AR074504A1 - Nucleotidos uracil ciclopropilicos - Google Patents
Nucleotidos uracil ciclopropilicosInfo
- Publication number
- AR074504A1 AR074504A1 ARP090104736A ARP090104736A AR074504A1 AR 074504 A1 AR074504 A1 AR 074504A1 AR P090104736 A ARP090104736 A AR P090104736A AR P090104736 A ARP090104736 A AR P090104736A AR 074504 A1 AR074504 A1 AR 074504A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- benzyl
- phenyl
- hydrogen
- formula
- Prior art date
Links
- ISAKRJDGNUQOIC-UHFFFAOYSA-N Uracil Chemical compound O=C1C=CNC(=O)N1 ISAKRJDGNUQOIC-UHFFFAOYSA-N 0.000 title 2
- 239000002773 nucleotide Substances 0.000 title 1
- 229940035893 uracil Drugs 0.000 title 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000001475 halogen functional group Chemical group 0.000 abstract 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 239000001177 diphosphate Substances 0.000 abstract 1
- XPPKVPWEQAFLFU-UHFFFAOYSA-J diphosphate(4-) Chemical compound [O-]P([O-])(=O)OP([O-])([O-])=O XPPKVPWEQAFLFU-UHFFFAOYSA-J 0.000 abstract 1
- 235000011180 diphosphates Nutrition 0.000 abstract 1
- 125000004185 ester group Chemical group 0.000 abstract 1
- 125000001041 indolyl group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 150000004712 monophosphates Chemical class 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000001226 triphosphate Substances 0.000 abstract 1
- 235000011178 triphosphate Nutrition 0.000 abstract 1
- UNXRWKVEANCORM-UHFFFAOYSA-N triphosphoric acid Chemical compound OP(O)(=O)OP(O)(=O)OP(O)(O)=O UNXRWKVEANCORM-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
- C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
- A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Virology (AREA)
- Molecular Biology (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Compuestos, o una sal o solvato de los mismos, y formulaciones farmacéuticas y el uso de compuestos de fórmula (1) como inhibidores de HCV. Reivindicación 1: Un compuesto de fórmula 1 que incluye cualquier estereoisómero posible del mismo, donde R1 es hidrógeno o halo; R4 es un éster de monofosfato, difosfato o trifosfato, o R4 es un grupo de fórmula (2); R7 es fenilo, opcionalmente sustituido con 1, 2, o con 3 sustituyentes, cada uno seleccionado independientemente entre halo, alquilo C1-6, alquenilo C3-6, alcoxi C1-6, alcoxicarbonilo C1-6, hidroxi, y amino; o R7 es naftilo; o R7 es indolilo o N-alquiloxi C1-6 carbonilindolilo; R8 es hidrógeno, alquilo C1-6, bencilo; R8' es hidrógeno, alquilo C1-6, bencilo; R8 y R8' conjuntamente con el átomo de carbono al cual están unidos forman cicloalquilo C3-7; R9 es alquilo C1-10, cicloalquilo C3-7, bencilo, o fenilo, donde el fenilo puede estar opcionalmente sustituido con 1, 2 o 3 sustituyentes cada uno independientemente seleccionado entre hidroxi, alcoxi C1-6, amino, mono- y dialquilamino C1-6; o una sal o solvato farmacéuticamente aceptable del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08171006 | 2008-12-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR074504A1 true AR074504A1 (es) | 2011-01-19 |
Family
ID=40852521
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090104736A AR074504A1 (es) | 2008-12-08 | 2009-12-07 | Nucleotidos uracil ciclopropilicos |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US8399429B2 (es) |
| EP (1) | EP2373671B1 (es) |
