Hoffmann-la Roche Inc.

Daniel Obrecht

Klaus Muller

Arnold Trzeciak

Alfred Grieder

Albert E Fischli

Wilhelm Bannwarth

Eva-Maria Gutknecht

Andreas Knierzinger

Fernand Gerber

Christine Abrecht

This invention is directed to tetrahydronaphthalene compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, bromine, cyano, formyl, hydroxy, lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, aryloxy, lower aralkoxy or aryl; R.sup.2 is an amino acid residue or a chain of 2 to 20 amino acid residues wherein reactive moieties in the side chains of the amino acid residue(s) is/are protected or unprotected, and wherein the amino group of the N-terminal amino acid is a free or protected amino group; A.sup.1, A.sup.2, A.sup.3 and A.sup.4 each are .alpha.-amino acid residues wherein A.sup.1 and A.sup.2 are in the L configuration and A.sup.3 and A.sup.4 are in the D configuration when the .alpha.-C atom of said .alpha.-amino acid residue is asymmetric; X is oxygen or sulphur; Y is a residue of the formula ##STR2## n is 0 or 1; R.sup.3 is hydrogen or lower alkyl; R.sup.4 is hydrogen or lower alkyl; and Z and the two C atoms together are an aromatic ring selected from the group of benzene, furan, thiophene, pyridine or pyrimidine, wherein said aromatic ring is substituted or unsubstituted; and salts thereof and their intermediates. The compounds are useful as mimetics of exposed helical domains of proteins in order to clarify their role with respect to interactions with other proteins or with DNA or RNA through .alpha.-helical conformation. They are therefore valuable aids in the determination of biologically active peptide sequences and are accordingly so-called 'research tools'. They are also potentially useful as medicaments.

Tetrahydronaphthalene compounds

There are described compounds of the formula ##STR1## Wherein the variables have been defined herein. The compounds are useful as research tools in the determination of biologically active peptides sequences and also potentially suitable as medicaments, some of them being useful in the prevention or control of the formation of blood platelet thrombi, and some compounds are useful as intermediates.

Tri- and tetracyclic compounds

Tri-and tetracyclic compounds

The present invention is concerned with tetrahydronaphthalene derivatives which are mimics of domains of peptides or proteins which can interact with other proteins or with DNA or RNA through .alpha.-helical conformation, said tetrahydronaphthalene derivatives having the formulae: ##STR1## are valuable aids in the determination of biologically active peptide sequences and are accordingly so-called 'research tools'. They are, however, also potentially suitable as medicaments.

Tetrahydronaphthalene derivatives

Propiolophenone derivatives of the formula ##STR1## wherein R.sup.6 is hydrogen, lower alkyl or a group of the formula ##STR2## as well as corresponding hydroxy compounds of the formula ##STR3## wherein R.sup.6' is hydrogen, lower alkyl, a group of formula (a), (b), (c), (d) or (e) or a group of the formula

Propiolophenone derivatives

Styryl ketones of the formula ##STR1## wherein R.sup.8 and R.sup.9 are independently hydrogen or lower alkyl or together represent an additional carbon-carbon bond and

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Basel, Switzerland

Daniel Obrecht