JP2008521930A5 - - Google Patents
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- Publication number
- JP2008521930A5 JP2008521930A5 JP2007544558A JP2007544558A JP2008521930A5 JP 2008521930 A5 JP2008521930 A5 JP 2008521930A5 JP 2007544558 A JP2007544558 A JP 2007544558A JP 2007544558 A JP2007544558 A JP 2007544558A JP 2008521930 A5 JP2008521930 A5 JP 2008521930A5
- Authority
- JP
- Japan
- Prior art keywords
- eniluracil
- prodrug
- administered
- dpd inhibitor
- dose
- 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.)
- Pending
Links
- 229960002949 fluorouracil Drugs 0.000 claims 41
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims 40
- 239000003112 inhibitor Substances 0.000 claims 28
- JOZGNYDSEBIJDH-UHFFFAOYSA-N eniluracil Chemical group O=C1NC=C(C#C)C(=O)N1 JOZGNYDSEBIJDH-UHFFFAOYSA-N 0.000 claims 24
- 229950010213 eniluracil Drugs 0.000 claims 24
- UEJQGOKMPMUMTO-UHFFFAOYSA-N C(C#C)OC1=NC=C(C(=N1)OCC#C)F Chemical compound C(C#C)OC1=NC=C(C(=N1)OCC#C)F UEJQGOKMPMUMTO-UHFFFAOYSA-N 0.000 claims 22
- GAGWJHPBXLXJQN-UORFTKCHSA-N Capecitabine Chemical compound C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1[C@H]1[C@H](O)[C@H](O)[C@@H](C)O1 GAGWJHPBXLXJQN-UORFTKCHSA-N 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 8
- GAGWJHPBXLXJQN-UHFFFAOYSA-N Capecitabine Natural products C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1C1C(O)C(O)C(C)O1 GAGWJHPBXLXJQN-UHFFFAOYSA-N 0.000 claims 7
- 229960004117 capecitabine Drugs 0.000 claims 7
- 238000009472 formulation Methods 0.000 claims 7
- 239000000203 mixture Substances 0.000 claims 7
- -1 5′-deoxy-4 ′ Chemical compound 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 239000003981 vehicle Substances 0.000 claims 3
- FHIDNBAQOFJWCA-UAKXSSHOSA-N 5-fluorouridine Chemical compound O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C(F)=C1 FHIDNBAQOFJWCA-UAKXSSHOSA-N 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- ISAKRJDGNUQOIC-UHFFFAOYSA-N Uracil Natural products O=C1C=CNC(=O)N1 ISAKRJDGNUQOIC-UHFFFAOYSA-N 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 238000013270 controlled release Methods 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940035893 uracil Drugs 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- HAUXRJCZDHHADG-UHFFFAOYSA-N 2,4-dioxo-1h-pyrimidine-5-carbonitrile Chemical compound O=C1NC=C(C#N)C(=O)N1 HAUXRJCZDHHADG-UHFFFAOYSA-N 0.000 claims 1
- IDYKCXHJJGMAEV-RRKCRQDMSA-N 4-amino-5-fluoro-1-[(2r,4s,5r)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one Chemical compound C1=C(F)C(N)=NC(=O)N1[C@@H]1O[C@H](CO)[C@@H](O)C1 IDYKCXHJJGMAEV-RRKCRQDMSA-N 0.000 claims 1
- CYMBDTMRFAUHRM-UHFFFAOYSA-N 5-(1-chloroethenyl)-1h-pyrimidine-2,4-dione Chemical compound ClC(=C)C1=CNC(=O)NC1=O CYMBDTMRFAUHRM-UHFFFAOYSA-N 0.000 claims 1
- XFPGPBKTWIFNAA-UHFFFAOYSA-N 5-(2-bromo-1-chloroethenyl)-1h-pyrimidine-2,4-dione Chemical compound BrC=C(Cl)C1=CNC(=O)NC1=O XFPGPBKTWIFNAA-UHFFFAOYSA-N 0.000 claims 1
