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1. WO2006122931 - BETA-CARBOLINE DERIVATIVES AND THERI USE AS GHSR MODULATORS

Publication Number WO/2006/122931
Publication Date 23.11.2006
International Application No. PCT/EP2006/062343
International Filing Date 16.05.2006
IPC
C07D 471/20 2006.1
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
20Spiro-condensed systems
A61K 31/438 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
438the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61P 3/04 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
04Anorexiants; Antiobesity agents
CPC
A61P 3/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
04Anorexiants; Antiobesity agents
C07D 471/20
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
20Spiro-condensed systems
Applicants
  • BIOVITRUM AB (PUBL) [SE]/[SE] (AllExceptUS)
  • GRAFFNER NORDBERG, Malin [SE]/[SE] (UsOnly)
  • BARF, Tjeerd [NL]/[NL] (UsOnly)
  • MOTT, Andrew [GB]/[SE] (UsOnly)
Inventors
  • GRAFFNER NORDBERG, Malin
  • BARF, Tjeerd
  • MOTT, Andrew
Agents
  • HÖGLUND, Lars
Priority Data
0501148-120.05.2005SE
60/692,33920.06.2005US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) BETA-CARBOLINE DERIVATIVES AND THERI USE AS GHSR MODULATORS
(FR) DERIVES DE BETA-CARBOLINE ET LEUR UTILISATION COMME MODULATEURS DE GHSR
Abstract
(EN) The present invention relates to compounds of Formula (I): wherein R1 to R3 are as described herein, processes for preparing the compounds, pharmaceutical compositions comprising the compounds, and use of the compounds and compositions in the prophylaxis or treatment of a GHSR receptor-related disorder. Examples of such disorders are obesity and related disorders such as diabetes type II, dyslipidemia and the metabolic syndrome Prader-Willi syndrome, cardiovascular diseases such as atherosclerotic vascular disease, angina pectoris, myocardial infarction and stroke, intestinal inflammation that is associated with inflammatory bowel diseases (IBD) such as Crohn's disease and ulcerative colitis, acromegaly and cancer, in particular breast, lung, prostate, thyroid and endocrine pituary carcinomas.
(FR) La présente invention concerne des composés de formule (I), dans laquelle R1 à R3 sont tels que définis dans la description, des procédés de préparation de ces composé, des compositions pharmaceutiques renfermant ces composés, ainsi que l'utilisation de ces composés et de ces compositions dans la prévention ou le traitement d'un trouble associé au récepteur GHSR. Par exemple, ces troubles incluent l'obésité et des troubles associés tels que le diabète de type II, la dyslipidémie et le syndrome de Prader-Willi métabolique, les maladies cardiovasculaires telles que la maladie vasculaire athérosclérotique, l'angine de poitrine, l'infarctus du myocarde et l'accident cérébrovasculaire, l'inflammation intestinale associée aux maladies du côlon inflammatoires (MII) telles que la maladie de Crohn et la rectocolite hémorragique, l'acromégalie et le cancer, notamment du sein, du poumon, de la prostate et de la thyroïde, ainsi que les carcinomes pituitaires endocriniens.
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