JP2014503516A5 - - Google Patents
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- JP2014503516A5 JP2014503516A5 JP2013543356A JP2013543356A JP2014503516A5 JP 2014503516 A5 JP2014503516 A5 JP 2014503516A5 JP 2013543356 A JP2013543356 A JP 2013543356A JP 2013543356 A JP2013543356 A JP 2013543356A JP 2014503516 A5 JP2014503516 A5 JP 2014503516A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- aryl
- nhc
- cycloalkyl
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 39
- 125000000217 alkyl group Chemical group 0.000 claims description 24
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 22
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims description 21
- 125000002947 alkylene group Chemical group 0.000 claims description 20
- 125000000623 heterocyclic group Chemical group 0.000 claims description 19
- 125000003107 substituted aryl group Chemical group 0.000 claims description 18
- 239000003112 inhibitor Substances 0.000 claims description 16
- 150000003839 salts Chemical class 0.000 claims description 14
- 125000004450 alkenylene group Chemical group 0.000 claims description 13
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 13
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims description 12
- 125000004399 C1-C4 alkenyl group Chemical group 0.000 claims description 11
- 125000000304 alkynyl group Chemical group 0.000 claims description 11
- 125000003118 aryl group Chemical group 0.000 claims description 10
- 125000006557 (C2-C5) alkylene group Chemical group 0.000 claims description 8
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims description 8
- 125000000753 cycloalkyl 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
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 125000001424 substituent group Chemical group 0.000 claims description 8
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims description 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 7
- 229910052760 oxygen Inorganic materials 0.000 claims description 7
- 125000004419 alkynylene group Chemical group 0.000 claims description 5
- 125000000732 arylene group Chemical group 0.000 claims description 5
- 229910052799 carbon Inorganic materials 0.000 claims description 5
- 238000000034 method Methods 0.000 claims description 5
- 229910052717 sulfur Inorganic materials 0.000 claims description 5
- 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
- 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
- 229940124615 TLR 7 agonist Drugs 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 229910052736 halogen Inorganic materials 0.000 claims description 4
- 150000002367 halogens Chemical class 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
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 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
- 230000009385 viral infection Effects 0.000 claims description 4
- 125000003342 alkenyl group Chemical group 0.000 claims description 3
- 125000005549 heteroarylene group Chemical group 0.000 claims description 3
- -1 substituted Chemical class 0.000 claims description 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
- 241000711549 Hepacivirus C Species 0.000 claims description 2
- 208000036142 Viral infection Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000005551 pyridylene group Chemical group 0.000 claims description 2
- 125000001475 halogen functional group Chemical group 0.000 claims 4
- 208000004576 Flaviviridae Infections Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 description 4
- 241000710781 Flaviviridae Species 0.000 description 2
- 125000005724 cycloalkenylene group Chemical group 0.000 description 2
