CN102482268B - 作为用于糖尿病治疗的bace2抑制剂的2-氨基二氢[1，3]噻嗪 - Google Patents

作为用于糖尿病治疗的bace2抑制剂的2-氨基二氢[1，3]噻嗪 Download PDF

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Publication number
CN102482268B
CN102482268B CN201080039905.XA CN201080039905A CN102482268B CN 102482268 B CN102482268 B CN 102482268B CN 201080039905 A CN201080039905 A CN 201080039905A CN 102482268 B CN102482268 B CN 102482268B
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China
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phenyl
halogen
alkyl
fluoro
formula
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Expired - Fee Related
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CN201080039905.XA
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English (en)
Chinese (zh)
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CN102482268A (zh
Inventor
杰里米·比彻姆
阿涅丝·贝纳尔多
汉斯·希尔珀特
克里斯蒂亚诺·米廖里尼
威廉·里布莱
王海燕
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • 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
    • 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
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D279/04—1,3-Thiazines; Hydrogenated 1,3-thiazines
    • C07D279/06—1,3-Thiazines; Hydrogenated 1,3-thiazines not condensed with other 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201080039905.XA 2009-09-11 2010-09-07 作为用于糖尿病治疗的bace2抑制剂的2-氨基二氢[1，3]噻嗪 Expired - Fee Related CN102482268B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP09170126.8 2009-09-11
EP09170126 2009-09-11
EP09172068 2009-10-02
EP09172068.0 2009-10-02
PCT/EP2010/063071 WO2011029803A1 (en) 2009-09-11 2010-09-07 2 -aminodihydro [1, 3] thiazines as bace 2 inhibitors for the treatment of diabetes

Publications (2)

Publication Number Publication Date
CN102482268A CN102482268A (zh) 2012-05-30
CN102482268B true CN102482268B (zh) 2014-11-26

Family

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Family Applications (1)

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CN201080039905.XA Expired - Fee Related CN102482268B (zh) 2009-09-11 2010-09-07 作为用于糖尿病治疗的bace2抑制剂的2-氨基二氢[1，3]噻嗪

Country Status (10)

Country Link
US (3) US20110065695A1 (enExample)
EP (1) EP2475658A1 (enExample)
JP (1) JP2013503838A (enExample)
CN (1) CN102482268B (enExample)
AR (1) AR078163A1 (enExample)
CA (1) CA2771374A1 (enExample)
IN (1) IN2012DN01233A (enExample)
SG (1) SG179034A1 (enExample)
TW (1) TW201114765A (enExample)
WO (1) WO2011029803A1 (enExample)

