Timothy Norris

US Patent:

6344563, Feb 5, 2002

Filed:

Jun 29, 2000

Appl. No.:

09/606609

Inventors:

Timothy Norris - Gales Ferry CT 06335
Megan E. Hnatow - Charlestown MA 02129
John F. Lambert - North Stonington CT 06359

International Classification:

C07D23356

US Classification:

5483111

Abstract:

process is described for preparing a compound of Formula (1. 3. 0): comprising: establishing a reaction mixture consisting of in an aprotic solvent; in the presence of a strong base in solid form selected from the group consisting of sodium hydroxide, NaOH; and potassium hydroxide, KOH;âand optionallyâin the presence of a catalytic amount of cesium carbonate, Cs CO , or of a phase transfer catalyst, especially a quaternary ammonium salt or a phosphonium saltâfollowed byâheating said reaction mixture under a nitrogen atmosphere; whereby there is produced a compound of Formula (1. 3. 0); and in a preferred embodiment the aprotic solvent is DMSO, the strong base in solid form is NaOH in powder or pellet form, and the phase transfer catalyst is tetra-n-butylammonium chloride (TBAC), which is used to prepare a preferred compound, useful as a 5-lipoxygenase inhibitor, of the formula: especially the substantially pure methanesulfonate salt thereof.

US Patent:

6346624, Feb 12, 2002

Filed:

Jun 29, 2000

Appl. No.:

09/607011

Inventors:

Timothy Norris - Gales Ferry CT
Megan E. Hnatow - Charlestown MA
John F. Lambert - North Stonington CT

Assignee:

Pfizer Inc - New York NY

International Classification:

C07D23360

US Classification:

5483111

Abstract:

A novel process intermediate, tetrahydro-4-[3-(4-fluorophenyl)thio]phenyl-2H-pyran-4-carboxamide, of the formula: is described, as well as its use in a process of preparing 5-lipoxygenase inhibitors of the formula: which comprises establishing a reaction mixture consisting of: and an electron deficient monocyclic or benzo-fused bicyclic N-heterocycle containing two nitrogen atoms of the formula: âin an aprotic solvent; in the presence of a carbonate of the formula: (M) -CO , where M is an alkali metal, Group 1/Ia element, selected from the group consisting of lithium, Li; sodium,Na; potassium, K; rubidium, Rb; and cesium, Cs; followed by heating of said reaction mixture under a nitrogen atmosphere; whereby there is produced the desired compound of the above-recited formula.

US Patent:

6359137, Mar 19, 2002

Filed:

Aug 26, 1999

Appl. No.:

09/383320

Inventors:

Timothy Norris - Gales Ferry CT
Keith M. DeVries - Chester CT
Peter R. Rose - Ledyard CT

Assignee:

Pfizer Inc. - New York NY

International Classification:

C07D47104

US Classification:

546123, 548515

Abstract:

Trovafloxacin acid salts are prepared via the hydrolysis of imine intermediates using mineral acid including, but not limited to, methanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid, nitric acid, sulfuric acid, phosphoric acid, hydrochloric acid, hydrobromic acid, tartaric acid, citric acid, acetic acid, and maleic acid. Trovafloxacin acid salts are useful as antibiotic agents.

US Patent:

6476040, Nov 5, 2002

Filed:

Mar 30, 2000

Appl. No.:

09/538635

Inventors:

Timothy Norris - Gales Ferry CT
Dinos P. Santafianos - Groton CT
Richard S. Lehner - Ledyard CT

Assignee:

Pfizer Inc. - New York NY
Pfizer Products Inc. - Groton CT

International Classification:

A01N 4354

US Classification:

514259, 544283, 544293

Abstract:

The present invention relates to methods and intermediates for preparing compounds of the formula 1 and the pharmaceutically acceptable salts and solvates thereof, as well as structurally related compounds, wherein R , R and R are as defined herein. The foregoing compounds are useful in the treatment of hyperproliferative disorders, such as cancers, in mammals.

US Patent:

6706721, Mar 16, 2004

Filed:

Jul 29, 1999

Appl. No.:

09/355534

Inventors:

Douglas John Meldrum Allen - New London CT
Timothy Norris - Gales Ferry CT
Jeffrey William Raggon - Teecomwas CT
Dinos Paul Santafianos - Manchester CT
Ravi Mysore Shanker - Groton CT

Assignee:

OSI Pharmaceuticals, Inc. - Melville NY

International Classification:

C07D23994

US Classification:

5142663, 544293

Abstract:

The present invention relates to the anhydrous and hydrate forms of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate. The invention also relates to pharmaceutical compositions containing N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate and to methods of treating hyperproliferative disorders, such as cancer, by administering N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate.

US Patent:

6753334, Jun 22, 2004

Filed:

Nov 27, 2001

Appl. No.:

09/995133

Inventors:

John F. Lambert - North Stonington CT
Timothy Norris - Gales Ferry CT

Assignee:

Pfizer, Inc. - New York NY
Pfizer Products, Inc. - Groton CT

International Classification:

C07D21538

US Classification:

514314, 546167, 546171

Abstract:

This invention relates to methods of preparing sodium-hydrogen exchanger type 1 (NHE-1) inhibitors of formula Iâ intermediates of the NHE-1 inhibitors and a new almost colorless form of the NHE-1 inhibitor N-(5-cyclopropyl-1-quinolin-5-yl-1H-pyrazole-4-carbonyl)-guanidine.

US Patent:

6900221, May 31, 2005

Filed:

Nov 9, 2000

Appl. No.:

09/711272

Inventors:

Timothy Norris - Gales Ferry CT, US
Jeffrey W. Raggon - North Stonington CT, US
Richard D. Connell - East Lyme CT, US
James D. Moyer - East Lyme CT, US
Michael J. Morin - Waterford CT, US
Shama M. Kajiji - Mystic CT, US
Barbara A. Foster - Mystic CT, US
Karen J. Ferrante - East Greenwich RI, US
Sandra L. Silberman - Randolph NJ, US

Assignee:

OSI Pharmaceuticals, Inc. - Melville NY

International Classification:

C07D239/94
A61K031/517
A61P035/00

US Classification:

5142664, 544293

Abstract:

The present invention relates to a stable crystalline form of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride designated the B polymorph, its production in essentially pure form, and its use. The invention also relates to the pharmaceutical compositions containing the stable polymorph B form of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine as hydrochloride, as well other forms of the compound, and to methods of treating hyperproliferative disorders, such as cancer, by administering the compound.

US Patent:

7019009, Mar 28, 2006

Filed:

Oct 21, 2003

Appl. No.:

10/689773

Inventors:

Roberto Colon-Cruz - Groton CT, US
Timothy Norris - Gales Ferry CT, US

Assignee:

Pfizer Inc. - New York NY

International Classification:

A61K 31/496
C07D 417/14

US Classification:

51425404, 544368

Abstract:

A process for preparing acyl derivatives as prodrugs of 5-(2-(4-(1,2 benzisothiazole-3-yl)-1-piperazinyl)ethyl-6-chloro-1,3-dihydro-2H-indol-2-one and pharmaceutically acceptable acid addition salts and methods of use as an antipsychotic.