C07K5/068

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.

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.

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.

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.

AROMATIC-CATIONIC PEPTIDES AND USES OF SAME

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.

Antibacterial agents

The invention concerns agents with antibacterial activity, their production and use in the treatment of bacterial infections in animals, including man. The agents are derivatives of vancomycin-type antibiotics, of structure XW-L-V, wherein X is hydrogen, acetyl or a lipophilic membrane-insertive element, W is a basic peptide or basic amino acid; L is a linking group and V is a glycopeptide moiety which inhibits peptidoglycan biosynthesis in bacteria.

N-carboxyanhydride-based-scale synthesis of elamipretide

Disclosed are methods of making elamipretide (MTP-131), a peptide compound with therapeutic potential for treating various mitochondrial myopathies. The synthesis of the peptide can be achieved via the use of N-carboxyanhydride-modified amino acid residues, which increases the efficiency of the synthetic process and the purity of the peptide product generated.

PROTEASE-ACTIVATED CONTRAST AGENTS FOR IN VIVO IMAGING

Compounds useful as contrast agents in image-guided surgery are provided. The compounds comprise a latent cationic lysosomotropic fragment that is detectable upon cleavage by lysosomal proteases within treated tissues, particularly within tumors and other diseased tissues. Also provided are compositions comprising the compounds and methods for using the compounds, for example in dynamically monitoring protease activity in vivo during image-guided tumor resection surgery.

CRYSTALLINE DIPEPTIDES USEFUL IN THE SYNTHESIS OF ELAMIPRETIDE
20200283476 · 2020-09-10 ·

Disclosed are crystalline forms of L-Lys(Boc)-Phe-NH.sub.2 and Boc-D-Arg-DMT.

METHODS, COMPOUNDS, COMPOSITIONS AND VEHICLES FOR DELIVERING 3-AMINO-1-PROPANESULFONIC ACID

The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to the prevention and treatment of Alzheimer's disease