AR123582A1 - Triazinonas inhibidores de la producción de inflamasoma de nlrp3 - Google Patents
Triazinonas inhibidores de la producción de inflamasoma de nlrp3Info
- Publication number
- AR123582A1 AR123582A1 ARP210102642A ARP210102642A AR123582A1 AR 123582 A1 AR123582 A1 AR 123582A1 AR P210102642 A ARP210102642 A AR P210102642A AR P210102642 A ARP210102642 A AR P210102642A AR 123582 A1 AR123582 A1 AR 123582A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- formula
- optionally substituted
- compound
- 3alkyl
- Prior art date
Links
- QMNWYGTWTXOQTP-UHFFFAOYSA-N 1h-triazin-6-one Chemical compound O=C1C=CN=NN1 QMNWYGTWTXOQTP-UHFFFAOYSA-N 0.000 title 1
- 102000000874 Pyrin Domain-Containing 3 Protein NLR Family Human genes 0.000 title 1
- 108010001946 Pyrin Domain-Containing 3 Protein NLR Family Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 8
- 150000001875 compounds Chemical class 0.000 abstract 7
- 125000001424 substituent group Chemical group 0.000 abstract 5
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 4
- 125000001475 halogen functional group Chemical group 0.000 abstract 4
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 abstract 2
- 238000006243 chemical reaction Methods 0.000 abstract 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 238000010640 amide synthesis reaction Methods 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000009466 transformation Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/28—Cinnolines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- 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
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Physical Education & Sports Medicine (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Neurosurgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable de este, en donde: R¹ representa: (i) cicloalquilo C₃₋₆ opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de -OH, -alquilo C₁₋₃ e hidroxialquilo C₁₋₃; (ii) arilo o heteroarilo, cada uno de los cuales está opcionalmente sustituido con 1 a 3 sustituyentes seleccionados independientemente de halo, =O, -OH, -O-alquilo C₁₋₃, -alquilo C₁₋₃, haloalquilo C₁₋₃, hidroxialquilo C₁₋₃, alcoxi C₁₋₃, haloalcoxi C₁₋₃; o (iii) heterociclilo, opcionalmente sustituido con 1 a 3 sustituyentes seleccionados independientemente de =O, alquilo C₁₋₃ y cicloalquilo C₃₋₆; R² representa: (i) alquilo C₁₋₃ opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de halo, -OH y -O-alquilo C₁₋₃; (ii) cicloalquilo C₃₋₆; o (iii) alquenilo C₂₋₄ opcionalmente sustituido con -O-alquilo C₁₋₃; R³ representa: (i) hidrógeno; (ii) halo; (iii) alquilo C₁₋₄ opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de halo, -OH y -O-alquilo C₁₋₃; (iv) alquenilo C₂₋₄ opcionalmente sustituido con -O-alquilo C₁₋₃; (v) cicloalquilo C₃₋₆; o (vi) -O-alquilo C₁₋₃. Reivindicación 18: Un proceso para la preparación de un compuesto de fórmula (1) de acuerdo con cualquiera de las reivindicaciones 1 a 10, que comprende: (i) la reacción de un compuesto de fórmula (2), o un derivado de este, en donde R² y R³ son como se definen en la reivindicación 1, con un compuesto de fórmula (3), H₂N-R¹ (3) o un derivado de este, en donde R¹ es como se define en la reivindicación 1, en condiciones de reacción de formación de amida; (ii) la reacción de un compuesto de fórmula (4), en donde R¹ y R³ son como se definen en la reivindicación 1, con un compuesto de fórmula (5), R²-LGᵃ (5) en donde LGᵃ representa un grupo saliente adecuado y R² es como se define en la reivindicación 1; (iii) mediante transformación de un cierto compuesto de formula (1) en otro.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP20382845.4A EP3974415A1 (en) | 2020-09-24 | 2020-09-24 | Nlrp3 modulators |
