JP5600754B2 - ピラジン誘導体および神経障害の処置におけるそれらの使用 - Google Patents

ピラジン誘導体および神経障害の処置におけるそれらの使用 Download PDF

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JP5600754B2
JP5600754B2 JP2012546418A JP2012546418A JP5600754B2 JP 5600754 B2 JP5600754 B2 JP 5600754B2 JP 2012546418 A JP2012546418 A JP 2012546418A JP 2012546418 A JP2012546418 A JP 2012546418A JP 5600754 B2 JP5600754 B2 JP 5600754B2
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JP2013516395A5 (enExample
JP2013516395A (ja
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マリナ・ティンテルノート−ブロムライ
シーム・ヤコブ・フェーンストラ
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ノバルティス アーゲー
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • 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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2012546418A 2009-12-31 2010-12-22 ピラジン誘導体および神経障害の処置におけるそれらの使用 Expired - Fee Related JP5600754B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US29172409P 2009-12-31 2009-12-31
US61/291,724 2009-12-31
PCT/EP2010/070502 WO2011080176A1 (en) 2009-12-31 2010-12-22 Pyrazine derivatives and their use in the treatment of neurological disorders

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JP2013516395A JP2013516395A (ja) 2013-05-13
JP2013516395A5 JP2013516395A5 (enExample) 2014-08-21
JP5600754B2 true JP5600754B2 (ja) 2014-10-01

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JP2012546418A Expired - Fee Related JP5600754B2 (ja) 2009-12-31 2010-12-22 ピラジン誘導体および神経障害の処置におけるそれらの使用

Country Status (27)

Country Link
US (2) US20120277244A1 (enExample)
EP (1) EP2519515B1 (enExample)
JP (1) JP5600754B2 (enExample)
KR (1) KR101419157B1 (enExample)
CN (1) CN102712621B (enExample)
AU (1) AU2010338365B2 (enExample)
BR (1) BR112012015916A2 (enExample)
CA (1) CA2785341A1 (enExample)
CL (1) CL2012001762A1 (enExample)
CR (1) CR20120332A (enExample)
CU (1) CU20120099A7 (enExample)
EA (1) EA201200952A1 (enExample)
EC (1) ECSP12012065A (enExample)
ES (1) ES2445536T3 (enExample)
GT (1) GT201200219A (enExample)
HN (1) HN2012001413A (enExample)
IL (1) IL220268A0 (enExample)
MX (1) MX2012007754A (enExample)
NZ (1) NZ600136A (enExample)
PE (1) PE20121640A1 (enExample)
PH (1) PH12012501007A1 (enExample)
PL (1) PL2519515T3 (enExample)
PT (1) PT2519515E (enExample)
SG (1) SG181431A1 (enExample)
TN (1) TN2012000249A1 (enExample)
WO (1) WO2011080176A1 (enExample)
ZA (1) ZA201203614B (enExample)

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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
AU2009258496B8 (en) 2008-06-13 2014-06-26 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity
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UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
UA110467C2 (uk) 2009-12-11 2016-01-12 Шионогі Енд Ко., Лтд. Похідні оксазину
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)
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)
KR20130089231A (ko) * 2010-06-28 2013-08-09 얀센 파마슈티카 엔.브이. 알츠하이머병 및 다른 형태의 치매 치료용으로 유용한 3-아미노-5,6-디하이드로-1ｈ-피라진-2-온 유도체
CN103261199A (zh) 2010-10-29 2013-08-21 盐野义制药株式会社 萘啶衍生物
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
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)
US8524897B2 (en) 2011-01-12 2013-09-03 Novartis Ag Crystalline oxazine derivative
PT2663561E (pt) 2011-01-13 2016-06-07 Novartis Ag Derivados heterocíclicos novos e sua utilização no tratamento de distúrbios neurológicos
JP2014505689A (ja) * 2011-01-13 2014-03-06 ノバルティス アーゲー 代謝障害の処置用ｂａｃｅ−２阻害剤
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)
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
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
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
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
US8338413B1 (en) 2012-03-07 2012-12-25 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
AU2013363151A1 (en) 2012-12-20 2015-06-04 Merck Sharp & Dohme Corp. C5, C6 oxacyclic-fused iminothiazine dioxide compounds as BACE inhibitors
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
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
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
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CN107011134B (zh) * 2017-04-28 2021-02-05 浙江中欣氟材股份有限公司 一种2-氟-5-溴苯乙酮的合成方法

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Publication number Publication date
CA2785341A1 (en) 2011-07-07
PH12012501007A1 (en) 2013-01-14
AU2010338365B2 (en) 2014-01-30
KR101419157B1 (ko) 2014-07-11
TN2012000249A1 (en) 2013-12-12
GT201200219A (es) 2013-10-10
WO2011080176A1 (en) 2011-07-07
CU20120099A7 (es) 2012-07-31
ZA201203614B (en) 2013-01-30
SG181431A1 (en) 2012-07-30
AU2010338365A1 (en) 2012-06-07
BR112012015916A2 (pt) 2017-04-25
NZ600136A (en) 2013-09-27
CN102712621A (zh) 2012-10-03
US20120277244A1 (en) 2012-11-01
IL220268A0 (en) 2012-07-31
CL2012001762A1 (es) 2012-12-21
US20150322038A1 (en) 2015-11-12
CR20120332A (es) 2012-07-12
EP2519515B1 (en) 2013-11-06
HK1172023A1 (en) 2013-04-12
KR20120102795A (ko) 2012-09-18
PE20121640A1 (es) 2012-12-17
JP2013516395A (ja) 2013-05-13
CN102712621B (zh) 2015-03-11
PT2519515E (pt) 2014-02-17
MX2012007754A (es) 2012-08-01
HN2012001413A (es) 2015-03-23
ECSP12012065A (es) 2012-08-31
ES2445536T3 (es) 2014-03-03
EP2519515A1 (en) 2012-11-07
PL2519515T3 (pl) 2014-04-30
EA201200952A1 (ru) 2013-02-28

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