JP2013517291A5 - - Google Patents
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- Publication number
- JP2013517291A5 JP2013517291A5 JP2012549122A JP2012549122A JP2013517291A5 JP 2013517291 A5 JP2013517291 A5 JP 2013517291A5 JP 2012549122 A JP2012549122 A JP 2012549122A JP 2012549122 A JP2012549122 A JP 2012549122A JP 2013517291 A5 JP2013517291 A5 JP 2013517291A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- substituted
- compound according
- alkyl
- membered
- 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
Links
- -1 cycloalkyl ethylene Chemical group 0.000 claims description 45
- 150000001875 compounds Chemical class 0.000 claims description 42
- 125000000217 alkyl group Chemical group 0.000 claims description 41
- 125000000623 heterocyclic group Chemical group 0.000 claims description 32
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 30
- 125000003118 aryl group Chemical group 0.000 claims description 30
- 239000003112 inhibitor Substances 0.000 claims description 26
- 125000003342 alkenyl group Chemical group 0.000 claims description 23
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 claims description 18
- 125000000304 alkynyl group Chemical group 0.000 claims description 18
- 150000002148 esters Chemical class 0.000 claims description 15
- 150000003839 salts Chemical class 0.000 claims description 15
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 13
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 13
- 125000004104 aryloxy group Chemical group 0.000 claims description 12
- 125000003545 alkoxy group Chemical group 0.000 claims description 10
- 239000003814 drug Substances 0.000 claims description 10
- 239000000203 mixture Substances 0.000 claims description 10
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 8
- 108700008776 hepatitis C virus NS-5 Proteins 0.000 claims description 8
- 239000002777 nucleoside Substances 0.000 claims description 8
- 150000003833 nucleoside derivatives Chemical class 0.000 claims description 8
- 230000009385 viral infection Effects 0.000 claims description 8
- 208000036142 Viral infection Diseases 0.000 claims description 7
- 125000005133 alkynyloxy group Chemical group 0.000 claims description 7
- 125000004429 atom Chemical group 0.000 claims description 7
- 229910052736 halogen Inorganic materials 0.000 claims description 7
- 150000002367 halogens Chemical class 0.000 claims description 7
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- KJTLQQUUPVSXIM-ZCFIWIBFSA-M (R)-mevalonate Chemical compound OCC[C@](O)(C)CC([O-])=O KJTLQQUUPVSXIM-ZCFIWIBFSA-M 0.000 claims description 4
- 229940123073 Angiotensin antagonist Drugs 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
- 241000710781 Flaviviridae Species 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
- 241000700605 Viruses Species 0.000 claims description 4
- 239000002333 angiotensin II receptor antagonist Substances 0.000 claims description 4
- 239000005557 antagonist Substances 0.000 claims description 4
- 239000003795 chemical substances by application Substances 0.000 claims description 4
- 239000000134 cyclophilin inhibitor Substances 0.000 claims description 4
- 229940079593 drug Drugs 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
- 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
- 241000711549 Hepacivirus C Species 0.000 claims description 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 3
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 claims description 2
- 241000710780 Bovine viral diarrhea virus 1 Species 0.000 claims description 2
- 241000725619 Dengue virus Species 0.000 claims description 2
- 239000005977 Ethylene Substances 0.000 claims description 2
- 241000710842 Japanese encephalitis virus Species 0.000 claims description 2
- 241000710912 Kunjin virus Species 0.000 claims description 2
- 241000725177 Omsk hemorrhagic fever virus Species 0.000 claims description 2
- 241000710888 St. Louis encephalitis virus Species 0.000 claims description 2
- 241000710771 Tick-borne encephalitis virus Species 0.000 claims description 2
- 241000710886 West Nile virus Species 0.000 claims description 2
- 241000710772 Yellow fever virus Species 0.000 claims description 2
- 241000907316 Zika virus Species 0.000 claims description 2
- 125000002393 azetidinyl group Chemical group 0.000 claims description 2
- 125000000000 cycloalkoxy group Chemical group 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 206010014599 encephalitis Diseases 0.000 claims description 2
- 125000005842 heteroatom Chemical group 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000003386 piperidinyl group Chemical group 0.000 claims description 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 2
- 229910052717 sulfur Inorganic materials 0.000 claims description 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 2
- 125000003507 tetrahydrothiofenyl group Chemical group 0.000 claims description 2
- 229940051021 yellow-fever virus Drugs 0.000 claims description 2
- 230000003510 anti-fibrotic effect Effects 0.000 claims 2
- 125000003320 C2-C6 alkenyloxy group Chemical group 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 description 26
- 125000004446 heteroarylalkyl group Chemical group 0.000 description 14
- 229910052799 carbon Inorganic materials 0.000 description 7
- 125000005553 heteroaryloxy group Chemical group 0.000 description 6
- 125000003302 alkenyloxy group Chemical group 0.000 description 5
- 238000000034 method Methods 0.000 description 5
- 229910052739 hydrogen Inorganic materials 0.000 description 3
- 206010016654 Fibrosis Diseases 0.000 description 2
- 230000004761 fibrosis Effects 0.000 description 2
- 125000004641 (C1-C12) haloalkyl group Chemical group 0.000 description 1
- 241000700721 Hepatitis B virus Species 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 125000001188 haloalkyl group Chemical group 0.000 description 1
- 125000004415 heterocyclylalkyl group Chemical group 0.000 description 1
- 125000002883 imidazolyl group Chemical group 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 125000003373 pyrazinyl group Chemical group 0.000 description 1
- 125000002098 pyridazinyl group Chemical group 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 125000005493 quinolyl group Chemical group 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US29557610P | 2010-01-15 | 2010-01-15 | |
| US61/295,576 | 2010-01-15 | ||
| US35348110P | 2010-06-10 | 2010-06-10 | |
| US61/353,481 | 2010-06-10 | ||
| PCT/US2011/021335 WO2011088345A1 (en) | 2010-01-15 | 2011-01-14 | Inhibitors of flaviviridae viruses |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015215450A Division JP2016041732A (ja) | 2010-01-15 | 2015-11-02 | フラビウイルス科ウイルスのインヒビター |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013517291A JP2013517291A (ja) | 2013-05-16 |
| JP2013517291A5 true JP2013517291A5 (https=) | 2014-02-13 |
| JP5868872B2 JP5868872B2 (ja) | 2016-02-24 |
Family
ID=43538203
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012549122A Active JP5868872B2 (ja) | 2010-01-15 | 2011-01-14 | フラビウイルス科ウイルスのインヒビター |
