CN102574845B - 1H-咪唑并[4,5-c]喹啉酮衍生物 - Google Patents

1H-咪唑并[4,5-c]喹啉酮衍生物 Download PDF

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Publication number
CN102574845B
CN102574845B CN201080034616.0A CN201080034616A CN102574845B CN 102574845 B CN102574845 B CN 102574845B CN 201080034616 A CN201080034616 A CN 201080034616A CN 102574845 B CN102574845 B CN 102574845B
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pyridyl
methyl
pyridin
substituted
amino
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Expired - Fee Related
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Chinese (zh)
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CN102574845A (zh
Inventor
P·菲雷
F·S·卡尔特霍夫
R·马
C·拉格特
F·施陶费尔
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Novartis AG
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/12Keratolytics, e.g. wart or anti-corn preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201080034616.0A 2009-06-04 2010-06-02 1H-咪唑并[4,5-c]喹啉酮衍生物 Expired - Fee Related CN102574845B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US18414109P 2009-06-04 2009-06-04
US61/184,141 2009-06-04
PCT/EP2010/057719 WO2010139731A1 (en) 2009-06-04 2010-06-02 1H-IMIDAZO[4,5-c]QUINOLINONE DERIVATIVES

Publications (2)

Publication Number Publication Date
CN102574845A CN102574845A (zh) 2012-07-11
CN102574845B true CN102574845B (zh) 2015-09-02

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Country Link
US (2) US8476294B2 (enExample)
EP (1) EP2438064A1 (enExample)
JP (1) JP5596137B2 (enExample)
KR (1) KR101445458B1 (enExample)
CN (1) CN102574845B (enExample)
AR (1) AR076949A1 (enExample)
AU (1) AU2010255727B2 (enExample)
BR (1) BRPI1010621A2 (enExample)
CA (1) CA2763821A1 (enExample)
CL (1) CL2011003052A1 (enExample)
CO (1) CO6470887A2 (enExample)
CR (1) CR20110608A (enExample)
CU (1) CU24064B1 (enExample)
DO (1) DOP2011000373A (enExample)
EA (1) EA020715B1 (enExample)
EC (1) ECSP11011500A (enExample)
GE (1) GEP20156267B (enExample)
IL (1) IL216452A0 (enExample)
MA (1) MA33332B1 (enExample)
MX (1) MX2011012943A (enExample)
NI (1) NI201100209A (enExample)
NZ (1) NZ596487A (enExample)
PE (1) PE20120224A1 (enExample)
SG (1) SG176572A1 (enExample)
TN (1) TN2011000626A1 (enExample)
TW (1) TWI464168B (enExample)
UA (1) UA106074C2 (enExample)
UY (1) UY32682A (enExample)
WO (1) WO2010139731A1 (enExample)
ZA (1) ZA201108439B (enExample)

