Diaza-spiro[3,5] nonane derivatives

US6113527A · kind A · utility

Assignee

• Hoffmann-La Roche Inc. · US

Inventors

• Geo Adam · Schopfheim, DE
• Andrea Cesura · Nyon, CH
• François Jenck · Riedisheim, FR
• Sabine Kolczewski · Lörrach, DE
• Stephan Rover · Weil am Rhein, DE
• Jurgen Wichmann · Steinen, DE

Key dates

• Filing date: Jun 11, 1999
• Grant date: Sep 5, 2000
• Expiry date: Jun 11, 2019

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P25/30
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to compounds of the general formula ##STR1## wherein R.sup.1 is C.sub.6-12 -cycloalkyl, optionally substituted by lower alkyl or C(O)O lower alkyl, indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; acenaphthen-1-yl; bicyclo[3.3.1]non-9-yl, octahydro-inden-2-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl, decahydro-azulen-2-yl; bicyclo[6.2.0]dec-9-yl; decahydro-naphthalen-1-yl, decahydro-naphthalen-2-yl; tetrahydro-naphthalen-1-yl, tetrahydro-naphthalen-2-yl or 2-oxo-1,2-diphenyl-ethyl; PA1 R.sup.2 is .dbd.O or hydrogen, PA1 R.sup.3 is hydrogen, isoindolyl-1,3-dione, lower alkoxy, lower alkyl, amino, benzyloxy, --CH.sub.2 OR.sup.5 or --CH.sub.2 N(R.sup.5).sub.2 ; PA1 R.sup.4 is hydrogen or --CH.sub.2 OR.sup.5 ; PA1 R.sup.5 is hydrogen or lower alkyl; ##STR2## is cyclohexyl or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; to racemic mixtures and their corresponding enantiomers and or pharmaceutically acceptable acid addition salts thereof. The compounds of the present invention are agonists of the orphamin FQ (OFQ) receptor and therefore useful in the treatment of diseases, related to this receptor.