C07C13/00

Biologically active compound conjugated to a stapled or stitched peptide

The invention relates to improvements in drug delivery and more particularly to the use of Cell Penetrating Agents (CPA's) or Cell Penetrating Peptides (CPP's) which have been stabilized by, for example: i) stapling two amino acids to form Stapled CPP's (StaP's) or ii) stitching three or more amino acids to form stitched CPP's (StiP's). These stabilized CPP's are conjugated to a drug or Biologically Active Compound (BAC) directly or via a Bi-Functional Linker (BFL) so that the BAC can be carried through a cell membrane by the CPP. The resulting molecules are referred to as Drug Carrying Cell Penetrating Molecules (DCCPM's). The preferred BAC is an electrically low charge carrying oligonucleotide such as a phosphorodiamidate morpholino oligonucleotide (PMO). The invention also relates to a method of facilitating the uptake of a BAC into a cell, the use of a DCCPM in the treatment of a disease requiring alteration of an endogenous or exogenous gene, a method of improving the bioavailability of a drug or BAC, a method of introducing a drug or BAC to a site which is refractory to the drug or BAC in its native state, a method of treating a subject comprising administering the DCCPM's of the invention and to a pharmaceutical composition comprising the DCCPM and one or more pharmaceutically acceptable excipients.

Biologically active compound conjugated to a stapled or stitched peptide

The invention relates to improvements in drug delivery and more particularly to the use of Cell Penetrating Agents (CPA's) or Cell Penetrating Peptides (CPP's) which have been stabilized by, for example: i) stapling two amino acids to form Stapled CPP's (StaP's) or ii) stitching three or more amino acids to form stitched CPP's (StiP's). These stabilized CPP's are conjugated to a drug or Biologically Active Compound (BAC) directly or via a Bi-Functional Linker (BFL) so that the BAC can be carried through a cell membrane by the CPP. The resulting molecules are referred to as Drug Carrying Cell Penetrating Molecules (DCCPM's). The preferred BAC is an electrically low charge carrying oligonucleotide such as a phosphorodiamidate morpholino oligonucleotide (PMO). The invention also relates to a method of facilitating the uptake of a BAC into a cell, the use of a DCCPM in the treatment of a disease requiring alteration of an endogenous or exogenous gene, a method of improving the bioavailability of a drug or BAC, a method of introducing a drug or BAC to a site which is refractory to the drug or BAC in its native state, a method of treating a subject comprising administering the DCCPM's of the invention and to a pharmaceutical composition comprising the DCCPM and one or more pharmaceutically acceptable excipients.

BIOLOGICALLY ACTIVE COMPOUNDS
20230158166 · 2023-05-25 ·

The invention relates to improvements in drug delivery and more particularly to the use of Cell Penetrating Agents (CPA's) or Cell Penetrating Peptides (CPP's) which have been stabilized by, for example: i) stapling two amino acids to form Stapled CPP's (StaP's) or ii) stitching three or more amino acids to form stitched CPP's (StiP's). These stabilized CPP's are conjugated to a drug or Biologically Active Compound (BAC) directly or via a Bi-Functional Linker (BFL) so that the BAC can be carried though a cell membrane by the CPP. The resulting molecules are referred to as Drug Carrying Cell Penetrating Molecules (DCCPM's). The preferred BAC is an electrically low charge carrying oligonucleotide such as a phosphorodiamidate morpholino oligonucleotide (PMO). The invention also relates to a method of facilitating the uptake of a BAC into a cell, the use of a DCCPM in the treatment of a disease requiring alteration of an endogenous or exogenous gene, a method of improving the bioavailability of a drug or BAC, a method of introducing a drug or BAC to a site which is refractory to the drug or BAC in its native state, a method of treating a subject comprising administering the DCCPM's of the invention and to a pharmaceutical composition comprising the DCCPM and one or more pharmaceutically acceptable excipients.

BIOLOGICALLY ACTIVE COMPOUNDS
20230158166 · 2023-05-25 ·

The invention relates to improvements in drug delivery and more particularly to the use of Cell Penetrating Agents (CPA's) or Cell Penetrating Peptides (CPP's) which have been stabilized by, for example: i) stapling two amino acids to form Stapled CPP's (StaP's) or ii) stitching three or more amino acids to form stitched CPP's (StiP's). These stabilized CPP's are conjugated to a drug or Biologically Active Compound (BAC) directly or via a Bi-Functional Linker (BFL) so that the BAC can be carried though a cell membrane by the CPP. The resulting molecules are referred to as Drug Carrying Cell Penetrating Molecules (DCCPM's). The preferred BAC is an electrically low charge carrying oligonucleotide such as a phosphorodiamidate morpholino oligonucleotide (PMO). The invention also relates to a method of facilitating the uptake of a BAC into a cell, the use of a DCCPM in the treatment of a disease requiring alteration of an endogenous or exogenous gene, a method of improving the bioavailability of a drug or BAC, a method of introducing a drug or BAC to a site which is refractory to the drug or BAC in its native state, a method of treating a subject comprising administering the DCCPM's of the invention and to a pharmaceutical composition comprising the DCCPM and one or more pharmaceutically acceptable excipients.

POLYMER, MIXTURE AND COMPOUND CONTAINING SAME, AND ORGANIC ELECTRONIC DEVICE AND MONOMER THEREOF
20170358751 · 2017-12-14 ·

Disclosed are a polymer, and a mixture or a formulation and an organic electronic device containing same, and applications thereof, and further a monomer of which the polymer is made; the polymer comprises on its side chain a repeating structure unit E, characterizing in that its (S1(E)−T1(E))≦0.35 eV or even less, which may allow the said polymer having thermally activated delayed fluorescence (TADF) property. Thus a TADF polymer suitable for printing processes is provided, thereby reducing OLED manufacturing costs.

Method for the Production of Carbon Nanotube Structures
20170327378 · 2017-11-16 ·

The present invention relates to a method for the production of carbon nanotube structures.

ORGANIC LIGHT-EMITTING DEVICE

Provided is an organic light-emitting device including a first compound and a second compound that offers low driving voltage and high efficiency. The organic light-emitting device includes an emission layer between a first electrode and a second electrode, and an electron transport region between the second electrode and the emission layer. The electron transport region includes the first compound. A hole transport region between the first electrode and the emission layer includes the second compound.

TH17 DIFFERENTIATION MARKERS FOR ACNE AND USES THEREOF
20210404004 · 2021-12-30 · ·

A method is described for using IL-12Rβ1/IL-23R, CCR6, BATF, AHR, STAT3, IRF4 crucial actors in TH17 cells differentiation as markers for acne. Also described are methods of their use to diagnose acne, and to screen inhibitors of Th17 differentiation. In particular, methods are described for inhibiting IL12Rβ1/1L-23R, CCR6, BATF, AHR, STAT3, IRF4 and the use of these screened inhibitors in acne treatment.

Organic light-emitting device

Provided is an organic light-emitting device including a first compound and a second compound that offers low driving voltage and high efficiency. The organic light-emitting device includes an emission layer between a first electrode and a second electrode, and an electron transport region between the second electrode and the emission layer. The electron transport region includes the first compound. A hole transport region between the first electrode and the emission layer includes the second compound.

Organic light-emitting device

Provided is an organic light-emitting device including a first compound and a second compound that offers low driving voltage and high efficiency. The organic light-emitting device includes an emission layer between a first electrode and a second electrode, and an electron transport region between the second electrode and the emission layer. The electron transport region includes the first compound. A hole transport region between the first electrode and the emission layer includes the second compound.