ES2608871T3 - Alafenamide hemifumarate de tenofovir - Google Patents
Alafenamide hemifumarate de tenofovir Download PDFInfo
- Publication number
- ES2608871T3 ES2608871T3 ES12753867.6T ES12753867T ES2608871T3 ES 2608871 T3 ES2608871 T3 ES 2608871T3 ES 12753867 T ES12753867 T ES 12753867T ES 2608871 T3 ES2608871 T3 ES 2608871T3
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- Prior art keywords
- tenofovir alafenamide
- tenofovir
- hemifumarate
- alafenamide
- monofumate
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
- C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed 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
- A61K31/495—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
- A61K31/52—Purines, e.g. adenine
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
- A61K31/685—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
-
- 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
-
- 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
-
- 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
-
- 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
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Molecular Biology (AREA)
- Virology (AREA)
- Epidemiology (AREA)
- Communicable Diseases (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicinal Preparation (AREA)
- Peptides Or Proteins (AREA)
Abstract
Hemifumarato de tenofovir alafenamida.
Description
Datos TGA
[0062] Los datos de TGA se obtuvieron usando 4,161 mg de hemifumarato de tenofovir alafenamida. Se calentó a 10ºC/min en el intervalo de 25-200ºC. La muestra perdió 0,3% de peso antes de la fusión (Fig. 3). Se determinó que es una forma anhidra.
Análisis DVS
[0063] El análisis DVS se realizó utilizando 4,951 mg de hemifumarato de tenofovir alafenamida. El material se mantuvo a 25ºC en nitrógeno a humedades comprendidas entre 10% y 90% de humedad relativa; Cada etapa se equilibró durante 120 minutos. La isoterma de adsorción se muestra en la FIG. 4. Se demostró que el material era no higroscópico, y absorbía 0,65% de agua a una humedad relativa de 90%.
Purga de la impureza diastereomérica
[0064] En las síntesis anteriores de tenofovir alafenamida, una de las principales impurezas es típicamente el diastereómero 9-[(R)-2-[[(R)-[[(S)-1-(isopropoxicarbonilo)etilo]amino]fenoxifosfinilo]metoxi]propilo]adenina. La forma de hemifumarato de tenofovir alafenamida del Ejemplo 3 tiene una capacidad excepcional para purgar esta impureza diastereomérica, en comparación con la capacidad de la forma de monofumarato (descrita en la Patente de Estados Unidos nº 7.390.791). Los datos de la Tabla 2 (a continuación) demuestran que el hemifumarato de tenofovir alafenamida (Lote 2) purgó la impureza diastereomérica a menos de una décima parte de la concentración inicial, mientras que la forma de monofumarato de tenofovir alafenamida (Lote 1) sólo purgó ligeramente la impureza diastereomérica.
Tabla 2. Comparación de capacidades de purga
- Lote
- La impureza diastereomérica en material de partida Solvente Carga de ácido fumárico (equivalente molar) Producto obtenido La impureza diastereomérica de producto
- 1
- 9,3% ACN 0,9 Forma de monofumarato 7,6%
- 2
- 10,0% ACN 0,5 Forma de hemifumarato 0,65%
Estabilidad química
[0065] La estabilidad química de la forma de hemifumarato de tenofovir alafenamida se comparó con la forma de monofumarato. Como se muestra en la Tabla 3 (a continuación), en condiciones idénticas, la forma de hemifumarato de tenofovir alafenamida era químicamente más estable y exhibe una mejor estabilidad de almacenamiento a largo plazo, con significativamente menos degradación (% Deg Total. Productos) que la forma de monofumarato. Condiciones evaluadas incluyen la temperatura, la humedad relativa (RH), y el estado abierto o cerrado de la tapa del recipiente.
Tabla 3. Estabilidad química Comparación
- Condición de almacenamiento
- Puntos de tiempo (semanas) Forma de monofumarato Forma de hemifumarato
- % TA* Área normalizada
- % Total Deg. Productos % TA área normalizada Total% Deg. Productos
- 40°C/75% RH tapa cerrada
- 0 97,1 0,69 98,4 0,05
- 1
- 97,0 0,87 98,4 0,14
- 2
- 96,6 1,18 98,5 0,14
- 4
- 96,4 1,49 98,4 0,25
- 8
- 95,4 2,36 98,0 0,49
- 40°C/75% RH tapa abierta
- 0 97,1 0,69 98,4 0,05
- 1
- 96,9 0,90 98,5 0,15
- 2
- 96,6 1,10 98,5 0,14
- 4
- 96,2 1,67 98,4 0,26
- 8
- 95,0 2,74 98,1 0,50
- 70°C tapa cerrada
- 0 97,1 0,69 98,4 0,05
- 2
- 96,2 1,83 98,5 0,22
- 4
- 93,3 4,78 98,4 0,33
- TA es tenofovir alafenamida
Claims (1)
-
imagen1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161524224P | 2011-08-16 | 2011-08-16 | |
| US201161524224P | 2011-08-16 | ||
| PCT/US2012/050920 WO2013025788A1 (en) | 2011-08-16 | 2012-08-15 | Tenofovir alafenamide hemifumarate |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| ES2608871T3 true ES2608871T3 (es) | 2017-04-17 |
| ES2608871T5 ES2608871T5 (es) | 2024-04-04 |
Family
ID=46785793
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES12753867T Active ES2608871T5 (es) | 2011-08-16 | 2012-08-15 | Alafenamide hemifumarate de tenofovir |
Country Status (41)
Families Citing this family (94)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
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