| JP2015215450A Withdrawn JP2016041732A (ja) | 2010-01-15 | 2015-11-02 | フラビウイルス科ウイルスのインヒビター |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015215450A Withdrawn JP2016041732A (ja) | 2010-01-15 | 2015-11-02 | フラビウイルス科ウイルスのインヒビター |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US8513298B2 (https=) |
| EP (2) | EP3219713A1 (https=) |
| JP (2) | JP5868872B2 (https=) |
| KR (1) | KR101727776B1 (https=) |
| CN (1) | CN102712633B (https=) |
| AP (1) | AP3576A (https=) |
| AR (1) | AR080001A1 (https=) |
| AU (1) | AU2011205744B2 (https=) |
| BR (1) | BR112012017382A2 (https=) |
| CA (1) | CA2785567C (https=) |
| CL (1) | CL2012001960A1 (https=) |
| CR (1) | CR20120417A (https=) |
| EA (1) | EA021196B1 (https=) |
| EC (1) | ECSP12012104A (https=) |
| ES (1) | ES2626150T3 (https=) |
| IL (1) | IL220545B (https=) |
| MX (1) | MX2012008211A (https=) |
| NZ (1) | NZ600817A (https=) |
| PE (1) | PE20130281A1 (https=) |
| PL (1) | PL2523950T3 (https=) |
| PT (1) | PT2523950T (https=) |
| SG (2) | SG182475A1 (https=) |
| SI (1) | SI2523950T1 (https=) |
| TW (1) | TWI491609B (https=) |
| UY (1) | UY33183A (https=) |
| WO (1) | WO2011088345A1 (https=) |
| ZA (1) | ZA201205248B (https=) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011011303A1 (en) * | 2009-07-21 | 2011-01-27 | Gilead Sciences, Inc. | Inhibitors of flaviviridae viruses |
| ES2559437T3 (es) | 2009-09-09 | 2016-02-12 | Gilead Sciences, Inc. | Inhibidores de virus de la familia Flaviviridae |
| CA2785563C (en) | 2010-01-15 | 2019-05-14 | Gilead Sciences, Inc. | Inhibitors of flaviviridae viruses |
| AP3576A (en) | 2010-01-15 | 2016-02-08 | Gilead Sciences Inc | Inhibitors of flaviviridae viruses |
| AU2011349844B2 (en) * | 2010-12-20 | 2017-06-01 | Gilead Sciences, Inc. | Combinations for treating HCV |
| DE102011003295A1 (de) * | 2011-01-28 | 2012-08-02 | Kiekert Ag | Kraftfahrzeugschloss |
| AU2012280959B2 (en) * | 2011-07-13 | 2015-08-06 | Gilead Sciences, Inc. | Thiophen-2-carboxylic acid derivatives useful as inhibitors of Flaviviridae viruses |
| PL2709613T5 (pl) * | 2011-09-16 | 2020-12-14 | Gilead Pharmasset Llc | Metody leczenia hcv |
| CN103087052A (zh) * | 2011-10-31 | 2013-05-08 | 上海壹志医药科技有限公司 | 噻吩衍生物及其药物用途 |
| EA026235B1 (ru) * | 2012-06-08 | 2017-03-31 | Джилид Сайэнс, Инк. | Макроциклические ингибиторы вирусов flaviviridae |
| PT2859009T (pt) | 2012-06-08 | 2018-01-18 | Gilead Sciences Inc | Inibidores macrocíclicos dos vírus flaviviridae |
| AR091279A1 (es) | 2012-06-08 | 2015-01-21 | Gilead Sciences Inc | Inhibidores macrociclicos de virus flaviviridae |
| 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 |
| PT2950786T (pt) | 2013-01-31 | 2020-03-03 | Gilead Pharmasset Llc | Formulação de combinação de dois compostos antivirais |
| WO2016065248A1 (en) | 2014-10-23 | 2016-04-28 | Complete Genomics, Inc. | Signal confinement sequencing (scs) and nucleotide analogues for signal confinement sequencing |
| DK3236972T3 (en) | 2014-12-26 | 2021-10-04 | Univ Emory | Antivirale N4-hydroxycytidin-derivativer |
| US10328061B2 (en) | 2016-05-02 | 2019-06-25 | Florida State University Research Foundation, Inc. | Treatment of Zika virus infections using alpha-glucosidase inhibitors |
| EP3454862B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| 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 |
| 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 |
| EP4491236A3 (en) | 2016-05-10 | 2025-04-02 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| EP4067368A1 (en) | 2016-06-01 | 2022-10-05 | Athira Pharma, Inc. | Compounds |
| EP4717317A2 (en) | 2017-06-20 | 2026-04-01 | C4 Therapeutics, Inc. | N/o-linked degrons and degronimers for protein degradation |
| JP6804790B1 (ja) | 2017-12-07 | 2020-12-23 | エモリー ユニバーシティー | Ｎ４−ヒドロキシシチジンおよび誘導体ならびにそれらに関連する抗ウイルス用途 |
| CN108096562B (zh) * | 2017-12-25 | 2021-05-11 | 武汉百药联科科技有限公司 | 20s蛋白酶体抑制剂在制备治疗日本乙型脑炎病毒感染的药物中的用途 |
| CA3189027A1 (en) | 2020-07-11 | 2022-01-20 | Pfizer Inc. | Antiviral heteroaryl ketone derivatives |
| US11351149B2 (en) | 2020-09-03 | 2022-06-07 | Pfizer Inc. | Nitrile-containing antiviral compounds |
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| JP2013512247A (ja) | 2009-11-25 | 2013-04-11 | バーテックス ファーマシューティカルズ 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のための５−アルキニル−チオフェン−２−カルボン酸誘導体およびそれらの使用 |
| CA2785563C (en) * | 2010-01-15 | 2019-05-14 | Gilead Sciences, Inc. | Inhibitors of flaviviridae viruses |
| AP3576A (en) * | 2010-01-15 | 2016-02-08 | Gilead Sciences Inc | Inhibitors of flaviviridae viruses |
| AU2011276526A1 (en) | 2010-06-28 | 2013-01-10 | Vertex Pharmaceuticals Incorporated | Compounds and methods for the treatment or prevention of Flavivirus infections |
| AU2012280959B2 (en) | 2011-07-13 | 2015-08-06 | Gilead Sciences, Inc. | Thiophen-2-carboxylic acid derivatives useful as inhibitors of Flaviviridae viruses |
-
2011
- 2011-01-14 AP AP2012006414A patent/AP3576A/xx active
- 2011-01-14 PL PL11700988T patent/PL2523950T3/pl unknown
- 2011-01-14 KR KR1020127021314A patent/KR101727776B1/ko active Active
- 2011-01-14 PT PT117009886T patent/PT2523950T/pt unknown
- 2011-01-14 TW TW100101437A patent/TWI491609B/zh active
- 2011-01-14 SG SG2012051181A patent/SG182475A1/en unknown
- 2011-01-14 UY UY0001033183A patent/UY33183A/es not_active Application Discontinuation
- 2011-01-14 SI SI201131169A patent/SI2523950T1/sl unknown
- 2011-01-14 PE PE2012000999A patent/PE20130281A1/es not_active Application Discontinuation
- 2011-01-14 CN CN201180005975.8A patent/CN102712633B/zh active Active
- 2011-01-14 EP EP17160365.7A patent/EP3219713A1/en not_active Withdrawn
- 2011-01-14 JP JP2012549122A patent/JP5868872B2/ja active Active
- 2011-01-14 BR BR112012017382A patent/BR112012017382A2/pt not_active Application Discontinuation
- 2011-01-14 CA CA2785567A patent/CA2785567C/en active Active
- 2011-01-14 SG SG10201500298PA patent/SG10201500298PA/en unknown
- 2011-01-14 AR ARP110100126A patent/AR080001A1/es unknown
- 2011-01-14 NZ NZ600817A patent/NZ600817A/en not_active IP Right Cessation
- 2011-01-14 MX MX2012008211A patent/MX2012008211A/es active IP Right Grant
- 2011-01-14 US US13/007,150 patent/US8513298B2/en active Active
- 2011-01-14 EA EA201290576A patent/EA021196B1/ru not_active IP Right Cessation
- 2011-01-14 WO PCT/US2011/021335 patent/WO2011088345A1/en not_active Ceased
- 2011-01-14 EP EP11700988.6A patent/EP2523950B1/en active Active
- 2011-01-14 ES ES11700988.6T patent/ES2626150T3/es active Active
- 2011-01-14 AU AU2011205744A patent/AU2011205744B2/en active Active
-
2012
- 2012-06-21 IL IL220545A patent/IL220545B/en not_active IP Right Cessation
- 2012-07-13 CL CL2012001960A patent/CL2012001960A1/es unknown
- 2012-07-13 ZA ZA2012/05248A patent/ZA201205248B/en unknown
- 2012-08-10 CR CR20120417A patent/CR20120417A/es unknown
- 2012-08-13 EC ECSP12012104 patent/ECSP12012104A/es unknown
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2013
- 2013-07-11 US US13/939,695 patent/US9321753B2/en active Active
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2015
- 2015-11-02 JP JP2015215450A patent/JP2016041732A/ja not_active Withdrawn