EA020815B1 - Ингибиторы вируса гепатита с - Google Patents
Ингибиторы вируса гепатита с Download PDFInfo
- Publication number
- EA020815B1 EA020815B1 EA201270656A EA201270656A EA020815B1 EA 020815 B1 EA020815 B1 EA 020815B1 EA 201270656 A EA201270656 A EA 201270656A EA 201270656 A EA201270656 A EA 201270656A EA 020815 B1 EA020815 B1 EA 020815B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- sar
- mmol
- found
- nmr
- analytically calculated
- Prior art date
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- 241000711549 Hepacivirus C Species 0.000 title abstract description 5
- 239000003112 inhibitor Substances 0.000 title description 23
- 150000001875 compounds Chemical class 0.000 claims abstract description 212
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- 150000003839 salts Chemical class 0.000 claims description 86
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- -1 cyano, cyclopropyl halogen Chemical group 0.000 claims description 79
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- 229910052736 halogen Inorganic materials 0.000 claims description 23
- 150000002367 halogens Chemical class 0.000 claims description 21
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 19
- 150000002431 hydrogen Chemical group 0.000 claims description 7
- 125000004432 carbon atom Chemical group C* 0.000 claims description 5
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 5
- 125000001589 carboacyl group Chemical group 0.000 claims description 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 3
- 125000006432 1-methyl cyclopropyl group Chemical group [H]C([H])([H])C1(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims description 2
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- 101100405319 Arabidopsis thaliana NSI gene Proteins 0.000 description 18
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- SANWDQJIWZEKOD-UHFFFAOYSA-N tributyl(furan-2-yl)stannane Chemical compound CCCC[Sn](CCCC)(CCCC)C1=CC=CO1 SANWDQJIWZEKOD-UHFFFAOYSA-N 0.000 description 1
- IMFACGCPASFAPR-UHFFFAOYSA-N tributylamine Chemical compound CCCCN(CCCC)CCCC IMFACGCPASFAPR-UHFFFAOYSA-N 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical class [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 229940066528 trichloroacetate Drugs 0.000 description 1
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Classifications
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- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/19—Cytokines; Lymphokines; Interferons
- A61K38/21—Interferons [IFN]
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- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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Landscapes
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- Health & Medical Sciences (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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| PCT/US2010/060077 WO2011075439A1 (en) | 2009-12-16 | 2010-12-13 | Hepatitis c virus inhibitors |
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| EA201270656A1 EA201270656A1 (ru) | 2012-11-30 |
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| WO2010075376A2 (en) * | 2008-12-23 | 2010-07-01 | Abbott Laboratories | Anti-viral compounds |
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| SG174398A1 (en) | 2009-03-23 | 2011-10-28 | Glenmark Pharmaceuticals Sa | Furopyrimidinedione derivatives as trpa1 modulators |
| US20190127365A1 (en) | 2017-11-01 | 2019-05-02 | Merck Sharp & Dohme Corp. | Inhibitors of hepatitis c virus replication |
| CN102427729B (zh) | 2009-03-27 | 2014-09-03 | 默沙东公司 | 丙型肝炎病毒复制的抑制剂 |
| US8796466B2 (en) | 2009-03-30 | 2014-08-05 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| TW201038559A (en) | 2009-04-09 | 2010-11-01 | Bristol Myers Squibb Co | Hepatitis C virus inhibitors |
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| EP2419404B1 (en) * | 2009-04-15 | 2015-11-04 | AbbVie Inc. | Anti-viral compounds |
| US9139569B2 (en) | 2009-05-12 | 2015-09-22 | Merck Sharp & Dohme Corp. | Fused tricyclic aryl compounds useful for the treatment of viral diseases |
| RS56654B8 (sr) | 2009-05-13 | 2021-06-30 | Gilead Pharmasset Llc | Antiviralna jedinjenja |
| US8772505B2 (en) | 2009-05-29 | 2014-07-08 | Merck Sharp & Dohme Corp. | Antiviral compounds composed of three aligned aryl moieties to treat diseases such as hepatitis C |
| US8138215B2 (en) | 2009-05-29 | 2012-03-20 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| CA2763140A1 (en) | 2009-05-29 | 2010-12-02 | Schering Corporation | Antiviral compounds composed of three linked aryl moieties to treat diseases such as hepatitis c |
