摘要:
Compounds and their pharmaceutically acceptable salts, their synthesis and labeling, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, including Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment are provided. Also provided is the use of the disclosed compounds as imaging agents and methods for in vivo imaging and detection of amyloid and synuclein.
摘要:
Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, AA/SAA amyloidosis, such as observed in systemic AA amyloidosis and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.
摘要:
A pharmaceutical composition that includes a peptide of formula Y-(X-aa)-Z. (X-aa) is generally an amino acid sequence selected from -Arg-Val-Ser-Val-Arg-Trp-, -Arg-Val-Ala-Val-Ile-, -His-Gly-Arg-Leu-Val-Phe-, -Leu-Ala-Phe-Val-Leu-Arg-, and -Thr-Leu-Phe-Leu-Ala-Arg-. And Y is generally an amino terminal modifying group selected from an amino acid, a N-acylated amino acid, a peptide, a N-acylated peptide, and hydrogen. And Z- is carboxyl-terminal modifying group selected from hydrogen, an amino acid, a C-amidated amino acid, a peptide, a C-amidated peptide, or an amide or hydroxyl group such as an alkyl amide, an aryl amide, or an alcohol. A composition of matter that includes at least one of the peptide sequences -Arg-Val-Ala-Val-Ile-, -Leu-Ala-Phe-Val-Leu-Arg-, -Thr-Leu-Phe-Leu-Ala-Arg-, -Arg-Val-Ser-Val-Arg-Trp-, -His-Gly-Arg-Leu-Val-Phe-. Preferably at least one amino acid of the peptide sequence is a D-amino acid.
摘要:
A method of induction of amyloid plaques includes immobilizing a quantity of a selected sulfated glycosaminoglycan (SGAG) on a selected medium and adding to the immobilized SGAG on the medium a quantity of dissolved low fibrillar Aβ 1-40 (LFAβ). The LFAβ is added preferably in a Aβ:SGAG w/w ratio of about 1:1. SGAGs are preferably selected from heparin, heparan sulfate, keratan sulfate, dermatan sulfate, chondroitin-4-sulfate and chondroitin-6-sulfate. Screening methods and kits for screening either immobilize a quantity of a selected sulfated glycosaminoglycan (SGAG) on a selected medium, followed by adding to a quantity of dissolved low fibrillar Aβ 1-40 (LFAβ) a selected quantity of the selected amyloid therapeutic candidate to create a test solution, and then adding to the immobilized SGAG on the medium a selected quantity of the test solution to test for inhibition, or preform amyloid plaques on the medium by immobilizing a quantity of a selected sulfated glycosaminoglycan (SGAG) or a GAG-related macromolecule on a selected medium and then adding a selected quantity of dissolved low fibrillar Aβ 1-40 (LFAβ), followed by adding to the amyloid plaques on the medium a selected quantity of a test solution of a selected amyloid therapeutic candidate to test for disruption.
摘要:
The use of 3,4,3′,4′-tetrahydroxychalcone in the treatment of amyloid diseases, especially Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease.
摘要:
Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.
摘要:
Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.
摘要:
Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.