Compositions and methods for reducing amyloid beta formation on and composition therefore

A composition and compound technology, which is applied in the direction of drug combination, active ingredient of heterocyclic compound, pharmaceutical formulation, etc., can solve problems such as the inability to successfully develop therapeutic agents for dementia

Pending Publication Date: 2022-01-07
ARIBIO CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Accept that this traditional approach does not allow for the successful development of therapeutics for dementia

Method used

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  • Compositions and methods for reducing amyloid beta formation on and composition therefore
  • Compositions and methods for reducing amyloid beta formation on and composition therefore
  • Compositions and methods for reducing amyloid beta formation on and composition therefore

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0103] Embodiment 1. The selectivity test (IC of the composition of the present invention to PDE5) 50 , inhibitory concentration 50)

Embodiment 1-1

[0104] Embodiment 1-1. is used for the test method of PDE5 selectivity

[0105] In order to test the selective inhibitory activity (IC of the composition of the present invention) to PDE5 (phosphodiesterase 5) 50 , inhibitory concentration 50), the test was performed by MDS Pharma Services, analysis agency CRO (analysis agency CRO) and ScottishBiomedical. Results were measured using the PDE SPA assay kit (Amersham Pharmacia Biotech). MDS Pharma Services analyzed PDE1 (bovine heart); PDE 2, 3, 5 (human platelets); PDE4 (human U937 cells); and PDE6 (bovine rod cells) and Scottish Biomedical analyzed PDE 5, 7-11 (recombinant human enzyme). Add test samples (100 μL each) to PDE family proteins (10 μl), [ 3 H]-cGMP (5Ci / mL), bovine serum albumin (0.5mg / mL) and MgCl 2 (5mM) in a mixture in Tris-HCl buffer (15mM, pH 7.5). The reaction begins with the addition of PDE family proteins. Each sample was stored in a 30° C. water bath for 30 minutes, and then SPA beads (PerkinElmer) (...

Embodiment 1-2

[0106] Example 1-2. Results of PDE5 selectivity tests for compositions of the present invention

[0107] Based on the inhibitory activity of the composition of the present invention on 11 PDE families (MDS Pharma Services and Scotish Biomedical), the IC of the composition of the present invention on PDE5 50 was 0.338 nM (MDS Pharma Services) and was 30-376,471 times selective over the remaining 10 PDE family proteins (Table 1).

[0108] Table 1. Selectivity results for PDE families of the invention

[0109]

[0110] a MDS Pharma Services; PDE1 (bovine heart); PDE 2, 3, 5 (human platelets); PDE4 (human U937 cells); PDE6 (bovine rod cells).

[0111] b Scottish Biomedical; PDE 5, 7-11 (recombinant human enzyme); NI = no inhibition observed.

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Abstract

The present invention provides methods for reducing amyloid beta formation and for treating diseases associated with the accumulation of amyloid beta., The present invention provides (1) A[beta]aggregation inhibition by A[beta] Oligomer / Fibril formation inhibition, (2) BACE-1 reduced a through beta- Amyloidogenic Processing inhibition, (3) cerebral blood flow to the increase of the cell outer A[beta] Monomer, Oligomer & A[beta] Fibril / Plaque reduction, (4) NO / cGMP / PKG / CREB Pathway to the activation of Neuronal cell Death inhibition and Neurogenesis, Synaptogenesis, Angiogenesis promotion, (5) DKK-1 inhibition by Wnt Signaling in the activation of synaptic plasticity recovery and A[beta] production Positive Feedback Loop for inhibition of APP generates reduced and A[beta] accumulation suppression, (6) Autophagy activation by cells within Toxic Mirodenafil, Sildenafil, Vardenafil, Tadalafil, Udenafil, Dasantafil, and Avanafil for the treatment of inhibition of A[beta] Fibril / Plaque formation through removal of Soluble A[beta] Oligomer; and a Pharmaceutically Acceptable Salt, Solvate, and Hydrate in selected compounds key of ingredient containing drug compound composition, and this with the treatment method provided.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of priority to U.S. Provisional Application Serial No. 62 / 822,975, filed March 24, 2019, the contents of which are incorporated herein by reference. technical field [0003] The present invention relates to methods for reducing beta amyloid formation and for treating diseases associated with the accumulation of beta amyloid. Background technique [0004] Dementia refers to a clinical disease with multiple cognitive impairments (or MCD, multiple cognitive deficits), which is an acquired brain disease exhibiting a multifaceted pathogenesis caused by multiple genetic and environmental risk factors. A representative of dementia-causing diseases is Alzheimer's disease, which is prevalent mainly in the elderly and accounts for 60-70% of all dementias (Ann Neurol. 1993 May; 33(5):494-501.). With the recent rapid aging of the population, a more progressive form of dementia in the elderly ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/53A61K31/519A61K31/506A61K31/4985A61K31/522A61P25/28
CPCA61K31/53A61K31/519A61K31/506A61K31/4985A61K31/522A61P25/28A61K2300/00
Inventor 郑在晙崔润杓姜秉宇弗雷德·金郑媄先
Owner ARIBIO CO LTD
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