JP2007515184A5 - - Google Patents
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- JP2007515184A5 JP2007515184A5 JP2006547281A JP2006547281A JP2007515184A5 JP 2007515184 A5 JP2007515184 A5 JP 2007515184A5 JP 2006547281 A JP2006547281 A JP 2006547281A JP 2006547281 A JP2006547281 A JP 2006547281A JP 2007515184 A5 JP2007515184 A5 JP 2007515184A5
- Authority
- JP
- Japan
- Prior art keywords
- candidate compound
- compound
- determining
- metabolic
- candidate
- 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 277
- 238000000034 method Methods 0.000 claims 209
- 230000002503 metabolic effect Effects 0.000 claims 67
- UEZVMMHDMIWARA-UHFFFAOYSA-M phosphonate Chemical compound [O-]P(=O)=O UEZVMMHDMIWARA-UHFFFAOYSA-M 0.000 claims 46
- 229940124158 Protease/peptidase inhibitor Drugs 0.000 claims 40
- 230000003834 intracellular effect Effects 0.000 claims 40
- 239000000137 peptide hydrolase inhibitor Substances 0.000 claims 40
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 26
- 230000036436 anti-hiv Effects 0.000 claims 21
- 210000003819 peripheral blood mononuclear cell Anatomy 0.000 claims 20
- 150000001413 amino acids Chemical class 0.000 claims 19
- 210000004027 cell Anatomy 0.000 claims 19
- 102000004157 Hydrolases Human genes 0.000 claims 18
- 108090000604 Hydrolases Proteins 0.000 claims 18
- ABLZXFCXXLZCGV-UHFFFAOYSA-N Phosphorous acid Chemical group OP(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 claims 18
- 239000002207 metabolite Substances 0.000 claims 17
- 230000002688 persistence Effects 0.000 claims 16
- 230000000694 effects Effects 0.000 claims 15
- 210000003563 lymphoid tissue Anatomy 0.000 claims 15
- 210000001519 tissue Anatomy 0.000 claims 14
- 210000002443 helper t lymphocyte Anatomy 0.000 claims 13
- 230000007062 hydrolysis Effects 0.000 claims 13
- 238000006460 hydrolysis reaction Methods 0.000 claims 13
- 210000001165 lymph node Anatomy 0.000 claims 13
- -1 amino acid phosphonoamidate Chemical class 0.000 claims 10
- 239000000651 prodrug Substances 0.000 claims 10
- 229940002612 prodrug Drugs 0.000 claims 10
- 108010010369 HIV Protease Proteins 0.000 claims 8
- 239000002777 nucleoside Substances 0.000 claims 8
- 150000003833 nucleoside derivatives Chemical class 0.000 claims 8
- 239000002253 acid Substances 0.000 claims 7
- 125000000539 amino acid group Chemical group 0.000 claims 5
- 125000003277 amino group Chemical group 0.000 claims 5
- 238000004113 cell culture Methods 0.000 claims 5
- 239000002726 nonnucleoside reverse transcriptase inhibitor Substances 0.000 claims 5
- 108010002459 HIV Integrase Proteins 0.000 claims 4
- 108010078851 HIV Reverse Transcriptase Proteins 0.000 claims 4
- BVMWIXWOIGJRGE-UHFFFAOYSA-N NP(O)=O Chemical compound NP(O)=O BVMWIXWOIGJRGE-UHFFFAOYSA-N 0.000 claims 4
- 108091005804 Peptidases Proteins 0.000 claims 4
- 239000004365 Protease Substances 0.000 claims 4
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 claims 4
- 125000003275 alpha amino acid group Chemical group 0.000 claims 4
- 125000002843 carboxylic acid group Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 230000000058 esterolytic effect Effects 0.000 claims 4
- 238000000338 in vitro Methods 0.000 claims 4
- 230000002401 inhibitory effect Effects 0.000 claims 4
- 238000012216 screening Methods 0.000 claims 4
- 238000006467 substitution reaction Methods 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- 230000001225 therapeutic effect Effects 0.000 claims 4
- 108010051152 Carboxylesterase Proteins 0.000 claims 2
- 102000013392 Carboxylesterase Human genes 0.000 claims 2
