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1. WO2011076687 - PYRIDINONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF

Publication Number WO/2011/076687
Publication Date 30.06.2011
International Application No. PCT/EP2010/070092
International Filing Date 17.12.2010
IPC
C07D 498/04 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
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 513/04 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
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/437 2006.01
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
4353ortho- or peri-condensed with heterocyclic ring systems
437the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61P 5/04 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5Drugs for disorders of the endocrine system
02of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
04for decreasing, blocking or antagonising the activity of the hypothalamic hormones
CPC
A61P 15/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 37/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
A61P 5/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5Drugs for disorders of the endocrine system
02of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
04for decreasing, blocking or antagonising the activity of the hypothalamic hormones
C07D 498/04
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
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 513/04
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
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Applicants
  • BAYER PHARMA AKTIENGESELLSCHAFT [DE]/[DE] (AllExceptUS)
  • HÜBNER, Jan [DE]/[DE] (UsOnly)
  • WEGSCHEID-GERLACH, Christof [DE]/[DE] (UsOnly)
  • PANKNIN, Olaf [DE]/[DE] (UsOnly)
  • RING, Sven [DE]/[DE] (UsOnly)
  • BÄURLE, Stefan [DE]/[DE] (UsOnly)
  • HUWE, Christoph [DE]/[DE] (UsOnly)
  • NOWAK, Katrin [DE]/[DE] (UsOnly)
  • NUBBEMEYER, Reinhard [DE]/[DE] (UsOnly)
  • MUHN, Hans-Peter [DE]/[DE] (UsOnly)
Inventors
  • HÜBNER, Jan
  • WEGSCHEID-GERLACH, Christof
  • PANKNIN, Olaf
  • RING, Sven
  • BÄURLE, Stefan
  • HUWE, Christoph
  • NOWAK, Katrin
  • NUBBEMEYER, Reinhard
  • MUHN, Hans-Peter
Common Representative
  • BAYER PHARMA AKTIENGESELLSCHAFT
Priority Data
09075567.922.12.2009EP
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PYRIDINONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF
(FR) DÉRIVÉS DE PYRIDINONE ET COMPOSITIONS PHARMACEUTIQUES ASSOCIÉES
Abstract
(EN)
Pyridinone derivatives, process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially sex-hormone-related conditions in both men and women, as well as a mammal in general (also referred to herein as a "subject"). For example, such conditions include endometriosis, uterine fibroids, polycystic ovarian disease, heavy menstrual bleeding, particularly menorrahagia and dysmenorrehea, hirsutism, precocious puberty, gonadal steroid-dependent neoplasia such as cancers of the prostate, breast and ovary, gonadotrope pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hypertrophy, contraception and infertility (e.g., assisted reproductive therapy such as in vitro fertilization). The present application relates in particular to pyridinone derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists.
(FR)
L'invention concerne des dérivés de pyridinone, un procédé pour les préparer, leur utilisation pour le traitement et/ou la prophylaxie de maladies, et leur utilisation pour la fabrication de médicaments pour le traitement et/ou la prophylaxie de maladies, en particulier des affections liées aux hormones sexuelles chez les hommes et les femmes ainsi que chez un mammifère en général (également désigné ici par « sujet »). Par exemple, ces affections comprennent l'endométriose, les fibromyomes utérins, une polykystose ovarienne, des saignements menstruels abondants, en particulier, ménorragie et dysménorrhée, l'hirsutisme, la puberté précoce, une néoplasie gonadique dépendante des stéroïdes, comme des cancers de la prostate, du sein et de l'ovaire, les adénomes hypophysaires gonadotropes, l'apnée du sommeil, le syndrome de l'intestin irritable, le syndrome prémenstruel, l'hypertrophie bénigne de la prostate, la contraception et la stérilité (par exemple, thérapie de procréation assistée, comme la fécondation in vitro). La présente demande concerne en particulier des dérivés de pyridinone comme des antagonistes de récepteur de gonadolibérine (GnRH).
Also published as
Latest bibliographic data on file with the International Bureau