174069-67-1Relevant articles and documents
Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists
Imada, Takashi,Cho, Nobuo,Imaeda, Toshihiro,Hayase, Yoji,Sasaki, Satoshi,Kasai, Shizuo,Harada, Masataka,Matsumoto, Hirokazu,Endo, Satoshi,Suzuki, Nobuhiro,Furuya, Shuichi
, p. 3809 - 3825 (2007/10/03)
Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one-based non-peptide luteinizing hormone-releasing hormone (LHRH) receptor antagonists are described. Starting with the thienopyridin-4-one derivative 26d (T-98475) an optimization study was performed, which resulted in the identification of a highly potent and orally bioavailable LHRH receptor antagonist, 3-(N-benzyl-N-methylaminomethyl)-7-(2,6- difluorobenzyl)-4,7-dihydro-2-[4-(1-hydroxy-1-cyclopropanecarboxamido)phen-yl] -5-isobutyryl-4-oxothieno[2,3-b]pyridine (33c). Compound 33c displayed subnanomolar in vitro activities for the human receptor and its oral administration caused effective suppression of the plasma LH levels in castrated male cynomolgus monkeys. Furthermore, SAR studies revealed that a hydroxyalkylamido moiety on the 2-phenyl ring is virtually equivalent to an alkylureido moiety, at least in this series of compounds.
Prolactin production inhibitory agent
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, (2008/06/13)
The prolactin production inhibition agent of the present invention containing a condensed cyclic compound, which is characterized by containing a condensed bicyclic structure of an optionally substituted homo or hetero 5- to 7-membered ring with an optionally substituted homo or hetero 5- to 7-membered ring, or a salt thereof, can be used, as a medicine, for the prophylaxis or therapy of diseases accompanied with an excess prolactin production or diseases having enhanced reactivity with prolactin, or is useful for inhibiting puerperal lactation, and also useful as a prophylactic or therapeutic agent of galactorrhea, hyperprolactinemic ovulation disturbance, amenorrhea-galactorrhea syndrome, prolactinoma, and besides, interbrain tumor, and acromegaly, pituitary gigantism.