JP2002519355A5 - - Google Patents
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- Publication number
- JP2002519355A5 JP2002519355A5 JP2000557262A JP2000557262A JP2002519355A5 JP 2002519355 A5 JP2002519355 A5 JP 2002519355A5 JP 2000557262 A JP2000557262 A JP 2000557262A JP 2000557262 A JP2000557262 A JP 2000557262A JP 2002519355 A5 JP2002519355 A5 JP 2002519355A5
- Authority
- JP
- Japan
- Prior art keywords
- following formula
- embedded image
- cycloalkyl
- hiv
- alkyl
- 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
- 230000002401 inhibitory effect Effects 0.000 description 19
- 150000001875 compounds Chemical class 0.000 description 18
- 229910052739 hydrogen Inorganic materials 0.000 description 16
- 239000001257 hydrogen Substances 0.000 description 16
- 150000002431 hydrogen Chemical class 0.000 description 16
- 125000000217 alkyl group Chemical group 0.000 description 12
- 125000000753 cycloalkyl group Chemical group 0.000 description 12
- 230000010076 replication Effects 0.000 description 9
- KDCGOANMDULRCW-UHFFFAOYSA-N 7H-purine Chemical compound N1=CNC2=NC=NC2=C1 KDCGOANMDULRCW-UHFFFAOYSA-N 0.000 description 8
- 125000002252 acyl group Chemical group 0.000 description 8
- 125000003118 aryl group Chemical group 0.000 description 8
- 150000002148 esters Chemical class 0.000 description 8
- 125000005843 halogen group Chemical group 0.000 description 8
- 150000003839 salts Chemical class 0.000 description 7
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 6
- 125000001246 bromo group Chemical group Br* 0.000 description 6
- 125000006575 electron-withdrawing group Chemical group 0.000 description 6
- 229910052760 oxygen Inorganic materials 0.000 description 6
- 239000001301 oxygen Substances 0.000 description 6
- PMMYEEVYMWASQN-DMTCNVIQSA-N Hydroxyproline Chemical group O[C@H]1CN[C@H](C(O)=O)C1 PMMYEEVYMWASQN-DMTCNVIQSA-N 0.000 description 4
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 description 4
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 description 4
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 description 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 4
- ISAKRJDGNUQOIC-UHFFFAOYSA-N Uracil Chemical compound O=C1C=CNC(=O)N1 ISAKRJDGNUQOIC-UHFFFAOYSA-N 0.000 description 4
- 235000001014 amino acid Nutrition 0.000 description 4
- 150000001413 amino acids Chemical class 0.000 description 4
- 150000001540 azides Chemical class 0.000 description 4
- OPTASPLRGRRNAP-UHFFFAOYSA-N cytosine Chemical compound NC=1C=CNC(=O)N=1 OPTASPLRGRRNAP-UHFFFAOYSA-N 0.000 description 4
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 4
- 229910052717 sulfur Inorganic materials 0.000 description 4
- 239000011593 sulfur Substances 0.000 description 4
- RWQNBRDOKXIBIV-UHFFFAOYSA-N thymine Chemical compound CC1=CNC(=O)NC1=O RWQNBRDOKXIBIV-UHFFFAOYSA-N 0.000 description 4
- 108010078851 HIV Reverse Transcriptase Proteins 0.000 description 3
- 125000000539 amino acid group Chemical group 0.000 description 3
- 239000003937 drug carrier Substances 0.000 description 3
- 239000002777 nucleoside Substances 0.000 description 3
- 150000003833 nucleoside derivatives Chemical class 0.000 description 3
- 241000282412 Homo Species 0.000 description 2
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 description 2
- QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 description 2
- QIVBCDIJIAJPQS-UHFFFAOYSA-N Tryptophan Natural products C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 description 2
- 235000004279 alanine Nutrition 0.000 description 2
- 125000004799 bromophenyl group Chemical group 0.000 description 2
- 229940104302 cytosine Drugs 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 229940113082 thymine Drugs 0.000 description 2
- 229940035893 uracil Drugs 0.000 description 2
