JP2016527217A5 - - Google Patents
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- JP2016527217A5 JP2016527217A5 JP2016525819A JP2016525819A JP2016527217A5 JP 2016527217 A5 JP2016527217 A5 JP 2016527217A5 JP 2016525819 A JP2016525819 A JP 2016525819A JP 2016525819 A JP2016525819 A JP 2016525819A JP 2016527217 A5 JP2016527217 A5 JP 2016527217A5
- Authority
- JP
- Japan
- Prior art keywords
- compound according
- independently hydrogen
- alkyl
- halo
- hydrogen
- 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 72
- 229910052739 hydrogen Inorganic materials 0.000 claims description 64
- 239000001257 hydrogen Substances 0.000 claims description 64
- 125000000217 alkyl group Chemical group 0.000 claims description 38
- 125000005843 halogen group Chemical group 0.000 claims description 37
- 150000002431 hydrogen Chemical class 0.000 claims description 30
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 27
- -1 2,3-difluorophenyl Chemical group 0.000 claims description 24
- 239000008194 pharmaceutical composition Substances 0.000 claims description 18
- 150000003839 salts Chemical class 0.000 claims description 18
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims description 12
- 125000002837 carbocyclic group Chemical group 0.000 claims description 12
- 229910052799 carbon Inorganic materials 0.000 claims description 12
- 150000001721 carbon Chemical group 0.000 claims description 12
- 125000004432 carbon atom Chemical group C* 0.000 claims description 12
- 239000003814 drug Substances 0.000 claims description 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 12
- 229940124597 therapeutic agent Drugs 0.000 claims description 10
- 208000031886 HIV Infections Diseases 0.000 claims description 8
- 229910052736 halogen Inorganic materials 0.000 claims description 8
- VCMJCVGFSROFHV-WZGZYPNHSA-N tenofovir disoproxil fumarate Chemical compound OC(=O)\C=C\C(O)=O.N1=CN=C2N(C[C@@H](C)OCP(=O)(OCOC(=O)OC(C)C)OCOC(=O)OC(C)C)C=NC2=C1N VCMJCVGFSROFHV-WZGZYPNHSA-N 0.000 claims description 8
- 208000037357 HIV infectious disease Diseases 0.000 claims description 7
- 150000002367 halogens Chemical class 0.000 claims description 7
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims description 7
- 229960004556 tenofovir Drugs 0.000 claims description 6
- 125000004215 2,4-difluorophenyl group Chemical group [H]C1=C([H])C(*)=C(F)C([H])=C1F 0.000 claims description 4
- 239000003112 inhibitor Substances 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 239000002777 nucleoside Substances 0.000 claims description 4
- 150000003833 nucleoside derivatives Chemical class 0.000 claims description 4
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 2
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims description 2
- 108010078851 HIV Reverse Transcriptase Proteins 0.000 claims description 2
- 102100034343 Integrase Human genes 0.000 claims description 2
- 108010092799 RNA-directed DNA polymerase Proteins 0.000 claims description 2
- 229960000531 abacavir sulfate Drugs 0.000 claims description 2
- WMHSRBZIJNQHKT-FFKFEZPRSA-N abacavir sulfate Chemical compound OS(O)(=O)=O.C=12N=CN([C@H]3C=C[C@@H](CO)C3)C2=NC(N)=NC=1NC1CC1.C=12N=CN([C@H]3C=C[C@@H](CO)C3)C2=NC(N)=NC=1NC1CC1 WMHSRBZIJNQHKT-FFKFEZPRSA-N 0.000 claims description 2
- 239000002259 anti human immunodeficiency virus agent Substances 0.000 claims description 2
- 229940124411 anti-hiv antiviral agent Drugs 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 239000004030 hiv protease inhibitor Substances 0.000 claims description 2
- 229960001627 lamivudine Drugs 0.000 claims description 2
