Frances J Nelson

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:

20020188132, Dec 12, 2002

Filed:

Dec 4, 2000

Appl. No.:

09/999908

Inventors:

Jeremy Levin - New City NY, US
James Chen - Bedminster NJ, US
Frances Nelson - Wyckoff NJ, US

International Classification:

C07F009/576
C07F009/28
C07D277/38

US Classification:

546/309000, 546/022000, 548/112000, 548/190000, 548/253000, 548/326500, 562/622000

Abstract:

Compounds of the formula: are useful in treating disease conditions mediated by TNF- such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.

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:

62009966, Mar 13, 2001

Filed:

Jan 27, 2000

Appl. No.:

9/492976

Inventors:

Jeremy I. Levin - New City NY
James M. Chen - Bedminster NJ
Frances C. Nelson - Wyckoff NJ

Assignee:

American Cyanamid Company - Madison NJ

International Classification:

A61K 3144
C07D21372
C07D21172
C07D21370
C07D21184

US Classification:

514347

Abstract:

Compounds of the formula: ##STR1## are useful in treating disease conditions mediated by TNF-. alpha. such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.

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.

Address:

217 Morgan Dr APT B, Morgantown, WV 26505

Phone:

3045994937

VIN:

4A3AB36F77E033759

Make:

MITSUBISHI

Model:

GALANT

Year:

2007