Patent classifications
A61K47/542
LIPID COMPOSITIONS COMPRISING PEPTIDE-LIPID CONJUGATES
A lipid composition containing a nucleic acid, wherein the lipid composition comprises a peptide-lipid conjugate, is provided. The peptide of the peptide-lipid conjugates can be from 4 to 52 amino acids in length. Methods of using the lipid composition in the in vivo delivery of nucleic acids are further provided.
Pharmaceutical formulation comprising incretin-insulin conjugates
This disclosure relates to stable aqueous pharmaceutical formulations comprising a therapeutically effective amount of an incretin-insulin conjugate as well as methods of using the same, and aqueous pharmaceutical formulations containing an incretin-insulin conjugate which are stable and which provide a protracted pharmacodynamics profile, which include L-arginine HCl and phenol (or m-cresol) as stabilizing agents. The invention also provide a method of treating a patient or individual having a metabolic disease, comprising administering to the patient or individual an effective amount of any of the aqueous pharmaceutical formulations described herein.
Compositions comprising methylphenidate-prodrugs, processes of making and using the same
The present technology is directed to compositions comprising d-threo-methylphenidate conjugates and/or unconjugated methylphenidate. The present technology also relates to compositions and oral formulations comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof. The present technology additionally relates to a pharmaceutical kit containing the composition comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof.
Methods of treating eye disease with tobramycin-related compositions
Disclosed herein are methods of treating conditions of the eye comprising delivering an effective amount of a composition comprising tobramycin or a tobramycin derivative exhibiting similar properties complexed to an agent which facilitates improved permeation of corneal cells, retention in corneal cells, or both. In aspects, such compositions further comprise, or such methods further comprise associated administration of (e.g., as a combined product or via co-administration), one or more additional active agents capable of supporting the treatment of the indication for which the compounds of the invention are directed, such as additional antibacterial compounds, anti-inflammatory agents (e.g., steroids), and the like.
GLP2 RECEPTOR AGONISTS AND METHODS OF USE
Peptide conjugates comprising a peptide that modulates the GLP-2 receptor are provided. The peptide conjugates may be used for treating conditions responsive to modulation of the GLP-2 receptor. Further provided are stapled GLP-2 peptide conjugates.
A METHOD FOR MODIFICATION OF PEPTIDES IMMOBILIZED ON A SOLID SUPPORT BY TRACELESS REDUCTIVELY CLEAVABLE LINKER MOLECULES
The present invention relates to a method for modifying and purifying peptides comprising an immobilizing step, a modification step and a releasing step. In the immobilizing step, a crude linker-tagged peptide L-P is coupled to a solid support yielding an immobilized linker-tagged peptide S-L-P. Subsequently, the immobilized linker-tagged peptide S-L-P is modified with one or more organic molecules yielding an immobilized linker-tagged peptide S-L-mP. Finally, the modified peptide is released via a reduced intermediate RI. The linker molecule is a compound of formula 1, X—Tb—Va-U—Y—Z (1), which can be coupled to a purification resin via the moiety X and to a peptide via the moiety Y under the release of the leaving group Z. T is an optional spacer moiety and V is an optional electron withdrawing moiety. U is an aryl or 5- or 6-membered heteroaryl moiety bound to at least one electron withdrawing moiety V, W or E. The linker is stable under acidic conditions and releases the peptide upon addition of a reducing agent.
LIQUID COMPOSITIONS COMPRISING A LEVODOPA AMINO ACID CONJUGATE AND USES THEREOF
Disclosed herein are liquid pharmaceutical formulations comprising levodopa amino acid conjugates that may further comprise a decarboxylase inhibitor, such as carbidopa, an antioxidant, a solvent, or any other pharmaceutically acceptable excipient. Further disclosed are methods of treating generative conditions and/or conditions characterized by reduced levels of dopamine in the brain, such as Parkinson's disease, comprising administering the disclosed liquid pharmaceutical formulations. Disclosed also are LDAA conjugate compounds.
Methods to induce targeted protein degradation through bifunctional molecules
The present application provides bifunctional compounds which act as protein degradation inducing moieties. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of the bifunctional compounds that link a cereblon-binding moiety to a ligand that is capable of binding to the targeted protein which can be utilized in the treatment of proliferative disorders. The present application also provides methods for making compounds of the application and intermediates thereof.
PSMA-targeting amanitin conjugates
The invention relates to a PSMA-targeting conjugate comprising (a) an amatoxin; (b) a small molecule PSMA-targeting moiety; and (c) optionally a linker linking said amatoxin and said small molecule PSMA-targeting moiety. The invention furthermore relates to a pharmaceutical composition comprising such conjugate.
Supramolecular glycosaminoglycans
Provided herein are glycosylated peptide amphiphiles (GPAs), supramolecular glyconanostructures assembled therefrom, and methods of use thereof. In particular, provided herein are glycosaminoglycan (GAG) mimetic peptide amphiphiles (PAs) and supramolecular GAG mimetic nanostructures assembled therefrom that mimic the biological activities of GAGs, such as heparin, heparan sulfate, hyaluronic acid etc.