AR123648A1 - Compuestos de carbamoilpiridona tricíclicos puenteados y sus usos - Google Patents
Compuestos de carbamoilpiridona tricíclicos puenteados y sus usosInfo
- Publication number
- AR123648A1 AR123648A1 ARP210102713A ARP210102713A AR123648A1 AR 123648 A1 AR123648 A1 AR 123648A1 AR P210102713 A ARP210102713 A AR P210102713A AR P210102713 A ARP210102713 A AR P210102713A AR 123648 A1 AR123648 A1 AR 123648A1
- Authority
- AR
- Argentina
- Prior art keywords
- 4alkyl
- alkyl
- halo
- haloc1
- haloalkyl
- Prior art date
Links
- OHEKQGOBJIKKIF-AWEZNQCLSA-N (12as)-n-[(4-fluorophenyl)methyl]-7-hydroxy-6,8-dioxo-3,4,12,12a-tetrahydro-2h-pyrido[5,6]pyrazino[2,6-b][1,3]oxazine-9-carboxamide Chemical class C([C@@H]1OCCCN1C(=O)C1=C(C2=O)O)N1C=C2C(=O)NCC1=CC=C(F)C=C1 OHEKQGOBJIKKIF-AWEZNQCLSA-N 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 9
- 125000005843 halogen group Chemical group 0.000 abstract 9
- 150000001875 compounds Chemical class 0.000 abstract 5
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 125000006661 (C4-C6) heterocyclic group Chemical group 0.000 abstract 3
- -1 haloC1−4alkyl Chemical group 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 abstract 2
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 2
- 241000725303 Human immunodeficiency virus Species 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000000172 C5-C10 aryl group Chemical group 0.000 abstract 1
- 208000015181 infectious disease Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/18—Bridged systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4995—Pyrazines or piperazines forming part of bridged ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/22—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Virology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Se describen compuestos para uso en el tratamiento o prevención de infección con el virus de la inmunodeficiencia humana (VIH). Los compuestos tienen la siguiente fórmula (1), incluyendo sus estereoisómeros y sus sales farmacéuticamente aceptables. También se describen métodos asociados con la preparación y uso de los compuestos descriptos, así como composiciones farmacéuticas que comprenden dichos compuestos. Reivindicación 1: Un compuesto de la fórmula (1) o una sal aceptable farmacéuticamente de este, en donde R¹ es arilo C₆₋₁₀ o heteroarilo de 5 a 10 miembros, en donde el arilo C₆₋₁₀ o heteroarilo de 5 a 10 miembros se sustituye opcionalmente con uno a cuatro RA¹, en donde cada RA¹ es independientemente halo, alquilo C₁₋₆, haloalquilo C₁₋₄, ciano, -O-alquilo C₁₋₄, o alquilo C₁₋₄-O-alquilo C₁₋₄; R² es H, alquilo C₁₋₆, o haloalquilo C₁₋₄; R³ es halo o -OR³ᵃ, en donde R³ᵃ es H, -alquilo C₁₋₆, -haloalquilo C₁₋₄, o -cicloalquilo C₃₋₆; o R³ᵃ y uno cualquiera de R², R⁵ᵃ, y R⁶ᵃ junto con los carbonos a los que están unidos forman un anillo heterocíclico de 4 a 6 miembros que contiene uno o dos heteroátomos seleccionados independientemente de N, O, y S; R³ᵇ es H, -alquilo C₁₋₆, -haloalquilo C₁₋₄, o -alquileno C₁₋₄-O-alquilo C₁₋₄; R⁴ᵃ es -alquilo C₁₋₆ o -haloalquilo C₁₋₄; R⁴ᵇ es H, halo, -alquilo C₁₋₆, o -haloalquilo C₁₋₄; W¹ es un enlace o -CR⁵ᵃR⁵ᵇ-; R⁵ᵃ y R⁵ᵇ son independientemente H, alquilo C₁₋₆, haloalquilo C₁₋₄, o halo; o R⁵ᵃ y R³ᵃ junto con los carbonos a los que están unidos forman un anillo