JP2005535564A5 - - Google Patents
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- Publication number
- JP2005535564A5 JP2005535564A5 JP2003570813A JP2003570813A JP2005535564A5 JP 2005535564 A5 JP2005535564 A5 JP 2005535564A5 JP 2003570813 A JP2003570813 A JP 2003570813A JP 2003570813 A JP2003570813 A JP 2003570813A JP 2005535564 A5 JP2005535564 A5 JP 2005535564A5
- Authority
- JP
- Japan
- Prior art keywords
- ester
- uridine
- alkyl
- deoxy
- aryl
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 58
- XCCTYIAWTASOJW-XVFCMESISA-N Uridine-5'-Diphosphate Chemical compound O[C@@H]1[C@H](O)[C@@H](COP(O)(=O)OP(O)(O)=O)O[C@H]1N1C(=O)NC(=O)C=C1 XCCTYIAWTASOJW-XVFCMESISA-N 0.000 claims 55
- 125000003118 aryl group Chemical group 0.000 claims 44
- 125000003710 aryl alkyl group Chemical group 0.000 claims 43
- 125000000753 cycloalkyl group Chemical group 0.000 claims 42
- 150000002148 esters Chemical class 0.000 claims 39
- 125000004430 oxygen atom Chemical group O* 0.000 claims 25
- 125000001424 substituent group Chemical group 0.000 claims 25
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 23
- 239000000203 mixture Substances 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 15
- 229910052799 carbon Inorganic materials 0.000 claims 14
- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- 150000001721 carbon Chemical group 0.000 claims 9
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 claims 9
- -1 2-deoxy-2-acetamidoglucosyl Chemical group 0.000 claims 8
- ZWIADYZPOWUWEW-XVFCMESISA-N CDP Chemical compound O=C1N=C(N)C=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](COP(O)(=O)OP(O)(O)=O)O1 ZWIADYZPOWUWEW-XVFCMESISA-N 0.000 claims 8
- DRTQHJPVMGBUCF-XVFCMESISA-N Uridine Chemical compound O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C=C1 DRTQHJPVMGBUCF-XVFCMESISA-N 0.000 claims 8
- 229910052760 oxygen Inorganic materials 0.000 claims 8
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 claims 7
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 7
- 125000000623 heterocyclic group Chemical group 0.000 claims 7
- 125000002092 orthoester group Chemical group 0.000 claims 7
- 125000005018 aryl alkenyl group Chemical group 0.000 claims 6
- 125000005015 aryl alkynyl group Chemical group 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 125000001054 5 membered carbocyclic group Chemical group 0.000 claims 4
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims 4
- AEMOLEFTQBMNLQ-AQKNRBDQSA-N D-glucopyranuronic acid Chemical compound OC1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O AEMOLEFTQBMNLQ-AQKNRBDQSA-N 0.000 claims 4
- DRTQHJPVMGBUCF-PSQAKQOGSA-N beta-L-uridine Natural products O[C@H]1[C@@H](O)[C@H](CO)O[C@@H]1N1C(=O)NC(=O)C=C1 DRTQHJPVMGBUCF-PSQAKQOGSA-N 0.000 claims 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 4
- 150000005676 cyclic carbonates Chemical class 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- DRTQHJPVMGBUCF-UHFFFAOYSA-N uracil arabinoside Natural products OC1C(O)C(CO)OC1N1C(=O)NC(=O)C=C1 DRTQHJPVMGBUCF-UHFFFAOYSA-N 0.000 claims 4
- 229940045145 uridine Drugs 0.000 claims 4
- UHDGCWIWMRVCDJ-UHFFFAOYSA-N 1-beta-D-Xylofuranosyl-NH-Cytosine Natural products O=C1N=C(N)C=CN1C1C(O)C(O)C(CO)O1 UHDGCWIWMRVCDJ-UHFFFAOYSA-N 0.000 claims 3
- UHDGCWIWMRVCDJ-PSQAKQOGSA-N Cytidine Natural products O=C1N=C(N)C=CN1[C@@H]1[C@@H](O)[C@@H](O)[C@H](CO)O1 UHDGCWIWMRVCDJ-PSQAKQOGSA-N 0.000 claims 3
- DHKHKXVYLBGOIT-UHFFFAOYSA-N acetaldehyde Diethyl Acetal Natural products CCOC(C)OCC DHKHKXVYLBGOIT-UHFFFAOYSA-N 0.000 claims 3
