CN114105977A - ***受体调节剂化合物及其用途 - Google Patents
***受体调节剂化合物及其用途 Download PDFInfo
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- CN114105977A CN114105977A CN202110997502.6A CN202110997502A CN114105977A CN 114105977 A CN114105977 A CN 114105977A CN 202110997502 A CN202110997502 A CN 202110997502A CN 114105977 A CN114105977 A CN 114105977A
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- Prior art keywords
- cycloalkyl
- radical
- compound
- pharmaceutically acceptable
- acceptable salt
- Prior art date
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- 238000005481 NMR spectroscopy Methods 0.000 description 4
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
Abstract
Description
测试化合物 | ER水平DC<sub>50</sub>(nM) | 最大ER下调率(%) |
实施例1 | 0.07 | 103.36 |
实施例2 | 0.14 | 95.76 |
实施例3 | 0.45 | 79.50 |
实施例4 | 0.12 | 95.84 |
实施例5 | 0.36 | 90.21 |
实施例6 | 0.23 | 84.93 |
实施例7 | 0.22 | 90.95 |
实施例8 | 0.31 | 95.37 |
实施例9 | 0.22 | 107.81 |
测试化合物 | T47D IC<sub>50</sub>(nM) |
实施例1 | 0.17 |
化合物编号 | MCF-7细胞增殖抑制IC<sub>50</sub>(nM) |
实施例1 | 0.07 |
Claims (13)
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CN107108611A (zh) * | 2014-12-18 | 2017-08-29 | 豪夫迈·罗氏有限公司 | 四氢‑吡啶并[3,4‑b]吲哚***受体调节剂及其用途 |
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