TWI680971B - 化合物及其作爲β-分泌酶1抑制劑之用途 - Google Patents

化合物及其作爲β-分泌酶1抑制劑之用途 Download PDF

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TWI680971B
TWI680971B TW105112413A TW105112413A TWI680971B TW I680971 B TWI680971 B TW I680971B TW 105112413 A TW105112413 A TW 105112413A TW 105112413 A TW105112413 A TW 105112413A TW I680971 B TWI680971 B TW I680971B
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dibenzo
imino
prop
thiophen
mmol
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TW201702240A (zh
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林曉汶
渡 馬
游書杰
日平 彭
郡 羅
丹霞 湯
湯瑪斯 馬隆
D 安德魯 懷特
理查 貝瑞希斯
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新源生物科技股份有限公司
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  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
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TW105112413A 2015-04-21 2016-04-21 化合物及其作爲β-分泌酶1抑制劑之用途 TWI680971B (zh)

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US201562150715P 2015-04-21 2015-04-21
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CN (1) CN107613771B (enExample)
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Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10947223B2 (en) 2016-12-15 2021-03-16 Amgen Inc. Substituted oxazines as beta-secretase inhibitors
CA3047287A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
JP7148518B2 (ja) 2016-12-15 2022-10-05 アムジエン・インコーポレーテツド β-セクレターゼ阻害剤としての二環式チアジンおよびオキサジン誘導体ならびに使用方法
MX387729B (es) * 2016-12-15 2025-03-18 Amgen Inc Derivados de dióxido de 1,4-tiazina y dióxido 1,2,4-tiadiazina como inhibidores de beta-secretasa y métodos de uso.
WO2018112083A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Thiazine derivatives as beta-secretase inhibitors and methods of use
GB201805816D0 (en) * 2018-04-06 2018-05-23 Ucb Biopharma Sprl Therapeutic agents
CN109180670A (zh) * 2018-09-17 2019-01-11 广东东阳光药业有限公司 亚氨基噻二嗪二氧化物衍生物及其用途
CN109180672A (zh) * 2018-09-29 2019-01-11 广东东阳光药业有限公司 亚氨基噻二嗪二氧化物衍生物及其用途
CN109796447B (zh) * 2019-01-07 2020-03-13 广东东阳光药业有限公司 亚氨基噻二嗪二氧化物衍生物及其用途
GB201906804D0 (en) 2019-05-14 2019-06-26 Ucb Biopharma Sprl Therapeutic agents
US20220289685A1 (en) 2019-08-19 2022-09-15 UCB Biopharma SRL Antimalarial hexahydropyrimidine analogues
GB202010606D0 (en) 2020-07-10 2020-08-26 Ucb Biopharma Sprl Therapeutic agents
CR20230576A (es) 2021-06-14 2024-04-05 Scorpion Therapeutics Inc Derivados de la urea que pueden ser utilizados para tratar el cáncer
EP4476201A1 (en) 2022-02-08 2024-12-18 UCB Biopharma SRL Antimalarial hexahydropyrimidine analogues

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101084199A (zh) * 2004-10-15 2007-12-05 阿斯利康(瑞典)有限公司 取代的氨基化合物及其用途
US7763609B2 (en) * 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
CN103874496A (zh) * 2011-08-22 2014-06-18 默沙东公司 作为bace抑制剂的2-螺-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其用途

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2548388A1 (en) * 2003-12-15 2005-06-30 Schering Corporation Heterocyclic aspartyl protease inhibitors
AU2006307314C1 (en) * 2005-10-25 2011-08-25 Shionogi & Co., Ltd. Aminodihydrothiazine derivative
PE20080155A1 (es) 2006-06-12 2008-03-10 Schering Corp Compuestos heterociclicos como inhibidores de aspartil-proteasa
ES2476605T3 (es) * 2007-04-24 2014-07-15 Shionogi & Co., Ltd. Derivados de aminohidrotiazina sustituidos con grupos cíclicos
EP2161271A1 (en) * 2008-09-08 2010-03-10 Università Degli Studi Di Milano - Bicocca Alpha-carboline inhibitors of NMP-ALK, RET, and Bcr-Abl
UA108363C2 (uk) * 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
US8815881B2 (en) * 2010-08-09 2014-08-26 Hoffmann-La Roche Inc. 1,4,5,6-tetrahydro-pyrimidin-2-ylamine compounds
EP2694489B1 (en) * 2011-04-07 2017-09-06 Merck Sharp & Dohme Corp. C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
US9145426B2 (en) 2011-04-07 2015-09-29 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
CN103596939A (zh) * 2011-04-13 2014-02-19 默沙东公司 作为bace抑制剂的5-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其应用
AU2012243329B2 (en) * 2011-04-13 2015-09-17 Merck Sharp & Dohme Corp. 5-substituted iminothiazines and their mono-and dioxides as BACE inhibitors,compositions,and their use
US9416129B2 (en) * 2012-10-17 2016-08-16 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use
CA2825821A1 (en) * 2013-08-28 2015-02-28 Chiesi Farmaceutici S.P.A. 1-phenylalkanecarboxylic acid derivatives for the treatment of alzheimer's disease and multiple sclerosis
CN104910238B (zh) 2014-03-14 2017-08-11 中国科学院上海药物研究所 一类五环三萜类化合物及其在制备治疗阿尔兹海默病的药物中的用途

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7763609B2 (en) * 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
CN101084199A (zh) * 2004-10-15 2007-12-05 阿斯利康(瑞典)有限公司 取代的氨基化合物及其用途
CN103874496A (zh) * 2011-08-22 2014-06-18 默沙东公司 作为bace抑制剂的2-螺-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其用途

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