Pyrrolidin-2-one and piperidin-2-one derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors

Patent metadata

Field	Value
Publication number	US-9012494-B2
Application number	US-63267505-A
Country	US
Kind code	B2
Filing date	Apr 29, 2005
Priority date	May 7, 2004
Publication date	Apr 21, 2015
Grant date	Apr 21, 2015

Abstract

The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein
n is 1 or 2; L represents a C 1-3 alkyl linker optionally substituted with one or two substituents selected from C 1-4 alkyl, C 1-3 alkyloxy-C 1-4 alkyl-, hydroxy-C 1-4 alkyl, hydroxy, C 1-3 alkyloxy- or phenyl-C 1-4 alkyl; M represents a direct bond or a C 1-3 alkyl linker optionally substituted with one or two substituents selected from hydroxy, C 1-4 alkyl or C 1-4 alkyloxy; R 1 and R 2 each independently represent hydrogen, halo, cyano, hydroxy, C 1-4 alkyl optionally substituted with halo, C 1-4 alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar 1 and halo; or R 1 and R 2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R 3 represents hydrogen, halo, C 1-4 alkyl, C 1-4 alkyloxy-, cyano or hydroxy; R 4 represents hydrogen, halo, C 1-4 alkyl, C 1-4 alkyloxy-, cyano or hydroxy; R 5 represents hydrogen, C 1-4 alkyl or Ar 2 -C 1-4 alky-; R 6 represents hydrogen, halo, C 1-4 alkyl or C 1-4 alkyoxy-; Ar 1 and Ar 2 each independently represent phenyl or naphtyl wherein said phenyl and naphtyl are optionally substituted with C 1-4 alkyl, C 1-4 alkyloxy-, or phenyl-C 1-4 alkyl;

for use as a medicine.

First claim

The invention claimed is:

1. A compound having the formula

a N-oxide form, a pharmaceutically acceptable addition salt or a stereochemically isomeric form thereof, wherein
n is 1;
L represents a C 1 -linker substituted with one or two C 1-4 alkyl substituents;
M represents a C 1-3 alkanediyl linker substituted with one or two substituents selected from the group consisting…

Assignees

• Jaroskova Libuse
• Linders Joannes Theodorus Maria
• Buyck Christophe Francis Robert Nestor
• Van Der Veken Louis Jozef Elisabeth
• Dimitrov Vladimir Dimtchev
• Nikiforov Theo Teofanov
• Janssen Pharmaceutica Nv

Inventors

• Jaroskova Libuse
• Linders Joannes Theodorus Maria
• Buyck Christophe Francis Robert Nestor
• Van Der Veken Louis Jozef Elisabeth
• Dimitrov Vladimir Dimtchev
• Nikiforov Theo Teofanov

Classifications

• A61P43/00

  Human Necessities · mapped topic

• A61P9/00

  Human Necessities · mapped topic

• A61P3/04

  Human Necessities · mapped topic

• A61P9/10

  Human Necessities · mapped topic

• A61P3/10

  Human Necessities · mapped topic