JP2002502836A5 - - Google Patents
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- JP2002502836A5 JP2002502836A5 JP2000530488A JP2000530488A JP2002502836A5 JP 2002502836 A5 JP2002502836 A5 JP 2002502836A5 JP 2000530488 A JP2000530488 A JP 2000530488A JP 2000530488 A JP2000530488 A JP 2000530488A JP 2002502836 A5 JP2002502836 A5 JP 2002502836A5
- Authority
- JP
- Japan
- Prior art keywords
- xii
- embedded image
- vii
- prodrug
- hydroxylated
- 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.)
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- 239000000651 prodrug Substances 0.000 description 7
- 229940002612 prodrugs Drugs 0.000 description 7
- 206010028980 Neoplasm Diseases 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 238000007262 aromatic hydroxylation reaction Methods 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 230000002255 enzymatic Effects 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- IHAWCLXPXUOJEO-JXMROGBWSA-N COc1ccc(/C=C/C(c(cc2OC)cc(OC)c2OC)=O)cc1 Chemical compound COc1ccc(/C=C/C(c(cc2OC)cc(OC)c2OC)=O)cc1 IHAWCLXPXUOJEO-JXMROGBWSA-N 0.000 description 1
- 102100004047 CYP1B1 Human genes 0.000 description 1
- 101710036800 CYP1B1 Proteins 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- 230000000394 mitotic Effects 0.000 description 1
Description
【特許請求の範囲】
【請求項１】 腫瘍の治療用の薬剤の製造における、一般式ＶII又はＸIIのいずれか一方を有する、酵素による芳香族ヒドロキシル化によって活性化されたプロドラッグの使用。
（ＶII ）：
【化１】
（ＸII ）：
【化２】
【請求項２】 前記薬剤がさらに薬学的に許容しうるキャリア、希釈剤または賦形剤を含有する、請求項１に記載のプロドラッグの使用。
【請求項３】 プロドラッグがＣＹＰ１Ｂ１によってヒドロキシル化される請求項１または２に記載のプロドラッグの使用。
【請求項４】 プロドラッグが、一般式VII及びXIIからなる群のいずれか一方から選択され、かつ、ヒドロキシル化された状態の有糸分裂阻害剤である請求項１から３のいずれか１項に記載のプロドラッグの使用。
【請求項５】 （ｉ）一般式ＶIIまたはＸIIのいずれか一方を有する化合物を細胞試料に投与する工程と、
（ＶII ）：
【化３】
（ＸII ）：
【化４】
（ｉｉ）前記細胞中に、前記化合物のヒドロキシル化された代謝物が存在するか、存在しないかを測定する工程と、
（ｉｉｉ）工程（ｉｉ）の結果を腫瘍状の細胞試料の存在又は不在と相互に関連させる工程と、
からなる腫瘍の状態の細胞試料の診断方法。
【請求項６】 腫瘍の治療用の薬剤の製造における、一般式ＶII又はＸIIのいずれか一方を有する、酵素による芳香族ヒドロキシル化によって活性化されたプロドラッグの使用による治療法。
（ＶII ）：
【化５】
（ＸII ）：
【化６】
【請求項１】 腫瘍の治療用の薬剤の製造における、一般式ＶII又はＸIIのいずれか一方を有する、酵素による芳香族ヒドロキシル化によって活性化されたプロドラッグの使用。
（ＶII ）：
【化１】
【化２】
【請求項３】 プロドラッグがＣＹＰ１Ｂ１によってヒドロキシル化される請求項１または２に記載のプロドラッグの使用。
【請求項４】 プロドラッグが、一般式VII及びXIIからなる群のいずれか一方から選択され、かつ、ヒドロキシル化された状態の有糸分裂阻害剤である請求項１から３のいずれか１項に記載のプロドラッグの使用。
【請求項５】 （ｉ）一般式ＶIIまたはＸIIのいずれか一方を有する化合物を細胞試料に投与する工程と、
（ＶII ）：
【化３】
【化４】
（ｉｉｉ）工程（ｉｉ）の結果を腫瘍状の細胞試料の存在又は不在と相互に関連させる工程と、
からなる腫瘍の状態の細胞試料の診断方法。
【請求項６】 腫瘍の治療用の薬剤の製造における、一般式ＶII又はＸIIのいずれか一方を有する、酵素による芳香族ヒドロキシル化によって活性化されたプロドラッグの使用による治療法。
（ＶII ）：
【化５】
【化６】
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9802522.4A GB9802522D0 (en) | 1998-02-06 | 1998-02-06 | Hydroxylation activated prodrugs |
| US09/115,015 | 1998-07-14 | ||
| US9802522.4 | 1998-07-14 | ||
| US09/115,015 US6214886B1 (en) | 1998-02-06 | 1998-07-14 | Hydroxylation activated prodrugs |
| PCT/GB1999/000155 WO1999040056A1 (en) | 1998-02-06 | 1999-02-02 | Hydroxylation activated prodrugs |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2002502836A JP2002502836A (ja) | 2002-01-29 |
| JP2002502836A5 true JP2002502836A5 (ja) | 2006-03-16 |
| JP4642226B2 JP4642226B2 (ja) | 2011-03-02 |
Family
ID=26313066
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000530488A Expired - Fee Related JP4642226B2 (ja) | 1998-02-06 | 1999-02-02 | ヒドロキシル化により活性化されたプロドラッグ |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US6677383B1 (ja) |
| EP (1) | EP1051383B1 (ja) |
| JP (1) | JP4642226B2 (ja) |
| AT (1) | ATE272040T1 (ja) |
