C07K5/097

High penetration drugs and their compositions thereof for treatment of Parkinson diseases
11084813 · 2021-08-10 · ·

One aspect of the invention provides a composition of novel high penetration compositions (HPC) or a high penetration prodrug (HPP) for treatment of Parkinson's disease. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

Process for the preparation of cyclic depsipeptides

Processes for preparing compounds of Formula (1) and Formula (2) are described, wherein X, Y, Z, R.sub.1-R.sub.7, L and n are defined herein. Intermediates useful in the preparation of the compounds of Formula (1) and Formula (2) are also described. ##STR00001##

Inhibitors of transglutaminases

The invention relates to the compound of general formula (I) as novel inhibitors of transglutaminases, to methods for producing the inventive compounds, to pharmaceutical compositions containing said inventive compounds and to their use for the prophylaxis and treatment of diseases associated with transglutaminases.

Transfection complexes and methods of using the same
11085056 · 2021-08-10 · ·

Disclosed herein are transfection complexes comprising at least one cell surface ligand; at least one helper lipid component; and a transfection enhancer. Also disclosed are pharmaceutical compositions comprising the disclosed transfection complexes, and a pharmaceutically acceptable carrier. Further, disclosed are methods of transfecting a cell, the method comprising the steps of: obtaining a transfection complex as disclosed; and contacting a cell with the transfection complex.

Peptide macrocycles against Acinetobacter baumannii

The present invention provides compounds of formula (I) ##STR00001## wherein X.sup.1 to X.sup.8 and R.sup.1 to R.sup.8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.

MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS

Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

Trifluoromethylpropanamide derivatives as HTRA1 inhibitors

The invention provides novel compounds having the general formula (I) ##STR00001##
wherein R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.3, R.sup.8, R.sup.10, R.sup.11 and R.sup.23 are as described herein, compositions including the compounds and methods of using the compounds.

INHIBITORS OF BLOOD COAGULATION FACTOR XIII
20210147478 · 2021-05-20 ·

The invention relates to a compound of general formula (I) as novel inhibitor of blood coagulation factor XIII, methods for synthesis thereof and to use thereof for the prophylaxis or treatment of diseases associated with blood coagulation factor XIII.

##STR00001##

MODIFIED PEPTIDES FOR USE IN TREATING NEURODEGENERATIVE DISORDERS

The invention relates to neurodegenerative disorders, and in particular to novel peptides, peptidomimetics, compositions, therapies and methods for treating such conditions, for example Alzheimer's disease.

Methods and compositions for preventing and treating A-beta oligomer-associated and/or -induced diseases and conditions

The disclosure pertains to methods of treating or preventing a disease or condition associated with and/or induced by soluble A-beta oligomer such as Alzheimer's disease by administering to a subject in need thereof conformation specific and/or selective antibodies or binding fragments thereof and related products.