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1. WO2013041458 - FSH RECEPTOR ANTAGONISTS

Publication Number WO/2013/041458
Publication Date 28.03.2013
International Application No. PCT/EP2012/068080
International Filing Date 14.09.2012
IPC
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic 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
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic 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
12
in which the condensed system contains three hetero rings
14
Ortho-condensed systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15
Drugs for genital or sexual disorders; Contraceptives
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
4353
ortho- or peri-condensed with heterocyclic ring systems
437
the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
4353
ortho- or peri-condensed with heterocyclic ring systems
4375
the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4427
containing further heterocyclic ring systems
444
containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
47
Quinolines; Isoquinolines
4738
ortho- or peri-condensed with heterocyclic ring systems
4745
condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506
not condensed and containing further heterocyclic rings
C07D 471/04 (2006.01)
C07D 471/14 (2006.01)
A61P 15/00 (2006.01)
A61K 31/437 (2006.01)
A61K 31/4375 (2006.01)
A61K 31/444 (2006.01)
CPC
A61K 31/4375
A61K 31/4745
C07D 471/04
C07D 471/14
Applicants
  • MERCK SHARP & DOHME B.V. [NL/NL]; Waardeweg 39 NL-2031 BN Haarlem, NL (AllExceptUS)
  • BLACKABY, Wesley, Peter [GB/GB]; GB (UsOnly)
  • DE KORT, Martin [NL/NL]; NL (UsOnly)
  • ENTHOVEN, Mark [NL/NL]; NL (UsOnly)
  • HINCHLIFFE, Paul, Stuart [GB/GB]; GB (UsOnly)
  • POULIE, Christian Bernard Matthijs [NL/NL]; NL (UsOnly)
  • TIMMERS, Cornelis, Marius [NL/NL]; NL (UsOnly)
  • VERKAIK, Saskia [NL/NL]; NL (UsOnly)
Inventors
  • BLACKABY, Wesley, Peter; GB
  • DE KORT, Martin; NL
  • ENTHOVEN, Mark; NL
  • HINCHLIFFE, Paul, Stuart; GB
  • POULIE, Christian Bernard Matthijs; NL
  • TIMMERS, Cornelis, Marius; NL
  • VERKAIK, Saskia; NL
Agents
  • JAAP, David, Robert; Merck Sharp & Dohme Ltd Hertford Road Hoddesdon Hertfordshire EN11 9BU, GB
Priority Data
11182306.822.09.2011EP
61/537,65322.09.2011US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) FSH RECEPTOR ANTAGONISTS
(FR) ANTAGONISTES DU RÉCEPTEUR DE LA FSH
Abstract
(EN)
The invention relates to FSH receptor antagonist according to general formula (I) or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders.
(FR)
L'invention concerne un antagoniste du récepteur de la FSH de formule générale (I) ou un sel pharmaceutiquement acceptable de celui-ci, ainsi qu'une composition pharmaceutique le contenant. Ces composés peuvent être utilisés pour le traitement et la prévention de l'endométriose, pour le traitement et la prévention du cancer du sein hormono-dépendant pré-ménopausique et péri-ménopausique, pour la contraception et pour le traitement de fibromes utérins et d'autres troubles liés au cycle menstruel.
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