AR116474A1 - DERIVADOS DEL ÁCIDO 6,7-DIHIDRO-2H-BENZOFURO[2,3-a]QUINOLIZIN-3-CARBOXÍLICO COMO AGENTES ANTIVIRALES PARA EL TRATAMIENTO O PREVENCIÓN DE UNA INFECCIÓN POR HBV - Google Patents
DERIVADOS DEL ÁCIDO 6,7-DIHIDRO-2H-BENZOFURO[2,3-a]QUINOLIZIN-3-CARBOXÍLICO COMO AGENTES ANTIVIRALES PARA EL TRATAMIENTO O PREVENCIÓN DE UNA INFECCIÓN POR HBVInfo
- Publication number
- AR116474A1 AR116474A1 ARP190102685A ARP190102685A AR116474A1 AR 116474 A1 AR116474 A1 AR 116474A1 AR P190102685 A ARP190102685 A AR P190102685A AR P190102685 A ARP190102685 A AR P190102685A AR 116474 A1 AR116474 A1 AR 116474A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- alternatively
- taken together
- double bonds
- ring containing
- Prior art date
Links
- 239000003443 antiviral agent Substances 0.000 title abstract 2
- 208000015181 infectious disease Diseases 0.000 title abstract 2
- 230000002265 prevention Effects 0.000 title abstract 2
- 239000002253 acid Substances 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 4
- 150000002431 hydrogen Chemical group 0.000 abstract 4
- 125000003107 substituted aryl group Chemical group 0.000 abstract 4
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 3
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- -1 6,7-dihydro-2H-benzofuro [2,3-a] quinolizine-3-carboxylic acid Chemical compound 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 abstract 1
- 241000700721 Hepatitis B virus Species 0.000 abstract 1
- 230000000840 anti-viral effect Effects 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 238000002648 combination therapy Methods 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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
- C07D491/02—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 two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- 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
- C07D491/12—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 three hetero rings
- C07D491/14—Ortho-condensed systems
- C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P31/20—Antivirals for DNA viruses
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- Biotechnology (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Compuestos derivados del ácido 6,7-dihidro-2H-benzofuro[2,3-a]quinolizin-3-carboxílico como agentes antivirales para el tratamiento o prevención de una infección con el virus de la hepatitis B (HBV), utilizando los mismos en terapias combinadas con otros agentes con actividad antiviral. Se provee además una composición farmacéutica que comprende éstos compuestos. Reivindicación 1: Un compuesto representado por la fórmula (1), o una sal de uso farmacéutico aceptable del mismo, donde: Z¹ es O, NR¹ o S; Z² es N o CR²; Z³ es N o CR³; Z⁴ es N o CR⁴, Z⁵ es N o CR⁵; R¹ es hidrógeno, alquilo C₁₋₈ opcionalmente sustituido, alquenilo C₂₋₈ opcionalmente sustituido, cicloalquilo C₃₋₈ opcionalmente sustituido, heterocicloalquilo de 3- a 8- miembros opcionalmente sustituido, arilo opcionalmente sustituido o heteroarilo opcionalmente sustituido; R², R³, R⁴ y R⁵ se seleccionan independientemente: 1) hidrógeno; 2) halógeno; 3) -NO₂; 4) ciano; 5) alquilo C₁₋₈ opcionalmente sustituido; 6) alquenilo C₂₋₈ opcionalmente sustituido; 7) alquinilo C₂₋₈ opcionalmente sustituido; 8) cicloalquilo C₃₋₈ opcionalmente sustituido; 9) heterocicloalquilo de 3- a 8- miembros opcionalmente sustituido; 10) arilo opcionalmente sustituido; 11) arilalquilo opcionalmente sustituido; 12) heteroarilo opcionalmente sustituido; 13) heteroarilalquilo opcionalmente sustituido; 14) -SR¹¹; 15) -S(O)₂R¹¹; 16) -S(O)₂N(R¹¹)(R¹²); 17) -C(O)R¹¹; 18) -C(O)OR¹¹; 19) -C(O)N(R¹¹)(R¹²); 20) -C(O)N(R¹¹)S(O)₂(R¹²); 21) -N(R¹¹)(R¹²); 22) -N(R¹³)C(O)N(R¹¹)(R¹²); 23) -N(R¹¹)C(O)(R¹²); 24) -N(R¹¹)C(O)₂(R¹²); 25) -N(R¹³)S(O)₂N(R¹¹)(R¹²); 26) -N(R¹¹)S(O)₂(R¹²); 27) -OR¹¹; 28) -OC(O)R¹¹; 29) -OC(O)OR¹¹; y 30) -OC(O)N(R¹¹)(R¹²); donde R¹¹, R¹² y R¹³ es cada uno independientemente seleccionado de hidrógeno, alquilo C₁₋₈ opcionalmente substituido, alquenilo C₂₋₈ opcionalmente substituido, cicloalquilo C₃₋₈ opcionalmente substituido, heterocicloalquilo de 3- a 8- miembros opcionalmente substituido, arilo opcionalmente substituido y heteroarilo