Patent classifications
A61K9/2054
THERAPEUTIC COMPOSITIONS FOR TREATMENT OF HUMAN IMMUNODEFICIENCY VIRUS
A solid oral dosage form is provided, comprising a compound of Formula I or a pharmaceutically acceptable salt thereof, tenofovir alafenamide or a pharmaceutically acceptable salt thereof, and emtricitabine or a pharmaceutically acceptable salt thereof.
SOLID ORAL DOSAGE FORM COMPRISING NAPROXEN AND VITAMIN B6
The present invention relates to a solid oral dosage form comprising naproxen and vitamin B6. Preferably, it is a solid oral dosage form for use in the treatment of pain such as low back pain. It is a fixed-dose combination (FDC) which increases patient compliance. The method of preparing such solid oral dosage form comprises the extragranular addition of vitamin B6 to an intragranular composition, wherein said intragranular composition comprises naproxen or a pharmaceutically acceptable salt thereof and at least one binder.
1-(((2S,3S,4S)-3-ETHYL-4-FLUORO-5-OXOPYRROLIDIN-2-YL)METHOXY)-7-METHOXYISOQUINOLINE-6-CARBOXAMIDE COMBINATIONS AND ORAL DOSAGE FORMS
The present invention is related to the discovery of new oral dosage formulations and combination therapies for 1-(((2S,3S,4S)-3-ethyl-4-fluoro-5-oxopyrrolidin-2-yl)methoxy)-7-methoxyisoquinoline-6-carboxamide, or a pharmaceutically acceptable salt thereof, for treating conditions ameliorated by inhibition of IRAK4.
ACTIVATING PYRUVATE KINASE R
The compound (S)-1-(5-((2,3-dihydro-[1,4]dioxino[2,3-b]pyridin-7-yl)sulfonyl)-3,4,5,6-tetrahydropyrrolo[3,4-c]pyrroll-2(1H)-yl)-3-hydroxy-2-phenylpropan-1-one, or a pharmaceutically acceptable salt thereof, is useful to increase the affinity of hemoglobin for oxygen. Methods and compositions for the treatment of a hemoglobinopathies are provided herein, including certain pharmaceutical compositions for activating PKR.
COMPOSITION OF ACYLETHANOLAMIDES FROM OLIVE OIL FATTY ACIDS
A composition of acylethanolamides is obtained from olive oil fatty acids and is used in treating neuroinflammation. The acylethanolamide complex includes (weight percentages):
TABLE-US-00001 oleoylethanolamide (OEA) C18:1 60-65% palmitoylethanolamide (PEA) C16:0 5-20% linoleylethanolamide (LEA) C18:2 5-20% stearoylethanolamide (SEA) C18:0 1-2% palmitoylethanolamide (POEA) C16:1 0.1-0.8% myristoylethanolamide (MEA) C14:0 0.02-0.15% mixture of glycerides 4-6% glycerol .sup. 6-8%.
A method obtains the acylethanolamide complex and formulations contain the acylethanolamide complex.
ORALLY DISINTEGRATING TABLET COMPRISING AMORPHOUS SOLID DISPERSION OF NILOTINIB AND IN VITRO CHARACTERIZATION THEREOF
Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor nilotinib. The pharmaceutical compositions may be used in methods of treating a proliferative disorder such as cancer. In particular, the present disclosure provides a pharmaceutical composition in the form of an orally disintegrating tablet. In some embodiments, the pharmaceutical compositions can be administered without regard to food consumption. In other embodiments, the pharmaceutical compositions can be administered at a significantly lower dose as compared to a commercially available immediate-release nilotinib formulation, while providing a comparable therapeutic effect. The disclosure further provides a discriminating in vitro dissolution characterization method.
BRK inhibitory compound
The present invention relates to a compound represented by general formula (I) (wherein, all symbols represent the same meanings as the symbols set forth in the specification), a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug of any of these. Since the compound has a Brk inhibitory activity, the compound is useful as a drug ingredient for the prevention and/or treatment of Brk-related diseases such as cancer, for example. ##STR00001##
Pharmaceutical composition of apixaban
The present disclosure relates to a stable, reproducible and bioequivalent apixaban compositions, wherein the composition comprising apixaban having a D.sub.90 particle size of more than 100 microns, preferably between 300 and 1000 microns, and more preferably between 350 and 800 microns, and further comprising one or more pharmaceutically acceptable excipients. The present disclosure further provides a process for preparation of a pharmaceutical composition comprising apixaban by wet granulation.
Cancer therapy by degrading dual MEK signaling
The discovery of mutant or fusion kinases that drive oncogenesis, and the subsequent approval of specific inhibitors for these enzymes, has been instrumental in the management of some cancers. However, acquired resistance remains a significant problem in the clinic, limiting the long-term effectiveness of most of these drugs. Herein is demonstrated a strategy to overcome this resistance through drug-induced MEK cleavage (via direct procaspase-3 activation) combined with targeted kinase inhibition. This combination effect is shown to be general across diverse tumor histologies (melanoma, lung cancer, and leukemia) and driver mutations (mutant BRAF or EGFR, fusion kinases EML4-ALK and BCR-ABL). Caspase-3-mediated degradation of MEK kinases results in sustained pathway inhibition and substantially delayed or eliminated resistance in cancer cells in a manner superior to combinations with MEK inhibitors. These data suggest the generality of drug-mediated MEK kinase cleavage as a therapeutic strategy to prevent resistance to targeted anticancer therapies.
PHARMACEUTICAL COMPOSITION COMPRISING THIRD GENERATION SMALL MOLECULE EGFR INHIBITOR AND PREPARATION METHOD THEREOF
A pharmaceutical composition comprising a small molecule EGFR inhibitor and a preparation method therefor, the composition comprising N-(5-((4-(1-cyclopropyl-1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide, an isomer, solvate, hydrate, or pharmaceutically acceptable salt thereof, or a combination thereof that acts as an active ingredient, and at least one pharmaceutically acceptable excipient.