C07D209/24

AMINO ACID-, PEPTIDE- AND POLYPEPTIDE-LIPIDS, ISOMERS, COMPOSITIONS, AND USES THEREOF

Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as APPLs. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein:

##STR00001##

wherein m, n, p, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.8, Z, W, Y, and Z are as defined herein.

AMINO ACID-, PEPTIDE- AND POLYPEPTIDE-LIPIDS, ISOMERS, COMPOSITIONS, AND USES THEREOF

Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as APPLs. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein:

##STR00001##

wherein m, n, p, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.8, Z, W, Y, and Z are as defined herein.

Systems and methods for production of artificial eumelanin

Black photoactive materials that comprise synthetic eumelanin polymers are provided, as are methods of making and using the polymers. The synthetic eumelanin polymers are made from the plant oil vanillin, and exhibit defined structural and chemical characteristics (e.g. homogeneity, solubility, etc.) that make them suitable for use in devices that require photoactive materials, such as solar cells.

Systems and methods for production of artificial eumelanin

Black photoactive materials that comprise synthetic eumelanin polymers are provided, as are methods of making and using the polymers. The synthetic eumelanin polymers are made from the plant oil vanillin, and exhibit defined structural and chemical characteristics (e.g. homogeneity, solubility, etc.) that make them suitable for use in devices that require photoactive materials, such as solar cells.

Process for the preparation of Zafirlukast and analogs thereof

The present invention relates to a process for the preparation of (1-alkylindol-3-ylmethyl) benzoic acid derivatives, in particular Zafirlukast and analogs thereof. Further, this process is based on protection group free and CH bond activation strategy involving all step catalytic transformation sequence and comprises the following steps: Sonogashira coupling, indole formation by Sp.sup.3 CH activation, reductive hydrogenation and amidation.

Method for oxygenative coupling of alkynes using acid catalyst

The present disclosure relates to a method for preparing various physiologically active pharmaceutical ingredients, such as a 1,1-diaryl compound and a 1,1-diheteroaryl compound (specifically, a 1,1-diaryl carbonyl compound), in an economical and convenient manner under mild conditions without using an expensive transition metal catalyst by activating an alkyne compound (e.g., an ynamide) using a Brnsted acid as a catalyst to induce a reaction of the activated alkyne compound and a NO bond oxidant to form an adduct intermediate and then inducing a coupling reaction of the adduct intermediate with various nucleophilic organic compounds (e.g., a nucleophilic arene compound).

Method for oxygenative coupling of alkynes using acid catalyst

The present disclosure relates to a method for preparing various physiologically active pharmaceutical ingredients, such as a 1,1-diaryl compound and a 1,1-diheteroaryl compound (specifically, a 1,1-diaryl carbonyl compound), in an economical and convenient manner under mild conditions without using an expensive transition metal catalyst by activating an alkyne compound (e.g., an ynamide) using a Brnsted acid as a catalyst to induce a reaction of the activated alkyne compound and a NO bond oxidant to form an adduct intermediate and then inducing a coupling reaction of the adduct intermediate with various nucleophilic organic compounds (e.g., a nucleophilic arene compound).

ASH1L INHIBITORS AND METHODS OF TREATMENT THEREWITH

Provided herein are small molecules that bind to ASH1L and inhibit ASH1L activity, and methods of use thereof for the treatment of disease, including acute leukemia, solid cancers and other diseases dependent on activity of ASH1L.

ASH1L INHIBITORS AND METHODS OF TREATMENT THEREWITH

Provided herein are small molecules that bind to ASH1L and inhibit ASH1L activity, and methods of use thereof for the treatment of disease, including acute leukemia, solid cancers and other diseases dependent on activity of ASH1L.

PSMA TARGETED FLUORESCENT AGENTS FOR IMAGE GUIDED SURGERY
20200216402 · 2020-07-09 ·

Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.