Pfizer Corporation

Warner-lambert Company

Keith Michael DeVries

Philip Charles Levett

Brian C Vanderplas

Albert Shaw Wood

Laurence James Harris

Joanna Teresa Negri

Ravi Mysore Shanker

Mark Edward Bunnage

Frank J Urban

John Paul Mathias

Peter Robert Rose

Jeffrey W Raggon

Philip D Hammen

Stephen Derek Albert Street

John L Tucker

Robert L Dow

David James Rawson

Timothy Norris

Dennis J Hoover

Stephen Wayne Wright

Willard McKowan Welch, Jr

Charlotte Moira Norfor Allerton

Christopher Gordon Barber

Darrell E Fox

Anabella Villalobos

Michel A Couturier

Brian M Andresen

Fumitaka Ito

Jeffrey B Jorgensen

Diane M Rescek

A process for the preparation of Compounds of the formula (1): wherein R, R, Rand Rare as defined or a pharmaceutically or veterinarily acceptable salt or polymorph thereof, or a pharmaceutically or veterinarily acceptable solvate or pro-drug thereof: are potent and selective inhibitors of type 5 cyclic guanosine 3',5&#x2032;-monophosphate phosphodiestbrase (cGMP PDE5) and have utility in the treatment of, inter alia, male erectile dysfunction (MED) and female sexual dysfunction (FSD).

Process for preparing pharmaceutically active compounds

Process for the preparation of pyrazolo&lsqb;4,3-d&rsqb;pyrimidin-7-one compounds and intermediates thereof

Pharmaceutically active compounds

Process for preparing hydroxypyrrolidinyl ethylamine compounds useful as kappa agonists

The present invention provides novel processes for preparing 3(S)-&lsqb;(5-chloro-1H-indole-2-carbonyl)-amino&rsqb;-2(R)-hydroxy-4-phenyl-butyric acid. Also provided are novel intermediates used in those processes. Further, the 3(S)-&lsqb;(5-chloro-1H-indole-2-carbonyl)-amino&rsqb;-2(R)-hydroxy-4-phenyl-butyric acid prepared by the novel processes can be further reacted to yield known indole 2-carboxamides and derivatives thereof possessing glycogen phosphorylase inhibitory activity, which are useful in the treatment of mammals, especially human beings, having glycogen phosphorylase dependent diseases or conditions.

Processes and intermediates for preparing 3(S)-&lsqb;(5-chloro-1H-indole-2-carbonyl)-amino&rsqb;-2(R)-hydroxy-4-phenyl-butyric acid

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.

Process for preparing trovafloxacin acid salts

The present invention relates to novel atropisomers of 2-(aryl or heteroaryl)-3-aryl-4(3H)-quinazolinones of the formula I, and their pharmaceutically acceptable salts, and pharmaceutical compositions and methods of treating neurodegenerative and CNS-trauma related conditions.

Atropisomers of 3-aryl-4(3H)-quinazolinones and their use as AMPA-receptor antagonists

This invention relates to processes for preparing compounds of the formula (I)

Process for substituted pyridines

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

A new pyridine carbaldehyde is useful for the synthesis of compounds which are effective for treating neurodegeneration conditions and CNS trauma.

Process and intermediates for 3-heteroaryl-4(3H) quinazolines

A method for preparing hydroxamic acid derivatives which are useful as analgesic, antiinflammatory, or neuroprotective agents.

Process for pyrrolidinyl hydroxamic acid compounds

A process of purifying a (6-chloro-2-carbazolyl)methyl-malonic acid di(C.sub.1 -C.sub.6 alkyl) ester of Formula (I): ##STR1## wherein R.sub.a and R.sub.b must be the same and are selected from the group consisting of C.sub.1 -C.sub.6 alkyl; comprises phase separating one or more impurities from said carbazole ester at least once wherein the solvent used to carry out said phase separation is acetic acid. In a preferred embodiment said acetic acid is glacial acetic acid which is maintained at a temperature of from about 30.degree. to about 110.degree.0 C. and said carbazole ester is obtained in a purity of at least 99.90% by weight, so that the amount of impurities present therein is 0.10% or less by weight. In a more preferred embodiment of said process, said temperature is from about 50.degree. to about 70.degree. C., and said phase separation is carried out only once.

Method of purifying carbazole ester precursors of

Processes and intermediates for preparing 5,

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Chester, CT, United States of America

Keith Michael DeVries