Patent classifications
A61K9/1635
Radiopaque polymers
A hydrophilic polymer comprising pendent groups of the formula I: Wherein: W is independently selected from —OH, —COOH, —SO.sub.3H, —OPO.sub.3H, —O—(C.sub.1-4alkyl), —O—(C.sub.1-4alkyl)OH, —O—(C.sub.1-4alkyl)R.sup.2, —O—(C.sub.2H.sub.5O).sub.qR.sup.1—(C═O)—O—C.sub.1-4alkyl and —O—(C═O)C.sub.1-4alkyl; or a group —BZ; wherein —OH, COOH, O—PO.sub.3H and SO.sub.3H maybe in the form of a pharmaceutically acceptable salt; wherein: B is a bond, or a straight branched alkanediyl, oxyalkylene, alkylene oxaalkylene, or alkylene (oligooxalkylene) group, optionally containing one or more fluorine substituents; and Z is an ammonium, phosphonium, or sulphonium phosphate or phosphonate ester zwitterionic group; X is either a bond or a linking group having 1 to 8 carbons and optionally 1 to 4 heteroatoms selected from O, N and S; G is a coupling group through which the group of the formula I is coupled to the polymer and is selected from ether, ester, amide, carbonate, carbamate, 1,3 dioxolone, and 1,3 dioxane; R.sup.1 is H or C.sub.1-4 alkyl; R.sup.2 is —COOH, —SO.sub.3H, or —OPO.sub.3H.sub.2 q is an integer from 1 to 4; n is an integer from 1 to 4; p is an integer from 1 to 3; and n+p is from 2 to 5; and wherein —COOH, —OPO.sub.3H.sub.2 and —SO.sub.3H as well as phenolic —OH maybe in the form of a pharmaceutically acceptable salt.
GRANULES AND PREPARATION USING SAME
Provided is a melt granulated product with a high particle size homogeneity. Alternatively, provided is a pharmaceutical composition using said melt granulated product. Alternatively, provided is a melt granulated product with a high drug content. Alternatively, provided is a pharmaceutical composition using the melt granulated product. According to one embodiment of the present invention, a granule is provided that comprises an active ingredient, a melt component, and a polymer, wherein the active ingredient, the melt component and the polymer are bound. In addition, the melt component may be solid at room temperature, and have a melting point of 100° C. or less. The polymer may be solid at room temperature, and have a glass transition point of 100° C. or less.
CHEMICAL COMPOSITION
A solid composition comprising nanoparticles of atovaquone dispersed within one or more carrier materials, wherein the atovaquone is present in an amount of at least 10 wt %. Also described is an intramuscularly- or subcutaneously-injectable formulation of nanoparticles of atovaquone.
STABILIZED FORMULATIONS OF 4-AMINO-3-SUBSTITUTED BUTANOIC ACID DERIVATIVES
Pharmaceutical compositions including an active ingredient and a stabilizer, as well as methods of manufacture of the compositions, and methods of their use. The composition may include the active ingredient dispersed throughout a matrix of the stabilizer. In some embodiments, the active ingredient and the stabilizer are intimately mixed in a matrix formulation. In some embodiments, the active ingredient is selected from 4 amino-3-(4-chlorophenyl)butanoic acid) (“baclofen”) and its pharmaceutically acceptable salts.
AMORPHOUS SOLID DISPERSION OF 8-CHLORO-N-(4-(TRIFLUOROMETHOXY)PHENYL)QUINOLIN-2-AMINE
The present invention relates to an amorphous solid dispersion comprising ABX464 and at least one pharmaceutically acceptable carrier. The present invention also concerns a pharmaceutical composition comprising said ASD, processes for their preparation, an ASD obtainable by specific processes, their use as a medicament and more particularly their use in the treatment and/or prevention of inflammatory diseases, diseases caused by viruses and/or cancer or dysplasia.
NANOPARTICLES CONTAINING COMPLEXES OF NUCLEIC ACIDS AND CATIONIC COPOLYMERS, PROCESS FOR PREPARING THEM AND THEIR USE FOR GENE TRANSFER IN CELLS
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The invention relates to nanoparticles containing complexes constituted by nucleic acids and cationic copolymers containing the recurring structural units of formulae (Ia) and (Ib) wherein R.sup.1 and R.sup.6 independently represent hydrogen, alkyl or —COOR.sup.9, R.sup.2 and R.sup.7 independently represent hydrogen or alkyl, R.sup.3 is selected from the group consisting of —O—R.sup.10—, —COO—R.sup.10, —CONH—R.sup.10- or —R.sup.10—, R.sup.4 represents hydrogen, alkyl, cycloalkyl, aryl, aralkyl or alkylaryl, R.sup.5 represents hydrogen, alkyl, cycloalkyl, aryl, aralkyl, alkylaryl or —(alkylene-NH—).sub.malkyl, or R.sup.4 and R.sup.5 together with the nitrogen atom they have in common form a heterocyclic ring, R.sup.8 is selected from the group consisting of —O—R.sup.11, —COO—R.sup.11, —CONH—R.sup.11 or —R.sup.11, R.sup.9 and R.sup.11 independently represent hydrogen or a monovalent organic residue, R.sup.10 represents a bivalent organic residue, and m is an integer from 1 to 5, with the proviso that the nanoparticles have a diameter (z-average) of less than or equal to 900 nm as determined by dynamic light scattering and that the molar ratio of nitrogen atoms in the copolymer to the phosphate groups in the nucleic acid ranges between 1 and 200. The nanoparticles according to the invention allow the transfer of nucleic acids into cells with great efficiency.
TREATMENT OF PROSTATE CANCER WITH A COMBINATION OF ABIRATERONE ACETATE AND NIRAPARIB
The present disclosure relates to a combination of abiraterone acetate and niraparib, free-dose and fixed-dose combinations of abiraterone acetate and niraparib, and methods of treatment of prostate cancer with said combinations.
LARAZOTIDE DERIVATIVES COMPRISING D-AMINO ACIDS
The present invention provides compositions comprising an effective amount of a peptide having the amino acid sequence Gly-Gly-(d)Val-(d)Leu-(d)Val-(d)Gln-(d)Pro-Gly (SEQ ID NO: 6) to promote tight junction integrity, or a pharmaceutically acceptable salt thereof, and a pharmaceutically-acceptable carrier. The present invention further provides methods of using the larazotide derivative compositions for promoting tight junction integrity in patients in need thereof.
SEMAGLUTIDE DEPOT SYSTEMS AND USE THEREOF
The present invention provides parenteral pharmaceutical compositions comprising therapeutically effective amounts of semaglutide or pharmaceutically acceptable salts thereof, the parenteral pharmaceutical compositions are formulated in depot form and provide low-burst release and a continued release profile. The present invention further provides methods of use of the parenteral pharmaceutical compositions for treating type-2 diabetes mellitus, obesity, and Parkinson's disease.
Methods and compositions for self-regulated release of active pharmaceutical ingredients
An abuse deterrent pharmaceutical composition including a drug susceptible to abuse, a first acid soluble ingredient, a first buffering ingredient, and a delayed release buffering component.