CN110200968A - 包含戊二酰亚胺衍生物的药物组合物及其用于治疗嗜酸细胞性疾病的用途 - Google Patents
包含戊二酰亚胺衍生物的药物组合物及其用于治疗嗜酸细胞性疾病的用途 Download PDFInfo
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Landscapes
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| RU2013150861 | 2013-11-14 | ||
| RU2013150861/15A RU2552929C1 (ru) | 2013-11-14 | 2013-11-14 | Фармацевтическая композиция, содержащая производные глутаримидов, и их применение для лечения эозинофильных заболеваний |
| CN201480062492.5A CN105722511B (zh) | 2013-11-14 | 2014-11-12 | 包含戊二酰亚胺衍生物的药物组合物及其用于治疗嗜酸细胞性疾病的用途 |
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| US7608693B2 (en) | 2006-10-02 | 2009-10-27 | Regeneron Pharmaceuticals, Inc. | High affinity human antibodies to human IL-4 receptor |
| CN118286417A (zh) | 2012-09-07 | 2024-07-05 | 瑞泽恩制药公司 | 以il-4r拮抗剂治疗特应性皮炎的方法 |
| EP3722290B1 (en) * | 2013-04-12 | 2023-06-21 | VALENTA-INTELLEKT Limited | Glutarimide derivative, use thereof, pharmaceutical composition based thereon and methods for producing the glutarimide derivative |
| TWI634900B (zh) | 2013-07-11 | 2018-09-11 | 再生元醫藥公司 | 藉由投與ｉｌ－４ｒ抑制劑治療嗜酸性食道炎的方法 |
| PT3110848T (pt) | 2014-09-24 | 2024-03-05 | Regeneron Pharma | Métodos para tratamento de infeção cutânea por administração de um antagonista do il-4r |
| KR102872485B1 (ko) | 2016-09-01 | 2025-10-20 | 리제너론 파아마슈티컬스, 인크. | Il-4r 길항제를 투여함에 의해 알레르기를 예방하거나 치료하기 위한 방법 |
| CN106539792B (zh) * | 2016-11-07 | 2017-08-25 | 王晓旭 | 一种治疗高血脂症的药物 |
| GEAP202115467A (en) | 2017-09-07 | 2021-10-11 | Obschestvo S Ogranichennoi Otvetstvennostiyu Pharmenterprises | Use of a glutarimide derivative to treat diseases related to the aberrant activity of cytokines |
| RU2712281C1 (ru) * | 2018-11-23 | 2020-01-28 | Общество С Ограниченной Ответственностью "Хемиммьюн Терапьютикс" | Применение производного глутаримида для преодоления резистентности к стероидам и терапии заболеваний, ассоциированных с аберрантным сигналингом интерферона гамма |
| KR20210143246A (ko) | 2019-03-21 | 2021-11-26 | 리제너론 파아마슈티컬스, 인크. | 알레르기 치료용 il-4/il-13 경로 억제제 및 형질 세포 절제의 병용 |
| JP7736667B2 (ja) | 2019-08-05 | 2025-09-09 | リジェネロン・ファーマシューティカルズ・インコーポレイテッド | Ｉｌ－４ｒアンタゴニストを投与することによるアトピー性皮膚炎の治療方法 |
| US11504426B2 (en) | 2019-08-05 | 2022-11-22 | Regeneron Pharmaceuticals, Inc. | Methods for treating allergy and enhancing allergen-specific immunotherapy by administering an IL-4R antagonist |
| BR112022019244A2 (pt) * | 2020-04-07 | 2022-11-08 | Hofseth Biocare Asa | Método para reduzir a função efetora de eosinófilos, artigo de fabricação e kit |
| TN2022000350A1 (en) * | 2020-06-26 | 2024-07-04 | Ltd “Valenta Intellekt” | Use of a glutarimide derivative for treating diseases associated with aberrant interleukin-6 activity |
| WO2023113650A1 (ru) * | 2021-12-15 | 2023-06-22 | Владимир Евгеньевич НЕБОЛЬСИН | Фармацевтическая композиция 1-[2-(1-метилимидазол-4-ил)-этил]пергидроазин-2,6-дион для терапии заболеваний верхних дыхательных путей |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106061962A (zh) * | 2013-04-12 | 2016-10-26 | 制药有限责任公司 | 戊二酰亚胺衍生物、其用途、基于所述衍生物的药物组合物及戊二酰亚胺衍生物的制备方法 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH02196767A (ja) * | 1988-10-11 | 1990-08-03 | Kyowa Hakko Kogyo Co Ltd | ヒドロキサム酸誘導体 |
| EP0564520A1 (en) | 1990-12-24 | 1993-10-13 | Merrell Dow Pharmaceuticals Inc. | Use of certain glutarimide derivatives in the treatment of depression and mania |
| AU6702894A (en) | 1993-04-09 | 1994-11-08 | Cell Therapeutics, Inc. | Ring-substituted cell signaling inhibitors |
| AUPO005496A0 (en) | 1996-05-24 | 1996-06-13 | Bresagen Limited | An interleukin-5 antagonist |
| RU2141483C1 (ru) | 1997-07-04 | 1999-11-20 | Небольсин Владимир Евгеньевич | Производные пептидов или их фармацевтически приемлемые соли, способ их получения, применение и фармацевтическая композиция |
| DE60230656D1 (de) | 2001-11-07 | 2009-02-12 | Cytos Biotechnology Ag | Antigenraster welche il-5, il-13 oder eotaxin präshilen erkrankungen |
| EP1741709A1 (en) | 2005-06-28 | 2007-01-10 | Sanofi-Aventis Deutschland GmbH | Heteroaryl-substituted amides comprising a saturated linker group, and their use as pharmaceuticals |
| WO2007007054A1 (en) | 2005-07-08 | 2007-01-18 | Cancer Research Technology Limited | Phthalamides, succinimides and related compounds and their use as pharmaceuticals |
| PT3072525T (pt) | 2007-05-14 | 2018-04-20 | Astrazeneca Ab | Métodos para reduzir os níveis de basófilos |
| RU2406727C2 (ru) * | 2008-02-13 | 2010-12-20 | Общество С Ограниченной Ответственностью "Фарминтерпрайсез" | Фармацевтическая композиция, содержащая n-ацильные производные аминокислот, и их применение в качестве противоаллергических, антианафилактических и противовоспалительных средств |
| RU2378284C2 (ru) * | 2008-02-13 | 2010-01-10 | Общество С Ограниченной Ответственностью "Фарминтерпрайсез" | Способы получения n-ацильных производных аминокислот (варианты) |
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