JP2006524487A5 - - Google Patents
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- JP2006524487A5 JP2006524487A5 JP2004571244A JP2004571244A JP2006524487A5 JP 2006524487 A5 JP2006524487 A5 JP 2006524487A5 JP 2004571244 A JP2004571244 A JP 2004571244A JP 2004571244 A JP2004571244 A JP 2004571244A JP 2006524487 A5 JP2006524487 A5 JP 2006524487A5
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- JP
- Japan
- Prior art keywords
- candidate compound
- compound
- metabolite
- candidate
- group
- 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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- 150000001875 compounds Chemical class 0.000 claims 97
- 238000000034 method Methods 0.000 claims 44
- 239000002207 metabolite Substances 0.000 claims 24
- ABLZXFCXXLZCGV-UHFFFAOYSA-N Phosphorous acid Chemical group OP(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 claims 15
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 14
- 239000000651 prodrug Substances 0.000 claims 10
- 229940002612 prodrug Drugs 0.000 claims 10
- -1 amino acid phosphonoamidate Chemical class 0.000 claims 7
- 150000001413 amino acids Chemical class 0.000 claims 7
- 230000036436 anti-hiv Effects 0.000 claims 6
- 230000000694 effects Effects 0.000 claims 6
- 230000003834 intracellular effect Effects 0.000 claims 6
- 210000003819 peripheral blood mononuclear cell Anatomy 0.000 claims 6
- 239000002253 acid Substances 0.000 claims 5
- 230000007062 hydrolysis Effects 0.000 claims 5
- 238000006460 hydrolysis reaction Methods 0.000 claims 5
- 108090000604 Hydrolases Proteins 0.000 claims 4
- 102000004157 Hydrolases Human genes 0.000 claims 4
- 125000002843 carboxylic acid group Chemical group 0.000 claims 4
- 210000003563 lymphoid tissue Anatomy 0.000 claims 4
- 210000001519 tissue Anatomy 0.000 claims 3
- 108010051152 Carboxylesterase Proteins 0.000 claims 2
- 102000013392 Carboxylesterase Human genes 0.000 claims 2
- 108010010369 HIV Protease Proteins 0.000 claims 2
- 108010058834 acylcarnitine hydrolase Proteins 0.000 claims 2
- 125000000539 amino acid group Chemical group 0.000 claims 2
- 125000003277 amino group Chemical group 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 230000000058 esterolytic effect Effects 0.000 claims 2
- 210000002443 helper t lymphocyte Anatomy 0.000 claims 2
- 210000001165 lymph node Anatomy 0.000 claims 2
- 239000002777 nucleoside Substances 0.000 claims 2
- 150000003833 nucleoside derivatives Chemical class 0.000 claims 2
- 230000002688 persistence Effects 0.000 claims 2
- 125000004437 phosphorous atom Chemical group 0.000 claims 2
- 229910052698 phosphorus Inorganic materials 0.000 claims 2
- 108010002459 HIV Integrase Proteins 0.000 claims 1
- 108010078851 HIV Reverse Transcriptase Proteins 0.000 claims 1
- 108091005804 Peptidases Proteins 0.000 claims 1
- 239000004365 Protease Substances 0.000 claims 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 claims 1
- 150000001733 carboxylic acid esters Chemical class 0.000 claims 1
- 238000004113 cell culture Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 238000000099 in vitro assay Methods 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- VGKONPUVOVVNSU-UHFFFAOYSA-N naphthalen-1-yl acetate Chemical compound C1=CC=C2C(OC(=O)C)=CC=CC2=C1 VGKONPUVOVVNSU-UHFFFAOYSA-N 0.000 claims 1
- 150000007524 organic acids Chemical class 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- UEZVMMHDMIWARA-UHFFFAOYSA-M phosphonate Chemical compound [O-]P(=O)=O UEZVMMHDMIWARA-UHFFFAOYSA-M 0.000 claims 1
