JP2014524472A - Ｂａｃｅ阻害剤としての２−スピロ置換イミノチアジンならびにそのモノオキシドおよびジオキシド、組成物、ならびにそれらの使用 - Google Patents

Ｂａｃｅ阻害剤としての２−スピロ置換イミノチアジンならびにそのモノオキシドおよびジオキシド、組成物、ならびにそれらの使用 Download PDF

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JP2014524472A
JP2014524472A JP2014527238A JP2014527238A JP2014524472A JP 2014524472 A JP2014524472 A JP 2014524472A JP 2014527238 A JP2014527238 A JP 2014527238A JP 2014527238 A JP2014527238 A JP 2014527238A JP 2014524472 A JP2014524472 A JP 2014524472A
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heteroalkyl
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JP2014524472A5 (enExample
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ウー，ウエン−リエン
バーネツト，ドウエイン，エー
スタンフオード，アンドリユー
カミング，ジヤレツド，エヌ
アスベロム，テオドロス
ベネツト，チヤド
サシスクマール，タバラクラムガラ，ケー
スコツト，ジヤツク，デイー
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Merck Sharp and Dohme LLC
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • C07D417/14—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 three or more hetero rings
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
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    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D279/14—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
    • C07D279/18—[b, e]-condensed with two six-membered rings
    • C07D279/34—[b, e]-condensed with two six-membered rings with hetero atoms directly attached to the ring sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • C07D417/02—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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • C07D417/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • C07D417/02—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
    • 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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    • C07D513/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—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
    • 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
    • C07D513/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Otolaryngology (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2014527238A 2011-08-22 2012-08-21 Ｂａｃｅ阻害剤としての２−スピロ置換イミノチアジンならびにそのモノオキシドおよびジオキシド、組成物、ならびにそれらの使用 Pending JP2014524472A (ja)

Applications Claiming Priority (3)

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US201161526049P 2011-08-22 2011-08-22
US61/526,049 2011-08-22
PCT/US2012/051687 WO2013028670A1 (en) 2011-08-22 2012-08-21 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use

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JP2014524472A true JP2014524472A (ja) 2014-09-22
JP2014524472A5 JP2014524472A5 (enExample) 2015-10-15

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US (1) US9181236B2 (enExample)
EP (1) EP2747769B1 (enExample)
JP (1) JP2014524472A (enExample)
KR (1) KR20140054295A (enExample)
CN (1) CN103874496A (enExample)
AU (1) AU2012298983A1 (enExample)
BR (1) BR112014004181A2 (enExample)
CA (1) CA2844988A1 (enExample)
MX (1) MX2014002113A (enExample)
RU (1) RU2014111055A (enExample)
WO (1) WO2013028670A1 (enExample)

Cited By (4)

* Cited by examiner, † Cited by third party
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JP2015517548A (ja) * 2012-05-24 2015-06-22 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｂａｃｅ１阻害薬としての５−アミノ［１，４］チアジン類
JP2018507879A (ja) * 2015-03-20 2018-03-22 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｂａｃｅ１阻害剤
JP2018513191A (ja) * 2015-04-21 2018-05-24 オールジェネシス バイオセラピューティクス インコーポレイテッド Ｂａｃｅ１阻害剤としての化合物およびそれらの使用
JP2020503291A (ja) * 2016-12-15 2020-01-30 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１，４−チアジンジオキシドおよび１，２，４−チアジアジンジオキシド誘導体ならびに使用方法

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WO2011044187A1 (en) 2009-10-08 2011-04-14 Schering Corporation Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2485920B1 (en) 2009-10-08 2016-04-27 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
EP2694521B1 (en) 2011-04-07 2015-11-25 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
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
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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SI2841437T1 (sl) 2012-04-26 2017-09-29 Bristol-Myers Squibb Company Derivati imidazotiadiazola in imidazopirazina kot proteazno aktivirani receptor 4 (PAR4) inhibitorji za zdravljenje agregacije trombocitov
WO2014059185A1 (en) 2012-10-12 2014-04-17 Amgen Inc. Amino - dihydrothiazine and amino - dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
EP2934539B1 (en) 2012-12-20 2019-03-27 Merck Sharp & Dohme Corp. C5, c6 oxacyclic-fused iminothiazine dioxide compounds as bace inhibitors
WO2014134341A1 (en) 2013-03-01 2014-09-04 Amgen Inc. Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
MX374512B (es) 2013-03-08 2025-03-06 Amgen Inc Compuestos de 1,3-oxazin-2-amina fusionados con ciclopropilo perfluorado como inhibidores de beta-secretasa y métodos de uso.
WO2014150344A1 (en) * 2013-03-15 2014-09-25 Merck Sharp & Dohme Corp. C2-azaspiro iminothiazine dioxides as bace inhibitors
WO2015017407A1 (en) * 2013-07-30 2015-02-05 Amgen Inc. Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta- secretase
WO2015038446A1 (en) * 2013-09-13 2015-03-19 Merck Sharp & Dohme Corp. C5-spiro iminothiazine dioxides as bace inhibitors, compositions, and their use
WO2015095104A1 (en) * 2013-12-18 2015-06-25 Merck Sharp & Dohme Corp. Iminothiadiazepane dioxide compounds as bace inhibitors, compositions, and their use
WO2015094930A1 (en) * 2013-12-18 2015-06-25 Merck Sharp & Dohme Corp. C-6 spirocarbocyclic iminothiadiazine dioxides as bace inhibitors, compositions, and their use
CN105683199B (zh) * 2013-12-20 2018-06-26 豪夫迈·罗氏有限公司 5-芳基-1-亚氨基-1-氧代-[1，2，4]噻二嗪
US9732088B2 (en) 2014-06-02 2017-08-15 Merck Sharp & Dohme Corp. C2-carbocyclic iminothiazine dioxides as BACE inhibitors, compositions, and their use
CN106795147B (zh) 2014-08-08 2020-09-22 美国安进公司 作为β-分泌酶抑制剂的环丙基稠合噻嗪-2-胺化合物和使用方法
WO2016085780A1 (en) * 2014-11-25 2016-06-02 Merck Sharp & Dohme Corp. C5-c6-oxacyclic fused iminopyrimidinone compounds as bace inhibitors, compositions, and their use
WO2017024180A1 (en) 2015-08-06 2017-02-09 Amgen Inc. Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
JP6895424B2 (ja) * 2015-08-12 2021-06-30 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｂａｃｅ１阻害剤
WO2017095759A1 (en) 2015-12-04 2017-06-08 Merck Sharp & Dohme Corp. C5-c6-carbocyclic fused iminothiadiazine dioxides as bace inhibitors, compositions, and their use
MX394391B (es) 2016-12-15 2025-03-24 Amgen Inc Derivados de tiazina y oxazina biciclicos como inhibidores de beta-secretasa y metodos de uso.
CA3047288A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Thiazine derivatives as beta-secretase inhibitors and methods of use
EP3555085B1 (en) 2016-12-15 2020-12-02 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
AU2017376441B2 (en) 2016-12-15 2021-10-14 Amgen Inc. Oxazine derivatives as beta-secretase inhibitors and methods of use
AU2019258575A1 (en) 2018-04-27 2020-10-29 Shionogi & Co., Ltd. Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity
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
JP2023533616A (ja) * 2020-06-30 2023-08-03 ４イー セラピューティクス， インコーポレイテッド Ｍｎｋ阻害を示すピリジン－１，５－ジオン及びそれらの使用方法
CN113105318B (zh) * 2021-02-23 2022-05-20 中山大学 一种2,2-二氟环丁烷-1-羧酸的制备方法及应用

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