JPWO2020089778A5 - - Google Patents
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- Publication number
- JPWO2020089778A5 JPWO2020089778A5 JP2021523159A JP2021523159A JPWO2020089778A5 JP WO2020089778 A5 JPWO2020089778 A5 JP WO2020089778A5 JP 2021523159 A JP2021523159 A JP 2021523159A JP 2021523159 A JP2021523159 A JP 2021523159A JP WO2020089778 A5 JPWO2020089778 A5 JP WO2020089778A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- salt
- salt according
- hiv
- fluorines
- 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
- 150000003839 salts Chemical class 0.000 claims description 42
- 150000001875 compounds Chemical class 0.000 claims description 40
- 235000019000 fluorine Nutrition 0.000 claims description 14
- 125000001153 fluoro group Chemical group F* 0.000 claims description 14
- 229910052739 hydrogen Inorganic materials 0.000 claims description 10
- 125000000217 alkyl group Chemical group 0.000 claims description 9
- 239000003112 inhibitor Substances 0.000 claims description 9
- 208000031886 HIV Infections Diseases 0.000 claims description 8
- 208000037357 HIV infectious disease Diseases 0.000 claims description 8
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 8
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims description 8
- 239000000203 mixture Substances 0.000 claims description 7
- 108010078851 HIV Reverse Transcriptase Proteins 0.000 claims description 4
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims description 4
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims description 4
- 125000002947 alkylene group Chemical group 0.000 claims description 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 239000001257 hydrogen Substances 0.000 claims description 4
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 4
- 239000002777 nucleoside Substances 0.000 claims description 4
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims description 4
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 claims description 4
- 150000003833 nucleoside derivatives Chemical class 0.000 claims description 3
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims description 2
- 208000030507 AIDS Diseases 0.000 claims description 2
- 102100035875 C-C chemokine receptor type 5 Human genes 0.000 claims description 2
- 101710149870 C-C chemokine receptor type 5 Proteins 0.000 claims description 2
- 102100031650 C-X-C chemokine receptor type 4 Human genes 0.000 claims description 2
- 101000922348 Homo sapiens C-X-C chemokine receptor type 4 Proteins 0.000 claims description 2
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 239000002835 hiv fusion inhibitor Substances 0.000 claims description 2
- 239000004030 hiv protease inhibitor Substances 0.000 claims description 2
- 238000010255 intramuscular injection Methods 0.000 claims description 2
- 239000007927 intramuscular injection Substances 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 230000035800 maturation Effects 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 238000010254 subcutaneous injection Methods 0.000 claims description 2
- 239000007929 subcutaneous injection Substances 0.000 claims description 2
- 238000002560 therapeutic procedure Methods 0.000 claims description 2
- 108010002459 HIV Integrase Proteins 0.000 claims 1
- 229940122440 HIV protease inhibitor Drugs 0.000 claims 1
- 239000000126 substance Substances 0.000 description 13
- 238000000034 method Methods 0.000 description 4
- PIVQQUNOTICCSA-UHFFFAOYSA-N ANTU Chemical compound C1=CC=C2C(NC(=S)N)=CC=CC2=C1 PIVQQUNOTICCSA-UHFFFAOYSA-N 0.000 description 1
- 229940099797 HIV integrase inhibitor Drugs 0.000 description 1
- 230000034303 cell budding Effects 0.000 description 1
- 239000003084 hiv integrase inhibitor Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862751733P | 2018-10-29 | 2018-10-29 | |
| US62/751,733 | 2018-10-29 | ||
| PCT/IB2019/059238 WO2020089778A1 (en) | 2018-10-29 | 2019-10-28 | Quinazolinyl-indazole derivatives and their use as inhibitors of human immunodeficiency virus replication |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022505989A JP2022505989A (ja) | 2022-01-14 |
| JPWO2020089778A5 true JPWO2020089778A5 (https=) | 2022-11-04 |
| JP2022505989A5 JP2022505989A5 (https=) | 2022-11-04 |
| JP7526174B2 JP7526174B2 (ja) | 2024-07-31 |
