Pfizer Corporation

Osi Pharmaceuticals, Inc.

Cultor Corporation

Jeffrey W Raggon

Ravi Mysore Shanker

Anthony D Piscopio

Robert Wayne Dugger

Timothy Norris

Joel Michael Hawkins

Michael J Castaldi

Sally Gut Ruggeri

Sarah E Kelly

Stephane Caron

Richard D Connell

Frank J Urban

Keith Michael DeVries

James Dale Moyer

Shama Kajiji

Gordon D Gruetzmacher

Brian C Vanderplas

Bishop Wlodecki

Douglas John Meldrum Allen

Sandra Leta Silberman

Barbara A Foster

Karen J Ferrante

Dinos Paul Santafianos

Stephanie Caron

Michael J Morin

Michael Aaron Brodney

Christopher John Helal

George Joseph Quallich

Yong Tao

Paul D Hill

Nga M Do

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.

N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate anhydrate and monohydrate

The present invention relates to novel benzyl(idene)-lactam derivatives, compounds of the formula I wherein Ris a group of the formula Gor Gdepicted below, wherein R, R, R, RX, a, n and m are as defined herein, their pharmaceutically acceptable salts, and pharmaceutical compositions which include selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT) receptors, specifically, of one or both of the 5-HTand 5-HTreceptors. The compounds of the invention are useful in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HTagonist or antagonist is indicated and have reduced potential for cardiac side effects, in particular QTc prolongation.

Benzyl(idene)-lactam derivatives

A method of monotherapy for a subject suffering from abnormal cell growth expressing the epidermal growth factor receptor (EGFR) which comprises orally administering to the subject a therapeutically effective amount of a crystalline polymorph of the hydrochloride salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine so as to treat the subject.

Treating abnormal cell growth with a stable polymorph of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride

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.

Stable polymorph on N-(3-ethynylphenyl)-6, 7-bis (2methoxyethoxy)-4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof

N-(3-ethynylphenylamino)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate anhydrate and monohydrate

Processes and intermediates for preparing substituted chromanol derivatives

Process for preparing cyclic thioamides

The invention relates to processes for preparing a compound of the formula

The instant invention relates to intermediates of Formula II, ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, and to processes for preparing such intermediates. This invention also relates to processes for preparing compounds of Formula III, ##STR2## and enantiomers thereof, wherein R.sup.2, R.sup.3 and R.sup.4 are as defined in the specification. Compounds of Formula II and Formula III are intermediates in the preparation of a potent .beta..sub.3 adrenergic receptor agonist. The instant invention also relates to processes for preparing the .beta..sub.3 adrenergic receptor agonist using the compounds of Formula II and Formula III.

Process and intermediates for a .beta..sub.3 -adrenergic receptor agonist

Processes for preparing substituted chromanol derivatives

There is disclosed a low calorie fat substitute comprising a sorbitol fatty acid ester with a degree of substitution of about five fatty acid groups. Foodstuffs containing the sorbitol ester are also disclosed. Processes for preparing the sorbitol fatty acid esters are also disclosed.

Low calorie fat substitute

There is disclosed a low calorie fat substitute comprising a sorbitol fatty acid ester with a degree of substitution of about four fatty acid groups. Foodstuffs containing the sorbitol tetraester are also disclosed.

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Uncasville, CT, United States of America

Jeffrey W Raggon