Title:
PYRROLO-PYRIDINE DERIVATIVE
Document Type and Number:
Japanese Patent JP2710751
Kind Code:
B2
Abstract:
PURPOSE: To provide the pyrrolo-pyridine derivatives which are antagonists of dopamine receptor subtypes within the brain, useful for treating and preventing mental disorders such as schizophrenia.
CONSTITUTION: The compounds are those represented by formula I, e.g. 3-(4- phenylpyperazin-1-yl)methyl-1H-pyrrolo[2,3-b]pyridine, which are obtained by allowing compounds of formula II and compounds of formula III (Rp is R or a protective group) to react with each other in the presence of formaldehyde and by optionally de-protecting and N-alkylating the reaction products. They have a selective affinity for the dopamine D4 receptor subtype over other dopamine receptor subtypes, D2 subtype in particular, and therefore have fewer side-effects compared with the ordinary neuroleptic drugs. In formula I, R is H or 1-6C alkyl; R1 is H, 1-6C alkyl, 1-6C alkoxy, aryl or the like; R2 is 1-6C alkyl, 2-6C alkenyl or the like; R3 to R5 are each H, a hydrocarbon, a heterocyclic ring, halgencyano or the like.
Inventors:
Raymond Baker
Nail Roy Carteis
Jianatsutsu, Jozef Krugowski
Paul David Leeson
Mark Peter Ritzil
Adrian Leonard Smith
Nail Roy Carteis
Jianatsutsu, Jozef Krugowski
Paul David Leeson
Mark Peter Ritzil
Adrian Leonard Smith
Application Number:
JP3124194A
Publication Date:
February 10, 1998
Filing Date:
March 01, 1994
Export Citation:
Assignee:
Merck Sharp End Dome Limited
International Classes:
A61K31/44; A61K31/47; A61K31/495; A61K31/435; A61K31/535; A61K31/55; A61P25/18; C07D471/04; C07D519/00; C07D209/00; C07D221/00; (IPC1-7): C07D471/04; C07D519/00
Other References:
【文献】米国特許3362956(US,A)
Attorney, Agent or Firm:
Yoshio Kawaguchi (2 outside)