JP2013504576A5 - - Google Patents
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- Publication number
- JP2013504576A5 JP2013504576A5 JP2012528855A JP2012528855A JP2013504576A5 JP 2013504576 A5 JP2013504576 A5 JP 2013504576A5 JP 2012528855 A JP2012528855 A JP 2012528855A JP 2012528855 A JP2012528855 A JP 2012528855A JP 2013504576 A5 JP2013504576 A5 JP 2013504576A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- pharmaceutically acceptable
- compound
- acceptable salt
- substituted
- 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.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims description 59
- 125000000217 alkyl group Chemical group 0.000 claims description 38
- -1 TLR-7 agonists Substances 0.000 claims description 36
- 125000003118 aryl group Chemical group 0.000 claims description 30
- 125000000623 heterocyclic group Chemical group 0.000 claims description 30
- 150000003839 salts Chemical class 0.000 claims description 29
- 239000003112 inhibitor Substances 0.000 claims description 24
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 claims description 21
- 125000002947 alkylene group Chemical group 0.000 claims description 10
- 239000003814 drug Substances 0.000 claims description 10
- 239000005557 antagonist Substances 0.000 claims description 8
- 108700008776 hepatitis C virus NS-5 Proteins 0.000 claims description 8
- 239000000203 mixture Substances 0.000 claims description 8
- 239000002777 nucleoside Substances 0.000 claims description 8
- 150000003833 nucleoside derivatives Chemical class 0.000 claims description 8
- 229910052736 halogen Inorganic materials 0.000 claims description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 230000009385 viral infection Effects 0.000 claims description 5
- KJTLQQUUPVSXIM-ZCFIWIBFSA-M (R)-mevalonate Chemical compound OCC[C@](O)(C)CC([O-])=O KJTLQQUUPVSXIM-ZCFIWIBFSA-M 0.000 claims description 4
- 101001023866 Arabidopsis thaliana Mannosyl-oligosaccharide glucosidase GCS1 Proteins 0.000 claims description 4
- KJTLQQUUPVSXIM-UHFFFAOYSA-N DL-mevalonic acid Natural products OCCC(O)(C)CC(O)=O KJTLQQUUPVSXIM-UHFFFAOYSA-N 0.000 claims description 4
- FWKQNCXZGNBPFD-UHFFFAOYSA-N Guaiazulene Chemical compound CC(C)C1=CC=C(C)C2=CC=C(C)C2=C1 FWKQNCXZGNBPFD-UHFFFAOYSA-N 0.000 claims description 4
- 229940124771 HCV-NS3 protease inhibitor Drugs 0.000 claims description 4
- 102000014150 Interferons Human genes 0.000 claims description 4
- 108010050904 Interferons Proteins 0.000 claims description 4
- 101800001014 Non-structural protein 5A Proteins 0.000 claims description 4
- IWUCXVSUMQZMFG-AFCXAGJDSA-N Ribavirin Chemical compound N1=C(C(=O)N)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 IWUCXVSUMQZMFG-AFCXAGJDSA-N 0.000 claims description 4
- 208000036142 Viral infection Diseases 0.000 claims description 4
- 230000003510 anti-fibrotic effect Effects 0.000 claims description 4
- 239000003795 chemical substances by application Substances 0.000 claims description 4
- 125000002993 cycloalkylene group Chemical group 0.000 claims description 4
- 239000000134 cyclophilin inhibitor Substances 0.000 claims description 4
- 229940079593 drug Drugs 0.000 claims description 4
- 239000002308 endothelin receptor antagonist Substances 0.000 claims description 4
- 239000003623 enhancer Substances 0.000 claims description 4
- 229940079322 interferon Drugs 0.000 claims description 4
- 239000002773 nucleotide Substances 0.000 claims description 4
- 125000003729 nucleotide group Chemical group 0.000 claims description 4
- 230000036454 renin-angiotensin system Effects 0.000 claims description 4
- 229960000329 ribavirin Drugs 0.000 claims description 4
