AR128053A1 - Sal derivada de triazolona como inhibidor de elastasa de neutrófilos - Google Patents
Sal derivada de triazolona como inhibidor de elastasa de neutrófilosInfo
- Publication number
- AR128053A1 AR128053A1 ARP220103535A ARP220103535A AR128053A1 AR 128053 A1 AR128053 A1 AR 128053A1 AR P220103535 A ARP220103535 A AR P220103535A AR P220103535 A ARP220103535 A AR P220103535A AR 128053 A1 AR128053 A1 AR 128053A1
- Authority
- AR
- Argentina
- Prior art keywords
- formula
- compound
- phenyl
- triazolone
- crystalline form
- Prior art date
Links
- 150000003839 salts Chemical class 0.000 title abstract 4
- FFSJPOPLSWBGQY-UHFFFAOYSA-N triazol-4-one Chemical compound O=C1C=NN=N1 FFSJPOPLSWBGQY-UHFFFAOYSA-N 0.000 title abstract 3
- 102000002255 Secretory Proteinase Inhibitory Proteins Human genes 0.000 title 1
- 108010000303 Secretory Proteinase Inhibitory Proteins Proteins 0.000 title 1
- 239000003591 leukocyte elastase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 5
- 238000000034 method Methods 0.000 abstract 4
- IHTRPSMRGYWUIM-HSZRJFAPSA-O 2-[5-cyano-2-[(5r)-6-methoxycarbonyl-7-methyl-3-oxo-8-[3-(trifluoromethyl)phenyl]-2,5-dihydro-[1,2,4]triazolo[4,3-a]pyrimidin-5-yl]phenyl]ethyl-trimethylazanium Chemical compound C1([C@H]2N3C(=O)NN=C3N(C(C)=C2C(=O)OC)C=2C=C(C=CC=2)C(F)(F)F)=CC=C(C#N)C=C1CC[N+](C)(C)C IHTRPSMRGYWUIM-HSZRJFAPSA-O 0.000 abstract 3
- 229950000339 xinafoate Drugs 0.000 abstract 3
- 229910002483 Cu Ka Inorganic materials 0.000 abstract 1
- 108010028275 Leukocyte Elastase Proteins 0.000 abstract 1
- 102000016799 Leukocyte elastase Human genes 0.000 abstract 1
- 229910052784 alkaline earth metal Inorganic materials 0.000 abstract 1
- -1 alkaline earth metal cation Chemical class 0.000 abstract 1
- 150000001449 anionic compounds Chemical class 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 238000002425 crystallisation Methods 0.000 abstract 1
- 230000008025 crystallization Effects 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 229910001412 inorganic anion Inorganic materials 0.000 abstract 1
- 150000002891 organic anions Chemical class 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 230000005855 radiation Effects 0.000 abstract 1
- 239000012266 salt solution Substances 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C65/01—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups
- C07C65/105—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic
- C07C65/11—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic with carboxyl groups on a condensed ring system containing two rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2602/00—Systems containing two condensed rings
- C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
- C07C2602/04—One of the condensed rings being a six-membered aromatic ring
- C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (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 That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La presente invención se refiere, en general, a una novedosa sal derivada de triazolona particularmente útil como inhibidor de elastasa de neutrófilos y a su uso como medicamento, la invención también se refiere a su proceso de síntesis y sus composiciones farmacéuticas. La invención también se refiere al proceso para aislar mediante cristalización el compuesto (1). La invención también se refiere a una forma cristalina de un compuesto de fórmula (1). Reivindicación 1: El compuesto xinafoato de (2-{5-ciano-2-[(R)-6-metoxicarbonil-7-metil-3-oxo-8-(3-trifluorometil-fenil)-2,3,5,8-tetrahidro-[1,2,4]triazolo[4,3-a]pirimidin-5-il]-fenil}-etil)-trimetil-amonio de fórmula (1). Reivindicación 2: Un proceso para la preparación del compuesto de fórmula (1) según la reivindicación 1, al hacer reaccionar el derivado de triazolona de fórmula (2) con la sal de xinafoato de fórmula (3) dicho proceso comprende los pasos de: 1) disolver en agua sal de (2-{5-ciano-2-[(R)-6-metoxicarbonil-7-metil-3-oxo-8-(3-trifluorometil-fenil)-2,3,5,8-tetrahidro-[1,2,4]triazolo[4,3-a]pirimidin-5-il]-fenil}-etil)-trimetil-amonio (2) caracterizado porque X⁻ es un anión orgánico o inorgánico, 2) agregar una solución de sal de xinafoato de fórmula (3) donde Y⁺ es un alcalino o catión metálico alcalinotérreo. Reivindicación 6: Una forma cristalina de un compuesto de fórmula (1), caracterizada porque dicha forma cristalina caracterizada por al menos uno de los siguientes picos de XRPD: 8,6, 9,9 y 23,2 ± 0,2 grados/2q [radiación Cu Ka (l = 1,5406 Å)].
