3-oxo-2,1-benzisoxazol-1(3H)-carboxamides for treatment of CNS diseases

US6589949B1 · kind B1 · utility

Assignee

• BAYER HEALTHCARE LLC · DE

Inventors

• Toshiya Moriwaki · Nara, JP
• Chantal Fürstner · Neheim, DE
• Bernd Riedl · Wuppertal, DE
• Jens-Kerim Ergüden · Uerdingen, DE
• Frank-Gerhard Boss · Wuppertal, DE
• Bernard Schmidt · Lindlar, DE
• Franz-Josef van der Staay · Dronten, NL
• Werner Schroder · Wuppertal, DE
• Karl-Heinz Schlemmer · Wuppertal, DE
• Nagahiro Yoshida · Kyoto, JP

Key dates

• Filing date: Oct 22, 2002
• Grant date: Jul 8, 2003
• Expiry date: Oct 22, 2022

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P25/28
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to novel 3-oxo-2,1-benzisomazol-1(3H)-carboxamides (I), where R1, R2 are the same or different and independently=H, halogen, C1 C6 alkyl C1 C6 alkoxy, C1 C3 perfluoroalkyl, or a group NR5R6; R3, R4 are the same or different and independently=C1 C8 alkyl, whose carbon chain is optionally interrupted by an O, S or NR7 and is optionally singly or severally substituted by C3 C6 cycloalkyl, C1 C4 alkoxy, OH, halogen or NR8R9; C3 C8 cycloalkyl whose carbon chain is optionally interrupted by an O, S or NR10 and is optionally singly or severally substituted by C1 C4 alkoxy, OH, halogen or NR11R12, or R3 and R4 together with a nitrogen atom form a saturated or partially unsaturated 3- to 10-membered mono- or bi-cyclic heteocycle, which, optionally, contains up to two further heteroatoms, from N, O or S and is, optionally, substituted by C1 C4 alkyl, C1 C4 alkoxy, OH, halogen, COOR13 or NR14R15 and X=O or S. The invention further relates to methods for production thereof and use thereof in the production of medicaments for the prophylaxis and/or treatment of diseases of the central nervous system, in particular, cognitive disorders, such as Alzheimer's disease and other…