- HZCAHMRRMINHDJ-DBRKOABJSA-N ribavirin Natural products O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1N=CN=C1 HZCAHMRRMINHDJ-DBRKOABJSA-N 0.000 claims description 4
- 229940124597 therapeutic agent Drugs 0.000 claims description 4
- 229940044616 toll-like receptor 7 agonist Drugs 0.000 claims description 4
- 241000710781 Flaviviridae Species 0.000 claims description 3
- 125000004419 alkynylene group Chemical group 0.000 claims description 3
- 125000000732 arylene group Chemical group 0.000 claims description 3
- 150000002148 esters Chemical class 0.000 claims description 3
- 241000711549 Hepacivirus C Species 0.000 claims description 2
- 239000000654 additive Substances 0.000 claims description 2
- 230000000996 additive effect Effects 0.000 claims description 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000004956 cyclohexylene group Chemical group 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 208000010710 hepatitis C virus infection Diseases 0.000 claims description 2
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims description 2
- 125000004437 phosphorous atom Chemical group 0.000 claims description 2
- 230000002265 prevention Effects 0.000 claims description 2
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims description 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 claims 1
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 description 29
- 125000001072 heteroaryl group Chemical group 0.000 description 29
- 125000003342 alkenyl group Chemical group 0.000 description 19
- 125000000304 alkynyl group Chemical group 0.000 description 19
- 125000004446 heteroarylalkyl group Chemical group 0.000 description 19
- 125000004429 atom Chemical group 0.000 description 11
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 description 10
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 description 10
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 description 10
- 0 CC(C)(C)C#Cc1cc(N([C@](CC2)CC[C@@]2O*(C)(C)O)C([C@@]2CC=C(C)CC2)=O)c(C(O)=O)[s]1 Chemical compound CC(C)(C)C#Cc1cc(N([C@](CC2)CC[C@@]2O*(C)(C)O)C([C@@]2CC=C(C)CC2)=O)c(C(O)=O)[s]1 0.000 description 6
- 125000003320 C2-C6 alkenyloxy group Chemical group 0.000 description 5
- 125000003545 alkoxy group Chemical group 0.000 description 5
- 125000005133 alkynyloxy group Chemical group 0.000 description 5
- 125000004104 aryloxy group Chemical group 0.000 description 5
- 125000000000 cycloalkoxy group Chemical group 0.000 description 5
- 150000002367 halogens Chemical class 0.000 description 5
- 125000005553 heteroaryloxy group Chemical group 0.000 description 5
- 125000005844 heterocyclyloxy group Chemical group 0.000 description 5
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 125000004641 (C1-C12) haloalkyl group Chemical group 0.000 description 2
- HPXRVTGHNJAIIH-UHFFFAOYSA-N OC1CCCCC1 Chemical compound OC1CCCCC1 HPXRVTGHNJAIIH-UHFFFAOYSA-N 0.000 description 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 125000004450 alkenylene group Chemical group 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 238000012512 characterization method Methods 0.000 description 1
- 238000002955 isolation Methods 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24087409P | 2009-09-09 | 2009-09-09 | |
| US61/240,874 | 2009-09-09 | ||
| PCT/US2010/047983 WO2011031669A1 (en) | 2009-09-09 | 2010-09-07 | Inhibitors of flaviviridae viruses |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013504576A JP2013504576A (ja) | 2013-02-07 |
| JP2013504576A5 true JP2013504576A5 (enExample) | 2013-10-10 |
| JP5774008B2 JP5774008B2 (ja) | 2015-09-02 |
Family
ID=43028061
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012528855A Expired - Fee Related JP5774008B2 (ja) | 2009-09-09 | 2010-09-07 | Ｆｌａｖｉｖｉｒｉｄａｅウイルスの阻害剤 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US8501714B2 (enExample) |
