KR101419157B1 - 피라진 유도체 및 신경계 장애의 치료에서의 그의 용도 - Google Patents

피라진 유도체 및 신경계 장애의 치료에서의 그의 용도 Download PDF

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Publication number
KR101419157B1
KR101419157B1 KR1020127019872A KR20127019872A KR101419157B1 KR 101419157 B1 KR101419157 B1 KR 101419157B1 KR 1020127019872 A KR1020127019872 A KR 1020127019872A KR 20127019872 A KR20127019872 A KR 20127019872A KR 101419157 B1 KR101419157 B1 KR 101419157B1
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KR
South Korea
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alkyl
alkoxy
halogen
amino
phenyl
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Expired - Fee Related
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KR1020127019872A
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English (en)
Korean (ko)
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KR20120102795A (ko
Inventor
마리나 틴텔노트-블롬레이
시엠 야콥 벤스트라
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노파르티스 아게
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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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (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)
KR1020127019872A 2009-12-31 2010-12-22 피라진 유도체 및 신경계 장애의 치료에서의 그의 용도 Expired - Fee Related KR101419157B1 (ko)

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
KR20120102795A KR20120102795A (ko) 2012-09-18
KR101419157B1 true KR101419157B1 (ko) 2014-07-11

Family

ID=43598456

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020127019872A Expired - Fee Related KR101419157B1 (ko) 2009-12-31 2010-12-22 피라진 유도체 및 신경계 장애의 치료에서의 그의 용도

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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KR101052122B1 (ko) 2005-10-25 2011-07-26 시오노기세야쿠 가부시키가이샤 아미노디히드로티아진 유도체
EP2147914B1 (en) 2007-04-24 2014-06-04 Shionogi&Co., Ltd. Aminodihydrothiazine derivatives substituted with cyclic groups
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
MX2010013256A (es) 2008-06-13 2010-12-21 Shionogi & Co Derivado heterociclico que contiene azufre que tiene actividad inhibitoria de beta-secretasa.
JPWO2010047372A1 (ja) 2008-10-22 2012-03-22 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
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
JPWO2011071135A1 (ja) 2009-12-11 2013-04-22 塩野義製薬株式会社 オキサジン誘導体
EA201291366A1 (ru) * 2010-06-09 2013-04-30 Янссен Фармацевтика Нв Производные 5-амино-3,6-дигидро-1h-пиразин-2-она в качестве ингибиторов бета-секретазы (bace)
EA021240B1 (ru) 2010-06-09 2015-05-29 Янссен Фармацевтика Нв Производные 5,6-дигидро-2h-[1,4]оксазин-3-иламина в качестве ингибиторов бета-секретазы (bace)
EP2585440A1 (en) * 2010-06-28 2013-05-01 Janssen Pharmaceutica, N.V. 3-amino-5,6-dihydro-1h-pyrazin-2-one derivatives useful for the treatement of alzheimer's disease and other forms of dementia
CA2816285A1 (en) 2010-10-29 2012-05-03 Shionogi & Co., Ltd. Naphthyridine derivative
EP2634188A4 (en) 2010-10-29 2014-05-07 Shionogi & Co FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE
US9840507B2 (en) 2010-12-22 2017-12-12 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
CN106117193B (zh) 2011-01-13 2019-09-13 诺华股份有限公司 新的杂环衍生物及其在神经性疾病治疗中的应用
EP2663308A1 (en) * 2011-01-13 2013-11-20 Novartis AG Bace-2 inhibitors for the treatment of metabolic disorders
HUE026338T2 (en) 2011-03-01 2016-05-30 Janssen Pharmaceutica Nv 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-ylamine derivatives useful as inhibitors of beta-secretase (bace)
MX340031B (es) 2011-03-09 2016-06-21 Janssen Pharmaceutica Nv Derivados de 3,4-dihidropirrolo[1,2-a]pirazin-1-ilamina utiles como inhibidores de beta-secretasa (bace).
US9221839B2 (en) 2011-04-07 2015-12-29 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
MX2013011947A (es) 2011-04-13 2014-01-16 Merck Sharp & Dohme Iminotiazinas 5-sustituidas y sus monoxidos y dioxidos como inhibidores de la enzima que encinde la proteina precursora amiloide en el sitio beta, composiciones y su uso.
TW201247635A (en) 2011-04-26 2012-12-01 Shionogi & Co Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them
EP2747769B1 (en) 2011-08-22 2017-08-02 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use
US8338413B1 (en) 2012-03-07 2012-12-25 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
JP2016501827A (ja) 2012-10-24 2016-01-21 塩野義製薬株式会社 Ｂａｃｅ１阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体
EP2934539B1 (en) 2012-12-20 2019-03-27 Merck Sharp & Dohme Corp. C5, c6 oxacyclic-fused iminothiazine dioxide compounds as bace inhibitors
ES2721073T3 (es) 2013-06-12 2019-07-26 Janssen Pharmaceutica Nv Derivados de 4-amino-6-fenil-6,7-dihidro[1,2,3]triazolo[1,5 a]pirazina como inhibidores de beta-secretasa (BACE)
CA2911690C (en) 2013-06-12 2021-08-24 Janssen Pharmaceutica Nv 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace)
MX368326B (es) 2013-06-12 2019-09-27 Janssen Pharmaceutica Nv Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5-a]pirazin-3(2h )-ona como inhibidores de beta-secretasa (bace).
AU2015367594C1 (en) 2014-12-18 2019-10-31 Janssen Pharmaceutica Nv 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2H-pyrrol-5-amine compound inhibitors of beta-secretase
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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WO2001025229A1 (en) * 1999-10-01 2001-04-12 Fujisawa Pharmaceutical Co., Ltd. Amide compounds
WO2008079933A2 (en) * 2006-12-22 2008-07-03 Novartis Ag Heteroaryl-heteroaryl compounds as cdk inhibitors for the treatment of cancer, inflammation and viral infections
EP1942105A1 (en) * 2005-10-25 2008-07-09 Shionogi Co., Ltd. Aminodihydrothiazine derivative