| JP (1) | JP5683480B2 (es) |
| KR (1) | KR20110104000A (es) |
| CN (1) | CN102256991B (es) |
| AP (1) | AP2011005717A0 (es) |
| AR (1) | AR074504A1 (es) |
| AU (1) | AU2009326125B2 (es) |
| BR (1) | BRPI0922681A2 (es) |
| CA (1) | CA2745523C (es) |
| CL (1) | CL2011001364A1 (es) |
| EA (1) | EA020244B1 (es) |
| ES (1) | ES2525007T3 (es) |
| IL (1) | IL212897A (es) |
| MX (1) | MX2011006023A (es) |
| PA (1) | PA8852101A1 (es) |
| SG (1) | SG171973A1 (es) |
| TW (1) | TW201036989A (es) |
| UY (1) | UY32308A (es) |
| WO (1) | WO2010066699A1 (es) |
| ZA (1) | ZA201104231B (es) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO3027B1 (ar) * | 2009-05-14 | 2016-09-05 | Janssen Products Lp | نيوكليوسيدات يوراسيل سبيرواوكسيتان |
| US9676797B2 (en) | 2015-09-02 | 2017-06-13 | Abbvie Inc. | Anti-viral compounds |
| AR091156A1 (es) | 2012-05-25 | 2015-01-14 | Jansen R & D Ireland | Nucleosidos de espirooxetano de uracilo |
| PL3150616T3 (pl) * | 2012-11-16 | 2017-09-29 | University College Cardiff Consultants Limited | Mieszanina Rp/Sp gemcytabino-[fenylo-(benzyloksy-l-alaninylo)]-fosforynu |
| EP2940031B1 (en) * | 2013-03-08 | 2017-09-27 | Nanjing Sanhome Pharmaceutical Co., Ltd. | Nucleoside phosphoramidate compounds for use in the treatment of hcv |
| CN103848876B (zh) * | 2013-03-25 | 2016-05-11 | 安徽贝克联合制药有限公司 | 一种核苷磷酰胺前药及其制备方法和其应用 |
| WO2014169278A1 (en) | 2013-04-12 | 2014-10-16 | Achillion Pharmaceuticals, Inc. | Highly active nucleoside derivative for the treatment of hcv |
| CN105348342B (zh) * | 2014-09-30 | 2018-09-21 | 南京正大天晴制药有限公司 | 核苷氨基磷酸酯化合物及药物组合物和用途 |
| WO2016073756A1 (en) * | 2014-11-06 | 2016-05-12 | Enanta Pharmaceuticals, Inc. | Deuterated nucleoside/tide derivatives |
| CN105801646B (zh) * | 2014-12-31 | 2019-08-16 | 浙江大德药业集团有限公司 | 炔基取代的核苷氨基磷酸酯 |
| WO2016134053A1 (en) * | 2015-02-18 | 2016-08-25 | Abbvie Inc. | Anti-viral compounds |
| GEP20237502B (en) | 2015-03-06 | 2023-04-25 | Atea Pharmaceuticals Inc | B-D-2'-DEOXY-2'a-FLUORO-2'-B-C-SUBSTITUTED-2-MODIFIED-N6-SUBSTITUTED PURINE NUCLEOTIDES FOR HCV TREATMENT |
| US10711029B2 (en) | 2016-07-14 | 2020-07-14 | Atea Pharmaceuticals, Inc. | Beta-d-2′-deoxy-2′-alpha-fluoro-2′-beta-c-substituted-4′fluoro-n6-substituted-6-amino-2-substituted purine nucleotides for the treatment of hepatitis c virus infection |
| EA202190602A3 (ru) | 2016-09-07 | 2021-11-30 | Атеа Фармасьютикалс, Инк. | 2'-замещенные-n6-замещенные пуриновые нуклеотиды для лечения вызванных рнк-вирусом заболеваний |
| GEP20237457B (en) | 2017-02-01 | 2023-01-10 | Atea Pharmaceuticals Inc | Nucleotide hemi-sulfate salt for treatment of hepatitis c virus |
| JP2021521118A (ja) | 2018-04-10 | 2021-08-26 | アテア ファーマシューティカルズ， インコーポレイテッド | 肝硬変を伴うｈｃｖ感染患者の治療 |
| US10874687B1 (en) | 2020-02-27 | 2020-12-29 | Atea Pharmaceuticals, Inc. | Highly active compounds against COVID-19 |
| KR20240022574A (ko) | 2021-06-17 | 2024-02-20 | 아테아 파마슈티컬즈, 인크. | 유리한 항-hcv 조합 요법 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4916122A (en) * | 1987-01-28 | 1990-04-10 | University Of Georgia Research Foundation, Inc. | 3'-Azido-2',3'-dideoxyuridine anti-retroviral composition |
| ES2189721T3 (es) | 1992-12-29 | 2003-07-16 | Abbott Lab | Inhibidores de proteasa retroviral. |
| US20010021509A1 (en) * | 1997-10-23 | 2001-09-13 | Sathe Ganesh Madhusudan | cDNA clone HNEAA81 that encodes a human 7-transmembrane receptor |
