AR112402A1 - Dihidrooxadiazinonas - Google Patents
DihidrooxadiazinonasInfo
- Publication number
- AR112402A1 AR112402A1 ARP180102218A AR112402A1 AR 112402 A1 AR112402 A1 AR 112402A1 AR P180102218 A ARP180102218 A AR P180102218A AR 112402 A1 AR112402 A1 AR 112402A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- alkyl
- optionally substituted
- independently selected
- substituents
- Prior art date
Links
- 125000001424 substituent group Chemical group 0.000 abstract 16
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 11
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 11
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 8
- 125000005843 halogen group Chemical group 0.000 abstract 7
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 7
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 5
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 4
- 125000004043 oxo group Chemical group O=* 0.000 abstract 4
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000002950 monocyclic group Chemical group 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- -1 4-pyridinyl Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
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- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines having two or more nitrogen atoms in the same ring, e.g. oxadiazines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
- C07D273/02—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00 having two nitrogen atoms and only one oxygen atom
- C07D273/04—Six-membered rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- 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
- 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
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Catalysts (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Reivindicación 1: Un compuesto de la fórmula (1), caracterizado porque R¹ se selecciona de un átomo de hidrógeno, un átomo de halógeno, un grupo ciano, un grupo alquilo-C₁₋₃, un grupo haloalquilo-C₁₋₃, y un grupo haloalcoxi-C₁₋₃; R² se selecciona de un átomo de hidrógeno, y un átomo de halógeno; R³ se selecciona de, un grupo alquilo-C₁₋₆ que está opcionalmente sustituido con uno o dos sustituyentes y cada sustituyente se selecciona independientemente de un grupo hidroxi, un grupo alcoxi-C₁₋₄, y un grupo heterocicloalquilo de 3 a 7 miembros; un grupo alquenilo-C₂₋₆, que está opcionalmente sustituido con un grupo alcoxi-C₁₋₄; un grupo cicloalquilo-C₃₋₉, que está opcionalmente sustituido con un grupo hidroxi; un grupo cicloalquenilo-C₅₋₉, que está opcionalmente sustituido con un grupo hidroxi; un grupo heterocicloalquilo de 3 a 9 miembros, que comprende uno, dos o tres heteroátomos que independientemente se seleccionan de -O-, -S-, -S(O)-, S(O)₂, y -NR⁹-, y dicho grupo heterocicloalquilo además comprende opcionalmente un grupo puente seleccionado de -O-, -NR⁹-, -CH₂-, -CH₂-CH₂-, -O-CH₂-, -CH₂-O-, -NR⁹-CH₂-, y -CH₂-NR⁹-; y dicho grupo heterocicloalquilo está opcionalmente sustituido con uno, dos o tres sustituyentes y cada sustituyente se selecciona independientemente de un átomo de halógeno; un grupo oxo (=O); un grupo ciano; un grupo hidroxi; un grupo alquilo-C₁₋₃, que además está opcionalmente sustituido con