- 238000012216 screening Methods 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
Applications Claiming Priority (8)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US37562202P | 2002-04-26 | 2002-04-26 | |
| US37577902P | 2002-04-26 | 2002-04-26 | |
| US37583402P | 2002-04-26 | 2002-04-26 | |
| US37566502P | 2002-04-26 | 2002-04-26 | |
| PCT/US2003/012901 WO2003090690A2 (en) | 2002-04-26 | 2003-04-25 | Cellular accumulation of phosphonate analogs of hiv protease inhibitor compounds and the compounds as such |
| PCT/US2003/012926 WO2003091264A2 (en) | 2002-04-26 | 2003-04-25 | Non nucleoside reverse transcriptase inhibitors |
| PCT/US2003/012943 WO2003090691A2 (en) | 2002-04-26 | 2003-04-25 | Method and compositions for identifying anti-hiv therapeutic compounds |
| PCT/EP2003/012423 WO2004096818A2 (en) | 2002-04-26 | 2003-11-06 | Method and compositions for identifying anti-hiv therapeutic compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006524487A JP2006524487A (ja) | 2006-11-02 |
| JP2006524487A5 true JP2006524487A5 (https=) | 2006-12-28 |
Family
ID=29273807
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003587329A Expired - Lifetime JP4942915B2 (ja) | 2002-04-26 | 2003-04-25 | Hivプロテアーゼ阻害剤化合物のホスホネートアナログの細胞蓄積 |
| JP2003587330A Pending JP2006508634A (ja) | 2002-04-26 | 2003-04-25 | 抗hiv治療化合物を同定するための方法および組成物 |
| JP2003587822A Pending JP2005523922A (ja) | 2002-04-26 | 2003-04-25 | 非ヌクレオシド逆転写酵素阻害剤 |
| JP2004571244A Pending JP2006524487A (ja) | 2002-04-26 | 2003-11-06 | 抗hiv治療化合物を同定するための方法および組成物 |
| JP2009052719A Pending JP2009112319A (ja) | 2002-04-26 | 2009-03-05 | 抗hiv治療化合物を同定するための方法および組成物 |
Family Applications Before (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003587329A Expired - Lifetime JP4942915B2 (ja) | 2002-04-26 | 2003-04-25 | Hivプロテアーゼ阻害剤化合物のホスホネートアナログの細胞蓄積 |
| JP2003587330A Pending JP2006508634A (ja) | 2002-04-26 | 2003-04-25 | 抗hiv治療化合物を同定するための方法および組成物 |
| JP2003587822A Pending JP2005523922A (ja) | 2002-04-26 | 2003-04-25 | 非ヌクレオシド逆転写酵素阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009052719A Pending JP2009112319A (ja) | 2002-04-26 | 2009-03-05 | 抗hiv治療化合物を同定するための方法および組成物 |
Country Status (27)
| Country | Link |
|---|---|
| US (7) | US20070010489A1 (https=) |
| EP (4) | EP1575486A4 (https=) |
| JP (5) | JP4942915B2 (https=) |
| KR (2) | KR20040108756A (https=) |
| CN (4) | CN101074242A (https=) |
| AT (1) | ATE367394T1 (https=) |
| AU (4) | AU2003231765B9 (https=) |
| BR (2) | BR0309557A (https=) |
| CA (3) | CA2481449A1 (https=) |
| CY (1) | CY1108036T1 (https=) |
| DE (1) | DE60315023T2 (https=) |
| DK (1) | DK1509537T3 (https=) |
| EA (2) | EA008775B1 (https=) |
| ES (1) | ES2290485T3 (https=) |
| HR (2) | HRP20041114A2 (https=) |
| IL (2) | IL164491A0 (https=) |
| IS (2) | IS2714B (https=) |
| MX (2) | MXPA04010527A (https=) |
| NO (2) | NO20045152L (https=) |
| NZ (1) | NZ535828A (https=) |
| PL (2) | PL211979B1 (https=) |
| PT (1) | PT1509537E (https=) |
| SI (1) | SI1509537T1 (https=) |
| TW (2) | TW200408645A (https=) |
| UA (1) | UA80819C2 (https=) |
| WO (4) | WO2003091264A2 (https=) |
| ZA (2) | ZA200409376B (https=) |
Families Citing this family (131)
| Publication number | Priority date | Publication date | Assignee | Title |
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| NO20045680L (no) | Bakterietransformerende middel |