- BLXGZIDBSXVMLU-UHFFFAOYSA-N 5-(2-bromoethenyl)-1h-pyrimidine-2,4-dione Chemical compound BrC=CC1=CNC(=O)NC1=O BLXGZIDBSXVMLU-UHFFFAOYSA-N 0.000 claims 1
- LKTQRCSUYNIRSM-UHFFFAOYSA-N 5-(2-bromoethynyl)-1h-pyrimidine-2,4-dione Chemical compound BrC#CC1=CNC(=O)NC1=O LKTQRCSUYNIRSM-UHFFFAOYSA-N 0.000 claims 1
- FBOIBTWYSVRYTJ-VBLCRABPSA-N 5-[(3S,4S,5S)-6-fluoro-3,4,5-trihydroxyoxan-2-yl]-1H-pyrimidine-2,4-dione Chemical compound FC1[C@H]([C@H]([C@@H](C(O1)C=1C(NC(NC=1)=O)=O)O)O)O FBOIBTWYSVRYTJ-VBLCRABPSA-N 0.000 claims 1
- BLXGZIDBSXVMLU-OWOJBTEDSA-N 5-[(e)-2-bromoethenyl]-1h-pyrimidine-2,4-dione Chemical compound Br\C=C\C1=CNC(=O)NC1=O BLXGZIDBSXVMLU-OWOJBTEDSA-N 0.000 claims 1
- LQLQRFGHAALLLE-UHFFFAOYSA-N 5-bromouracil Chemical compound BrC1=CNC(=O)NC1=O LQLQRFGHAALLLE-UHFFFAOYSA-N 0.000 claims 1
- ZRYZBEQILKESAW-UHFFFAOYSA-N 5-ethenyl-1h-pyrimidine-2,4-dione Chemical compound C=CC1=CNC(=O)NC1=O ZRYZBEQILKESAW-UHFFFAOYSA-N 0.000 claims 1
- STRZQWQNZQMHQR-UAKXSSHOSA-N 5-fluorocytidine Chemical compound C1=C(F)C(N)=NC(=O)N1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 STRZQWQNZQMHQR-UAKXSSHOSA-N 0.000 claims 1
- TUFMBCUUDJKPJB-UHFFFAOYSA-N 5-hex-1-ynyl-1h-pyrimidine-2,4-dione Chemical compound CCCCC#CC1=CNC(=O)NC1=O TUFMBCUUDJKPJB-UHFFFAOYSA-N 0.000 claims 1
- KSNXJLQDQOIRIP-UHFFFAOYSA-N 5-iodouracil Chemical compound IC1=CNC(=O)NC1=O KSNXJLQDQOIRIP-UHFFFAOYSA-N 0.000 claims 1
- KFRZFMXZIDRZJI-UHFFFAOYSA-N 5-phenylselanyl-1,3-diazinane-2,4,6-trione Chemical compound O=C1NC(=O)NC(=O)C1[Se]C1=CC=CC=C1 KFRZFMXZIDRZJI-UHFFFAOYSA-N 0.000 claims 1
- ZEGGHGSNGZPEHQ-UHFFFAOYSA-N 5-phenylselanyl-1h-pyrimidine-2,4-dione Chemical compound O=C1NC(=O)NC=C1[Se]C1=CC=CC=C1 ZEGGHGSNGZPEHQ-UHFFFAOYSA-N 0.000 claims 1
- KRPWRQUISWCMBL-UHFFFAOYSA-N 5-phenylsulfanyl-1,3-diazinane-2,4,6-trione Chemical compound O=C1NC(=O)NC(=O)C1SC1=CC=CC=C1 KRPWRQUISWCMBL-UHFFFAOYSA-N 0.000 claims 1
- MFORXTHLVUSZNY-UHFFFAOYSA-N 5-phenylsulfanyl-1h-pyrimidine-2,4-dione Chemical compound O=C1NC(=O)NC=C1SC1=CC=CC=C1 MFORXTHLVUSZNY-UHFFFAOYSA-N 0.000 claims 1
- UJBCLAXPPIDQEE-UHFFFAOYSA-N 5-prop-1-ynyl-1h-pyrimidine-2,4-dione Chemical compound CC#CC1=CNC(=O)NC1=O UJBCLAXPPIDQEE-UHFFFAOYSA-N 0.000 claims 1
- WFWLQNSHRPWKFK-UHFFFAOYSA-N Tegafur Chemical compound O=C1NC(=O)C(F)=CN1C1OCCC1 WFWLQNSHRPWKFK-UHFFFAOYSA-N 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- ZWAOHEXOSAUJHY-ZIYNGMLESA-N doxifluridine Chemical compound O[C@@H]1[C@H](O)[C@@H](C)O[C@H]1N1C(=O)NC(=O)C(F)=C1 ZWAOHEXOSAUJHY-ZIYNGMLESA-N 0.000 claims 1
- ODKNJVUHOIMIIZ-RRKCRQDMSA-N floxuridine Chemical compound C1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C(F)=C1 ODKNJVUHOIMIIZ-RRKCRQDMSA-N 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 230000002427 irreversible effect Effects 0.000 claims 1
