Bryan H O'Hara

US Patent:

20010039348, Nov 8, 2001

Filed:

Apr 30, 2001

Appl. No.:

09/845428

Inventors:

Jonathan Bloom - Nyack NY, US
Kevin Curran - Nyack NY, US
Martin DiGrandi - Piermont NY, US
Russell Dushin - Garrison NY, US
Stanley Lang - Carlsbad CA, US
Emily Norton - Nyack NY, US
Adma Ross - Rockland NY, US
Bryan O'Hara - Norwood NJ, US

Assignee:

American Home Products Corporation - Madison NJ

International Classification:

C07D217/12
C07D215/12

US Classification:

546/139000, 546/176000, 558/418000, 564/027000

Abstract:

Compounds having the formula: wherein R-Rare independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, —CN, —NO, —COR, —COR, —OR, —SR, —SOR, —SOR, —CONRR, —NRN(RR), —N(RR) or W-Y-(CH)-Z provided that at least one of R-Ris not hydrogen; or Rand Ror Rand R, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl; Rand Rare independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; Ris hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or Rand R, taken together may form a 3 to 7 membered heterocycloalkyl; W is O, NR, or is absent; Y is —(CO)— or —(CO)—, or is absent; Z is alkyl of 1 to 4 carbon atoms, —CN, —COR, COR, —CONRR, —OCOR, —NRCOR, —OCONR, —OR, —SR, —SOR, —SOR, SR6N(R7R8), —N(RR) or phenyl; G is aryl or fused bicyclic heteroaryl; X is a bond, —NH, alkyl of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, thioalkyl of 1 to 6 carbon atoms, alkylamino of 1 to 6 carbon atoms, or (CH)J; J is alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or benzyl; and n is an integer from 1 to 6; useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.

US Patent:

20020026055, Feb 28, 2002

Filed:

Mar 12, 2001

Appl. No.:

09/804510

Inventors:

Jonathan Bloom - Nyack NY, US
Martin DiGrandi - Piermont NY, US
Russell Dushin - Garrison NY, US
Stanley Lang - Carlsbad CA, US
Bryan O'Hara - Norwood NJ, US

Assignee:

American Home Products Corporation - Madison NJ

International Classification:

C 07D 4 1/02
C07D213/44

US Classification:

546/262000, 546/279100, 546/308000

Abstract:

Compounds of the formula wherein A is heteroaryl; R-Rare independently hydrogen, alkyl of 1 to 4 carbon atoms, perhaloalkyl of 1 to 4 carbon atoms, halogen, alkoxy of 1 to 4 carbon atoms, or cyano, or R, and Ror Rand Rmay be taken together to form aryl of 5 to 7 carbon atoms; W is O, NR, or is absent; G is aryl or heteroaryl; and X is a bond X is a bond, —NH, alkyl of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, thioalkyl of 1 to 6 carbon atoms, alkylamino of 1 to 6 carbon atoms, or (CH)J; and J is alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or benzyl; and n is an integer from 1 to 6; or a pharmaceutical salt thereof, useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.

US Patent:

20030007983, Jan 9, 2003

Filed:

Dec 6, 2001

Appl. No.:

10/006626

Inventors:

Stephen Goff - Tenafly NJ, US
Gilda Tachedjian - East Malvern, AU
Bryan O'Hara - Norwood NJ, US

International Classification:

C12Q001/70
C12P021/06
C12P019/34
A61K039/00
A61K039/38
A61K039/21

US Classification:

424/208100, 424/207100, 424/184100, 435/005000, 435/091100, 435/069100

Abstract:

This invention provides methods of determining whether a compound inhibits HIV-1 reverse transcriptase. This invention provides methods of determining whether a compound inhibits formation of a complex between a p66 and p51 subunit polypeptides of HIV-1 reverse transcriptase. This invention provides a method of determining whether a compound enhances formation of a complex between a p66 and p51 subunit polypeptides of HIV-1 reverse transcriptase. This invention provides methods of determining whether a compound inhibits formation of a complex between two p66 subunit polypeptides of HIV-1 reverse transcriptase. This invention provides methods of determining whether a compound enhances formation of a complex between two p66 subunit polypeptides of HIV-1 reverse transcriptase.