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DE102010035744A1 (de) 2010-08-28 2012-03-01 Merck Patent Gmbh Imidazolonylchinoline
KR20140014104A (ko) * 2010-12-06 2014-02-05 피라말 엔터프라이지즈 리미티드 치환된 이미다조퀴놀린 유도체
JO3003B1 (ar) 2011-01-14 2016-09-05 Lilly Co Eli مركب أيميدازو [4، 5 -c ] كينولين-2- واحد واستخدامه كمثبط كيناز PI3/mtor
US9284315B2 (en) 2011-11-17 2016-03-15 Zuanzhu Pharma Co., Ltd. Three-ring PI3K and/or mTOR inhibitor
WO2014141118A1 (en) * 2013-03-14 2014-09-18 Piramal Enterprises Limited Imidazo[4,5-c]quinoline derivatives and uses thereof
JP6419783B2 (ja) 2013-04-15 2018-11-07 エフ エム シー コーポレーションFmc Corporation 殺菌・殺カビ性アミド
CN105531348B (zh) * 2013-09-11 2017-11-07 默克专利有限公司 杂环化合物
CN104513254B (zh) 2013-09-30 2019-07-26 上海璎黎药业有限公司 稠合嘧啶类化合物、中间体、其制备方法、组合物和应用
JP6606428B2 (ja) * 2013-10-11 2019-11-13 国立大学法人 東京医科歯科大学 脊髄小脳変性症を予防又は治療するための薬剤
CN104447740B (zh) * 2013-11-20 2017-02-22 北京富龙康泰生物技术有限公司 咪唑酮类衍生物、其药物组合物和用途
NO2714752T3 (enExample) 2014-05-08 2018-04-21
HRP20181670T1 (hr) 2014-06-03 2018-12-14 Idorsia Pharmaceuticals Ltd Spojevi pirazola i njihova uporaba kao blokatora kalcijevih kanala t-tipa
HUE054745T2 (hu) * 2015-04-02 2021-09-28 Merck Patent Gmbh Imidazolonilkinolinok és alkalmazásuk ATM-kináz-inhibitorokként
GB201516504D0 (en) 2015-09-17 2015-11-04 Astrazeneca Ab Imadazo(4,5-c)quinolin-2-one Compounds and their use in treating cancer
GB201519568D0 (en) * 2015-11-05 2015-12-23 Astrazeneca Ab Imidazo[4,5-c]quinolin-2-one compounds and their use in treating cancer
US10988472B2 (en) 2016-10-13 2021-04-27 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Compounds and method for blocking transmission of malarial parasite
EP3554490B1 (en) 2016-12-16 2022-02-16 Idorsia Pharmaceuticals Ltd Pharmaceutical combination comprising a t-type calcium channel blocker
TWI808960B (zh) 2017-02-06 2023-07-21 瑞士商愛杜西亞製藥有限公司 用於合成1-芳基-1-三氟甲基環丙烷之新穎方法
JOP20190209A1 (ar) * 2017-03-16 2019-09-12 Astrazeneca Ab مركبات إيميدازو [ 4، 5-c ] كينولين-2-أون ديوترومية واستخدامها في علاج السرطان
JP7569688B2 (ja) 2017-12-22 2024-10-18 ハイバーセル,インコーポレイテッド ホスファチジルイノシトールリン酸キナーゼ阻害剤としてのアミノピリジン誘導体
TW202112767A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物
CA3154475A1 (en) * 2019-09-23 2021-04-01 Nanjing Zhengxiang Pharmaceuticals Co., Ltd. Phosphodiesterase inhibitors and use
WO2022060377A1 (en) * 2020-09-21 2022-03-24 Wei Zhong Substituted 1-(3,3-difluoropiperidin-4-yl)-imidazo[4,5-c] quinolin-2-one compounds with blood-brain barrier penetrable capability
US20230380203A1 (en) * 2021-01-26 2023-11-23 Boe Technology Group Co., Ltd. Quantum dot light-emitting device, display apparatus and manufacturing method
CN116768928A (zh) * 2023-06-15 2023-09-19 上海毕臣生化科技有限公司 一种3-叔丁基-5-硼酸酯基吡啶的合成方法
CN117384154A (zh) * 2023-09-04 2024-01-12 广州医科大学 一种吡咯并喹啉酮化合物、合成方法及其应用

Citations (6)

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WO2003097641A2 (en) * 2002-05-21 2003-11-27 Novartis Ag 1h-imidazo[4,5-c] quinoline derivatives in the treatment of protein kinase dependent diseases
WO2005054238A1 (en) * 2003-11-21 2005-06-16 Novartis Ag 1h-imidazo[4,5-c]quinoline derivatives in the treatment of protein kinase dependent diseases
WO2006122806A2 (en) * 2005-05-20 2006-11-23 Novartis Ag 1,3-dihydro-imidazo [4,5-c] quinolin-2-ones as lipid kinase inhibitors
WO2008103636A1 (en) * 2007-02-20 2008-08-28 Novartis Ag Imidazoquinolines as dual lipid kinase and mtor inhibitors
WO2009013305A1 (en) * 2007-07-24 2009-01-29 Novartis Ag Use of imidazoquinolines for the treatment of egfr dependent diseases or diseases that have acquired resistance to agents that target egfr family members
WO2010038165A1 (en) * 2008-09-30 2010-04-08 Pfizer Inc. Imidazo[1,5]naphthyridine compounds, their pharmaceutical use and compositions