- JTEGQNOMFQHVDC-NKWVEPMBSA-N lamivudine Chemical compound O=C1N=C(N)C=CN1[C@H]1O[C@@H](CO)SC1 JTEGQNOMFQHVDC-NKWVEPMBSA-N 0.000 claims description 2
- 238000013160 medical therapy Methods 0.000 claims description 2
- 239000002773 nucleotide Substances 0.000 claims description 2
- 125000003729 nucleotide group Chemical group 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 229960004693 tenofovir disoproxil fumarate Drugs 0.000 claims description 2
- 230000001225 therapeutic effect Effects 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 7
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000000069 prophylactic effect Effects 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 description 2
- 0 *C(*)(*)NC(C(C1=O)=CN(C[C@@](*C2IC3C2)N3C2=O)C2=C1O)=O Chemical compound *C(*)(*)NC(C(C1=O)=CN(C[C@@](*C2IC3C2)N3C2=O)C2=C1O)=O 0.000 description 1
- 125000004211 3,5-difluorophenyl group Chemical group [H]C1=C(F)C([H])=C(*)C([H])=C1F 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 230000003449 preventive effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361845806P | 2013-07-12 | 2013-07-12 | |
| US61/845,806 | 2013-07-12 | ||
| PCT/US2014/046413 WO2015006731A1 (en) | 2013-07-12 | 2014-07-11 | Polycyclic-carbamoylpyridone compounds and their use for the treatment of hiv infections |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016527217A JP2016527217A (ja) | 2016-09-08 |
| JP2016527217A5 true JP2016527217A5 (enExample) | 2017-08-24 |
| JP6411491B2 JP6411491B2 (ja) | 2018-10-24 |
Family
ID=51257629
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016525819A Active JP6411491B2 (ja) | 2013-07-12 | 2014-07-11 | 多環式カルバモイルピリドン化合物およびｈｉｖ感染症を処置するためのその使用 |
Country Status (18)
| Country | Link |
|---|---|
| US (6) | US9421214B2 (enExample) |
| EP (2) | EP3019503B1 (enExample) |
| JP (1) | JP6411491B2 (enExample) |
| AU (3) | AU2014286993B2 (enExample) |
| CA (1) | CA2916993C (enExample) |
| CY (1) | CY1119544T1 (enExample) |
| DK (1) | DK3019503T3 (enExample) |
| ES (2) | ES2859102T3 (enExample) |
| HR (1) | HRP20171808T1 (enExample) |
| HU (1) | HUE037347T2 (enExample) |
| LT (1) | LT3019503T (enExample) |
| NO (1) | NO3011851T3 (enExample) |
| PL (2) | PL3252058T3 (enExample) |
| PT (2) | PT3252058T (enExample) |
| RS (1) | RS56540B1 (enExample) |
| SI (2) | SI3019503T1 (enExample) |
| SM (1) | SMT201700498T1 (enExample) |
| WO (1) | WO2015006731A1 (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA030003B1 (ru) * | 2012-12-21 | 2018-06-29 | Джилид Сайэнс, Инк. | Полициклическое карбамоилпиридоновое соединение и его фармацевтическое применение для лечения вич-инфекции |
| NO2865735T3 (enExample) | 2013-07-12 | 2018-07-21 | ||
| DK3019503T3 (da) * | 2013-07-12 | 2017-11-20 | Gilead Sciences Inc | Polycykliske-carbamoylpyridon-forbindelser og anvendelse deraf til behandling af hiv-infektioner |
| TWI744723B (zh) | 2014-06-20 | 2021-11-01 | 美商基利科學股份有限公司 | 多環型胺甲醯基吡啶酮化合物之合成 |
| WO2016027879A1 (ja) | 2014-08-22 | 2016-02-25 | 塩野義製薬株式会社 | インテグラーゼ阻害活性を有する多環性ピリドン誘導体 |
| SG11201606876RA (en) | 2015-03-04 | 2016-10-28 | Gilead Sciences Inc | Toll like receptor modulator compounds |
| CA2980362C (en) * | 2015-04-02 | 2020-02-25 | Gilead Sciences, Inc. | Polycyclic-carbamoylpyridone compounds and their pharmaceutical use |
| MA42684A (fr) | 2015-08-26 | 2018-07-04 | Gilead Sciences Inc | Modulateurs deutérés du récepteur toll |
| US20180263985A1 (en) | 2015-09-15 | 2018-09-20 | Gilead Sciences, Inc. | Modulators of toll-like receptors for the treatment of hiv |
| WO2018044838A1 (en) * | 2016-08-31 | 2018-03-08 | Viiv Healthcare Company | Combinations and uses and treatments thereof |