| EP (1) | EP2507249B1 (enExample) |
| JP (1) | JP5774008B2 (enExample) |
| KR (1) | KR20120081123A (enExample) |
| CN (1) | CN102498118A (enExample) |
| AU (1) | AU2010292411B2 (enExample) |
| BR (1) | BR112012005438A2 (enExample) |
| CA (1) | CA2771124C (enExample) |
| ES (1) | ES2559437T3 (enExample) |
| IN (1) | IN2012DN01855A (enExample) |
| MX (1) | MX2012002925A (enExample) |
| NZ (1) | NZ598208A (enExample) |
| PT (1) | PT2507249E (enExample) |
| WO (1) | WO2011031669A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101330547A (zh) * | 2007-06-20 | 2008-12-24 | 朗迅科技公司 | 在VoIP网络中分布的用于提供服务的媒体资源 |
| AP3409A (en) * | 2009-07-21 | 2015-08-31 | Gilead Sciences Inc | Inhibitors of flaviviridae viruses |
| BR112012005438A2 (pt) * | 2009-09-09 | 2018-03-20 | Gilead Sciences Inc | inibidores de vírus flaviviridae |
| ES2543105T3 (es) | 2010-01-15 | 2015-08-14 | Gilead Sciences, Inc. | Inhibidores de virus flaviviridae |
| SG182475A1 (en) | 2010-01-15 | 2012-08-30 | Gilead Sciences Inc | Inhibitors of flaviviridae viruses |
| EP2585448A1 (en) * | 2010-06-28 | 2013-05-01 | Vertex Pharmaceuticals Incorporated | Compounds and methods for the treatment or prevention of flavivirus infections |
| AU2011281546B2 (en) | 2010-07-22 | 2014-07-10 | Novartis Ag | 2,3,5-trisubstituted thiophene compounds and uses thereof |
| US20130203706A1 (en) * | 2011-06-28 | 2013-08-08 | Vertex Pharmaceuticals Incorporated | Compounds and methods for the treatment or prevention of flavivirus infections |
| EP2734515B1 (en) * | 2011-07-13 | 2015-11-04 | Gilead Sciences, Inc. | Thiophen-2-carboxylic acid derivatives useful as inhibitors of flaviviridae viruses |
| GB201116559D0 (en) | 2011-09-26 | 2011-11-09 | Univ Leuven Kath | Novel viral replication inhibitors |
| US8841340B2 (en) | 2012-08-17 | 2014-09-23 | Gilead Sciences, Inc. | Solid forms of an antiviral compound |
| US8927741B2 (en) | 2012-08-17 | 2015-01-06 | Gilead Sciences, Inc. | Synthesis of an antiviral compound |
| US8759544B2 (en) | 2012-08-17 | 2014-06-24 | Gilead Sciences, Inc. | Synthesis of an antiviral compound |
| SMT202100592T1 (it) | 2014-12-26 | 2021-11-12 | Univ Emory | Derivati antivirali della n4-idrossicitidina |
| FR3046793B1 (fr) * | 2016-01-14 | 2018-01-05 | Les Laboratoires Servier | Nouveaux derives de phosphinanes et azaphosphinanes, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| CN109641874A (zh) | 2016-05-10 | 2019-04-16 | C4医药公司 | 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体 |
| ES2989988T3 (es) | 2016-05-10 | 2024-11-28 | C4 Therapeutics Inc | Degronímeros heterorocíclicos para la degradación de proteínas diana |
| CN109790143A (zh) | 2016-05-10 | 2019-05-21 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
| WO2017197036A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| CN118440096A (zh) | 2017-06-20 | 2024-08-06 | C4医药公司 | 用于蛋白降解的n/o-连接的降解决定子和降解决定子体 |
| KR20240011880A (ko) | 2017-12-07 | 2024-01-26 | 에모리 유니버시티 | N4-하이드록시사이티딘 및 유도체 및 이와 관련된 항-바이러스 용도 |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5861421A (en) | 1995-12-21 | 1999-01-19 | Smithkline Beecham Corporation | 4,4-(disubstituted) cyclohexan-1-one monomers and related compounds |
| US20020002199A1 (en) | 1998-03-12 | 2002-01-03 | Lone Jeppesen | Modulators of protein tyrosine phosphatases (ptpases) |
| US20050119332A1 (en) | 1998-03-12 | 2005-06-02 | Lone Jeppesen | Substituted thiophene compounds as modulators of protein tyrosine phosphatases (PTPases) |
| US6887877B2 (en) | 2001-06-11 | 2005-05-03 | Virochem Pharma Inc. | Compounds and methods for the treatment or prevention of Flavivirus infections |
| EP2206709A3 (en) * | 2001-06-11 | 2011-06-29 | Virochem Pharma Inc. | Thiophene derivatives as antiviral agents for flavivirus infection |
| NZ540799A (en) * | 2002-12-10 | 2008-09-26 | Virochem Pharma Inc | Compounds and methods for the treatment or prevention of flavivirus infections |
| ES2345438T3 (es) | 2002-12-10 | 2010-09-23 | Virochem Pharma Inc. | Compuestos y metodos para el tratamiento o prevencion de infecciones por flavivirus. |
| DE10359791A1 (de) | 2003-12-19 | 2005-07-21 | Bayer Healthcare Ag | Substituierte Thiophene |
| WO2005081954A2 (en) | 2004-02-25 | 2005-09-09 | Wyeth | Inhibitors of protein tyrosine phosphatase 1b |
| BRPI0508230A (pt) | 2004-03-30 | 2007-07-17 | Chiron Corp | derivados de tiofeno substituìdo como agentes anti-cáncer |
| DE102004061746A1 (de) | 2004-12-22 | 2006-07-06 | Bayer Healthcare Ag | Alkinyl-substituierte Thiophene |
| DE102005028077A1 (de) | 2004-12-22 | 2006-07-13 | Aicuris Gmbh & Co. Kg | Alkinyl-substituierte Thiophene |
| KR20080016597A (ko) | 2005-05-13 | 2008-02-21 | 바이로켐 파마 인코포레이티드 | 플라비바이러스 감염의 예방 또는 치료용 화합물 및 그의예방 또는 치료 방법 |
| AU2007214710A1 (en) | 2006-02-15 | 2007-08-23 | Sanofi-Aventis | Novel amino alcohol-substituted arylthienopyrimidinones, process for their preparation and their use as medicaments |
| EP2559692A1 (en) | 2006-11-15 | 2013-02-20 | Virochem Pharma Inc. | Thiophene analogues for the treatment or prevention of Flavivirus infections |
| US20090274655A1 (en) | 2006-11-17 | 2009-11-05 | Richard Martin Grimes | 2-carboxy thiophene derivatives as anti viral agents |
| KR20110098779A (ko) | 2008-12-03 | 2011-09-01 | 프레시디오 파마슈티칼스, 인코포레이티드 | Ｈｃｖ ｎｓ5ａ의 억제제 |
| AP3409A (en) | 2009-07-21 | 2015-08-31 | Gilead Sciences Inc | Inhibitors of flaviviridae viruses |
| BR112012005438A2 (pt) * | 2009-09-09 | 2018-03-20 | Gilead Sciences Inc | inibidores de vírus flaviviridae |
| AU2010326225A1 (en) | 2009-11-25 | 2012-06-07 | Vertex Pharmaceuticals Incorporated | 5-alkynyl-thiophene-2-carboxylic acid derivatives and their use for the treatment or prevention of flavivirus infections |
| ES2543105T3 (es) | 2010-01-15 | 2015-08-14 | Gilead Sciences, Inc. | Inhibidores de virus flaviviridae |
| SG182475A1 (en) | 2010-01-15 | 2012-08-30 | Gilead Sciences Inc | Inhibitors of flaviviridae viruses |
| AR081691A1 (es) | 2010-06-28 | 2012-10-10 | Vertex Pharma | Derivados de tiofeno, metodos para su preparacion y su uso en el tratamiento o la prevencion de infecciones por flavivirus |
| EP2734515B1 (en) | 2011-07-13 | 2015-11-04 | Gilead Sciences, Inc. | Thiophen-2-carboxylic acid derivatives useful as inhibitors of flaviviridae viruses |
-
2010
- 2010-09-07 BR BR112012005438A patent/BR112012005438A2/pt not_active IP Right Cessation
- 2010-09-07 CA CA2771124A patent/CA2771124C/en not_active Expired - Fee Related
- 2010-09-07 CN CN2010800404113A patent/CN102498118A/zh active Pending
- 2010-09-07 IN IN1855DEN2012 patent/IN2012DN01855A/en unknown
- 2010-09-07 MX MX2012002925A patent/MX2012002925A/es active IP Right Grant
- 2010-09-07 AU AU2010292411A patent/AU2010292411B2/en not_active Ceased
- 2010-09-07 KR KR1020127008996A patent/KR20120081123A/ko not_active Withdrawn
- 2010-09-07 ES ES10763902.3T patent/ES2559437T3/es active Active
- 2010-09-07 WO PCT/US2010/047983 patent/WO2011031669A1/en not_active Ceased
- 2010-09-07 US US13/392,467 patent/US8501714B2/en active Active
- 2010-09-07 NZ NZ598208A patent/NZ598208A/en not_active IP Right Cessation
- 2010-09-07 PT PT107639023T patent/PT2507249E/pt unknown
- 2010-09-07 JP JP2012528855A patent/JP5774008B2/ja not_active Expired - Fee Related
- 2010-09-07 EP EP10763902.3A patent/EP2507249B1/en active Active
-
2013
- 2013-06-26 US US13/927,355 patent/US8765722B2/en active Active
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