CN102971321B - 咪唑并吡嗪 - Google Patents

咪唑并吡嗪 Download PDF

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Publication number
CN102971321B
CN102971321B CN201180024369.0A CN201180024369A CN102971321B CN 102971321 B CN102971321 B CN 102971321B CN 201180024369 A CN201180024369 A CN 201180024369A CN 102971321 B CN102971321 B CN 102971321B
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CN
China
Prior art keywords
cyclopropyl
base
pyrazine
alkyl
benzamide
Prior art date
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.)
Expired - Fee Related
Application number
CN201180024369.0A
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English (en)
Chinese (zh)
Other versions
CN102971321A (zh
Inventor
U·克拉尔
M·科皮茨
D·科泽蒙德
R·博尔曼
B·巴德尔
P·利瑙
G·西迈斯特
S·佩克特
D·阮
W·斯科特
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Bayer Pharma AG
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Bayer Pharma AG
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Publication of CN102971321A publication Critical patent/CN102971321A/zh
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Publication of CN102971321B publication Critical patent/CN102971321B/zh
Expired - Fee Related legal-status Critical Current
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Classifications

    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201180024369.0A 2010-03-18 2011-03-16 咪唑并吡嗪 Expired - Fee Related CN102971321B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP10075121 2010-03-18
EP10075121.3 2010-03-18
PCT/EP2011/053967 WO2011113862A1 (en) 2010-03-18 2011-03-16 Imidazopyrazines

Publications (2)

Publication Number Publication Date
CN102971321A CN102971321A (zh) 2013-03-13
CN102971321B true CN102971321B (zh) 2015-07-29

Family

ID=43778175

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201180024369.0A Expired - Fee Related CN102971321B (zh) 2010-03-18 2011-03-16 咪唑并吡嗪

Country Status (7)

Country Link
US (1) US9468642B2 (https=)
EP (1) EP2547680B1 (https=)
JP (1) JP5841078B2 (https=)
CN (1) CN102971321B (https=)
CA (1) CA2793279A1 (https=)
ES (1) ES2551407T3 (https=)
WO (1) WO2011113862A1 (https=)

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* Cited by examiner, † Cited by third party
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TWI541243B (zh) 2010-09-10 2016-07-11 拜耳知識產權公司 經取代咪唑并嗒
JP5822944B2 (ja) * 2010-12-17 2015-11-25 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ 過剰増殖性障害の治療におけるｍｐｓ−１およびｔｋｋ阻害剤として使用するための２置換イミダゾピラジン
US9284317B2 (en) * 2010-12-17 2016-03-15 Bayer Intellectual Property Gmbh Substituted imidazo[1,2-a]pyrazines as MPS-1 inhibitors
JP2013545779A (ja) * 2010-12-17 2013-12-26 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング 過剰増殖性障害の治療におけるｍｐｓ−１およびｔｋｋ阻害剤として使用するための６置換イミダゾピラジン
WO2014020043A1 (en) 2012-08-02 2014-02-06 Bayer Pharma Aktiengesellschaft Combinations for the treatment of cancer
WO2014020041A1 (en) 2012-08-02 2014-02-06 Bayer Pharma Aktiengesellschaft Combinations for the treatment of cancer
EP3105219B9 (en) 2014-02-13 2018-10-03 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
MX373103B (es) 2014-02-13 2020-04-17 Incyte Holdings Corp Ciclopropilaminas como inhibidores de desmetilasa específica de lisina 1 (lsd1).
SI3105218T1 (sl) 2014-02-13 2019-11-29 Incyte Corp Ciklopropilamini kot inhibitorji LSD1
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
TWI687419B (zh) 2014-07-10 2020-03-11 美商英塞特公司 作為ｌｓｄ１抑制劑之咪唑并吡啶及咪唑并吡嗪
EP3277689B1 (en) 2015-04-03 2019-09-04 Incyte Corporation Heterocyclic compounds as lsd1 inhibitors
FI3283642T3 (fi) 2015-04-17 2024-01-11 Crossfire Oncology Holding B V Prognostisia biomarkkereita ttk-inhibiittorikemoterapiaan
LT3334709T (lt) 2015-08-12 2025-03-10 Incyte Holdings Corporation Lsd1 inhibitoriaus druskos
JP6999574B2 (ja) 2016-04-22 2022-01-18 インサイト・コーポレイション Ｌｓｄ１阻害剤の製剤
US10239885B1 (en) 2018-06-18 2019-03-26 Avista Pharma Solutions, Inc. Compound 1-[2-[4-(2-ethyl-6,8-dimethylimidazo[1,2-α]pyrazin-3-yl)phenyl]ethyl]-3-(p-tolylsulfonyl)urea as a prostaglandin EP4 receptor antagonist
WO2020047198A1 (en) 2018-08-31 2020-03-05 Incyte Corporation Salts of an lsd1 inhibitor and processes for preparing the same
US11512088B2 (en) 2019-01-30 2022-11-29 Avista Pharma Solutions, Inc. Synthetic process and intermediates
WO2020160075A1 (en) 2019-01-30 2020-08-06 Avista Pharma Solutions, Inc. Chemical compounds