- XAHPWAQGQWVKGX-MGBMXIFSSA-N CC(C)C(C(N[C@@H](Cc1cccc(O)c1)C(N(CCC1)N[C@@H]1C(OCc1cc(/C=C/CC[C@H]([C@H]2C)OC)c[s]1)=O)=O)=O)NC2=O Chemical compound CC(C)C(C(N[C@@H](Cc1cccc(O)c1)C(N(CCC1)N[C@@H]1C(OCc1cc(/C=C/CC[C@H]([C@H]2C)OC)c[s]1)=O)=O)=O)NC2=O XAHPWAQGQWVKGX-MGBMXIFSSA-N 0.000 description 1
- YTSTXQUADYXTMD-QJOREFBCSA-N CC(C)[C@@H](C(N[C@@H](Cc1cccc(O)c1)C(N(CCC1)NC1C(O[C@H](C)c1cc(/C=C/CC[C@H](C2)OC)ccc1)=O)=O)=O)NC2=O Chemical compound CC(C)[C@@H](C(N[C@@H](Cc1cccc(O)c1)C(N(CCC1)NC1C(O[C@H](C)c1cc(/C=C/CC[C@H](C2)OC)ccc1)=O)=O)=O)NC2=O YTSTXQUADYXTMD-QJOREFBCSA-N 0.000 description 1
- XIZJVYLKZRFALP-URIPJOPDSA-N CC(C)[C@@H](C(N[C@@H](Cc1cccc(O)c1)C(N(CCC1)N[C@@H]1C(NCc1cc(CC[C@@H]([C@H](C)C(C)[C@H]2C)OC)ccc1)=O)=O)=O)NC2=O Chemical compound CC(C)[C@@H](C(N[C@@H](Cc1cccc(O)c1)C(N(CCC1)N[C@@H]1C(NCc1cc(CC[C@@H]([C@H](C)C(C)[C@H]2C)OC)ccc1)=O)=O)=O)NC2=O XIZJVYLKZRFALP-URIPJOPDSA-N 0.000 description 1
- AUWZUEKUKUVCMS-RNGFSWOKSA-N CC(C)[C@@H](C(N[C@@H](Cc1cccc(O)c1)C(N(CCC1)N[C@@H]1C(OCCCC/C=C/CC[C@H]([C@H]1C)OC)=O)=O)=O)NC1=O Chemical compound CC(C)[C@@H](C(N[C@@H](Cc1cccc(O)c1)C(N(CCC1)N[C@@H]1C(OCCCC/C=C/CC[C@H]([C@H]1C)OC)=O)=O)=O)NC1=O AUWZUEKUKUVCMS-RNGFSWOKSA-N 0.000 description 1
- WPBKXFHONNKPJX-FKVNTWOLSA-N CCOC(CC/C=C/c1cccc(COC(C(CCC2)NN2C(C(Cc2cccc(O)c2)NC([C@H](C(C)C)N2)=O)=O)=O)c1)[C@@H](C)C2=O Chemical compound CCOC(CC/C=C/c1cccc(COC(C(CCC2)NN2C(C(Cc2cccc(O)c2)NC([C@H](C(C)C)N2)=O)=O)=O)c1)[C@@H](C)C2=O WPBKXFHONNKPJX-FKVNTWOLSA-N 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 125000004429 atom Chemical group 0.000 description 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 238000012512 characterization method Methods 0.000 description 1
- 238000002955 isolation Methods 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 125000005717 substituted cycloalkylene group Chemical group 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 125000005556 thienylene group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US42207110P | 2010-12-10 | 2010-12-10 | |
| US61/422,071 | 2010-12-10 | ||
| PCT/US2011/064009 WO2012078915A1 (en) | 2010-12-10 | 2011-12-08 | Macrocyclic inhibitors of flaviviridae viruses |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014503516A JP2014503516A (ja) | 2014-02-13 |
| JP2014503516A5 true JP2014503516A5 (https=) | 2015-01-29 |
| JP5847193B2 JP5847193B2 (ja) | 2016-01-20 |
Family
ID=45464097
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013543356A Expired - Fee Related JP5847193B2 (ja) | 2010-12-10 | 2011-12-08 | フラビウイルス科ウイルスの大環状インヒビター |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US8513184B2 (https=) |
| EP (1) | EP2649076B1 (https=) |
| JP (1) | JP5847193B2 (https=) |
| KR (1) | KR20140031841A (https=) |
| CN (1) | CN103403009B (https=) |
| AR (1) | AR084217A1 (https=) |
| AU (1) | AU2011338262B2 (https=) |
| BR (1) | BR112013014063A2 (https=) |
| CA (1) | CA2819824A1 (https=) |
| EA (1) | EA026114B1 (https=) |
| ES (1) | ES2536321T3 (https=) |
| IL (1) | IL226739A (https=) |
| MX (1) | MX2013006475A (https=) |
| NZ (1) | NZ612159A (https=) |
| PL (1) | PL2649076T3 (https=) |
| PT (1) | PT2649076E (https=) |
| PY (1) | PY1153144A (https=) |
| SI (1) | SI2649076T1 (https=) |
| TW (1) | TWI520966B (https=) |
| UY (1) | UY33775A (https=) |
| WO (1) | WO2012078915A1 (https=) |
Families Citing this family (74)
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| 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 |
| EA026235B1 (ru) * | 2012-06-08 | 2017-03-31 | Джилид Сайэнс, Инк. | Макроциклические ингибиторы вирусов flaviviridae |
