CN1518546A - 作为vegrf-2和vegfr-3抑制剂的选择性邻氨基苯甲酰胺吡啶酰胺 - Google Patents

作为vegrf-2和vegfr-3抑制剂的选择性邻氨基苯甲酰胺吡啶酰胺 Download PDF

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Publication number
CN1518546A
CN1518546A CNA028095804A CN02809580A CN1518546A CN 1518546 A CN1518546 A CN 1518546A CN A028095804 A CNA028095804 A CN A028095804A CN 02809580 A CN02809580 A CN 02809580A CN 1518546 A CN1518546 A CN 1518546A
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alkyl
group
aryl
halogen
optionally
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Pending
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CNA028095804A
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Chinese (zh)
Inventor
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亚力山大·恩斯特
安德烈亚斯·胡特
马丁·克吕格尔
���ġ��ٶ��º�
卡尔－海因茨·蒂尔奥赫
安德烈亚斯·门拉德
马丁·哈贝赖
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Bayer Pharma AG
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Schering AG
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Priority claimed from DE2001123574 external-priority patent/DE10123574A1/de
Priority claimed from DE2001125294 external-priority patent/DE10125294A1/de
Priority claimed from DE2001164590 external-priority patent/DE10164590A1/de
Application filed by Schering AG filed Critical Schering AG
Publication of CN1518546A publication Critical patent/CN1518546A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
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    • A61P17/06—Antipsoriatics
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    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/06—Antibacterial agents for tuberculosis
    • 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
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Vascular Medicine (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
CNA028095804A 2001-05-08 2002-05-03 作为vegrf-2和vegfr-3抑制剂的选择性邻氨基苯甲酰胺吡啶酰胺 Pending CN1518546A (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
DE10123574.7 2001-05-08
DE2001123574 DE10123574A1 (de) 2001-05-08 2001-05-08 Selektive Anthranylamid-Derivate als VEGFR II Inhibitoren
DE2001125294 DE10125294A1 (de) 2001-05-15 2001-05-15 Selektive Anthranylamid-Derivate als VEGFR-2 und VEGFR-3 Inhibitoren
DE10125294.3 2001-05-15
DE2001164590 DE10164590A1 (de) 2001-12-21 2001-12-21 Anthranylamidpyridinamide als VEGFR-2 und VEGFR-3 Inhibitoren
DE10164590.2 2001-12-21

Publications (1)

Publication Number Publication Date
CN1518546A true CN1518546A (zh) 2004-08-04

Family

ID=27214428

Family Applications (1)

Application Number Title Priority Date Filing Date
CNA028095804A Pending CN1518546A (zh) 2001-05-08 2002-05-03 作为vegrf-2和vegfr-3抑制剂的选择性邻氨基苯甲酰胺吡啶酰胺

Country Status (14)

Country Link
US (1) US20040254185A1 (https=)
EP (1) EP1392680B1 (https=)
JP (1) JP2004528379A (https=)
KR (1) KR20030094395A (https=)
CN (1) CN1518546A (https=)
BR (1) BR0209485A (https=)
CA (1) CA2453223A1 (https=)
DE (1) DE50213703D1 (https=)
IL (1) IL158783A0 (https=)
MX (1) MXPA03010099A (https=)
NO (1) NO20034957D0 (https=)
PE (1) PE20021092A1 (https=)
PL (1) PL364478A1 (https=)
WO (1) WO2002090352A2 (https=)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104163794A (zh) * 2013-10-17 2014-11-26 中国药科大学 2-氨基芳环类血管内皮生长因子受体(vegfr)抑制剂及其制备方法和用途
CN106496107A (zh) * 2016-08-31 2017-03-15 浙江永宁药业股份有限公司 Vegfr‑2抑制剂及其制备方法
CN108467360A (zh) * 2018-06-22 2018-08-31 江苏美迪克化学品有限公司 一种阿帕替尼的制备方法及其中间体
CN113228201A (zh) * 2018-08-13 2021-08-06 健康科学西部大学 治疗青光眼的钙蛋白酶-2选择性抑制剂化合物
WO2025113390A1 (zh) * 2023-11-27 2025-06-05 南开大学 一种苯并吡喃结构的查尔酮类衍生物及其制备方法和应用

