C07C235/64

Multivalent compounds for use in the treatment and prevention of brain damage
09975846 · 2018-05-22 · ·

The present invention relates to compounds of general formula (I) ##STR00001## and pharmaceutically acceptable salts thereof; wherein R1-R11, L, Z, Y, and Z are as defined in the claims. The invention also relates to said compounds for use as a medicament and particularly in the treatment of traumatic brain injury.

Multivalent compounds for use in the treatment and prevention of brain damage
09975846 · 2018-05-22 · ·

The present invention relates to compounds of general formula (I) ##STR00001## and pharmaceutically acceptable salts thereof; wherein R1-R11, L, Z, Y, and Z are as defined in the claims. The invention also relates to said compounds for use as a medicament and particularly in the treatment of traumatic brain injury.

Histone acetyltransferase modulators and uses thereof

The invention provides compounds and compositions comprising compounds that modulate histone acyl transferase (HAT). The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a compound that modulates HAT to a subject.

Phosphonium compound, preparation method thereof, epoxy resin composition including the same, and semiconductor device prepared by using the same

A phosphonium compound, a method of preparing the same, an epoxy resin composition including the same, and a semiconductor device encapsulated with the same, the compound being represented by Formula 1: ##STR00001##

Phosphonium compound, preparation method thereof, epoxy resin composition including the same, and semiconductor device prepared by using the same

A phosphonium compound, a method of preparing the same, an epoxy resin composition including the same, and a semiconductor device encapsulated with the same, the compound being represented by Formula 1: ##STR00001##

NOVEL METHODS

Provided are uses of selective aquaporin inhibitors, e.g., of aquaporin-4 or aquaporin-2, e.g., certain phenylbenzamide compounds, for the treatment or prophylaxis of transplant rejection and the protection of the heart during heart surgery. Provided is the use of selective aquaporin inhibitors, e.g., of aquaporin-4 (AQP4) or aquaporin-2 (AQP2) for the treatment or prophylaxis of transplant rejection and for the protection of the heart during heart surgery.

NOVEL METHODS

Provided are uses of selective aquaporin inhibitors, e.g., of aquaporin-4 or aquaporin-2, e.g., certain phenylbenzamide compounds, for the treatment or prophylaxis of transplant rejection and the protection of the heart during heart surgery. Provided is the use of selective aquaporin inhibitors, e.g., of aquaporin-4 (AQP4) or aquaporin-2 (AQP2) for the treatment or prophylaxis of transplant rejection and for the protection of the heart during heart surgery.

Crystal structure of bifunctional transglycosylase PBP1b from E. coli and inhibitors thereof

The crystal structure at 2.16 resolution of the full-length bacterial bifunctional transglycosylase penicillin-binding protein 1b (PBP1b) from Escherichia coli, in complex with its inhibitor moenomycin, is provided. The atomic coordinates of the complex as well as the moenomycin binding site are provided. Three dimensional structures of amino acid residues involved in moenomycin binding and transglycosylation activity are identified. Binding site for peptidoglycan synthesis inhibitors comprising inhibitor-binding site comprises amino acid residues from at least one of transglycosylase (TG), UvrB domain 2 homolog (UB2H) and transmembrane (TM) domains of PBP1b are identified at an atomic level of resolution. Methods for rational drug design based on the atomic coordinates are provided. Methods for screening for antibiotics based on anisotropic binding assay and transglycosylase inhibitor assays are provided. Novel antibiotics based on the screening assays of the invention are disclosed.

Crystal structure of bifunctional transglycosylase PBP1b from E. coli and inhibitors thereof

The crystal structure at 2.16 resolution of the full-length bacterial bifunctional transglycosylase penicillin-binding protein 1b (PBP1b) from Escherichia coli, in complex with its inhibitor moenomycin, is provided. The atomic coordinates of the complex as well as the moenomycin binding site are provided. Three dimensional structures of amino acid residues involved in moenomycin binding and transglycosylation activity are identified. Binding site for peptidoglycan synthesis inhibitors comprising inhibitor-binding site comprises amino acid residues from at least one of transglycosylase (TG), UvrB domain 2 homolog (UB2H) and transmembrane (TM) domains of PBP1b are identified at an atomic level of resolution. Methods for rational drug design based on the atomic coordinates are provided. Methods for screening for antibiotics based on anisotropic binding assay and transglycosylase inhibitor assays are provided. Novel antibiotics based on the screening assays of the invention are disclosed.

STAT3 inhibitor

Provided are STAT3 inhibitors and methods of treating inflammation or a hyperproliferative disease such as, e.g., cancer. In some aspects, compounds may be used to treat breast cancer, a head/neck cancer, a lung cancer, a prostate cancer, or pancreatic cancer.