JP2016503414A5 - - Google Patents
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- Publication number
- JP2016503414A5 JP2016503414A5 JP2015542007A JP2015542007A JP2016503414A5 JP 2016503414 A5 JP2016503414 A5 JP 2016503414A5 JP 2015542007 A JP2015542007 A JP 2015542007A JP 2015542007 A JP2015542007 A JP 2015542007A JP 2016503414 A5 JP2016503414 A5 JP 2016503414A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- group
- substituted
- composition according
- alkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 239000008194 pharmaceutical composition Substances 0.000 claims 14
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 125000004404 heteroalkyl group Chemical group 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 5
- 125000003710 aryl alkyl group Chemical group 0.000 claims 4
- 125000000547 substituted alkyl group Chemical group 0.000 claims 4
- 239000002246 antineoplastic agent Substances 0.000 claims 3
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 2
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims 1
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims 1
- 239000002136 L01XE07 - Lapatinib Substances 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 229940041181 antineoplastic drug Drugs 0.000 claims 1
- VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 claims 1
- 229960004562 carboplatin Drugs 0.000 claims 1
- 229960005395 cetuximab Drugs 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 229960004316 cisplatin Drugs 0.000 claims 1
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229960001433 erlotinib Drugs 0.000 claims 1
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims 1
- 229960002584 gefitinib Drugs 0.000 claims 1
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims 1
- 229960004891 lapatinib Drugs 0.000 claims 1
- BCFGMOOMADDAQU-UHFFFAOYSA-N lapatinib Chemical compound O1C(CNCCS(=O)(=O)C)=CC=C1C1=CC=C(N=CN=C2NC=3C=C(Cl)C(OCC=4C=C(F)C=CC=4)=CC=3)C2=C1 BCFGMOOMADDAQU-UHFFFAOYSA-N 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 229950008001 matuzumab Drugs 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 229940127084 other anti-cancer agent Drugs 0.000 claims 1
- 229960001756 oxaliplatin Drugs 0.000 claims 1
- DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 230000003439 radiotherapeutic effect Effects 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 229950008250 zalutumumab Drugs 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261725643P | 2012-11-13 | 2012-11-13 | |
| US61/725,643 | 2012-11-13 | ||
| PCT/US2013/069640 WO2014078295A1 (en) | 2012-11-13 | 2013-11-12 | Gemcitabine prodrugs and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016503414A JP2016503414A (ja) | 2016-02-04 |
| JP2016503414A5 true JP2016503414A5 (https=) | 2017-01-05 |
| JP6420247B2 JP6420247B2 (ja) | 2018-11-07 |
Family
ID=50681903
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015542007A Active JP6420247B2 (ja) | 2012-11-13 | 2013-11-12 | ゲムシタビンプロドラッグ及びその使用 |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US8956613B2 (https=) |
| EP (1) | EP2919790B1 (https=) |
| JP (1) | JP6420247B2 (https=) |
| KR (1) | KR20150082606A (https=) |
| CN (1) | CN104968353B (https=) |
| AU (1) | AU2013345007B2 (https=) |
| BR (1) | BR112015010941A2 (https=) |
| CA (1) | CA2891124A1 (https=) |
| SG (1) | SG11201503773SA (https=) |
| WO (1) | WO2014078295A1 (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2891124A1 (en) | 2012-11-13 | 2014-05-22 | BoYen Therapeutics, Inc. | Gemcitabine prodrugs and uses thereof |
| SG11201608303QA (en) | 2014-04-04 | 2016-11-29 | Del Mar Pharmaceuticals | Use of dianhydrogalactitol and analogs or derivatives thereof 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 |
| 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 |
| 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 |
| ITUB20159671A1 (it) * | 2015-12-22 | 2017-06-22 | Maurizio Ceruti | Carbammati lipidici di farmaci antitumorali |
| HUE050290T2 (hu) * | 2015-12-23 | 2020-11-30 | NuCana plc | Kombinált terápia |
| 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 |
| WO2018200859A1 (en) | 2017-04-26 | 2018-11-01 | Kalman Thomas I | 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 |
| AU2019258590B2 (en) * | 2018-04-26 | 2022-09-08 | NanoMed Holdings Pty Ltd | Gemcitabine amphiphile prodrugs |
| 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 |
| CA2278056C (en) | 1997-01-24 | 2006-12-12 | Norsk Hydro Asa | Gemcitabine derivatives |
| 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 |
| WO2004041203A2 (en) * | 2002-11-04 | 2004-05-21 | 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 |
| EP1804838A2 (en) | 2004-09-15 | 2007-07-11 | Drug Discovery Laboratory AS | Drug conjugates of long chain fatty acid or ester moieties as protein binding prodrugs |
| CA2589850C (en) | 2004-12-17 | 2012-05-01 | 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 |
| EP2043653B1 (en) | 2006-06-21 | 2013-12-25 | 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 |
| CA2739757C (en) | 2008-10-07 | 2016-07-05 | Rexahn Pharmaceuticals, Inc. | Hpma - docetaxel or gemcitabine conjugates and uses therefore |
| 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 |
| KR20120086729A (ko) | 2009-11-20 | 2012-08-03 | 클라비스 파마 에이에스에이 | 젬시타빈 유도체의 비경구적 제제 |
| 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 |
| WO2013019945A2 (en) | 2011-08-02 | 2013-02-07 | Clovis Oncology, Inc.. | Method for selection of chemotherapeutic agents for adenocarcinoma cancer |
| 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 |
| CA2891124A1 (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 CA CA2891124A patent/CA2891124A1/en not_active Abandoned
- 2013-11-12 JP JP2015542007A patent/JP6420247B2/ja active Active
- 2013-11-12 BR BR112015010941A patent/BR112015010941A2/pt not_active IP Right Cessation
- 2013-11-12 US US14/077,778 patent/US8956613B2/en not_active Expired - Fee Related
- 2013-11-12 SG SG11201503773SA patent/SG11201503773SA/en unknown
- 2013-11-12 KR KR1020157015453A patent/KR20150082606A/ko not_active Ceased
- 2013-11-12 WO PCT/US2013/069640 patent/WO2014078295A1/en not_active Ceased
- 2013-11-12 AU AU2013345007A patent/AU2013345007B2/en active Active
- 2013-11-12 CN CN201380059144.8A patent/CN104968353B/zh active Active
- 2013-11-12 EP EP13855096.7A patent/EP2919790B1/en active Active
-
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
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