- UHDGCWIWMRVCDJ-ZAKLUEHWSA-N cytidine Chemical compound O=C1N=C(N)C=CN1[C@H]1[C@H](O)[C@@H](O)[C@H](CO)O1 UHDGCWIWMRVCDJ-ZAKLUEHWSA-N 0.000 claims 3
- 230000004410 intraocular pressure Effects 0.000 claims 3
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical class CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 2
- 229910019142 PO4 Inorganic materials 0.000 claims 2
- ISAKRJDGNUQOIC-UHFFFAOYSA-N Uracil Chemical group O=C1C=CNC(=O)N1 ISAKRJDGNUQOIC-UHFFFAOYSA-N 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 239000001177 diphosphate Substances 0.000 claims 2
- 235000011180 diphosphates Nutrition 0.000 claims 2
- 125000004494 ethyl ester group Chemical group 0.000 claims 2
- 239000013022 formulation composition Substances 0.000 claims 2
- 125000000625 hexosyl group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 2
- 239000010452 phosphate Substances 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 238000006467 substitution reaction Methods 0.000 claims 2
- GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 claims 1
- 125000000189 2-deoxyribosyl group Chemical group C1(C[C@H](O)[C@H](O1)CO)* 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 1
- 101150065749 Churc1 gene Proteins 0.000 claims 1
- AEMOLEFTQBMNLQ-VANFPWTGSA-N D-mannopyranuronic acid Chemical compound OC1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@@H]1O AEMOLEFTQBMNLQ-VANFPWTGSA-N 0.000 claims 1
- 125000000824 D-ribofuranosyl group Chemical group [H]OC([H])([H])[C@@]1([H])OC([H])(*)[C@]([H])(O[H])[C@]1([H])O[H] 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 1
- 239000004472 Lysine Substances 0.000 claims 1
- 125000003047 N-acetyl group Chemical group 0.000 claims 1
- 206010030043 Ocular hypertension Diseases 0.000 claims 1
- 102100038239 Protein Churchill Human genes 0.000 claims 1
- 241000051616 Ulmus minor Species 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000003368 amide group Chemical group 0.000 claims 1
- 150000001412 amines Chemical group 0.000 claims 1
- 150000001413 amino acids Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000011203 carbon fibre reinforced carbon Substances 0.000 claims 1
- UJLXYODCHAELLY-XLPZGREQSA-N dTDP Chemical compound O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](COP(O)(=O)OP(O)(O)=O)[C@@H](O)C1 UJLXYODCHAELLY-XLPZGREQSA-N 0.000 claims 1
- XPPKVPWEQAFLFU-UHFFFAOYSA-M diphosphate(1-) Chemical compound OP(O)(=O)OP(O)([O-])=O XPPKVPWEQAFLFU-UHFFFAOYSA-M 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000003843 furanosyl group Chemical group 0.000 claims 1
- 229930182830 galactose Natural products 0.000 claims 1
- 125000002519 galactosyl group Chemical group C1([C@H](O)[C@@H](O)[C@@H](O)[C@H](O1)CO)* 0.000 claims 1
- 125000002791 glucosyl group Chemical group C1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)* 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 239000002932 luster Substances 0.000 claims 1
- 125000000311 mannosyl group Chemical group C1([C@@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)* 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 150000002978 peroxides Chemical class 0.000 claims 1
- 108090000765 processed proteins & peptides Proteins 0.000 claims 1
- 150000003214 pyranose derivatives Chemical group 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 239000001226 triphosphate Substances 0.000 claims 1
- 235000011178 triphosphate Nutrition 0.000 claims 1
- UNXRWKVEANCORM-UHFFFAOYSA-N triphosphoric acid Chemical compound OP(O)(=O)OP(O)(=O)OP(O)(O)=O UNXRWKVEANCORM-UHFFFAOYSA-N 0.000 claims 1
- 229940035893 uracil Drugs 0.000 claims 1
