TWI547494B - 作為激酶抑制劑之胺基喹唑啉類 - Google Patents

作為激酶抑制劑之胺基喹唑啉類 Download PDF

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TWI547494B
TWI547494B TW101129650A TW101129650A TWI547494B TW I547494 B TWI547494 B TW I547494B TW 101129650 A TW101129650 A TW 101129650A TW 101129650 A TW101129650 A TW 101129650A TW I547494 B TWI547494 B TW I547494B
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Taiwan
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alkyl
group
benzo
alkoxy
thiazol
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TW101129650A
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Chinese (zh)
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TW201321377A (zh
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麥可 拜瑞
琳達 卡西利亞斯
亞當 查恩利
麥可 迪馬蒂諾
曉陽 董
帕特里克 埃德姆
帕梅拉 海爾
羅伯特 馬奎斯
喬希 雷曼錄
約瑟夫 羅馬諾
艾美 沙哈
羅伯特 辛翰
王忠仁
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葛蘭素史克智慧財產發展有限公司
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • 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
    • 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
    • C07D417/14—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 three or more hetero rings
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Transplantation (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Emergency Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
TW101129650A 2011-08-18 2012-08-16 作為激酶抑制劑之胺基喹唑啉類 TWI547494B (zh)

Applications Claiming Priority (1)

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US201161524925P 2011-08-18 2011-08-18

Publications (2)

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TW201321377A TW201321377A (zh) 2013-06-01
TWI547494B true TWI547494B (zh) 2016-09-01

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US (4) US9604938B2 (cg-RX-API-DMAC7.html)
EP (1) EP2744501B1 (cg-RX-API-DMAC7.html)
JP (1) JP6090801B2 (cg-RX-API-DMAC7.html)
KR (1) KR20140054246A (cg-RX-API-DMAC7.html)
CN (1) CN103874495B (cg-RX-API-DMAC7.html)
AU (1) AU2012296411B2 (cg-RX-API-DMAC7.html)
BR (1) BR112014003693A2 (cg-RX-API-DMAC7.html)
CA (1) CA2845630C (cg-RX-API-DMAC7.html)
CL (1) CL2014000398A1 (cg-RX-API-DMAC7.html)
CO (1) CO6880068A2 (cg-RX-API-DMAC7.html)
CR (1) CR20140079A (cg-RX-API-DMAC7.html)
DO (1) DOP2014000033A (cg-RX-API-DMAC7.html)
EA (1) EA025436B1 (cg-RX-API-DMAC7.html)
ES (1) ES2615749T3 (cg-RX-API-DMAC7.html)
IL (1) IL230902A0 (cg-RX-API-DMAC7.html)
MA (1) MA35434B1 (cg-RX-API-DMAC7.html)
MX (1) MX2014001879A (cg-RX-API-DMAC7.html)
PE (1) PE20141408A1 (cg-RX-API-DMAC7.html)
PH (1) PH12014500373A1 (cg-RX-API-DMAC7.html)
SG (1) SG2014009526A (cg-RX-API-DMAC7.html)
TW (1) TWI547494B (cg-RX-API-DMAC7.html)
WO (1) WO2013025958A1 (cg-RX-API-DMAC7.html)

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WO2012122011A2 (en) 2011-03-04 2012-09-13 Glaxosmithkline Llc Amino-quinolines as kinase inhibitors
TWI547494B (zh) 2011-08-18 2016-09-01 葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之胺基喹唑啉類
TW201425307A (zh) 2012-09-13 2014-07-01 Glaxosmithkline Llc 作為激酶抑制劑之胺基－喹啉類
TWI592417B (zh) 2012-09-13 2017-07-21 葛蘭素史克智慧財產發展有限公司 胺基喹唑啉激酶抑制劑之前藥
BR112015019624A2 (pt) 2013-02-21 2017-07-18 Glaxosmithkline Ip Dev Ltd quinazolinas como inibidores de quinase
HK1218263A1 (zh) * 2013-03-15 2017-02-10 昂科迪塞恩股份有限公司 大环rip2激酶抑制剂
CA2958782C (en) * 2014-09-17 2024-01-09 Oncodesign S.A. Macrocyclic rip2 kinase inhibitors
GB201506872D0 (en) 2015-04-22 2015-06-03 Ge Oil & Gas Uk Ltd Novel compounds
UY36680A (es) 2015-05-19 2016-12-30 Glaxosmithkline Ip Dev Ltd Amidas heterocíclicas como inhibidores de quinasa
GB201516243D0 (en) 2015-09-14 2015-10-28 Glaxosmithkline Ip Dev Ltd Novel compounds
JP2019514878A (ja) * 2016-04-20 2019-06-06 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ Ｒｉｐｋ２阻害剤を含むコンジュゲート
WO2018130443A1 (de) 2017-01-10 2018-07-19 Bayer Aktiengesellschaft Heterocyclen-derivate als schädlingsbekämpfungsmittel
KR102515694B1 (ko) 2017-01-10 2023-03-29 바이엘 악티엔게젤샤프트 해충 방제제로서의 헤테로사이클 유도체
WO2020043122A1 (zh) * 2018-08-28 2020-03-05 南京明德新药研发有限公司 作为rip2激酶抑制剂的喹唑啉类衍生物
WO2020094613A1 (en) 2018-11-06 2020-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Nod2 inhibitors for the treatment of hereditary periodic fevers
JP7124266B2 (ja) 2020-05-28 2022-08-24 幸水 深谷 柑橘類果実製造方法および柑橘類果実
CN116033828B (zh) 2020-07-02 2025-05-16 拜耳公司 作为害虫防治剂的杂环衍生物
CN114014890A (zh) * 2021-03-12 2022-02-08 爱科诺生物医药(香港)有限公司 具有rip2激酶抑制活性的化合物，包含其的药物组合物，及其应用
WO2024059169A1 (en) * 2022-09-14 2024-03-21 Blueprint Medicines Corporation Egfr inhibitors
GB2631397A (en) * 2023-06-28 2025-01-08 Sevenless Therapeutics Ltd New treatments for pain
WO2025078493A1 (en) 2023-10-11 2025-04-17 Institut National de la Santé et de la Recherche Médicale Local administration of ripk2 inhibitors for the curative treatment of allergic asthma
WO2025092821A1 (zh) * 2023-11-01 2025-05-08 成都赜灵生物医药科技有限公司 喹唑啉衍生物类ripk2抑制剂及其用途

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