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1. 发明授权

US06255339B1 Tetrahydronaphthofuranone derivatives and process for producing the same 失效
标题翻译：四氢萘并呋喃酮衍生物及其制备方法
公开(公告)号：US06255339B1
公开(公告)日：2001-07-03
申请号：US09117070
申请日：1998-07-21
申请人： Kenichi Kurihara , Rie Shinei , Kiyoshi Tanabe , Yasuo Yamamoto , Keiichi Ajito , Kaori Miyajima , Yuji Tabata , Shohei Yasuda , Kuniaki Tatsuta , Tsuneo Okonogi
发明人： Kenichi Kurihara , Rie Shinei , Kiyoshi Tanabe , Yasuo Yamamoto , Keiichi Ajito , Kaori Miyajima , Yuji Tabata , Shohei Yasuda , Kuniaki Tatsuta , Tsuneo Okonogi
IPC分类号： A61K3134
CPC分类号： C07D307/92 , C07D407/12 , C07D407/14 , C07D409/12 , C07D417/12
摘要： Compounds represented by the following formula (I) and pharmaceutically acceptable salts thereof are disclosed. The compounds have progesterone receptor binding inhibitory activity and, hence, can be used as therapeutic and prophylactic agents for progesterone-related diseases. Specifically, they are useful as abortifacients, oral contraceptive pills, carcinostatic agents for breast cancer and ovarian cancer, therapeutic agents for endometriosis, meningioma, and myeloma, and therapeutic and prophylactic agents for osteoporosis and climacteric disturbance. wherein R1 and R2 represent a hydroxyl group, alkyloxy, alkenyloxy, alkynyloxy, cycloalkyloxy, alkoxyalkyloxy, cycloalkyloxy containig one oxygen atom, aralkyloxy, alkylcarbonyloxy, alkenylcarbonyloxy, alkynylcarbonyloxy, cycloalkylcarbonyloxy, alkoxycarbonyloxy, aryloxy carbonyloxy, aralkylcarbonyloxy, aromatic acyloxy, heteroaromatic acyloxy, saturated heterocyclic carbonyloxy, alkylsulfonyloxy, aromatic sulfonyloxy, alkylcarbamoyloxy, aromatic carbamoyloxy, alkylcarbonylamino, or aromatic acylamino, provided that R1 may further represent a hydrogen atom, alkyl, alkenyl, or alkynyl; and R3, R4, and R5 each independently represent a hydrogen atom, alkyl or alkenyl.
摘要翻译：公开了由下式（I）表示的化合物及其药学上可接受的盐。所述化合物具有孕酮受体结合抑制活性，因此可用作孕酮相关疾病的治疗和预防剂。具体地说，它们可用作流产者，口服避孕药，乳腺癌和卵巢癌的制癌剂，子宫内膜异位症的治疗剂，脑膜瘤和骨髓瘤，以及骨质疏松症和更年期障碍的治疗和预防剂。其中R1和R2表示羟基，烷氧基，链烯氧基，炔氧基，环烷氧基，烷氧基烷氧基，含有一个氧原子的环烷氧基，芳烷氧基，烷基羰基氧基，链烯基羰基氧基，炔基羰氧基，环烷基羰基氧基，烷氧基羰基氧基，芳氧基羰基氧基，芳烷基羰基氧基，芳香酰氧基，杂芳基酰氧基，饱和杂环羰氧基，烷基磺酰氧基，芳香磺酰氧基，烷基氨基甲酰氧基，芳族氨基甲酰氧基，烷基羰基氨基或芳族酰氨基，条件是R 1可以进一步代表氢原子，烷基，烯基或炔基; 并且R 3，R 4和R 5各自独立地表示氢原子，烷基或链烯基。

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