AR126929A1 - Formas sólidas de ácido 2-[(4-{6-[(4-ciano-2-fluorobencil)oxi]piridin-2-il}piperidin-1-il)metil]-1-[(2s)-oxetan-2-ilmetil]-1h-bencimidazol-6-carboxílico, sal de 1,3-dihidroxi-2-(hidroximetil)propan-2-amina - Google Patents
Formas sólidas de ácido 2-[(4-{6-[(4-ciano-2-fluorobencil)oxi]piridin-2-il}piperidin-1-il)metil]-1-[(2s)-oxetan-2-ilmetil]-1h-bencimidazol-6-carboxílico, sal de 1,3-dihidroxi-2-(hidroximetil)propan-2-aminaInfo
- Publication number
- AR126929A1 AR126929A1 ARP220102349A ARP220102349A AR126929A1 AR 126929 A1 AR126929 A1 AR 126929A1 AR P220102349 A ARP220102349 A AR P220102349A AR P220102349 A ARP220102349 A AR P220102349A AR 126929 A1 AR126929 A1 AR 126929A1
- Authority
- AR
- Argentina
- Prior art keywords
- oxetan
- fluorobenzyl
- propan
- benzimidazole
- pyridin
- Prior art date
Links
- -1 4-CYANO-2-FLUOROBENZYL Chemical class 0.000 title abstract 4
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical class OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 title abstract 4
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 title 1
- 239000011973 solid acid Substances 0.000 title 1
- 239000002253 acid Substances 0.000 abstract 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 229910002483 Cu Ka Inorganic materials 0.000 abstract 1
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 abstract 1
- 102100032882 Glucagon-like peptide 1 receptor Human genes 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000001144 powder X-ray diffraction data Methods 0.000 abstract 1
- 230000005855 radiation Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000007787 solid Substances 0.000 abstract 1
- 238000001228 spectrum Methods 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/68—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings and hydroxy groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
- C07C215/70—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings and hydroxy groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Formas sólidas de ácido 2-[(4-{6-[(4-ciano-2-fluorobencil)oxi]piridin-2-il}piperidin1-il)metil]-1-[(2S)-oxetan-2-ilmetil]-1H-bencimidazol-6-carboxílico, sal de 1,3-dihidroxi-2-(hidroximetil)propan-2-amina, por ejemplo, Forma 1 o Forma 2; así como también composiciones farmacéuticas, y los usos de estas para el tratamiento de enfermedades, afecciones o trastornos modulados por GLP-1R en un mamífero, tal como un ser humano. Reivindicación 1: Una forma cristalina de ácido 2-[(4-{6-[(4-ciano-2-fluorobencil)oxi]piridin-2-il}piperidin-1-il)metil]-1-[(2S)-oxetan-2-ilmetil]-1H-bencimidazol-6-carboxílico, sal de 1,3-dihidroxi-2-(hidroximetil)propan-2-amina, caracterizada porque la forma cristalina es la Forma 1, y en donde la forma cristalina tiene una pureza mayor de 90%. Reivindicación 2: La forma cristalina de acuerdo con la reivindicación 1, y caracterizada porque la forma cristalina tiene un patrón de difracción de rayos X de polvo (PXRD) que comprende un pico, en términos de 2q (fuente de radiación Cu Ka, longitud de onda de 1,5406 Å), seleccionado de aquellos a 14,3 ± 0,2º, 17,5 ± 0,2º y 18,0 ± 0,2º. Reivindicación 11: Una forma amorfa de ácido 2-[(4-{6-[(4-ciano-2-fluorobencil)oxi]piridin-2-il}piperidin-1-il)metil]-1-[(2S)-oxetan-2-ilmetil]-1H-bencimidazol-6-carboxílico, sal de 1,3-dihidroxi-2-(hidroximetil)propan-2-amina, caracterizada porque la amorfa es la Forma 2, y en donde la forma amorfa tiene una pureza mayor de 90%. Reivindicación 12: La forma amorfa de acuerdo con la reivindicación 11, caracterizada porque la forma amorfa tiene un espectro ¹³C ssRMN que comprende un pico, en términos de desplazamientos químicos, seleccionado de aquellos a 174,0 ± 0,2 ppm, 143,9 ± 0,3 ppm y 62,2 ± 0,3 ppm.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202163239056P | 2021-08-31 | 2021-08-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR126929A1 true AR126929A1 (es) | 2023-11-29 |
