JP2008540390A - キナーゼ酵素活性阻害剤としてのキノリン及びキノキサリン誘導体 - Google Patents

キナーゼ酵素活性阻害剤としてのキノリン及びキノキサリン誘導体 Download PDF

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Publication number
JP2008540390A
JP2008540390A JP2008509501A JP2008509501A JP2008540390A JP 2008540390 A JP2008540390 A JP 2008540390A JP 2008509501 A JP2008509501 A JP 2008509501A JP 2008509501 A JP2008509501 A JP 2008509501A JP 2008540390 A JP2008540390 A JP 2008540390A
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Japan
Prior art keywords
methoxy
yloxy
quinolin
amino
mmol
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Pending
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JP2008509501A
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Japanese (ja)
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JP2008540390A5 (enExample
Inventor
デビッドソン，アラン，ホーンスビー
デイビス，スティーブン，ジョン
モファット，デビッド，フェストゥス，チャールズ
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Chroma Therapeutics Ltd
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Chroma Therapeutics Ltd
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Publication of JP2008540390A publication Critical patent/JP2008540390A/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/38—Nitrogen atoms
    • C07D215/42—Nitrogen atoms attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/233—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/36—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/38—Nitrogen atoms
    • C07D215/42—Nitrogen atoms attached in position 4
    • C07D215/44—Nitrogen atoms attached in position 4 with aryl radicals attached to said nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/90—Oxygen atoms with acyclic radicals attached in position 2 or 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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 two hetero rings
    • C07D401/12—Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Materials For Medical Uses (AREA)
JP2008509501A 2005-05-05 2006-05-04 キナーゼ酵素活性阻害剤としてのキノリン及びキノキサリン誘導体 Pending JP2008540390A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0509227.5A GB0509227D0 (en) 2005-05-05 2005-05-05 Intracellular enzyme inhibitors
PCT/GB2006/001609 WO2006117552A1 (en) 2005-05-05 2006-05-04 Quinoline and quinoxaline derivatives as inhibitors of kinase enzymatic activity

Publications (2)

Publication Number Publication Date
JP2008540390A true JP2008540390A (ja) 2008-11-20
JP2008540390A5 JP2008540390A5 (enExample) 2009-06-18

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ID=34685159

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JP2008509501A Pending JP2008540390A (ja) 2005-05-05 2006-05-04 キナーゼ酵素活性阻害剤としてのキノリン及びキノキサリン誘導体

Country Status (15)

Country Link
US (1) US8148531B2 (enExample)
EP (1) EP1877383B1 (enExample)
JP (1) JP2008540390A (enExample)
KR (1) KR20080010400A (enExample)
CN (1) CN101166726A (enExample)
AT (1) ATE523492T1 (enExample)
AU (1) AU2006243068B2 (enExample)
BR (1) BRPI0609857A2 (enExample)
CA (1) CA2606338A1 (enExample)
GB (1) GB0509227D0 (enExample)
IL (1) IL186551A0 (enExample)
MX (1) MX2007013276A (enExample)
NZ (1) NZ562520A (enExample)
WO (1) WO2006117552A1 (enExample)
ZA (1) ZA200709304B (enExample)

Cited By (6)

* Cited by examiner, † Cited by third party
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JP2008542196A (ja) * 2005-05-05 2008-11-27 クロマ セラピューティクス リミテッド カルボキシルエステラーゼにより加水分解可能なアルファアミノ酸エステル−薬剤複合体
JP2009529002A (ja) * 2006-03-02 2009-08-13 アストラゼネカ アクチボラグ キノリン誘導体
JP2011241170A (ja) * 2010-05-18 2011-12-01 Mercian Corp ビタミンｄ誘導体およびその製造方法
WO2013129443A1 (ja) * 2012-02-29 2013-09-06 大鵬薬品工業株式会社 新規ピペリジン化合物又はその塩
JP2016513108A (ja) * 2013-02-15 2016-05-12 カラ ファーマシューティカルズ インコーポレイテッド 治療用化合物およびその使用
JP2022512358A (ja) * 2018-12-12 2022-02-03 タラピューティクス サイエンス インコーポレイテッド キノリン構造を有するｐａｎ－ＫＩＴキナーゼ阻害剤及びその適用

