PROPANE-1,3-DION DERIVATIVE OR SALT THEREOF

It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by -SO 2 -R 3 in a propane-1,3-dione...

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Main Authors ISAO KINOYAMA, TAKASHI SHIN, TATSUHISA TAKAHASHI, ITSURO SHIMADA, HIROFUMI YAMAMOTO, KEI OHNUKI, TAKANORI KOIKE, TOSHIYUKI KUSAYAMA, HIROYUKI HISAMICHI, KAZUHIKO OSODA, MASAAKI HIRANO, EIJI KAWAMINAMI, SHUNICHIRO MATSUMOTO
Format Patent
LanguageEnglish
Portuguese
Published 04.01.2013
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by -SO 2 -R 3 in a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.
Bibliography:Application Number: PT20060730589T