Sanofi-a Ventis Deutschland Gmbh

Aventis Pharma Deutschland, Gmbh

Genentech, Inc.

Theodor Andreas Wollmann

Robert S McDowell

Thomas Gadek

Gerhard Jaehne

Wendelin Frick

Gerhard Breipohl

Anuschirwan Peyman

David William Will

Jean-Francois Gourvest

Jean-Marie Ruxer

Andreas Lindenschmidt

Guenter Billen

Heiner Jendralla

Bernd Junker

David Rigal

Frank Cullmann

Anuschirwam Peyman

Gerhard Brejpohl

Regina Duffy

Robert Mcdowell

Jean-François Gourvest

Provided are certain crystalline hydrates of the formula I in which n has a value of from 0.5 to 1.8. The compound may be suitable, for example, as a hypolipidemic.

Certain crystalline diphenylazetidinone hydrates, pharmaceutical compositions thereof and methods for their use

The present invention is directed to the preparation of novel compounds useful in the treatment of hyperlipidemia, arteriosclerosis, hypercholesterolemia, and other related metabolic disorders. More specifically, the present invention is a novel process for the preparation of 1,4-diphenylazetidinone derivatives from &#x3b2;-substituted amino amides which are protected in the presence of silylating agents and at least one cyclization catalyst whose structural formula is represented by one of the general formula: wherein the various R-groups are defined herein.

Method for producing 1,4-diphenyl azetidinone derivatives

The present invention relates to ethyl (2S)-2-(naphthalene-1-sulfonylamino)-3-(4-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)ethyl)benzoylamino)propionate hemifumarate of formula (I), and to a process for its preparation comprising reacting 4-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)ethyl)benzoic acid or a derivative thereof and ethyl (2S)-3-amino-2-(naphthalene-1-sulfonylamino)propionate. The compound of formula (I) is a valuable pharmaceutical which can be used, for example, in the treatment or prophylaxis of diseases which can be influenced by inhibiting the vitronectin receptor, in particular of bone diseases such as osteoporosis. The invention furthermore relates to chemical intermediates useful for the preparation of the compound of formula (I).

1,4,5,6-tetrahydropyrimidine derivative as a vitronectin inhibitor

(2S)-2-(Adamantan-1-ylmethoxycarbonylamino)-3-(4-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)ethyl)benzoylamino)propionic acid isopropyl ester, its preparation and its use The present invention relates to (2S)-2-(adamantan-1-ylmethoxycarbonylamino)-3-(4-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)ethyl)benzoylamino)propionic acid isopropyl ester of the formula Iand its physiologically tolerable salts, their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them. The compound of the formula I and its physiologically tolerable salts are valuable pharmacologically active compounds which can be used, for example, in the treatment or prophylaxis of diseases which can be influenced by inhibiting the vitronectin receptor, for example of bone diseases such as osteoporosis.

(2S)-2-(adamantan-1-ylmethoxycarbonylamino)-3-(4-(2-(1,4,5,6-tetrhydropyrimidin-2-ylcarbamoyl)ethyl)benzoylamino)propionic acid isopropyl ester, its preparation and its use

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Hattersheim, Germany

Theodor Andreas Wollmann