Title:
ACRIDANONE DERIVATIVES
Document Type and Number:
Japanese Patent JPS59108783
Kind Code:
A
Abstract:
For the Contracting States BE CH DE FR GB IT LI LU NL SE 1. Acridanone derivatives of the general formula see diagramm : EP0110298,P20,F1 wherein the dotted line signifies an optional bond, R**1 signifies hydrogen, halogen or nitro, R**2 signifies hydrogen or lower alkyl, one of the symbols R**3 and R**4 signifies hydrogen or lower alkyl and the other together with R signifies an additional bond, A signifies lower alkylene, R**5 signifies a 5-membered, nitrogen-containig, optionally lower alkyl-substituted aromatic heterocycle, amino or a group see diagramm : EP0110298,P20,F2 or see diagramm : EP0110298,P20,F3 the symbol see diagramm : EP0110298,P20,F4 signifies a 5- or 6-membered, optionally lower-alkyl substituted saturated heterocycle which can contain as a ring member an oxygen or sulphur atom or the group >NH ou >N(B)n -A**1-R**6, B signifies the group -CO-, -COO- or -SO2 -, n signifies the number 0 or 1, A**1 signifies lower alkylene, R**6 signifies hydrogen, amino, lower alkylamino or di(lower alkyl)amino and R**7 signifies hydrogen or lower alkyl, and the residues denoted as lower contain 1 to 7 carbon atoms, and pharmaceutically acceptable acid addition salts thereof. For the Contracting State AT 1. A process for the manufacture of acridanone derivatives of the general formula see diagramm : EP0110298,P22,F1 wherein the dotted line signifies an optional bond, R**1 signifies hydrogen, halogen or nitro, R**2 signifies hydrogen or lower alkyl, one of the symbols R**3 and R**4 signifies hydrogen or lower alkyl and the other together with R signifies an additional bond, A signifies lower alkylene, R**5 signifies a 5-membered, nitrogen-containing, optionally lower alkyl-substituted aromatic heterocycle, amino or a group see diagramm : EP0110298,P23,F2 or see diagramm : EP0110298,P23,F3 the symbol see diagramm : EP0110298,P23,F4 signifies a 5- or 6-membered, optionally lower-alkyl substituted saturated heterocycle which can contain as a ring member an oxygen or sulphur atom or the group >NH ou >N(B)n -A**1-R**6, B signifies the group -CO-, -COO- or -SO2 -, n signifies the number 0 or 1, A**1 signifies lower alkylene, R**6 signifies hydrogen, amino, lower alkylamino or di(lower alkyl)amino and R**7 signifies hydrogen or lower alkyl, and the residues denoted as lower contains 1 to 7 carbon atoms, and pharmaceutically acceptable acid addition salts thereof, characterized by a) cyclizing a compound of the general formula see diagramm : EP0110298,P23,F5 wherein one of the symbols R**31 and R**41 signifies hydrogen or lower alkyl and the other signifies hydrogen, R**42 signifies hydrogen or lower alkyl, R**51 signifies a residue R**5, but does not contain a primary or secondary basic amino group, and X' signifies a leaving group, and R**1, R**2 and R**5 have the above significance, b) reacting a compound of the general formula see diagramm : EP0110298,P23,F6 wherein A, R**1, R**42 and R**51 have the above significance, with a compound of the general formula see diagramm : EP0110298,P23,F7 wherein X" signifies a leaving group and the dotted line and R**2 have the above significance, or c) reacting a compound of the general formula see diagramm : EP0110298,P23,F8 wherein Y(anion) signifies an anion and X signifies a leaving group, and A, R**1 and R**51 have the above significance, with a compound of the general formula see diagramm : EP0110298,P23,F9 wherein the dotted line, R, R**2, R**3 and R**4 have the above significance, or d) cleaving off the N-protecting group in a compound of the general formula see diagramm : EP0110298,P24,F10 wherein R**8 signifies a residue R**5 which contains a primary or secondary basic amino group blocked by a N-protecting group and the dotted line, R, R**1, R**2, R**3 and R**4 have the above significance, and e) if desired, converting a compound of formula I obtained into a pharmaceutically acceptable acid addition salt.
Inventors:
URUSU BUROMUBATSUHAA
HERUMUUTO RINKU
MARUKU MONTAFUON
HERUMUUTO RINKU
MARUKU MONTAFUON
Application Number:
JP22146083A
Publication Date:
June 23, 1984
Filing Date:
November 26, 1983
Export Citation:
Assignee:
HOFFMANN LA ROCHE
International Classes:
A61K31/00; A61K31/435; A61P33/10; C07D219/06; C07D219/10; C07D417/12; C07D417/14; (IPC1-7): A61K31/645; C07D417/12; C07D417/14
Attorney, Agent or Firm:
Heikichi Odashima