- 0 **C(C(*)=C(*)N1C2C(*)(*)C(*)(*)C(COP(*P(O)(O*3*****3)=*)(O)=I)*2)=NC1=O Chemical compound **C(C(*)=C(*)N1C2C(*)(*)C(*)(*)C(COP(*P(O)(O*3*****3)=*)(O)=I)*2)=NC1=O 0.000 description 4
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10/087,551 US6897201B2 (en) | 2000-08-21 | 2002-02-27 | Compositions and methods for the treatment of glaucoma or ocular hypertension |
| PCT/US2003/006685 WO2003072066A2 (en) | 2002-02-27 | 2003-02-27 | Compositions and methods for the treatment of glaucoma and ocular hypertension |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005535564A JP2005535564A (ja) | 2005-11-24 |
| JP2005535564A5 true JP2005535564A5 (https=) | 2006-04-06 |
Family
ID=27765359
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003570813A Pending JP2005535564A (ja) | 2002-02-27 | 2003-02-27 | 緑内障または高眼圧症の治療のための組成物および方法 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US6897201B2 (https=) |
| JP (1) | JP2005535564A (https=) |
| AU (1) | AU2003223224A1 (https=) |
| GB (1) | GB2402674B (https=) |
| TW (1) | TW200305427A (https=) |
| WO (1) | WO2003072066A2 (https=) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6897201B2 (en) | 2000-08-21 | 2005-05-24 | Inspire Pharmaceuticals, Inc. | Compositions and methods for the treatment of glaucoma or ocular hypertension |
| EP2345657A1 (en) * | 2003-05-30 | 2011-07-20 | Pharmasset, Inc. | Modified fluorinated nucleoside analogues |
| US7488100B2 (en) * | 2003-09-03 | 2009-02-10 | Samuel Roberts | Bicycle light |
| CN101023094B (zh) * | 2004-07-21 | 2011-05-18 | 法莫赛特股份有限公司 | 烷基取代的2-脱氧-2-氟代-d-呋喃核糖基嘧啶和嘌呤及其衍生物的制备 |
| AU2005285045B2 (en) * | 2004-09-14 | 2011-10-13 | Gilead Sciences, Inc. | Preparation of 2'fluoro-2'- alkyl- substituted or other optionally substituted ribofuranosyl pyrimidines and purines and their derivatives |
| EP1863826A1 (en) * | 2005-03-30 | 2007-12-12 | Inspire Pharmaceuticals, Inc. | Process for the preparation of 4,6-disubstituted-tetrahydro-furo, thieno, pyrrolo and cyclopenta-[3,4][1,3]dioxoles |
| US7964580B2 (en) | 2007-03-30 | 2011-06-21 | Pharmasset, Inc. | Nucleoside phosphoramidate prodrugs |
| US8173621B2 (en) | 2008-06-11 | 2012-05-08 | Gilead Pharmasset Llc | Nucleoside cyclicphosphates |
| KR20110098849A (ko) | 2008-12-23 | 2011-09-01 | 파마셋 인코포레이티드 | 뉴클레오시드 유사체 |
| PT2376088T (pt) | 2008-12-23 | 2017-05-02 | Gilead Pharmasset Llc | Fosforamidatos de nucleósidos de 2-amino-purina 6-osubstituída |
| SG194404A1 (en) | 2008-12-23 | 2013-11-29 | Gilead Pharmasset Llc | Synthesis of purine nucleosides |
| TWI598358B (zh) | 2009-05-20 | 2017-09-11 | 基利法瑪席特有限責任公司 | 核苷磷醯胺 |
| US8618076B2 (en) | 2009-05-20 | 2013-12-31 | Gilead Pharmasset Llc | Nucleoside phosphoramidates |
| PL3290428T3 (pl) | 2010-03-31 | 2022-02-07 | Gilead Pharmasset Llc | Tabletka zawierająca krystaliczny (S)-2-(((S)-(((2R,3R,4R,5R)-5-(2,4-diokso-3,4-dihydropirymidyn-1(2H)-ylo)-4-fluoro-3-hydroksy-4-metylotetrahydrofuran-2-ylo)metoksy)(fenoksy)fosforylo)amino)propanian izopropylu |
| PT2609923T (pt) | 2010-03-31 | 2017-08-30 | Gilead Pharmasset Llc | Processo para a cristalização de 2-(((s)- (perfluorofenoxi)(fenoxi)fosforil)amino)propanoato de (s)-isopropilo |
| AU2011336632B2 (en) | 2010-11-30 | 2015-09-03 | Gilead Pharmasset Llc | Compounds |
| US8889159B2 (en) | 2011-11-29 | 2014-11-18 | Gilead Pharmasset Llc | Compositions and methods for treating hepatitis C virus |
| EA201690473A1 (ru) | 2013-08-27 | 2017-03-31 | ГАЙЛИД ФАРМАССЕТ ЭлЭлСи | Комбинированный состав двух противовирусных соединений |
| US9808531B2 (en) | 2015-09-22 | 2017-11-07 | Graybug Vision, Inc. | Compounds and compositions for the treatment of ocular disorders |
