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1. WO2005048916 - TETRAHYDROSPIRO-BETA-CARBOLINE-1,3 '-PYRROLIDINE DERIVATIVES AND THEIR USE IN GHSR-RELATED DISORDERS

Publication Number WO/2005/048916
Publication Date 02.06.2005
International Application No. PCT/SE2004/001688
International Filing Date 18.11.2004
Chapter 2 Demand Filed 02.06.2005
IPC
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 471/18 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
18Bridged systems
C07D 471/22 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
22in which the condensed systems contains four or more hetero rings
C07D 491/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
C07D 491/20 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
12in which the condensed system contains three hetero rings
20Spiro-condensed systems
C07D 491/22 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
22in which the condensed system contains four or more hetero rings
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
A61P 3/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 5/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5Drugs for disorders of the endocrine system
06of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
08for decreasing, blocking or antagonising the activity of the anterior pituitary hormones
A61P 9/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
A61P 9/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
10for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Applicants
  • BIOVITRUM AB [SE]/[SE] (AllExceptUS)
  • BRANDT, Peter [SE]/[SE] (UsOnly)
  • BREMBERG, Ulf [SE]/[SE] (UsOnly)
  • CROSSLEY, Roger [GB]/[GB] (UsOnly)
  • GRAFFNER NORDBERG, Malin [SE]/[SE] (UsOnly)
  • JENMALM JENSEN, Annika [SE]/[SE] (UsOnly)
  • RINGBERG, Erik [SE]/[SE] (UsOnly)
  • WARD, Terry [GB]/[GB] (UsOnly)
Inventors
  • BRANDT, Peter
  • BREMBERG, Ulf
  • CROSSLEY, Roger
  • GRAFFNER NORDBERG, Malin
  • JENMALM JENSEN, Annika
  • RINGBERG, Erik
  • WARD, Terry
Agents
  • HÖGLUND, Lars
Priority Data
0303078-020.11.2003SE
60/560,69008.04.2004US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) TETRAHYDROSPIRO-BETA-CARBOLINE-1,3 '-PYRROLIDINE DERIVATIVES AND THEIR USE IN GHSR-RELATED DISORDERS
(FR) NOUVELLES CARBOLINES-BETA EN TANT QU'ANTAGONISTES DE RECEPTEUR DE SECRETAGOGUE D'HORMONE DE CROISSANCE
Abstract
(EN)
The present invention relates to compounds of Formula (I): Formula (I) wherein R3-R8, X, and Y 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, acromegaly and cancer, in particular breast, lung, prostate, thyroid and endocrine pituary carcinomas.
(FR)
La présente invention a trait à des composés de formule (I), dans laquelle : R3-R8, X et Y sont tels que définis dans la description, à des procédés pour la préparation des composés, à des compositions pharmaceutiques comportant les composés, et à l'utilisation des composés et des compositions dans la prophylaxie ou le traitement de trouble lié au récepteur de sécrétagogue d'hormone de croissance. Des exemples de tels troubles sont l'obésité et des troubles associés tels que le diabète de type II, la dyslipidémie et le syndrome métabolique du syndrome Prader-Willi, des maladies cardio-vasculaires telles que la maladie vasculaire athérosclérotique, l'angine de poitrine, l'infarctus du myocarde et l'accident cérébrovasculaire, l'acromégalie et le cancer, notamment les carcinomes mammaire, pulmonaire, prostatique, thyroïdien et endocrinien hypophysaire.
Also published as
Latest bibliographic data on file with the International Bureau