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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (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 (https=)
EP (1) EP2519515B1 (https=)
JP (1) JP5600754B2 (https=)
KR (1) KR101419157B1 (https=)
CN (1) CN102712621B (https=)
AU (1) AU2010338365B2 (https=)
BR (1) BR112012015916A2 (https=)
CA (1) CA2785341A1 (https=)
CL (1) CL2012001762A1 (https=)
CR (1) CR20120332A (https=)
CU (1) CU20120099A7 (https=)
EA (1) EA201200952A1 (https=)
EC (1) ECSP12012065A (https=)
ES (1) ES2445536T3 (https=)
GT (1) GT201200219A (https=)
HN (1) HN2012001413A (https=)
IL (1) IL220268A0 (https=)
MX (1) MX2012007754A (https=)
NZ (1) NZ600136A (https=)
PE (1) PE20121640A1 (https=)
PH (1) PH12012501007A1 (https=)
PL (1) PL2519515T3 (https=)
PT (1) PT2519515E (https=)
SG (1) SG181431A1 (https=)
TN (1) TN2012000249A1 (https=)
WO (1) WO2011080176A1 (https=)
ZA (1) ZA201203614B (https=)

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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
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KR101730937B1 (ko) 2010-06-09 2017-04-27 얀센 파마슈티카 엔.브이. 베타-세크레타아제(ｂａｃｅ) 저해제로 유용한 5,6-디하이드로-2ｈ-[1,4]옥사진-3-일-아민 유도체
CN102985412A (zh) * 2010-06-28 2013-03-20 詹森药业有限公司 可用于治疗阿尔茨海默病及其它形式的痴呆的3-氨基-5,6-二氢-1h-吡嗪-2-酮衍生物
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
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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
MX2013008192A (es) * 2011-01-13 2013-12-16 Novartis Ag Inhibidores de bace-2 para tratamiento de transtornos metabolicos.
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
EP2683721B1 (en) 2011-03-09 2015-01-28 Janssen Pharmaceutica N.V. 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
JP2014514302A (ja) 2011-04-13 2014-06-19 メルク・シャープ・アンド・ドーム・コーポレーション Ｂａｃｅ阻害薬としての５−置換されたイミノチアジン類およびそれのモノおよびジオキシド、組成物およびそれらの使用
TW201247635A (en) 2011-04-26 2012-12-01 Shionogi & Co Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them
RU2014111055A (ru) 2011-08-22 2015-09-27 Мерк Шарп И Доум Корп. 2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение
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
EP2934539B1 (en) 2012-12-20 2019-03-27 Merck Sharp & Dohme Corp. C5, c6 oxacyclic-fused iminothiazine dioxide compounds as bace inhibitors
CA2912156C (en) 2013-06-12 2021-07-20 Janssen Pharmaceutica Nv 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace)
KR102243134B1 (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 유도체
WO2014198854A1 (en) 2013-06-12 2014-12-18 Janssen Pharmaceutica Nv 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace)
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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

Also Published As

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

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