| US8211928B2 (en) | 2009-05-29 | 2012-07-03 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| US8937150B2 (en) | 2009-06-11 | 2015-01-20 | Abbvie Inc. | Anti-viral compounds |
| US8716454B2 (en) | 2009-06-11 | 2014-05-06 | Abbvie Inc. | Solid compositions |
| US9394279B2 (en) | 2009-06-11 | 2016-07-19 | Abbvie Inc. | Anti-viral compounds |
| EA020031B1 (ru) * | 2009-06-11 | 2014-08-29 | Эббви Бахамаз Лтд. | Противовирусные соединения |
| EP2454254A2 (en) | 2009-07-16 | 2012-05-23 | Vertex Pharmaceuticals Incorporated | Benzimidazole analogues for the treatment or prevention of flavivirus infections |
| US20110274648A1 (en) | 2009-11-11 | 2011-11-10 | Bristol-Myers Squibb Company | Hepatitis C Virus Inhibitors |
| US20110269956A1 (en) | 2009-11-11 | 2011-11-03 | Bristol-Myers Squibb Company | Hepatitis C Virus Inhibitors |
| US20110281910A1 (en) | 2009-11-12 | 2011-11-17 | Bristol-Myers Squibb Company | Hepatitis C Virus Inhibitors |
| CA2785488A1 (en) | 2009-12-22 | 2011-07-21 | Merck Sharp & Dohme Corp. | Fused tricyclic compounds and methods of use thereof for the treatment of viral diseases |
| US20130072523A1 (en) * | 2009-12-24 | 2013-03-21 | Vertex Pharmaceuticals Incorporated | Analogues for the treatment or prevention of flavivirus infections |
| US8362020B2 (en) | 2009-12-30 | 2013-01-29 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| EP2545060B1 (en) | 2010-03-09 | 2015-11-25 | Merck Sharp & Dohme Corp. | Fused tricyclic silyl compounds and methods of use thereof for the treatment of viral diseases |
| MX2012010918A (es) | 2010-03-24 | 2013-01-18 | Vertex Pharma | Analogos para el tratamiento o prevencion de infecciones por flavivirus. |
| NZ605440A (en) | 2010-06-10 | 2014-05-30 | Abbvie Bahamas Ltd | Solid compositions comprising an hcv inhibitor |
| EP2616461A4 (en) | 2010-08-26 | 2014-03-26 | Rfs Pharma Llc | POTENTIVE AND SELECTIVE INHIBITORS OF HEPATITIS C VIRUS |
| EP2621279B1 (en) | 2010-09-29 | 2018-04-04 | Merck Sharp & Dohme Corp. | Fused tetracycle derivatives and methods of use thereof for the treatment of viral diseases |
| WO2012048421A1 (en) * | 2010-10-14 | 2012-04-19 | Boehringer Ingelheim International Gmbh | Hepatitis c inhibitor compounds |
| US8921372B2 (en) | 2010-11-04 | 2014-12-30 | Theravance Biopharma R&D Ip, Llc | Inhibitors of hepatitis C virus |
| WO2012068234A2 (en) | 2010-11-17 | 2012-05-24 | Gilead Sciences, Inc. | Antiviral compounds |
| US8552047B2 (en) * | 2011-02-07 | 2013-10-08 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| WO2012122716A1 (en) | 2011-03-17 | 2012-09-20 | Merck Sharp & Dohme Corp. | Tetracyclic xanthene derivatives and methods of use thereof for treatment of viral diseases |
| US9546160B2 (en) | 2011-05-12 | 2017-01-17 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
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| EP2747569A4 (en) * | 2011-08-24 | 2015-07-08 | Glaxosmithkline Llc | COMBINATION TREATMENTS FOR HEPATITIS C |
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| EP2755982A4 (en) * | 2011-09-14 | 2015-03-25 | Merck Sharp & Dohme | SILICULAR HETEROCYCLIC DERIVATIVES AND METHOD FOR THEIR USE FOR THE TREATMENT OF VIRUS DISEASES |
| SI2709613T2 (sl) | 2011-09-16 | 2020-12-31 | Gilead Pharmasset LLC c/o Gilead Sciences, Inc. | Postopki za zdravljenje HCV |
| KR20140091036A (ko) | 2011-11-03 | 2014-07-18 | 세라밴스 인코포레이티드 | 단편 [2-[4-(바이페닐-4-일)-1h-이미다조-2-일]피롤리딘-1-카르보닐메틸]아민을 포함하는 간상 c형 간염 바이러스 억제제 |
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Also Published As
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| PH12012500979A1 (en) | 2014-09-05 |
| TN2012000264A1 (en) | 2013-12-12 |
| US20110286961A1 (en) | 2011-11-24 |
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| EP2513091A1 (en) | 2012-10-24 |
| TW201130825A (en) | 2011-09-16 |
| JP5785189B2 (ja) | 2015-09-24 |
| NZ601220A (en) | 2014-07-25 |
| CO6561788A2 (es) | 2012-11-15 |
| BR112012014677A2 (pt) | 2015-09-15 |
| KR20120107991A (ko) | 2012-10-04 |
| TWI487702B (zh) | 2015-06-11 |
| MA33806B1 (fr) | 2012-12-03 |
| US8377980B2 (en) | 2013-02-19 |
| AU2010332034A1 (en) | 2012-08-02 |
| CN102741242A (zh) | 2012-10-17 |
| AU2010332034B2 (en) | 2016-04-14 |
| EA201270656A1 (ru) | 2012-11-30 |
| AR079634A1 (es) | 2012-02-08 |
| SG181700A1 (en) | 2012-07-30 |
| CA2784662A1 (en) | 2011-06-23 |
| JP2013514359A (ja) | 2013-04-25 |
| PE20121479A1 (es) | 2012-11-07 |
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