| EP3506902A4 (en) * | 2016-08-31 | 2020-04-22 | VIIV Healthcare Company | COMBINATIONS AND USES AND TREATMENTS THEREOF |
| SI3507276T1 (sl) | 2016-09-02 | 2022-01-31 | Gilead Sciences, Inc. | Spojine modulatorja toličnih receptorjev |
| WO2018045150A1 (en) | 2016-09-02 | 2018-03-08 | Gilead Sciences, Inc. | 4,6-diamino-pyrido[3,2-d]pyrimidine derivaties as toll like receptor modulators |
| JOP20190130A1 (ar) | 2016-12-02 | 2019-06-02 | Merck Sharp & Dohme | مركبات حلقية غير متجانسة رباعية الحلقات مفيدة كمثبطات إنزيم مدمج لفيروس نقص المناعة البشرية (hiv) |
| EP3805221A4 (en) | 2018-05-31 | 2022-01-05 | Shionogi & Co., Ltd | POLYCYCLIC PYRIDONE DERIVATIVE |
| CR20230571A (es) | 2018-05-31 | 2024-01-22 | Shionogi & Co | DERIVADO POLICÍCLICO DE CARBAMOILPIRIDONA (divisional 2020-0644) |
| KR20240151256A (ko) | 2019-03-22 | 2024-10-17 | 길리애드 사이언시즈, 인코포레이티드 | 가교된 트리시클릭 카르바모일피리돈 화합물 및 그의 제약 용도 |
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| US11248005B2 (en) | 2019-07-08 | 2022-02-15 | Lupin Limited | Process for preparation of intermediates used for the synthesis of HIV integrase inhibitor |
| WO2021107065A1 (ja) | 2019-11-28 | 2021-06-03 | 塩野義製薬株式会社 | 多環性ピリドピラジン誘導体 |
| US12564595B2 (en) | 2019-11-28 | 2026-03-03 | Shionogi & Co., Ltd. | Prophylactic and therapeutic pharmaceutical agent for HIV infectious diseases characterized by comprising combination of integrase inhibitor and anti-HIV agent |
| EP4110783A1 (en) | 2020-02-24 | 2023-01-04 | Gilead Sciences, Inc. | Tetracyclic compounds for treating hiv infection |
| CN116390924B (zh) | 2020-09-30 | 2025-11-07 | 吉利德科学公司 | 桥连三环氨基甲酰基吡啶酮化合物及其用途 |
| CR20260070A (es) | 2021-01-19 | 2026-04-24 | Gilead Sciences Inc | COMPUESTOS DE PIRIDOTRIAZINA SUSTITUIDOS Y USOS DE ESTOS (Divisional 2023-0315) |
| TWI856796B (zh) | 2022-04-06 | 2024-09-21 | 美商基利科學股份有限公司 | 橋聯三環胺甲醯基吡啶酮化合物及其用途 |
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2014
- 2014-07-11 DK DK14745052.2T patent/DK3019503T3/da active
- 2014-07-11 EP EP14745052.2A patent/EP3019503B1/en active Active
- 2014-07-11 JP JP2016525819A patent/JP6411491B2/ja active Active
- 2014-07-11 PT PT171774334T patent/PT3252058T/pt unknown
- 2014-07-11 RS RS20171145A patent/RS56540B1/sr unknown
- 2014-07-11 AU AU2014286993A patent/AU2014286993B2/en active Active
- 2014-07-11 EP EP17177433.4A patent/EP3252058B1/en active Active
- 2014-07-11 PL PL17177433T patent/PL3252058T3/pl unknown
- 2014-07-11 WO PCT/US2014/046413 patent/WO2015006731A1/en not_active Ceased
- 2014-07-11 ES ES17177433T patent/ES2859102T3/es active Active
- 2014-07-11 HU HUE14745052A patent/HUE037347T2/hu unknown
- 2014-07-11 LT LTEP14745052.2T patent/LT3019503T/lt unknown
- 2014-07-11 PL PL14745052T patent/PL3019503T3/pl unknown
- 2014-07-11 HR HRP20171808TT patent/HRP20171808T1/hr unknown
- 2014-07-11 SI SI201430395T patent/SI3019503T1/sl unknown
- 2014-07-11 CA CA2916993A patent/CA2916993C/en active Active
- 2014-07-11 US US14/329,694 patent/US9421214B2/en active Active
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- 2014-07-11 ES ES14745052.2T patent/ES2645192T3/es active Active
- 2014-07-11 SM SM20170498T patent/SMT201700498T1/it unknown
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2015
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2016
- 2016-07-12 US US15/208,304 patent/US9700554B2/en active Active
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2017
- 2017-06-09 US US15/618,464 patent/US20180153887A1/en not_active Abandoned
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2018
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2020
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2022
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