Publications (1)
Publication Number | Publication Date |
---|---|
AR123582A1 true AR123582A1 (es) | 2022-12-21 |
Family
ID=72709314
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP210102642A AR123582A1 (es) | 2020-09-24 | 2021-09-23 | Triazinonas inhibidores de la producción de inflamasoma de nlrp3 |
Country Status (13)
Country | Link |
---|---|
US (1) | US20230391756A1 (es) |
EP (2) | EP3974415A1 (es) |
JP (1) | JP2023542231A (es) |
KR (1) | KR20230074199A (es) |
CN (1) | CN116323585A (es) |
AR (1) | AR123582A1 (es) |
AU (1) | AU2021346843A1 (es) |
BR (1) | BR112023005214A2 (es) |
CA (1) | CA3192262A1 (es) |
MX (1) | MX2023003458A (es) |
TW (1) | TW202229244A (es) |
UY (1) | UY39434A (es) |
WO (1) | WO2022063876A1 (es) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2024057013A1 (en) | 2022-09-12 | 2024-03-21 | Exscientia Ai Limited | Nlrp3 modulators |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB201710851D0 (en) * | 2017-07-06 | 2017-08-23 | Galápagos Nv | Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis |
US11718631B2 (en) | 2017-10-17 | 2023-08-08 | Novartis Ag | Sulphonamides and compositions thereof for treating conditions associated with NLRP activity |
GB201721185D0 (en) | 2017-12-18 | 2018-01-31 | Nodthera Ltd | Sulphonyl urea derivatives |
GB201803393D0 (en) | 2018-03-02 | 2018-04-18 | Inflazome Ltd | Novel compounds |
CN112584899A (zh) | 2018-07-03 | 2021-03-30 | 诺华股份有限公司 | Nlrp调节剂 |
CN112513048A (zh) | 2018-07-20 | 2021-03-16 | 豪夫迈·罗氏有限公司 | 作为白细胞介素-1活性抑制剂的磺酰亚胺酰胺类化合物 |
CN112424207B (zh) | 2018-07-25 | 2024-03-19 | 诺华股份有限公司 | Nlrp3炎性小体抑制剂 |
US20220098188A1 (en) | 2018-08-17 | 2022-03-31 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Small molecule pyrin-domain targeted nlrp3 inflammasome inhibitors |
-
2020
- 2020-09-24 EP EP20382845.4A patent/EP3974415A1/en not_active Ceased
-
2021
- 2021-09-23 AU AU2021346843A patent/AU2021346843A1/en active Pending
- 2021-09-23 WO PCT/EP2021/076164 patent/WO2022063876A1/en unknown
- 2021-09-23 MX MX2023003458A patent/MX2023003458A/es unknown
- 2021-09-23 CN CN202180064525.XA patent/CN116323585A/zh active Pending
- 2021-09-23 KR KR1020237013218A patent/KR20230074199A/ko unknown
- 2021-09-23 AR ARP210102642A patent/AR123582A1/es unknown
- 2021-09-23 BR BR112023005214A patent/BR112023005214A2/pt unknown
- 2021-09-23 UY UY0001039434A patent/UY39434A/es unknown
- 2021-09-23 US US18/245,765 patent/US20230391756A1/en active Pending
- 2021-09-23 CA CA3192262A patent/CA3192262A1/en active Pending
- 2021-09-23 TW TW110135274A patent/TW202229244A/zh unknown
- 2021-09-23 EP EP21777807.5A patent/EP4217346A1/en active Pending
- 2021-09-23 JP JP2023518741A patent/JP2023542231A/ja active Pending
Also Published As
Publication number | Publication date |
---|---|
EP3974415A1 (en) | 2022-03-30 |
US20230391756A1 (en) | 2023-12-07 |
CA3192262A1 (en) | 2022-03-31 |
EP4217346A1 (en) | 2023-08-02 |
KR20230074199A (ko) | 2023-05-26 |
UY39434A (es) | 2022-03-31 |
BR112023005214A2 (pt) | 2023-04-25 |
JP2023542231A (ja) | 2023-10-05 |
TW202229244A (zh) | 2022-08-01 |
AU2021346843A1 (en) | 2023-06-08 |
AU2021346843A9 (en) | 2024-02-08 |
MX2023003458A (es) | 2023-04-19 |
CN116323585A (zh) | 2023-06-23 |
WO2022063876A1 (en) | 2022-03-31 |
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