The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Nov. 17, 1998

Filed:

Feb. 27, 1996
Applicant:
Inventors:

Christine Abrecht, Lengnau, CH;

Alfred Grieder, Sissach, CH;

Klaus Muller, Munchenstein, CH;

Daniel Obrecht, Basel, CH;

Assignee:

Hoffmann-La Roche Inc., Nutley, NJ (US);

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
C07K / ; C07K / ; C07D / ;
U.S. Cl.
CPC ...
530317 ; 530326 ; 530327 ; 530328 ; 530329 ; 530330 ; 530333 ; 530335 ; 530338 ; 540455 ; 556420 ; 560 10 ; 560 19 ; 560 28 ; 562427 ; 562428 ;
Abstract

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.


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