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EP1702919B1 (en) 2003-12-29 2012-05-30 Msd K.K. Novel 2-heteroaryl-substituted benzimidazole derivative
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US20100317850A1 (en) 2008-01-18 2010-12-16 Yuichi Suzuki Condensed aminodihydrothiazine derivative
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AR077328A1 (es) * 2009-07-24 2011-08-17 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos
EA201291366A1 (ru) * 2010-06-09 2013-04-30 Янссен Фармацевтика Нв Производные 5-амино-3,6-дигидро-1h-пиразин-2-она в качестве ингибиторов бета-секретазы (bace)
EP2585440A1 (en) * 2010-06-28 2013-05-01 Janssen Pharmaceutica, N.V. 3-amino-5,6-dihydro-1h-pyrazin-2-one derivatives useful for the treatement of alzheimer's disease and other forms of dementia

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Publication number Priority date Publication date Assignee Title
WO2001025229A1 (en) * 1999-10-01 2001-04-12 Fujisawa Pharmaceutical Co., Ltd. Amide compounds
EP1942105A1 (en) * 2005-10-25 2008-07-09 Shionogi Co., Ltd. Aminodihydrothiazine derivative
WO2008079933A2 (en) * 2006-12-22 2008-07-03 Novartis Ag Heteroaryl-heteroaryl compounds as cdk inhibitors for the treatment of cancer, inflammation and viral infections

Also Published As

Publication number Publication date
NZ600136A (en) 2013-09-27
HN2012001413A (es) 2015-03-23
JP2013516395A (ja) 2013-05-13
EP2519515A1 (en) 2012-11-07
PT2519515E (pt) 2014-02-17
CN102712621B (zh) 2015-03-11
HK1172023A1 (en) 2013-04-12
ECSP12012065A (es) 2012-08-31
ES2445536T3 (es) 2014-03-03
TN2012000249A1 (en) 2013-12-12
MX2012007754A (es) 2012-08-01
IL220268A0 (en) 2012-07-31
US20120277244A1 (en) 2012-11-01
WO2011080176A1 (en) 2011-07-07
US20150322038A1 (en) 2015-11-12
CU20120099A7 (es) 2012-07-31
ZA201203614B (en) 2013-01-30
EP2519515B1 (en) 2013-11-06
JP5600754B2 (ja) 2014-10-01
CL2012001762A1 (es) 2012-12-21
CA2785341A1 (en) 2011-07-07
AU2010338365A1 (en) 2012-06-07
PL2519515T3 (pl) 2014-04-30
BR112012015916A2 (pt) 2017-04-25
KR20120102795A (ko) 2012-09-18
SG181431A1 (en) 2012-07-30
EA201200952A1 (ru) 2013-02-28
CN102712621A (zh) 2012-10-03
GT201200219A (es) 2013-10-10
PE20121640A1 (es) 2012-12-17
PH12012501007A1 (en) 2013-01-14
AU2010338365B2 (en) 2014-01-30
CR20120332A (es) 2012-07-12

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