JP5658139B2 - Bace阻害剤 - Google Patents

Bace阻害剤 Download PDF

Info

Publication number
JP5658139B2
JP5658139B2 JP2011507529A JP2011507529A JP5658139B2 JP 5658139 B2 JP5658139 B2 JP 5658139B2 JP 2011507529 A JP2011507529 A JP 2011507529A JP 2011507529 A JP2011507529 A JP 2011507529A JP 5658139 B2 JP5658139 B2 JP 5658139B2
Authority
JP
Japan
Prior art keywords
compound
methyl
mmol
dihydro
formula
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
JP2011507529A
Other languages
English (en)
Japanese (ja)
Other versions
JP2011519854A5 (enExample
JP2011519854A (ja
Inventor
ジェイムズ・エドマンド・オーディア
ダスティン・ジェイムズ・マーゴット
スコット・マーティン・シーハン
ブライアン・モーガン・ワトソン
Original Assignee
イーライ リリー アンド カンパニー
イーライ リリー アンド カンパニー
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40839645&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=JP5658139(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by イーライ リリー アンド カンパニー, イーライ リリー アンド カンパニー filed Critical イーライ リリー アンド カンパニー
Publication of JP2011519854A publication Critical patent/JP2011519854A/ja
Publication of JP2011519854A5 publication Critical patent/JP2011519854A5/ja
Application granted granted Critical
Publication of JP5658139B2 publication Critical patent/JP5658139B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D279/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/041,3-Thiazines; Hydrogenated 1,3-thiazines
    • C07D279/061,3-Thiazines; Hydrogenated 1,3-thiazines not condensed with other rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Medicinal Chemistry (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2011507529A 2008-05-02 2009-04-15 Bace阻害剤 Expired - Fee Related JP5658139B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US4988108P 2008-05-02 2008-05-02
US61/049,881 2008-05-02
PCT/US2009/040589 WO2009134617A1 (en) 2008-05-02 2009-04-15 Aminodihydrothiazine derivatives as bace inhibitors for the treatment of alzheimer's disease

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2014208277A Division JP2015051980A (ja) 2008-05-02 2014-10-09 Bace阻害剤

Publications (3)

Publication Number Publication Date
JP2011519854A JP2011519854A (ja) 2011-07-14
JP2011519854A5 JP2011519854A5 (enExample) 2012-06-07
JP5658139B2 true JP5658139B2 (ja) 2015-01-21

Family

ID=40839645

Family Applications (3)

Application Number Title Priority Date Filing Date
JP2011507529A Expired - Fee Related JP5658139B2 (ja) 2008-05-02 2009-04-15 Bace阻害剤
JP2014208277A Pending JP2015051980A (ja) 2008-05-02 2014-10-09 Bace阻害剤
JP2016211189A Withdrawn JP2017048212A (ja) 2008-05-02 2016-10-28 Bace阻害剤

Family Applications After (2)

Application Number Title Priority Date Filing Date
JP2014208277A Pending JP2015051980A (ja) 2008-05-02 2014-10-09 Bace阻害剤
JP2016211189A Withdrawn JP2017048212A (ja) 2008-05-02 2016-10-28 Bace阻害剤

Country Status (32)

Country Link
US (1) US7648983B2 (enExample)
EP (1) EP2297120B1 (enExample)
JP (3) JP5658139B2 (enExample)
KR (1) KR101253835B1 (enExample)
CN (1) CN102015667B (enExample)
AR (1) AR071187A1 (enExample)
AU (1) AU2009241515B2 (enExample)
CA (1) CA2723207C (enExample)
CL (1) CL2009000860A1 (enExample)
CO (1) CO6311079A2 (enExample)
CR (1) CR11776A (enExample)
DK (1) DK2297120T3 (enExample)
DO (1) DOP2010000328A (enExample)
EA (1) EA016955B1 (enExample)
EC (1) ECSP10010582A (enExample)
ES (1) ES2549087T3 (enExample)
HR (1) HRP20150941T1 (enExample)
HU (1) HUE025520T2 (enExample)
IL (1) IL208350A (enExample)
MA (1) MA32351B1 (enExample)
MX (1) MX2010011972A (enExample)
NZ (1) NZ588300A (enExample)
PE (1) PE20091816A1 (enExample)
PL (1) PL2297120T3 (enExample)
PT (1) PT2297120E (enExample)
RS (1) RS54260B1 (enExample)
SI (1) SI2297120T1 (enExample)
SV (1) SV2010003718A (enExample)
TW (1) TWI431004B (enExample)
UA (1) UA102251C2 (enExample)
WO (1) WO2009134617A1 (enExample)
ZA (1) ZA201006868B (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015051980A (ja) * 2008-05-02 2015-03-19 イーライ リリー アンド カンパニー Bace阻害剤

