Disclosed are a thiazolone derivative of N6022 and a pharmaceutical use thereof. The characteristic structure of the thiazolone derivative of N6022 is:

##STR00001##

Compared to N6022, the compound of the present disclosure has good oral bioavailability and a longer half-life period. In in-vitro experiments, administering the compound of the present disclosure can improve migration ability, tube formation ability and, the permeability of human umbilical vein endothelial cells caused by high glucose, and administering the compound of the present disclosure at an animal level can obviously promote the angiogenesis and blood flow recovery of ischemic lateral limbs of diabetic mice. Overall, it suggests that the compound of the present disclosure can be used for treating diseases related to diabetic vascular complications.

Disclosed are a thiazolone derivative of N6022 and a pharmaceutical use thereof. The characteristic structure of the thiazolone derivative of N6022 is:

##STR00001##

Compared to N6022, the compound of the present disclosure has good oral bioavailability and a longer half-life period. In in-vitro experiments, administering the compound of the present disclosure can improve migration ability, tube formation ability and, the permeability of human umbilical vein endothelial cells caused by high glucose, and administering the compound of the present disclosure at an animal level can obviously promote the angiogenesis and blood flow recovery of ischemic lateral limbs of diabetic mice. Overall, it suggests that the compound of the present disclosure can be used for treating diseases related to diabetic vascular complications.

A method of inhibiting phosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system an effective amount of a of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1, and contains at least four of the six pharmacophores of FIGS. 35-40.

A method of inhibiting phosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system an effective amount of a of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1, and contains at least four of the six pharmacophores of FIGS. 35-40.

Disclosed are a thiazolone derivative of N6022 and a pharmaceutical use thereof. The characteristic structure of the thiazolone derivative of N6022 is: ##STR00001##
Compared to N6022, the compound of the present disclosure has good oral bioavailability and a longer half-life period. In in-vitro experiments, administering the compound of the present disclosure can improve migration ability, tube formation ability and, the permeability of human umbilical vein endothelial cells caused by high glucose, and administering the compound of the present disclosure at an animal level can obviously promote the angiogenesis and blood flow recovery of ischemic lateral limbs of diabetic mice. Overall, it suggests that the compound of the present disclosure can be used for treating diseases related to diabetic vascular complications.

Disclosed are a thiazolone derivative of N6022 and a pharmaceutical use thereof. The characteristic structure of the thiazolone derivative of N6022 is: ##STR00001##
Compared to N6022, the compound of the present disclosure has good oral bioavailability and a longer half-life period. In in-vitro experiments, administering the compound of the present disclosure can improve migration ability, tube formation ability and, the permeability of human umbilical vein endothelial cells caused by high glucose, and administering the compound of the present disclosure at an animal level can obviously promote the angiogenesis and blood flow recovery of ischemic lateral limbs of diabetic mice. Overall, it suggests that the compound of the present disclosure can be used for treating diseases related to diabetic vascular complications.

An assay for Alzheimer's disease pathology (AD) in a living patient is disclosed wherein an amount of α7nAChR or TLR4 in a FLNA-captured protein complex or α7nAChR in an Aβ-captured protein complex or α7nAChR-FLNA, TLR4-FLNA and/or α7nAChR-Aβ.sub.42 complex present as a protein-protein complex in a sample is determined and compared to the amount in a standard sample from a person free of AD pathology. An amount greater than in the standard sample indicates AD pathology. Also disclosed is an assay predictive of prognosis for treatment with a medicament in which the amount of an above protein or protein complex is determined and compared to an amount determined in the presence of a medicament that binds to a FLNA pentapeptide and contains at least four of the six pharmacophores of FIGS. 7-12. An amount of protein or protein complex determined in the presence of the medicament less than the first determined amount indicates a favorable treatment prognosis.

New isobutyramides.

Provided in the present application are an aromatic heterocyclic substituted olefin compound, a preparation method for same, a pharmaceutical composition of same, and applications thereof. The aromatic heterocyclic substituted olefin compound of the present invention is a novel ALK5 inhibitor and is for use in treating and/or preventing various ALK5-mediated diseases. ##STR00001##

A method of treating or preventing a fibrotic disease, disorder or condition includes administering to a subject in need of treatment a 15-PGDH inhibitor.