Bruce A Roth

US Patent:

6348487, Feb 19, 2002

Filed:

Oct 27, 2000

Appl. No.:

09/698342

Inventors:

David Thomas Connor - Ann Arbor MI
Shelly Ann Glase - Ann Arbor MI
Terri Stoeber Purchase - Ann Arbor MI
Bruce David Roth - Plymouth MI
Bharat Kalidas Trivedi - Farmington Hills MI

Assignee:

Millennium Pharmaceuticals, Inc. - Cambridge MA

International Classification:

A61K 31405

US Classification:

514415, 548491

Abstract:

Benzimidazole derivatives of Formula I or a pharmaceutically acceptable salt thereof are MCP-1 antagonists and are thus useful in the treatment of inflammation, atherosclerosis, restenosis, and immune disorders wherein A is N or CH; where W, X, Y, and Z can be independently CâR , CâR , CâR , CâR , or N; no more than two of W, X, Y, and Z can be N in any one structure, R , R , R , and R are as define in the specification.

US Patent:

6399612, Jun 4, 2002

Filed:

Oct 23, 2000

Appl. No.:

09/647400

Inventors:

Bruce David Roth - Plymouth MI
Gerald Paul Schielke - Ann Arbor MI
Lary Craswell Walker - Ann Arbor MI
Andrew David White - Pinckney MI

Assignee:

Warner-Lambert Company - Morris Plains NJ

International Classification:

A61K 31495

US Classification:

51425201, 514396, 514403, 514438, 514461, 514549, 514 29, 514 72, 514 73, 514229

Abstract:

Heteroaryl butyric acid compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, osteoporosis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimers disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinsons disease, Huntingtons disease, prion diseases, myasthenia gravis, and Duchennes muscular dystrophy.

US Patent:

6423689, Jul 23, 2002

Filed:

Dec 16, 1998

Appl. No.:

09/212785

Inventors:

Richard John Booth - Ann Arbor MI
Louis Brogley - Santa Cruz CA
Wayne Livingston Cody - Saline MI
David Thomas Connor - Ann Arbor MI
Harriet Wall Hamilton - Chelsea MI
John Xiaoqiang He - Indianapolis IN
Leonard Joseph Lescosky - Ann Arbor MI
Thomas Charles Malone - Canton MI
Laszlo Nadasdi - Oakland CA
Michael Francis Rafferty - Ann Arbor MI
Bruce David Roth - Plymouth MI
Diego F. Silva - Burlingame CA
Yuntao Song - Ann Arbor MI
Balazs G. Szoke - Palo Alto CA
Laszlo Urge - Menlo Park CA

Assignee:

Warner-Lambert Company - Morris Plains NJ
Neurex Corporation - Menlo Park CA

International Classification:

A61K 3805

US Classification:

514 19, 540483, 540607, 544159, 544168, 544391, 546221, 546224, 546233, 5483381, 548538, 548557, 548568, 548953, 548966, 564153, 564155, 564157

Abstract:

The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.

US Patent:

6458781, Oct 1, 2002

Filed:

Oct 25, 1999

Appl. No.:

09/403579

Inventors:

David Thomas Connor - Ann Arbor MI 48105
Thomas Charles Malone - Canton MI 48187
Michael Francis Rafferty - Ann Arbor MI 48105
Bruce David Roth - Plymouth MI 48170
Todd Robert Ryder - Ann Arbor MI 48103
Anthony Denver Sercel - Ann Arbor MI 48105
Yuntao Song - Ann Arbor MI 48108

International Classification:

C07D29520

US Classification:

51421203, 5142392, 5142551, 514453, 514485, 514522, 514524, 514617, 514630, 540529, 544175, 544391, 546226, 549356, 558414, 560 27, 564164, 564168, 564195

Abstract:

The present invention provides compounds that block calcium channels and have the Formula I: The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.

