The Procter Gamble Company

William Lee Seibel

Russell James Sheldon

Raymond Todd Henry

Jeffrey Joseph Ares

Thomas L Cupps

Sophie Eva Bogdan

Peter J Maurer

Daniel P Walker

Joseph H Gardner

Michael Selden Godlewski

Randy Stuart Muth

Sean Rees Klopfenstein

Sreenivasa Reddy Mundla

Guanidinylamino heterocycle compounds useful as &agr;-2 adrenoceptor agonists

2-imidazolinylaminoindole compounds useful as alpha-2 adrenoceptor agnonists

Guanidinyl heterocycle compounds useful as alpha-2 adrenoceptor agonists

This invention involves compounds having the following structure

Guanidinylamino heterocycle compounds useful as alpha-2 adrenoceptor agonists

This invention involves compounds having the following structure:

This invention involves compounds having the structure (I) as described in the claims, and enantiomers,optical isomers, stereoisomers, diastereomers, tautomers, addition salts, biohydrolyzable amides and esters thereof, as well as pharmaceutical compositions comprising such noved compounds. The invention also relates to the use of such compounds for preventing or treating disorders modulated by alpha-2 adrenoceptors.

This invention involves compounds having the following structure: ##STR1## wherein: a) R.sub.1 is hydrogen; or alkyl; bond (a) is a single or a double bond;

2-imidazolinylaminoindole compounds useful as alpha-2 adrenoceptor

2-imidazolinylaminobenzoxazole compounds useful as alpha-2 adrenoceptor

The present invention provides a process for making 2-amino-2-imidazoline, guanidine, and 2-amino-3,4,5,6-tetrahydroyrimidine derivatives by preparing the corresponding activated 2-thio-subsituted-2-derivative in a two-step, one-pot procedure and by further reacting yields this isolated derivative with the appropriate amine or its salts in the presence of a proton source. The present process allows for the preparation of 2-amino-2-imidazolines, quanidines, and 2-amino-3,4,5,6-tetrahydropyrimidines under reaction conditions that eliminate the need for lengthy, costly, or multiple low yielding steps, and highly toxic reactants. This process allows for improved yields and product purity and provides additional synthetic flexibility.

Process for making 2-amino-2-imidazoline, guanidine and

The subject invention relates to compounds having the structure: ##STR1## wherein (a) n is an integer from 1 to about 3;

2-Imidazolinylamino heterocyclic compounds useful as alpha-2

2-imidazolinylamino heterocyclic compounds useful as alpha-2

The subject invention involves halogenated amino acid derivatives useful as antimicrobial agents having the structure: ##STR1## wherein --R is hydrogen or 2-aminoethyl; --R' is hydroxy, alkoxy, aryloxy, or an amino acid residue bonded at the amino nitrogen; --R' is hydrogen or an amino acid residue bonded at the carbonyl carbon; --X is halogen; and --Y is hydrogen or halogen.

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Hamilton, OH, United States of America

William Lee Seibel