| ES2981607T3 (es) * | 2015-09-23 | 2024-10-09 | Eyepoint Pharmaceuticals Inc | Activadores de Tie-2 para uso en el tratamiento de la presión intraocular |
| CA3056923A1 (en) | 2017-03-23 | 2018-09-27 | Graybug Vision, Inc. | Drugs and compositions for the treatment of ocular disorders |
| US11160870B2 (en) | 2017-05-10 | 2021-11-02 | Graybug Vision, Inc. | Extended release microparticles and suspensions thereof for medical therapy |
| AU2018385762A1 (en) * | 2017-12-14 | 2020-06-04 | Graybug Vision, Inc. | Drugs and compositions for ocular delivery |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0492903A1 (en) | 1990-12-21 | 1992-07-01 | MERCK SHARP & DOHME LTD. | Substituted pyrazines, pyrimidines and pyridazines for use in the treatment of glaucoma |
| US5654285A (en) | 1991-04-06 | 1997-08-05 | Astra Pharmaceuticals Limited | ADP and ATP analogues, process for making and administration to inhibit ADP-induced platelet aggregation |
| EP0508687B1 (en) | 1991-04-06 | 1995-09-13 | Astra Pharmaceuticals Limited | ATP analogues |
| SK281309B6 (sk) | 1993-02-10 | 2001-02-12 | Astra Pharmaceuticals Limited | N-alkyl-2-substituované adenozíntrifosfátové deriváty, spôsob ich prípravy, farmaceutické prostriedky obsahujúce tieto deriváty a použitie týchto derivátov |
| US5545626A (en) * | 1994-01-19 | 1996-08-13 | The Trustees Of Columbia University In The City Of New York | Method of treating glaucoma with oligonucleotides |
| TR199800019T1 (xx) | 1995-07-11 | 1998-05-21 | Astra Pharmaceuticals Limited | Trombosit topaklanmas�n� �nleyici yeni maddeler. |
| EP0946561B1 (en) | 1996-12-20 | 2002-02-13 | AstraZeneca AB | Triazolo(4,5-d)pyrimidinyl derivatives and their use as medicaments |
| SE9702774D0 (sv) | 1997-07-22 | 1997-07-22 | Astra Pharma Prod | Novel compounds |
| CA2332540A1 (en) * | 1998-05-22 | 1999-12-02 | Benjamin R. Yerxa | Therapeutic dinucleotide and derivatives |
| US6528516B1 (en) | 1998-07-16 | 2003-03-04 | Trustees Of The University Of Pennsylvania, The Center For Technology Transfer | Methods for reducing intraocular pressure using A3 adenosine receptor antagonists |
| SE9804175D0 (sv) | 1998-12-02 | 1998-12-02 | Astra Pharma Prod | New assay |
| TWI229674B (en) | 1998-12-04 | 2005-03-21 | Astra Pharma Prod | Novel triazolo[4,5-d]pyrimidine compounds, pharmaceutical composition containing the same, their process for preparation and uses |
| SE9903290D0 (sv) | 1999-09-15 | 1999-09-15 | Astra Pharma Prod | Novel compounds |
| SE9904129D0 (sv) | 1999-11-15 | 1999-11-15 | Astra Pharma Prod | Novel compounds |
| SE9904377D0 (sv) | 1999-12-01 | 1999-12-01 | Astra Pharma Prod | Pharmaceutical combinations |
| US6897201B2 (en) | 2000-08-21 | 2005-05-24 | Inspire Pharmaceuticals, Inc. | Compositions and methods for the treatment of glaucoma or ocular hypertension |
| WO2002079150A2 (en) * | 2001-03-30 | 2002-10-10 | Sloan-Kettering Institute For Cancer Research | Glycorandomization and the production of novel erythronolide and coumarin analogs |
-
2002
- 2002-02-27 US US10/087,551 patent/US6897201B2/en not_active Expired - Fee Related
-
2003
- 2003-02-27 GB GB0419174A patent/GB2402674B/en not_active Expired - Fee Related
- 2003-02-27 AU AU2003223224A patent/AU2003223224A1/en not_active Abandoned
- 2003-02-27 WO PCT/US2003/006685 patent/WO2003072066A2/en not_active Ceased
- 2003-02-27 JP JP2003570813A patent/JP2005535564A/ja active Pending
- 2003-02-27 TW TW092104211A patent/TW200305427A/zh unknown
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