US Patent:

6458806, Oct 1, 2002

Filed:

Aug 12, 1997

Appl. No.:

08/909790

Inventors:

Richard John Booth - Ypsilanti MI
Kenneth Gordon Carson - Needham MA
David Thomas Connor - Ann Arbor MI
Roberta Ellen Glynn - Waltham MA
Bruce David Roth - Plymouth MI
Charles F. Schwender - Glen Gardner NJ
Bharat Kalidas Trivedi - Farmington Hills MI
Paul Charles Unangst - Ann Arbor MI

Assignee:

Millennium Pharmaceuticals, Inc. - Cambridge MA

International Classification:

A61K 31445

US Classification:

514315, 514327, 514316, 514317, 514318, 514326, 514331, 546184, 546186, 546187, 546192

Abstract:

Aryl alkenamides derivatives of Formula I or a pharmaceutically acceptable salt thereof are novel MCP-1 antagonists and are thus useful in the treatment of inflammation, atherosclerosis, restenosis, and immune disorders such as arthritis and transplant rejection where V O,S, NH or a bond; Ar can be unsubstituted or substituted benzimidazole, phenyl, biphenyl, pyridyl, naphthyl, quinoline or isoquinoline. The other meanings for the terms are recited in the specification below.

US Patent:

6458815, Oct 1, 2002

Filed:

Apr 13, 2001

Appl. No.:

09/835239

Inventors:

Helen Tsenwhei Lee - Ann Arbor MI
Randy Ranjee Ramharack - Ann Arbor MI
Bruce David Roth - Plymouth MI
Karen Elaine Sexton - Ann Arbor MI

Assignee:

Warner-Lambert Company - Morris Plains NJ

International Classification:

A61K 314436

US Classification:

514342, 5462804, 546294, 546293

Abstract:

The present invention provides compounds having the Formula I The present invention also provides methods of treating or preventing atherosclerosis, coronary heart disease, and restenosis using the compounds of Formula I, and pharmaceutical compositions comprising the compounds of Formula I.

US Patent:

6506751, Jan 14, 2003

Filed:

Nov 2, 2000

Appl. No.:

09/705219

Inventors:

Stephanie Elizabeth Ault Justus - Livonia MI
Helen Tsenwhei Lee - Ann Arbor MI
Jason Keith Pontrello - Kalamazoo MI
Bruce David Roth - Plymouth MI
Karen Elaine Sexton - Ann Arbor MI
Michael William Wilson - Ann Arbor MI

Assignee:

Millennium Pharmaceuticals, Inc. - Cambridge MA

International Classification:

C07D41306

US Classification:

5142368, 546175, 546187, 546194, 546209, 544133, 548182, 548183, 548186, 548187, 514314, 514316, 514326, 514369

Abstract:

Disclosed are compounds of the Formula I wherein: Z is C or nothing, provided that when Z is nothing, R and R are nothing; A is S, S O or O S O; R and R are independently hydrogen, lower alkyl, halogen, hydroxy or lower alkoxy, (un)substituted aryl, (un)substituted arylalkyl, (un)substituted heteroaryl or(un)substituted heteroarylakyl; R and R independently represent hydrogen, lower alkyl, cycloalkyl, aminoalkyl, mono- or dialkylaminoalkyl, (un)substituted aryl or (un)substituted heteroaryl; R represents a (un)substituted carbocyclic group containing from 3-7 members, up to two of which members are optionally hetero atoms; or R is (CR R )â(CH ) âXR R ; X is S or N; R , R , R , R , and n are as defined in the specification. The compounds are useful in the treatment and prevention of the AIDS virus. Intermediates useful in the preparation of the final products, pharmaceutical compositions containing the final products are also taught.

US Patent:

6534521, Mar 18, 2003

Filed:

Oct 25, 2001

Appl. No.:

10/029786

Inventors:

David Thomas Connor - Ann Arbor MI
Shelly Ann Glase - Ann Arbor MI
Terri Stoeber Purchase - Ann Arbor MI
Bruce David Roth - Plymouth MI
Bharat Kalidas Trivedi - Farmington Hills MI

Assignee:

Millennium Pharmaceuticals, Inc. - Cambridge MA

International Classification:

A61K 31437

US Classification:

514303, 546118

Abstract:

The present invention relates to novel compounds and medical methods of treatment of inflammation, atherosclerosis, restenosis, and immune disorders especially those associated with lymphocyte or monocyte accumulation such as arthritis and transplant rejection. More particularly, the present invention concerns the use of 2-phenyl benzimidazole derivatives.