TWI702953B - 包含ａｚｄ９２９１之醫藥組合物及錠劑以及其用途 - Google Patents
包含ａｚｄ９２９１之醫藥組合物及錠劑以及其用途 Download PDFInfo
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- TWI702953B TWI702953B TW103146652A TW103146652A TWI702953B TW I702953 B TWI702953 B TW I702953B TW 103146652 A TW103146652 A TW 103146652A TW 103146652 A TW103146652 A TW 103146652A TW I702953 B TWI702953 B TW I702953B
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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- A—HUMAN NECESSITIES
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- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
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| GB201400034D0 (en) * | 2014-01-02 | 2014-02-19 | Astrazeneca Ab | Pharmaceutical Compositions comprising AZD9291 |
| NO2699580T3 (enExample) | 2014-01-24 | 2018-02-24 | ||
| CN109311858B (zh) | 2016-05-26 | 2021-12-03 | 里科瑞尔姆Ip控股有限责任公司 | Egfr抑制剂化合物 |
| CN108057036B (zh) * | 2016-11-07 | 2023-06-13 | 正大天晴药业集团股份有限公司 | 一种egfr抑制剂的固体药物组合物 |
| CN107176954B (zh) * | 2017-06-02 | 2019-01-11 | 无锡双良生物科技有限公司 | 一种egfr抑制剂的药用盐及其晶型、制备方法和应用 |
| CN110013468B (zh) * | 2018-01-09 | 2022-02-18 | 北京福元医药股份有限公司 | 一种azd9291氘代衍生物药物制剂 |
| WO2019138346A1 (en) * | 2018-01-10 | 2019-07-18 | Alembic Pharmaceuticals Limited | Pharmaceutical composition of osimertinib |
| MA51823A (fr) * | 2018-02-12 | 2021-05-19 | Astrazeneca Ab | Osimertinib destiné à être utilisé dans le traitement du cancer du poumon non à petites cellules |
| SI3758708T1 (sl) * | 2018-03-01 | 2025-04-30 | Astrazeneca Ab | Farmacevtski sestavki, ki vsebujejo (2S)-{(1S)-1-ciano-2-[4-(3-metil-2-okso-2,3-dihidro-1,3-benzoksazol-5-il)fenil]etil}-1,4-oksazepan-2-karboksamid |
| KR102511672B1 (ko) * | 2018-03-23 | 2023-03-17 | 우시 상량 바이오테크놀로지 씨오., 엘티디. | 의약 조성물, 그 제조방법 및 사용 |
| CA3106269A1 (en) | 2018-07-17 | 2020-01-23 | Insmed Incorporated | Certain (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides for treating lupus nephritis |
| KR20200043618A (ko) * | 2018-10-18 | 2020-04-28 | 주식회사유한양행 | 아미노피리미딘 유도체 또는 이의 염을 포함하는 경구투여용 약학 조성물 |
| CN113645976A (zh) | 2019-03-29 | 2021-11-12 | 阿斯利康(瑞典)有限公司 | 用于治疗非小细胞肺癌的奧希替尼 |
| WO2021094379A1 (en) | 2019-11-12 | 2021-05-20 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
| CA3166980A1 (en) | 2020-01-20 | 2021-07-29 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
| US20210369709A1 (en) | 2020-05-27 | 2021-12-02 | Astrazeneca Ab | EGFR TKIs FOR USE IN THE TREATMENT OF NON-SMALL CELL LUNG CANCER |
| TW202304457A (zh) * | 2021-03-22 | 2023-02-01 | 瑞典商阿斯特捷利康公司 | 配製物 |
| CN119278041A (zh) | 2022-03-31 | 2025-01-07 | 阿斯利康(瑞典)有限公司 | 用于治疗癌症的与akt抑制剂组合的表皮生长因子受体（egfr）酪氨酸激酶抑制剂 |
| WO2023209090A1 (en) | 2022-04-28 | 2023-11-02 | Astrazeneca Ab | Bicyclic heteroaromatic compounds and their application in the treatment of cancer |
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| MA71241A (fr) | 2022-06-27 | 2025-04-30 | Astrazeneca Ab | Combinaisons impliquant des inhibiteurs de tyrosine kinase du récepteur du facteur de croissance épidermique pour traiter le cancer |
| JP2025522965A (ja) | 2022-07-08 | 2025-07-17 | アストラゼネカ・アクチエボラーグ | 癌の治療のためのｈｇｆ受容体阻害剤と組み合わせた上皮成長因子受容体チロシンキナーゼ阻害剤 |
| EP4646265A1 (en) | 2023-01-06 | 2025-11-12 | Insmed Incorporated | Novel, reversible dpp1 inhibitors and uses thereof |
| WO2025092926A1 (zh) * | 2023-10-31 | 2025-05-08 | 浙江同源康医药股份有限公司 | 一种嘧啶类衍生物的药物组合物 |
