Patent · US Active

2-arylbenzothiophene derivatives or pharmaceutically acceptable salts thereof, preparation method thereof, and pharmaceutical composition for the diagnosis or treatment of degenerative brain disease containing the same as active ingredient

US8497260B2 · kind B2 · utility

1Cited by
5References
11Claims
0Family size

Assignee

Inventors

Key dates

Filing dateOct 15, 2009
Grant dateJul 30, 2013
Priority date
Expiry dateJan 10, 2031

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D409/04
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

Abstract

2-arylbenzothiophene derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition for the diagnosis or treatment of degenerative brain disease containing the same as an active ingredient. Since the 2-arylbenzothiophene derivatives of Formula 1 have a relatively high binding affinity for β-amyloid, they can be used as diagnostic reagents for diagnosing Alzheimer's disease at an early stage by non-invasive techniques when they are labeled with radioisotopes:wherein R1-R4, V, W, X, Y and Z are as defined in the Detailed Descript of the specification. Further, when the pharmaceutical composition containing the 2-arylbenzothiophene derivative binds with a low-molecular weight β-amyloid peptide binding compound, generation of malignant high-molecular weight β-amyloid deposits is minimized. Accordingly, the pharmaceutical composition can be used as a therapeutic agent of degenerative brain disease such as Alzheimer's disease.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.