C07K5/06156

AMIDE DERIVATIVES OF N-UREA SUBSTITUTED AMINO ACIDS AS FORMYL PEPTIDE RECEPTOR LIKE-1 (FPRL-1) RECEPTOR MODULATORS

The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.

Agent for Eliminating Pluripotent Stem Cells

An agent for eliminating a pluripotent stem cell, the agent comprising an antibody-drug conjugate that releases a compound represented by formula (1-1):

##STR00001##

wherein b represents an integer of 1 to 5; and Z represents a group represented by formula (Z-1) or formula (Z-2),
or a salt thereof.

METHOD OF PREPARING A DON PRODRUG FROM L-PYROGLUTAMIC ACID

The present disclosure provides a method of preparing a compound of Formula I, wherein R.sup.1 is C.sub.1-C.sub.4 alkyl; R.sup.2 is C1-C4 alkyl; and R.sup.3 is selected from the group consisting of C.sub.1-C.sub.6 alkyl, (aryl)alkyl, and (heteroaryl)alkyl in >95% chemical purity and >95% enantiomeric excess.

##STR00001##

PIEZOELECTRIC PEPTIDE-BASED MATERIALS AND PIEZOELECTRIC DEVICES CONTAINING SAME

A piezoelectric transducer is provided herein, comprising a three-dimensional structure made of a plurality of peptides, the peptides being self-assembling and the structure being piezoelectric, wherein at least a portion, or each, of said plurality of peptides comprises peptides of 2 to 10 amino acid residues, provided that the plurality of peptides is not consisted of a plurality of Phe-Phe dipeptides. Further described herein are peptides having an amino acid sequence Hyp-Phe-Phe, Boc-Dip-Dip, (L)Trp-(D)Trp or (D)Trp-(L)Trp, as well as three-dimensional structures comprising such peptides.

Tripeptide compound, preparation method therefor, and application thereof

Provided are a tripeptide compound, a preparation method therefor, and an application thereof. The structure of the related compound is represented by formula (I). The provided compound has angiotensin converting enzyme inhibiting bioactivity, and the compound and a pharmaceutical composition thereof play a role in preventing and treating hypertension and other cardiocerebral vascular system diseases.

INHIBITORS OF GROWTH FACTOR ACTIVATION ENZYMES

The present invention generally relates to compounds that are useful for inhibiting one or more of hepatocyte growth factor activator, matriptase, hepsin, Factor Xa, or thrombin. The present invention also relates to various methods of using the inhibitor compounds including treating a malignancy, a pre-malignant condition, or cancer by administering an effective amount of the inhibitor to a subject in need thereof.

CRYSTALLINE FORMS OF SOLVATES OF TRYPTOPHAN DERIVATIVES, COMPOSITIONS COMPRISING THEM AND USES THEREOF

The invention provides crystalline forms of solvates of tryptophan derivatives of compound (1), compositions comprising them, processes for their preparations and methods of use thereof.

Method of preparing a DON prodrug from L-pyroglutamic acid

The present disclosure provides a method of preparing a compound of Formula I, wherein R.sup.1 is C.sub.1-C.sub.4 alkyl; R.sup.2 is C1-C4 alkyl; and R.sup.3 is selected from the group consisting of C.sub.1-C.sub.6 alkyl, (aryl)alkyl, and (heteroaryl)alkyl in >95% chemical purity and >95% enantiomeric excess. ##STR00001##

SULFOMALEIMIDE-BASED LINKERS AND CORRESPONDING CONJUGATES

The present invention relates to a linker of the following formula (I) or a salt thereof: (I). The present invention relates to a linker-drug conjugate of the following formula (II) or a salt thereof: (II). The present invention relates also to a binding unit-drug corrugate, such as an antibody-drug conjugate, of the following formula (III) or (IV) or a salt thereof: (III), (IV), as well as a pharmaceutical composition comprising such a binding unit-drug corrugate and its use in the treatment of cancer.

##STR00001##

N-acyldipeptide derivatives and their uses

Methods of treating aging related skin changes and of increasing skin thickness with topical administration of N-acyldipeptide derivatives are described. Compositions comprising N-acyldipeptide derivatives, are therapeutically effective for increasing skin thickness, and for treating extrinsic and intrinsic aging and aging related skin changes, such as fine lines, wrinkles, photoaging, hyperpigmentation, laxity, age spots, lentigines, mottled skin, and cellulite.