Frances Mccray Nelson

US Patent:

6465508, Oct 15, 2002

Filed:

Feb 23, 2001

Appl. No.:

09/792798

Inventors:

Frances Christy Nelson - Wyckoff NJ
Arie Zask - New York NY
James Ming Chen - San Ramon CA
Dominick Mobilio - Warren NJ
Ramaswamy Nilakantan - Closter NJ

Assignee:

Wyeth - Madison NJ

International Classification:

A61K 3138

US Classification:

514443, 514469, 514470, 549 49, 549 51, 549 52, 549 53, 549 57, 549 58, 549466, 549467, 549468, 549470, 549471

Abstract:

Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs.

US Patent:

6825352, Nov 30, 2004

Filed:

Aug 30, 2002

Appl. No.:

10/231584

Inventors:

Frances Christy Nelson - Wyckoff NJ
Arie Zask - New York NY
James Ming Chen - San Ramon CA
Dominick Mobilio - Warren NJ
Ramaswamy Nilakantan - Closter NJ

Assignee:

Wyeth - Madison NJ

International Classification:

C07D21516

US Classification:

546153, 546155, 546156, 546157, 546159, 546162, 546167, 546168, 546170, 548483, 548484, 548486, 548492, 548494, 548503, 548509, 548511

Abstract:

Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs.

US Patent:

7470794, Dec 30, 2008

Filed:

Nov 4, 2004

Appl. No.:

10/980990

Inventors:

Frances Christy Nelson - Wyckoff NJ, US
Arie Zask - New York NY, US
James Ming Chen - San Ramon CA, US
Dominick Mobilio - Warren NJ, US
Ramaswamy Nilakantan - Closter NJ, US

Assignee:

Wyeth - Madison NJ

International Classification:

C07D 263/02

US Classification:

548215

Abstract:

Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs.

US Patent:

20010051614, Dec 13, 2001

Filed:

Nov 29, 2000

Appl. No.:

09/725707

Inventors:

Jeremy Levin - Nanuet NY, US
Frances Nelson - Wyckoff NJ, US

International Classification:

A61K031/675
A61K031/54
A61K031/5375
A61K031/53
A61K031/495

US Classification:

514/079000, 514/085000, 514/089000, 514/091000, 514/231200, 514/227500, 514/241000, 514/247000, 514/255010, 514/350000, 514/370000, 514/377000, 514/398000, 514/423000

Abstract:

The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stromelysins and collagenases) and TNF- converting enzyme (TACE, tumor necrosis factor- converting enzyme) which are useful for the treatment of diseases in which these enzymes are implicated such as arthritis, tumor growth and metastasis, angiogenesis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, proteinuria, aneurysmal aortic disease, degenerative cartilage loss following traumatic joint injury, demyelinating diseases of the nervous system, graft rejection, cachexia, anorexia, inflammation, fever, insulin resistance, septic shock, congestive heart failure, inflammatory disease of the central nervous system, inflammatory bowel disease, HIV infection, age related macular degeneration, diabetic retinopathy, proliferative vitreoretinopathy, retinopathy of prematurity, ocular inflammation, keratoconus, Sjogren's syndrome, myopia, ocular tumors, ocular angiogenesis/neovascularization. The TACE and MMP inhibiting ortho-sulfonamido aryl hydroxamic acids of the present invention are represented by the formula where the hydroxamic acid moiety and the sulfonamido moiety are bonded to adjacent carbons on group A where A is defined as: a 5-6 membered heteroaryl having from 1 to 3 heteroatoms independently selected from N, O, and S and optionally substituted by R, Rand R; and Z, R, R, R, R, R, R, R, Rand Rare described in the specification, and the pharmaceutically acceptable salts thereof and the optical isomers and diastereomers thereof.

US Patent:

6162814, Dec 19, 2000

Filed:

Jun 11, 1999

Appl. No.:

9/330877

Inventors:

Jeremy Ian Levin - Nanuet NY
Frances Christy Nelson - Wyckoff NJ

Assignee:

American Cyanamid Company - Madison NJ

International Classification:

C07D40912
C07D33338
A61K 31381

US Classification:

514336

Abstract:

The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e. g. gelatinases, stromelysins and collagenases) and TNF-. alpha. converting enzyme (TACE, tumor necrosis factor-. alpha. converting enzyme) which are useful for the treatment of diseases in which these enzymes are implicated such as arthritis, tumor growth and metastasis, angiogenesis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, proteinuria, aneurysmal aortic disease, degenerative cartilage loss following traumatic joint injury, demyelinating diseases of the nervous system, graft rejection, cachexia, anorexia, inflammation, fever, insulin resistance, septic shock, congestive heart failure, inflammatory disease of the central nervous system, inflammatory bowel disease, HIV infection, age related macular degeneration, diabetic retinopathy, proliferative vitreoretinopathy, retinopathy of prematurity, ocular inflammation, keratoconus, Sjogren's syndrome, myopia, ocular tumors, ocular angiogenesis/neovascularization. The TACE and MMP inhibiting ortho-sulfonamide aryl hydroxamic acids of the present invention are represented by the formula ##STR1## where the hydroxamic acid moiety and the sulfanamido moiety are bonded to adjacent carbons on group A where A is defined as: a 5-6 membered heteroaryl having from 1 to 3 heteroatoms independently selected from N, O, and S and optionally substituted by R. sup. 1, R. sup. 2 and R. sup. 3 ; and Z, R. sup. 1, R. sup. 2, R. sup. 3, R. sup. 4, R. sup. 5, R. sup. 6, R. sup. 7, R. sup. 8 and R. sup.

