Zeneca Limited

Astra Zeneca U.k. Limited

Richard E Shute

Alan Wellington Faull

Andrew G Brewster

Robert J Pearce

Peter W Caulkett

Michael J Smithers

John Wall Rayner

Michael Garth Wayne

George R Brown

Stuart D Mills

Andrew Bruce Holmes

Theresa Rachel Early

Catherine Janet Smith

Melanie Wing-Sze Tsang

Sturat D Mills

A method of synthesizing a compound of formula I: comprising the step of reacting a moiety of formula II: with a moiety of formula III: in compressed carbon dioxide in the presence of a transition metal catalyst and a base, wherein L is a labile leaving group; Ris optionally substituted Caryl; Ris selected from optionally substituted Caryl, optionally substituted Cheterocyclyl, optionally substituted Calkyl, and optionally substituted sulfonyl; Ris selected from H and optionally substituted Calkyl, Cheterocyclyl and Caryl; or Rand Rtogether with the nitrogen atom to which they are attached form optionally substituted nitrogen-containing Cheterocylyl or Cheteroaryl; and RRand Rare independently selected from optionally substituted Calkyl, Caryl, Cheterocyclyl, hydroxy, halo, amino and Calkoxy, or two of R, Rand R, together with the silicon atom to which they are attached, may form a silicon containing Cheterocyclyl group. 

Methods of amination

The invention concerns acid derivatives of formula I

Acid derivatives

Certain�(piperidin-4-yl-alkanoyl)carbazoyl!-carboxy-phenoxy derivatives

Compounds of formula I ##STR1## and metabolically labile esters and amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.13, M.sup.2, X.sup.1, Z.sup.1, Z.sup.1a, X.sup.2 and A.sup.1 have the meanings given in the specification. The compounds are useful as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa. Novel intermediates are also disclosed.

Heterocyclic derivatives

Certain diacyl hydrazine derivatives

The invention concerns chemical compounds of formula I

Acylurea derivatives

Heterocyclic compounds

Compounds of formula I ##STR1## and metabolically labile esters and amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.13, M.sup.2, X.sup.1, Z.sup.1, Z.sup.1a, X.sup.2 and A.sup.1 have the meanings given in the specification. The compounds are useful as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa. Intermediates are also disclosed.

The invention concerns allophanic acid derivatives of formula I

Allophanic acid derivatives

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Macclesfield, United Kingdom

Richard E Shute