un grupo hidroxi; un grupo haloalquilo-C₁₋₃; un grupo alcoxi C₁₋₃; un grupo haloalcoxi-C₁₋₃; un grupo C(O)NR⁵R⁶; y un grupo NR⁵R⁶; un grupo heterocicloalquilo de 5 a 9 miembros que está parcialmente insaturado y opcionalmente sustituido con uno, dos o tres sustituyentes y cada sustituyente se selecciona independientemente de un grupo oxo (=O), un grupo alquilo-C₁₋₃, un grupo -C(O)R⁵R⁶ y un átomo de halógeno; un grupo arilo que está opcionalmente sustituido con uno, dos, tres o cuatro sustituyentes y cada sustituyente se selecciona independientemente de un átomo de halógeno, un grupo hidroxi, un grupo ciano, un grupo alquilo-C₁₋₃, un grupo haloalquilo-C₁₋₃, un grupo alcoxi-C₁₋₃, un grupo haloalcoxi-C₁₋₃ y un grupo NR⁵R⁶; un grupo heteroarilo mono- o bicíclico que está opcionalmente sustituido con uno, dos o tres sustituyentes y cada sustituyente se selecciona independientemente de un átomo de halógeno, un grupo alquilo-C₁₋₃, un grupo ciano, un grupo haloalquilo-C₁₋₃, un grupo hidroxialquilo-C₁₋₃, un grupo alcoxi-C₁₋₃, un grupo hidroxi y un grupo NR⁵R⁶, con la condición que dicho grupo heteroarilo monocíclico no sea 4-piridinilo; y un grupo NR⁷R⁸; R⁴ se selecciona de un átomo de hidrógeno, y un grupo alquilo-C₁₋₃; R⁵ / R⁶ se seleccionan independientemente de un átomo de hidrógeno, un grupo alquilo-C₁₋₆, un grupo alquileno-C₁₋₅-alquilo-O-C₁₋₅, un grupo alquileno-C₁₋₅-alquilo-S-C₁₋₅, un grupo cicloalquilo-C₃₋₆, y un grupo heterocicloalquilo-C₃₋₅; R⁷ / R⁸ se seleccionan independientemente de un átomo de hidrógeno, con la condición que R⁷ = R⁸ = el hidrógeno esté excluido, un grupo alquilo-C₁₋₆, que está opcionalmente sustituido con uno, dos, tres o cuatro sustituyentes y dicho sustituyente se selecciona independientemente de un átomo de halógeno, un grupo ciano, un grupo hidroxi, un grupo C(O)NR⁵R⁶, un grupo NR⁵R⁶, un grupo alcoxi-C₁₋₃, un grupo cicloalquilo-C₃₋₇ que está opcionalmente sustituido con uno o dos sustituyentes y dichos sustituyentes se seleccionan independientemente de un grupo alquilo-C₁₋₃, un grupo oxo (=O), un grupo hidroxi y un grupo hidroxialquilo-C₁₋₃; un grupo heterocicloalquilo de 3 a 7 miembros que está opcionalmente sustituido con un grupo alquilo-C₁₋₃, o un grupo oxo (=O); un grupo heteroarilo, que está opcionalmente sustituido con un grupo alquilo-C₁₋₃; un grupo alquileno-C₁₋₅-alquilo-O-C₁₋₅; un grupo alquileno-C₁₋₅-alquilo-S-C₁₋₅; un grupo alquileno-C₁₋₅-alquilo-NR⁵-C₁₋₅; un grupo cicloalquilo-C₃₋₆ que está opcionalmente sustituido con un grupo hidroxi; y un grupo heterocicloalquilo de 3 a 6 miembros, que está opcionalmente sustituido con uno o dos sustituyentes, dicho sustituyente se selecciona independientemente de un grupo alquilo-C₁₋₃ y un grupo hidroxi; R⁹ es un átomo de hidrógeno o un grupo alquilo-C₁₋₃ o un enlace; o un estereoisómero, un tautómero, un N-óxido, un hidrato, un solvato, o una sal de los mismos, o una mezcla de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762541627P | 2017-08-04 | 2017-08-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR112402A1 true AR112402A1 (es) | 2019-10-23 |
Family
ID=63207725
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP180102218 AR112402A1 (es) | 2017-08-04 | 2018-08-03 | Dihidrooxadiazinonas |
Country Status (26)