Family
ID=83283403
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP220102349A AR126929A1 (es) | 2021-08-31 | 2022-08-30 | Formas sólidas de ácido 2-[(4-{6-[(4-ciano-2-fluorobencil)oxi]piridin-2-il}piperidin-1-il)metil]-1-[(2s)-oxetan-2-ilmetil]-1h-bencimidazol-6-carboxílico, sal de 1,3-dihidroxi-2-(hidroximetil)propan-2-amina |
Country Status (10)
| Country | Link |
|---|---|
| EP (1) | EP4396182A1 (es) |
| JP (1) | JP2023035972A (es) |
| KR (1) | KR20240054335A (es) |
| CN (1) | CN117940422A (es) |
| AR (1) | AR126929A1 (es) |
| AU (1) | AU2022336407A1 (es) |
| BR (1) | BR112024002129A2 (es) |
| CA (1) | CA3230347A1 (es) |
| TW (1) | TWI831350B (es) |
| WO (1) | WO2023031741A1 (es) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12024507B2 (en) | 2021-10-25 | 2024-07-02 | Terns Pharmaceuticals, Inc. | Compounds as GLP-1R agonists |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| US4485045A (en) | 1981-07-06 | 1984-11-27 | Research Corporation | Synthetic phosphatidyl cholines useful in forming liposomes |
| US4544545A (en) | 1983-06-20 | 1985-10-01 | Trustees University Of Massachusetts | Liposomes containing modified cholesterol for organ targeting |
| US5013556A (en) | 1989-10-20 | 1991-05-07 | Liposome Technology, Inc. | Liposomes with enhanced circulation time |
| ES2602111T3 (es) | 2010-09-30 | 2017-02-17 | Pfizer Inc | Inhibidores de acetil-CoA carboxilasas de N1-pirazoloespirocetona |
| CU24152B1 (es) | 2010-12-20 | 2016-02-29 | Irm Llc | 1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr |
| MX2018007755A (es) | 2015-12-29 | 2018-11-09 | Pfizer | 3-azabiciclo[3.1.0]hexanos sustituidos como inhibidores de cetohexoquinasa. |
| AR109179A1 (es) | 2016-08-19 | 2018-11-07 | Pfizer | Inhibidores de diacilglicerol aciltransferasa 2 |
| PE20191501A1 (es) | 2016-12-16 | 2019-10-22 | Pfizer | Agonistas receptores de glp-1 y sus usos de los mismos |
| AU2018372109B2 (en) | 2017-11-21 | 2021-07-01 | Pfizer Inc. | Crystalline 2-amino-2-(hydroxymethyl)propane-1,3-diol salt of 4-(4-(1-isopropyl-7-oxo-1,4,6,7-tetrahydrospiro(indazole-5,4'-piperidine)-1'-carbonyl)-6-methoxypyridin-2-yl)benzoic acid |
| US20220387402A1 (en) * | 2019-05-20 | 2022-12-08 | Pfizer Inc. | Combinations comprising benzodioxol as glp-1r agonists for use in the treatment of nash/nafld and related diseases |
-
2022
- 2022-08-25 CA CA3230347A patent/CA3230347A1/en active Pending
- 2022-08-25 CN CN202280058596.3A patent/CN117940422A/zh active Pending
- 2022-08-25 KR KR1020247010668A patent/KR20240054335A/ko unknown
- 2022-08-25 AU AU2022336407A patent/AU2022336407A1/en active Pending
- 2022-08-25 EP EP22769388.4A patent/EP4396182A1/en active Pending
- 2022-08-25 WO PCT/IB2022/057973 patent/WO2023031741A1/en active Application Filing
- 2022-08-25 BR BR112024002129A patent/BR112024002129A2/pt unknown
- 2022-08-29 JP JP2022135473A patent/JP2023035972A/ja active Pending
- 2022-08-30 AR ARP220102349A patent/AR126929A1/es unknown
- 2022-08-30 TW TW111132626A patent/TWI831350B/zh active
Also Published As
| Publication number | Publication date |
|---|---|
| TWI831350B (zh) | 2024-02-01 |
| CA3230347A1 (en) | 2023-03-09 |
| BR112024002129A2 (pt) | 2024-04-30 |
| AU2022336407A1 (en) | 2024-02-22 |
| EP4396182A1 (en) | 2024-07-10 |
| CN117940422A (zh) | 2024-04-26 |
| TW202313595A (zh) | 2023-04-01 |
| JP2023035972A (ja) | 2023-03-13 |
| KR20240054335A (ko) | 2024-04-25 |
| WO2023031741A1 (en) | 2023-03-09 |
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