Pfizer Corporation

Other

Frank R Busch

Peter Robert Rose

Russell J Shine

Dennis Michael Godek

Stanley W Walinsky

John F Lambert

Derek Lawrence Tickner

Charles K Chiu

Clifford N Meltz

Sabeto A DiRoma

Ronald J Post

Carol A Rose

Susan L Orrill

Harry O Tobiassen

Gregory J Withbroe

Brian Thomas O'Neill

George Joseph Quallich

Robert Wayne Dugger

Zheng Jane Li

Joseph Francis Krzyzaniak

Douglas J M Allen

Douglas J Allen

Daniel R Arenson

Michel A Couturier

Richard S Lehner

Paul Bowles

Bijan Rasadi

Kathleen D Goggin

Douglas J Allan

Angela G Hausberger

Mark T Barrila

Meldrum Allen

Douglas John

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

Methods for preparing sodium-hydrogen exchanger type-1 inhibitors

The stratified two cycle engine comprises: a cylinder having an upper end and a lower end, a head at the upper end and fuel and air intake ports at the lower end; at least one spark plug mounted in the head; a sleeve in the cylinder having an upper end and a lower end and the cylinder having exhaust ports at the upper end which are covered and uncovered by the upper end of the sleeve; a piston in the sleeve and connected to a crank shaft; a first exhaust manifold at one side of the cylinder at the upper end thereof adjacent one exhaust port in the cylinder and having first exhaust gas throttle valve means associated therewith; at least a first and a second fuel and air intake manifolds at one side of the cylinder and at the other side of the cylinder in communication with first and second fuel and air intake ports in the cylinder; throttle valve means in each intake manifold; a reed cage assembly in each intake manifold adjacent the associated intake port for injecting a fuel and air mixture into the cylinder; control means for controlling the injection of fuel and air mixture into the cylinder so that fuel and air mixture is injected into the cylinder through only one intake port when the engine is operating from zero to one half full load; and an operating connection between the crank shaft and the sleeve for causing reciprocation of the sleeve relative to movement of the piston to open and close the exhaust ports and the air and fuel intake ports in the cylinder.

Two cycle stratified charge gasoline engine

The invention is directed to the mesylate dihydrate salts of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydro-2H-indol-2-one, pharmaceutical compositions containing said ziprasidone mesylate dihydrates, and methods of adminsitering the ziprasidone mesylate dihydrates to treat psychotic diseases.

Mesylate dihydrate salts of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)-ethyl)-6-chloro-1,3-dihydro-2(1H)-indol-2-one (&equals;ziprasidone), its preparation and its use as dopamine D2 antagonist

Compositions comprising crystalline ziprasidone free base or crystalline ziprasidone hydrochloride particles having a mean particle size less than 85 .mu.m, and a pharmaceutically acceptable carrier, are substantially bioequivalent and can be used to treat psychoses such as schizophrenia.

Ziprasidone formulations

Mesylate trihydrate salt of

Process for steroidal peracyl glycosides

Method for making steroidal peracyl glycosides

A method for preparing a compound of the formula ##STR1## wherein Q is C--H or N; R.sup.1 is C.sub.1-C.sub.4 alkyl, benzyl or p-nitrobenzyl and X and Y are independently selected from fluoro and chloro comprising reacting a compound of the formula ##STR2## wherein Q is &gt;C--H or N; X and Y are independently selected from fluoro and chloro; and Z is fluoro, chloro, 1-imidazolyl or substituted 1-imidazolyl, wherein the 1-imidazolyl group is substituted with one or two substituents independently selected from C.sub.1 to C.sub.4 alkyl, with a compound of the formula

Preparation of beta-ketoesters useful in preparing quinolone antibiotics

A process for preparing a compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof, which comprises reacting a piperazine salt of the formula ##STR2## with an alkyl halide containing compound of the formula ##STR3## in water with a reagent to neutralize the hydrohalic acid and heating the mixture under conditions which are suitable to effect the coupling of said piperazine salt with said alkyl halide containing compound.

Process for preparing aryl piperazinyl-heterocyclic compounds with a

The monohydrate of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydr o-2H-indole-2-one hydrochloride has advantageous stability for formulation as a neuroleptic agent.

Monohydrate of

Improved processes for preparation of racemic, cis- and optically active (3S,4R)-3[1(R)-t-butyl-dimethylsilyloxy)-ethyl]-4-[1-oxo-3-thiolanylthio(t hiocarbonyl)thio]azetidin-2-ones, process improvements for certain intermediates therefor and a novel intermediate for said racemic, cis- and trans-compounds, which compounds are useful as intermediates for antibacterial 5R,6S-6-[1(R)-hydroxyethyl]-2-(1-oxo-3-thiolanylthio)-2-penem-3-carboxylic acids and the pharmaceutically-acceptable salts and the pivaloyloxymethyl esters thereof.

Processes for

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Gales Ferry, CT, United States of America

Frank R Busch