C07K5/068

Pharmaceutical composition for the prevention and treatment of cardiovascular disease comprising the peptide having the ability to inhibit angiotensin-1 converting enzyme as an active ingredient

The present invention relates to a peptide separated from the fraction of oyster enzyme hydrolysate displaying the ability of suppressing angiotensin converting enzyme (ACE) and a pharmaceutical composition for the prevention and treatment of cardiovascular disease comprising the said peptide as an active ingredient. Particularly, the peptide separated from the fraction of the oyster enzyme hydrolysate of the present invention significantly inhibits ACE activity, and thus brings blood pressure regulating effect and antihypertensive effect. Therefore, the fraction of the oyster enzyme hydrolysate of the invention or the peptide separated from the same can be effectively used as an active ingredient of a pharmaceutical composition for the prevention or treatment of cardiovascular disease.

Crystalline dipeptides useful in the synthesis of elamipretide

Disclosed are crystalline forms of L-Lys(Boc)-Phe-NH.sub.2 and Boc-D-Arg-DMT. The crystalline forms may be used in the synthesis of elamipretide.

SUBSTITUTION OF HISTIDINE WITH 2-THIOHISTIDINE IN BIOACTIVE PEPTIDES
20240199687 · 2024-06-20 ·

Presented is a method to incorporate 2-thiohistidine (2-thioHis) into a peptide. Also provided are peptides incorporating 2-thioHis, compositions, and methods of using the peptides incorporating 2-thioHis. The methods may be methods for scavenging metals and/or radicals or reducing oxidative stress. 2-thioHis has the following structure:

##STR00001##

Peptide macrocycles against <i>Acinetobacter baumannii</i>

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.

Conjugates and methods of using the same

Disclosed are conjugates including a recognition element covalently bonded to or linked through a linker to a payload. The payload is a pharmaceutical agent (e.g., an antineoplastic agent, anti-infective agent, or anti-inflammatory agent) or a diagnostic agent. Also disclosed are methods of using the conjugates.

NMDA ANTAGONIST PRODRUGS

Prodrugs of an NMDA antagonist, (S)-1-phenyl-2-(pyridin-2-yl)ethanamine, useful for the treatment of depression (particularly major depressive disorder) or pain; compositions comprising them, and methods of making them.

NEUROPEPTIDE S RECEPTOR (NPSR) AGONISTS

Neuropeptide S receptor agonists are provided. The NPS agonists include trimeric, tetrameric, pentameric or hexameric peptidomimetic analogs exhibiting affinity for and activity at the neuropeptide S receptor. The peptidomimetic molecules may be useful in the treatment of disorders, syndromes and conditions mediated by modulation of the neuropeptide S receptor such as substance abuse, narcolepsy, insomnia, obesity, cognitive decline, dementia, Alzheimer's disease, panic disorder, generalized anxiety, PTSD, phobias, schizophrenia and as supportive medication during any kind of cessation program in cognitive behavioral therapy, such as drug addiction, eating disorders and gambling.

DIPEPTIDE ANALOGS AS TGF-BETA INHIBITORS

The present disclosure is concerned with dipeptide analogs that are capable of inhibiting TGF- and methods of treating cancers such as, for example, multiple myeloma and a hematologic malignancy, methods for immunotherapy, and methods of treating fibrotic conditions using these compounds. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

AROMATIC-CATIONIC PEPTIDES AND USES OF SAME
20190106458 · 2019-04-11 ·

The disclosure provides compositions and methods relating to aromatic-cationic peptides. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide to subjects in need thereof For example, the peptides may be administered to subjects in need of a mitochondrial-targeted antioxidant.

Macrocyclic inhibitors of flaviviridae viruses

Provided are compounds of Formula I: ##STR00001## and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of virus infections, particularly hepatitis C infections.