Henry L Strong

US Patent:

7297795, Nov 20, 2007

Filed:

Aug 16, 2004

Appl. No.:

10/918947

Inventors:

Karen Wiggins Sutherland - New City NY, US
Gregg Brian Feigelson - Chester NY, US
Diane Harris Boschelli - New City NY, US
David Michael Blum - Upper Saddle River NJ, US
Henry Lee Strong - Somerset NJ, US

Assignee:

Wyeth Holdings Corporation - Madison NJ

International Classification:

C07D 215/44

US Classification:

546159, 546160

Abstract:

This invention discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile comprising combining an amine compound with a cyanoacetic acid and an acid catalyst to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline in an alcoholic solvent and a trialkylorthoformate to yield a 3-amino-2-cyanoacrylamide; combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride in acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 4-amino-3-quinolinecarbonitrile and also discloses a process for the preparation of a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile comprising combining a disubstituted 3-amino thiophene with a cyanoacetamide and trialkylorthoformate in an alcoholic solvent to obtain a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride and acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile and also discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile by combining an amine compound with a cyanoacetic acid and a peptide coupling reagent to obtain a suspension; filtering the suspension to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline, an alcoholic solvent, and triethylorthoformate to yield a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride to yield a 4-amino-3-quinolinecarbonitrile.

US Patent:

20080033175, Feb 7, 2008

Filed:

Oct 5, 2007

Appl. No.:

11/973259

Inventors:

Karen Sutherland - New City NY, US
Gregg Feigelson - Chester NY, US
Diane Boschelli - New City NY, US
David Blum - Upper Saddle River NJ, US
Henry Strong - Somerset NJ, US

Assignee:

Wyeth Holdings Corporation - Madison NJ

International Classification:

C07D 401/00
C07D 471/02

US Classification:

544363000, 546114000

Abstract:

This invention discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile comprising combining an amine compound with a cyanoacetic acid and an acid catalyst to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline in an alcoholic solvent and a trialkylorthoformate to yield a 3-amino-2-cyanoacrylamide; combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride in acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 4-amino-3-quinolinecarbonitrile and also discloses a process for the preparation of a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile comprising combining a disubstituted 3-amino thiophene with a cyanoacetamide and trialkylorthoformate in an alcoholic solvent to obtain a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride and acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile and also discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile by combining an amine compound with a cyanoacetic acid and a peptide coupling reagent to obtain a suspension; filtering the suspension to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline, an alcoholic solvent, and triethylorthoformate to yield a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride to yield a 4-amino-3-quinolinecarbonitrile.

US Patent:

20080058521, Mar 6, 2008

Filed:

Jan 25, 2007

Appl. No.:

11/698258

Inventors:

Lalitha Krishnan - Suffern NY, US
David Blum - Upper Saddle River NJ, US
Anja Dilley - Blooming Grove NY, US
Sherry Pan - Asburn VA, US
John Potoski - West Nyack NY, US
Uresh Shah - Cranbury NJ, US
Archana Sharma - Congers NY, US
Henry Strong - Somerset NJ, US
Yanzhong Wu - Bardonia NY, US
Mei-Yi Zhang - Princeton NJ, US
Cynthia Blum - Upper Saddle River NJ, US

Assignee:

Wyeth - Madison NJ

International Classification:

C07D 239/02
C07D 213/02
C07D 241/02
C07D 333/52

US Classification:

544331000, 544405000, 546281100, 549057000

Abstract:

The present invention provides improved synthetic methods for the preparation of compounds that modulate proliferation or differentiation in a cell or tissue.

US Patent:

20080058523, Mar 6, 2008

Filed:

Jun 7, 2007

Appl. No.:

11/811328

Inventors:

Weiguo Liu - Parsippany NJ, US
Vladimir Dragan - Chester NY, US
Henry Strong - Somerset NJ, US
Yanzhong Wu - Bardonia NY, US
Zhixin Wen - Nanuet NY, US
Jessica Liang - Annandale NJ, US
Haris Durutlic - New Windsor NY, US
Karen Sutherland - New City NY, US
Anthony Pilcher - Colchester VT, US

International Classification:

C07D 401/10
C07D 401/14

US Classification:

544363000

Abstract:

The present invention relates to processes for synthesizing piperazine-piperidine compounds, and compounds useful as 5-HTbinding agents, particularly as 5-HTreceptor antagonists and agonists. The processes also allow for safer and environmentally tolerant production of these useful compounds.