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1. WO1996032392 - ANELLATED $g(b)-CARBOLINES

Publication Number WO/1996/032392
Publication Date 17.10.1996
International Application No. PCT/DE1996/000632
International Filing Date 03.04.1996
Chapter 2 Demand Filed 09.10.1996
IPC
C07D 471/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 471/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
C07D 498/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
498Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
C07D 513/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
513Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/, C07D477/232
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
CPC
A61P 25/28
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 471/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
C07D 513/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
513Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
Applicants
  • SCHERING AKTIENGESELLSCHAFT [DE]/[DE] (AllExceptUS)
  • SEIDELMANN, Dieter [DE]/[DE] (UsOnly)
  • HUTH, Andreas [DE]/[DE] (UsOnly)
  • OLESEN, Preben, H. [DK]/[DK] (UsOnly)
  • OTTOW, Eckhard [DE]/[DE] (UsOnly)
  • TURNER, Jonathan [GB]/[DE] (UsOnly)
  • HILLMANN, Margrit [DE]/[DE] (UsOnly)
  • COLE, Belinda [GB]/[DE] (UsOnly)
Inventors
  • SEIDELMANN, Dieter
  • HUTH, Andreas
  • OLESEN, Preben, H.
  • OTTOW, Eckhard
  • TURNER, Jonathan
  • HILLMANN, Margrit
  • COLE, Belinda
Priority Data
195 14 524.012.04.1995DE
Publication Language German (DE)
Filing Language German (DE)
Designated States
Title
(DE) ANELLIERTE $g(b)-CARBOLINE
(EN) ANELLATED $g(b)-CARBOLINES
(FR) $g(b)-CARBOLINES ANNELEES
Abstract
(DE)
Es werden Verbindungen der Formel (I), worin A einen 5-6 gliedrigen ungesättigten Ring darstellt, in dem 1-2 C-Atome durch N, O und/oder S ersetzt sein können und der mit R5 und R6 substituiert sein kann, beschrieben sowie das Verfahren zu deren Herstellung. Die Verbindungen der Formel (I) sowie deren Salze sind auf Grund ihrer Affinität zu Benzodiazepin-Rezeptoren als Arzneimittel verwendbar. Sie besitzen unterschiedliche intrinsische Wirksamkeit (d.h. agonistische, antagonistische und/oder invers agonistische Wirksamkeit) an verschiedenen Isoformen des GABA-Benzodiazepin-Rezeptors.
(EN)
Described are compounds of formula (I), wherein A is a 5-6 membered unsaturated ring in which 1-2 C atoms can be substituted by N, O and/or S and which can be substituted with R5 and R6, and the method for preparing them. Because of their affinity for benzodiazepine receptors, the compounds of formula (I) as well as their salts can be used as drugs. They have different intrinsic efficacy (i.e. agonistic, antagonistic and/or inversely agonistic efficacy) with different isoforms of the GABA benzodiazepine receptor.
(FR)
L'invention concerne des composés de la formule (I) dans laquelle A désigne un composé cyclique insaturé à 5 ou 6 chaînons, dans lequel 1 à 2 atomes de C peuvent être substitués par N, O et/ou S, et qui peut être substitué par R5 et R6. L'invention concerne également leur procédé de préparation. Les composés de la formule (I) et leurs sels s'utilisent comme médicaments en raison de leur affinité envers les récepteurs de benzodiazépine. Ces composés présentent une efficacité intrinsèque différenciée (c.-à-d. efficacité agoniste, antagoniste et/ou inversement agoniste) sur diverses isoformes du récepteur de GABA-benzodiazépine.
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