AR126977A2 - DOSAGE FORM COMPOSITIONS COMPRISING A BRUTON'S TYROSINE KINASE INHIBITOR - Google Patents
DOSAGE FORM COMPOSITIONS COMPRISING A BRUTON'S TYROSINE KINASE INHIBITORInfo
- Publication number
- AR126977A2 AR126977A2 ARP220102392A ARP220102392A AR126977A2 AR 126977 A2 AR126977 A2 AR 126977A2 AR P220102392 A ARP220102392 A AR P220102392A AR P220102392 A ARP220102392 A AR P220102392A AR 126977 A2 AR126977 A2 AR 126977A2
- Authority
- AR
- Argentina
- Prior art keywords
- bruton
- free base
- crystalline salts
- kinase inhibitor
- kinase
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title abstract 2
- 229940125814 BTK kinase inhibitor Drugs 0.000 title 1
- 239000002552 dosage form Substances 0.000 title 1
- 239000012458 free base Substances 0.000 abstract 4
- 150000003839 salts Chemical class 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 abstract 2
- 229920001577 copolymer Polymers 0.000 abstract 2
- 229940043355 kinase inhibitor Drugs 0.000 abstract 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 abstract 2
- 239000007962 solid dispersion Substances 0.000 abstract 2
- 102000001714 Agammaglobulinaemia Tyrosine Kinase Human genes 0.000 abstract 1
- 108010029445 Agammaglobulinaemia Tyrosine Kinase Proteins 0.000 abstract 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 abstract 1
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 abstract 1
- CERQOIWHTDAKMF-UHFFFAOYSA-M Methacrylate Chemical compound CC(=C)C([O-])=O CERQOIWHTDAKMF-UHFFFAOYSA-M 0.000 abstract 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 239000002202 Polyethylene glycol Substances 0.000 abstract 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000001530 fumaric acid Substances 0.000 abstract 1
- 229920000578 graft copolymer Polymers 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- 229920001223 polyethylene glycol Polymers 0.000 abstract 1
- 229920000642 polymer Polymers 0.000 abstract 1
- 229920002689 polyvinyl acetate Polymers 0.000 abstract 1
- 239000011118 polyvinyl acetate Substances 0.000 abstract 1
- 239000007916 tablet composition Substances 0.000 abstract 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 abstract 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La invención se refiere, en general, a composiciones farmacéuticas en comprimido que comprenden ácido fumárico y el compuesto de base libre de (S)-2-(3-(hidroximetil)-1-metil-5-((5-(2-metil-4-(oxetan-3-il)piperazin-1-il)piridin-2-il)amino)-6-oxo-1,6-dihidro-[3,4-bipiridin]-2-il)-7,7-dimetil-2,3,4,6,7,8-hexahidro-1H-ciclopenta[4,5]pirrolo[1,2-a]pirazin-1-ona que es un inhibidor de la tirosina cinasa de Bruton. La invención se refiere además a dispersiones sólidas amorfas que comprenden al menos un polímero y la base libre del compuesto inhibidor de la cinasa de Bruton. La invención se refiere además a sales cristalinas de mesilato, sales cristalinas de cloruro y sales cristalinas de sulfato de la base libre del compuesto inhibidor de la cinasa de Bruton. En algunos aspectos, las sales cristalinas son polimorfos individuales. Reivindicación 1: Una composición de dispersión sólida amorfa adecuada para el tratamiento de trastornos mediados por la actividad de la tirosina cinasa de Bruton, caracterizada porque comprende: (1) un componente polimérico, en donde el componente polimérico es copolímero de metacrilato, copolímero de amino metacrilato, polietilenglicol, acetato de polivinilo, o copolímero injertado de polivinilcaprolactama, o cualquier combinación de los mismos; y (2) de 20% en peso a 50% en peso de una base libre de estructura [1].The invention relates generally to pharmaceutical tablet compositions comprising fumaric acid and the free base compound of (S)-2-(3-(hydroxymethyl)-1-methyl-5-((5-(2 -methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4-bipyridin]-2-yl )-7,7-dimethyl-2,3,4,6,7,8-hexahydro-1H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one which is a tyrosine inhibitor Bruton kinase. The invention further relates to amorphous solid dispersions comprising at least one polymer and the free base of the Bruton's kinase inhibitor compound. The invention further relates to mesylate crystalline salts, chloride crystalline salts and sulfate crystalline salts of the free base of the Bruton's kinase inhibitor compound. In some aspects, crystalline salts are individual polymorphs. Claim 1: An amorphous solid dispersion composition suitable for the treatment of disorders mediated by the activity of Bruton's tyrosine kinase, characterized in that it comprises: (1) a polymeric component, wherein the polymeric component is methacrylate copolymer, amino copolymer methacrylate, polyethylene glycol, polyvinyl acetate, or polyvinylcaprolactam graft copolymer, or any combination thereof; and (2) from 20% by weight to 50% by weight of a structure-free base [1].
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ARP220102392A AR126977A2 (en) | 2022-09-05 | 2022-09-05 | DOSAGE FORM COMPOSITIONS COMPRISING A BRUTON'S TYROSINE KINASE INHIBITOR |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ARP220102392A AR126977A2 (en) | 2022-09-05 | 2022-09-05 | DOSAGE FORM COMPOSITIONS COMPRISING A BRUTON'S TYROSINE KINASE INHIBITOR |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR126977A2 true AR126977A2 (en) | 2023-12-06 |
Family
ID=89309898
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP220102392A AR126977A2 (en) | 2022-09-05 | 2022-09-05 | DOSAGE FORM COMPOSITIONS COMPRISING A BRUTON'S TYROSINE KINASE INHIBITOR |
Country Status (1)
| Country | Link |
|---|---|
| AR (1) | AR126977A2 (en) |
-
2022
- 2022-09-05 AR ARP220102392A patent/AR126977A2/en unknown
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