Patent classifications
A61P39/04
ION CAPTURE COMPOSITION FOR INGESTION
The invention is directed to ion-capture compositions for ingestion and methods of use thereof. An aspect of the invention is drawn towards a method for selectively capturing at least one ion from the digestive system of a subject, the method comprising administering orally to the subject the ion-capture composition.
DICARBOXYLIC ACID BISAMIDE DERIVATIVES, USE THEREOF, PHARMACEUTICAL COMPOSITION BASED THEREON AND METHODS FOR PRODUCING DICARBOXYLIC ACID BISAMIDE DERIVATIVES
The present invention relates to novel biologically active compounds, in particular dicarboxylic acid bisamide derivatives of general formula I:
##STR00001##
or pharmaceutically acceptable salts thereof, which are able to form complexes with or chelate metal ions. The invention also relates to the use of said compounds as an agent for the prevention and/or treatment of cardiovascular, viral, cancer, neurodegenerative and inflammatory diseases, diabetes, age-related diseases, diseases caused by microbial toxins, alcoholism and alcoholic cirrhosis, anaemia, porphyria cutanea tarda, and transition metal salt poisoning. The present invention also relates to novel methods for preparing dicarboxylic acid bisamide derivatives of general formula I.
Formulations of hydroxypyridonate actinide/lanthanide decorporation agents
Provided herein are pharmaceutical formularions comprising a 1,2-HOPO chelating agent and/or 3,2-HOPO chelating agent.
Formulations of hydroxypyridonate actinide/lanthanide decorporation agents
Provided herein are pharmaceutical formularions comprising a 1,2-HOPO chelating agent and/or 3,2-HOPO chelating agent.
METHODS FOR THE DIAGNOSIS AND TREATMENT OF CYTOKINE RELEASE SYNDROME
The invention relates to methods and pharmaceutical compositions for the treatment of Cytokine Release Syndrome (CRS). The invention also relates to methods for the diagnosis of patients suffering from Cytokine Release Syndrome. The inventors investigate iron homeostasis and the role of CD44-mediated iron endocytosis in the severe inflammatory response and Cytokine Release Syndrome, particularly in SARS-CoV-2 patients. The inventors demonstrate that during activation of M1 macrophages, iron endocytosis is upregulated in a CD44-dependent manner and that CD44 protein levels increase. This effect is specific to M1 macrophages, whereas levels of the canonical iron endocytosis protein TfR1/CD71 remain unchanged. In the present invention, the inventors provide in vitro evidences towards a direct role of CD44-mediated iron endocytosis in the severe inflammatory response such as Cytokine Release Syndrome observed in SARS-CoV-2 patients. Thus, the present invention relates to an antagonist of CD44/Hyaluronic Acid pathway for use in the treatment of cytokine release syndrome in a subject in need thereof, particularly severe COVID-19-related cytokine release syndrome.
Solid forms of a compound modulating kinases
Solid forms of the compound, [5-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-pyridin-2-yl]-(6-trifluoromethyl-pyridin-3-ylmethyl)-amine HCl salt (Compound I) and its free base, active on the receptor protein kinases c-Kit and/or c-Fms and/or Flt3, were prepared and characterized: ##STR00001## Also provided are methods of using the solid forms.
Polymeric iron chelating agent
Disclosed is a water-insoluble polymeric iron chelating agent having a polymer backbone and an aromatic ring attached to the polymer backbone through an —NH—CH.sub.2— bond, wherein the aromatic ring has one or two first functional groups in the form of hydroxyl group and one or two second functional groups located at the ortho position with respect to the first functional group; and wherein the second functional group is —OH, —COOH, or a group represented by formula (I) wherein A represents —CH.sub.3, —CH.sub.2—CH.sub.3, —CH.sub.2—C.sub.6H.sub.5, —CH.sub.2—C.sub.5H.sub.4N or —CH.sub.2—COOH and B represents —CH.sub.2—COOH. The water-insoluble polymeric iron chelating agent of the present invention offers the advantages of being capable of selectively chelating iron ions, particularly biologically unstable iron, and being insoluble in water, and moreover not being incorporated in metabolic processes in vivo.
Therapeutic agents for use in the propylaxis and/or treatment of hyperkinetic movement disorders
(RS)-[2-(3,4-dimethoxyphenyl)ethyl][2-hydroxy-3-(3-methylphenoxy)propyl]amine having the formula (IA), or a pharmaceutically acceptable salt thereof for the formulation of a pharmaceutical composition is useful for the prophylaxis and/or the treatment of hyperkinetic movement disorders associated with Huntington's disease, Wilson's disease, Tourette syndrome, restless leg syndrome, and tardive dyskinesia.
ORAL FORMULATIONS OF DEFERASIROX
Orally administerable deferasirox formulations are disclosed having reduced release under gastric conditions and fast release at near neutral pH or at neutral pH.
BIFUNCTIONAL do2pa DERIVATIVES, CHELATES WITH METALLIC CATIONS AND USE THEREOF
Disclosed are chelates resulting from the complexation of bifunctional do2pa derivatives ligands of formula (I), wherein the substituents R.sup.1, R.sup.1′, R.sup.2, R.sup.2′, R.sup.3, R.sup.3′, L.sup.1, L.sup.1′, L.sup.2 and L.sup.2′ are defined as in the claims, with metallic cations, especially Pb(II) and Bi(III). Also disclosed are bifunctional do2pa derivatives ligands of formula (I), as well as the use of chelates in nuclear medicine and the use of ligands in cations detection or epuration of effluents.
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