US Patent:

59624817, Oct 5, 1999

Filed:

Oct 6, 1997

Appl. No.:

8/944400

Inventors:

Jeremy Ian Levin - Nanuet NY
Frances Christy Nelson - Wyckoff NJ

Assignee:

American Cyanamid Company - Madison NJ

International Classification:

C07D21378
A61K 3144

US Classification:

514352

Abstract:

The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e. g. gelatinases, stromelysins and collagenases) and TNF-. alpha. converting enzyme (TACE, tumor necrosis factor-. alpha. converting enzyme) which are useful for the treatment of diseases in which these enzymes are implicated such as arthritis, tumor growth and metastasis, angiogenesis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, proteinuria, aneurysmal aortic disease, degenerative cartilage loss following traumatic joint injury, demyelinating diseases of the nervous system, graft rejection, cachexia, anorexia, inflammation, fever, insulin resistance, septic shock, congestive heart failure, inflammatory disease of the central nervous system, inflammatory bowel disease, HIV infection, age related macular degeneration, diabetic retinopathy, proliferative vitreoretinopathy, retinopathy of prematurity, ocular inflammation, keratoconus, Sjogren's syndrome, myopia, ocular tumors, ocular angiogenesis/neovascularization. The TACE and MMP inhibiting ortho-sulfonamido aryl hydroxamic acids of the present invention are represented by the formula ##STR1## where the hydroxamic acid moiety and the sulfonamido moiety are bonded to adjacent carbons on group A where A is defined as: a 5-6 membered heteroaryl having from 1 to 3 heteroatoms independently selected from N, O, and S and optionally substituted by R. sup. 1, R. sup. 2 and R. sup. 3 ; and Z, R. sup. 1, R. sup. 2, R. sup. 3, R. sup. 4, R. sup. 5, R. sup. 6, R. sup. 7, R. sup. 8 and R. sup.

US Patent:

61977950, Mar 6, 2001

Filed:

Jun 11, 1999

Appl. No.:

9/330717

Inventors:

Jeremy Ian Levin - Nanuet NY
Frances Christy Nelson - Wyckoff NJ

Assignee:

American Cyanamid Company - Madison NJ

International Classification:

C07D21378
A61K 3144

US Classification:

514352

Abstract:

The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e. g. gelatinases, stromelysins and collagenases) and TNF-. alpha. converting enzyme (TACE, tumor necrosis factor-. alpha. converting enzyme) which are useful for the treatment of diseases in which these enzymes are implicated such as arhritis, tumor growth and metastasis, angiogenesis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, proteinuria, aneurysmal aortic disease, degenerative cartilage loss following traumatic joint injury, demyelinating diseases of the nervous system, graft rejection, cachexia, anorexia, inflammation, fever, insulin resistance, septic shock, congestive heart failure, inflammatory disease of the central nervous system, inflammatory bowel disease, HIV infection, age related macular degeneration, diabetic retinopathy, proliferative vitreoretinopathy, retinopathy of prematurity, ocular inflammation, keratoconus, Sjogren's syndrome, myopia, ocular tumors, ocular angiogenesis/neovascularization. The TACE and MMP inhibiting ortho-sulfonamido aryl hydroxamic acids of the present invention are represented by the formula ##STR1## where the hydroxamic acid moiety and the sulfonamido moiety are bonded to adjacent carbons on group A where A is defined as: a 5-6 membered heteroaryl having from 1 to 3 heteroatoms independently selected from N, O, and S and optionally substituted by R. sup. 1, R. sup. 2 and R. sup. 3 ; and Z, R. sup. 1, R. sup. 2, R. sup. 3, R. sup. 4, R. sup. 5, R. sup. 6, R. sup. 7, R. sup. 8 and R. sup.

US Patent:

59290978, Jul 27, 1999

Filed:

Oct 6, 1997

Appl. No.:

8/944593

Inventors:

Jeremy Ian Levin - Nanuet NY
Mila T. Du - Suffern NY
Aranapakam Mudumbai Venkatesan - Rego Park NY
Frances Christy Nelson - Wyckoff NJ
Arie Zask - New York NY
Yansong Gu - Pearl River NY

Assignee:

American Cyanamid Company - Madison NJ

International Classification:

C07D21302
C07C31108
A61K 3118
A61K 3144

US Classification:

514351

Abstract:

The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e. g. gelatinases, stromelysins and collagenases) and TNF-. alpha. converting enzyme (TACE, tumor necrosis factor-. alpha. converting enzyme) which are useful for the treatment of diseases in which these enzymes are implicated such as arthritis, tumor growth and metastasis, angiogenesis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, proteinuria, aneurysmal aortic disease, degenerative cartilage loss following traumatic joint injury, demyelinating diseases of the nervous system, graft rejection, cachexia, anorexia, inflammation, fever, insulin resistance, septic shock, congestive heart failure, inflammatory disease of the central nervous system, inflammatory bowel disease, HIV infection, age related macular degeneration, diabetic retinopathy, proliferative vitreoretinopathy, retinopathy of prematurity, ocular inflammation, keratoconus, Sjogren's syndrome, myopia, ocular tumors, ocular angiogenesis/neovascularization. The TACE and MMP inhibiting ortho-sulfonamido aryl hydroxamic acids of the present invention are represented by the formula ##STR1## where the hydroxamic acid moiety and the sulfonamido moiety are bonded to adjacent carbons on group A.