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
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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
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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)
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
EP09152805.9 2009-02-13
EP09152805 2009-02-13
PCT/EP2010/000717 WO2010091824A1 (en) 2009-02-13 2010-02-05 Fused pyrimidines as akt inhibitors

Publications (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 (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
SG11201505631PA (en) 2013-01-23 2015-08-28 Astrazeneca Ab Chemical compounds
US10526660B2 (en) 2013-09-12 2020-01-07 Dana-Farber Cancer Institute, Inc. Methods for evaluating and treating Waldenstrom's macroglobulinemia
TWI720451B (zh) 2014-02-13 2021-03-01 美商英塞特控股公司 作為lsd1抑制劑之環丙胺
KR102421235B1 (ko) 2014-02-13 2022-07-15 인사이트 코포레이션 Lsd1 저해제로서 사이클로프로필아민
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
WO2016007722A1 (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
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
SG11201708047UA (en) 2015-04-03 2017-10-30 Incyte Corp Heterocyclic compounds as lsd1 inhibitors
CN110402244B (zh) 2015-08-12 2023-02-03 因赛特公司 Lsd1抑制剂的盐
WO2020047198A1 (en) 2018-08-31 2020-03-05 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
AU2005233584B2 (en) 2004-04-09 2010-12-09 Merck Sharp & Dohme Corp. 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
US7713973B2 (en) * 2004-10-15 2010-05-11 Takeda Pharmaceutical Company Limited Kinase inhibitors
JP2008530111A (ja) 2005-02-14 2008-08-07 メルク エンド カムパニー インコーポレーテッド Ａｋｔ活性の阻害剤
DK1898903T3 (da) 2005-06-10 2013-07-01 Merck Sharp & Dohme Inhibitorer af Akt-aktivitet
DE102007012645A1 (de) * 2007-03-16 2008-09-18 Bayer Healthcare Ag Substituierte Imidazo- und Triazolopyrimidine
PA8793301A1 (es) * 2007-08-14 2009-04-23 Bayer Schering Pharma Ag Imidazoles bicíclicos fusionados
PL2188291T3 (pl) * 2007-08-14 2013-06-28 Bayer Ip Gmbh Skondensowane bicykliczne pirymidyny

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

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