A61K47/40

Pharmaceutical aqueous formulation comprising 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea
11541058 · 2023-01-03 · ·

The present invention relates to a pharmaceutical aqueous formulation comprising 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea, or a pharmaceutically acceptable alkanesulphonate salt thereof, that is a clear solution. Such a formulation is particularly suitable for intravenous or parenteral administration to a patient.

Peptide composition for treating excitatory neurotoxicity related injuries

There is provided in the present application a pharmaceutical composition comprising a peptide comprising the amino acid sequence of YEKLLDTEI (SEQ ID NO: 1) or a functional variant thereof, a pH adjusting agent, and a filler. The peptide is an active peptide for the treatment of a central nervous system injury. The present application also provides a pharmaceutical composition comprising a chimeric peptide comprising an active peptide and an internalization peptide, a pH adjusting agent, and a filler. The present application also provides medical use of a pharmaceutical composition comprising the active peptide or the chimeric peptide.

Peptide composition for treating excitatory neurotoxicity related injuries

There is provided in the present application a pharmaceutical composition comprising a peptide comprising the amino acid sequence of YEKLLDTEI (SEQ ID NO: 1) or a functional variant thereof, a pH adjusting agent, and a filler. The peptide is an active peptide for the treatment of a central nervous system injury. The present application also provides a pharmaceutical composition comprising a chimeric peptide comprising an active peptide and an internalization peptide, a pH adjusting agent, and a filler. The present application also provides medical use of a pharmaceutical composition comprising the active peptide or the chimeric peptide.

USE OF CYCLODEXTRINS AS A RADIOSTABILIZER
20220409752 · 2022-12-29 ·

The present invention provides a radiopharmaceutical composition comprising the following four components: (i) a radio-labelled compound; (ii) ethanol; (iii) a stabilizer of the radio-labelled compound; and (iv) a cyclodextrin.

The present invention also provides a radiopharmaceutical composition comprising: (i) a radio-labelled compound; (ii) a stabilizer of the radio-labelled compound, wherein the stabilizer comprises: ascorbic acid, aspartic acid, cysteine, maleic acid, gentisic acid, glutathione, glutamic acid, mannitol, nicotinamide, calcium chloride, N-t-butyl-alpha-phenylnitrone (PBN), tartaric acid, para-aminobenzoic acid (pABA), chloride ions or salts or combinations thereof; and (iii) a cyclodextrin.

USE OF CYCLODEXTRINS AS A RADIOSTABILIZER
20220409752 · 2022-12-29 ·

The present invention provides a radiopharmaceutical composition comprising the following four components: (i) a radio-labelled compound; (ii) ethanol; (iii) a stabilizer of the radio-labelled compound; and (iv) a cyclodextrin.

The present invention also provides a radiopharmaceutical composition comprising: (i) a radio-labelled compound; (ii) a stabilizer of the radio-labelled compound, wherein the stabilizer comprises: ascorbic acid, aspartic acid, cysteine, maleic acid, gentisic acid, glutathione, glutamic acid, mannitol, nicotinamide, calcium chloride, N-t-butyl-alpha-phenylnitrone (PBN), tartaric acid, para-aminobenzoic acid (pABA), chloride ions or salts or combinations thereof; and (iii) a cyclodextrin.

BENZODIAZEPINE DERIVATIVES FOR TREATING A RESPIRATORY SYNCYTIAL VIRUS (RSV) INFECTION

Benzodiazepine derivatives of formula (I): wherein: each of R.sup.1 and R.sup.2 is independently H or halo; R.sup.3 is H, C.sub.1-C.sub.6 alkyl, —NHR.sup.8 or —OR′; either (i) a, c, and e are all bonds, with b, d and f absent; orb, d and f are all bonds, with a, c and e absent; R.sup.4 is H or a group selected from C.sub.1-C.sub.6 alkyl, C.sub.3-C.sub.6 cycloalkyl and 4- to 10-membered heterocyclyl, the group being unsubstituted or substituted; R.sup.5 is H or halo; R.sup.6 is —OR.sup.8, —NR.sup.8R.sup.9 or —R.sup.8; R.sup.7 is H or halo; each of R.sup.8 and R.sup.9 is independently H or a group selected from C.sub.1-C.sub.6 alkyl, C.sub.3-C.sub.6 cycloalkyl and 4- to 10-membered heterocyclyl, the group being unsubstituted or substituted; R′ is H or C.sub.1-C.sub.6 alkyl; and one of V and W is CH and the other is N or CH; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.

BENZODIAZEPINE DERIVATIVES FOR TREATING A RESPIRATORY SYNCYTIAL VIRUS (RSV) INFECTION

Benzodiazepine derivatives of formula (I): wherein: each of R.sup.1 and R.sup.2 is independently H or halo; R.sup.3 is H, C.sub.1-C.sub.6 alkyl, —NHR.sup.8 or —OR′; either (i) a, c, and e are all bonds, with b, d and f absent; orb, d and f are all bonds, with a, c and e absent; R.sup.4 is H or a group selected from C.sub.1-C.sub.6 alkyl, C.sub.3-C.sub.6 cycloalkyl and 4- to 10-membered heterocyclyl, the group being unsubstituted or substituted; R.sup.5 is H or halo; R.sup.6 is —OR.sup.8, —NR.sup.8R.sup.9 or —R.sup.8; R.sup.7 is H or halo; each of R.sup.8 and R.sup.9 is independently H or a group selected from C.sub.1-C.sub.6 alkyl, C.sub.3-C.sub.6 cycloalkyl and 4- to 10-membered heterocyclyl, the group being unsubstituted or substituted; R′ is H or C.sub.1-C.sub.6 alkyl; and one of V and W is CH and the other is N or CH; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.

Thermo-responsive hydrogel for intratumoral administration as a treatment in solid tumor cancers

A room temperature injectable thermo-responsive hydrogel comprises a P407 poloxamer base hydrogel, chitosan, 2-Hydroxypropyl β-cyclodextrin and genipin. The chitosan and genipin form an interpenetrating scaffold within the hydrogel in which the chitosan is crosslinked with genipin. Chemotherapeutic drugs can be added to the hydrogel singly or in combination in effective amounts without any loss of thermo-responsiveness in the hydrogel. Therapeutic use of the thermo-responsive hydrogel in the intratumoural treatment of solid cancer is also described.

Thermo-responsive hydrogel for intratumoral administration as a treatment in solid tumor cancers

A room temperature injectable thermo-responsive hydrogel comprises a P407 poloxamer base hydrogel, chitosan, 2-Hydroxypropyl β-cyclodextrin and genipin. The chitosan and genipin form an interpenetrating scaffold within the hydrogel in which the chitosan is crosslinked with genipin. Chemotherapeutic drugs can be added to the hydrogel singly or in combination in effective amounts without any loss of thermo-responsiveness in the hydrogel. Therapeutic use of the thermo-responsive hydrogel in the intratumoural treatment of solid cancer is also described.

METHODS AND COMPOSITIONS FOR SOFT ANTICHOLINERGIC ESTERS
20220401410 · 2022-12-22 ·

Intra-oral formulations comprising soft anticholinergic alkyl esters are useful for treating excessive drooling conditions in subjects, such as humans, suffering from sialorrhea. Preferably, at least one soft anticholinergic ester is provided in an effective amount or concentration in an anhydrous intra-oral formulation that can inhibit excessive drooling resulting from a condition known as sialorrhea.