| MY140819A (en) * | 2002-06-28 | 2010-01-29 | Idenix Caymans Ltd | Modified 2' and 3'-nucleoside prodrugs for treating flaviviridae |
| EP1653976A4 (en) * | 2003-02-19 | 2009-07-29 | Univ Yale | ANTI-VIRAL NUCLEOSIDE ANALOGUE AND METHOD FOR THE TREATMENT OF VIRUS INFECTIONS, IN PARTICULAR HIV INFECTIONS |
| PL1628685T3 (pl) * | 2003-04-25 | 2011-05-31 | Gilead Sciences Inc | Przeciwwirusowe analogi fosfonianowe |
| WO2006094347A1 (en) * | 2005-03-08 | 2006-09-14 | Biota Scientific Management Pty Ltd. | Bicyclic nucleosides and nucleotides as therapeutic agents |
| SI2084175T1 (sl) | 2006-10-10 | 2011-05-31 | Medivir Ab | Hcv nukleozidni inhibitor |
-
2009
- 2009-12-03 PA PA20098852101A patent/PA8852101A1/es unknown
- 2009-12-07 AR ARP090104736A patent/AR074504A1/es not_active Application Discontinuation
- 2009-12-07 TW TW098141651A patent/TW201036989A/zh unknown
- 2009-12-08 CN CN200980150162.0A patent/CN102256991B/zh not_active Expired - Fee Related
- 2009-12-08 WO PCT/EP2009/066562 patent/WO2010066699A1/en not_active Ceased
- 2009-12-08 US US13/130,602 patent/US8399429B2/en not_active Expired - Fee Related
- 2009-12-08 UY UY0001032308A patent/UY32308A/es unknown
- 2009-12-08 CA CA2745523A patent/CA2745523C/en not_active Expired - Fee Related
- 2009-12-08 AU AU2009326125A patent/AU2009326125B2/en not_active Ceased
- 2009-12-08 EP EP09764845.5A patent/EP2373671B1/en not_active Not-in-force
- 2009-12-08 KR KR1020117015453A patent/KR20110104000A/ko not_active Withdrawn
- 2009-12-08 BR BRPI0922681A patent/BRPI0922681A2/pt not_active Application Discontinuation
- 2009-12-08 SG SG2011040979A patent/SG171973A1/en unknown
- 2009-12-08 MX MX2011006023A patent/MX2011006023A/es active IP Right Grant
- 2009-12-08 EA EA201170780A patent/EA020244B1/ru not_active IP Right Cessation
- 2009-12-08 JP JP2011539051A patent/JP5683480B2/ja not_active Expired - Fee Related
- 2009-12-08 AP AP2011005717A patent/AP2011005717A0/xx unknown
- 2009-12-08 ES ES09764845.5T patent/ES2525007T3/es active Active
-
2011
- 2011-05-16 IL IL212897A patent/IL212897A/en not_active IP Right Cessation
- 2011-06-07 ZA ZA2011/04231A patent/ZA201104231B/en unknown
- 2011-06-07 CL CL2011001364A patent/CL2011001364A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2009326125A1 (en) | 2010-06-17 |
| CA2745523A1 (en) | 2010-06-17 |
| ES2525007T3 (es) | 2014-12-17 |
| WO2010066699A1 (en) | 2010-06-17 |
| BRPI0922681A2 (pt) | 2016-01-05 |
| EA201170780A1 (ru) | 2011-12-30 |
| CN102256991B (zh) | 2015-08-12 |
| MX2011006023A (es) | 2011-06-28 |
| SG171973A1 (en) | 2011-07-28 |
| CN102256991A (zh) | 2011-11-23 |
| AU2009326125B2 (en) | 2015-03-12 |
| UY32308A (es) | 2010-06-30 |
| CL2011001364A1 (es) | 2011-09-23 |
| PA8852101A1 (es) | 2010-07-27 |
| KR20110104000A (ko) | 2011-09-21 |
| JP2012510980A (ja) | 2012-05-17 |
| AP2011005717A0 (en) | 2011-06-30 |
| EP2373671B1 (en) | 2014-09-10 |
| JP5683480B2 (ja) | 2015-03-11 |
| EP2373671A1 (en) | 2011-10-12 |
| EA020244B1 (ru) | 2014-09-30 |
| TW201036989A (en) | 2010-10-16 |
| US8399429B2 (en) | 2013-03-19 |
| US20110230436A1 (en) | 2011-09-22 |
| ZA201104231B (en) | 2012-11-28 |
| IL212897A (en) | 2013-12-31 |
| CA2745523C (en) | 2017-07-04 |
| IL212897A0 (en) | 2011-07-31 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |