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 (https=) | 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 (https=) |
| EP (1) | EP2507249B1 (https=) |
| JP (1) | JP5774008B2 (https=) |
| KR (1) | KR20120081123A (https=) |
| CN (1) | CN102498118A (https=) |
| AU (1) | AU2010292411B2 (https=) |
| BR (1) | BR112012005438A2 (https=) |
| CA (1) | CA2771124C (https=) |
| ES (1) | ES2559437T3 (https=) |
| IN (1) | IN2012DN01855A (https=) |
| MX (1) | MX2012002925A (https=) |
| NZ (1) | NZ598208A (https=) |
| PT (1) | PT2507249E (https=) |
| WO (1) | WO2011031669A1 (https=) |
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 |
| AU2010276441B2 (en) | 2009-07-21 | 2015-07-02 | Gilead Sciences, Inc. | Inhibitors of Flaviviridae viruses |
| WO2011031669A1 (en) * | 2009-09-09 | 2011-03-17 | Gilead Sciences, Inc. | Inhibitors of flaviviridae viruses |
| US8524764B2 (en) * | 2010-01-15 | 2013-09-03 | Gilead Sciences, Inc. | Inhibitors of Flaviviridae viruses |
| MX2012008211A (es) * | 2010-01-15 | 2012-08-08 | Gilead Sciences Inc | Inhibidores de virus flaviviridae. |
| WO2012006060A1 (en) * | 2010-06-28 | 2012-01-12 | Vertex Pharmaceuticals Incorporated | Compounds and methods for the treatment or prevention of flavivirus infections |
| MA34462B1 (fr) | 2010-07-22 | 2013-08-01 | Novartis Ag | Composes de thiophene 2,3,5- trisubstitues et leurs utilisations |
| US20130203706A1 (en) * | 2011-06-28 | 2013-08-08 | Vertex Pharmaceuticals Incorporated | Compounds and methods for the treatment or prevention of flavivirus infections |
| PT2734515E (pt) | 2011-07-13 | 2016-03-11 | Gilead Sciences Inc | Derivados de ácido tiofen-2-carboxílico úteis como inibidores de vírus flaviviridae |
| GB201116559D0 (en) | 2011-09-26 | 2011-11-09 | Univ Leuven Kath | Novel viral replication inhibitors |
| 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 |
| US8841340B2 (en) | 2012-08-17 | 2014-09-23 | Gilead Sciences, Inc. | Solid forms of an antiviral compound |
| JP7381190B2 (ja) | 2014-12-26 | 2023-11-15 | エモリー・ユニバーシテイ | Ｎ４－ヒドロキシシチジン及び誘導体並びにそれに関連する抗ウイルス用途 |
| 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 |
| EP3454856B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| ES2990061T3 (es) | 2016-05-10 | 2024-11-28 | C4 Therapeutics Inc | Degronímeros espirocíclicos 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 |
| CN110769822A (zh) | 2017-06-20 | 2020-02-07 | 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 |
| PT3706762T (pt) | 2017-12-07 | 2024-12-05 | Univ Emory | N4-hidroxicitidina e derivados e utilizações antivirais relacionadas com os mesmos |
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 |
| US20050119332A1 (en) | 1998-03-12 | 2005-06-02 | Lone Jeppesen | Substituted thiophene compounds as modulators of protein tyrosine phosphatases (PTPases) |
| US20020002199A1 (en) | 1998-03-12 | 2002-01-03 | Lone Jeppesen | Modulators of protein tyrosine phosphatases (ptpases) |
| WO2002100846A1 (en) | 2001-06-11 | 2002-12-19 | Shire Biochem Inc. | Compounds and methods for the treatment or prevention of flavivirus infections |
| US6881741B2 (en) | 2001-06-11 | 2005-04-19 | Virochem Pharma Inc. | Compounds and methods for the treatment or prevention of Flavivirus infections |
| MXPA05006196A (es) * | 2002-12-10 | 2006-01-27 | Virochem Pharma Inc | Compuestos y metodos para el tratamiento o prevencion de infecciones por flavivirus. |
| KR101058696B1 (ko) | 2002-12-10 | 2011-08-22 | 바이로켐 파마 인코포레이티드 | 후라비바이러스 감염의 치료 또는 예방을 위한 화합물과방법 |
| 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 |
| WO2005095386A1 (en) | 2004-03-30 | 2005-10-13 | Chiron Corporation | Substituted thiophene derivatives as anti-cancer agents |
| DE102005028077A1 (de) | 2004-12-22 | 2006-07-13 | Aicuris Gmbh & Co. Kg | Alkinyl-substituierte Thiophene |
| DE102004061746A1 (de) | 2004-12-22 | 2006-07-06 | Bayer Healthcare Ag | Alkinyl-substituierte Thiophene |
| WO2006119646A1 (en) | 2005-05-13 | 2006-11-16 | Virochem Pharma Inc. | Compounds and methods for the treatment or prevention of flavivirus infections |
| WO2007093365A2 (en) | 2006-02-15 | 2007-08-23 | Sanofi-Aventis | Novel amino alcohol-substituted arylthienopyrimidinones, process for their preparation and their use as medicaments |
| JP5290186B2 (ja) | 2006-11-15 | 2013-09-18 | ヴァイロケム ファーマ インコーポレイテッド | フラビウイルス感染症の治療または予防用のチオフェン類似体 |
| US20090274655A1 (en) | 2006-11-17 | 2009-11-05 | Richard Martin Grimes | 2-carboxy thiophene derivatives as anti viral agents |
| CA2750577A1 (en) | 2008-12-03 | 2010-06-10 | Presidio Pharmaceuticals, Inc. | Inhibitors of hcv ns5a |
| AU2010276441B2 (en) | 2009-07-21 | 2015-07-02 | Gilead Sciences, Inc. | Inhibitors of Flaviviridae viruses |
| WO2011031669A1 (en) * | 2009-09-09 | 2011-03-17 | Gilead Sciences, Inc. | Inhibitors of flaviviridae viruses |
| EP2504329A1 (en) | 2009-11-25 | 2012-10-03 | Vertex Pharmaceuticals Incorporated | 5-alkynyl-thiophene-2-carboxylic acid derivatives and their use for the treatment or prevention of flavivirus infections |
| MX2012008211A (es) | 2010-01-15 | 2012-08-08 | Gilead Sciences Inc | Inhibidores de virus flaviviridae. |
| US8524764B2 (en) | 2010-01-15 | 2013-09-03 | Gilead Sciences, Inc. | Inhibitors of Flaviviridae viruses |
| EP2585447A2 (en) | 2010-06-28 | 2013-05-01 | Vertex Pharmaceuticals Incorporated | Compounds and methods for the treatment or prevention of flavivirus infections |
| PT2734515E (pt) | 2011-07-13 | 2016-03-11 | Gilead Sciences Inc | Derivados de ácido tiofen-2-carboxílico úteis como inibidores de vírus flaviviridae |
-
2010
- 2010-09-07 WO PCT/US2010/047983 patent/WO2011031669A1/en not_active Ceased
- 2010-09-07 AU AU2010292411A patent/AU2010292411B2/en not_active Ceased
- 2010-09-07 CN CN2010800404113A patent/CN102498118A/zh active Pending
- 2010-09-07 ES ES10763902.3T patent/ES2559437T3/es active Active
- 2010-09-07 US US13/392,467 patent/US8501714B2/en active Active
- 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 NZ NZ598208A patent/NZ598208A/en not_active IP Right Cessation
- 2010-09-07 EP EP10763902.3A patent/EP2507249B1/en active Active
- 2010-09-07 IN IN1855DEN2012 patent/IN2012DN01855A/en unknown
- 2010-09-07 CA CA2771124A patent/CA2771124C/en not_active Expired - Fee Related
- 2010-09-07 MX MX2012002925A patent/MX2012002925A/es active IP Right Grant
- 2010-09-07 BR BR112012005438A patent/BR112012005438A2/pt not_active IP Right Cessation
- 2010-09-07 KR KR1020127008996A patent/KR20120081123A/ko not_active Withdrawn
-
2013
- 2013-06-26 US US13/927,355 patent/US8765722B2/en active Active
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