CN113101292B - 双炔失碳酯组合物和疾病治疗方法 - Google Patents
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| CN105279394B (zh) * | 2015-10-13 | 2017-12-26 | 山西农业大学 | 用于神经肽受体筛选的方法 |
| JP6788255B2 (ja) * | 2015-11-19 | 2020-11-25 | 国立大学法人信州大学 | 新規ベクター及びこれを用いた可溶化タンパク質の製造方法 |
| IL284875B (en) | 2016-10-11 | 2022-07-01 | Univ Duke | Zofoxifene treatment for breast cancer |
| US11040054B2 (en) | 2016-11-14 | 2021-06-22 | The Brigham And Women's Hospital, Inc. | Estrogen sensing through GPER1 regulates normal and malignant liver growth |
| EP3568132B1 (en) | 2017-01-10 | 2025-12-03 | Wang, Wei | Lasofoxifene modulation of membrane-initiated estrogen signals and methods for tumor treatment |
| WO2019041078A1 (en) * | 2017-08-28 | 2019-03-07 | Zhejiang Jiachi Pharmaceutical Development Ltd. | ASYMMETRIC SYNTHESIS AND USES OF COMPOUNDS IN TREATMENT OF DISEASES |
| CN109662968B (zh) * | 2017-10-13 | 2021-05-18 | 上海奥奇医药科技有限公司 | 含A-失碳-5α雄甾烷化合物的升白制剂及其应用 |
| EP3773524B1 (en) | 2018-04-10 | 2025-04-09 | Duke University | Lasofoxifene for the treatment of er+ breast cancer carrying the mutation d538g or y537s |
| CN111773388B (zh) * | 2019-04-04 | 2023-07-18 | 上海奥奇医药科技有限公司 | A-失碳-5α雄甾烷化合物类药物与抗癌药物的联合应用 |
| US20210299098A1 (en) * | 2020-03-31 | 2021-09-30 | Cipla Limited | Selective estrogen receptor modulator for treatment of pancreatic cancer |
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| GB202116903D0 (en) | 2021-11-18 | 2022-01-05 | Sermonix Pharmaceuticals Inc | Lasofoxifene treatment of aromatase-resistant er+ cancer |
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| US5001120A (en) * | 1989-05-10 | 1991-03-19 | Natural Pharmacia International, Inc. | Use of A-Nor-steroids as malignant cells growth inhibitors |
| CN101987081A (zh) * | 2010-07-16 | 2011-03-23 | 钟术光 | 一种控释制剂 |
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| MXPA05003054A (es) * | 2002-09-20 | 2005-05-27 | Pfizer Prod Inc | Ligandos de amida y sulfonamida para el receptor de estrogenos. |
| WO2005048942A2 (en) * | 2003-11-13 | 2005-06-02 | Pharmacia Corporation | Combination therapy comprising a cox-2 inhibitor and an antineoplastic agent |
| JP2008505079A (ja) * | 2004-06-30 | 2008-02-21 | メルク エンド カムパニー インコーポレーテッド | エストロゲン受容体調節剤 |
| US20090215731A1 (en) | 2005-10-19 | 2009-08-27 | Chavah Pty Ltd. | Reduction of Side Effects From Aromatase Inhibitors Used for Treating Breast Cancer |
| CN101297970A (zh) * | 2006-03-17 | 2008-11-05 | 山东蓝金生物工程有限公司 | 同载抗代谢药物及其增效剂的抗癌缓释注射剂 |
| WO2007129062A1 (en) | 2006-05-08 | 2007-11-15 | Astex Therapeutics Limited | Pharmaceutical combinations of diazole derivatives for cancer treatment |
| US9220771B2 (en) | 2010-07-16 | 2015-12-29 | Merck Patent Gmbh | Peptide for use in the treatment of breast cancer and/or bone metastases |
| CN103562226A (zh) | 2011-03-11 | 2014-02-05 | 梅里麦克制药股份有限公司 | 使用egfr家族受体的抑制剂来治疗激素难治性乳腺癌 |
| CN102218069B (zh) * | 2011-04-08 | 2012-09-26 | 上海奥奇医药科技有限公司 | A-失碳-5α-雄甾烷化合物在制备抗恶性肿瘤药物中的应用 |
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5001120A (en) * | 1989-05-10 | 1991-03-19 | Natural Pharmacia International, Inc. | Use of A-Nor-steroids as malignant cells growth inhibitors |
| CN101987081A (zh) * | 2010-07-16 | 2011-03-23 | 钟术光 | 一种控释制剂 |
Non-Patent Citations (4)
| Title |
|---|
| Whole body correction of mucopolysaccharidosis IIIA by intracerebrospinal fluid gene therapy;Virginia Haurigot et al.,;《The Journal of Clinical Investigation》;第123卷(第8期);第3254-3271页 * |
| α-双炔失碳酯及其代谢产物双炔失碳醇的体外抗肿瘤作用比较;顾健,胥彬;肿瘤(第02期);全文 * |
| α-双炔失碳酯对人卵巢癌细胞生长的影响及其与ER的关系;冯炜炜,曹斌融,丰有吉;现代妇产科进展(第04期);全文 * |
| 米非司酮和米索前列醇配伍双炔失碳酯减少药物流产失血量的研究;黄晓燕,林小娜,陈湫波;宁波医学(第04期);全文 * |
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| US10857158B2 (en) | 2020-12-08 |
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| US20190262360A1 (en) | 2019-08-29 |
| US20210069212A1 (en) | 2021-03-11 |
| EP3139928A1 (en) | 2017-03-15 |
| CN111956653B (zh) | 2023-06-30 |
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