| Country | Link |
|---|---|
| US (3) | US11427553B2 (es) |
| EP (1) | EP3661517B1 (es) |
| JP (2) | JP7676141B2 (es) |
| KR (1) | KR20200036914A (es) |
| CN (1) | CN111212647B (es) |
| AR (1) | AR112402A1 (es) |
| AU (1) | AU2018309356B2 (es) |
| BR (1) | BR112020002351A2 (es) |
| CA (1) | CA3071800A1 (es) |
| CL (1) | CL2020000303A1 (es) |
| CO (1) | CO2020001242A2 (es) |
| CR (1) | CR20200057A (es) |
| CU (1) | CU24608B1 (es) |
| EA (1) | EA202090448A1 (es) |
| EC (1) | ECSP20008441A (es) |
| IL (1) | IL272098B2 (es) |
| JO (1) | JOP20200024A1 (es) |
| MA (1) | MA49750A (es) |
| MX (1) | MX2020001404A (es) |
| PE (1) | PE20200936A1 (es) |
| PH (1) | PH12020500134A1 (es) |
| SG (1) | SG11201913775UA (es) |
| TW (1) | TWI791581B (es) |
| UA (1) | UA125731C2 (es) |
| UY (1) | UY37832A (es) |
| WO (1) | WO2019025562A1 (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JOP20200024A1 (ar) | 2017-08-04 | 2020-02-02 | Bayer Ag | مركبات ثنائي هيدروكساديازينون |
| EP3661917B1 (en) | 2017-08-04 | 2022-05-11 | Bayer Aktiengesellschaft | 6-((3-trifluoromethyl)phenyl)-4,5-dihydropyridazin-3(2h)-one derivatives as pde3a and pde3b inhibitors for treating cancer |
| TW202031677A (zh) | 2018-11-01 | 2020-09-01 | 美商博得學院股份有限公司 | Ｐｄｅ３調節劑反應性癌症之鑑定 |
| WO2020157188A1 (en) * | 2019-02-01 | 2020-08-06 | Bayer Aktiengesellschaft | Dihydrooxadiazinones for the treatment of hyperproliferative diseases |
| TWI750573B (zh) | 2019-02-01 | 2021-12-21 | 德商拜耳廠股份有限公司 | 1,2,4-三-3(2h)-酮化合物 |
| JP2024508171A (ja) * | 2021-03-03 | 2024-02-22 | バイエル アクチェンゲゼルシャフト | 肉腫の処置のための置換３，６－ジヒドロ－２ｈ－１，３，４－オキサジアジン－２－オン |
| EP4289829A1 (en) | 2022-06-10 | 2023-12-13 | Bayer Aktiengesellschaft | Crystalline forms of (6s)-5-[4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-6-methyl-3,6-dihydro- 2h-1,3,4-oxadiazin-2-one |
| EP4289828A1 (en) | 2022-06-10 | 2023-12-13 | Bayer Aktiengesellschaft | Method for the preparation of a 3,6-dihydro-2h-1,3,4-oxadiazin-2-one |
| WO2024109919A1 (zh) * | 2022-11-24 | 2024-05-30 | 盛睿泽华医药科技（苏州）有限公司 | 吡啶酮化合物及其制备方法和用途 |
| CN117903077B (zh) * | 2023-01-13 | 2024-09-03 | 上海超阳药业有限公司 | 二氢噁二嗪酮化合物及其应用 |
| CN118420559B (zh) * | 2023-04-27 | 2025-02-14 | 上海超阳药业有限公司 | 氘代噁二嗪酮化合物及其用途 |
| CN118047833B (zh) * | 2024-01-31 | 2025-03-14 | 海南大学 | 含二茂铁的取代氨基乙酰胺类化合物及其制备方法和应用 |
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| CN108883112B (zh) | 2016-02-05 | 2022-07-26 | 拜耳医药股份公司 | 用于癌症患者分级和癌症治疗的化合物、组合物和方法 |
| KR101831772B1 (ko) * | 2016-03-24 | 2018-03-06 | 아이디에스(주) | 복합 광원 모듈을 가지는 카메라 접사용 기구 및 이를 이용한 지문 시편 촬영 방법 |
| TWI808055B (zh) | 2016-05-11 | 2023-07-11 | 美商滬亞生物國際有限公司 | Hdac 抑制劑與 pd-1 抑制劑之組合治療 |
| TWI794171B (zh) | 2016-05-11 | 2023-03-01 | 美商滬亞生物國際有限公司 | Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療 |
| EP3661917B1 (en) | 2017-08-04 | 2022-05-11 | Bayer Aktiengesellschaft | 6-((3-trifluoromethyl)phenyl)-4,5-dihydropyridazin-3(2h)-one derivatives as pde3a and pde3b inhibitors for treating cancer |
| JOP20200024A1 (ar) | 2017-08-04 | 2020-02-02 | Bayer Ag | مركبات ثنائي هيدروكساديازينون |
| TW202031677A (zh) | 2018-11-01 | 2020-09-01 | 美商博得學院股份有限公司 | Ｐｄｅ３調節劑反應性癌症之鑑定 |
| TWI750573B (zh) | 2019-02-01 | 2021-12-21 | 德商拜耳廠股份有限公司 | 1,2,4-三-3(2h)-酮化合物 |
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