US Patent:

20030036653, Feb 20, 2003

Filed:

Mar 15, 2002

Appl. No.:

10/099695

Inventors:

Jonathan Bloom - Nyack NY, US
Martin DiGrandi - Piermont NY, US
Russell Dushin - Garrison NY, US
Stanley Lang - Carlsbad CA, US
Bryan O'Hara - Norwood NJ, US

Assignee:

American Home Products Corporation - Madison NJ

International Classification:

C07D217/14
C07D215/14
C07D223/16
C07D209/04

US Classification:

546/146000, 546/175000, 540/593000, 548/503000, 560/016000

Abstract:

Compounds of the formula R-Rare independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, —CN, —NO, —COR, —COR, —OR, —SR, —SOR, —SOR, —CONRR, —NRN(RR), —(RR) or W—Y—(CH)—Z; or Rand Ror Rand R, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl; Rand Rare independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; Ris hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or Rand R, taken together may form a 3 to 7 membered heterocycloalkyl; A is heteroaryl;

US Patent:

62077155, Mar 27, 2001

Filed:

Nov 22, 1999

Appl. No.:

9/444897

Inventors:

Jonathan Bloom - Nyack NY
Kevin Curran - Nyack NY
Martin DiGrandi - Piermont NY
Russell Dushin - Garrison NY
Stanley Lang - Carlsbad CA
Emily Norton - Nyack NY
Adma Ross - Suffern NY
Bryan O'Hara - Norwood NJ

Assignee:

American Home Products Corporation - Madison NJ

International Classification:

A01N47/28

US Classification:

514580

Abstract:

Compounds of the formula: ##STR1## are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpes virus.

US Patent:

62620827, Jul 17, 2001

Filed:

Sep 25, 2000

Appl. No.:

9/669483

Inventors:

Jonathan Bloom - Nyack NY
Martin DiGrandi - Piermont NY
Russell Dushin - Garrison NY
Stanley Lang - Carlsbad CA
Bryan O'Hara - Norwood NJ

International Classification:

C07D40112
A61K 3144

US Classification:

514336

Abstract:

Compounds of the formula ##STR1## wherein R. sub. 1 -R. sub. 5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, --CN, --NO. sub. 2, --CO. sub. 2 R. sub. 6, --COR. sub. 6, --OR. sub. 6, --SR. sub. 6, --SOR. sub. 6, --SO. sub. 2 R. sub. 6, --CONR. sub. 7 R. sub. 8, --NR. sub. 6 N(R. sub. 7 R. sub. 8), --N(R. sub. 7 R. sub. 8) or W--Y--(CH. sub. 2). sub. n --Z; or R. sub. 2 and R. sub. 3 or R. sub. 3 and R. sub. 4, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl; R. sub. 6 and R. sub. 7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R. sub. 8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or R. sub. 7 and R. sub.

US Patent:

62712365, Aug 7, 2001

Filed:

Sep 26, 2000

Appl. No.:

9/669943

Inventors:

Jonathan Bloom - Nyack NY
Martin DiGrandi - Piermont NY
Russell Dushin - Garrison NY
Stanley Lang - Carlsbad CA
Bryan O'Hara - Norwood NJ

International Classification:

C07D40102
A61K 3144

US Classification:

51425505

Abstract:

Compounds of the formula ##STR1## wherein R. sub. 1 -R. sub. 5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, --CN, --NO. sub. 2, --CO. sub. 2 R. sub. 6, --COR. sub. 6, --OR. sub. 6, --SR. sub. 6, --SOR. sub. 6, --SO. sub. 2 R. sub. 6, --CONR. sub. 7 R. sub. 8, --NR. sub. 6 N(R. sub. 7 R. sub. 8), --N(R. sub. 7 R. sub. 8) or W--Y--(CH. sub. 2). sub. n --Z; or R. sub. 2 and R. sub. 3 or R. sub. 3 and R. sub. 4, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl; R. sub. 6 and R. sub. 7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R. sub. 8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or R. sub. 7 and R. sub.

US Patent:

62553496, Jul 3, 2001

Filed:

Nov 22, 1999

Appl. No.:

9/444734

Inventors:

Jonathan Bloom - Nyack NY
Kevin Curran - Nyack NY
Martin DiGrandi - Congers NY
Russell Dushin - Garrison NY
Stanley Lang - Blauvent NY
Emily Norton - Nyack NY
Adma Ross - Suffern NY
Bryan O'Hara - Norwood NJ

Assignee:

American Home Products Corporation - Madison NJ

International Classification:

A61K 3117
C07D33500
C07D27300

US Classification:

514585

Abstract:

Compounds having the formula: ##STR1## wherein R. sub. 1 -R. sub. 5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, --CN, --NO. sub. 2, --CO. sub. 2 R. sub. 6, --COR. sub. 6, --OR. sub. 6, --SR. sub. 6, --SOR. sub. 6, --SO. sub. 2 R. sub. 6, --CONR. sub. 7 R. sub. 8, --NR. sub. 6 N(R. sub. 7 R. sub. 8), --N(R. sub. 7 R. sub. 8) or W--Y--(CH. sub. 2). sub. n --Z provided that at least one of R. sub. 1 -R. sub. 5 is not hydrogen; or R. sub. 2 and R. sub. 3 or R. sub. 3 and R. sub. 4, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl; R. sub. 6 and R. sub. 7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R. sub.