JP2016517871A - 新規モルホリニルアントラサイクリン誘導体 - Google Patents

新規モルホリニルアントラサイクリン誘導体 Download PDF

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Publication number
JP2016517871A
JP2016517871A JP2016511009A JP2016511009A JP2016517871A JP 2016517871 A JP2016517871 A JP 2016517871A JP 2016511009 A JP2016511009 A JP 2016511009A JP 2016511009 A JP2016511009 A JP 2016511009A JP 2016517871 A JP2016517871 A JP 2016517871A
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Prior art keywords
formula
compound
cancer
alkyl
defined above
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JP2016511009A
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Japanese (ja)
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JP2016517871A5 (enExample
Inventor
ベリア，イタロ
カルーソ，ミケーレ
ルーピ，ビットーリア
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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
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Publication of JP2016517871A publication Critical patent/JP2016517871A/ja
Publication of JP2016517871A5 publication Critical patent/JP2016517871A5/ja
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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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Communicable Diseases (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Transplantation (AREA)
  • Hematology (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)
JP2016511009A 2013-04-29 2014-04-23 新規モルホリニルアントラサイクリン誘導体 Pending JP2016517871A (ja)

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
JP2016517871A true JP2016517871A (ja) 2016-06-20
JP2016517871A5 JP2016517871A5 (enExample) 2017-06-08

Family

ID=48190306

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016511009A Pending JP2016517871A (ja) 2013-04-29 2014-04-23 新規モルホリニルアントラサイクリン誘導体

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 (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5262269A (en) * 1975-11-18 1977-05-23 Farmaceutici Italia Production of novel anthracignolin and malign amoebocyte growth inhibiting agent containing same
JPS63313796A (ja) * 1987-04-21 1988-12-21 フアルマシア・エ・アツプジヨン・エツセ・ピー・アー ４−デメントキシ−４−アミノ−アントラサイクリン類
JPH03504609A (ja) * 1989-03-13 1991-10-09 フアルミタリア・カルロ・エルバ・エツセ・エルレ・エルレ 新規な３′‐（４‐モルホリニル）‐及び３′‐（２‐メトキシ‐４‐モルホリニル）‐アントラサイクリン誘導体
JPH04503210A (ja) * 1989-02-07 1992-06-11 フアルミタリア・カルロ・エルバ・エツセ・エルレ・エルレ 新規４′‐エピ‐４′‐アミノアンスラサイクリン
JPH04247096A (ja) * 1990-09-12 1992-09-03 Farmitalia Carlo Erba Spa １３−ジヒドロ−３′−（２−アルコキシ−４−モルホリニル）アンスラサイクリン
JPH11513040A (ja) * 1996-07-11 1999-11-09 フアルマシア・エ・アツプジヨン・エツセ・ピー・アー モルホリニルアントラサイクリン誘導体
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 (9)

* 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
US4133877A (en) 1976-07-08 1979-01-09 Societa Farmaceutici Italia S.P.A. Anthracycline ethers and use therefor
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
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
GB2296495B (en) * 1994-12-23 1998-04-15 Erba Carlo Spa Anthracycline derivatives
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
MX2011000509A (es) * 2008-07-15 2011-04-05 Genentech Inc Conjugados derivados de antraciclina, proceso para su preparacion y su uso como compuestos antitumorales.

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5262269A (en) * 1975-11-18 1977-05-23 Farmaceutici Italia Production of novel anthracignolin and malign amoebocyte growth inhibiting agent containing same
JPS63313796A (ja) * 1987-04-21 1988-12-21 フアルマシア・エ・アツプジヨン・エツセ・ピー・アー ４−デメントキシ−４−アミノ−アントラサイクリン類
JPH04503210A (ja) * 1989-02-07 1992-06-11 フアルミタリア・カルロ・エルバ・エツセ・エルレ・エルレ 新規４′‐エピ‐４′‐アミノアンスラサイクリン
JPH03504609A (ja) * 1989-03-13 1991-10-09 フアルミタリア・カルロ・エルバ・エツセ・エルレ・エルレ 新規な３′‐（４‐モルホリニル）‐及び３′‐（２‐メトキシ‐４‐モルホリニル）‐アントラサイクリン誘導体
JPH04247096A (ja) * 1990-09-12 1992-09-03 Farmitalia Carlo Erba Spa １３−ジヒドロ−３′−（２−アルコキシ−４−モルホリニル）アンスラサイクリン
JPH11513040A (ja) * 1996-07-11 1999-11-09 フアルマシア・エ・アツプジヨン・エツセ・ピー・アー モルホリニルアントラサイクリン誘導体
WO2012073217A1 (en) * 2010-12-02 2012-06-07 Nerviano Medical Sciences S.R.L. Process for the preparation of morpholinyl anthracycline derivatives

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
CN105164138A (zh) 2015-12-16
EP2991993A1 (en) 2016-03-09
CN105164138B (zh) 2017-11-07

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