JP2002535010A5 - - Google Patents
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- JP2002535010A5 JP2002535010A5 JP2000596173A JP2000596173A JP2002535010A5 JP 2002535010 A5 JP2002535010 A5 JP 2002535010A5 JP 2000596173 A JP2000596173 A JP 2000596173A JP 2000596173 A JP2000596173 A JP 2000596173A JP 2002535010 A5 JP2002535010 A5 JP 2002535010A5
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- JP
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- compound
- formula
- enzyme
- assay
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- 150000001875 compounds Chemical class 0.000 description 12
- 238000004166 bioassay Methods 0.000 description 5
- 102000004190 Enzymes Human genes 0.000 description 4
- 108090000790 Enzymes Proteins 0.000 description 4
- 230000002401 inhibitory effect Effects 0.000 description 3
- 238000006900 dealkylation reaction Methods 0.000 description 2
- 102100004057 CYP3A4 Human genes 0.000 description 1
- 101710007540 CYP3A4 Proteins 0.000 description 1
- YZTJYBJCZXZGCT-UHFFFAOYSA-N Phenylpiperazine Chemical compound C1CNCCN1C1=CC=CC=C1 YZTJYBJCZXZGCT-UHFFFAOYSA-N 0.000 description 1
- 230000005284 excitation Effects 0.000 description 1
- 238000001917 fluorescence detection Methods 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 238000000034 method Methods 0.000 description 1
Description
【特許請求の範囲】
【請求項１】 酵素ＣＹＰ３Ａ４のインヒビターを試験するためのアッセイであって、該酵素および式(Ｉ):
【化１】
の化合物を試験化合物と接触させ、該酵素による式(Ｉ)の化合物のＯ-脱アルキル化の阻害を測定することから成るアッセイ。
【請求項２】 酵素による式(Ｉ)の化合物のＯ-脱アルキル化の阻害を、式(ＩＩ):
【化２】
の化合物を定量することにより測定する請求項１記載のアッセイ。
【請求項３】 式(ＩＩ)の化合物を蛍光検出により定量する請求項２記載のアッセイ。
【請求項４】 式(ＩＩ)の化合物を、５３０ｎｍの励起波長および５９０ｎｍの放出波長を走査することにより定量する請求項３記載のアッセイ。
【請求項５】 請求項１に定義する式(Ｉ)の化合物。
【請求項６】 請求項１に定義する式(Ｉ)の化合物の製造法であって、式(ＩＩＩ):
【化３】
(式中、Ｌは脱離基である)
の化合物の、１-フェニルピペラジンとの反応を含む方法。
【請求項１】 酵素ＣＹＰ３Ａ４のインヒビターを試験するためのアッセイであって、該酵素および式(Ｉ):
【化１】
【請求項２】 酵素による式(Ｉ)の化合物のＯ-脱アルキル化の阻害を、式(ＩＩ):
【化２】
【請求項３】 式(ＩＩ)の化合物を蛍光検出により定量する請求項２記載のアッセイ。
【請求項４】 式(ＩＩ)の化合物を、５３０ｎｍの励起波長および５９０ｎｍの放出波長を走査することにより定量する請求項３記載のアッセイ。
【請求項５】 請求項１に定義する式(Ｉ)の化合物。
【請求項６】 請求項１に定義する式(Ｉ)の化合物の製造法であって、式(ＩＩＩ):
【化３】
の化合物の、１-フェニルピペラジンとの反応を含む方法。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB9902068.7 | 1999-01-29 | ||
| GBGB9902068.7A GB9902068D0 (en) | 1999-01-29 | 1999-01-29 | Compounds |
| PCT/EP2000/000297 WO2000044933A1 (en) | 1999-01-29 | 2000-01-13 | Resorufin derivatives as substrates for cyp3a4 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2002535010A JP2002535010A (ja) | 2002-10-22 |
| JP2002535010A5 true JP2002535010A5 (ja) | 2007-04-12 |
| JP4422346B2 JP4422346B2 (ja) | 2010-02-24 |
Family
ID=10846789
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000596173A Expired - Fee Related JP4422346B2 (ja) | 1999-01-29 | 2000-01-13 | Ｃｙｐ３ａ４の基質としてのレゾルフィン誘導体 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US6762034B1 (ja) |
| EP (1) | EP1147216B1 (ja) |
| JP (1) | JP4422346B2 (ja) |
| AT (1) | ATE275637T1 (ja) |
| DE (1) | DE60013554T2 (ja) |
| ES (1) | ES2228457T3 (ja) |
| GB (1) | GB9902068D0 (ja) |
| WO (1) | WO2000044933A1 (ja) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7056654B2 (en) * | 1999-12-13 | 2006-06-06 | Smithkline Beecham Corporation | Screening assay for inhibitors of human cytochrome P-450 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3526565A1 (de) * | 1985-07-25 | 1987-02-05 | Boehringer Mannheim Gmbh | Resorufin-derivate, verfahren zu deren herstellung sowie deren verwendung in fluoreszenzimmunoassays |
| US6143492A (en) * | 1998-12-14 | 2000-11-07 | Aurora Biosciences Corporation | Optical molecular sensors for cytochrome P450 activity |
-
1999
- 1999-01-29 GB GBGB9902068.7A patent/GB9902068D0/en not_active Ceased
-
2000
- 2000-01-13 EP EP00903581A patent/EP1147216B1/en not_active Expired - Lifetime
- 2000-01-13 DE DE60013554T patent/DE60013554T2/de not_active Expired - Lifetime
- 2000-01-13 JP JP2000596173A patent/JP4422346B2/ja not_active Expired - Fee Related
- 2000-01-13 ES ES00903581T patent/ES2228457T3/es not_active Expired - Lifetime
- 2000-01-13 WO PCT/EP2000/000297 patent/WO2000044933A1/en active IP Right Grant
- 2000-01-13 US US09/890,009 patent/US6762034B1/en not_active Expired - Fee Related
- 2000-01-13 AT AT00903581T patent/ATE275637T1/de not_active IP Right Cessation
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