Patent classifications
A61K9/485
CRYSTALLINE FORMS OF 2-[(2S)-1-AZABICYCLO[2.2.2]OCT-2-YL]-6-(3-METHYL-1H-PYRAZOL-4-YL)THIENO[3,2-D]PYRIMIDIN-4(3H)-ONE HEMIHYDRATE
The present disclosure relates to crystalline forms of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4(3H)-one hemihydrate (Compound 1) and/or tautomers thereof, wherein Compound 1 has the structure: (I).0.5H.sub.2O; processes for preparing crystalline forms of Compound 1 and/or tautomers thereof; pharmaceutical compositions comprising the crystalline forms; methods of inhibiting a cell division cycle 7 in a mammal comprising administering the crystalline forms; and methods of treating a cell division cycle 7 mediated cancer in a mammal comprising administering the crystalline forms or a pharmaceutical composition comprising the crystalline forms.
##STR00001##
Methods of treating cancer using PRMT5 inhibitors
The present disclosure provides methods for treating a human patient diagnosed with a cancer, comprising administering a therapeutically effective amount of a PRMT5 (protein arginine methyltransferase 5) inhibitor, certain methods comprising (i) administering to the patient initial doses of at least about 0.1 mg per day of the PRMT5 inhibitor that is (1S,2R,3S,5R)-3-(2-(2-amino-3-bromoquinolin-7-yl)ethyl)-5-(4-amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclopentane-1,2-diol or a pharmaceutically acceptable addition salt or solvate thereof for an initial dosing period of about 5 to about 21 days; and (ii) administering to the patient subsequent doses of at least about 0.1 mg per day of the PRMT5 inhibitor for one or more subsequent dosing periods of about 5 to about 21 days each. In these methods, a first subsequent dosing period is separated in time from the initial dosing period by at least about 5 days and the subsequent dosing periods are separated in time from each other by at least about 5 days.
GABA COMPLEX COMPOSITION
The present disclosure relates to a composition for improving sleep quality, including γ-aminobutyric acid (GABA) or a salt, hydrate or solvate thereof; and at least one of arginine, niacin, and salts, hydrates and solvates thereof. The composition for improving sleep quality may improve the sleep quality by increasing melatonin secretion. In addition, in another aspect, the present disclosure provides a composition for alleviating stress, including γ-aminobutyric acid (GABA) or a salt, hydrate or solvate thereof; and at least one of arginine, niacin, and salts, hydrates and solvates thereof.
CRYSTALLINE FORMS OF AN IRREVERSIBLE INHIBITOR OF MENIN-MLL INTERACTION
Described herein is N-[4-[4-(4-morpholinyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl]-4-[[3(R)-[(1-oxo-2-propen-1-yl)amino]-1-piperidinyl]methyl]-2-pyridinecarboxamide, including crystalline forms, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the compound, as well as methods of using the compound, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
Sustained Release Formulation Containing Aspalathus linearis Extract
A multi-unit pharmaceutical composition comprising an immediate release component comprising a polyphenol-containing Aspalathus linearis extract and one or more pharmaceutically acceptable excipients, and a sustained release component comprising a polyphenol-containing Aspalathus linearis extract and one or more pharmaceutically acceptable excipients, wherein the composition provides a substantially linear polyphenol release profile over a predetermined period, for example about 8 hours.
Pharmaceutical compositions comprising DGLA and use of same
The present disclosure provides orally deliverable pharmaceutical compositions comprising DGLA and to methods of using same to treat a variety of conditions and disorders.
Instant release pharmaceutical preparation of anticoagulant and preparation method therefor
The present invention relates to the technical field of medicine and relates to an instant release pharmaceutical preparation of an anticoagulant and a preparation method therefor. The instant release pharmaceutical preparation of an anticoagulant comprises a vicagrel compound or a pharmaceutically acceptable form thereof, the preparation is a tablet or a capsule, the vicagrel or the pharmaceutically acceptable form thereof is provided at a suitable particle size, and the D90 thereof <50 μm. With regard to the drug-containing particles obtained by the present invention, a pharmaceutical preparation formed therefrom exhibits rapid release characteristics in an in vitro dissolution test and exhibits considerable advantages in pharmacokinetics in vivo, showing a greater degree (AUC) and rate (C.sub.max) of drug absorption. Further provided by the present invention is a method for preparing an instant release pharmaceutical preparation of an anticoagulant; according to the formulation of the drug-containing particles as disclosed by the present invention, a capsule or tablet instant release preparation having excellent stability may be obtained by means of a combination of optional preparation steps.
Deuterated N,N-dimethyltryptamine compounds
Compounds, compositions, methods, and uses are described for therapeutic deuterated N,N-dimethyltryptamine compounds (e.g., a single compound or a plurality of deuterated N,N-dimethyltryptamine compounds) such as N,N-dimethyltryptamine compounds, α-protio, α-deutero-N,N-dimethyltryptamine compounds, α,α-dideutero-N,N-dimethyltryptamine compounds, and pharmaceutically acceptable salts of these compounds. The deuterated N,N-dimethyltryptamine compound may have an increased half-life compared with the half-life of undeuterated N,N-dimethyltryptamine. For example, a deuterated N,N-dimethyltryptamine compound may be used in therapy and have a Formula (I): ##STR00001## wherein: the ratio of deuterium:protium in the compound is greater than that found naturally in hydrogen; each R.sup.1 is independently selected from H and D; R.sup.2 is selected from CH.sub.3 and CD.sub.3; R.sup.3 is selected from CH.sub.3 and CD.sub.3; each .sup.yH is independently selected from H and D, or a pharmaceutically acceptable salt thereof.
OXAZINE MONOACYLGLYCEROL LIPASE (MAGL) INHIBITORS
The invention provides new heterocyclic compounds having the general formula (Ic)
##STR00001##
wherein A, L, X, m, n and R.sup.20 to R.sup.23 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.
INSTANT RELEASE PHARMACEUTICAL PREPARATION OF ANTICOAGULANT AND PREPARATION METHOD THEREFOR
The present invention relates to the technical field of medicine and relates to an instant release pharmaceutical preparation of an anticoagulant and a preparation method therefor. The instant release pharmaceutical preparation of an anticoagulant comprises a vicagrel compound or a pharmaceutically acceptable form thereof, the preparation is a tablet or a capsule, the vicagrel or the pharmaceutically acceptable form thereof is provided at a suitable particle size, and the D90 thereof <50 μm. With regard to the drug-containing particles obtained by the present invention, a pharmaceutical preparation formed therefrom exhibits rapid release characteristics in an in vitro dissolution test and exhibits considerable advantages in pharmacokinetics in vivo, showing a greater degree (AUC) and rate (C.sub.max) of drug absorption. Further provided by the present invention is a method for preparing an instant release pharmaceutical preparation of an anticoagulant; according to the formulation of the drug-containing particles as disclosed by the present invention, a capsule or tablet instant release preparation having excellent stability may be obtained by means of a combination of optional preparation steps.