opcionalmente sustituido; alternativamente, R¹¹ y R¹² están tomados junto con el átomo de nitrógeno al cual están unidos para formar un anillo heterocíclico de 3 - 8 miembros opcionalmente sustituido que contiene 0, 1, 2 ó 3 dobles enlaces; alternativamente, Z² es CR², Z³ es CR³, y R² y R³ se toman juntos para formar un anillo heterocíclico o carbocíclico de 3 - 8 miembros opcionalmente sustituido que contiene 0, 1, 2 ó 3 enlaces dobles; alternativamente, Z³ es CR³, Z⁴ es CR⁴, y R³ y R⁴ se toman juntos para formar un anillo heterocíclico o carbocíclico de 3 - 8 miembros opcionalmente sustituido que contiene 0, 1, 2 ó 3 enlaces dobles; alternativamente, Z⁴ es CR⁴, Z⁵ es CR⁵, y R⁴ y R⁵ se toman juntos para formar un anillo heterocíclico o carbocíclico de 3 - 8 miembros opcionalmente sustituido que contiene 0, 1, 2 ó 3 enlaces dobles; Q¹, Q², Q³, y Q⁴ son cada uno independientemente seleccionado de hidrógeno, halo, NR¹¹, alquilo C₁₋₆ opcionalmente sustituido, alcoxi C₁₋₆ opcionalmente sustituido, cicloalquilo C₃₋₈ opcionalmente sustituido; heterocicloalquilo de 3- a 8- miembros opcionalmente sustituido; arilo opcionalmente sustituido y heteroarilo opcionalmente sustituido; alternativamente, Q¹ se toma junto con Q² o Q³ para formar un anillo heterocíclico o carbocíclico de 3 - 8 miembros opcionalmente sustituido que contiene 0, 1, 2 ó 3 enlaces dobles; alternativamente, Q² se toma junto con Q⁴ para formar un anillo heterocíclico o carbocíclico de 3 - 8 miembros opcionalmente sustituido que contiene 0, 1, 2 ó 3 enlaces dobles; alternativamente, Q³ y Q⁴ se toman juntos para formar un anillo heterocíclico o carbocíclico de 3 - 8 miembros opcionalmente sustituido que contiene 0, 1, 2 ó 3 enlaces dobles; Y¹ es hidrógeno, halo, o alquilo C₁₋₆ opcionalmente sustituido; Y² es O, NR¹¹, N(OR¹¹), o N(NR¹¹); Y³ es -COOR¹¹, -C(O)NHSO₂R¹¹, -C(O)NHSO₂NR¹¹R¹², 5-tetrazolilo o 1,2,4-oxadiazol-3-il-5(4H)-ona; e Y⁴ es hidrógeno o metilo opcionalmente sustituido; alternativamente, Y² e Y³ se toman juntos para formar un anillo heterocíclico de 5 - 12 miembros opcionalmente sustituido que contiene 1, 2 ó 3 enlaces dobles.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862734424P | 2018-09-21 | 2018-09-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR116474A1 true AR116474A1 (es) | 2021-05-12 |
Family
ID=69885310
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP190102685A AR116474A1 (es) | 2018-09-21 | 2019-09-20 | DERIVADOS DEL ÁCIDO 6,7-DIHIDRO-2H-BENZOFURO[2,3-a]QUINOLIZIN-3-CARBOXÍLICO COMO AGENTES ANTIVIRALES PARA EL TRATAMIENTO O PREVENCIÓN DE UNA INFECCIÓN POR HBV |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US10865211B2 (es) |
| EP (1) | EP3852751A4 (es) |
| JP (1) | JP2022500466A (es) |
| KR (1) | KR20210065965A (es) |
| CN (1) | CN112955142A (es) |
| AR (1) | AR116474A1 (es) |
| AU (1) | AU2019342750A1 (es) |
| BR (1) | BR112021005091A2 (es) |
| CA (1) | CA3113235A1 (es) |
| IL (1) | IL281564A (es) |
| MX (1) | MX2021003253A (es) |
| TW (1) | TW202024093A (es) |
| UY (1) | UY38383A (es) |
| WO (1) | WO2020061435A1 (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109069488B (zh) | 2016-03-07 | 2021-09-07 | 英安塔制药有限公司 | 乙型肝炎抗病毒剂 |
| IL272941B2 (en) | 2017-08-28 | 2023-03-01 | Enanta Pharm Inc | Antiviral agents for viral hepatitis b |
| WO2020043080A1 (en) | 2018-08-28 | 2020-03-05 | Sunshine Lake Pharma Co., Ltd. | Fused tricyclic compounds and uses thereof in medicine |
| KR20210065965A (ko) | 2018-09-21 | 2021-06-04 | 이난타 파마슈티칼스, 인코포레이티드 | 항바이러스제로서 작용화된 헤테로사이클 |
| KR20210069680A (ko) | 2018-09-30 | 2021-06-11 | 선샤인 레이크 파르마 컴퍼니 리미티드 | 융합된 사환형 화합물 및 약물에서의 이의 용도 |
| US11198693B2 (en) | 2018-11-21 | 2021-12-14 | Enanta Pharmaceuticals, Inc. | Functionalized heterocycles as antiviral agents |
| US11738019B2 (en) | 2019-07-11 | 2023-08-29 | Enanta Pharmaceuticals, Inc. | Substituted heterocycles as antiviral agents |
| US11236108B2 (en) | 2019-09-17 | 2022-02-01 | Enanta Pharmaceuticals, Inc. | Functionalized heterocycles as antiviral agents |
| WO2021188414A1 (en) | 2020-03-16 | 2021-09-23 | Enanta Pharmaceuticals, Inc. | Functionalized heterocyclic compounds as antiviral agents |
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