Citations (4)

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WO2008057512A2 (en) * 2006-11-08 2008-05-15 Schering Corporation Imidazopyrazines as protein kinase inhibitors
WO2009024585A2 (en) * 2007-08-21 2009-02-26 Biofocus Dpi Limited Imidazo [1,2-a] pyrazine compounds for treatment of viral infections such as hepatitis
WO2010069684A1 (en) * 2008-12-17 2010-06-24 Biomarin Iga, Ltd. Compounds for treatment of duchenne muscular dystrophy
WO2011013729A1 (ja) * 2009-07-30 2011-02-03 オンコセラピー・サイエンス株式会社 Ｔｔｋ阻害作用を有する縮合イミダゾール誘導体

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TW200413378A (en) 2002-09-23 2004-08-01 Schering Corp Novel imidazopyrazines as cyclin dependent kinase inhibitors
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EP1945216A1 (en) 2005-11-10 2008-07-23 Schering Corporation Methods for inhibiting protein kinases
US7893058B2 (en) 2006-05-15 2011-02-22 Janssen Pharmaceutica Nv Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases
AR061229A1 (es) 2006-06-06 2008-08-13 Schering Corp Imidazopirazinas como inhibidores de la proteina quinasa
US20090175852A1 (en) 2006-06-06 2009-07-09 Schering Corporation Imidazopyrazines as protein kinase inhibitors
US8268809B2 (en) 2006-09-05 2012-09-18 Emory University Kinase inhibitors for preventing or treating pathogen infection and method of use thereof
US20100298314A1 (en) 2006-12-20 2010-11-25 Schering Corporation Novel jnk inhibitors
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Patent Citations (4)

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WO2008057512A2 (en) * 2006-11-08 2008-05-15 Schering Corporation Imidazopyrazines as protein kinase inhibitors
WO2009024585A2 (en) * 2007-08-21 2009-02-26 Biofocus Dpi Limited Imidazo [1,2-a] pyrazine compounds for treatment of viral infections such as hepatitis
WO2010069684A1 (en) * 2008-12-17 2010-06-24 Biomarin Iga, Ltd. Compounds for treatment of duchenne muscular dystrophy
WO2011013729A1 (ja) * 2009-07-30 2011-02-03 オンコセラピー・サイエンス株式会社 Ｔｔｋ阻害作用を有する縮合イミダゾール誘導体

Non-Patent Citations (1)

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Also Published As

Publication number Publication date
EP2547680B1 (en) 2015-08-05
US20130195848A1 (en) 2013-08-01
EP2547680A1 (en) 2013-01-23
ES2551407T3 (es) 2015-11-18
US9468642B2 (en) 2016-10-18
HK1183297A1 (zh) 2013-12-20
WO2011113862A1 (en) 2011-09-22
CA2793279A1 (en) 2011-09-22
JP5841078B2 (ja) 2016-01-06
JP2013522275A (ja) 2013-06-13
CN102971321A (zh) 2013-03-13

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