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MX2007004403A (es) 2004-10-12 2007-04-27 Astrazeneca Ab Derivados de quinazolina.
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
US7572809B2 (en) * 2005-12-19 2009-08-11 Hoffmann-La Roche Inc. Isoquinoline aminopyrazole derivatives
US20110053931A1 (en) * 2006-06-08 2011-03-03 John Gaudino Quinoline compounds and methods of use
GB0619753D0 (en) * 2006-10-06 2006-11-15 Chroma Therapeutics Ltd Enzyme inhibitors
JP2010505962A (ja) 2006-10-09 2010-02-25 武田薬品工業株式会社 キナーゼ阻害剤
CA2668070A1 (en) * 2006-10-30 2008-05-08 Chroma Therapeutics Ltd. Hydroxamates as inhibitors of histone deacetylase
GB0803747D0 (en) 2008-02-29 2008-04-09 Martin Enzyme and receptor modulation
JP5746015B2 (ja) * 2008-04-16 2015-07-08 マックス プランク ゲゼルシャフト ツゥアー フェデルゥン デル ヴィッセンシャフテン エー フォー Ａｘｌキナーゼ阻害剤としてのキノリン誘導体
GB0903480D0 (en) 2009-02-27 2009-04-08 Chroma Therapeutics Ltd Enzyme Inhibitors
EP2311809A1 (en) * 2009-10-16 2011-04-20 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Quinolinyloxyphenylsulfonamides
RU2449988C1 (ru) * 2011-04-29 2012-05-10 Федеральное Государственное Бюджетное Учреждение Науки Институт Физиологически Активных Веществ Российской Академии Наук (Ифав Ран) 2,2,2-трифтор-1-трифторметилэтиловый эфир циклогексилкарбаминовой кислоты в качестве эффективного средства для селективного необратимого ингибирования карбоксилэстеразы
WO2013032951A1 (en) 2011-08-26 2013-03-07 Neupharma, Inc. Certain chemical entities, compositions, and methods
AU2012308238B2 (en) 2011-09-14 2017-05-25 Neupharma, Inc. Certain chemical entities, compositions, and methods
US9249110B2 (en) 2011-09-21 2016-02-02 Neupharma, Inc. Substituted quinoxalines as B-raf kinase inhibitors
WO2013049701A1 (en) 2011-09-30 2013-04-04 Neupharma, Inc. Certain chemical entities, compositions, and methods
EP2806874B1 (en) 2012-01-25 2017-11-15 Neupharma, Inc. Quinoxaline-oxy-phenyl derivatives as kinase inhibitors
CN103304489B (zh) * 2012-03-16 2015-03-11 中国农业科学院兰州畜牧与兽药研究所 嘧啶苯甲酰胺类化合物及其制备和应用
GB201211310D0 (en) 2012-06-26 2012-08-08 Chroma Therapeutics Ltd CSF-1R kinase inhibitors
EP2864291B1 (en) 2012-06-26 2016-10-05 Bayer Pharma Aktiengesellschaft N-[4-(quinolin-4-yloxy)cyclohexyl(methyl)](hetero)arylcarboxamides as androgen receptor antagonists, production and use thereof as medicinal products
CN104812389B (zh) 2012-09-24 2020-07-17 润新生物公司 某些化学实体、组合物及方法
SI3222616T1 (sl) 2012-10-17 2019-10-30 Macrophage Pharma Ltd N-(2-(4-(6-amino-5-(2,4-difluorobenzoil)-2-oksopiridin-1(2H)-IL)-3,5- difluorofenil)etil)-L-alanin in njegov terbutil ester
US9725421B2 (en) 2012-11-12 2017-08-08 Neupharma, Inc. Substituted quinoxalines as B-raf kinase inhibitors
CN103965107B (zh) * 2013-02-06 2016-08-17 沈阳药科大学 2-芳基取代喹啉类化合物及其用途
US9353123B2 (en) 2013-02-20 2016-05-31 Kala Pharmaceuticals, Inc. Therapeutic compounds and uses thereof
US9688688B2 (en) 2013-02-20 2017-06-27 Kala Pharmaceuticals, Inc. Crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one and uses thereof
WO2015002427A1 (ko) * 2013-07-01 2015-01-08 (주) 엘지화학 폴리오르가노실록산 화합물, 제조방법 및 이를 포함하는 코폴리카보네이트 수지
US9890173B2 (en) 2013-11-01 2018-02-13 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
KR20160099084A (ko) 2013-11-01 2016-08-19 칼라 파마슈티컬스, 인크. 치료 화합물의 결정질 형태 및 그의 용도
CN104072492A (zh) * 2013-11-27 2014-10-01 苏州摩尔医药有限公司 一种抗肿瘤靶向治疗药物Tivozanib的合成方法
CN105085433B (zh) * 2014-05-19 2019-06-25 中国科学院上海药物研究所 取代酰胺苯酚类化合物及其制备方法、药物组合物和用途
SG10201900631TA (en) 2014-08-01 2019-02-27 Nuevolution As Compounds active towards bromodomains
US20190112317A1 (en) 2015-10-05 2019-04-18 The Trustees Of Columbia University In The City Of New York Activators of autophagic flux and phospholipase d and clearance of protein aggregates including tau and treatment of proteinopathies
WO2017168448A1 (en) 2016-03-30 2017-10-05 Council Of Scientific & Industrial Research Silicon incorporated quinolines with anti-malarial and anti-toxoplasmosis activity
CN106083715A (zh) * 2016-06-01 2016-11-09 谢阳 一种喹啉、喹唑啉类化合物及其药物组合物和应用
US10253036B2 (en) 2016-09-08 2019-04-09 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
WO2018048750A1 (en) 2016-09-08 2018-03-15 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
EP3509421A4 (en) 2016-09-08 2020-05-20 Kala Pharmaceuticals, Inc. CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF
SG11201903091VA (en) * 2016-10-10 2019-05-30 Dev Ct Biotechnology Quinoxaline compounds as type iii receptor tyrosine kinase inhibitors
GB201713975D0 (en) 2017-08-31 2017-10-18 Macrophage Pharma Ltd Medical use
CN112778217B (zh) * 2019-11-08 2024-01-26 沈阳化工研究院有限公司 一种喹唑啉类化合物及其应用
AU2022293015A1 (en) * 2021-06-17 2023-11-30 Ashishkumar Ravindra MISHRA A process for preparation of an intermediate of l-glufosinate

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