Intermediates in the preparation of substituted chroman derivatives

US6384225B1 · kind B1 · utility

Assignee

• ASTRAZENECA AB · SE

Inventors

• Stefan Berg · Ekerö, SE
• Mats Linderberg · Gately Drive, SE
• Svante Ross · Gately Drive, SE
• Seth-Olov Thorberg · Haditha, IQ
• Bengt Ulff · Gately Drive, SE

Key dates

• Filing date: Aug 31, 2000
• Grant date: May 7, 2002
• Expiry date: Oct 18, 2020

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P35/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to new piperidinyl- or piperazinyl-substituted-3,4-dihydro-2H-1-benzopyran derivatives having the formula I whereinX is N or CH;Y is NR2CH2, CH2NR2, NR2CO, CONR2 or NR2SO2 wherein R2 is H or C1-C6 alkyl;R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl;R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl,wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted;n is 0-4;R9 is C1-C6 alkyl, C3-C6 cycloalkyl, OCF3, OCHF2, OCH2F, halogen, CONR6R7, CN, CF3, OH, C114 C6 alkoxy, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8; wherein R6, R7 and R8 are as defined above,as (R)-enantiomers, (S)-enantiomers or racemates in the form of a free base or pharmaceutically acceptable salts or solvates thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds in therapy.