CN102361872B - 作为akt抑制剂的稠合嘧啶 - Google Patents

作为akt抑制剂的稠合嘧啶 Download PDF

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Publication number
CN102361872B
CN102361872B CN201080012970.3A CN201080012970A CN102361872B CN 102361872 B CN102361872 B CN 102361872B CN 201080012970 A CN201080012970 A CN 201080012970A CN 102361872 B CN102361872 B CN 102361872B
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CN
China
Prior art keywords
compound
compounds
alkyl
formula
hydrogen
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
CN201080012970.3A
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English (en)
Chinese (zh)
Other versions
CN102361872A (zh
Inventor
M·芬内曼
T·贝尔
T·迈尔
S·赫尔德
G·贝内克
F·德默尔
A·齐尔希
A·施特鲁布
T·贝克尔斯
S·英斯
H·雷温克尔
刘宁姝
U·伯默
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 Pharma AG
Original Assignee
Bayer Pharma AG
Bayer Intellectual Property GmbH
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Publication of CN102361872A publication Critical patent/CN102361872A/zh
Application granted granted Critical
Publication of CN102361872B publication Critical patent/CN102361872B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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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

Landscapes

  • 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)
CN201080012970.3A 2009-02-13 2010-02-05 作为akt抑制剂的稠合嘧啶 Expired - Fee Related CN102361872B (zh)

Applications Claiming Priority (3)

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

Publications (2)

Publication Number Publication Date
CN102361872A CN102361872A (zh) 2012-02-22
CN102361872B true CN102361872B (zh) 2014-12-03

Family

ID=42019301

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201080012970.3A Expired - Fee Related CN102361872B (zh) 2009-02-13 2010-02-05 作为akt抑制剂的稠合嘧啶

Country Status (7)

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

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
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
EP3105218B1 (en) 2014-02-13 2019-09-25 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
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
WO2016007731A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyridines and imidazopyrazines as lsd1 inhibitors
US9695167B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors
US9695180B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors
EP3277689B1 (en) 2015-04-03 2019-09-04 Incyte Corporation Heterocyclic compounds as lsd1 inhibitors
MY189367A (en) 2015-08-12 2022-02-08 Incyte Corp Salts of an lsd1 inhibitor
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1668619A (zh) * 2002-04-19 2005-09-14 细胞基因组公司 咪唑并[1,2－а]吡嗪－8－基胺,其制备方法及使用方法
CN1809354A (zh) * 2003-04-24 2006-07-26 麦克公司 Akt活性抑制剂
CN101242834A (zh) * 2004-12-15 2008-08-13 默克公司 Akt活性抑制剂

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2561311A1 (en) 2004-04-09 2005-10-27 Merck & Co., Inc. Inhibitors of akt activity
EP1784175A4 (en) 2004-08-23 2009-07-22 Merck & Co Inc INHIBITORS OF ACT ACTIVITY
EP1812439B2 (en) * 2004-10-15 2017-12-06 Takeda Pharmaceutical Company Limited Kinase inhibitors
AU2006216998B2 (en) 2005-02-14 2010-12-23 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
EP1898903B8 (en) 2005-06-10 2013-05-15 Merck Sharp & Dohme Corp. Inhibitors of akt activity
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1668619A (zh) * 2002-04-19 2005-09-14 细胞基因组公司 咪唑并[1,2－а]吡嗪－8－基胺,其制备方法及使用方法
CN1809354A (zh) * 2003-04-24 2006-07-26 麦克公司 Akt活性抑制剂
CN101242834A (zh) * 2004-12-15 2008-08-13 默克公司 Akt活性抑制剂

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Rapid assembly of diverse and potent allosteric Akt inhibitors;Zhicai Wu，等;《Bioorganic & Medicinal Chemistry Letters》;20071017;第18卷(第6期);第2212页第1栏Scheme 1 *

Also Published As

Publication number Publication date
JP5667085B2 (ja) 2015-02-12
CA2752114A1 (en) 2010-08-19
CN102361872A (zh) 2012-02-22
JP2012517965A (ja) 2012-08-09
EP2396331A1 (en) 2011-12-21
ES2435804T3 (es) 2013-12-23
US20130310362A1 (en) 2013-11-21
EP2396331B1 (en) 2013-10-16
CA2752114C (en) 2017-06-20
WO2010091824A1 (en) 2010-08-19
HK1166984A1 (en) 2012-11-16

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