BR112013021986A2 - "derivados de fosforamidato de 5-fluoro-2'-desoxiuridina, seus usos e seu processo de preparação, composição farmacêutica e método para sua preparação" - Google Patents
"derivados de fosforamidato de 5-fluoro-2'-desoxiuridina, seus usos e seu processo de preparação, composição farmacêutica e método para sua preparação"Info
- Publication number
- BR112013021986A2 BR112013021986A2 BR112013021986A BR112013021986A BR112013021986A2 BR 112013021986 A2 BR112013021986 A2 BR 112013021986A2 BR 112013021986 A BR112013021986 A BR 112013021986A BR 112013021986 A BR112013021986 A BR 112013021986A BR 112013021986 A2 BR112013021986 A2 BR 112013021986A2
- Authority
- BR
- Brazil
- Prior art keywords
- fluoro
- preparation
- phosphoramidate derivatives
- cells
- pharmaceutical composition
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/655—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
- C07F9/65515—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a five-membered ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
- C07F9/6581—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
- C07F9/6584—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
- C07F9/65842—Cyclic amide derivatives of acids of phosphorus, in which one nitrogen atom belongs to the ring
- C07F9/65844—Cyclic amide derivatives of acids of phosphorus, in which one nitrogen atom belongs to the ring the phosphorus atom being part of a five-membered ring which may be condensed with another ring system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
- C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
-
- 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
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
- A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biochemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
Abstract
resumo patente de invenção: "derivados de fosforamidato de 5-fluoro-2'-desoxiuridina para o uso no tratamento de câncer". a presente invenção refere-se aos derivados de fosforamidato de 5-fluoro-2'-desoxiuridina são descritos para o uso no tratamento de câncer, especialmente no tratamento de câncer onde o paciente exibe resistência, por exemplo, em um paciente com células com um nível diminuído de proteínas transportadoras de nucleosídeo e/ou com células deficientes de nucleosídeo cinase e/ou com células infectadas por micoplasma e/ou com células com um nível aumentado de timidilato sintase.
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB1103582.1A GB201103582D0 (pt) | 2011-03-01 | 2011-03-01 | |
GB1103582.1 | 2011-03-01 | ||
GBGB1105660.3A GB201105660D0 (en) | 2011-04-01 | 2011-04-01 | Chemical compounds |
GB1105660.3 | 2011-04-01 | ||
PCT/GB2012/050457 WO2012117246A1 (en) | 2011-03-01 | 2012-02-29 | Phosphoramidate derivatives of 5 - fluoro - 2 ' - deoxyuridine for use in the treatment of cancer |
Publications (2)
Publication Number | Publication Date |
---|---|
BR112013021986A2 true BR112013021986A2 (pt) | 2016-11-16 |
BR112013021986B1 BR112013021986B1 (pt) | 2021-07-27 |
Family
ID=45841523
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112013021986-6A BR112013021986B1 (pt) | 2011-03-01 | 2012-02-29 | Derivados de fosforamidato de 5-fluoro-2'-desoxiuridina, seus usos e seu processo de preparação, composição farmacêutica e seu método de preparação |
Country Status (29)
Country | Link |
---|---|
US (7) | US8933053B2 (pt) |
EP (4) | EP2681227B1 (pt) |
JP (1) | JP5978232B2 (pt) |
KR (1) | KR101885940B1 (pt) |
CN (2) | CN103403013B (pt) |
AU (1) | AU2012223012C1 (pt) |
BR (1) | BR112013021986B1 (pt) |
CA (1) | CA2828326C (pt) |
CL (1) | CL2013002517A1 (pt) |
CY (2) | CY1117445T1 (pt) |
DK (3) | DK2681227T3 (pt) |
ES (3) | ES2686219T3 (pt) |
HK (1) | HK1192758A1 (pt) |
HR (2) | HRP20211967T1 (pt) |
HU (2) | HUE060127T2 (pt) |
IL (1) | IL228169A (pt) |
LT (1) | LT3447061T (pt) |
MX (1) | MX339822B (pt) |
NZ (1) | NZ615270A (pt) |
PH (1) | PH12015500485B1 (pt) |
PL (3) | PL3031812T3 (pt) |
PT (2) | PT3447061T (pt) |
RS (2) | RS54776B1 (pt) |
RU (1) | RU2614406C2 (pt) |
SG (1) | SG192841A1 (pt) |
SI (2) | SI3447061T1 (pt) |
SM (1) | SMT201600132B (pt) |
WO (1) | WO2012117246A1 (pt) |
ZA (2) | ZA201306468B (pt) |
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GB201016855D0 (en) | 2010-10-06 | 2010-11-17 | Nucana Biomed Ltd | Chemical compounds |
WO2012117246A1 (en) | 2011-03-01 | 2012-09-07 | Nucana Biomed Limited | Phosphoramidate derivatives of 5 - fluoro - 2 ' - deoxyuridine for use in the treatment of cancer |
SI3235824T1 (sl) | 2012-11-16 | 2019-08-30 | University College Cardiff Consultants Limited | Zmes rp / sp gemcitabin-(fenil-(benziloksi-l-alaninil))-fosfata |
WO2015013352A2 (en) * | 2013-07-25 | 2015-01-29 | Patel Hasmukh B | Nucleoside phosphoramidates and phosphoramidites |
CN104447923B (zh) * | 2013-09-23 | 2018-03-30 | 中国药科大学 | 2’‑脱氧‑2’‑氟‑2’‑甲基核苷衍生物及其制备方法与在制药中的用途 |
RU2553996C1 (ru) * | 2013-11-27 | 2015-06-20 | Андрей Александрович Иващенко | Замещенные (2r,3r,5r)-3-гидрокси-(5-пиримидин-1-ил)тетрагидрофуран-2-илметил арил фосфорамидаты |
CN106659765B (zh) | 2014-04-04 | 2021-08-13 | 德玛医药 | 二脱水半乳糖醇及其类似物或衍生物用于治疗非小细胞肺癌和卵巢癌的用途 |
WO2015181624A2 (en) * | 2014-05-28 | 2015-12-03 | Idenix Pharmaceuticals, Inc | Nucleoside derivatives for the treatment of cancer |
CN105153257B (zh) * | 2014-06-12 | 2019-03-05 | 正大天晴药业集团股份有限公司 | 索非布韦的制备方法 |
RS60968B1 (sr) | 2014-06-25 | 2020-11-30 | NuCana plc | Prolekovi gemcitabina |
PL225283B1 (pl) * | 2014-07-24 | 2017-03-31 | Univ Im Adama Mickiewicza W Poznaniu | Pochodne 2,3’-anhydro-2’-deoksy-5-fluorourydyny o działaniu cytotoksycznym, sposób wytwarzania i zastosowanie |
DK3224268T3 (da) | 2014-11-28 | 2019-09-02 | NuCana plc | Nye 2'- og/eller 5'-aminosyreesterphosphoramidat 3'-deoxyadenosinderivater som anti-cancerforbindelser |
CN108368147A (zh) * | 2015-05-27 | 2018-08-03 | 南方研究院 | 用于治疗癌症的核苷酸 |
CN108431016A (zh) * | 2015-11-16 | 2018-08-21 | 艾可瑞恩治疗公司 | 核酸前体药物 |
GB201522764D0 (en) * | 2015-12-23 | 2016-02-03 | Nucana Biomed Ltd | Formulations of phosphate derivatives |
GB201609600D0 (en) * | 2016-06-01 | 2016-07-13 | Nucuna Biomed Ltd | Cancer treatments |
GB201609601D0 (en) * | 2016-06-01 | 2016-07-13 | Nucana Biomed Ltd | Phosphoramidate compounds |
LU100724B1 (en) | 2016-07-14 | 2018-07-31 | Atea Pharmaceuticals Inc | Beta-d-2'-deoxy-2'-alpha-fluoro-2'-beta-c-substituted-4'-fluoro-n6-substituted-6-amino-2-substituted purine nucleotides for the treatment of hepatitis c virus infection |
EP3865136A1 (en) | 2016-09-07 | 2021-08-18 | ATEA Pharmaceuticals, Inc. | 2'-substituted-n6-substituted purine nucleotides for corona virus treatment |
EP3538124A4 (en) | 2016-11-13 | 2020-07-22 | Imagine Pharma | COMPOSITIONS AND METHODS FOR TREATING DIABETES, HIGH BLOOD PRESSURE AND HYPERCHOLESTERINEMIA |
CN109863160B (zh) | 2016-12-23 | 2022-06-07 | 四川科伦博泰生物医药股份有限公司 | 核苷磷酸类化合物及其制备方法和用途 |
RU2644156C1 (ru) * | 2017-02-28 | 2018-02-08 | Александр Васильевич Иващенко | Пролекарство ингибитора NS5B HCV полимеразы, способ его получения и применения |
GB201709471D0 (en) * | 2017-06-14 | 2017-07-26 | Nucana Biomed Ltd | Diastereoselective synthesis of hosphate derivatives |
JP2020530035A (ja) | 2017-08-08 | 2020-10-15 | スン・ヤット−セン・ユニバーシティSun Yat−Sen University | 多剤耐性腫瘍を治療するための方法および組成物 |
GB201713916D0 (en) * | 2017-08-30 | 2017-10-11 | Nucana Biomed Ltd | Treatment regimens |
GB201715011D0 (en) | 2017-09-18 | 2017-11-01 | Nucana Biomed Ltd | Floxuridine synthesis |
GB201720279D0 (en) | 2017-12-05 | 2018-01-17 | Nucana Biomed Ltd | Anticancer compounds |
CN111836823B (zh) * | 2018-03-09 | 2023-06-30 | 国立研究开发法人科学技术振兴机构 | β修饰磷酸化合物前体、β修饰磷酸化合物、反应阻碍剂和包含这些化合物的医药品以及反应阻碍方法 |
CN110387226A (zh) * | 2018-04-20 | 2019-10-29 | 天津大学 | 一种用于检测肿瘤的荧光探针及用途 |
US20220017940A1 (en) * | 2018-11-30 | 2022-01-20 | The University Of Tokyo | Fluorescent probe for detecting carboxypeptidase activity |
GB201904544D0 (en) | 2019-04-01 | 2019-05-15 | NuCana plc | Anticancer compounds |
CN110840907B (zh) * | 2019-08-16 | 2022-11-25 | 南京医科大学 | 一类自由基敏感的尿嘧啶类ProTide前药及其药物用途 |
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US10874687B1 (en) | 2020-02-27 | 2020-12-29 | Atea Pharmaceuticals, Inc. | Highly active compounds against COVID-19 |
EP4204428A1 (en) * | 2020-08-31 | 2023-07-05 | Emory University | 5'-substituted nucleoside monophosphates, prodrugs thereof, and uses related thereto |
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DE10109657A1 (de) | 2001-02-28 | 2002-09-05 | Menarini Ricerche Spa | Verfahren zur Herstellung von (E)-5-(2-Bromvinyl)-2`-desoxyuridin |
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WO2012117246A1 (en) * | 2011-03-01 | 2012-09-07 | Nucana Biomed Limited | Phosphoramidate derivatives of 5 - fluoro - 2 ' - deoxyuridine for use in the treatment of cancer |
MX2020004054A (es) | 2014-06-25 | 2021-11-30 | NuCana plc | Formulacion que comprende un profarmaco de gemcitabina. |
DK3224268T3 (da) | 2014-11-28 | 2019-09-02 | NuCana plc | Nye 2'- og/eller 5'-aminosyreesterphosphoramidat 3'-deoxyadenosinderivater som anti-cancerforbindelser |
KR20180021697A (ko) | 2015-05-14 | 2018-03-05 | 뉴카나 피엘씨 | 암 치료 |
GB201522764D0 (en) | 2015-12-23 | 2016-02-03 | Nucana Biomed Ltd | Formulations of phosphate derivatives |
GB201609600D0 (en) | 2016-06-01 | 2016-07-13 | Nucuna Biomed Ltd | Cancer treatments |
GB201709471D0 (en) | 2017-06-14 | 2017-07-26 | Nucana Biomed Ltd | Diastereoselective synthesis of hosphate derivatives |
-
2012
- 2012-02-29 WO PCT/GB2012/050457 patent/WO2012117246A1/en active Application Filing
- 2012-02-29 PL PL16150494T patent/PL3031812T3/pl unknown
- 2012-02-29 US US14/000,682 patent/US8933053B2/en active Active
- 2012-02-29 CN CN201280010761.4A patent/CN103403013B/zh active Active
- 2012-02-29 SI SI201231972T patent/SI3447061T1/sl unknown
- 2012-02-29 PL PL18178715T patent/PL3447061T3/pl unknown
- 2012-02-29 EP EP12709146.0A patent/EP2681227B1/en active Active
- 2012-02-29 RS RS20160211A patent/RS54776B1/sr unknown
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