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US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
US6878714B2 (en) * 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US20030134836A1 (en) * 2001-01-12 2003-07-17 Amgen Inc. Substituted arylamine derivatives and methods of use
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
US7307088B2 (en) 2002-07-09 2007-12-11 Amgen Inc. Substituted anthranilic amide derivatives and methods of use
CA2493026C (en) * 2002-07-31 2011-05-24 Bayer Schering Pharma Aktiengesellschaft Vegfr-2 and vegfr-3 inhibitory anthranilamide pyridines
US7615565B2 (en) * 2002-07-31 2009-11-10 Bayer Schering Pharma Aktiengesellschaft VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridines
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JP2006526660A (ja) * 2003-06-05 2006-11-24 バーテックス　ファーマシューティカルズ　インコーポレイテッド Ｖｒ１レセプターのモジュレーター
DE10327719A1 (de) * 2003-06-13 2005-01-20 Schering Ag VEGFR-2 und VEGFR-3 Inhibitorische Anthranylamidpyridone
US7202260B2 (en) * 2003-06-13 2007-04-10 Schering Ag VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridones
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UA89035C2 (ru) 2003-12-03 2009-12-25 Лео Фарма А/С Эфиры гидроксамовых кислот и их фармацевтическое применение
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CN1660811A (zh) * 2004-02-27 2005-08-31 中国科学院上海药物研究所 1，4－二取代苯类化合物及其制备方法和用途
US7550499B2 (en) 2004-05-12 2009-06-23 Bristol-Myers Squibb Company Urea antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
EP1655295A1 (en) 2004-11-03 2006-05-10 Schering Aktiengesellschaft Anthranilamide pyridinureas as VEGF receptor kinase inhibitors
EP1655297A1 (en) * 2004-11-03 2006-05-10 Schering Aktiengesellschaft Nicotinamide pyridinureas as vascular endothelial growth factor (VEGF) receptor kinase inhibitors
EP1657241A1 (en) 2004-11-03 2006-05-17 Schering Aktiengesellschaft Novel anthranilamide pyridinureas as VEGF receptor kinase inhibitors
US7906533B2 (en) 2004-11-03 2011-03-15 Bayer Schering Pharma Ag Nicotinamide pyridinureas as vascular endothelial growth factor (VEGF) receptor kinase inhibitors
KR20060071812A (ko) * 2004-12-22 2006-06-27 주식회사 엘지생명과학 신규한 3-(2-아미노-6-피리디닐)-4-히드록시페닐 아민유도체
WO2006070878A1 (ja) * 2004-12-28 2006-07-06 Astellas Pharma Inc. カルボン酸誘導体またはその塩
EP1954696B1 (en) 2005-01-19 2011-02-23 Bristol-Myers Squibb Company 2-phenoxy-n-(1,3,4-thiadizol-2-yl)pyridin-3-amine derivatives and related compounds as p2y1 receptor inhibitors for the treatment of thromboembolic disorders
JP4585978B2 (ja) * 2005-03-03 2010-11-24 参天製薬株式会社 キノリルアルキルチオ基を有する新規環式化合物
WO2007002634A1 (en) * 2005-06-27 2007-01-04 Bristol-Myers Squibb Company Carbocycle and heterocycle antagonists of p2y1 receptor useful in the treatment of thrombotic conditions
EP1899299B1 (en) 2005-06-27 2010-10-20 Bristol-Myers Squibb Company C-linked cyclic antagonists of p2y1 receptor useful in the treatment of thrombotic conditions
AR056867A1 (es) 2005-06-27 2007-10-31 Bristol Myers Squibb Co Antagonistas heterociclicos n- enlazados del receptor de p2y1 utiles en el tratamiento de condiciones tromboticas. composiciones farmaceuticas.
DE602006020871D1 (de) 2005-06-27 2011-05-05 Bristol Myers Squibb Co Lineare harnstoffmimetika-antagonisten des p2y1-rezeptors zur behandlung von thromboseleiden
US8247556B2 (en) 2005-10-21 2012-08-21 Amgen Inc. Method for preparing 6-substituted-7-aza-indoles
BRPI0619208A2 (pt) * 2005-11-30 2011-09-20 Astellas Pharma Inc derivado de 2-aminobenzamida c07d 307/14 c07d 307/22 c07d 309/14 c07d 319/12 c07d 401/12 c07d 405/12 c07d 413/12 c07d 417/12
US7960569B2 (en) 2006-10-17 2011-06-14 Bristol-Myers Squibb Company Indole antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
AR065015A1 (es) * 2007-01-26 2009-05-13 Smithkline Beecham Corp Derivados de antranilamida, composiciones farmaceuticas que los contienen, y usos para el tratamiento del cancer
FR2917413B1 (fr) 2007-06-13 2009-08-21 Sanofi Aventis Sa Derives de 7-alkynyl-1,8-naphthyridones, leur preparation et leur application en therapeutique
EP2346827B1 (en) * 2008-08-27 2013-11-13 Leo Pharma A/S Pyridine derivatives as vegfr-2 receptor and protein tyrosine kinase inhibitors
US9340555B2 (en) 2009-09-03 2016-05-17 Allergan, Inc. Compounds as tyrosine kinase modulators
IN2012DN02493A (https=) 2009-09-03 2015-08-28 Allergan Inc
KR101524923B1 (ko) * 2013-08-02 2015-06-01 가톨릭대학교 산학협력단 ＩＦＮ－γ의 발현을 증가시키는 ＶＥＧＦＲ－３ 억제제를 유효성분으로 포함하는 급성골수성백혈병 치료용 약학적 조성물
KR102371269B1 (ko) * 2020-03-11 2022-03-07 연세대학교 산학협력단 VEGFR-3 발현 조절을 통한 mTOR 관련 질환의 예방 또는 치료 방법

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UA71587C2 (uk) * 1998-11-10 2004-12-15 Шерінг Акцієнгезелльшафт Аміди антранілової кислоти та їхнє застосування як лікарських засобів
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DE10023492A1 (de) * 2000-05-09 2001-11-22 Schering Ag Aza- und Polyazanthranylamide und deren Verwendung als Arzneimittel
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US7615565B2 (en) * 2002-07-31 2009-11-10 Bayer Schering Pharma Aktiengesellschaft VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridines

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104163794A (zh) * 2013-10-17 2014-11-26 中国药科大学 2-氨基芳环类血管内皮生长因子受体(vegfr)抑制剂及其制备方法和用途
CN106496107A (zh) * 2016-08-31 2017-03-15 浙江永宁药业股份有限公司 Vegfr‑2抑制剂及其制备方法
CN108467360A (zh) * 2018-06-22 2018-08-31 江苏美迪克化学品有限公司 一种阿帕替尼的制备方法及其中间体
CN108467360B (zh) * 2018-06-22 2021-04-30 江苏美迪克化学品有限公司 一种阿帕替尼的制备方法及其中间体
CN113228201A (zh) * 2018-08-13 2021-08-06 健康科学西部大学 治疗青光眼的钙蛋白酶-2选择性抑制剂化合物
WO2025113390A1 (zh) * 2023-11-27 2025-06-05 南开大学 一种苯并吡喃结构的查尔酮类衍生物及其制备方法和应用

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