- 0 CC(C(N1)=O)=CC(C2[C@@]3O[C@@](COP(*)(Oc4ccc(*)cc4)=O)C=C3)*2C1=O Chemical compound CC(C(N1)=O)=CC(C2[C@@]3O[C@@](COP(*)(Oc4ccc(*)cc4)=O)C=C3)*2C1=O 0.000 description 1
- 102100034343 Integrase Human genes 0.000 description 1
- 108010092799 RNA-directed DNA polymerase Proteins 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US09/107,716 US6030957A (en) | 1998-06-29 | 1998-06-29 | Aryl phosphate derivatives of d4T having anti-HIV activity |
| US09/107,716 | 1998-06-30 | ||
| PCT/US1999/014774 WO2000000501A1 (en) | 1998-06-29 | 1999-06-29 | ARYL PHOSPHATE DERIVATIVES OF d4T HAVING ANTI-HIV ACTIVITY |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2002519355A JP2002519355A (ja) | 2002-07-02 |
| JP2002519355A5 true JP2002519355A5 (https=) | 2006-08-31 |
Family
ID=22318071
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000557262A Pending JP2002519355A (ja) | 1998-06-29 | 1999-06-29 | 抗ＨＩＶ活性を有するｄ４Ｔのアリールフォスフェート誘導体 |
Country Status (14)
| Country | Link |
|---|---|
| US (7) | US6030957A (https=) |
| EP (1) | EP1090018B1 (https=) |
| JP (1) | JP2002519355A (https=) |
| KR (1) | KR20010071673A (https=) |
| CN (1) | CN1314909A (https=) |
| AT (1) | ATE277940T1 (https=) |
| AU (1) | AU4846999A (https=) |
| BR (1) | BR9911685A (https=) |
| CA (1) | CA2336285A1 (https=) |
| DE (1) | DE69920696T2 (https=) |
| HU (1) | HUP0102527A3 (https=) |
| IL (1) | IL140388A0 (https=) |
| NO (1) | NO20006685L (https=) |
| WO (1) | WO2000000501A1 (https=) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6030957A (en) * | 1998-06-29 | 2000-02-29 | Wayne Hughes Institute | Aryl phosphate derivatives of d4T having anti-HIV activity |
| US7144874B2 (en) * | 2002-10-25 | 2006-12-05 | Parker Hughes Institute | Aryl phosphate derivatives of d4T having activity against resistant HIV strains |
| US20070015733A1 (en) * | 1998-06-29 | 2007-01-18 | Parker Hughes Institute | Aryl Phosphate Derivatives of d4T having Activity Against Resistant HIV Strains |
| AU3897800A (en) * | 1999-03-19 | 2000-10-09 | Parker Hughes Institute | One pot synthesis of 5'-hydroxy phosphorylated nucleoside derivatives, and compounds formed thereby |
| US6825177B2 (en) * | 2000-10-30 | 2004-11-30 | Parker Hughes Institute | Aryl phosphate derivatives of d4T with potent anti-viral activity |
| DK1334108T3 (da) * | 2000-11-13 | 2005-07-11 | Parker Hughes Inst | Arylfosfatderivater af d4T |
| CA2487419A1 (en) * | 2002-05-28 | 2003-12-04 | Regents Of The University Of Minnesota | Crisp polypeptides as contraceptives and inhibitors of sperm capacitation |
| US20030236218A1 (en) * | 2002-06-12 | 2003-12-25 | Uckun Fatih M. | Aryl phosphate derivatives of d4T with selective activity against adenovirus and HIV |
| US20040076931A1 (en) * | 2002-10-18 | 2004-04-22 | Cashflow Technologies, Inc. | Educational interactive games |
| US20040077607A1 (en) * | 2002-10-21 | 2004-04-22 | Uckun Fatih M. | Aryl phosphate derivatives of d4T with potent anti-viral activity against hemorrhagic fever viruses |
| GB0401088D0 (en) | 2004-01-19 | 2004-02-18 | Univ Cardiff | Phosphoramidate derivatives |
| EP1773355B1 (en) * | 2004-06-24 | 2014-06-25 | Merck Sharp & Dohme Corp. | Nucleoside aryl phosphoramidates for the treatment of rna-dependent rna viral infection |
| WO2006026656A1 (en) * | 2004-08-31 | 2006-03-09 | Parker Hughes Institute | Cytotoxic nucleoside analog compound 003 for treating cancer |
| CA2589935A1 (en) | 2004-12-09 | 2006-06-15 | Regents Of The University Of Minnesota | Nucleosides with antiviral and anticancer activity |
| EP1866064A4 (en) * | 2005-03-09 | 2009-08-19 | Univ California | NANOCOMPOSITE MEMBRANES AND METHOD FOR THE PRODUCTION AND USE THEREOF |
| US7892618B2 (en) * | 2005-03-21 | 2011-02-22 | Sony Corporation | Deterring theft of optical media |
| GB0623493D0 (en) * | 2006-11-24 | 2007-01-03 | Univ Cardiff | Chemical compounds |
| AU2010226466A1 (en) * | 2009-03-20 | 2011-10-20 | Alios Biopharma, Inc. | Substituted nucleoside and nucleotide analogs |
