
Keith P Wilson - Hopkinton MA, US

Assignee:

Vertex Pharmaceuticals Incorporated - Cambridge MA

International Classification:

G01N 33/48
G01N 33/50
G06F 19/00
C07K 17/00

US Classification:

702 27, 530350, 435 71, 702 19

Abstract:

The present invention relates to a data storage medium encoded with the corresponding structure coordinates of molecules and molecular complexes which comprise the active site-binding pockets of JNK3. A computer comprising such data storage material is capable of displaying such molecules and molecular complexes, or their structural homologues, as a graphical three-dimensional representation on a computer screen. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen and design compounds, including inhibitory compounds, that bind to JNK3 or homologues thereof. This invention also relates to molecules and molecular complexes which comprise the active site binding pockets of JNK3 or close structural homologues of the active site binding pockets.

US Patent:

7790713, Sep 7, 2010

Filed:

Jan 18, 2007

Appl. No.:

11/655938

Inventors:

Mark James Batchelor - Cumnor Hill, GB
David Bebbington - Pewsey, GB
Guy W. Bemis - Arlington MA, US
Wolf Herman Fridman - Paris, FR
Roger John Gillespie - Nr. Malmesbury, GB
Julian M. C. Golec - Swindon, GB
Yong Gu - Brookline MA, US
David J. Lauffer - Stow MA, US
David J. Livingston - Newtonville MA, US
Saroop Singh Matharu - Cricklade, GB
Michael D. Mullican - Needham MA, US
Mark A. Murcko - Holliston MA, US
Robert Murdoch - Highworth, GB
Philip Nyce - Milbury MA, US
Andrea L. C. Robidoux - Andover MA, US
Michael Su - Newton MA, US
M. Woods Wannamaker - Stow MA, US
Keith P. Wilson - Hopkinton MA, US
Robert E. Zelle - Stow MA, US

Assignee:

Vertex Pharmaceuticals Incorporated - Cambridge MA

International Classification:

C07D 243/12
A61K 31/55
A61P 29/00

US Classification:

514221, 540517

Abstract:

The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-γ-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-γ-mediated diseases and decreasing IGIF and IFN-γ production using the compounds and compositions of this invention. This invention also relates to methods for preparing-N-acylamino compounds.

US Patent:

7951809, May 31, 2011

Filed:

Apr 3, 2008

Appl. No.:

12/062495

Inventors:

Guy W. Bemis - Arlington MA, US
Francesco G. Salituro - Marlborough MA, US
John P. Duffy - Northborough MA, US
John E. Cochran - North Andover MA, US
Edmund M. Harrington - South Boston MA, US
Mark A. Murcko - Holliston MA, US
Keith P. Wilson - Hopkinton MA, US
Michael Su - Newton MA, US
Vincent P. Galullo - Watertown MA, US

Assignee:

Vertex Pharmaceuticals Incorporated - Cambridge MA

International Classification:

C07D 239/70
A61K 31/519

US Classification:

5142594, 51425941, 544282

Abstract:

The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.