Aventis Pharmaceuticals Products Inc.

Sanofi

Aventis Pharmaceuticals Inc.

Sanofi-aventis

Aventis Pharma S.a.

Adam W Sledeski

Matthew R Powers

James J Mencel

Benoit J Vanasse

James P Sherbine

Rick G Woodward

Walter Rodriguez

Robert C Liu

John J Shay, Jr

Gregory G Kubiak

Patrick Leon

Yong Mi Choi-Sledeski

Gregory Bernard Poli

Michael K O'Brien

Zofia J Chrzan

Patrick Wai-Kwok Shum

Narasimha M Vemuri

Anthony J Gardetto

Vincent Windisch

Diane C Salazar

David Toledo-Velasquez

Nakyen Choy

Luc Grondard

Michel Lavigne

Christophe Daubie

Ching T Tsuei

Robert Stammler

Tory H Powner

Laurence Pailleres-Hubert

Benoit Viguier

Geoffrey A D'Netto

Diane C Salazar, Deceased

John J Shay

The present invention is an improved method for the preparation of (4-fluoro-3-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester, compound of formula I. The invention is directed to a method of synthesis for the compound of formula I in three steps, comprising formation of 5-((tert-butoxycarbonyl)aminomethyl)-2-fluorobenzeneboronic acid (compound 11), reaction of compound 11 under Suzuki coupling conditions to yield (4-fluoro-2-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester and selective hydrogenation of the aforementioned product under hydrogenation conditions yields compound I. The invention is also directed to the intermediates 5-((tert-butoxycarbonyl)amino-methyl)-2-fluorobenzeneboronic acid (compound 11), and (4-fluoro-3-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester (compound 13).

Synthesis of (4-fluoro-3-piperidin-4-yl-benzyl)-carbamic acid tert-butyl ester and intermediates thereof

The present invention is directed to a method for the preparation of 2,2,2-trifluoro-n-(4-fluoro-3-pyridin-4-yl-benzyl)-acetamide hydrochloride of the formula: and reaction intermediates used in the method.

Method and intermediates for the preparation of 2,2,2-trifluoro-N-(4-fluoro-3-pyridin-4-yl-benzyl)-acetamide hydrochloride

The present invention is directed to an indole benzylamine compound of formula I: useful as an inhibitor of tryptase. In addition, the present invention is directed to the use of the compound for treating a patient suffering from, or subject to, a physiological condition in need of amelioration by inhibition of tryptase, comprising administering to the patient of a therapeutically effective amount of the compound, and to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier.

[4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-[7-flouro-1-(2-methoxy-ethyl)-4-trifluorom as an inhibitor of mast cell tryptase

STABLE NON-HYGROSCOPIC CRYSTALLINE FORM OF N-&lsqb;N-&lsqb;N-(4-(PIPERIDIN-4-YL)BUTANOYL)-N-ETHYLGLYCYL&rsqb;ASPARTYL&rsqb;-L-&bgr;-CYCLOHEXYL ALANINE AMIDE, INTERMEDIATES THEREOF, AND PREPARATION THEREOF AND OF ANTITHROMBOTIC AZACYCLOALKYLALKANOYL PEPTIDES AND PSEUDOPEPTIDES

This invention is directed to a process for the solid phase, fragment-based synthesis of resin-bound cyclic peptide analogs of parathyroid hormones and analogs of parathyroid hormone-related proteins, which analogs contain at least one bridge between the side chains of two non-adjacent amino acid residues, and to peptide fragments useful therefor.

Process for the preparation of resin-bound cyclic peptides

This invention is directed to a process for preparing N6-substituted adenosine derivatives, to intermediates useful therefor and to methods of preparing these intermediates.

Process for preparing N6-substituted adenosine derivatives

The invention is directed to improved methods for preparing N6-substituted adenosine derivatives, to intermediates useful therefor and to methods of preparing these intermediates.

This invention is directed to a process for preparing a pseudotetrapeptide of formula I

Process for the preparation of azacycloalkylakanoyl pseudotetrapeptides

The invention is directed to a non-hygroscopic stable crystalline form of the antithrombotic compound N-[N-[N-(4-piperdin-4-yl)butanoyl)-N-ethylglycyl]-(L)-aspartyl]-(L)-.beta. -cyclohexyl-alanine amide, to processes for preparing said stable crystalline form, to a pharmaceutical composition thereof, and intermediates thereof, and the invention is directed also to processes for preparing a compound of the formula ##STR1## wherein: A, B, Z, E.sup.1, E.sup.2, G, R, m, n, and p are as defined herein.

Stable non-hygroscopic crystalline form of

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Belle Mead, NJ, United States of America

Adam W Sledeski