Families Citing this family (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
SG162790A1 (en) 2005-06-14 2010-07-29 Schering Corp Aspartyl protease inhibitors
CN101394852A (zh) 2005-06-14 2009-03-25 先灵公司 作为蛋白酶抑制剂的化合物的制备和用途
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
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
ES2548774T3 (es) * 2008-01-18 2015-10-20 Eisai R&D Management Co., Ltd. Derivado de aminodihidrotiazina condensado
US8541427B2 (en) 2008-04-22 2013-09-24 Merck, Sharp & Dohme, Corp. Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use
AU2009258496B8 (en) 2008-06-13 2014-06-26 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity
WO2010013794A1 (en) * 2008-07-28 2010-02-04 Eisai R&D Management Co., Ltd. Spiroaminodihydrothiazine derivatives
EP2324032B1 (en) 2008-08-19 2014-10-01 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
CN102209721A (zh) 2008-09-11 2011-10-05 安姆根有限公司 作为β-分泌酶调节剂的螺四环化合物及其使用方法
KR20110076965A (ko) * 2008-09-30 2011-07-06 에자이 알앤드디 매니지먼트 가부시키가이샤 신규한 축합 아미노 디하이드로티아진 유도체
WO2010047372A1 (ja) 2008-10-22 2010-04-29 塩野義製薬株式会社 Bace1阻害活性を有する2-アミノピリミジン-4-オンおよび2-アミノピリジン誘導体
CN102348698B (zh) 2009-03-13 2015-06-03 生命医药公司 β-分泌酶的抑制剂
GB0912778D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
GB0912777D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydropyrimidone derivatives
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
AU2013234424B9 (en) * 2009-10-08 2014-07-03 Merck Sharp & Dohme Llc Iminothiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
US8563543B2 (en) 2009-10-08 2013-10-22 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
US8569310B2 (en) 2009-10-08 2013-10-29 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use
EP2485590B1 (en) 2009-10-08 2015-01-07 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
EP2514747A4 (en) 2009-12-09 2013-05-08 Shionogi & Co SUBSTITUTED AMINOTHIAZINE DERIVATIVE
JP5554346B2 (ja) * 2009-12-09 2014-07-23 塩野義製薬株式会社 含硫黄複素環誘導体を含有するアルツハイマー症の治療用または予防用医薬組成物
UA110467C2 (uk) 2009-12-11 2016-01-12 Шионогі Енд Ко., Лтд. Похідні оксазину
WO2011077726A1 (ja) 2009-12-24 2011-06-30 塩野義製薬株式会社 4-アミノ-1,3-チアジンまたはオキサジン誘導体
EP2539322B1 (en) 2010-02-24 2014-01-01 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
JP5584352B2 (ja) 2010-03-15 2014-09-03 アムジエン・インコーポレーテツド β−セクレターゼ調節剤としてのアミノ−ジヒドロオキサジン系およびアミノ−ジヒドロチアジン系スピロ化合物ならびにそれらの医学的用途
JP2013522305A (ja) 2010-03-15 2013-06-13 アムジエン・インコーポレーテツド β−セクレターゼ調節剤としてのスピロ−四環式環化合物
PH12012502377A1 (en) 2010-06-09 2014-10-14 Janssen Pharmaceutica Nv 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace)
US20130079349A1 (en) * 2010-06-09 2013-03-28 Janssen Pharmaceutica Nv 5-amino-3,6-dihydro-1h-pyrazin-2-one derivatives useful as inhibitors of beta-secretase (bace)
EP2601197B1 (en) 2010-08-05 2014-06-25 Amgen Inc. Amino-iso-indole, amino-aza-iso-indole, amino-dihydroisoquinoline and amino-benzoxazine compounds as beta-secretase modulators and methods of use
JP5766198B2 (ja) 2010-10-29 2015-08-19 塩野義製薬株式会社 縮合アミノジヒドロピリミジン誘導体
CN103261199A (zh) 2010-10-29 2013-08-21 盐野义制药株式会社 萘啶衍生物
WO2012071279A1 (en) 2010-11-23 2012-05-31 Amgen Inc. Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use
NZ610948A (en) 2010-12-22 2014-06-27 Janssen Pharmaceutica Nv 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (bace)
GB201100181D0 (en) 2011-01-06 2011-02-23 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101139D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
CA2814014A1 (en) 2011-01-21 2012-07-26 Branko MITASEV Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives
GB201101140D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
US9346827B2 (en) 2011-02-07 2016-05-24 Amgen Inc. 5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use
WO2012112462A1 (en) 2011-02-15 2012-08-23 Amgen Inc. Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use
JP5853033B2 (ja) 2011-03-01 2016-02-09 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap β−セクレターゼ(BACE)の阻害剤として有用な6,7−ジヒドロ−ピラゾロ[1,5−a]ピラジン−4−イルアミン誘導体
BR112013022917A2 (pt) 2011-03-09 2016-12-06 Janssen Pharmaceutica Nv derivados 3,4-dihidro-pirrolo[1,2-a]pirazino-1-ilamina úteis como inibidores de beta-secretase (bace)
US9145426B2 (en) 2011-04-07 2015-09-29 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
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
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
WO2012147762A1 (ja) 2011-04-26 2012-11-01 塩野義製薬株式会社 ピリジン誘導体およびそれを含有するbace1阻害剤
KR20140054295A (ko) 2011-08-22 2014-05-08 머크 샤프 앤드 돔 코포레이션 Bace 억제제로서의 2-스피로-치환된 이미노티아진 및 그의 모노- 및 디옥시드, 조성물 및 그의 용도
JP2014526560A (ja) 2011-09-21 2014-10-06 アムジエン・インコーポレーテツド β‐セクレターゼ調節因子としてのアミノオキサジン化合物およびアミノジヒドロチアジン化合物および使用方法
TWI557112B (zh) 2012-03-05 2016-11-11 百靈佳殷格翰國際股份有限公司 β-分泌酶抑制劑
TW201422592A (zh) 2012-08-27 2014-06-16 Boehringer Ingelheim Int β-分泌酶抑制劑
WO2014052398A1 (en) 2012-09-28 2014-04-03 Vitae Pharmaceuticals, Inc. Inhibitor of beta-secretase
US9556135B2 (en) 2012-10-12 2017-01-31 Amgen, Inc. Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
WO2014062549A1 (en) 2012-10-17 2014-04-24 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds 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
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING 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
ES2769578T3 (es) 2013-02-12 2020-06-26 Buck Inst Res Aging Hidantoínas que modulan el procesamiento de APP mediado por BACE
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
AP2015008716A0 (en) 2013-03-08 2015-09-30 Amgen Inc Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
TWI593692B (zh) * 2013-03-12 2017-08-01 美國禮來大藥廠 四氫吡咯并噻嗪化合物
JP6325092B2 (ja) 2013-06-12 2018-05-16 ヤンセン ファーマシューティカ エヌ.ベー. βーセクレターゼ(BACE)の阻害剤としての4−アミノ−6−フェニル−5,6−ジヒドロイミダゾ[1,5−A]ピラジン誘導体
KR102243133B1 (ko) 2013-06-12 2021-04-22 얀센 파마슈티카 엔.브이. 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-6,7-디하이드로[1,2,3]트리아졸로[1,5-a]피라진 유도체
KR102243135B1 (ko) 2013-06-12 2021-04-22 얀센 파마슈티카 엔.브이. 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-5,6-디하이드로이미다조[1,5-a]피라진-3(2h)-온 유도체
JO3318B1 (ar) * 2013-06-18 2019-03-13 Lilly Co Eli مثبطات bace
US9096615B2 (en) 2013-07-30 2015-08-04 Amgen Inc. Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta-secretase and methods of use thereof
JP6483146B2 (ja) * 2014-02-19 2019-03-13 ハー・ルンドベック・アクチエゼルスカベット アルツハイマー病治療用のbace1阻害剤としての2−アミノ−3,5,5−トリフルオロ−3,4,5,6−テトラヒドロピリジン
JP6576433B2 (ja) 2014-08-08 2019-09-18 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シクロプロピル縮合チアジン−2−アミン化合物及び使用方法
EP3233834B1 (en) 2014-12-18 2019-11-13 Janssen Pharmaceutica NV 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine derivatives useful as inhibitors of beta-secretase
CN107257795A (zh) * 2015-03-19 2017-10-17 伊莱利利公司 选择性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
WO2017061534A1 (en) 2015-10-08 2017-04-13 Shionogi & Co., Ltd. Dihydrothiazine derivatives
WO2018031334A1 (en) * 2016-08-11 2018-02-15 Eli Lilly And Company Aminothiazines and their use as bace1 inhibitors
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.
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
CA3047287A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
US10947223B2 (en) 2016-12-15 2021-03-16 Amgen Inc. Substituted oxazines as beta-secretase inhibitors
WO2018112083A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Thiazine derivatives as beta-secretase inhibitors and methods of use
AR110747A1 (es) * 2017-01-27 2019-05-02 Lilly Co Eli Compuestos de 5-metil-1,2,4-oxadiazol-3-ilo
CA3098430A1 (en) 2018-04-27 2019-10-31 Shionogi & Co., Ltd. Tetrahydropyranooxazine derivatives having selective bace1 inhibitory activity