- 108010058834 acylcarnitine hydrolase Proteins 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 125000004437 phosphorous atom Chemical group 0.000 claims 2
- 229910052698 phosphorus Inorganic materials 0.000 claims 2
- 150000001733 carboxylic acid esters Chemical class 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000000099 in vitro assay Methods 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
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10/740,694 US20050239054A1 (en) | 2002-04-26 | 2003-12-22 | Method and compositions for identifying anti-HIV therapeutic compounds |
| PCT/US2004/042991 WO2005064008A1 (en) | 2003-12-22 | 2004-12-22 | Method and compositions for identifying anti-hiv therapeutic compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007515184A JP2007515184A (ja) | 2007-06-14 |
| JP2007515184A5 true JP2007515184A5 (https=) | 2008-02-14 |
Family
ID=34739022
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006547281A Withdrawn JP2007515184A (ja) | 2003-12-22 | 2004-12-22 | 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 (6)
| Country | Link |
|---|---|
| US (1) | US20050239054A1 (https=) |
| EP (1) | EP1711617A1 (https=) |
| JP (1) | JP2007515184A (https=) |
| AU (1) | AU2004309379A1 (https=) |
| CA (1) | CA2550730A1 (https=) |
| WO (1) | WO2005064008A1 (https=) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003231765B9 (en) * | 2002-04-26 | 2010-01-28 | Gilead Sciences, Inc. | Cellular accumulation of phosphonate analogs of HIV protease inhibitor compounds and the compounds as such |
| EP2359833A1 (en) | 2003-04-25 | 2011-08-24 | Gilead Sciences, Inc. | Antiviral phosphonate analogs |
| US7685737B2 (en) | 2004-07-19 | 2010-03-30 | Earthrenew, Inc. | Process and system for drying and heat treating materials |
| US7024800B2 (en) | 2004-07-19 | 2006-04-11 | Earthrenew, Inc. | Process and system for drying and heat treating materials |
| ME03423B (me) | 2004-07-27 | 2020-01-20 | Gilead Sciences Inc | Fosfonatni analozi jedinjenja hiv inhibitora |
| CA2599228C (en) * | 2005-01-27 | 2014-05-13 | Tibotec Pharmaceuticals Ltd. | Hiv inhibiting 2-( 4-cyanophenylamino) pyrimidine derivatives |
| US20110178092A1 (en) * | 2005-06-22 | 2011-07-21 | Akbar Ali | HIV-1 Protease Inhibitors |
| US7610692B2 (en) | 2006-01-18 | 2009-11-03 | Earthrenew, Inc. | Systems for prevention of HAP emissions and for efficient drying/dehydration processes |
| WO2007126812A2 (en) * | 2006-03-29 | 2007-11-08 | Gilead Sciences, Inc. | Process for preparation of hiv protease inhibitors |
| NZ573888A (en) | 2006-07-21 | 2012-02-24 | Gilead Sciences Inc | Aza-peptide protease inhibitors |
| WO2008076826A1 (en) * | 2006-12-13 | 2008-06-26 | Threshold Pharmaceuticals, Inc. | Pyrophosphoramide alkylators |
| CN101557706B (zh) * | 2006-12-14 | 2013-08-07 | 泰华制药工业有限公司 | 雷沙吉兰碱结晶固体 |
| CN101784532B (zh) * | 2007-06-29 | 2014-10-22 | 韩国化学研究院 | Hiv逆转录酶抑制剂 |
| KR20100041798A (ko) * | 2007-06-29 | 2010-04-22 | 한국화학연구원 | 신규 ｈｉｖ 역전사효소 억제제 |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| PT2300013T (pt) | 2008-05-21 | 2017-10-31 | Ariad Pharma Inc | Derivados de fósforo como inibidores de cinases |
| US8334409B2 (en) * | 2008-06-19 | 2012-12-18 | Teva Pharmaceutical Industries, Ltd. | Process for purifying rasagiline base |
| UA103329C2 (ru) | 2008-07-08 | 2013-10-10 | Гилиад Сайенсиз, Инк. | Соли соединений-ингибиторов вич |
| EP2304820A1 (en) * | 2008-07-18 | 2011-04-06 | Georgia Tech Research Corporation | Stable electrodes with modified work functions and methods for organic electronic devices |
| JP5699127B2 (ja) | 2009-04-06 | 2015-04-08 | ジョージア・テック・リサーチ・コーポレーション | 新規なホスホン酸表面改質剤を含む電子デバイス |