Citations (3)
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|---|---|---|---|---|
| US20090017024A1 (en) * | 2007-07-12 | 2009-01-15 | Tragara Pharmaceuticals, Inc. | Methods and Compositions for the Treatment of Cancer, Tumors, and Tumor-Related Disorders |
| US20090028868A1 (en) * | 2006-02-09 | 2009-01-29 | Daiichi Sankyo Company, Limited | Anti-cancer pharmaceutical compositions and methods for treating patients with cancer |
| WO2013014448A1 (en) * | 2011-07-27 | 2013-01-31 | Astrazeneca Ab | 2 - (2, 4, 5 - substituted -anilino) pyrimidine derivatives as egfr modulators useful for treating cancer |
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| IL110376A (en) * | 1993-08-02 | 1998-08-16 | Bristol Myers Squibb Co | Pharmaceutical compositions containing ifetroban salts and methods for the preparation thereof |
| SE9802973D0 (sv) * | 1998-09-03 | 1998-09-03 | Astra Ab | Immediate release tablet |
| WO2001076565A1 (fr) * | 2000-04-12 | 2001-10-18 | Banyu Pharmaceutical Co., Ltd. | Compositions et preparations se desintegrant dans la cavite buccale |
| US6881737B2 (en) | 2001-04-11 | 2005-04-19 | Amgen Inc. | Substituted triazinyl acrylamide derivatives and methods of use |
| MY135609A (en) | 2002-02-26 | 2008-05-30 | Astrazeneca Ab | Pharmaceutical formulation of iressa comprising a water-soluble cellulose derivative |
| WO2006037763A1 (en) | 2004-10-05 | 2006-04-13 | Altana Pharma Ag | Oral pharmaceutical preparation for proton pump antagonists |
| ES2279715B1 (es) * | 2005-12-26 | 2008-06-01 | Laboratorios Lesvi, S.L. | Formulacion oral de olanzapina. |
| JP5576922B2 (ja) * | 2006-04-20 | 2014-08-20 | 信越化学工業株式会社 | 腸溶性固体分散体を含んでなる固形製剤 |
| EP2696857A1 (en) | 2011-04-11 | 2014-02-19 | Alfred E. Tiefenbacher (GmbH & Co. KG) | Pharmaceutical composition comprising bosentan |
| KR101317809B1 (ko) | 2011-06-07 | 2013-10-16 | 한미약품 주식회사 | 암세포의 성장을 억제하는 아마이드 유도체 및 비금속염 활택제를 포함하는 약학 조성물 |
| EP3181128B1 (en) * | 2012-01-13 | 2023-03-08 | XSpray Pharma AB (publ) | Nilotinib pharmaceuticalcomposition |
| WO2013160916A1 (en) | 2012-04-25 | 2013-10-31 | Hetero Research Foundation | Sunitinib malate solid dispersion |
| GB201400034D0 (en) * | 2014-01-02 | 2014-02-19 | Astrazeneca Ab | Pharmaceutical Compositions comprising AZD9291 |
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2014
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090028868A1 (en) * | 2006-02-09 | 2009-01-29 | Daiichi Sankyo Company, Limited | Anti-cancer pharmaceutical compositions and methods for treating patients with cancer |
| US20090017024A1 (en) * | 2007-07-12 | 2009-01-15 | Tragara Pharmaceuticals, Inc. | Methods and Compositions for the Treatment of Cancer, Tumors, and Tumor-Related Disorders |
| WO2013014448A1 (en) * | 2011-07-27 | 2013-01-31 | Astrazeneca Ab | 2 - (2, 4, 5 - substituted -anilino) pyrimidine derivatives as egfr modulators useful for treating cancer |
Non-Patent Citations (2)
| Title |
|---|
| Bala R et al., "Polymers in fast disintegrating tablets–a review", Asian Journal of Pharmaceutical and Clinical Research, Vol 5, No.2, P.8-14, 2012 * |
| Jacob S et al., "Novel co-processed excipients of mannitol and microcrystalline cellulose for preparing fast dissolving tablets of glipizide", Indian Journal of Pharmaceutical Sciences, Vol.69, No.5, P.633-639, 2007/9-10 * |
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