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP21217146 | 2021-12-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR128053A1 true AR128053A1 (es) | 2024-03-20 |
Family
ID=79025003
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP220103535A AR128053A1 (es) | 2021-12-22 | 2022-12-21 | Sal derivada de triazolona como inhibidor de elastasa de neutrófilos |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US20250059195A1 (es) |
| EP (1) | EP4452980A1 (es) |
| JP (1) | JP2025500406A (es) |
| KR (1) | KR20240124375A (es) |
| CN (1) | CN118434738A (es) |
| AR (1) | AR128053A1 (es) |
| AU (1) | AU2022420749A1 (es) |
| CA (1) | CA3241713A1 (es) |
| CL (1) | CL2024001852A1 (es) |
| CO (1) | CO2024009342A2 (es) |
| GE (1) | GEAP202416568A (es) |
| IL (1) | IL313643A (es) |
| MX (1) | MX2024007587A (es) |
| PE (1) | PE20241624A1 (es) |
| TW (1) | TW202340195A (es) |
| WO (1) | WO2023118252A1 (es) |
| ZA (1) | ZA202405639B (es) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2022234302A1 (en) | 2021-03-10 | 2023-10-12 | Jnana Therapeutics Inc. | Small molecule inhibitors of mammalian slc6a19 function |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU650953B2 (en) | 1991-03-21 | 1994-07-07 | Novartis Ag | Inhaler |
| GB201004179D0 (en) | 2010-03-12 | 2010-04-28 | Pulmagen Therapeutics Inflamma | Enzyme inhibitors |
| GB201004178D0 (en) | 2010-03-12 | 2010-04-28 | Pulmagen Therapeutics Inflamma | Enzyme inhibitors |
| ES2700226T3 (es) | 2012-12-18 | 2019-02-14 | Chiesi Farm Spa | Derivados de 3-oxo-2,3,5,8-tetrahidro-[1,2,4]triazolo[4,3-a]pirimidina para el tratamiento de enfermedades respiratorias |
-
2022
- 2022-12-21 AR ARP220103535A patent/AR128053A1/es unknown
- 2022-12-21 JP JP2024537882A patent/JP2025500406A/ja active Pending
- 2022-12-21 PE PE2024001388A patent/PE20241624A1/es unknown
- 2022-12-21 KR KR1020247024263A patent/KR20240124375A/ko active Pending
- 2022-12-21 GE GEAP202416568A patent/GEAP202416568A/en unknown
- 2022-12-21 MX MX2024007587A patent/MX2024007587A/es unknown
- 2022-12-21 CA CA3241713A patent/CA3241713A1/en active Pending
- 2022-12-21 EP EP22843260.5A patent/EP4452980A1/en active Pending
- 2022-12-21 TW TW111149083A patent/TW202340195A/zh unknown
- 2022-12-21 IL IL313643A patent/IL313643A/en unknown
- 2022-12-21 US US18/720,015 patent/US20250059195A1/en active Pending
- 2022-12-21 WO PCT/EP2022/087155 patent/WO2023118252A1/en not_active Ceased
- 2022-12-21 CN CN202280083759.3A patent/CN118434738A/zh active Pending
- 2022-12-21 AU AU2022420749A patent/AU2022420749A1/en active Pending
-
2024
- 2024-06-19 CL CL2024001852A patent/CL2024001852A1/es unknown
- 2024-07-15 CO CONC2024/0009342A patent/CO2024009342A2/es unknown
- 2024-07-19 ZA ZA2024/05639A patent/ZA202405639B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CL2024001852A1 (es) | 2024-09-27 |
| IL313643A (en) | 2024-08-01 |
| KR20240124375A (ko) | 2024-08-16 |
| CO2024009342A2 (es) | 2024-08-08 |
| US20250059195A1 (en) | 2025-02-20 |
| AU2022420749A1 (en) | 2024-08-01 |
| CN118434738A (zh) | 2024-08-02 |
| ZA202405639B (en) | 2025-10-29 |
| MX2024007587A (es) | 2024-07-04 |
| GEAP202416568A (en) | 2024-08-26 |
| JP2025500406A (ja) | 2025-01-09 |
| WO2023118252A1 (en) | 2023-06-29 |
| CA3241713A1 (en) | 2023-06-29 |
| PE20241624A1 (es) | 2024-08-07 |
| TW202340195A (zh) | 2023-10-16 |
| EP4452980A1 (en) | 2024-10-30 |
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