C07K5/06026

SMAC MIMETICS USED AS IAP INHIBITORS AND USE THEREOF

Disclosed are a class of SMAC mimetics used as IAP inhibitors, and in particular disclosed are compounds as shown in formula (I), isomers thereof, and pharmaceutically acceptable salts thereof. The IAP inhibitors are drugs for treating cancers, in particular breast cancer.

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METAL DI-AMINO ACID CHELATES OR METAL TRI-AMINO ACID CHELATES
20210371374 · 2021-12-02 ·

The present disclosure relates to metal di-amino acid chelates and metal tri-amino acid chelates.

Method of enhancing a brain or cognitive function
11369659 · 2022-06-28 · ·

There is provided a composition for improving memory, learning ability, and cognitive ability and a method of enhancing a brain or cognitive function by administering the composition to a subject in need thereof. It has been confirmed that a peptide having a C-terminal region ended to GAG had an effect of improving the memory. In order for the peptide to have the effect, it has been confirmed that the peptide should be a peptide of which the length consists of at least 4 amino acids. Further, it has been confirmed that a peptide of which the length of the peptide having the C-terminal region ended to GAG consists of 5 to 9 amino acids has the same effect. As a result, the peptide of the present invention can be used as the composition for improving memory, learning ability, and cognitive ability, and the method of enhancing a brain or cognitive function.

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.

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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.

SMAC mimetics used as IAP inhibitors and use thereof

Disclosed are a class of SMAC mimetics used as IAP inhibitors, and in particular disclosed are compounds as shown in formula (I), isomers thereof, and pharmaceutically acceptable salts thereof. The IAP inhibitors are drugs for treating cancers, in particular breast cancer. ##STR00001##

Reagents based on a tertiary amine backbone to introduce chemical functionality in nucleic acids and sequence-controlled polymers

It is provided an achiral, non-nucleosidic backbone for phosphoramidites that can be inserted with high yields in nucleic acid strands and sequence-controlled oligo(phosphodiester)s through solid phase synthesis (SPS) using a DNA synthesizer. From this backbone, platforms with useful chemical handles were synthesized, further functionalized, transformed into phosphoramidites and attached to nucleic acid strands and sequence-controlled oligo(phosphodiester)s. The backbone is based on a tertiary amine with a 3-6 carbon spacer between the central nitrogen and the two external hydroxyls. The spacer has been optimized to increase coupling yields and stability.

COMPOSITIONS COMPRISING ENZYME-CLEAVABLE AMPHETAMINE PRODRUGS AND INHIBITORS THEREOF

The embodiments provide Compound AM-9, Amphetamine-arginine-glycine-acetate, or acceptable salts, solvates, and hydrates thereof and Compound AM-10, Amphetamine-arginine-alanine-acetate. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug, Compound AM-9 or Compound AM-10, that provides controlled release of amphetamine Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of amphetamine from the prodrug so as to attenuate enzymatic cleavage of the prodrug.

CRYSTALLIZATION OF SMAC MIMIC USED AS IAP INHIBITOR AND PREPARATION METHOD THEREOF

Provided are a crystallization of an SMAC mimic used as an IAP inhibitor and a preparation method thereof; also comprised is the use of said crystallization in the preparation of a drug for treating cancer benefiting from cIAP1 inhibition. The compound of formula (I) has high crystallization stability and low hygroscopicity, and has advantages in terms of physical properties, safety, and metabolic stability, and has high drug value.

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SMAC mimetic

A SMAC mimetic and pharmaceutical compositions thereof and methods of use.