CN103596939A - 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 - Google Patents

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 Download PDF

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CN103596939A
CN103596939A CN201280028592.7A CN201280028592A CN103596939A CN 103596939 A CN103596939 A CN 103596939A CN 201280028592 A CN201280028592 A CN 201280028592A CN 103596939 A CN103596939 A CN 103596939A
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group
cycloalkyl
compound
mmol
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W-L.吴
D.A.伯内特
A.W.斯坦福
J.N.卡明
C.E.班尼特
E.J.吉尔伯特
X.彭
J.D.斯科特
Y.于
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Merck Sharp & Dohme LLC
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    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/12—1,4-Thiazines; Hydrogenated 1,4-thiazines not condensed with other rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201280028592.7A 2011-04-13 2012-04-12 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 Pending CN103596939A (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201161475215P 2011-04-13 2011-04-13
US61/475,215 2011-04-13
US201161503254P 2011-06-30 2011-06-30
US61/503,254 2011-06-30
CNPCT/CN2012/000435 2012-04-05
PCT/CN2012/000497 WO2012139425A1 (en) 2011-04-13 2012-04-12 5-substituted iminothiazines and their mono-and dioxides as bace inhibitors,compositions,and their use

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CN103596939A true CN103596939A (zh) 2014-02-19

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US (1) US9499502B2 (enExample)
EP (1) EP2697210B1 (enExample)
JP (1) JP2014514302A (enExample)
CN (1) CN103596939A (enExample)
AU (1) AU2012243329B2 (enExample)
BR (1) BR112013026341A2 (enExample)
CA (1) CA2832473A1 (enExample)
MX (1) MX2013011947A (enExample)
RU (1) RU2013150349A (enExample)
WO (1) WO2012139425A1 (enExample)

Cited By (11)

* Cited by examiner, † Cited by third party
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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
CN107406440A (zh) * 2015-03-20 2017-11-28 豪夫迈·罗氏有限公司 Bace1抑制剂
CN107613771A (zh) * 2015-04-21 2018-01-19 新源生物科技股份有限公司 化合物及其作为β‑分泌酶1抑制剂的用途
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
CN109180671A (zh) * 2018-09-21 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
CN109796447A (zh) * 2019-01-07 2019-05-24 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
CN110467611A (zh) * 2018-05-11 2019-11-19 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
CN113073098A (zh) * 2021-02-20 2021-07-06 北京理工大学 抑制BACE1基因表达的siRNA修饰物及其应用
CN113105318A (zh) * 2021-02-23 2021-07-13 中山大学 一种2,2-二氟环丁烷-1-羧酸的制备方法及应用
CN113880899A (zh) * 2020-10-30 2022-01-04 杭州拉林智能科技有限公司 黄酮苷-有机胺类神经激动剂复盐化合物及其制备方法和应用
CN119080651A (zh) * 2024-10-31 2024-12-06 汕头大学 一种可见光协同钴催化制备烯丙基砜类化合物的方法

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JP6111002B1 (ja) 2014-04-10 2017-04-05 ファイザー・インク ２−アミノ−６−メチル−４，４ａ，５，６−テトラヒドロピラノ［３，４−ｄ］［１，３］チアジン−８ａ（８Ｈ）−イル−１，３−チアゾール−４−イルアミド
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CN106661053B (zh) 2014-07-25 2019-07-12 豪夫迈·罗氏有限公司 吡啶基-三氮杂二环类化合物
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