CN103097384B - 取代的咪唑并[1,2‑a]嘧啶和吡啶 - Google Patents

取代的咪唑并[1,2‑a]嘧啶和吡啶 Download PDF

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Publication number
CN103097384B
CN103097384B CN201180043391.XA CN201180043391A CN103097384B CN 103097384 B CN103097384 B CN 103097384B CN 201180043391 A CN201180043391 A CN 201180043391A CN 103097384 B CN103097384 B CN 103097384B
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Prior art keywords
phenyl
imidazo
pyridin
cyclobutylamine
cyclobutyl
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Expired - Fee Related
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CN201180043391.XA
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Chinese (zh)
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CN103097384A (zh
Inventor
S·英斯
A·哈格巴尔特
O·波利茨
R·诺伊豪斯
U·伯默
W·斯科特
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Bayer Intellectual Property GmbH
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    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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
    • C07D487/02—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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/04—Esters of boric acids

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201180043391.XA 2010-07-12 2011-07-07 取代的咪唑并[1,2‑a]嘧啶和吡啶 Expired - Fee Related CN103097384B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP10169205 2010-07-12
EP10169205.1 2010-07-12
US39277910P 2010-10-13 2010-10-13
US61/392,779 2010-10-13
PCT/EP2011/061508 WO2012007345A2 (en) 2010-07-12 2011-07-07 Substituted imidazo[1,2-a]pyrimidines and -pyridines

Publications (2)

Publication Number Publication Date
CN103097384A CN103097384A (zh) 2013-05-08
CN103097384B true CN103097384B (zh) 2017-02-15

Family

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CN201180043391.XA Expired - Fee Related CN103097384B (zh) 2010-07-12 2011-07-07 取代的咪唑并[1,2‑a]嘧啶和吡啶

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Country Link
US (1) US8975265B2 (enExample)
EP (1) EP2593451B1 (enExample)
JP (1) JP5830094B2 (enExample)
CN (1) CN103097384B (enExample)
AR (1) AR090005A1 (enExample)
CA (1) CA2804845A1 (enExample)
ES (1) ES2552841T3 (enExample)
TW (1) TW201206933A (enExample)
UY (1) UY33503A (enExample)
WO (1) WO2012007345A2 (enExample)

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HUE027509T2 (en) * 2011-04-06 2016-10-28 Taiho Pharmaceutical Co Ltd New imidazo-oxazine compounds or salts thereof
EP2694510B1 (en) * 2011-04-07 2015-10-14 Bayer Intellectual Property GmbH Imidazopyridazines as akt kinase inhibitors
EP2802588B1 (en) * 2012-01-10 2016-05-25 Bayer Intellectual Property GmbH Substituted pyrazolopyrimidines as akt kinase inhibitors
US9260435B2 (en) * 2012-01-10 2016-02-16 Bayer Pharma Aktiengesellschaft Substituted imidazopyrazines as Akt kinase inhibitors
US9309243B2 (en) 2012-07-13 2016-04-12 Ucb Biopharma Sprl Imidazopyridine derivatives as modulators of TNF activity
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
US9670210B2 (en) 2014-02-13 2017-06-06 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
WO2015123437A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
WO2015123408A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
EP3125920B1 (en) 2014-04-04 2020-12-23 Del Mar Pharmaceuticals Dianhydrogalactitol, diacetyldianhydrogalactitol or dibromodulcitol to treat non-small-cell carcinoma of the lung and ovarian cancer
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
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
WO2016007736A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyrazines as lsd1 inhibitors
CN111943962A (zh) 2015-02-27 2020-11-17 大鹏药品工业株式会社 咪唑并噁嗪晶体、含有所述晶体的药物组合物和制备所述晶体的方法
MX373154B (es) 2015-04-03 2020-04-22 Incyte Holdings Corp Compuestos heterocíclicos como inhibidores de demetilasa 1 específica de lisina (lsd1).
CN106188063A (zh) * 2015-05-08 2016-12-07 中国科学院上海药物研究所 用作Lp-PLA2抑制剂的双环类化合物、其制备方法及医药用途
LT3334709T (lt) 2015-08-12 2025-03-10 Incyte Holdings Corporation Lsd1 inhibitoriaus druskos
US11883404B2 (en) 2016-03-04 2024-01-30 Taiho Pharmaceuticals Co., Ltd. Preparation and composition for treatment of malignant tumors
UA125559C2 (uk) 2016-04-22 2022-04-20 Інсайт Корпорейшн Композиції інгібітора lsd1
WO2018013430A2 (en) 2016-07-12 2018-01-18 Arisan Therapeutics Inc. Heterocyclic compounds for the treatment of arenavirus infection
KR20190043437A (ko) 2017-10-18 2019-04-26 씨제이헬스케어 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
GB201811695D0 (en) * 2018-07-17 2018-08-29 Salvensis Compounds for use in the treatment of fascioliasis
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
US12419865B2 (en) 2018-12-06 2025-09-23 Arisan Therapeutics Inc. Compounds for the treatment of arenavirus infection
CN109734713B (zh) * 2019-03-07 2021-06-04 东华理工大学 一种3-亚胺基咪唑并[1,2-a]吡啶化合物

Citations (1)

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WO2009148916A1 (en) * 2008-06-03 2009-12-10 Merck & Co., Inc. Inhibitors of akt activity

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AU2006258124B8 (en) * 2005-06-10 2010-01-07 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
AR064010A1 (es) * 2006-12-06 2009-03-04 Merck & Co Inc Inhibidores de la actividad de la akt
TW200924761A (en) * 2007-08-14 2009-06-16 Bayer Schering Pharma Ag Fused bicyclic imidazoles
US8129394B2 (en) 2008-03-21 2012-03-06 Novartis Ag Heteroaryl-substituted imidazole compounds and uses thereof
EP2391623A4 (en) 2009-02-02 2012-09-05 Merck Sharp & Dohme HAMMER OF ACT ACTIVITY
US8168652B2 (en) 2009-03-12 2012-05-01 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
EP2473495A1 (en) 2009-09-18 2012-07-11 Almac Discovery Limited Pharmaceutical compounds
GB0919380D0 (en) 2009-11-04 2009-12-23 Almac Discovery Ltd Pharmaceutical compouds

Patent Citations (1)

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WO2009148916A1 (en) * 2008-06-03 2009-12-10 Merck & Co., Inc. Inhibitors of akt activity

Also Published As

Publication number Publication date
EP2593451B1 (en) 2015-08-19
CN103097384A (zh) 2013-05-08
CA2804845A1 (en) 2012-01-19
EP2593451A2 (en) 2013-05-22
ES2552841T3 (es) 2015-12-02
UY33503A (es) 2012-02-29
JP2013531684A (ja) 2013-08-08
US8975265B2 (en) 2015-03-10
WO2012007345A3 (en) 2012-04-12
JP5830094B2 (ja) 2015-12-09
AR090005A1 (es) 2014-10-15
TW201206933A (en) 2012-02-16
US20130190332A1 (en) 2013-07-25
WO2012007345A2 (en) 2012-01-19

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