John W Inman

US Patent:

7528274, May 5, 2009

Filed:

Jul 25, 2002

Appl. No.:

10/485165

Inventors:

John K. Inman - Bethesda MD, US
Atul Goel - Lucknow, IN
Ettore Appella - Chevy Chase MD, US
Jim Turpin - Frederick MD, US
Marco Schito - Rockville MD, US

Assignee:

The United States of America as represented by the Department of Health and Human Services - Washington DC

International Classification:

C07C 327/16
A61K 31/21

US Classification:

558256, 558257, 549 70, 549 71, 549484, 546313, 514354, 514355, 514448, 514461, 514513

Abstract:

Certain thiol and acylthiol compounds inhibit retrovirus growth by attacking the highly conserved zinc finger regions of essential viral proteins. These compounds, compositions containing them, and methods of using them to treat retroviral infections such as HIV are described. These compounds are also useful for preparation of vaccines comprised of inactivated retroviruses such as HIV, prevention of the transmission of such retroviruses, and detection of retroviral proteins.

US Patent:

8076372, Dec 13, 2011

Filed:

Mar 30, 2009

Appl. No.:

12/414321

Inventors:

John K. Inman - Bethesda MD, US
Atul Goel - Lucknow, IN
Ettore Appella - Chevy Chase MD, US
Jim A. Turpin - Frederick MD, US
Marco Schito - Rockville MD, US

Assignee:

Government of the United States - Rockville MD

International Classification:

A61K 31/21

US Classification:

514513, 514354, 514355, 514448, 514461

Abstract:

Certain thiol and acylthiol compounds inhibit retrovirus growth by attacking the highly conserved zinc finger regions of essential viral proteins. These compounds, compositions containing them, and methods of using them to treat retroviral infections such as HIV are described. These compounds are also useful for preparation of vaccines comprised of inactivated retroviruses such as HIV, prevention of the transmission of such retroviruses, and detection of retroviral proteins.

US Patent:

20130096092, Apr 18, 2013

Filed:

Jun 10, 2011

Appl. No.:

13/703097

Inventors:

Daniel Appella - Rockville MD, US
Ettore Appella - Chevy Chase MD, US
John K. Inman - Bethesda MD, US
Lisa M. Miller Jenkins - Germantown MD, US
Ryo Hayashi - Saga, JP
Deyun Wang - Rockville MD, US

Assignee:

Health and Human Services - Bethesda MD

International Classification:

C07C 323/63
C07F 9/12
C07D 307/73
C07F 9/6571

US Classification:

514111, 560251, 514546, 560 27, 514485, 564154, 514616, 558 86, 558190, 514119, 549496, 514471, 564153

Abstract:

Disclosed are inhibitors of retroviral growth of formula (I), that are useful in treatment of retroviral infections such as HIV. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one compound or salt of the invention, a method for inactivating a virus, a method for dissociating a metal ion from a zinc finger-containing protein, and a method for inhibiting the transmission of a virus.

US Patent:

54441501, Aug 22, 1995

Filed:

Nov 19, 1993

Appl. No.:

8/154786

Inventors:

John K. Inman - Bethesda MD
Frank A. Robey - Bethesda MD

Assignee:

The United States of America as represented by the Department of Health
and Human Services - Washington DC

International Classification:

A61K 3702
C08G 6348

US Classification:

530300

Abstract:

A new amino acid derivative, N. sup. alpha. -tert-butoxycarbonyl-N. sup. e -(N-bromoacetyl-. beta. -alanyl)-L-lysine (BBAL), has been synthesized as a reagent to be used in solid-phase peptide synthesis for introducing a side-chain bromoacetyl group at any desired position in a peptide sequence. The bromoacetyl group subsequently serves as a sulfhydryl-selective cross-linking function for the preparation of cyclic peptides, peptide conjugates and polymers. BBAL residues are stable to final HF deprotection/cleavage. BBAL peptides can be directly coupled to other molecules or surfaces which possess free sulfhydryl groups by forming stable thioether linkages. Peptides containing both BBAL and cysteine residues can be self-coupled to produce either cyclic molecules or linear peptide polymers. Such peptide derivatives are useful in preparing potential peptide immunogens, vaccines and therapeutics, and for substances such as peptides linked to polymers, plastics, enamels and ceramics.

US Patent:

52868460, Feb 15, 1994

Filed:

Jun 14, 1991

Appl. No.:

7/715650

Inventors:

John K. Inman - Bethesda MD
Frank A. Robey - Bethesda MD

Assignee:

The Government of the United States of America as represented by the
Dept. of Health and Human Services - Washington DC

International Classification:

A61K 3702
C08G 6348

US Classification:

530300

Abstract:

A new amino derivative, N. sup. alpha. -tert-butoxycarbonyl-N. sup. epsilon. -(N-bromoacetyl-. beta. -alanyl)-L-lysine (BBAL), has been synthesized as a reagent to be used in solid-phase peptide synthesis for introducing a side-chain bromoacetyl group at any desired position in a peptide sequence. The bromoacetyl group subsequently serves as a sulfhydryl-selective cross-linking function for the preparation of cyclic peptides, peptide conjugates and polymers. BBAL residues are stable to final HF deprotection/cleavage. BBAL peptides can be directly coupled to other molecules or surfaces which possess free sulfhydryl groups by forming stable thioether linkages. Peptides containing both BBAL and cysteine residues can be self-coupled to produce either cyclic molecules or linear peptide polymers. Such peptide derivatives are useful in preparing potential peptide immunogens, vaccines and therapeutics, and for substances such as peptides linked to polymers, plastics, enamels and ceramics.

US Patent:

57705631, Jun 23, 1998

Filed:

Jun 7, 1995

Appl. No.:

8/487568

Inventors:

David D. Roberts - Bethesda MD
Philip J. Browning - Brentwood TN
Joseph L. Bryant - Bethesda MD
John K. Inman - Bethesda MD
Henry C. Krutzsch - Bethesda MD
Nenghua Guo - Gaithersburg MD

Assignee:

The United States of America as represented by the Department of Health
and Human Services - Washington DC

International Classification:

A61K 3800
A61K 3804
C07K 500
C07K 700

US Classification:

514 8

Abstract:

This invention identifies a biologically active group of peptide sequences from Type I repeat units of the extracellular matrix protein, human thrombospondin-1, identical or homologous to the sequence, KRFKQDGGWSHWSPWSSC (SEQ ID NO:30). The biological activities residing with the full sequences, portions thereof, and variants of the full or partial sequences are disclosed. The invention describes how biological activity may be enhanced by covalently linking these peptides to suitable carriers, preferably a branched, water-soluble polymer of low (or absent) toxicity and immunogenicity, such as polysucrose (Ficoll. TM. ). The invention describes (1) a method for preparing such conjugates, (2) the use of the defined peptides or their conjugates in blocking or modifying the action on cellular processes of heparin (e. g. , proliferation, adhesion, motility, extravasation and neovascularization), sulfatides, related sulfated glycoconjugates, fibronectin, and basic fibroblast growth factor, involving malignant cell lines and normal endothelial cells. Use of the defined peptides, analogs or peptidomimetics and their conjugates for treatment of metastatic tumors, breast carcinomas, melanomas, Kaposi's sarcomas, hemangiomas, diabetic retinopathies, and various pathological conditions dependent upon neovascularization is also disclosed.