heterocíclico de 4 a 6 miembros que contiene uno o dos heteroátomos seleccionados independientemente de N, O, y S; y R⁵ᵇ es H, alquilo C₁₋₆, haloalquilo C₁₋₄, o halo; W² es -CR⁶ᵃR⁶ᵇ- o -CR⁷ᵃ=CR⁷ᵇ-; R⁶ᵃ y R⁶ᵇ son independientemente H, alquilo C₁₋₆, haloalquilo C₁₋₄, halo, hidroxilo, ciano, -O-alquilo C₁₋₄, o alquileno C₁₋₄-O-alquilo C₁₋₄; o R⁶ᵃ y R³ᵃ junto con los carbonos a los que están unidos forman un anillo heterocíclico de 4 a 6 miembros que contiene uno o dos heteroátomos seleccionados independientemente de N, O, y S; y R⁶ᵇ es H, alquilo C₁₋₆, haloalquilo C₁₋₄, halo, hidroxilo, ciano, -O-alquilo C₁₋₄, o -alquileno C₁₋₄-O-alquilo C₁₋₄; R⁷ᵃ y R⁷ᵇ son independientemente H, halo, haloalquilo C₁₋₄, o alquilo C₁₋₆; o R⁷ᵃ y R⁷ᵇ junto con los carbonos a los que están unidos forman un arilo C₅₋₁₀ sustituido opcionalmente con uno a cuatro RA², en donde cada RA² es independientemente halo, ciano, o alquilo C₁₋₄.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063085704P | 2020-09-30 | 2020-09-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR123648A1 true AR123648A1 (es) | 2022-12-28 |
Family
ID=78463926
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP210102713A AR123648A1 (es) | 2020-09-30 | 2021-09-30 | Compuestos de carbamoilpiridona tricíclicos puenteados y sus usos |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US12421235B2 (es) |
| EP (1) | EP4222152B1 (es) |
| JP (2) | JP7691494B2 (es) |
| KR (1) | KR20230079137A (es) |
| CN (1) | CN116390924B (es) |
| AR (1) | AR123648A1 (es) |
| AU (2) | AU2021351491C1 (es) |
| CA (1) | CA3192145A1 (es) |
| TW (1) | TW202222798A (es) |
| WO (1) | WO2022072520A1 (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW202544011A (zh) | 2019-03-22 | 2025-11-16 | 美商基利科學股份有限公司 | 橋鍵聯三環胺甲醯吡啶酮化合物及其醫藥用途 |
| JP7453399B2 (ja) | 2020-02-24 | 2024-03-19 | ギリアード サイエンシーズ, インコーポレイテッド | Hiv感染症を治療するための四環式化合物及びその使用 |
| KR20230079137A (ko) | 2020-09-30 | 2023-06-05 | 길리애드 사이언시즈, 인코포레이티드 | 가교된 트리사이클릭 카르바모일피리돈 화합물 및 이의 용도 |
| PL4196479T3 (pl) | 2021-01-19 | 2024-03-18 | Gilead Sciences, Inc. | Podstawione związki pirydotriazynowe i ich zastosowania |
| 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 |
| WO2025080879A1 (en) * | 2023-10-11 | 2025-04-17 | Gilead Sciences, Inc. | Bridged tricyclic carbamoylpyridone compounds and uses thereof |
| WO2025080850A1 (en) * | 2023-10-11 | 2025-04-17 | Gilead Sciences, Inc. | Bridged tricyclic carbamoylpyridone compounds and uses thereof |
| WO2025080863A1 (en) * | 2023-10-11 | 2025-04-17 | Gilead Sciences, Inc. | Bridged tricyclic carbamoylpyridone compounds and uses thereof |
| CN119438457B (zh) * | 2024-12-18 | 2025-12-02 | 成都迈科康生物科技有限公司 | 一种测定脂质体佐剂中有关物质的方法及其应用 |
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- 2021-09-29 WO PCT/US2021/052683 patent/WO2022072520A1/en not_active Ceased
- 2021-09-29 US US17/489,406 patent/US12421235B2/en active Active
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| CN116390924B (zh) | 2025-11-07 |
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| CN116390924A (zh) | 2023-07-04 |
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| AU2024267005A1 (en) | 2024-12-19 |
| AU2021351491B2 (en) | 2024-09-05 |
| EP4222152A1 (en) | 2023-08-09 |
| US20240246975A1 (en) | 2024-07-25 |
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