CN105164138B - 新吗啉基蒽环类抗生素衍生物 - Google Patents

新吗啉基蒽环类抗生素衍生物 Download PDF

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Publication number
CN105164138B
CN105164138B CN201480023999.XA CN201480023999A CN105164138B CN 105164138 B CN105164138 B CN 105164138B CN 201480023999 A CN201480023999 A CN 201480023999A CN 105164138 B CN105164138 B CN 105164138B
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formula
compound
cancer
defined above
amino
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Chinese (zh)
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CN105164138A (zh
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I·贝里亚
M·卡鲁索
V·卢皮
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Nerviano Medical Sciences SRL
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Nerviano Medical Sciences SRL
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H9/00—Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic 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 three hetero rings
    • C07D498/14—Ortho-condensed systems
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Virology (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201480023999.XA 2013-04-29 2014-04-23 新吗啉基蒽环类抗生素衍生物 Expired - Fee Related CN105164138B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13165707.4 2013-04-29
EP13165707 2013-04-29
PCT/EP2014/058262 WO2014177441A1 (en) 2013-04-29 2014-04-23 New morpholinyl anthracycline derivatives

Publications (2)

Publication Number Publication Date
CN105164138A CN105164138A (zh) 2015-12-16
CN105164138B true CN105164138B (zh) 2017-11-07

Family

ID=48190306

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201480023999.XA Expired - Fee Related CN105164138B (zh) 2013-04-29 2014-04-23 新吗啉基蒽环类抗生素衍生物

Country Status (8)

Country Link
US (1) US9828405B2 (enExample)
EP (1) EP2991993B1 (enExample)
JP (1) JP2016517871A (enExample)
CN (1) CN105164138B (enExample)
DK (1) DK2991993T3 (enExample)
ES (1) ES2695162T3 (enExample)
RU (1) RU2666356C2 (enExample)
WO (1) WO2014177441A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6785780B2 (ja) * 2014-11-05 2020-11-18 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ 官能基化モルホリニルアントラサイクリン誘導体
CN108864221B (zh) * 2018-06-08 2022-04-01 中国科学院上海有机化学研究所 阿克拉霉素类似物及其制法和用途
CN110776501B (zh) * 2019-08-22 2021-04-02 联宁（苏州）生物制药有限公司 一种用于抗体药物偶联物的药物毒素pnu-159682的制备方法及其中间体
CN115043895A (zh) * 2022-07-15 2022-09-13 戊言医药科技（上海）有限公司 一种pnu-159682及其中间体的制备方法
CN115651043A (zh) * 2022-10-27 2023-01-31 戊言医药科技（上海）有限公司 一种蒽环类毒素衍生物的制备方法

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1990010639A2 (en) * 1989-03-13 1990-09-20 Farmitalia Carlo Erba S.R.L. New 3'-(4-morpholinyl)- and 3'-(2-methoxy-4-morpholinyl)- anthracycline derivatives
GB2247885A (en) * 1990-09-12 1992-03-18 Erba Carlo Spa 13-dihydro-3'-(2-alkoxy-4-morpholinyl)anthracyclines
GB2296495A (en) * 1994-12-23 1996-07-03 Erba Carlo Spa Morpholine and piperidine N-oxide based anthracycline derivatives as antitumour agents
WO1998002446A1 (en) * 1996-07-11 1998-01-22 Pharmacia & Upjohn S.P.A. Morpholinyl anthracycline derivatives
CN102159248A (zh) * 2008-07-15 2011-08-17 健泰科生物技术公司 蒽环类衍生物缀合物、它们的制备方法以及它们作为抗肿瘤化合物的用途
WO2012073217A1 (en) * 2010-12-02 2012-06-07 Nerviano Medical Sciences S.R.L. Process for the preparation of morpholinyl anthracycline derivatives

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3803124A (en) 1968-04-12 1974-04-09 Farmaceutici It Soc Process for the preparation of adriamycin and adriamycinone and adriamycin derivatives
GB1511680A (en) * 1975-11-18 1978-05-24 Farmaceutici Italia Daunosaminyl anthracyclinones
US4133877A (en) 1976-07-08 1979-01-09 Societa Farmaceutici Italia S.P.A. Anthracycline ethers and use therefor
NZ224252A (en) 1987-04-21 1991-09-25 Erba Carlo Spa An anthracycline glycoside and its preparation
GB8804429D0 (en) 1988-02-25 1988-03-23 Erba Carlo Spa New 4-demethyl-4-0-(fluorobenzensulfonyl)anthracycline glycosides
GB2225781A (en) 1988-05-13 1990-06-13 Erba Carlo Spa 10-Noranthracyclines
GB8902709D0 (en) 1989-02-07 1989-03-30 Erba Carlo Spa New 4'-epi-4'-amino anthracyclines
RU2081878C1 (ru) * 1989-03-13 1997-06-20 Фармиталиа Карло Эрба С.Р.Л. Антрациклин гликозид и способ его получения
EP0434960B1 (en) 1989-12-19 1996-09-18 PHARMACIA S.p.A. Chiral 1,5-diiodo-2-methoxy or benzyloxy intermediates
FR2856687B1 (fr) * 2003-06-25 2005-09-16 Servier Lab Nouveaux derives de benzo[a]pyrano[3,2-h]acridin-7-one, leur procede de preparation et les compositions pharmaceutiques qui les contiennent

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1990010639A2 (en) * 1989-03-13 1990-09-20 Farmitalia Carlo Erba S.R.L. New 3'-(4-morpholinyl)- and 3'-(2-methoxy-4-morpholinyl)- anthracycline derivatives
GB2247885A (en) * 1990-09-12 1992-03-18 Erba Carlo Spa 13-dihydro-3'-(2-alkoxy-4-morpholinyl)anthracyclines
GB2296495A (en) * 1994-12-23 1996-07-03 Erba Carlo Spa Morpholine and piperidine N-oxide based anthracycline derivatives as antitumour agents
WO1998002446A1 (en) * 1996-07-11 1998-01-22 Pharmacia & Upjohn S.P.A. Morpholinyl anthracycline derivatives
CN102159248A (zh) * 2008-07-15 2011-08-17 健泰科生物技术公司 蒽环类衍生物缀合物、它们的制备方法以及它们作为抗肿瘤化合物的用途
WO2012073217A1 (en) * 2010-12-02 2012-06-07 Nerviano Medical Sciences S.R.L. Process for the preparation of morpholinyl anthracycline derivatives

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
"Formation and Antitumor Activity of PNU-159682, A Major Metabolite of Nemorubicin in Human Liver Microsomes";Luigi Quintieri et al.;《Clinical Cancer Research》;20050215;第11卷;第1608–1617页 *
"Metabolism of methoxymorpholinodoxorubicin in rat, dog and monkey liver microsomes: comparison with human microsomes";Dominique Beulz-Riche et al.;《Fundamental & Clinical Pharmacology》;20011231;第15卷;第373–378页 *

Also Published As

Publication number Publication date
US20160075730A1 (en) 2016-03-17
HK1218646A1 (zh) 2017-03-03
WO2014177441A1 (en) 2014-11-06
RU2666356C2 (ru) 2018-09-07
US9828405B2 (en) 2017-11-28
ES2695162T3 (es) 2019-01-02
RU2015150994A (ru) 2017-06-06
EP2991993B1 (en) 2018-06-06
DK2991993T3 (en) 2018-07-30
JP2016517871A (ja) 2016-06-20
CN105164138A (zh) 2015-12-16
EP2991993A1 (en) 2016-03-09

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