On April 4, 2000, Suzuki, Nobuhiro; Takekawa, Shiro; Kubo, Keiji; Imaeda, Yasuhiro published a patent.Product Details of 29704-38-9 The title of the patent was Preparation of imidazole derivatives as gonadotropin-releasing hormone antagonists. And the patent contained the following:
Claimed are gonadotropin-releasing hormone (GnRH) antagonists containing the title compounds [I; ring A = (un)substituted Ph; ring B = (un)substituted cyclic group; R4 , R6 = H, (un)substituted C1-6 alkyl, C2-6 alkenyl, C3-7 cycloalkyl, (un)substituted C7-13 aralkyl, C2-7 alkoxycarbonyl; R5 = H, halo, (un)substituted C1-6 alkyl, C1-6 alkoxy, C2-7 alkoxycarbonyl, etc.; X = bond, C1-6 alkylene, C2-6 alkenylene, C1-6 alkylene-NHCO, C1-6 alkylene-O2NH; Y = CO, SO2, NHCO, C1-6 alkylene-CO, C2-6 alkylene-CO, C1-6 alkylene] or pharmacol. acceptable salts thereof. These compounds are useful for the treatment or prevention of gonadotropin-releasing hormone-related diseases such as sex hormone-dependent cancer, prostate cancer, uterine cancer, breast cancer, prostatic hypertrophy, true precocious puberty, endometriosis, hysteromyoma, pregnancy regulators, and menstruation regulators. Thus, 5-amino-2-(4-methoxyphenyl)benzimidazole was condensed with 4-pyrrolidinobenzoic acid using di-Et cyanophosphate in the presence of Et3N and 4-dimethylaminopyridine in DMF at room temperature for 1 h to give 41% 2-(4-methoxyphenyl)-5-((4-pyrrolidinobenzoyl)amino)benzimidazole (II). II in vitro showed IC50 of μg/mL for inhibiting the binding of [125I]leuprolelin to a membrane sample of CHO cell expressing human GnRH receptor. The experimental process involved the reaction of tert-Butyl 2-(4-nitrophenyl)acetate(cas: 29704-38-9).Product Details of 29704-38-9
The Article related to antitumor agents, benign prostatic hyperplasia, endometriosis, mammary gland neoplasm, menstruation (regulators), myoma (hysteromyoma), neoplasm (sex hormone-dependent), precocious puberty (true), pregnancy (regulators), prostate gland neoplasm, uterus neoplasm and other aspects.Product Details of 29704-38-9
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