Adamantyl acetamides as 11-β hydroxysteroid dehydrogenase inhibitors

US7968601B2 · kind B2 · utility

Assignee

• Janssen Pharmaceutica NA · BE

Inventors

• Joannes Theodorus Maria Linders · Eindhoven, NL
• Gustaaf Henri Maria Willemsens · Beerse, BE
• Ronaldus Arnodus Hendrika Joseph Gilissen · Beerse, BE
• Christophe Francis Robert Nestor Buyck · Temse, BE
• Greta Constantia Peter Vanhoof · Zoersel, BE
• Louis Jozef Elisabeth Van Der Veken · Vosselaar, BE
• Libuse Jaroskova · Vosselaar, BE

Key dates

• Filing date: Dec 18, 2007
• Grant date: Jun 28, 2011
• Expiry date: Mar 26, 2028

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2603/74
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

##STR00001## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n represents an integer being 1 or 2; R.sup.1 and R.sup.2 each independently represents hydrogen C.sub.1-4alkyl, NR.sup.9R.sup.10, C.sub.1-4alkyloxy; or R.sup.1 and R.sup.2 taken together with the carbon atom with which they are attached form a C.sub.3-6cycloalkyl; and where n is 2, either R.sup.1 or R.sup.2 may be absent to form an unsaturated bond; R.sup.3 represents a C.sub.6-12cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R.sup.3 represents a monovalent radical having one of the following formulae ##STR00002## wherein said C.sub.6-12cycloalkyl or monovalent radical may optionally be substituted with one, or where possible two, three or more substituents selected from the group consisting of C.sub.1-4alkyl, C.sub.1-4alkyloxy, halo or hydroxy; Q represents Het.sup.1 or Ar.sup.2 wherein said C.sub.3-8cycloalkyl, Het.sup.1 or Ar.sup.2 are optionally substituted with one or where possible two or more substituents selected from halo, C.sub.1-4alkyl, C.sub.1-4alkyloxy, hydroxy, nitro, NR.sup.5R.sup.6, C.sub.1-4alkyloxy substitute…