C07K5/06121

PSMA-targeted NIR dyes and their uses
11484607 · 2022-11-01 · ·

The present disclosure relates to prostate specific membrane antigen (PSMA) targeted compounds conjugated to near-infra red (NIR) dyes and methods for their therapeutic and diagnostic use. More specifically, this disclosure provides compounds and methods for diagnosing and treating diseases associated with cells and/or vasculature expressing prostate specific membrane antigen (PSMA), such as prostate cancer and related diseases. The disclosure further describes methods and compositions for making and using the compounds, methods incorporating the compounds, and kits incorporating the compounds.

METHOD FOR PHOTOCLEAVAGE OF AMIDE BONDS
20220289665 · 2022-09-15 ·

The present disclosure provides a method for photocleavage of an amide bond, the method has mild reaction conditions and can realize the cleavage of amide bonds by using light. The method comprises the following steps: subjecting 2,4-dinitrofluorobenzene to a reaction with an amino group of a substance represented by structural formula I with an α-amino acid at the end to produce a compound 1 represented by structural formula II; then under light irradiation, subjecting the compound 1 to a cleavage reaction of amide bond;

##STR00001##

Wherein, R1 is the side chain group of α-amino acid; R2 is: aryl, aliphatic hydrocarbon, —CH(R)—COOH or polypeptide.

COMPOUND, SYNTHESIS INTERMEDIATE, USE, PHARMACEUTICAL COMPOSITION AND NEUROMODULATORY THERAPEUTIC METHOD
20220098237 · 2022-03-31 ·

A peptide compound in the fields of pharmaceutical sciences, medicine, chemistry and biotechnology, that shows stability and ease of handling when compared to the more closely related peptidic compounds. A pharmaceutical composition that includes the peptidic compound and shows therapeutic results even when administered orally. In some embodiments, administration of the pharmaceutical composition provides superior therapeutic results when compared to the effects of hemopressin and cannabidiol. In some embodiments, oral administration of the pharmaceutical composition provides neuromodulation, both in the curative or prophylactic treatment of seizures, modulation of pain threshold and important neuroprotection, and reduction of the clinical symptoms of Multiple Sclerosis.

PSMA-TARGETED NIR DYES AND THEIR USES

The present disclosure relates to prostate specific membrane antigen (PSMA) targeted compounds conjugated to near-infra red (NIR) dyes and methods for their therapeutic and diagnostic use. More specifically, this disclosure provides compounds and methods for diagnosing and treating diseases associated with cells and/or vasculature expressing prostate specific membrane antigen (PSMA), such as prostate cancer and related diseases. The disclosure further describes methods and compositions for making and using the compounds, methods incorporating the compounds, and kits incorporating the compounds.

N-lipoic-amino acid or peptide, derivatives and their uses
11155531 · 2021-10-26 · ·

Novel compounds of N-Lipoic-amino acid, N-Lipoic-peptides and their derivatives are described. Also described are compositions and method of compositions containing the derivatives of the amino acids or peptides, and their uses including treating and preventing dermatological or cosmetic conditions or other disorders of the cutaneous system. Compositions and methods of using the compositions for skin lightening and cosmetics are also disclosed.

Tripeptide epoxy ketone protease inhibitors

Provided herein are tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): ##STR00001##
and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of diseases including inflammation and neurodegenerative disease.

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.

PSMA-TARGETED NIR DYES AND THEIR USES
20210046194 · 2021-02-18 ·

The present disclosure relates to prostate specific membrane antigen (PSMA) targeted compounds conjugated to near-infra red (NIR) dyes and methods for their therapeutic and diagnostic use. More specifically, this disclosure provides compounds and methods for diagnosing and treating diseases associated with cells and/or vasculature expressing prostate specific membrane antigen (PSMA), such as prostate cancer and related diseases. The disclosure further describes methods and compositions for making and using the compounds, methods incorporating the compounds, and kits incorporating the compounds.

UNIVERSAL ABT COMPOUNDS AND USES THEREOF
20200390895 · 2020-12-17 ·

Among other things, the present disclosure provides compounds comprising universal antibody binding moieties and targeting moieties. In some embodiments, provided compounds recruit various types of antibodies to diseased cells such as cancer cells, and induce immune activities to kill such cells. Provided technologies are useful for treating various diseases including cancer.

TRIPEPTIDE EPOXY KETONE PROTEASE INHIBITORS
20200207809 · 2020-07-02 ·

Provided herein are tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X):

##STR00001##

and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of diseases including inflammation and neurodegenerative disease.