- 230000007774 longterm Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000004005 microsphere Substances 0.000 claims 1
- 150000003014 phosphoric acid esters Chemical class 0.000 claims 1
- 230000002441 reversible effect Effects 0.000 claims 1
- 230000008685 targeting Effects 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63303404P | 2004-12-03 | 2004-12-03 | |
| PCT/US2005/043706 WO2006060697A1 (en) | 2004-12-03 | 2005-12-05 | Methods for administering dpd inhibitors in combination with 5-fu and 5-fu prodrugs |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012186899A Division JP2012229273A (ja) | 2004-12-03 | 2012-08-27 | ５−ｆｕおよび５−ｆｕプロドラッグと併用してｄｐｄ阻害物質を投与するための方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008521930A JP2008521930A (ja) | 2008-06-26 |
| JP2008521930A5 true JP2008521930A5 (enExample) | 2009-02-12 |
Family
ID=36087538
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007544558A Pending JP2008521930A (ja) | 2004-12-03 | 2005-12-05 | ５−ｆｕおよび５−ｆｕプロドラッグと併用してｄｐｄ阻害物質を投与するための方法 |
| JP2012186899A Pending JP2012229273A (ja) | 2004-12-03 | 2012-08-27 | ５−ｆｕおよび５−ｆｕプロドラッグと併用してｄｐｄ阻害物質を投与するための方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012186899A Pending JP2012229273A (ja) | 2004-12-03 | 2012-08-27 | ５−ｆｕおよび５−ｆｕプロドラッグと併用してｄｐｄ阻害物質を投与するための方法 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US8318756B2 (enExample) |
| EP (1) | EP1827443A1 (enExample) |
| JP (2) | JP2008521930A (enExample) |
| KR (1) | KR20070098798A (enExample) |
| CN (2) | CN102441170A (enExample) |
| AU (1) | AU2005311730B2 (enExample) |
| CA (1) | CA2587514A1 (enExample) |
| MX (1) | MX2007006646A (enExample) |
| NZ (1) | NZ555176A (enExample) |
| WO (1) | WO2006060697A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1827443A1 (en) * | 2004-12-03 | 2007-09-05 | Adherex Technologies, Inc. | Methods for administering dpd inhibitors in combination with 5-fu and 5-fu prodrugs |
| US20090196833A1 (en) * | 2008-02-06 | 2009-08-06 | Adherex Technologies Inc. | Compositions comprising topical dpd inhibitors and methods of using same in the treatment of hand-foot syndrome |
| WO2009118712A2 (en) * | 2008-03-27 | 2009-10-01 | Ecole Polytechnique Federale De Lausanne (Epfl) | Novel dihydroxypyrrolidine derivatives as anti-cancer agents |
| EP3792634A3 (en) * | 2009-07-17 | 2021-06-02 | Myriad Genetics, Inc. | Method of assaying 5-fu |
| US8658618B2 (en) * | 2009-10-14 | 2014-02-25 | Adherex Technologies, Inc. | Methods for preventing or reducing neurotoxicity associated with administering DPD inhibitors in combination with 5-FU and 5-FU prodrugs |
| WO2014089004A1 (en) * | 2012-12-04 | 2014-06-12 | Adherex Technologies, Inc. | Methods for treating 5-fluorouracil prodrug non-responsive cancer patients |
| CN106692173A (zh) * | 2015-11-18 | 2017-05-24 | 北京诺普德医药科技有限公司 | 一种抗肿瘤复方组合物及其应用 |
| CN106619689B (zh) * | 2016-12-30 | 2018-05-01 | 陈晓华 | 一种用于治疗癌症的药物组合物、试剂盒及其应用 |