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CN101346357B (zh) 2005-10-25 2014-04-02 盐野义制药株式会社 氨基二氢噻嗪衍生物
JP5383483B2 (ja) * 2007-04-24 2014-01-08 塩野義製薬株式会社 アルツハイマー症治療用医薬組成物
EP2689780A1 (en) 2007-04-24 2014-01-29 Shionogi & Co., Ltd. Intermediates for aminodihydrothiazine derivatives substituted with a cyclic group
KR101324426B1 (ko) 2008-06-13 2013-10-31 시오노기세야쿠 가부시키가이샤 β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체
CN102186841A (zh) * 2008-10-22 2011-09-14 盐野义制药株式会社 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
KR20120104570A (ko) 2009-12-11 2012-09-21 시오노기세야쿠 가부시키가이샤 옥사진 유도체
EP2634188A4 (en) 2010-10-29 2014-05-07 Shionogi & Co FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE
CN103261199A (zh) 2010-10-29 2013-08-21 盐野义制药株式会社 萘啶衍生物
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
RU2013150349A (ru) 2011-04-13 2015-05-20 Мерк Шарп И Доум Корп. 5-замещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов васе, содержащие их композиции и их применение
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
CN103608345A (zh) 2011-04-26 2014-02-26 盐野义制药株式会社 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂
US20140235626A1 (en) 2011-04-26 2014-08-21 Shionogi & Co., Ltd. Pyridine derivatives and a pharmaceutical composition for inhibiting bace1 containing them
US8927535B2 (en) * 2011-07-06 2015-01-06 Hoffman-La Roche Inc. Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors
US9181236B2 (en) 2011-08-22 2015-11-10 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use
JP2015514073A (ja) 2012-03-20 2015-05-18 エラン ファーマシューティカルズ， リミテッド・ライアビリティ・カンパニー スピロ環式ジヒドロ−チアジンおよびジヒドロ−オキサジンｂａｃｅ阻害剤、ならびにその組成物および使用
US9096541B2 (en) 2012-03-29 2015-08-04 Oklahoma Medical Research Foundation Inhibition of memapsin 1 cleavage in the treatment of diabetes
CA2872179A1 (en) 2012-05-24 2013-11-28 F. Hoffmann-La Roche Ag 5-amino[1,4]thiazines as bace 1 inhibitors
EA201492285A1 (ru) 2012-06-20 2015-04-30 Ф. Хоффманн-Ля Рош Аг Соединения n-алкилтриазола в качестве антагонистов лизофосфатидной кислоты (lpar)
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
WO2014065434A1 (en) 2012-10-24 2014-05-01 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity
WO2014078314A1 (en) 2012-11-15 2014-05-22 Amgen Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
JP6389830B2 (ja) 2013-03-01 2018-09-12 アムジエン・インコーポレーテツド ベータ−セクレターゼ阻害剤としてのパーフルオロ化５，６−ジヒドロ−４ｈ−１，３−オキサジン−２−アミン化合物および使用方法
JP6374889B2 (ja) 2013-03-08 2018-08-15 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過フッ素化シクロプロピル縮合１，３−オキサジン−２−アミン化合物、及び使用方法
US9550762B2 (en) 2014-08-08 2017-01-24 Amgen, Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
CN107406440B (zh) 2015-03-20 2021-05-07 豪夫迈·罗氏有限公司 Bace1抑制剂
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
MX386618B (es) 2016-12-15 2025-03-19 Amgen Inc Derivados de tiazina condensados con ciclopropilo como inhibidores de beta-secretasa y métodos de uso.
MX388697B (es) 2016-12-15 2025-03-20 Amgen Inc Derivados de tiazina como inhibidores de beta-secretasa y metodos de uso.
EP3555086B1 (en) 2016-12-15 2021-09-01 Amgen Inc. 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use
MA54101A (fr) 2016-12-15 2021-10-27 Amgen Inc Dérivés de thiazine et d'oxazine bicycliques en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation
MA52722A (fr) 2016-12-15 2021-04-14 Amgen Inc Dérivés d'oxazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008133274A1 (ja) * 2007-04-24 2008-11-06 Shionogi & Co., Ltd. 環式基で置換されたアミノジヒドロチアジン誘導体
WO2008133273A1 (ja) * 2007-04-24 2008-11-06 Shionogi & Co., Ltd. アルツハイマー症治療用医薬組成物
CN101346357A (zh) * 2005-10-25 2009-01-14 盐野义制药株式会社 氨基二氢噻嗪衍生物
WO2010063718A1 (en) * 2008-12-02 2010-06-10 ETH Zürich Screening assay for metabolic disease therapeuticals

Family Cites Families (1)

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KR101259240B1 (ko) * 2008-02-18 2013-04-29 시에나 바이오테크 에스.피.에이. 4,5-다이하이드로-옥사졸-2-일 아민 유도체

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101346357A (zh) * 2005-10-25 2009-01-14 盐野义制药株式会社 氨基二氢噻嗪衍生物
WO2008133274A1 (ja) * 2007-04-24 2008-11-06 Shionogi & Co., Ltd. 環式基で置換されたアミノジヒドロチアジン誘導体
WO2008133273A1 (ja) * 2007-04-24 2008-11-06 Shionogi & Co., Ltd. アルツハイマー症治療用医薬組成物
WO2010063718A1 (en) * 2008-12-02 2010-06-10 ETH Zürich Screening assay for metabolic disease therapeuticals

Also Published As

Publication number Publication date
CA2771374A1 (en) 2011-03-17
US20110065695A1 (en) 2011-03-17
JP2013503838A (ja) 2013-02-04
EP2475658A1 (en) 2012-07-18
WO2011029803A1 (en) 2011-03-17
US20130096107A1 (en) 2013-04-18
AR078163A1 (es) 2011-10-19
US20140221360A1 (en) 2014-08-07
SG179034A1 (en) 2012-04-27
IN2012DN01233A (enExample) 2015-05-15
TW201114765A (en) 2011-05-01
CN102482268A (zh) 2012-05-30

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