| AU (1) | AU2173899A (ja) |
| CA (1) | CA2319836C (ja) |
| DE (1) | DE69918950T2 (ja) |
| ES (1) | ES2226332T3 (ja) |
| WO (1) | WO1999040056A1 (ja) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE69918950T2 (de) | 1998-02-06 | 2005-07-28 | De Montfort University | Durch hydroxylierung aktivierte medikamentvorstufen |
| GB2334256A (en) | 1998-02-12 | 1999-08-18 | Univ Montfort | Hydroxylation activated prodrugs |
| US7321050B2 (en) | 1999-12-06 | 2008-01-22 | Welichem Biotech Inc. | Anti-inflammatory and psoriasis treatment and protein kinase inhibition by hydroxy stilbenes and novel stilbene derivatives and analogues |
| ES2334635T3 (es) * | 1999-12-06 | 2010-03-15 | Welichem Biotech Inc. | Polihidroxiestilbeno y oxidos de estilbeno como agentes antipsoriasicos e inhibidores de la proteina quinasa. |
| GB0007401D0 (en) | 2000-03-27 | 2000-05-17 | Cancer Res Campaign Tech | Substituted chalcones as therapeeutic compounds |
| JP2003531133A (ja) * | 2000-04-13 | 2003-10-21 | エイチエスシー リサーチ アンド ディベロップメント リミテッド パートナーシップ | 細胞増殖を調節する新規化合物 |
| ATE327750T1 (de) | 2001-02-22 | 2006-06-15 | Univ London Pharmacy | Benz-indol- und benzo-chinolin-derivate als prodrugs zur tumorbehandlung |
| ATE378328T1 (de) | 2001-02-22 | 2007-11-15 | Univ London Pharmacy | Pyrrolo-indol- und pyrrolo-chinolin-derivate als prodrugs zur tumorbehandlung |
| US6589997B2 (en) * | 2001-06-29 | 2003-07-08 | North Shore-Long Island Jewish Health System | Small-molecule modulators of hepatocyte growth factor/scatter factor activities |
| GB0123777D0 (en) * | 2001-10-03 | 2001-11-21 | Cancer Res Ventures Ltd | Substituted chalcones as therapeutic agents |
| GB0123780D0 (en) | 2001-10-03 | 2001-11-21 | Cancer Res Ventures Ltd | Substituted chalcones as therapeutic agents |
| US6919324B2 (en) * | 2001-10-26 | 2005-07-19 | Oxigene, Inc. | Functionalized stilbene derivatives as improved vascular targeting agents |
| GB0126889D0 (en) * | 2001-11-08 | 2002-01-02 | Paterson Inst For Cancer Res | Compounds and their uses |
| AU2003250701A1 (en) * | 2002-07-31 | 2004-02-16 | Wayne R. Danter | Protein tyrosine kinase inhibitors |
| ES2298563T3 (es) * | 2002-10-09 | 2008-05-16 | Critical Outcome Technologies, Inc. | Inhibidores de proteinas tirosina cinasas. |
| CN1744892A (zh) * | 2003-02-04 | 2006-03-08 | 株式会社益力多本社 | 乳癌耐性蛋白(bcrp)抑制剂 |
| US7598419B2 (en) * | 2004-03-26 | 2009-10-06 | Hsc Research And Development Limited Partnership | Compounds for modulating cell proliferation |
| EA014555B1 (ru) | 2005-03-30 | 2010-12-30 | Кабусики Кайся Якулт Хонса | Ингибитор bcrp/abcg2 |
| US8034815B2 (en) | 2007-01-11 | 2011-10-11 | Critical Outcome Technologies, Inc. | Compounds and method for treatment of cancer |
| US7784455B1 (en) * | 2007-09-18 | 2010-08-31 | Chong Carlton Le Loong | Reusable pellet shooting grenade |
| EP2225226B1 (en) | 2007-12-26 | 2016-08-17 | Critical Outcome Technologies, Inc. | Compounds and their use in a method for treatment of cancer |
| GB0803071D0 (en) * | 2008-02-20 | 2008-03-26 | Care Technologies Inc | Cancer detection methods and techniques |
| CA2730890C (en) | 2008-07-17 | 2018-05-15 | Critical Outcome Technologies Inc. | Thiosemicarbazone inhibitor compounds and cancer treatment methods |
| GB0907551D0 (en) | 2009-05-01 | 2009-06-10 | Univ Dundee | Treatment or prophylaxis of proliferative conditions |
