Karl David Salzwedel

US Patent:

8318425, Nov 27, 2012

Filed:

Jul 6, 2009

Appl. No.:

12/498157

Inventors:

Karl Salzwedel - Olney MD, US
Feng Li - Brookings SD, US
Carl T. Wild - Gaithersburg MD, US
Graham P. Allaway - Darnestown MD, US
Eric O. Freed - Frederick MD, US

Assignee:

The United States of America, as represented by the Secretary, Department & Human Services - Washington DC
Myrexis, Inc. - Salt Lake City UT

International Classification:

C12Q 1/70
C12Q 1/68
A01N 61/00
A01N 57/00
A61K 31/00
A61K 31/66

US Classification:

435 61, 435 5, 435 611, 435 612, 514 1, 514120, 514510

Abstract:

Inhibition of HIV-1 replication by disrupting the processing of the viral Gag capsid (CA) protein (p24) from the CA-spacer peptide 1 (SP1) protein precursor (p25) is disclosed. Amino acid sequences containing a mutation in the Gag p25 protein, with the mutation resulting in a decrease in the inhibition of processing of p25 to p24 by dimethylsuccinyl betulinic acid or dimethylsuccinyl betulin, polynucleotides encoding such mutated sequences and antibodies that selectively bind such mutated sequences are also included. Methods of inhibiting, inhibitory compounds and methods of discovering inhibitory compounds that target proteolytic processing of the HIV Gag protein are included. In one embodiment, such compounds inhibit the interaction of the HIV protease enzyme with Gag by binding to the Gag proteolytic cleavage site rather than to the protease enzyme. In another embodiment, viruses or recombinant proteins that contain mutations in the region of the Gag proteolytic cleavage site can be used in screening assays to identify compounds that target proteolytic processing.

US Patent:

20040132011, Jul 8, 2004

Filed:

Oct 16, 2003

Appl. No.:

10/685801

Inventors:

Graham Allaway - Darnestown MD, US
Carl Wild - Gaithersburg MD, US
Karl Salzwedel - Olney MD, US

Assignee:

Panacos Pharmaceuticals, Inc.

International Classification:

C12Q001/70

US Classification:

435/005000

Abstract:

The invention is directed to methods for identifying compounds that decrease the ability of a virus, such as HIV-1, to infect previously uninfected cells by inducing conformational changes in viral envelope proteins, and the compounds discovered by such methods.

US Patent:

20040265320, Dec 30, 2004

Filed:

Jan 29, 2004

Appl. No.:

10/766528

Inventors:

Karl Salzwedel - Olney MD, US
Feng Li - Gaithersburg MD, US
Carl Wild - Gaithersburg MD, US
Graham Allaway - Darnestown MD, US
Eric Freed - Frederick MD, US

International Classification:

A61K039/42

US Classification:

424/160100

Abstract:

Inhibition of HIV-1 replication by disrupting the processing of the viral Gag capsid (CA) protein (p24) from the CA-spacer peptide 1 (SP1) protein precursor (p25) is disclosed. Amino acid sequences containing a mutation in the Gag p25 protein, with the mutation resulting in a decrease in the inhibition of processing of p25 to p24 by dimethylsuccinyl betulinic acid or dimethylsuccinyl betulin, polynucleotides encoding such mutated sequences and antibodies that selectively bind such mutated sequences are also included. Methods of inhibiting, inhibitory compounds and methods of discovering inhibitory compounds that target proteolytic processing of the HIV Gag protein are included. In one embodiment, such compounds inhibit the interaction of the HIV protease enzyme with Gag by binding to the Gag proteolytic cleavage site rather than to the protease enzyme. In another embodiment, viruses or recombinant proteins that contain mutations in the region of the Gag proteolytic cleavage site can be used in screening assays to identify compounds that target proteolytic processing.

US Patent:

20050015039, Jan 20, 2005

Filed:

May 24, 2004

Appl. No.:

10/851637

Inventors:

Karl Salzwedel - Olney MD, US
Feng Li - Gaithersburg MD, US
Carl Wild - Gaithersburg MD, US
Graham Allaway - Darnestown MD, US
Eric Freed - Frederick MD, US

International Classification:

A61M037/00

US Classification:

604004010

Abstract:

Inhibition of HIV-1 replication by disrupting the processing of the viral Gag capsid (CA) protein (p24) from the CA-spacer peptide 1 (SP1) protein precursor (p25) is disclosed. Amino acid sequences containing a mutation in the Gag p25 protein, with the mutation resulting in a decrease in the inhibition of processing of p25 to p24 by dimethylsuccinyl betulinic acid or dimethylsuccinyl betulin, polynucleotides encoding such mutated sequences and antibodies that selectively bind such mutated sequences are also included. Methods of inhibiting, inhibitory compounds and methods of discovering inhibitory compounds that target proteolytic processing of the HIV Gag protein are included. In one embodiment, such compounds inhibit the interaction of the HIV protease enzyme with Gag by binding to Gag rather than to the protease enzyme. In another embodiment, viruses or recombinant proteins that contain mutations in the region of the Gag proteolytic cleavage site can be used in screening assays to identify compounds that target proteolytic processing.