| BR112013005872A2 (pt) | 2010-09-22 | 2019-09-24 | Alios Biopharma Inc | compostos, composição farmacêutica e respectivos usos |
| US9095599B2 (en) | 2011-01-03 | 2015-08-04 | Nanjing Molecular Research, Inc. | O-(substituted benzyl) phosphoramidate compounds and therapeutic use |
| EP2794630A4 (en) | 2011-12-22 | 2015-04-01 | Alios Biopharma Inc | SUBSTITUTED PHOSPHORTHIOAT NUCLEOTIDE ANALOGUE |
| WO2013142124A1 (en) | 2012-03-21 | 2013-09-26 | Vertex Pharmaceuticals Incorporated | Solid forms of a thiophosphoramidate nucleotide prodrug |
| US9012427B2 (en) | 2012-03-22 | 2015-04-21 | Alios Biopharma, Inc. | Pharmaceutical combinations comprising a thionucleotide analog |
| AU2014250762A1 (en) | 2013-04-12 | 2015-10-29 | Achillion Pharmaceuticals, Inc. | Highly active nucleoside derivative for the treatment of HCV |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4707362A (en) | 1985-02-15 | 1987-11-17 | Biotek, Inc. | Sustained release composition |
| US4841039A (en) | 1986-05-01 | 1989-06-20 | Emory University | 2',3'-dideoxy-5-substituted uridines and related compounds as antiviral agents |
| US4983393A (en) | 1987-07-21 | 1991-01-08 | Maximed Corporation | Intra-vaginal device and method for sustained drug release |
| JPH06189998A (ja) | 1992-11-06 | 1994-07-12 | C & Co:Yugen | コンド―ム |
| AU5691094A (en) | 1992-12-18 | 1994-07-19 | University Of Alberta, The | Dihydropyrimidine nucleosides with antiviral properties |
| ZA947572B (en) | 1993-09-29 | 1995-09-28 | Hampton Roads Medical College | Contraceptive compositions |
| US5672698A (en) * | 1993-11-15 | 1997-09-30 | Bristol-Myers Squibb Co. | Preparation of 2',3'-didehydro-3'-deoxythymidine from 5-methyluridine |
| US5659023A (en) * | 1995-02-01 | 1997-08-19 | Gilead Sciences, Inc. | Nucleotide analogues |
| GB9505025D0 (en) * | 1995-03-13 | 1995-05-03 | Medical Res Council | Chemical compounds |
| AP1406A (en) | 1996-05-09 | 2005-05-04 | Infectio Recherche Inc | Formulations for use in the prevention of pathogen induced diseases including HIV and HSV. |
| US6030957A (en) * | 1998-06-29 | 2000-02-29 | Wayne Hughes Institute | Aryl phosphate derivatives of d4T having anti-HIV activity |
-
1998
- 1998-06-29 US US09/107,716 patent/US6030957A/en not_active Expired - Fee Related
-
1999
- 1999-06-29 AU AU48469/99A patent/AU4846999A/en not_active Abandoned
- 1999-06-29 EP EP99932080A patent/EP1090018B1/en not_active Expired - Lifetime
- 1999-06-29 KR KR1020007014949A patent/KR20010071673A/ko not_active Withdrawn
- 1999-06-29 CN CN99810072A patent/CN1314909A/zh active Pending
- 1999-06-29 JP JP2000557262A patent/JP2002519355A/ja active Pending
- 1999-06-29 AT AT99932080T patent/ATE277940T1/de not_active IP Right Cessation
- 1999-06-29 BR BR9911685-5A patent/BR9911685A/pt not_active Application Discontinuation
- 1999-06-29 WO PCT/US1999/014774 patent/WO2000000501A1/en not_active Ceased
- 1999-06-29 HU HU0102527A patent/HUP0102527A3/hu unknown
- 1999-06-29 IL IL14038899A patent/IL140388A0/xx unknown
- 1999-06-29 DE DE69920696T patent/DE69920696T2/de not_active Expired - Fee Related
- 1999-06-29 CA CA002336285A patent/CA2336285A1/en not_active Abandoned
- 1999-11-29 US US09/450,082 patent/US6503890B1/en not_active Expired - Fee Related
- 1999-12-15 US US09/464,516 patent/US6350736B1/en not_active Expired - Fee Related
-
2000
- 2000-04-13 US US09/548,494 patent/US6670336B1/en not_active Expired - Fee Related
- 2000-04-13 US US09/548,492 patent/US6528495B1/en not_active Expired - Fee Related
- 2000-04-13 US US09/548,496 patent/US6537975B1/en not_active Expired - Fee Related
- 2000-12-28 NO NO20006685A patent/NO20006685L/no not_active Application Discontinuation
-
2003
- 2003-12-01 US US10/726,073 patent/US7071176B2/en not_active Expired - Fee Related
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