| EP3235818A3 (en) | 2010-04-01 | 2018-03-14 | Critical Outcome Technologies, Inc. | Compounds for the treatment of hiv |
| CA3091027A1 (en) | 2018-02-02 | 2019-08-08 | Maverix Oncology, Inc. | Small molecule drug conjugates of gemcitabine monophosphate |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6176433A (ja) * | 1984-09-21 | 1986-04-18 | Toyobo Co Ltd | 新規なカルコン誘導体 |
| US5773435A (en) | 1987-08-04 | 1998-06-30 | Bristol-Myers Squibb Company | Prodrugs for β-lactamase and uses thereof |
| AU632992B2 (en) * | 1987-12-24 | 1993-01-21 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Pharmaceutical compositions comprising benzylidene- and cinnamylidene-malononitrile derivatives for the inhibition of proliferative processes in mammalian cells, certain such novel compounds and their preparation |
| US5287386A (en) | 1991-03-27 | 1994-02-15 | Thinking Machines Corporation | Differential driver/receiver circuit |
| US5430062A (en) * | 1992-05-21 | 1995-07-04 | Research Corporation Technologies, Inc. | Stilbene derivatives as anticancer agents |
| DE4236237A1 (de) | 1992-10-27 | 1994-04-28 | Behringwerke Ag | Prodrugs, ihre Herstellung und Verwendung als Arzneimittel |
| DE4309344A1 (de) | 1993-03-23 | 1994-09-29 | Gerhard Prof Dr Eisenbrand | Antineoplastische Mittel mit verstärkter Wirksamkeit |
| US5276058A (en) * | 1993-06-09 | 1994-01-04 | Nippon Hypox Laboratories Incorporated | 3,4-dihydroxychalcone derivatives |
| EP0647450A1 (en) | 1993-09-09 | 1995-04-12 | BEHRINGWERKE Aktiengesellschaft | Improved prodrugs for enzyme mediated activation |
| FR2710798B1 (fr) | 1993-09-27 | 1995-11-10 | Alcatel Mobile Comm France | Chaîne d'amplification en mode de courant, amplificateur opérationnel, cellule de gain et élément d'amplification correspondants. |
| JPH08188546A (ja) * | 1995-01-04 | 1996-07-23 | Kyowa Hakko Kogyo Co Ltd | カルコン誘導体 |
| GB9519490D0 (en) | 1995-09-25 | 1995-11-29 | Melvin William T | Use of a cytochrome P450 enzyme in tumour cells as a marker and target |
| US5966032A (en) | 1996-09-27 | 1999-10-12 | Northern Telecom Limited | BiCMOS transceiver (driver and receiver) for gigahertz operation |
| GB9802522D0 (en) | 1998-02-06 | 1998-04-01 | Montford University De | Hydroxylation activated prodrugs |
| DE69918950T2 (de) | 1998-02-06 | 2005-07-28 | De Montfort University | Durch hydroxylierung aktivierte medikamentvorstufen |
| DE69909073T2 (de) | 1998-02-12 | 2004-05-19 | De Montfort University | Durch hydroxylierung aktivierte wirkstofffreigabe |
| GB2334256A (en) | 1998-02-12 | 1999-08-18 | Univ Montfort | Hydroxylation activated prodrugs |
-
1999
- 1999-02-02 DE DE69918950T patent/DE69918950T2/de not_active Expired - Lifetime
- 1999-02-02 AU AU21738/99A patent/AU2173899A/en not_active Abandoned
- 1999-02-02 CA CA2319836A patent/CA2319836C/en not_active Expired - Fee Related
- 1999-02-02 WO PCT/GB1999/000155 patent/WO1999040056A1/en active IP Right Grant
- 1999-02-02 ES ES99901732T patent/ES2226332T3/es not_active Expired - Lifetime
- 1999-02-02 AT AT99901732T patent/ATE272040T1/de active
- 1999-02-02 EP EP99901732A patent/EP1051383B1/en not_active Expired - Lifetime
- 1999-02-02 JP JP2000530488A patent/JP4642226B2/ja not_active Expired - Fee Related
-
2000
- 2000-08-07 US US09/633,699 patent/US6677383B1/en not_active Expired - Lifetime
-
2001
- 2001-01-19 US US09/765,861 patent/US6346550B2/en not_active Expired - Lifetime
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