Hiroaki M Mitsuya

7470506, Dec 30, 2008

Jun 23, 1999

09/720276

John W. Erickson - Frederick MD, US
Sergei V. Gulnik - Frederick MD, US
Hiroaki Mitsuya - Chevy Chase MD, US
Arun K. Ghosh - River Forest IL, US

The United States of America as represented by the Department of Health and Human Services - Washington DC
Board of Trustees of the University of Illinois - Urbana IL

C12Q 1/70

435 5

The present invention provides an assay for determining the biochemical fitness of a biochemical species in a mutant replicating biological entity relative to its predecessor. The present invention further provides a continuous fluorogenic assay for measuring the anti-HIV protease activity of protease inhibitor. The present invention also provides a method of administering a therapeutic compound that reduces the chances of the emergence of drug resistance in therapy. The present invention also provides a compound of formula (I) or a pharmaceutically acceptable salt, a prodrug, a composition, or an ester thereof, wherein A is a group of formulas (A), (B), (C) or (D); R, R, R, Ror Ris H, or an optionally substituted and/or heteroatom-bearing alkyl, alkenyl, alkynyl, or cyclic group; Y and/or Z are CH, O, S, SO, SO, amino, amides, carbamates, ureas, or thiocarbonyl derivatives thereof, optionally substituted with an alkyl, alkenyl, or alkynyl group; n is from 1 to 5; X is a bond, an optionally substituted methylene or ethylene, an amino, O or S; Q is C(O), C(S), or SO; m is from 0 to 6; Ris OH, ═O (keto), NH, or alkylamino, including esters, amides, and salts thereof; and W is C(O), C(S), S(O), or SO. Optionally, Rand R, together with the N—W bond of formula (I), comprises a macrocyclic ring.

8597876, Dec 3, 2013

Oct 11, 2007

11/870931

John W. Erickson - Frederick MD, US
Sergei V. Gulnik - Frederick MD, US
Hiroaki Mitsuya - Chevy Chase MD, US
Arun K. Ghosh - West Lafayette IN, US

The United States of America, as represented by the Secretary, Department of Health and Human Services - Washington DC
Board of Trustees of the University of Illinois - Urbana IL

C12Q 1/70

435 5, 514357, 514332, 514478, 514482, 5142282

Disclosed is a method of treating human immunodeficiency virus (HIV) infection in an antiretroviral treatment-experienced mammal, which involves administering to the mammal an effective amount of a compound of the formula:or a pharmaceutically acceptable salt, a prodrug, or an ester thereof, or a pharmaceutically acceptable composition of the compound, the salt, the prodrug, or the ester thereof, wherein A, X, Q, W, m, and R-Rare as defined herein.

20050158713, Jul 21, 2005

Jan 6, 2005

11/030632

John Erickson - Frederick MD, US
Sergei Gulnik - Frederick MD, US
Hiroaki Mitsuya - Chevy Chase MD, US
Arun Ghosh - River Forest IL, US

THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS - Urbana IL

C12Q001/70

435005000

The present invention provides an assay for determining the biochemical fitness of a biochemical species in a mutant replicating biological entity relative to its predecessor. The present invention further provides a continuous fluorogenic assay for measuring the anti-HIV protease activity of a protease inhibitor. The present invention also provides a method of administering a therapeutic compound that reduces the chances of the emergence of drug resistance in therapy. The present invention also provides a compound of the formula: or a pharmaceutically acceptable salt, a prodrug, a composition, or an ester thereof, wherein A is a group of the formula: R, R, R, R, or Ris H, or an optionally substituted and/or heteroatom-bearing alkyl, alkenyl, alkynyl, or cyclic group; Y and/or Z are CH, O, S, SO, SO, amino, amides, carbamates, ureas, or thiocarbonyl derivatives thereof, optionally substituted with an alkyl, alkenyl, or alkynyl group; n is from 1 to 5; X is a bond, an optionally substituted methylene or ethylene, an amino, 0 or S; Q is C(O), C(S), or SO; m is from 0 to 6; Ris OH, ═O (keto), NH, or alkylamino, including esters, amides, and salts thereof; and W is C(O), C(S), S(O), or SO. Optionally, Rand R, together with the N—W bond of formula (I), comprise a macrocyclic ring.

