Bryan P Mckibben

US Patent:

6664252, Dec 16, 2003

Filed:

Dec 1, 2000

Appl. No.:

09/728607

Inventors:

Arlindo L. Castelhano - New City NY
Bryan McKibben - White Plains NY
David J. Witter - Putman Valley NY

Assignee:

OSI Pharmaceuticals, Inc. - Melville NY

International Classification:

C07D48704

US Classification:

5142285, 5142342, 51425216, 544 61, 544117, 544280

Abstract:

This invention pertains to compounds having the structure: wherein NR R is a substituted or unsubstituted 4-8 membered ring; wherein R is a substituted or unsubstituted four to six membered ring; wherein R is H, alkyl, substituted alkyl, aryl, arylalkyl, amino, substituted aryl; wherein R is H, alkyl, substituted alkyl, or cycloalkyl; with the proviso that NR R is not 3-acetamido piperadino, 3-hydroxy pyrrolidino, 3-methyloxy carbonylmethyl pyrolidino, or 3-aminocarbonylmethyl pyrrolidino; with the proviso that NR R is 3-hydroxymethyl piperadino only when R is 4-pyridyl; which specifically inhibit the adenosine A receptor and the use of these compounds to treat a disease associated with A adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.

US Patent:

6673802, Jan 6, 2004

Filed:

Nov 30, 2001

Appl. No.:

10/006405

Inventors:

Arlindo L. Castelhano - New City NY
Bryan McKibben - White Plains NY
David J. Witter - Putman Valley NY

Assignee:

OSI Pharmaceuticals, Inc. - Melville NY

International Classification:

C07D47334

US Classification:

5142632, 544277, 544280, 206568, 548558, 548537

Abstract:

The subject invention provides a compound having the structure: or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the A3 adenosine receptor by administering a therapeutically effective amount of the compound.

US Patent:

6680322, Jan 20, 2004

Filed:

Dec 1, 2000

Appl. No.:

09/728316

Inventors:

Arlindo L. Castelhano - New City NY
Bryan McKibben - White Plains NY
David J. Witter - Putman Valley NY

Assignee:

OSI Pharmaceuticals, Inc. - Melville NY

International Classification:

C07D48704

US Classification:

514258, 544280

Abstract:

This invention pertains to compounds which specifically inhibit the adenosine A receptor and the use of these compounds to treat a disease associated with A adenosine receptors in a subject.

US Patent:

6680324, Jan 20, 2004

Filed:

Nov 30, 2001

Appl. No.:

10/000280

Inventors:

Arlindo L. Castelhano - New City NY
Bryan McKibben - White Plains NY
David J. Witter - Putman Valley NY

Assignee:

OSI Pharmaceuticals, Inc. - Melville NY

International Classification:

A61K 31505

US Classification:

5142651, 544280

Abstract:

This invention pertains to compounds which specifically inhibit the adenosine A receptor and the use of these compounds to treat a disease associated with A adenosine receptors in a subject.

US Patent:

6686366, Feb 3, 2004

Filed:

Dec 2, 1999

Appl. No.:

09/454075

Inventors:

Arlindo L. Castelhano - New City NY
Bryan McKibben - White Plains NY
David J. Witter - Putnam Valley NY

Assignee:

OSI Pharmaceuticals, Inc. - Melville NY

International Classification:

C07D48704

US Classification:

5142641, 544280

Abstract:

This invention pertains to compounds which specifically inhibit the adenosine A receptor and the use of these compounds to treat a disease associated with A adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.

US Patent:

6800633, Oct 5, 2004

Filed:

Dec 1, 2000

Appl. No.:

09/728229

Inventors:

Arlindo L. Castelhano - New City NY
Bryan McKibben - White Plains NY
David J. Witter - Putnam Valley NY

Assignee:

OSI Pharmaceuticals, Inc. - Melville NY

International Classification:

C07D48704

US Classification:

5142651, 544280

Abstract:

This invention pertains to compounds having the structure: wherein R and R are each independently a hydrogen atom, substituted alkyl, or a substituted or unsubstituted aryl, or alkylaryl moiety or together form a substituted or unsubstituted heterocyclic ring, provided that both R and R are both not hydrogen atoms or that neither R or R is 1-phenylethyl; R is a substituted or unsubstituted aryl, or alkylaryl moiety; R is a hydrogen atom or a substituted or unsubstituted alkyl, aryl, or alkylaryl moiety; and R and R are each independently a halogen atom, a hydrogen atom or a substituted or unsubstituted alkyl, aryl, or alkylaryl moiety, and the use of these compounds to treat a disease associated with increased levels of adenosine in a subject.

US Patent:

6878716, Apr 12, 2005

Filed:

Dec 2, 1999

Appl. No.:

09/454074

Inventors:

Arlindo L. Castelhano - New City NY, US
Bryan McKibben - White Plains NY, US
David J. Witter - Putnam Valley NY, US

Assignee:

OSI Pharmaceuticals, Inc. - Melville NY

International Classification:

A61K031/517
C07D239/94

US Classification:

5142641, 544279

Abstract:

This invention pertains to compounds which specifically inhibit the adenosine Areceptor and the use of these compounds to treat a disease associated with Aadenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.

US Patent:

6916804, Jul 12, 2005

Filed:

Dec 20, 2002

Appl. No.:

10/326204

Inventors:

Arlindo Castelhano - New City NY, US
Bryan McKibben - Hopewell Junction NY, US
Arno Steinig - East Northport NY, US
Eric Collington - Knebworth, GB

Assignee:

OSI Pharmaceuticals, Inc. - Melville NY

International Classification:

C07D239/02
C07D243/08
C07D413/00
A61K031/505
A61K031/535

US Classification:

51421706, 544329, 544295, 544296, 544122, 540575, 540601, 514256, 5142522, 51425218, 51425211, 5142358

Abstract:

The subject invention provides compounds having the structure: wherein Ris substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; Ris hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; Ris hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or Rand Rare joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present Ris oxygen; Rand Rare each independently substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or RNRtogether form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl moiety containing from 1 to 6 heteroatoms; Ris hydrogen, alkyl, halogen or cyano; and n is 0, 1, 2, 3 or 4, or an enantiomer, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the Aadenosine receptor by administering a therapeutically effective amount of the compounds of the invention.