CN102712621B - 吡嗪衍生物及其在治疗神经学障碍中的用途 - Google Patents

吡嗪衍生物及其在治疗神经学障碍中的用途 Download PDF

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Publication number
CN102712621B
CN102712621B CN201080060047.7A CN201080060047A CN102712621B CN 102712621 B CN102712621 B CN 102712621B CN 201080060047 A CN201080060047 A CN 201080060047A CN 102712621 B CN102712621 B CN 102712621B
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alkyl
alkoxy
halogen
amino
alkylthio
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Expired - Fee Related
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Chinese (zh)
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CN102712621A (zh
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M·廷特尔诺特-布洛姆雷
S·J·维恩施特拉
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Novartis AG
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Novartis AG
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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)
CN201080060047.7A 2009-12-31 2010-12-22 吡嗪衍生物及其在治疗神经学障碍中的用途 Expired - Fee Related CN102712621B (zh)

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

Publications (2)

Publication Number Publication Date
CN102712621A CN102712621A (zh) 2012-10-03
CN102712621B true CN102712621B (zh) 2015-03-11

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CN201080060047.7A Expired - Fee Related CN102712621B (zh) 2009-12-31 2010-12-22 吡嗪衍生物及其在治疗神经学障碍中的用途

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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CN103936690B (zh) 2005-10-25 2016-06-08 盐野义制药株式会社 氨基二氢噻嗪衍生物
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
RU2476430C2 (ru) 2007-04-24 2013-02-27 Сионоги Энд Ко., Лтд. Производные аминодигидротиазина, замещенные циклической группой
ES2738123T3 (es) 2008-06-13 2020-01-20 Shionogi & Co Derivado heterocíclico que contiene azufre que tiene actividad inhibitoria de ß-secretasa
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UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
WO2011071135A1 (ja) 2009-12-11 2011-06-16 塩野義製薬株式会社 オキサジン誘導体
CN102918036A (zh) * 2010-06-09 2013-02-06 詹森药业有限公司 用作β-分泌酶(BACE)抑制剂的5-氨基-3,6-二氢-1H-吡嗪-2-酮衍生物
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)
SG186408A1 (en) * 2010-06-28 2013-01-30 Janssen Pharmaceutica Nv 3-amino-5, 6-dihydro-1h-pyrazin-2-one derivatives useful for the treatment of alzheimer's disease and other forms of dementia
US8927721B2 (en) 2010-10-29 2015-01-06 Shionogi & Co., Ltd. Naphthyridine derivative
WO2012057247A1 (ja) 2010-10-29 2012-05-03 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
EP2655376B1 (en) 2010-12-22 2017-08-23 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
US20140128385A1 (en) * 2011-01-13 2014-05-08 Novartis Ag Bace-2 inhibitors for the treatment of metabolic disorders
CN103403001B (zh) * 2011-01-13 2016-08-17 诺瓦提斯公司 杂环衍生物及其在神经性疾病治疗中的应用
MY161407A (en) 2011-03-01 2017-04-14 Janssen Pharmaceutica Nv 6,7-DIHYDRO-PYRAZOLO[1,5-a]PYRAZIN-4-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
SG193342A1 (en) 2011-03-09 2013-10-30 Janssen Pharmaceutica Nv 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
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
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
JPWO2012147763A1 (ja) 2011-04-26 2014-07-28 塩野義製薬株式会社 オキサ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
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
CN104870000A (zh) 2012-12-20 2015-08-26 默沙东公司 作为bace抑制剂的c5,c6氧杂环稠合的亚胺基噻嗪二氧化物化合物,组合物及其用途
AU2014280124B2 (en) 2013-06-12 2018-11-01 Janssen Pharmaceutica Nv 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (BACE)
JP6387402B2 (ja) 2013-06-12 2018-09-05 ヤンセン ファーマシューティカ エヌ．ベー． β−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−３（２Ｈ）−オン誘導体
BR112015030597A2 (pt) 2013-06-12 2017-07-25 Janssen Pharmaceutica Nv derivados 4-amino-6-fenil-6,7-di-hidro[1,2,3]triazolo[1,5-a]pirazina como inibidores de beta-secretase (bace)
CN107108582B (zh) 2014-12-18 2019-10-18 詹森药业有限公司 β-分泌酶的2，3，4，5-四氢吡啶-6-胺化合物抑制剂
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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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
CN101568529A (zh) * 2006-12-22 2009-10-28 诺瓦提斯公司 作为cdk抑制剂、用于治疗癌症、炎症和病毒感染的杂芳基-杂芳基化合物

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CN1376153A (zh) * 1999-10-01 2002-10-23 藤泽药品工业株式会社 酰胺化合物
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
CN101568529A (zh) * 2006-12-22 2009-10-28 诺瓦提斯公司 作为cdk抑制剂、用于治疗癌症、炎症和病毒感染的杂芳基-杂芳基化合物

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CA2785341A1 (en) 2011-07-07
PL2519515T3 (pl) 2014-04-30
ZA201203614B (en) 2013-01-30
HN2012001413A (es) 2015-03-23
EP2519515A1 (en) 2012-11-07
WO2011080176A1 (en) 2011-07-07
MX2012007754A (es) 2012-08-01
PH12012501007A1 (en) 2013-01-14
EA201200952A1 (ru) 2013-02-28
AU2010338365B2 (en) 2014-01-30
KR101419157B1 (ko) 2014-07-11
US20120277244A1 (en) 2012-11-01
NZ600136A (en) 2013-09-27
JP2013516395A (ja) 2013-05-13
US20150322038A1 (en) 2015-11-12
PE20121640A1 (es) 2012-12-17
KR20120102795A (ko) 2012-09-18
CU20120099A7 (es) 2012-07-31
JP5600754B2 (ja) 2014-10-01
CN102712621A (zh) 2012-10-03
TN2012000249A1 (en) 2013-12-12
CR20120332A (es) 2012-07-12
GT201200219A (es) 2013-10-10
EP2519515B1 (en) 2013-11-06
ECSP12012065A (es) 2012-08-31
ES2445536T3 (es) 2014-03-03
IL220268A0 (en) 2012-07-31
CL2012001762A1 (es) 2012-12-21
SG181431A1 (en) 2012-07-30
HK1172023A1 (en) 2013-04-12
AU2010338365A1 (en) 2012-06-07
BR112012015916A2 (pt) 2017-04-25
PT2519515E (pt) 2014-02-17

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