| WO2020125550A1 (zh) * | 2018-12-19 | 2020-06-25 | 广州君赫生物科技有限公司 | 化合物在治疗与saicar累积相关的疾病的用途 |
| CN109655606A (zh) * | 2019-01-11 | 2019-04-19 | 华东师范大学 | 一种利用3d类器官评价药物肠毒性的检测方法 |
| WO2023283921A1 (zh) * | 2021-07-16 | 2023-01-19 | 北京深蓝泰医药科技有限公司 | Dpd抑制剂及其药物组合物和用途 |
| IL321302A (en) * | 2022-12-06 | 2025-08-01 | Elion Oncology Inc | Combined use of anilouracil and capecitabine for cancer treatment |
| WO2025015267A1 (en) * | 2023-07-13 | 2025-01-16 | Processa Pharmaceuticals, Inc. | Methods of personalizing cancer treatment |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8629892D0 (en) | 1986-12-15 | 1987-01-28 | Wellcome Found | Antiviral compounds |
| US5157114A (en) | 1988-08-19 | 1992-10-20 | Burroughs Wellcome Co. | 2',3'-dideoxy-3'-fluoro-5-ethyngluridine |
| SG49855A1 (en) | 1990-07-19 | 1998-06-15 | Wellcome Found | Enzyme inactivators |
| GB9020930D0 (en) * | 1990-09-26 | 1990-11-07 | Wellcome Found | Pharmaceutical combinations |
| IT1255522B (it) * | 1992-09-24 | 1995-11-09 | Ubaldo Conte | Compressa per impiego terapeutico atta a cedere una o piu' sostanze attive con differenti velocita' |
| US5476855A (en) | 1993-11-02 | 1995-12-19 | Mahmoud H. el Kouni | Enzyme inhibitors, their synthesis and methods for use |
| NZ330360A (en) | 1997-06-02 | 1999-03-29 | Hoffmann La Roche | 5'-deoxy-cytidine derivatives, their manufacture and use as antitumoral agents |
| US6716452B1 (en) * | 2000-08-22 | 2004-04-06 | New River Pharmaceuticals Inc. | Active agent delivery systems and methods for protecting and administering active agents |
| US20040028687A1 (en) * | 2002-01-15 | 2004-02-12 | Waelti Ernst Rudolf | Methods and compositions for the targeted delivery of therapeutic substances to specific cells and tissues |
| EP1827443A1 (en) * | 2004-12-03 | 2007-09-05 | Adherex Technologies, Inc. | Methods for administering dpd inhibitors in combination with 5-fu and 5-fu prodrugs |
-
2005
- 2005-12-05 EP EP05852819A patent/EP1827443A1/en not_active Withdrawn
- 2005-12-05 AU AU2005311730A patent/AU2005311730B2/en not_active Ceased
- 2005-12-05 KR KR1020077013028A patent/KR20070098798A/ko not_active Ceased
- 2005-12-05 CA CA002587514A patent/CA2587514A1/en not_active Abandoned
- 2005-12-05 WO PCT/US2005/043706 patent/WO2006060697A1/en not_active Ceased
- 2005-12-05 NZ NZ555176A patent/NZ555176A/en not_active IP Right Cessation
- 2005-12-05 MX MX2007006646A patent/MX2007006646A/es active IP Right Grant
- 2005-12-05 US US11/294,643 patent/US8318756B2/en active Active
- 2005-12-05 CN CN2011104284155A patent/CN102441170A/zh active Pending
- 2005-12-05 JP JP2007544558A patent/JP2008521930A/ja active Pending
- 2005-12-05 CN CNA2005800414059A patent/CN101068549A/zh active Pending
-
2012
- 2012-08-27 JP JP2012186899A patent/JP2012229273A/ja active Pending
- 2012-11-27 US US13/686,240 patent/US20130184232A1/en not_active Abandoned
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