Pfizer Corporation

Warner-lambert Company

Pfizer Products Inc.

Peter Robert Rose

Frank R Busch

George Joseph Quallich

Glenn R Williams

Timothy Norris

Joseph Francis Krzyzaniak

Keith Michael DeVries

Derek Lawrence Tickner

Evgenyi Y Shalaev

Lewin Theophilus Wint

Charles K Chiu

Clifford N Meltz

Antone John deBettencourt, Iii

Phillip James Johnson

Kevin Quackenbush

David E Bogle

Susan L Orrill

Harry O Tobiassen

Ronald J Post

Marie Louise Reynolds

George M Laurence

Zheng Jane Li

Tamim F Braish

Philip D Hammen

Darrell E Fox

Timothy Andrew Woods

Douglas J M Allen

Stephen S Massett

Douglas James Critcher

Aeri Park

Carl Bernard Ziegler

Yong Tao

Michel A Couturier

Timothy J N Watson

Carl B Ziegler, Jr

Paul Bowles

John L Tucker

Kevin Paul Girard

George Laurence

Gregory J Withbroe

Robert Eugene Handfield, Jr

Kevin J Quackenbush

Diane M Rescek

Marie L Reynolds

Brian Matthew Samas

David Sydney Bernard Daniels

Gregory Scott Goeken

Mark T Barrila

Glenn Robert Williams

David Everett Bogle

The present invention discloses a novel p-toluenesulfonic acid salt and a crystalline polymorphic Form 1 of said salt of 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one, pharmaceutical composition containing the same, as well as preparations and uses thereof. The present invention also discloses a novel phosphoric acid salt of 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one, pharma-ceutical composition containing the same, as well as preparations and uses thereof.

Pyrrolo[2,3-d]pyrimidine tosylate salt, crystalline form thereof and manufacturing process and intermediates thereto

This invention relates to a crystalline form of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclo-tetradecine-3-carbonitrile (lorlatinib) free base hydrate (Form). This invention also relates to pharmaceutical compositions comprising Form, and to methods of using Formand such compositions in the treatment of abnormal cell growth, such as cancer, in a mammal.

Crystalline form of lorlatinib free base hydrate

A process for forming amorphous atorvastatin comprising the steps of dissolving atorvastatin in a non-hydroxylic solvent and removing the solvent by freeze-drying, as well as processes of dissolving atorvastatin in a hydroxylic solvent with a solubilizing agent or an alkalizing agent or an antioxidant and removing the solvent by freeze-drying to afford amorphous atorvastatin.

Process for forming amorphous atorvastatin

Novel forms of [R-(R*,R*)]-2-(4-fluorophenyl)-&#x3b2;,&#x3b4;-dihydroxy-5-(1-methylethyl)-3-phenyl-4 -[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium salt designated Form XX, Form XXI, Form XXII, Form XXIII, Form XXIV, Form XXV, Form XXVI, Form XXVII, Form XXVIII, Form XXIX, and Form XXX, characterized by their X-ray powder diffraction, solid-state NMR, and/or Raman spectroscopy are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPH) and Alzheimer's disease.

Forms of [R-(R*,R*)]-2-(4-fluorophenyl)-&#x3b2;,&#x3b4;-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoicacid calcium salt (2:1)

An improved process for the preparation of 1,3 substituted indenes which are useful intermediates in the synthesis of aryl fused azapolycyclic compounds as agents for the treatment of neurological and psychological disorders.

Process for the preparation of 1,3-substituted indenes

The present invention is directed to the tartrate salts of 5,8,14-triazatetracyclo[10.3.1.00]-hexadeca-2(11),3,5,7,9-pentaene: and pharmaceutical compositions thereof. The present invention in particular is directed to the L-tartrate salt, and further to the various polymorphs of the L-tartrate salt, including two distinct anhydrous polymorphs (referred to herein as Forms A and B) and a hydrate polymorph (referred to herein as Form C). In addition, the present invention is also directed to the D-tartrate salt of 5,8,14-triazatetracyclo[10.3.1.00]-hexadeca-2(11),3,5,7,9-pentaene and the various polymorphs thereof; as well as the D,L-tartrate salt thereof and its polymorphs, and the meso-tartrate salt thereof and its polymorphs.

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The present invention is directed to the tartrate salts of 5,8,14-triazatetracyclo[10.3.1.00]-hexadeca-2(11),3,5,7,9-pentaene:and pharmaceutical compositions thereof. The present invention in particular is directed to the L-tartrate salt, and further to the various polymorphs of the L-tartrate salt, including two distinct anhydrous polymorphs (referred to herein as Forms A and B) and a hydrate polymorph (referred to herein as Form C). In addition, the present invention is also directed to the D-tartrate salt of 5,8,14-triazatetracyclo[10.3.1.00]-hexadeca-2(11),3,5,7,9-pentaene and the various polymorphs thereof; as well as the D,L-tartrate salt thereof and its polymorphs, and the meso-tartrate salt thereof and its polymorphs.

Tartrate salts of 5,8, 14-triazateracyclo[10.3.1.02,11 04.9]-hexadeca-2(11),3,5,7,9-pentaene and pharmaceutical compositions thereof

Citrate salt of 5,8,14-triazatetracyclo&lsqb;10.3.1.02,11.04,9&rsqb;-hexadeca-2(11),3,5,7,9-pentaene and pharmaceutical compositions thereof

The instant invention provides novel processes and intermediates useful in the preparation of certain N-(indole-2-carbonyl)-&bgr;-alaninamide compounds, which compounds are glycogen phosphorylase inhibitors useful in the treatment of diseases such as hypercholesterolemia, hyperglycemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis, diabetes, diabetic cardiomyopathy, infection, tissue ischemia, myocardial ischemia, and in inhibiting tumor growth.

Processes and intermediates for preparing glycogen phosphorylase inhibitors

N-(indole-2-carbonyl)-b-alaninamide crystal forms

Process for preparing growth hormone secretagogues

This invention relates to methods for preparing anhydrous CETP inhibitor, (2R,4S)-4-&lsqb;(3,5-bis-trifluoromethyl-benzyl)-methoxycarbonyl-amino&rsqb;-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester.

Preparation of anhydrous CETP inhibitor

Two crystalline polymorphic forms of (2-Benzhydryl-1-azo-bicyclo&lsqb;2.2.2&rsqb;oct-3-yl)-(5-isopropyl-2-methoxybenzyl)-amine citrate monohydrate (the monohydrates) are Form A and Form B. The pharmaceutical composition containing at least one of these polymorphs has advantageous stability for formulation to treat acute emesis in patient receiving chemotherapy. The administration of this pharmaceutical composition is conventional oral by preferably tablet or capsule and intravenous. A method of making A and B Forms is also disclosed.

Polymorphs of a crystalline azo-bicyclo (2.2.2) oct-3-yl amine citrate and their pharmaceutical compositions

Growing community of inventors

Ledyard, CT, United States of America

Peter Robert Rose