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996014842A1 (en) 1994-11-15 1996-05-23 Merck & Co., Inc. Substituted heterocycles as inhibitors of nitric oxide synthase
JPH08333258A (ja) 1994-12-14 1996-12-17 Japan Tobacco Inc チアジン又はチアゼピン誘導体及びそれら化合物を含有してなる一酸化窒素合成酵素阻害剤
GB0324498D0 (en) * 2003-07-21 2003-11-26 Aventis Pharma Inc Heterocyclic compounds as P2X7 ion channel blockers
US7592348B2 (en) * 2003-12-15 2009-09-22 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
CN101084198A (zh) * 2004-10-15 2007-12-05 阿斯利康(瑞典)有限公司 取代的氨基-嘧啶酮及其用途
AU2006307314C1 (en) * 2005-10-25 2011-08-25 Shionogi & Co., Ltd. Aminodihydrothiazine derivative
US20090099217A1 (en) * 2006-04-05 2009-04-16 Astex Therapeutics Ltd. 2-Aminopyrimidin-4-Ones And Their Use For Treating Or Preventing Alpha Beta-Related Pathologies
ES2476605T3 (es) 2007-04-24 2014-07-15 Shionogi & Co., Ltd. Derivados de aminohidrotiazina sustituidos con grupos cíclicos
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
TWI431004B (zh) * 2008-05-02 2014-03-21 Lilly Co Eli Bace抑制劑
AU2009258496B8 (en) * 2008-06-13 2014-06-26 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015051980A (ja) * 2008-05-02 2015-03-19 イーライ リリー アンド カンパニー Bace阻害剤