| US9834518B2 (en) | 2011-05-04 | 2017-12-05 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
| US20150166591A1 (en) | 2012-05-05 | 2015-06-18 | Ariad Pharmaceuticals, Inc. | Methods and compositions for raf kinase mediated diseases |
| SI3333173T1 (sl) | 2012-10-03 | 2019-08-30 | Gilead Sciences, Inc. | Postopki za pripravo analogov protivirusnega nukleotida |
| US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
| DK3236972T3 (en) | 2014-12-26 | 2021-10-04 | Univ Emory | Antivirale N4-hydroxycytidin-derivativer |
| CN107709288A (zh) * | 2016-02-03 | 2018-02-16 | 四川海思科制药有限公司 | 一种磷酰胺衍生物及制备方法和用途 |
| CN109305990B (zh) * | 2017-07-28 | 2021-02-26 | 四川海思科制药有限公司 | 一种磷酸衍生物及制备方法和用途 |
| SI3661937T1 (sl) | 2017-08-01 | 2021-11-30 | Gilead Sciences, Inc. | Kristalinične oblike etil((S)-((((2R,5R)-5-(6-amino-9H-purin-9-IL)-4- fluoro-2,5-dihidrofuran-2-IL)oksi)metil)(fenoksi)fosforil)-L-alaninata (GS-9131) za zdravljenje virusnih okužb |
| JP6804790B1 (ja) | 2017-12-07 | 2020-12-23 | エモリー ユニバーシティー | Ｎ４−ヒドロキシシチジンおよび誘導体ならびにそれらに関連する抗ウイルス用途 |
| JP2023539204A (ja) * | 2020-08-27 | 2023-09-13 | メルク・シャープ・アンド・ドーム・エルエルシー | 選択的細胞毒性薬としてのテトラヒドロキナゾリン誘導体 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5631370A (en) * | 1988-01-20 | 1997-05-20 | Regents Of The University Of Minnesota | Optically-active isomers of dideoxycarbocyclic nucleosides |
| US5177064A (en) * | 1990-07-13 | 1993-01-05 | University Of Florida | Targeted drug delivery via phosphonate derivatives |
| WO1995002582A1 (en) * | 1993-07-14 | 1995-01-26 | Ciba-Geigy Ag | Cyclic hydrazine compounds |
| US6067191A (en) * | 1993-11-23 | 2000-05-23 | Dofi Technologies | Technique for depth of field viewing of images using an aspherical lens |
| US5446137B1 (en) * | 1993-12-09 | 1998-10-06 | Behringwerke Ag | Oligonucleotides containing 4'-substituted nucleotides |
| US5750493A (en) * | 1995-08-30 | 1998-05-12 | Raymond F. Schinazi | Method to improve the biological and antiviral activity of protease inhibitors |
| US5914332A (en) * | 1995-12-13 | 1999-06-22 | Abbott Laboratories | Retroviral protease inhibiting compounds |
| US5874577A (en) * | 1996-04-03 | 1999-02-23 | Medichem Research, Inc. | Method for the preparing 9-12-(Diethoxyphosphonomethoxy)ethyl!adenine and analogues thereof |
| US6312662B1 (en) * | 1998-03-06 | 2001-11-06 | Metabasis Therapeutics, Inc. | Prodrugs phosphorus-containing compounds |
| US6258831B1 (en) * | 1999-03-31 | 2001-07-10 | The Procter & Gamble Company | Viral treatment |
| WO2001064693A1 (fr) * | 2000-02-29 | 2001-09-07 | Mitsubishi Pharma Corporation | Compose de nucleotide de phosphonate |
| CZ304734B6 (cs) * | 2000-07-21 | 2014-09-10 | Gilead Sciences, Inc. | Způsob přípravy 9-[2-(fosfonomethoxy)propyl]adeninu a 9-[2-(fosfonomethoxy)ethyl]adeninu |
| KR20020097384A (ko) * | 2001-06-20 | 2002-12-31 | 미쯔비시 도꾜 세이야꾸 가부시끼가이샤 | 기존의 약제에 내성변이를 가지는 바이러스에 유효한 약제 |
| AU2003231765B9 (en) * | 2002-04-26 | 2010-01-28 | Gilead Sciences, Inc. | Cellular accumulation of phosphonate analogs of HIV protease inhibitor compounds and the compounds as such |
-
2003
- 2003-12-22 US US10/740,694 patent/US20050239054A1/en not_active Abandoned
-
2004
- 2004-12-22 CA CA002550730A patent/CA2550730A1/en not_active Abandoned
- 2004-12-22 WO PCT/US2004/042991 patent/WO2005064008A1/en not_active Ceased
- 2004-12-22 AU AU2004309379A patent/AU2004309379A1/en not_active Abandoned
- 2004-12-22 EP EP04817046A patent/EP1711617A1/en not_active Withdrawn
- 2004-12-22 JP JP2006547281A patent/JP2007515184A/ja not_active Withdrawn
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