JP5667085B2 - Ａｋｔインヒビターとしての融合されたピリミジン - Google Patents

Ａｋｔインヒビターとしての融合されたピリミジン Download PDF

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Publication number
JP5667085B2
JP5667085B2 JP2011549472A JP2011549472A JP5667085B2 JP 5667085 B2 JP5667085 B2 JP 5667085B2 JP 2011549472 A JP2011549472 A JP 2011549472A JP 2011549472 A JP2011549472 A JP 2011549472A JP 5667085 B2 JP5667085 B2 JP 5667085B2
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JP
Japan
Prior art keywords
alkyl
compound
hydrogen
halogen
optionally
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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.)
Expired - Fee Related
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JP2011549472A
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English (en)
Japanese (ja)
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JP2012517965A (ja
JP2012517965A5 (enExample
Inventor
フェンネマン マティアス
フェンネマン マティアス
ベール トマス
ベール トマス
マイアー トマス
マイアー トマス
ヘルダー スベン
ヘルダー スベン
ベネケ ゲリット
ベネケ ゲリット
デーメル フロリアン
デーメル フロリアン
ツルヒ アルミン
ツルヒ アルミン
ストルブ アンドレアス
ストルブ アンドレアス
ベッケルズ トーマス
ベッケルズ トーマス
インス ステュアート
インス ステュアート
レービンケル ハルトムット
レービンケル ハルトムット
リウ ニングシュ
リウ ニングシュ
ベーマー ウルフ
ベーマー ウルフ
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer Intellectual Property GmbH
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Bayer Intellectual Property GmbH
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Publication date
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Publication of JP2012517965A publication Critical patent/JP2012517965A/ja
Publication of JP2012517965A5 publication Critical patent/JP2012517965A5/ja
Application granted granted Critical
Publication of JP5667085B2 publication Critical patent/JP5667085B2/ja
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
    • A61P35/00—Antineoplastic agents
    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2011549472A 2009-02-13 2010-02-05 Ａｋｔインヒビターとしての融合されたピリミジン Expired - Fee Related JP5667085B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09152805.9 2009-02-13
EP09152805 2009-02-13
PCT/EP2010/000717 WO2010091824A1 (en) 2009-02-13 2010-02-05 Fused pyrimidines as akt inhibitors

Publications (3)

Publication Number Publication Date
JP2012517965A JP2012517965A (ja) 2012-08-09
JP2012517965A5 JP2012517965A5 (enExample) 2014-09-04
JP5667085B2 true JP5667085B2 (ja) 2015-02-12

Family

ID=42019301

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2011549472A Expired - Fee Related JP5667085B2 (ja) 2009-02-13 2010-02-05 Ａｋｔインヒビターとしての融合されたピリミジン

Country Status (7)

Country Link
US (1) US20130310362A1 (enExample)
EP (1) EP2396331B1 (enExample)
JP (1) JP5667085B2 (enExample)
CN (1) CN102361872B (enExample)
CA (1) CA2752114C (enExample)
ES (1) ES2435804T3 (enExample)
WO (1) WO2010091824A1 (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2897279C (en) * 2013-01-23 2020-12-29 Astrazeneca Ab Aminopyrazine derivatives and pharmaceutical compositions thereof for use in the treatment of cancer
AU2014318614B2 (en) 2013-09-12 2021-01-07 Dana-Farber Cancer Institute Inc. Methods for evaluating and treating Waldenstrom's macroglobulinemia
CN106164066B (zh) 2014-02-13 2020-01-17 因赛特公司 作为lsd1抑制剂的环丙胺
JP6602779B2 (ja) 2014-02-13 2019-11-06 インサイト・コーポレイション Ｌｓｄ１阻害剤としてのシクロプロピルアミン類
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
EP2907811A1 (en) 2014-02-14 2015-08-19 Actelion Pharmaceuticals Ltd. Process for manufacturing pyrimidine sulfamide derivatives
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
US9695168B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]pyrazines as LSD1 inhibitors
CN107660205B (zh) 2015-04-03 2021-08-27 因赛特公司 作为lsd1抑制剂的杂环化合物
EA035534B1 (ru) 2015-08-12 2020-06-30 Инсайт Корпорейшн Соли ингибитора lsd1
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL164703A0 (en) * 2002-04-19 2005-12-18 Cellular Genomics Inc ImidazoÄ1,2-AÜpyrazin-8-ylamines method of making and method of use thereof
US7579355B2 (en) 2003-04-24 2009-08-25 Merck & Co., Inc. Inhibitors of Akt activity
WO2005100344A1 (en) 2004-04-09 2005-10-27 Merck & Co., Inc. Inhibitors of akt activity
JP2008510823A (ja) 2004-08-23 2008-04-10 メルク エンド カムパニー インコーポレーテッド Ａｋｔ活性阻害剤
WO2006044687A2 (en) * 2004-10-15 2006-04-27 Takeda San Diego, Inc. Kinase inhibitors
EP1827436A4 (en) 2004-12-15 2011-08-10 Merck Sharp & Dohme INHIBITORS OF ACT ACTIVITY
EP1850843A4 (en) 2005-02-14 2012-02-15 Merck Sharp & Dohme INHIBITORS OF ACT ACTIVITY
KR100959771B1 (ko) 2005-06-10 2010-05-28 머크 샤프 앤드 돔 코포레이션 Ａｋｔ 활성의 억제제
DE102007012645A1 (de) * 2007-03-16 2008-09-18 Bayer Healthcare Ag Substituierte Imidazo- und Triazolopyrimidine
WO2009021990A1 (en) * 2007-08-14 2009-02-19 Bayer Schering Pharma Aktiengesellschaft Fused imidazoles for cancer treatment
NZ583267A (en) * 2007-08-14 2012-03-30 Bayer Schering Pharma Ag Fused bicyclic pyrimidines

Also Published As

Publication number Publication date
WO2010091824A1 (en) 2010-08-19
US20130310362A1 (en) 2013-11-21
EP2396331B1 (en) 2013-10-16
CA2752114C (en) 2017-06-20
CA2752114A1 (en) 2010-08-19
EP2396331A1 (en) 2011-12-21
HK1166984A1 (en) 2012-11-16
JP2012517965A (ja) 2012-08-09
CN102361872A (zh) 2012-02-22
CN102361872B (zh) 2014-12-03
ES2435804T3 (es) 2013-12-23

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