Patent classifications
A61K9/485
FORMULATION COMPRISING HIF PROLYL HYDROXYLASE INHIBITORS
The present invention generally relates to a pharmaceutical composition of suitable HIF prolyl hydroxylase inhibitors. Preferably, the present invention discloses novel formulations of the compound of formula (Ia), or pharmaceutically acceptable salts of compounds of formula (Ia). More particularly the present invention relates to the pharmaceutical composition of compounds of formula (Ia) comprising compounds of formula (Ia) or its pharmaceutically acceptable salts.
##STR00001##
Methods of Treating Multiple Sclerosis
Provided herein are methods of treating multiple sclerosis with a fumarate, wherein the fumarate is a dialkyl fumarate, a monoalkyl fumarate, a combination of a dialkyl fumarate and a monoalkyl fumarate, a prodrug of monoalkyl fumarate, a deuterated form of any of the foregoing, or a pharmaceutically acceptable salt, clathrate, solvate, tautomer, or stereoisomer of any of the foregoing, or a combination of any of the foregoing. The methods provided herein improve the safety of treatment by informing and monitoring patients undergoing treatment regarding progressive multifocal leukoencephalopathy, and/or by monitoring lymphocyte count.
CALCIFEDIOL SOFT CAPSULES
The present invention relates to calcifediol soft capsules, to their use in the treatment or prevention of diseases related to vitamin D deficiency, such as vitamin D deficiency, demineralization such as hypocalcemia and hypophosphatemia, renal osteodystrophy, rickets, osteoporosis, osteopenia, osteoarthritis, osteoarthrosis, osteomalacia, hypoparathyroidism, and inflammatory bowel disease, and to their process of manufacture.
Combination Drug Therapy
A novel combination comprising the 17 α-hydroxylase/C17,20 lyase inhibitor, (3β)-17-(pyridin-3-yl)androsta-5,16-dien-3-ol or a pharmaceutically acceptable salt or solvate thereof, with a PI3Kβ inhibitor, 2-methyl-1-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-6-(4-morpholinyl)-1H-benzimidazole-4-carboxylic acid, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of 17 α-hydroxylase/C17,20 lyase and/or PI3Kβ is beneficial, e.g., cancer.
METHODS OF MAKING AND USING PDE9 INHIBITORS
The present invention relates to PDE9 inhibitors, their synthesis, and their use for treatment of benign prostate hyper-plasia, beta thalassemia, and sickle cell disease.
SUBSTITUTED IMIDAZO[5,1-d][1,2,3,5]TETRAZINES FOR THE TREATMENT OF CANCER
New synthetic methods to provide access to previously unexplored functionality at the C8 position of substituted imidazo[5,1-d][1,2,3,5]tetrazines of Formula I. Through synthesis and evaluation of a suite of compounds with a range of aqueous stabilities (from 0.5 to 40 hours), a predictive model for imidazotetrazine hydrolytic stability based on the Hammett constant of the C8 substituent was derived. Promising compounds were identified that possess activity against a panel of GBM cell lines, appropriate hydrolytic and metabolic stability, and brain-to-serum ratios dramatically elevated relative to TMZ, leading to lower hematological toxicity profiles and superior activity to TMZ in a mouse model of GBM.
##STR00001##
COMPOSITIONS AND METHODS FOR TREATING DISORDERS AMELIORATED BY MUSCARINIC RECEPTOR ACTIVATION
Provided herein is an oral pharmaceutical composition, comprising a plurality of xanomeline beads having a core comprising xanomeline or a salt thereof; and a plurality of trospium beads having a core comprising a salt of trospium.
Pharmacokinetics of combined release formulations of a γ-hydroxybutyric acid derivative
Pharmaceutical compositions comprising an immediate release component comprising 4-((L-valyl)oxy)butanoic acid and a modified release component comprising 4-((L-valyl)oxy)butanoic acid and the pharmacokinetics of 4-((L-valyl)oxy)butanoic acid and γ-hydroxybutyrate following oral administration of the pharmaceutical compositions is disclosed.
Bicyclic compounds as ATX inhibitors
The invention provides novel compounds having the general formula (I) ##STR00001##
wherein R.sup.1, R.sup.2, Y, W, A, X, m and n are as defined herein, compositions including the compounds and methods of using the compounds.
Compositions of CXCR4 inhibitors and methods of preparation and use
The present invention provides compositions and methods of use for treating, preventing, or ameliorating a disease, disorder, or condition associated with a chemokine receptor such as CXCR4.