Also Published As

Publication number Publication date
JP2017048212A (ja) 2017-03-09
CN102015667A (zh) 2011-04-13
US7648983B2 (en) 2010-01-19
EP2297120B1 (en) 2015-08-19
CA2723207A1 (en) 2009-11-05
TW200946522A (en) 2009-11-16
WO2009134617A1 (en) 2009-11-05
CO6311079A2 (es) 2011-08-22
CR11776A (es) 2011-01-28
MX2010011972A (es) 2010-11-25
KR101253835B1 (ko) 2013-04-15
HRP20150941T1 (hr) 2015-10-09
SI2297120T1 (sl) 2015-11-30
KR20100125475A (ko) 2010-11-30
TWI431004B (zh) 2014-03-21
NZ588300A (en) 2012-07-27
DK2297120T3 (en) 2015-10-12
PT2297120E (pt) 2015-10-26
PL2297120T3 (pl) 2016-01-29
CA2723207C (en) 2016-07-12
IL208350A0 (en) 2010-12-30
SV2010003718A (es) 2011-02-14
AU2009241515B2 (en) 2012-04-19
CL2009000860A1 (es) 2010-05-07
ZA201006868B (en) 2012-03-28
JP2011519854A (ja) 2011-07-14
MA32351B1 (fr) 2011-06-01
AU2009241515A1 (en) 2009-11-05
US20090275566A1 (en) 2009-11-05
IL208350A (en) 2014-05-28
HUE025520T2 (en) 2016-02-29
UA102251C2 (ru) 2013-06-25
ES2549087T3 (es) 2015-10-22
AR071187A1 (es) 2010-06-02
CN102015667B (zh) 2013-06-12
ECSP10010582A (es) 2010-11-30
JP2015051980A (ja) 2015-03-19
EA201071264A1 (ru) 2011-04-29
EA016955B1 (ru) 2012-08-30
RS54260B1 (sr) 2016-02-29
DOP2010000328A (es) 2010-11-15
EP2297120A1 (en) 2011-03-23
PE20091816A1 (es) 2009-11-25

Similar Documents

Publication Publication Date Title
JP5658139B2 (ja) Bace阻害剤
KR101362557B1 (ko) Bace 억제제
JP6095844B2 (ja) テトラヒドロピロロチアジン化合物
ES2937236T3 (es) Derivados de dihidro-pirrolo-piridina
JP6111001B1 (ja) 選択的bace1阻害剤
JP6243921B2 (ja) Bace阻害剤
KR101780140B1 (ko) Bace 억제제
JP2015512445A (ja) テトラヒドロピロロチアジン化合物
JP6543697B2 (ja) 2,2,2−トリフルオロエチル−チアジアジン類
KR20180134401A (ko) 예를 들어 알츠하이머병을 치료하기 위한 선택적 BACE1 억제제로서 N-[3-[2-아미노-5-(1,1-디플루오로에틸)-4,4a,5,7-테트라히드로푸로[3,4-d][1,3]옥사진-7a-일]-4-플루오로-페닐]-5-(트리플루오로메틸)피리딘-2-카르복스아미드 및 그의 (4aR,5S,7aS) 이성질체

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20120413

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20120413

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20131022

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20140610

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20141009

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20141021

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20141111

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20141127

R150 Certificate of patent or registration of utility model

Ref document number: 5658139

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees