BR112015010941A2 - pró-fármacos de gemcitabina e suas utilizações - Google Patents
pró-fármacos de gemcitabina e suas utilizaçõesInfo
- Publication number
- BR112015010941A2 BR112015010941A2 BR112015010941A BR112015010941A BR112015010941A2 BR 112015010941 A2 BR112015010941 A2 BR 112015010941A2 BR 112015010941 A BR112015010941 A BR 112015010941A BR 112015010941 A BR112015010941 A BR 112015010941A BR 112015010941 A2 BR112015010941 A2 BR 112015010941A2
- Authority
- BR
- Brazil
- Prior art keywords
- substituted
- group
- cycloheteroalkyl
- formula
- compounds
- Prior art date
Links
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 title abstract 2
- 229960005277 gemcitabine Drugs 0.000 title abstract 2
- 239000000651 prodrug Substances 0.000 title abstract 2
- 229940002612 prodrug Drugs 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 2
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000005907 cancer growth Effects 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000005017 substituted alkenyl group Chemical group 0.000 abstract 1
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 1
- 125000004426 substituted alkynyl group Chemical group 0.000 abstract 1
Classifications
-
- 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
-
- 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
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nutrition Science (AREA)
- Dermatology (AREA)
- Physiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Saccharide Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261725643P | 2012-11-13 | 2012-11-13 | |
| PCT/US2013/069640 WO2014078295A1 (en) | 2012-11-13 | 2013-11-12 | Gemcitabine prodrugs and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112015010941A2 true BR112015010941A2 (pt) | 2017-07-11 |
Family
ID=50681903
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112015010941A BR112015010941A2 (pt) | 2012-11-13 | 2013-11-12 | pró-fármacos de gemcitabina e suas utilizações |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US8956613B2 (enExample) |
| EP (1) | EP2919790B1 (enExample) |
| JP (1) | JP6420247B2 (enExample) |
| KR (1) | KR20150082606A (enExample) |
| CN (1) | CN104968353B (enExample) |
| AU (1) | AU2013345007B2 (enExample) |
| BR (1) | BR112015010941A2 (enExample) |
| CA (1) | CA2891124A1 (enExample) |
| SG (1) | SG11201503773SA (enExample) |
| WO (1) | WO2014078295A1 (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014078295A1 (en) | 2012-11-13 | 2014-05-22 | BoYen Therapeutics, Inc. | Gemcitabine prodrugs and uses thereof |
| EP3125920B1 (en) | 2014-04-04 | 2020-12-23 | Del Mar Pharmaceuticals | Dianhydrogalactitol, diacetyldianhydrogalactitol or dibromodulcitol to treat non-small-cell carcinoma of the lung and ovarian cancer |
| WO2016078397A1 (zh) * | 2014-11-17 | 2016-05-26 | 常州方圆制药有限公司 | 新型胞苷衍生物及其应用 |
| WO2016078399A1 (zh) * | 2014-11-17 | 2016-05-26 | 常州方圆制药有限公司 | 新型胞苷衍生物二聚体及其应用 |
| WO2016078160A1 (zh) * | 2014-11-17 | 2016-05-26 | 常州方圆制药有限公司 | 胞苷衍生物及其应用 |
| WO2016078163A1 (zh) | 2014-11-17 | 2016-05-26 | 常州方圆制药有限公司 | 新型胞苷衍生物二聚体及其应用 |
| ITUB20159671A1 (it) * | 2015-12-22 | 2017-06-22 | Maurizio Ceruti | Carbammati lipidici di farmaci antitumorali |
| PT3393478T (pt) * | 2015-12-23 | 2020-03-24 | NuCana plc | Terapia combinada |
| CN106946960A (zh) * | 2017-03-29 | 2017-07-14 | 郑州泰基鸿诺医药股份有限公司 | 一种吉西他滨前药的晶型、制备方法、用途和药物组合物 |
| CA3061621A1 (en) | 2017-04-26 | 2018-11-01 | Thomas I. Kalman | Multitargeted nucleoside derivatives |
| CN108329371B (zh) * | 2018-03-06 | 2021-04-09 | 沈阳药科大学 | 白蛋白结合型吉西他滨前药及其合成和应用 |
| JP7598313B2 (ja) * | 2018-04-26 | 2024-12-11 | ナノメッド ホールディングス プロプライエタリー リミテッド | ジェムシタビン両親媒性プロドラッグ |
| GR1009958B (el) * | 2019-04-24 | 2021-03-18 | ΕΝΟΡΑΣΙΣ ΑΝΩΝΥΜΗ ΕΜΠΟΡΙΚΗ ΕΤΑΙΡΕΙΑ ΦΑΡΜΑΚΕΥΤΙΚΩΝ ΚΑΙ ΙΑΤΡΙΚΩΝ ΥΛΙΚΩΝ ΚΑΙ ΜΗΧΑΝΗΜΑΤΩΝ με δ.τ. "ΕΝΟΡΑΣΙΣ Α.Ε." | Παραγωγα γεμσιταβινης και μεθοδοι δημιουργιας παραγωγων γεμσιταβινης |
| GB201906214D0 (en) | 2019-05-02 | 2019-06-19 | Econic Tech Ltd | A polyol block copolymer, compositions and processes therefor |
| GB201906210D0 (en) | 2019-05-02 | 2019-06-19 | Econic Tech Limited | A polyol block copolymer, compositions and processes therefor |
| CN114011581B (zh) * | 2021-11-09 | 2023-03-24 | 昆明理工大学 | 一种弱酸性条件下铜硫分离的抑制剂制备方法及其应用 |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4994558A (en) | 1986-12-24 | 1991-02-19 | Eli Lilly And Company | Immunoglobulin conjugates |
| US4814438A (en) | 1986-12-24 | 1989-03-21 | Eli Lilly And Company | Immunoglobulin conjugates of 2',2'-difluronucleosides |
| ATE236188T1 (de) * | 1997-01-24 | 2003-04-15 | Conpharma As | Gemcitabin-derivate |
| GB2321454A (en) | 1997-01-24 | 1998-07-29 | Norsk Hydro As | Gemcitabine esters and amides |
| US6376470B1 (en) | 1999-09-23 | 2002-04-23 | Enzon, Inc. | Polymer conjugates of ara-C and ara-C derivatives |
| US7265096B2 (en) | 2002-11-04 | 2007-09-04 | Xenoport, Inc. | Gemcitabine prodrugs, pharmaceutical compositions and uses thereof |
| GB0321613D0 (en) | 2003-09-15 | 2003-10-15 | Drug Discovery Lab As | Compounds |
| FR2874016B1 (fr) | 2004-06-30 | 2006-11-24 | Centre Nat Rech Scient Cnrse | Nanoparticules de derives de la gemcitabine |
| WO2006029081A2 (en) | 2004-09-02 | 2006-03-16 | Neopharm, Inc. | Nucleoside-lipid conjugates, their method of preparation and uses thereof |
| WO2006030217A2 (en) | 2004-09-15 | 2006-03-23 | Drug Discovery Laboratory As | Drug conjugates of long chain fatty acid or ester moieties as protein binding prodrugs |
| US7691827B2 (en) | 2004-12-17 | 2010-04-06 | Eli Lilly And Company | Amide prodrug of gemcitabine, compositions and use thereof |
| NO322682B1 (no) | 2005-03-18 | 2006-11-27 | Clavis Pharma Asa | Anvendelse av gemcitabinderivater for fremstilling av orale doseringsformer ved kreftbehandling, samt slike orale doseringsformer |
| AT502221A1 (de) | 2005-07-20 | 2007-02-15 | Pharmacon Forschung & Beratung Gmbh | Homogemcitabine, verfahren zu ihrer herstellung sowie deren verwendung |
| WO2007149891A2 (en) | 2006-06-21 | 2007-12-27 | Eli Lilly And Company | Crystalline forms of gemcitabine amide prodrug, compositions and use thereof |
| CN101209350B (zh) | 2006-12-30 | 2011-09-07 | 中国人民解放军军事医学科学院毒物药物研究所 | 以氨基酸为连接子的多聚谷氨酸-药物偶合物 |
| WO2010039039A1 (en) | 2008-10-03 | 2010-04-08 | Clavis Pharma Asa | Oral formulations of gemcitabine derivatives |
| JP2012505228A (ja) | 2008-10-07 | 2012-03-01 | レクサン ファーマシューティカルズ インコーポレイテッド | Ｈｐｍａ−ドセタキセルまたはゲムシタビンコンジュゲートおよびその使用 |
| CN101525361B (zh) | 2009-04-21 | 2010-11-17 | 济南圣鲁金药物技术开发有限公司 | 基于吉西他滨结构的前药及其合成方法及应用 |
| US8871780B2 (en) | 2009-07-02 | 2014-10-28 | Kempharm, Inc. | Phenylethanoic acid, phenylpropanoic acid and phenylpropenoic acid conjugates and prodrugs of hydrocodone, method of making and use thereof |
| JP2013511516A (ja) | 2009-11-20 | 2013-04-04 | クラヴィス・ファルマ・アーエスアー | ゲムシタビン誘導体の非経口製剤 |
| GB201016855D0 (en) | 2010-10-06 | 2010-11-17 | Nucana Biomed Ltd | Chemical compounds |
| WO2012098557A1 (en) | 2011-01-20 | 2012-07-26 | Institute Of Life Sciences | Pegylated gemcitabine derivative and process for preparing the same |
| EP2739290A4 (en) | 2011-08-02 | 2015-04-15 | Clovis Oncology Inc | METHOD FOR SELECTION OF CHEMOTHERAPEUTICS AGAINST ADENOCARCINOMAS |
| CN102432654A (zh) | 2011-09-26 | 2012-05-02 | 宋云龙 | 吉西他滨酰胺衍生物及其制备方法和用途 |
| WO2014078295A1 (en) | 2012-11-13 | 2014-05-22 | BoYen Therapeutics, Inc. | Gemcitabine prodrugs and uses thereof |
| CN103130854A (zh) | 2013-01-31 | 2013-06-05 | 华东师范大学 | 维生素e琥珀酸酯化吉西他滨前药及应用 |
-
2013
- 2013-11-12 WO PCT/US2013/069640 patent/WO2014078295A1/en not_active Ceased
- 2013-11-12 EP EP13855096.7A patent/EP2919790B1/en active Active
- 2013-11-12 CN CN201380059144.8A patent/CN104968353B/zh active Active
- 2013-11-12 SG SG11201503773SA patent/SG11201503773SA/en unknown
- 2013-11-12 KR KR1020157015453A patent/KR20150082606A/ko not_active Ceased
- 2013-11-12 US US14/077,778 patent/US8956613B2/en not_active Expired - Fee Related
- 2013-11-12 JP JP2015542007A patent/JP6420247B2/ja active Active
- 2013-11-12 AU AU2013345007A patent/AU2013345007B2/en active Active
- 2013-11-12 CA CA2891124A patent/CA2891124A1/en not_active Abandoned
- 2013-11-12 BR BR112015010941A patent/BR112015010941A2/pt not_active IP Right Cessation
-
2015
- 2015-01-16 US US14/599,166 patent/US9540410B2/en not_active Expired - Fee Related
-
2016
- 2016-12-05 US US15/369,187 patent/US9890189B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US20150132298A1 (en) | 2015-05-14 |
| EP2919790B1 (en) | 2018-04-04 |
| AU2013345007B2 (en) | 2018-08-30 |
| CN104968353B (zh) | 2017-12-22 |
| SG11201503773SA (en) | 2015-06-29 |
| US20140134160A1 (en) | 2014-05-15 |
| EP2919790A4 (en) | 2016-04-06 |
| CA2891124A1 (en) | 2014-05-22 |
| WO2014078295A1 (en) | 2014-05-22 |
| CN104968353A (zh) | 2015-10-07 |
| US9890189B2 (en) | 2018-02-13 |
| WO2014078295A8 (en) | 2015-05-21 |
| JP6420247B2 (ja) | 2018-11-07 |
| EP2919790A1 (en) | 2015-09-23 |
| AU2013345007A1 (en) | 2015-05-21 |
| JP2016503414A (ja) | 2016-02-04 |
| US9540410B2 (en) | 2017-01-10 |
| KR20150082606A (ko) | 2015-07-15 |
| US20170107245A1 (en) | 2017-04-20 |
| US8956613B2 (en) | 2015-02-17 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] | ||
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |