Daniel H Rich

US Patent:

6947847, Sep 20, 2005

Filed:

Mar 8, 2002

Appl. No.:

10/094049

Inventors:

Matthew G. Bursavich - Madison WI, US
Daniel H. Rich - Madison WI, US

Assignee:

Wisconsin Alumni Research Foundation - Madison WI

International Classification:

G01N033/48
G06G007/60

US Classification:

702 27, 703 11

Abstract:

Disclosed is are methods of generating chemical structures of putative non-peptide inhibitors of biologically-active receptors. The method includes constructing a model of a receptor-ligand complex using empirical three-dimensional data of the receptor-ligand complex. The conformation of the binding site between the receptor and the ligand is then altered to yield novel conformations not exhibited in either the native receptor or the bound receptor. These conformations are then used to generate models of non-peptide chemical structures that are complementary in structure to the altered conformations of the binding site. In this fashion, chemical structures of putative non-peptide inhibitors of the altered conformation are revealed.

US Patent:

7338965, Mar 4, 2008

Filed:

Nov 19, 2002

Appl. No.:

10/299746

Inventors:

Joseph B. Moon - Kalamazoo MI, US
Shon R. Pulley - Hickory Corners MI, US
Daniel H. Rich - Madison WI, US
David L. Brown - Chesterfield MO, US
Barbara Jagodzinska - Redwood City CA, US
Varghese John - San Francisco CA, US
John Jacobs - Kalamazoo MI, US

Assignee:

Pharmacia & Upjohn Company - Kalamazoo MI
Elan Pharmaceuticals, Inc. - South San Francisco CA

International Classification:

A61K 31/445
C07D 211/42

US Classification:

514327, 546222, 546217, 546221

Abstract:

The invention relates to substituted piperidine, piperazine, morpholine and thiomorpholine compounds useful in the treatment of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer's sufferers. One embodiment of the invention relates to compounds having the structure:.

US Patent:

63164051, Nov 13, 2001

Filed:

Feb 22, 1999

Appl. No.:

9/242724

Inventors:

Daniel H. Rich - Madison WI
Michael E. Solomon - Arlington MA

Assignee:

Wisconsin Alumni Research Foundation - Madison WI

International Classification:

A61K 3800
A61K 3812
C07K 1600
C07K 1700

US Classification:

514 9

Abstract:

Disclosed are conjugates of A. beta. -binding peptides and CsA analogs and conjugates of A. beta. -binding peptides and FK506 Binding Peptide inhibitors. These conjugates chemically induce dimerization of either cyclophilin or FK506 Binding Peptide with A. beta. peptide, a major component of amyloid plaques found in neurological disorders such as Alzheimer's disease, multiple sclerosis, and amyotrophic lateral sclerosis. The conjugates are useful in the treatment of neurological diseases involving the formation of amyloid plaques because they inhibit and/or prevent the aggregation and deposition of A. beta. peptide into plaques.

US Patent:

40627462, Dec 13, 1977

Filed:

May 7, 1975

Appl. No.:

5/575478

Inventors:

Daniel H. Rich - Madison WI
Sweet K. Gurwara - Williamsville NY

Assignee:

Wisconsin Alumni Research Foundation - Madison WI

International Classification:

C08L 8100

US Classification:

20415912

Abstract:

The invention is addressed to the preparation of 3-nitro-4-bromomethyl benzoic acid, as a new compound from which 3-nitro-4-bromomethyl benzoyl amide polystyrene resin can be prepared for solid synthesis of protected peptide acids and amides and separation thereof without cleavage of acid labile protecting groups or decomposition of aromatic acid groups and from which purified polypeptides can be formed.

US Patent:

53806565, Jan 10, 1995

Filed:

Dec 13, 1991

Appl. No.:

7/768325

Inventors:

Alan J. Barrett - Cambridgeshire, GB
David J. Buttle - Cambridgeshire, GB
Daniel H. Rich - Madison WI

Assignee:

The Boots Company PLC - Nottingham

International Classification:

C12N 950
A61K 3754

US Classification:

435219

Abstract:

A method of purifying chymopapain by active site directed affinity chromatography using inhibitory dipeptides as affinity ligands is presented. The inhibitory dipeptides have C-terminal aldehyde derivatives of phenylalanine selected from the group consisting of the semicarbazone, the methoxyimine and the oxime. The purified chymopapain has a specific activity against BAPNA (1 mM) at 40. degree. C. and pH 6. 8 of between 3000 and 4500 units per mg and contains less than 0. 2% each of papaya proteinase III (PPIII), papain and papaya proteinase IV (PPIV). The use of purified chymopapain in pharmaceutical compositions for the treatment of damaged mammalian spinal discs is also disclosed.

US Patent:

41896050, Feb 19, 1980

Filed:

Nov 10, 1977

Appl. No.:

5/850141

Inventors:

Daniel H. Rich - Madison WI
Sweet K. Gurwara - Williamsville NY

Assignee:

Wisconsin Alumni Research Foundation - Madison WI

International Classification:

C07C 7946

US Classification:

562438

Abstract:

The invention is addressed to the preparation of 3-nitro-4-bromomethyl benzoic acid, as a new compound from which 3-nitro-4-bromomethyl benzoyl amide polystyrene resin can be prepared for solid synthesis of protected peptide acids and amides and separation thereof without cleavage of acid labile protecting groups or decomposition of aromatic acid groups and from which purified polypeptides can be formed.

US Patent:

62709577, Aug 7, 2001

Filed:

Feb 22, 1999

Appl. No.:

9/242723

Inventors:

Daniel H. Rich - Madison WI
Michael E. Solomon - Arlington MA

Assignee:

Wisconsin Alumni Research Foundation - Madison WI

International Classification:

C12Q 170
A61K 4500

US Classification:

435 5

Abstract:

Disclosed are cyclosporin analogs having amino acid residue substitutions at positions 1, 3, or 7 of the cyclosporin peptide backbone. Also disclosed are conjugates of these cyclosporin analogs in which an HIV protease inhibitor moiety is conjugated to the position-7 amino acid residue of the cyclosporin. These compounds simultaneously bind to and inhibit cyclophilin and HIV protease. The compounds have good bioavailability and potent HIV inhibitory activity. They are useful in the treatment and prevention of HIV-mediated disorders, including AIDS.

US Patent:

62163396, Apr 17, 2001

Filed:

May 8, 1998

Appl. No.:

9/074743

Inventors:

Daniel Rich - Natick MA

Assignee:

3Com Corporation - Santa Clara CA

International Classification:

B23K 1904
H05K 500

US Classification:

29762

Abstract:

A tool-actuated ejector for extracting electronic modular components. The ejector, which functions as a levered cam, has a body with a first end, a second end and a pivot located intermediate the first and second ends. A tool-receiving socket mounts at the second end. A tool, such as a screwdriver with a blade that matches the shape of the socket, actuates the ejector by applying a force to the socket. A cam, located at the first end, engages the electronic modular component. To provide a mechanical advantage, the distance between the tool-receiving socket and the pivot, which constitutes one lever arm, is greater than the distance between the cam and the pivot, which constitutes a second lever arm. In addition, a shock absorber mounts on the body and gliders extend below the body to provide stability and balance to the ejector. The ejector mounts in a casing having a tool passage that communicates with the tool-receiving socket and the exterior of the casing.