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
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- 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) | EP3252058B1 (enExample) |
| JP (1) | JP6411491B2 (enExample) |
| AU (3) | AU2014286993B2 (enExample) |
| CA (1) | CA2916993C (enExample) |
| CY (1) | CY1119544T1 (enExample) |
| DK (1) | DK3019503T3 (enExample) |
| ES (2) | ES2645192T3 (enExample) |
| HR (1) | HRP20171808T1 (enExample) |
| HU (1) | HUE037347T2 (enExample) |
| LT (1) | LT3019503T (enExample) |
| NO (1) | NO3011851T3 (enExample) |
| PL (2) | PL3252058T3 (enExample) |
| PT (2) | PT3019503T (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 |
|---|---|---|---|---|
| CA2893843C (en) | 2012-12-21 | 2018-09-04 | Gilead Sciences, Inc. | Polycyclic-carbamoylpyridone compounds and their pharmaceutical use |
| DK3019503T3 (da) * | 2013-07-12 | 2017-11-20 | Gilead Sciences Inc | Polycykliske-carbamoylpyridon-forbindelser og anvendelse deraf til behandling af hiv-infektioner |
| NO2865735T3 (enExample) | 2013-07-12 | 2018-07-21 | ||
| TWI677489B (zh) | 2014-06-20 | 2019-11-21 | 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 |
| EP3757105B1 (en) | 2014-08-22 | 2024-07-24 | Shionogi & Co., Ltd. | Polycyclic pyridone derivative having integrase inhibitory activity |
| DK3097102T3 (en) | 2015-03-04 | 2018-01-22 | Gilead Sciences Inc | TOLL-LIKE RECEPTOR MODULATING 4,6-DIAMINO-PYRIDO [3,2-D] PYRIMIDINE COMPOUNDS |
| TR201905009T4 (tr) * | 2015-04-02 | 2019-05-21 | Gilead Sciences Inc | Polisiklik-karbamoilpiridon bileşikleri ve bunların farmasötik kullanımları. |
| JP2018525412A (ja) | 2015-08-26 | 2018-09-06 | ギリアード サイエンシーズ， インコーポレイテッド | 重水素化トール様受容体調節因子 |
| JP2018527366A (ja) | 2015-09-15 | 2018-09-20 | ギリアード サイエンシーズ， インコーポレイテッド | ＨＩＶを処置するためのｔｏｌｌ様レセプターのモジュレーター |
| WO2018044838A1 (en) * | 2016-08-31 | 2018-03-08 | Viiv Healthcare Company | Combinations and uses and treatments thereof |
| US20190183901A1 (en) * | 2016-08-31 | 2019-06-20 | Viiv Healthcare Company | Combinations and uses and treatments thereof |
| 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 |
| MA46093A (fr) | 2016-09-02 | 2021-05-19 | Gilead Sciences Inc | Composés modulateurs du recepteur de type toll |
| 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) |
| CA3102063A1 (en) | 2018-05-31 | 2019-12-05 | Shionogi & Co., Ltd. | Polycyclic carbamoylpyridone derivative |
| US11453669B2 (en) | 2018-05-31 | 2022-09-27 | Shionogi & Co., Ltd. | Polycyclic pyridone derivative |
| IL286328B1 (en) | 2019-03-22 | 2026-04-01 | Gilead Sciences Inc | Tricyclic bridging compounds of carbamoylpyridone and their pharmaceutical use |
| US20220305115A1 (en) | 2019-06-18 | 2022-09-29 | Janssen Sciences Ireland Unlimited Company | Combination of hepatitis b virus (hbv) vaccines and pyridopyrimidine derivatives |
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| EP4066839A4 (en) | 2019-11-28 | 2023-12-27 | Shionogi & Co., Ltd | PROPHYLACTIC AND THERAPEUTIC MEDICINAL PRODUCT FOR HIV INFECTIOUS DISEASES, CHARACTERIZED BY CONTAINING THE COMBINATION OF INTEGRAS INHIBITORS AND ANTI-HIV AGENTS |
| US12577241B2 (en) | 2019-11-28 | 2026-03-17 | Shionogi & Co., Ltd. | Polycyclic pyridopyrazine derivative |
| CR20220418A (es) | 2020-02-24 | 2022-10-10 | Gilead Sciences Inc | Compuestos tetracíclicos para el tratamiento de infecciones por vih |
| CA3192145A1 (en) | 2020-09-30 | 2022-04-07 | Gilead Sciences, Inc. | Bridged tricyclic carbamoylpyridone compounds and uses thereof |
| JP7591155B2 (ja) | 2021-01-19 | 2024-11-27 | ギリアード サイエンシーズ， インコーポレイテッド | 置換ピリドトリアジン化合物及びその使用 |
| 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 HR HRP20171808TT patent/HRP20171808T1/hr unknown
- 2014-07-11 LT LTEP14745052.2T patent/LT3019503T/lt unknown
- 2014-07-11 SM SM20170498T patent/SMT201700498T1/it unknown
- 2014-07-11 EP EP17177433.4A patent/EP3252058B1/en active Active
- 2014-07-11 SI SI201430395T patent/SI3019503T1/sl unknown
- 2014-07-11 ES ES14745052.2T patent/ES2645192T3/es active Active
- 2014-07-11 US US14/329,694 patent/US9421214B2/en active Active
- 2014-07-11 HU HUE14745052A patent/HUE037347T2/hu unknown
- 2014-07-11 ES ES17177433T patent/ES2859102T3/es active Active
- 2014-07-11 WO PCT/US2014/046413 patent/WO2015006731A1/en not_active Ceased
- 2014-07-11 CA CA2916993A patent/CA2916993C/en active Active
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- 2014-07-11 JP JP2016525819A patent/JP6411491B2/ja active Active
- 2014-07-11 PT PT147450522T patent/PT3019503T/pt unknown
- 2014-07-11 PL PL17177433T patent/PL3252058T3/pl unknown
- 2014-07-11 PT PT171774334T patent/PT3252058T/pt unknown
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- 2014-07-11 AU AU2014286993A patent/AU2014286993B2/en active Active
- 2014-07-11 PL PL14745052T patent/PL3019503T3/pl unknown
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2015
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- 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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