Family
ID=68425185
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021523159A Active JP7526174B2 (ja) | 2018-10-29 | 2019-10-28 | キナゾリニル－インダゾール誘導体及びそのヒト免疫不全ウイルス複製の阻害剤としてのその使用 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20210403465A1 (https=) |
| EP (1) | EP3873607B1 (https=) |
| JP (1) | JP7526174B2 (https=) |
| ES (1) | ES2969030T3 (https=) |
| WO (1) | WO2020089778A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2021004593A (es) | 2018-10-24 | 2021-06-15 | Viiv Healthcare Uk No 5 Ltd | Inhibidores de la replicacion del virus de la inmunodeficiencia humana. |
| US20210379071A1 (en) * | 2018-11-05 | 2021-12-09 | VIIV Healthcare UK (No.5) Limited | Inhibitors of human immunodeficiency virus replication |
| TWI902729B (zh) | 2019-11-28 | 2025-11-01 | 日商鹽野義製藥股份有限公司 | 以組合整合酶阻礙劑及抗ｈｉｖ藥為特徵之ｈｉｖ感染症的預防及治療用醫藥 |
| KR20220151655A (ko) * | 2020-03-06 | 2022-11-15 | 비브 헬스케어 유케이 (넘버5) 리미티드 | 인간 면역결핍 바이러스 복제의 억제제 |
| CN111548349A (zh) * | 2020-05-13 | 2020-08-18 | 厦门云凡医药科技有限公司 | 一种ret激酶抑制剂中间体及其制备方法 |
| US20250042926A1 (en) | 2023-05-31 | 2025-02-06 | Gilead Sciences, Inc. | Therapeutic compounds for hiv |
| AR132951A1 (es) | 2023-06-15 | 2025-08-13 | Viiv Healthcare Uk No 5 Ltd | Métodos e intermedios para preparar compuestos |
| US12594276B2 (en) | 2024-02-05 | 2026-04-07 | Viiv Healthcare Uk (No. 5) Limited | Inhibitors of human immunodeficiency virus replication |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102464654B (zh) | 2010-11-12 | 2016-01-13 | 上海泓博智源医药技术有限公司 | 抗病毒化合物 |
| EP2729448B1 (en) | 2011-07-06 | 2015-09-09 | Gilead Sciences, Inc. | Compounds for the treatment of hiv |
| CN102863512B (zh) | 2011-07-07 | 2016-04-20 | 上海泓博智源医药技术有限公司 | 抗病毒化合物 |
| CA2897268C (en) | 2013-01-09 | 2018-12-04 | Gilead Sciences, Inc. | Therapeutic compounds for the treatment of viral infections |
| TW201443037A (zh) | 2013-01-09 | 2014-11-16 | Gilead Sciences Inc | 治療用化合物 |
| CA2896244C (en) | 2013-01-09 | 2017-07-04 | Gilead Sciences, Inc. | 5-membered heteroaryls and their use as antiviral agents |
| TWI694071B (zh) | 2013-03-01 | 2020-05-21 | 美商基利科學股份有限公司 | 治療反轉錄病毒科(Retroviridae)病毒感染之治療性化合物 |
| WO2015130964A1 (en) | 2014-02-28 | 2015-09-03 | Gilead Sciences, Inc. | Therapeutic compounds |
| WO2015130966A1 (en) | 2014-02-28 | 2015-09-03 | Gilead Sciences, Inc. | Antiviral agents |
| PT3186239T (pt) | 2014-08-29 | 2019-01-10 | Gilead Sciences Inc | Agentes antirretrovirais |
| KR20230011471A (ko) | 2016-08-19 | 2023-01-20 | 길리애드 사이언시즈, 인코포레이티드 | Hiv 바이러스 감염의 예방적 또는 치유적 치료에 유용한 치료 화합물 |
| TW201906834A (zh) * | 2017-05-02 | 2019-02-16 | 英商Viiv醫療保健英國(No.5)有限公司 | 人類免疫不全病毒複製之抑制劑 |
| US10836746B2 (en) | 2018-02-15 | 2020-11-17 | Gilead Sciences, Inc. | Therapeutic compounds |
| WO2019161280A1 (en) | 2018-02-16 | 2019-08-22 | Gilead Sciences, Inc. | Methods and intermediates for preparing a therapeutic compound useful in the treatment of retroviridae viral infection |
| WO2019198024A1 (en) * | 2018-04-11 | 2019-10-17 | VIIV Healthcare UK (No.5) Limited | 4-oxo-3,4-dihydroquinazoline compounds as inhibitors of human immunodeficiency virus replication |
| WO2020053811A1 (en) | 2018-09-14 | 2020-03-19 | VIIV Healthcare UK (No.5) Limited | Inhibitors of human immunodeficiency virus replication |
| JP7433303B2 (ja) | 2018-09-20 | 2024-02-19 | ヴィーブ ヘルスケア ユーケー（ナンバー５）リミテッド | ヒト免疫不全ウイルス複製の阻害剤 |
| US20210395262A1 (en) | 2018-10-24 | 2021-12-23 | VIIV Healthcare UK (No.5) Limited | Inhibitors of human immunodeficiency virus replication |
| US20210393633A1 (en) | 2018-10-25 | 2021-12-23 | VIIV Healthcare UK (No.5) Limited | Inhibitors of human immunodeficiency virus replication |
| US20210379071A1 (en) | 2018-11-05 | 2021-12-09 | VIIV Healthcare UK (No.5) Limited | Inhibitors of human immunodeficiency virus replication |
| WO2020095177A1 (en) | 2018-11-05 | 2020-05-14 | VIIV Healthcare UK (No.5) Limited | Inhibitors of human immunodeficiency virus replication |
-
2019
- 2019-10-28 EP EP19797382.9A patent/EP3873607B1/en active Active
- 2019-10-28 JP JP2021523159A patent/JP7526174B2/ja active Active
- 2019-10-28 ES ES19797382T patent/ES2969030T3/es active Active
- 2019-10-28 WO PCT/IB2019/059238 patent/WO2020089778A1/en not_active Ceased
- 2019-10-28 US US17/285,680 patent/US20210403465A1/en not_active Abandoned
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