US Patent:

20080200550, Aug 21, 2008

Filed:

May 24, 2005

Appl. No.:

11/597431

Inventors:

Karl Salzwedel - Olney MD, US
Feng Li - Gaithersburg MD, US
Carl T. Wild - Gaithersburg MD, US
Graham P. Allaway - Darnestown MD, US
Eric O. Freed - Frederick MD, US

Assignee:

V.I. TECHNOLOGIES, INC. - Gaithersburg MD
THE GOV. OF US AS REP. BY THE SEC. DEP. OF HEALTH - Rockville MD

International Classification:

A61K 31/557

US Classification:

514573

Abstract:

Inhibition of HIV-1 replication by disrupting the processing of the viral Gag capsid (CA) protein (p24) from the CA-spacer peptide 1 (SP1) protein precursor (p25) is disclosed. Amino acid sequences containing a mutation in the Gag p25 protein, with the mutation resulting in a decrease in the inhibition of processing of p25 to p24 by dimethylsuccinyl betulinic acid or dimethylsuccinyl betulin, polynucleotides encoding such mutated sequences and antibodies that selectively bind such mutated sequences are also included. Methods of inhibiting, inhibitory compounds and methods of discovering inhibitory compounds that target proteolytic processing of the HIV Gag protein are included. In one embodiment, such compounds inhibit the interaction of the HIV protease enzyme with Gag by binding to Gag rather than to the protease enzyme. In another embodiment, viruses or recombinant proteins that contain mutations in the region of the Gag proteolytic cleavage site can be used in screening assays to identify compounds that target proteolytic processing.

US Patent:

20080233559, Sep 25, 2008

Filed:

Dec 21, 2007

Appl. No.:

11/962315

Inventors:

Karl SALZWEDEL - Olney MD, US
Feng Li - Gaithersburg MD, US
Carl T. Wild - Gaithersburg MD, US
Graham P. Allaway - Darnestown MD, US
Eric O. Freed - Frederick MD, US

International Classification:

C12Q 1/70

US Classification:

435 5

Abstract:

Inhibition of HIV-1 replication by disrupting the processing of the viral Gag capsid (CA) protein (p24) from the CA-spacer peptide 1 (SP1) protein precursor (p25) is disclosed. Amino acid sequences containing a mutation in the Gag p25 protein, with the mutation resulting in a decrease in the inhibition of processing of p25 to p24 by dimethylsuccinyl betulinic acid or dimethylsuccinyl betulin, polynucleotides encoding such mutated sequences and antibodies that selectively bind such mutated sequences are also included. Methods of inhibiting, inhibitory compounds and methods of discovering inhibitory compounds that target proteolytic processing of the HIV Gag protein are included. In one embodiment, such compounds inhibit the interaction of the HIV protease enzyme with Gag by binding to Gag rather than to the protease enzyme. In another embodiment, viruses or recombinant proteins that contain mutations in the region of the Gag proteolytic cleavage site can be used in screening assays to identify compounds that target proteolytic processing.

US Patent:

20090215778, Aug 27, 2009

Filed:

Apr 28, 2008

Appl. No.:

12/149178

Inventors:

Theodore J. Nitz - Boyds MD, US
Karl Salzwedel - Olney MD, US
Catherine Finnegan - Baltimore MD, US
Shirley Brunton - Windsor, GB
Stuart Flanagan - Wallingford, GB
Christian Montalbetti - Wallingford, GB
Thomas Stephen Coulter - Oxfordshire Wantage, GB

Assignee:

Panacos Pharmaceuticals, Inc. - Gaithersburg MD

International Classification:

C07D 487/04
A61K 31/496
A61K 31/519
A61K 31/5377
A61P 31/18

US Classification:

5142358, 544281, 51425216, 51425211, 544121

Abstract:

Derivatives of pyrazolopyrimidine compounds represented by Formula I are disclosed:These pyrazolopyrimidine derivatives and pharmaceutical compositions comprising these derivatives are useful in the treatment of HIV mediated diseases and conditions.