Patent classifications
A61P13/00
BROMODOMAIN INHIBITORS
The present invention provides for compounds of formula (I)
##STR00001## wherein A.sup.1, A.sup.2, A.sup.3, A.sup.4, X.sup.1, X.sup.2, Y.sup.1, L.sup.1, G.sup.1, R.sup.x, and R.sup.y have any of the values defined thereof in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
LYOPHILIZATION OF RNA
The present invention is directed to the field of RNA formulation, in particular to lyophilization of RNA. The invention provides a method for lyophilization of RNA. The present invention further concerns a lyophilized composition obtainable by the inventive method, a pharmaceutical composition, a vaccine and a kit or kit of parts. Moreover, the present invention provides a novel use of a lyoprotectant for lyophilizing RNA, the use of the inventive method in the manufacture of a medicament as well as the first and second medical use of the composition obtainable by the inventive method, the pharmaceutical composition, the vaccine or the kit or kit of parts according to the invention.
CD38 INHIBITORS
One embodiment of the invention is a compound represented by Formula I: or a pharmaceutically acceptable salt thereof. The variables in Formula I are defined herein. Compounds of Formula I are CD38 inhibitors, which can be used to treat a disease or condition in a subject that benefits from an increase in NAD+ or to treat a mitochondrial disorder in a subject.
##STR00001##
THIENO PYRIMIDINES AS FERROPORTIN INHIBITORS
The subject matter described herein is directed to ferroportin inhibitor compounds of Formula I and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of administering the compounds for prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis, and also kidney injuries.
Pharmaceutical compositions comprising sodium meta arsenite for treatment of multiple myeloma
The present application relates to pharmaceutical compositions and methods for treatment of urogenital diseases and bone metastasis in a human, which pharmaceutical composition contains an effective amount of arsenous acid alkaline or earth alkaline metal salt and/or a pharmaceutically acceptable adjuvant. According to the present invention, the alkaline arsenous acid metal salt is sodium meta-arsenita (AsO.sub.2Na) or potassium meta-arsenite (AsO.sub.2K). The effective amount of arsenous acid alkaline or earth alkaline metal salt is 0.0001-1500 mg/kg, preferably 1-1000 mg/kg, more preferably 1-150 mg/kg, and most preferably 50-100 mg/kg of body weight/day. The administration form of the pharmaceutical compositions of the invention is preferably oral, such as a tablet, capsule, powder and/or solution with a pharmaceutically acceptable carrier, diluent or excipient.
Guanidine compounds and use thereof
The present invention relates to guanidine compounds for inhibiting mitochondrial oxidative phosphorylation (OXPHOS) and use thereof. More specifically, the present invention relates to a pharmaceutical composition for preventing or treating a OXPHOS-related disease, particularly cancer, by inhibiting mitochondrial oxidative phosphorylation and reprogramming cellular metabolism.
TGF-β inhibitors
Disclosed are pyrazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure ##STR00001##
and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein A, X, Z, m, p, and R.sup.2 are as described herein. In certain embodiments, a compound disclosed herein inhibits the activity of one or more members of the TGF-β superfamily, and can be used to treat disease by blocking such activity.
PHENYL PYRROLE AMINOGUANIDINE SALTS AND FORMULATIONS
The disclosure relates to oral formulations for gastric delivery of a pharmaceutically acceptable salt of a phenyl pyrrole aminoguanidine compound.
Anti-inflammatory peptides and composition comprising the same
A peptide with anti-inflammatory activity is described, wherein the peptide comprises at least one amino acid sequence among SEQ ID NO: 2 to SEQ ID NO: 179, the peptide has above 80% homology of amino acid sequence with above-mentioned sequences, or the peptide is the fragment of the above-mentioned peptides. An inflammatory composition comprising the above mentioned peptides is also described. The peptides that have at least one amino acid sequence of SEQ ID NO: 2 to SEQ ID NO: 179 shows outstanding efficacy in both suppressing inflammation and in prophylactic means, Therefore, the composition comprising those peptides can be used as anti-inflammatory pharmaceutical compositions or as cosmetic compositions, in turn, treating and preventing a variety of different types of inflammatory diseases.
Heterocyclic P2X7 antagonists
Disclosed are compounds of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions containing them, and to a process for the preparation of the compounds: ##STR00001##
R.sup.1 is independently selected from hydrogen atom, amine group, monocyclic or bicyclic aliphatic, aromatic, heteroaliphatic or heteroaromatic ring. R.sup.2 is independently selected from monocyclic or bicylic aliphatic, heteroaliphatic, aromatic or heteroaromatic ring, C.sub.1-C.sub.6 alkyl, alkenyl or alkynyl chain. n is 1 or 2; preferably n is 1. m is 0, 1 or 2; preferably m is 0. R.sup.3 and R.sup.4 can be, independently, —H, —F, C.sub.1-C.sub.4 alkyl, —OH, —OC.sub.1-C.sub.4 alkyl; preferably they are both —H. X is O or S. R.sup.5 is —H or —CH.sub.3 optionally substituted by one or more fluorine atoms; preferably R.sup.5 is hydrogen. The compounds can be used in the treatment of conditions or diseases mediated by P2X7 receptor.