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BRPI0416801A (pt) 2003-11-21 2007-01-09 Novartis Ag derivados de 1h-imidazoquinolina como inibidores de proteìna sinase
AU2005284835A1 (en) 2004-09-14 2006-03-23 Novartis Vaccines And Diagnostics Inc. Imidazoquinoline compounds
CN101309687A (zh) 2005-11-04 2008-11-19 科勒制药集团公司 经羟基和烷氧基取代的1h-咪唑并喹啉及其方法
MX2009005360A (es) 2006-11-20 2009-06-05 Novartis Ag Sales y formas de cristal del 2-metil-2-[4-(3-metil-2-oxo-8-quinol in-3-il-2,3-dihidro-imidazo-[4,5-c]-quinolin-1-il)-fenil]-propion itrilo.
US20090082387A1 (en) * 2007-09-26 2009-03-26 Protia, Llc Deuterium-enriched nvp-bez234
CA2717948C (en) 2008-03-26 2016-09-06 Novartis Ag 5imidazoquinolines and pyrimidine derivatives as potent modulators of vegf-driven angiogenic processes
US20110212053A1 (en) 2008-06-19 2011-09-01 Dapeng Qian Phosphatidylinositol 3 kinase inhibitors

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003097641A2 (en) * 2002-05-21 2003-11-27 Novartis Ag 1h-imidazo[4,5-c] quinoline derivatives in the treatment of protein kinase dependent diseases
WO2005054238A1 (en) * 2003-11-21 2005-06-16 Novartis Ag 1h-imidazo[4,5-c]quinoline derivatives in the treatment of protein kinase dependent diseases
WO2006122806A2 (en) * 2005-05-20 2006-11-23 Novartis Ag 1,3-dihydro-imidazo [4,5-c] quinolin-2-ones as lipid kinase inhibitors
WO2008103636A1 (en) * 2007-02-20 2008-08-28 Novartis Ag Imidazoquinolines as dual lipid kinase and mtor inhibitors
WO2009013305A1 (en) * 2007-07-24 2009-01-29 Novartis Ag Use of imidazoquinolines for the treatment of egfr dependent diseases or diseases that have acquired resistance to agents that target egfr family members
WO2010038165A1 (en) * 2008-09-30 2010-04-08 Pfizer Inc. Imidazo[1,5]naphthyridine compounds, their pharmaceutical use and compositions

Also Published As

Publication number Publication date
US20100317657A1 (en) 2010-12-16
TN2011000626A1 (en) 2013-05-24
CU24064B1 (es) 2014-12-26
UA106074C2 (uk) 2014-07-25
EA201101704A1 (ru) 2012-07-30
NI201100209A (es) 2012-02-02
TW201102386A (en) 2011-01-16
BRPI1010621A2 (pt) 2016-06-21
JP5596137B2 (ja) 2014-09-24
WO2010139731A1 (en) 2010-12-09
EA020715B1 (ru) 2015-01-30
UY32682A (es) 2011-01-31
US8476294B2 (en) 2013-07-02
AR076949A1 (es) 2011-07-20
SG176572A1 (en) 2012-01-30
US20140005163A1 (en) 2014-01-02
IL216452A0 (en) 2012-01-31
JP2012528828A (ja) 2012-11-15
DOP2011000373A (es) 2011-12-31
CO6470887A2 (es) 2012-06-29
ZA201108439B (en) 2012-08-29
TWI464168B (zh) 2014-12-11
CL2011003052A1 (es) 2012-08-31
MA33332B1 (fr) 2012-06-01
GEP20156267B (en) 2015-04-14
CA2763821A1 (en) 2010-12-09
AU2010255727A1 (en) 2011-12-08
CR20110608A (es) 2012-01-16
EP2438064A1 (en) 2012-04-11
KR101445458B1 (ko) 2014-10-07
CU20110221A7 (es) 2012-03-15
PE20120224A1 (es) 2012-04-04
KR20120034710A (ko) 2012-04-12
AU2010255727B2 (en) 2013-02-28
CN102574845A (zh) 2012-07-11
MX2011012943A (es) 2012-01-27
NZ596487A (en) 2012-11-30
ECSP11011500A (es) 2012-01-31

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