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Heterocyclic kinase inhibitors
The present invention provides heterocyclic compounds for use as kinase inhibitors and in other applications. Also provided are pharmaceutical compositions and methods of treatments of diseases and conditions associated with P13 kinase activity....

Novel 3,5-disubstituted-3h-imidazo[4,5-b]pyridine and 3,5- disubstituted -3h-[1,2,3]triazolo[4,5-b] pyridine compounds as modulators of protein kinases
The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them....

Tetrahydroisoquinolines as antimalarial agents
The invention relates to novel tetrahydroisoquinoline derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially...

Pyrimidine compounds and methods of making and using same
Disclosed herein are pyrimidinyl compounds that are contemplated to be modulators of cystic fibrosis transmembrane regulators (CFTR), and methods of making and using same. Also provided are pharmaceutical compositions and methods of treating disorders associated with cystic fibrosis transmembrane regulators, such as airway inflammation, cystic fibrosis, and the like....

Inhibitors of p38
The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in...

Sulfonyl containing compounds as cysteine protease inhibitors
The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them....

Novel substituted bicyclic heterocyclic compounds as gamma secretase modulators
wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as...

Pharmaceutical compositions with attenuated release of phenolic opioids
Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise a phenolic opioid prodrug that provides enzymatically-controlled release of a phenolic opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the phenolic opioid from the prodrug so as to attenuate...

Compound, synthesis, composition and uses thereof
The instant application provides the disclosure for a compound of formula I, synthesis of compound of formula I and its pharmaceutical acceptable salts, as well as its polymorphs, solvates, and hydrates thereof. The pharmaceutically acceptable salt may be formulated for oral administration, systemic administration, transdermal administration and injection. The compound of...

Hemifumarate salt
The present invention relates to a hemifumarate salt of the compound (1S)-1-(2-(difluoromethyl)pyridin-4-yl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amine, Form A thereof and its pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy...

Optically pure quinazoline compounds
Optical pure quinazoline compounds, especially compounds of the general formula (I), wherein R1 and Y are defined as the specification, preparation methods of them, pharmaceutical compositions containing them and their uses are provided. Compounds of the general formula (VII), which are intermediates in the synthesis of the compounds of the general...

Phenoxiacetic acid derivatives
The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation....

Pharmaceutical compositions and methods of making same
Pharmaceutical compositions that include an amount of an acid addition salt of pazopanib equivalent to about 5 mg/mL pazopanib, about 2.0 to about 13.0% w/w of a modified cyclodextrin suitable for use in an ophthalmic formulation, and pH adjusting agent as well as methods of making the same are described....

Bicyclic heterocyclic spiro compounds
There are disclosed bicyclic heterocyclic spiro compounds; pharmaceutical compositions comprising these compounds; and methods for the treatment in a mammal of diseases and conditions which are susceptible to modulation of the M1 muscarinic receptor, including Alzheimer's disease, insulin resistance syndrome and type 2 diabetes. Other embodiments are also disclosed....

Compositions and methods for inhibition of hepatocyte growth factor receptor c-met signaling
Derivatives and analogs of inhibitors of receptor tyrosine kinase c-Met obtained by virtual screening, pharmaceutical compositions containing derivatives and analogs of c-Met inhibitors are provided. Methods of making derivatives and analogs of c-Met inhibitors and methods of use thereof are provided. Formula (I)...

Novel forms of eperisone
The invention relates to substantially enantiopure crystalline salt forms of (2RS)-I-(4-Ethylphenyl)-2-methyl-3-piperidin-1-ylpropan-1-one. The preparation and characterization of the substantially enantiopure crystalline salt forms according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the substantially enantiopure crystalline salt forms, which are useful to treat and/or...

Dual-acting antihypertensive agents
wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and...

Pharmaceutical compositions comprising 2-oxo-1-pyrrolidine derivatives
The present invention relates to an immediate release formulation of pharmaceutical compounds....

Compositions and methods for reducing proliferation and viability of lymphoblastoid cells
Pharmaceutical compositions including an HDAC inhibitor and a pharmaceutically acceptable carrier wherein the HDAC inhibitor is present in an amount sufficient to achieve a plasma concentration from about 100 nM to about 2 uM and methods of treatment using the same. Pharmaceutical compositions including an HDAC inhibitor and a pharmaceutically acceptable...

Novel peptides that bind to the erythropoietin receptor
The present invention relates to peptide compounds that are agonists of the erythropoietin receptor (EPO-R). The invention further relates to therapeutic methods using such peptide compounds to treat disorders associated with insufficient or defective red blood cell production. Pharmaceutical compositions, which comprise the peptide compounds of the invention, are also provided....

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Pharmaceutical Compositions patents

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