AU2010338365B2 - Pyrazine derivatives and their use in the treatment of neurological disorders - Google Patents

Pyrazine derivatives and their use in the treatment of neurological disorders Download PDF

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Publication number
AU2010338365B2
AU2010338365B2 AU2010338365A AU2010338365A AU2010338365B2 AU 2010338365 B2 AU2010338365 B2 AU 2010338365B2 AU 2010338365 A AU2010338365 A AU 2010338365A AU 2010338365 A AU2010338365 A AU 2010338365A AU 2010338365 B2 AU2010338365 B2 AU 2010338365B2
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AU
Australia
Prior art keywords
alkyl
alkoxy
alkylthio
halogen
amino
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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.)
Ceased
Application number
AU2010338365A
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English (en)
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AU2010338365A1 (en
Inventor
Marina Tintelnot-Blomley
Siem Jacob Veenstra
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Novartis AG
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Novartis AG
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43598456&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AU2010338365(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis AG filed Critical Novartis AG
Publication of AU2010338365A1 publication Critical patent/AU2010338365A1/en
Application granted granted Critical
Publication of AU2010338365B2 publication Critical patent/AU2010338365B2/en
Ceased legal-status Critical Current
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Classifications

    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (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)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (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)
AU2010338365A 2009-12-31 2010-12-22 Pyrazine derivatives and their use in the treatment of neurological disorders Ceased AU2010338365B2 (en)

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
AU2010338365A1 AU2010338365A1 (en) 2012-06-07
AU2010338365B2 true AU2010338365B2 (en) 2014-01-30

Family

ID=43598456

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2010338365A Ceased AU2010338365B2 (en) 2009-12-31 2010-12-22 Pyrazine derivatives and their use in the treatment of neurological disorders

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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US8173642B2 (en) 2005-10-25 2012-05-08 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives
MX2009011498A (es) 2007-04-24 2009-11-10 Shionogi & Co Derivados de aminodihidrotiazina sustituida con un grupo ciclico.
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
KR101324426B1 (ko) 2008-06-13 2013-10-31 시오노기세야쿠 가부시키가이샤 β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체
EP2360155A4 (en) 2008-10-22 2012-06-20 Shionogi & Co 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
RU2012129168A (ru) 2009-12-11 2014-01-20 Сионоги Энд Ко. Лтд. Производные оксазина
KR20130090793A (ko) * 2010-06-09 2013-08-14 얀센 파마슈티카 엔.브이. 베타-세크레타아제(ｂａｃｅ) 저해제로 유용한 5-아미노-3,6-디하이드로-1ｈ-피라진-2-온 유도체
AR081587A1 (es) 2010-06-09 2012-10-03 Janssen Pharmaceutica Nv DERIVADOS DE 5,6-DIHIDRO-2H-[1,4]OXAZIN-3-IL-AMINA UTILES COMO INHIBIDORES DE LA b-SECRETASA (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
AU2011347377B2 (en) 2010-12-22 2016-03-03 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
BR112013017988A2 (pt) * 2011-01-13 2019-09-24 Novartis Ag inibidores de bace-2 para o tratamento de distúrbios metabólicos
PH12013501480A1 (en) 2011-01-13 2022-10-26 Novartis Ag Novel heterocyclic derivatives and their use in the treatment of neurological disorders
EP2681219B1 (en) 2011-03-01 2015-10-28 Janssen Pharmaceutica, N.V. 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-ylamine derivatives useful as inhibitors of beta-secretase (bace)
CA2825620C (en) 2011-03-09 2019-04-23 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
WO2012138734A1 (en) 2011-04-07 2012-10-11 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
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
WO2013028670A1 (en) 2011-08-22 2013-02-28 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
WO2014099794A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. C5, c6 oxacyclic-fused iminothiazine dioxide compounds as bace inhibitors
BR112015030678A8 (pt) 2013-06-12 2020-01-07 Janssen Pharmaceutica Nv derivados 4-amino-6-fenil-5,6-di-hidroimidazo [1,5-a] pirazina como inibidores de beta-secretase (bace), composição farmacêutica, processo para preparação da mesma, e usos na fabricação de medicamentos
EA028775B1 (ru) 2013-06-12 2017-12-29 Янссен Фармацевтика Нв Производные 4-амино-6-фенил-6,7-дигидро[1,2,3]триазоло[1,5-a]пиразина в качестве ингибиторов бета-секретазы (bace)
EA032662B1 (ru) 2013-06-12 2019-06-28 Янссен Фармацевтика Нв ПРОИЗВОДНЫЕ 4-АМИНО-6-ФЕНИЛ-5,6-ДИГИДРОИМИДАЗО[1,5-а]ПИРАЗИН-3(2H)-ОНА В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (BACE)
EA031041B1 (ru) 2014-12-18 2018-11-30 Янссен Фармацевтика Нв Соединения 2,3,4,5-тетрагидропиридин-6-амин и 3,4-дигидро-2h-пиррол-5-амин - ингибиторы бета-секретазы
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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WO2002060492A1 (en) * 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
WO2007056341A1 (en) * 2005-11-08 2007-05-18 Vertex Pharmaceuticals Incorporated Heterocyclic modulators of atp-binding cassette transporters
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
WO2011009943A1 (en) * 2009-07-24 2011-01-27 Novartis Ag Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders

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KR20130090793A (ko) * 2010-06-09 2013-08-14 얀센 파마슈티카 엔.브이. 베타-세크레타아제(ｂａｃｅ) 저해제로 유용한 5-아미노-3,6-디하이드로-1ｈ-피라진-2-온 유도체
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

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001025229A1 (en) * 1999-10-01 2001-04-12 Fujisawa Pharmaceutical Co., Ltd. Amide compounds
WO2002060492A1 (en) * 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
EP1942105A1 (en) * 2005-10-25 2008-07-09 Shionogi Co., Ltd. Aminodihydrothiazine derivative
WO2007056341A1 (en) * 2005-11-08 2007-05-18 Vertex Pharmaceuticals Incorporated Heterocyclic modulators of atp-binding cassette transporters
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
WO2011009943A1 (en) * 2009-07-24 2011-01-27 Novartis Ag Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders

Also Published As

Publication number Publication date
CA2785341A1 (en) 2011-07-07
CN102712621A (zh) 2012-10-03
KR20120102795A (ko) 2012-09-18
PL2519515T3 (pl) 2014-04-30
BR112012015916A2 (pt) 2017-04-25
MX2012007754A (es) 2012-08-01
CN102712621B (zh) 2015-03-11
PH12012501007A1 (en) 2013-01-14
EA201200952A1 (ru) 2013-02-28
CR20120332A (es) 2012-07-12
NZ600136A (en) 2013-09-27
PE20121640A1 (es) 2012-12-17
HK1172023A1 (en) 2013-04-12
PT2519515E (pt) 2014-02-17
ZA201203614B (en) 2013-01-30
US20120277244A1 (en) 2012-11-01
GT201200219A (es) 2013-10-10
CU20120099A7 (es) 2012-07-31
EP2519515B1 (en) 2013-11-06
SG181431A1 (en) 2012-07-30
JP5600754B2 (ja) 2014-10-01
ES2445536T3 (es) 2014-03-03
TN2012000249A1 (en) 2013-12-12
AU2010338365A1 (en) 2012-06-07
JP2013516395A (ja) 2013-05-13
IL220268A0 (en) 2012-07-31
ECSP12012065A (es) 2012-08-31
HN2012001413A (es) 2015-03-23
CL2012001762A1 (es) 2012-12-21
KR101419157B1 (ko) 2014-07-11
US20150322038A1 (en) 2015-11-12
WO2011080176A1 (en) 2011-07-07
EP2519515A1 (en) 2012-11-07

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