CN104918933A - N-(5-(喹啉-6-基)吡啶-3-基)苯磺酰胺衍生物、制备方法及治疗用途 - Google Patents

N-(5-(喹啉-6-基)吡啶-3-基)苯磺酰胺衍生物、制备方法及治疗用途 Download PDF

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Publication number
CN104918933A
CN104918933A CN201380068855.1A CN201380068855A CN104918933A CN 104918933 A CN104918933 A CN 104918933A CN 201380068855 A CN201380068855 A CN 201380068855A CN 104918933 A CN104918933 A CN 104918933A
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China
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bases
quinoline
methyl
phenyl
methoxypyridine
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CN201380068855.1A
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English (en)
Inventor
朱驹
宋云龙
韩进松
陈颖
吕加国
周有骏
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Second Military Medical University SMMU
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Second Military Medical University SMMU
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Priority to CN201380068855.1A priority Critical patent/CN104918933A/zh
Publication of CN104918933A publication Critical patent/CN104918933A/zh
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    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • A61K31/4709—Non-condensed quinolines and containing further 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2009—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Inorganic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Dermatology (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

本发明涉及医药技术领域，具体涉及一类如式(1)所示的各种不同类型取代的N-(5-(喹啉-6-基)吡啶-3-基)苯磺酰胺衍生物（各基团具体定义见说明书）。本发明的化合物对人肺癌、结肠癌、肝癌、乳腺癌、脑星形胶质母细胞瘤等多种肿瘤均表现出良好的抗肿瘤活性，这为开发为高效、低毒、特异性强的抗肿瘤药物奠定了基础，具有很好的开发价值。本发明还涉及该类化合物的组合物、制备方法及其在制备抗肿瘤药物中的用途。

Description

PCT国内申请，说明书已公开。

Claims (1)

  1. PCT国内申请，权利要求书已公开。
CN201380068855.1A 2012-11-01 2013-10-31 N-(5-(喹啉-6-基)吡啶-3-基)苯磺酰胺衍生物、制备方法及治疗用途 Pending CN104918933A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201380068855.1A CN104918933A (zh) 2012-11-01 2013-10-31 N-(5-(喹啉-6-基)吡啶-3-基)苯磺酰胺衍生物、制备方法及治疗用途

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CN2012104305809 2012-11-01
CN201210430580.9A CN103788071A (zh) 2012-11-01 2012-11-01 N-(5-(喹啉-6-基)吡啶-3-基)苯磺酰胺衍生物、制备方法及治疗用途
CN201380068855.1A CN104918933A (zh) 2012-11-01 2013-10-31 N-(5-(喹啉-6-基)吡啶-3-基)苯磺酰胺衍生物、制备方法及治疗用途
PCT/CN2013/086349 WO2014067473A1 (zh) 2012-11-01 2013-10-31 N-(5-(喹啉-6-基)吡啶-3-基)苯磺酰胺衍生物、制备方法及治疗用途

Publications (1)

Publication Number Publication Date
CN104918933A true CN104918933A (zh) 2015-09-16

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CN201210430580.9A Pending CN103788071A (zh) 2012-11-01 2012-11-01 N-(5-(喹啉-6-基)吡啶-3-基)苯磺酰胺衍生物、制备方法及治疗用途
CN201380068855.1A Pending CN104918933A (zh) 2012-11-01 2013-10-31 N-(5-(喹啉-6-基)吡啶-3-基)苯磺酰胺衍生物、制备方法及治疗用途

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Country Status (4)

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US (1) US20160168118A1 (zh)
EP (1) EP2915810A4 (zh)
CN (2) CN103788071A (zh)
WO (1) WO2014067473A1 (zh)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105130954B (zh) * 2015-06-18 2017-10-31 浙江大学 3,4‑二取代‑6‑吡啶基喹啉类化合物及制备和应用
CA3008689A1 (en) * 2015-12-16 2017-06-22 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Pyrido[1,2-a]pyrimidone analog, crystal form thereof, intermediate thereof and preparation method therefor
CN105859684B (zh) * 2016-04-15 2017-03-22 四川赛诺唯新生物技术有限公司 一种稠环化合物、其制备方法和应用及其中间体化合物
AU2019360944B2 (en) * 2018-10-17 2022-09-29 Purdue Research Foundation Fibroblast activation protein (FAP) targeted imaging and therapy in fibrosis
WO2020191240A1 (en) * 2019-03-19 2020-09-24 Chemocentryx, Inc. Combination therapy using a chemokine receptor 2 (ccr2) antagonist and a pd-1 and/or pd-l1 inhibitor
WO2021055641A1 (en) * 2019-09-17 2021-03-25 Purdue Research Foundation Fibroblast activation protein (fap)-targeted imaging and therapy of cancers and other fibrotic and inflammatory diseases
CN110642854A (zh) * 2019-11-20 2020-01-03 成都克莱蒙医药科技有限公司 一种稠环化合物的多晶型、其组合物、制备方法及其应用
WO2021207682A2 (en) * 2020-04-09 2021-10-14 Philip Stewart Low Pi3 kinase inhibitors and uses thereof

Citations (3)

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WO2009155121A2 (en) * 2008-05-30 2009-12-23 Amgen Inc. Inhibitors of pi3 kinase
CN101754759A (zh) * 2007-05-18 2010-06-23 史密丝克莱恩比彻姆公司 用作pi3激酶抑制剂的喹啉衍生物
WO2011082285A1 (en) * 2009-12-30 2011-07-07 Avila Therapeutics, Inc. Ligand-directed covalent modification of protein

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2710018T (pt) * 2011-05-19 2022-03-01 Fundacion Del Sector Publico Estatal Centro Nac De Investigaciones Oncologicas Carlos Iii F S P Cnio Compostos macrocíclicos como inibidores de proteína quinases

Patent Citations (3)

* Cited by examiner, † Cited by third party
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CN101754759A (zh) * 2007-05-18 2010-06-23 史密丝克莱恩比彻姆公司 用作pi3激酶抑制剂的喹啉衍生物
WO2009155121A2 (en) * 2008-05-30 2009-12-23 Amgen Inc. Inhibitors of pi3 kinase
WO2011082285A1 (en) * 2009-12-30 2011-07-07 Avila Therapeutics, Inc. Ligand-directed covalent modification of protein

Also Published As

Publication number Publication date
EP2915810A1 (en) 2015-09-09
EP2915810A4 (en) 2016-04-13
CN103788071A (zh) 2014-05-14
WO2014067473A1 (zh) 2014-05-08
US20160168118A1 (en) 2016-06-16

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