A61K9/485

PHARMACEUTICAL COMPOSITION

A pharmaceutical composition of 2-amino-2-[2-(4-heptyloxy-3-trifluoromethylphenyl)ethyl]propane-1,3-diol or a salt thereof is provided. The composition is superior in storage stability and can suppress production of related substances.

An excipient selected from dibasic calcium phosphate, calcium dihydrogen phosphate, dibasic sodium phosphate, and sodium dihydrogen phosphate is used.

Pyridine and pyrazine derivatives as preferential cannabinoid 2 agonists

The invention relates to a compound of formula (I) ##STR00001##
wherein A.sup.1, A.sup.2 and R.sup.1-R.sup.5 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

NEW PYRIDO DIAZEPINE DERIVATIVES AS GABA A GAMMA1 PAM

The invention provides novel heterocyclic compounds having the general formula (I), and pharmaceutically acceptable salts thereof, wherein the variables are as described herein.

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Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds for the treatment or prevention of acute neurological disorders, chronic neurological disorders and/or cognitive disorders.

AN ORAL PHARMACEUTICAL COMPOSITION COMPRISING AN EXTRACT OF COMBINED HERBS COMPRISING LONGANAE ARILLUS FOR THE TREATMENT OR ALLEVIATION OF INFLAMMATORY DISEASE AND THE USE THEREOF
20230107274 · 2023-04-06 ·

The present invention relates to an oral pharmaceutical composition comprising a combined herb extract of Longanae Arillus, Ligustici Tenuissimi Rhizoma and Polygalae radix, the present inventors demonstrated that the anti-inflammatory/anti-rheumatic effects of inventive combined composition is potent by accomplishing in vitro experiments such as the inhibitory test on the expression of cytokines involved in inflammation (RPLPO, TSLP, GM-CSF and IL-1beta) (Experimental Example 1); Cell viability test on HT-29 and THP-1 cell (in vitro Experimental Example 2); Anti-inflammatory activity in THP-1 cell (in vitro, Experimental Example 3); inhibitory effect on autophagy activity (in vitro, Experimental Example 4.) as well as in vivo experiments such as inhibitory effect on arthritis sing by arthritis-induced rat animal model (in vivo, Experimental Example 5), therefore, it is confirmed that inventive combined extract is very useful in the alleviation or treatment of inflammatory disease and arthritis disease as a form of oral pharmaceutical composition.

COMPOUNDS AND METHODS FOR THE TREATMENT OF PARASITIC INFECTIONS

Cryptosporidium parvum is a highly prevalent zoonotic and anthroponotic protozoan parasite that causes a diarrheal syndrome in children and neonatal livestock, culminating in growth retardation and mortalities. Disclosed herein are inhibitors against the enzymatic activity of recombinant CpLDH protein that were identified. The inhibitors were tested for anti-Cryptosporidium effect using in vitro infection assays of HCT-8 cells monolayers. Compounds NSC158011 and NSC10447 were identified to inhibit the proliferation of intracellular C. parvum in vitro, with IC50 values of 14.88 and 72.65 μM, respectively. At doses tolerable in mice, both NSC158011 and NSC10447 significantly reduced the shedding of C. parvum oocysts in infected immunocompromised mice's feces and prevented intestinal villous atrophy as well as mucosal erosion due to C. parvum. These findings have unveiled anti-Cryptosporidium drug candidates that can be explored further for the development of therapeutic agents against C. parvum infections.

Two-stage microparticle-based therapeutic delivery system and method

A system for delivery of a therapeutic agent to a site in mucosal tissue is provided. The system includes a porous, mucoadhesive polymeric matrix having a first and a second opposed surfaces. The matrix is formed by a composition including chitosan. The composition may also include any or all of a hydration promotor, a microparticle adhesion inhibitor, and a microparticle aggregation inhibitor. A plurality of microparticles having an average diameter between 500 nm and 2000 nm are embedded within the matrix. The microparticles contain a therapeutic agent and have a coating around the therapeutic agent. The first surface of the matrix is configured to be attached to the site in the mucosal tissue and the matrix is configured to provide controlled release of the microparticles through the first surface. The coating of the microparticles includes chitosan so as to provide controlled release of the agent from the microparticles.

METHOD FOR STABILIZING HUMIDITY-SENSITIVE PHARMACEUTICAL SUBSTANCE AND STABILIZED PREPARATION THEREOF
20220313613 · 2022-10-06 · ·

An object of the present invention is to provide a method for stabilizing a substance DFP-11207 sensitive to humidity and unstable at high humidity, and a stabilized preparation thereof, and more specifically, provide a capsule preparation for treating cancer, containing DFP-11207 or a pharmaceutically acceptable salt thereof and a hygroscopic agent.

USE OF A PHOSPHODIESTERASE 10 INHIBITOR FOR THE TREATMENT OF TOURETTE SYNDROME
20230149372 · 2023-05-18 ·

Provided herein are methods of treating Tourette Syndrome in a subject in need thereof by administering to the subject compositions comprising a PDE10 inhibitor. Also disclosed are crystalline solid forms of the compound of Formula I and uses thereof:

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KINASE INHIBITOR SALTS AND COMPOSITIONS THEREOF

The present invention relates to cabozantinib lauryl sulfate salt and methods of use.

IMIDAZOPYRAZINE DERIVATIVES

The invention provides novel imidazopyrazine derivatives having the general formula (I), wherein R.sup.x and R.sup.3 to R.sup.5 are as described herein:

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or pharmaceutically acceptable salts thereof.

Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.