DK2991993T3 - NEW MORPHOLINYLANTHRACYCLINE DERIVATIVES - Google Patents
NEW MORPHOLINYLANTHRACYCLINE DERIVATIVES Download PDFInfo
- Publication number
- DK2991993T3 DK2991993T3 DK14719005.2T DK14719005T DK2991993T3 DK 2991993 T3 DK2991993 T3 DK 2991993T3 DK 14719005 T DK14719005 T DK 14719005T DK 2991993 T3 DK2991993 T3 DK 2991993T3
- Authority
- DK
- Denmark
- Prior art keywords
- formula
- compound
- defined above
- alkyl
- trihydroxy
- Prior art date
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- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 27
- 150000003839 salts Chemical class 0.000 claims description 27
- 239000001257 hydrogen Substances 0.000 claims description 23
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- 125000006239 protecting group Chemical group 0.000 claims description 23
- 238000002360 preparation method Methods 0.000 claims description 11
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 10
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 10
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- 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 claims description 8
- 101100134929 Gallus gallus COR9 gene Proteins 0.000 claims description 8
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 8
- MGNCLNQXLYJVJD-UHFFFAOYSA-N cyanuric chloride Chemical compound ClC1=NC(Cl)=NC(Cl)=N1 MGNCLNQXLYJVJD-UHFFFAOYSA-N 0.000 claims description 6
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- FFHWGQQFANVOHV-UHFFFAOYSA-N dimethyldioxirane Chemical compound CC1(C)OO1 FFHWGQQFANVOHV-UHFFFAOYSA-N 0.000 claims description 5
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- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 6
- 125000000350 glycoloyl group Chemical group O=C([*])C([H])([H])O[H] 0.000 claims 3
- VVQHEYOVOQBKAY-UHFFFAOYSA-N 1,2,3,4-tetrahydrotetracene-5,12-dione Chemical compound O=C1C2=CC3=CC=CC=C3C=C2C(=O)C2=C1CCCC2 VVQHEYOVOQBKAY-UHFFFAOYSA-N 0.000 claims 1
- 206010016935 Follicular thyroid cancer Diseases 0.000 claims 1
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- 229940045799 anthracyclines and related substance Drugs 0.000 abstract description 17
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- 125000002757 morpholinyl group Chemical group 0.000 abstract description 7
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Classifications
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- 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
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- 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
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- 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
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- 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
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- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
Landscapes
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- Organic Chemistry (AREA)
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- Orthopedic Medicine & Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Virology (AREA)
- Transplantation (AREA)
- Communicable Diseases (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13165707 | 2013-04-29 | ||
| PCT/EP2014/058262 WO2014177441A1 (en) | 2013-04-29 | 2014-04-23 | New morpholinyl anthracycline derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK2991993T3 true DK2991993T3 (en) | 2018-07-30 |
Family
ID=48190306
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK14719005.2T DK2991993T3 (en) | 2013-04-29 | 2014-04-23 | NEW MORPHOLINYLANTHRACYCLINE DERIVATIVES |
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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2715902C2 (ru) * | 2014-11-05 | 2020-03-04 | НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. | Функционализированные производные морфолинилантрациклина |
| 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 |
Family Cites Families (16)
| 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 |
| GB8905668D0 (en) * | 1989-03-13 | 1989-04-26 | Erba Carlo Spa | New 3'-(4-morpholinyl)-and 3'-(2-methoxy-4-morpholinyl)-anthracycline derivatives |
| 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 |
| GB9019933D0 (en) * | 1990-09-12 | 1990-10-24 | Erba Carlo Spa | 13-dihydro-3'-(2-alkoxy-4-morphlinyl)anthracyclines |
| GB2296495B (en) | 1994-12-23 | 1998-04-15 | Erba Carlo Spa | Anthracycline derivatives |
| GB2315067B (en) * | 1996-07-11 | 2000-02-16 | Pharmacia Spa | Morpholinyl 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 |
| AU2009270988A1 (en) * | 2008-07-15 | 2010-01-21 | Genentech, Inc. | Anthracycline derivative conjugates, process for their preparation and their use as antitumor compounds |
| EP2646456B1 (en) * | 2010-12-02 | 2015-01-21 | Nerviano Medical Sciences S.r.l. | Process for the preparation of morpholinyl anthracycline derivatives |
-
2014
- 2014-04-23 CN CN201480023999.XA patent/CN105164138B/zh not_active Expired - Fee Related
- 2014-04-23 WO PCT/EP2014/058262 patent/WO2014177441A1/en not_active Ceased
- 2014-04-23 JP JP2016511009A patent/JP2016517871A/ja active Pending
- 2014-04-23 US US14/787,667 patent/US9828405B2/en active Active
- 2014-04-23 RU RU2015150994A patent/RU2666356C2/ru active
- 2014-04-23 DK DK14719005.2T patent/DK2991993T3/en active
- 2014-04-23 ES ES14719005T patent/ES2695162T3/es active Active
- 2014-04-23 EP EP14719005.2A patent/EP2991993B1/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US9828405B2 (en) | 2017-11-28 |
| CN105164138A (zh) | 2015-12-16 |
| HK1218646A1 (zh) | 2017-03-03 |
| EP2991993B1 (en) | 2018-06-06 |
| RU2015150994A (ru) | 2017-06-06 |
| CN105164138B (zh) | 2017-11-07 |
| RU2666356C2 (ru) | 2018-09-07 |
| JP2016517871A (ja) | 2016-06-20 |
| WO2014177441A1 (en) | 2014-11-06 |
| ES2695162T3 (es) | 2019-01-02 |
| US20160075730A1 (en) | 2016-03-17 |
| EP2991993A1 (en) | 2016-03-09 |
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