| PT3087085T (pt) * | 2013-12-23 | 2019-06-04 | Gilead Sciences Inc | Síntese de um tripéptido macrocíclico inibidor de ns3 de hcv |
| CA2960436C (en) | 2014-09-16 | 2021-01-05 | Gilead Sciences, Inc. | Solid forms of a toll-like receptor modulator |
| DK3236972T3 (en) | 2014-12-26 | 2021-10-04 | Univ Emory | Antivirale N4-hydroxycytidin-derivativer |
| WO2016141092A1 (en) | 2015-03-04 | 2016-09-09 | Gilead Sciences, Inc. | Toll-like receptor modulating 4,6-diamino-pyrido[3,2-d]pyrimidine compounds |
| WO2017035230A1 (en) | 2015-08-26 | 2017-03-02 | Gilead Sciences, Inc. | Deuterated toll-like receptor modulators |
| EP4491236A3 (en) | 2016-05-10 | 2025-04-02 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| 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 |
| 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 |
| EP3454862B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| CN109414508A (zh) | 2016-05-27 | 2019-03-01 | 吉利德科学公司 | 使用ns5a、ns5b或ns3抑制剂治疗乙型肝炎病毒感染的方法 |
| BR102017010009A2 (pt) | 2016-05-27 | 2017-12-12 | Gilead Sciences, Inc. | Compounds for the treatment of hepatitis b virus infection |
| JOP20190024A1 (ar) | 2016-08-26 | 2019-02-19 | Gilead Sciences Inc | مركبات بيروليزين بها استبدال واستخداماتها |
| EP3507288B1 (en) | 2016-09-02 | 2020-08-26 | Gilead Sciences, Inc. | 4,6-diamino-pyrido[3,2-d]pyrimidine derivaties as toll like receptor modulators |
| CN109923106B (zh) | 2016-09-02 | 2022-09-13 | 吉利德科学公司 | toll样受体调节剂化合物 |
| IL265921B2 (en) | 2016-10-14 | 2024-05-01 | Prec Biosciences Inc | Engineered meganucleases specific for recognition sequences in the hepatitis b virus genome |
| TWI820984B (zh) | 2017-01-31 | 2023-11-01 | 美商基利科學股份有限公司 | 替諾福韋埃拉酚胺(tenofovir alafenamide)之晶型 |
| UY37581A (es) | 2017-02-02 | 2018-08-31 | Gilead Sciences Inc | Compuestos para el tratamiento de la infección por virus de la hepatitis b |
| BR102018007822A2 (pt) | 2017-04-20 | 2018-11-06 | Gilead Sciences, Inc. | composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição |
| EP4717317A2 (en) | 2017-06-20 | 2026-04-01 | C4 Therapeutics, Inc. | N/o-linked degrons and degronimers for protein degradation |
| JP6934562B2 (ja) | 2017-08-22 | 2021-09-15 | ギリアード サイエンシーズ， インコーポレイテッド | 治療用複素環式化合物 |
| 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 |
| CN111511754B (zh) | 2017-12-20 | 2023-09-12 | 捷克共和国有机化学与生物化学研究所 | 活化sting转接蛋白的具有膦酸酯键的2’3’环状二核苷酸 |
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| TW201945388A (zh) | 2018-04-12 | 2019-12-01 | 美商精密生物科學公司 | 對b型肝炎病毒基因體中之識別序列具有特異性之最佳化之經工程化巨核酸酶 |
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| WO2019211799A1 (en) | 2018-05-03 | 2019-11-07 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide |
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| KR102707808B1 (ko) | 2019-03-07 | 2024-09-19 | 인스티튜트 오브 오가닉 케미스트리 앤드 바이오케미스트리 에이에스 씨알 브이.브이.아이. | 2'3'-사이클릭 다이뉴클레오티드 및 이의 프로드럭 |
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| CN114796193B (zh) * | 2022-05-13 | 2023-07-18 | 黑龙江八一农垦大学 | 抗牛病毒性腹泻病毒的中药单体 |
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Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR006514A1 (es) | 1995-07-04 | 1999-09-08 | Sandoz Ag | Un macrolido, sus usos, un proceso para producirlo, un aislado biologicamente puro capaz de producirlo, y una composicion farmaceutica quelo comprende |
| US6124453A (en) | 1995-07-04 | 2000-09-26 | Novartis Ag | Macrolides |
| US20090221598A1 (en) * | 2005-06-17 | 2009-09-03 | Kai Lin | Use of Sanglifehrin in HCV |
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2011
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2013
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