首页> 外国专利> 5- 2-hydroxy-3-1-(3-trifluoromethylphenyl)-cyclopropyl-propionylamino -phtalide and 6- 2-hydroxy-3-1-(3-trifluoromethylphenyl)-cyclopropyl-propionylamino -4-methyl-2,3-benzoxazin-1-one derivatives with progesterone receptor modulating activity for use in fertility control, hormone replacement therapy and the treatment of gynecological disorders

5- 2-hydroxy-3-1-(3-trifluoromethylphenyl)-cyclopropyl-propionylamino -phtalide and 6- 2-hydroxy-3-1-(3-trifluoromethylphenyl)-cyclopropyl-propionylamino -4-methyl-2,3-benzoxazin-1-one derivatives with progesterone receptor modulating activity for use in fertility control, hormone replacement therapy and the treatment of gynecological disorders

机译：5- 2-羟基-3- [1-（3-三氟甲基苯基）-环丙基]-丙酰氨基-邻苯二甲酸酯和6--2-羟基-3- [1-（3-三氟甲基苯基）-环丙基]-丙酰氨基-4-甲基-具有黄体酮受体调节活性的2,3-苯并恶嗪-1-酮衍生物，用于生育控制，激素替代疗法和妇科疾病的治疗

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The present invention relates to non-steroidal progestins of the general formula (I) whereinR₁ and R₂ are independently of each other -H or -F,R₃ is -CH₃ or -CF₃, andAr is or a pharmaceutically acceptable derivative or analogue thereof. These progestins are suitable for selectively modulating progesterone receptor mediated effects in different target tissues, particularly in uterine tissue versus breast tissue. Therefore, the progestins of the present invention, optionally in combination with estrogens, may be used for contraception, hormone replacement therapy and the treatment of gynecological disorders. The present invention furthermore relates to methods for selectively modulating progesterone receptor mediated effects in different target tissues or organs.

机译：本发明涉及通式（I）的非甾体孕激素 <图像文件=“ IMGA0001.GIF” he =“ 36” id =“ ia01” imgContent =“ chem” imgFormat =“ GIF” wi =“ 72” /> R _{1 和R _{2 彼此独立-H或-F，R _{3 是-CH _{3 或-CF _{3 ，并且Ar是 <图像文件=“ IMGA0002.GIF” he =“ 42” id =“ ia02” imgContent =“ chem” imgFormat =“ GIF” wi =“ 92” /> 或药学上可接受的衍生物或其类似物。这些孕激素适用于选择性调节不同靶组织，特别是子宫组织对乳腺组织中孕激素受体介导的作用。因此，本发明的孕激素，任选地与雌激素组合，可以用于避孕，激素替代疗法和妇科疾病的治疗。本发明还涉及在不同靶组织或器官中选择性调节孕酮受体介导的作用的方法。}}}}} 展开▼

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公开/公告号EP1344776A1

专利类型

公开/公告日2003-09-17

原文格式PDF

申请/专利权人 SCHERING AKTIENGESELLSCHAFT;
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申请/专利号EP20020005530

发明设计人 SCHMEES NORBERT;LEHMANN MANFRED;FUHRMANN ULRIKE;MUHN PETER;HEGELE-HARTUNG CHRISTA;KLOTZBÜCHER MICHAEL;
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申请日2002-03-11

分类号C07D265/02;C07D307/88;A61K31/535;A61K31/365;

国家 EP

入库时间 2022-08-21 23:49:01

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