20140011815, Jan 9, 2014

Jul 2, 2013

13/933319

Hiroaki Mitsuya - Chevy Chase MD, US
Arun E. Ghosh - West Lafayette IN, US

C12Q 1/37
A61K 31/35
A61K 31/4725
A61K 31/427
A61K 31/496
A61K 31/341
A61K 31/343
A61K 31/4525

51425301, 435 24, 514470, 514456, 514321, 514365, 514307

The present invention provides an assay for determining the biochemical fitness of a biochemical species in a mutant replicating biological entity relative to its predecessor. The present invention further provides a continuous fluorogenic assay for measuring the anti-HIV protease activity of protease inhibitor. The present invention also provides a method of administering a therapeutic compound that reduces the chances of the emergence of drug resistance in therapy. The present invention also provides a compound of formula (I) or a pharmaceutically acceptable salt, a prodrug, a composition, or an ester thereof, wherein A is a group of formulas (A), (B), (C) or (D); R, R, R, Ror Ris H, or an optionally substituted and/or heteroatom-bearing alkyl, alkenyl, alkynyl, or cyclic group; Y and/or Z are CH, O, S, SO, SO, amino, amides, carbamates, ureas, or thiocarbonyl derivatives thereof, optionally substituted with an alkyl, alkenyl, or alkynyl group; n is from 1 to 5; X is a bond, an optionally substituted methylene or ethylene, an amino, O or S; Q is C(O), C(S), or SO; m is from 0 to 6; Ris OH, ═O (keto), NH, or alkylamino, including esters, amides, and salts thereof; and W is C(O), C(S), S(O), or SO. Optionally, Rand R, together with the N—W bond of formula (I), comprise a macrocyclic ring.

55808603, Dec 3, 1996

Dec 5, 1989

7/446155

Eiji Kojima - Iwakuni, JP
Hidetoshi Yoshioka - Iwakuni, JP
Kunichika Murakami - Iwakuni, JP
Hiroaki Mitsuya - Rockville MD
Takuma Shirasaka - Rockville MD
Samuel Broder - Bethesda MD

Sanyo Kokusaku Pulp Co., Ltd. - Tokyo

A61K 3170
C07H 19173

514 45

An anti-AIDS virus agent is disclosed, which is characterized in that it contains the 2',3'-dideoxypurinenucleosides represented by the chemical formula (I): ##STR1## as an effective ingredient.

RE338877, Apr 14, 1992

Nov 2, 1990

7/608431

Steve Tam - West Caldwell NJ
Manfred Weigele - West Paterson NJ
Samuel Broder - Bethesda MD
Hiroaki Mitsuya - Rockville MD

Hoffmann-La Roche Inc. - Nutley NJ
United States of America - Washington DC

A61K 3170
A61K 900
A61K 922

536 22

A-B-C wherein A and C are each independently 2',3'dideoxynucleosides and B is a linking group; and a method of treating or preventing a retroviral injection in a subject by administering the compounds of the invention.

48373117, Jun 6, 1989

Jun 22, 1987

7/064631

Steve Tam - West Caldwell NJ
Manfred Weigele - North Caldwell NJ
Samuel Broger - Bethesda MD
Hiroaki Mitsuya - Rockville MD

Hoffman-La Roche Inc. - Nutley NJ
United States of America - Washington DC

A61K 3170
A61K 900
A61K 922

536 22

A-B-C wherein A and C are each independently 2',3' dideoxynucleosides and B is a linking group; and a method of treating or preventing a retroviral injection in a subject by administering the compounds of the invention.

56165668, Apr 1, 1997

Apr 30, 1993

8/056043

Hiroaki Mitsuya - Rockville MD
Samuel Broder - Bethesda MD
Robert Yarchoan - Bethesda MD

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

A61K 3170
C07H 19173
C07H 1920

514 47

A method for inhibiting intracellular replication of HIV in an HIV-infected individual comprising contacting the HIV reverse transcriptase in the HIV-infected cells with 2',3'-dideoxyadenosine-5'-triphosphate whose source is 2',3'-dideoxyadenosine or a pharmaceutically acceptable salt or prodrug thereof.