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EP0659418A1 Expired / Lapsed EP ⏱️ 0.0 years remaining

2-Phenyl-3-azoylbenzothiophene for treating Alzheimer's disease

Assignee: Eli Lilly and Co
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Filing: 1994-12-19
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Granted: —
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Expires: 2014-12-19
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Abstract

Abstract This invention encompasses methods for the inhibition of Alzheimer's Disease comprising administering to a human in need thereof an effective amount of a compound of Formula I wherein R¹ and R³ are independently hydrogen, -CH₃, wherein Ar is optionally substituted phenyl; R² is selected from the group consisting of pyrrolidine, hexamethylenemino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof. The present invention also provides methods of increasing TGF-β expression in the brain, comprising administering to a human in need thereof an effective amount of a compound of formula 1. The present invention also provides methods of inhibiting the β-amyloid peptide mediated neurotoxicity or inflammatory response associated with Alzheimer's Disease (AD) comprising administering to a human in need thereof an effective amount of a compound of formula 1.

Inventors

  • 👤 Patrick Cornelious May

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-23 05:40
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/38; A61K31/395; A61K31/40; A61K31/4025; A61K31/435; A61K31/44; A61K31/445; A61K31/4523; A61K31/4535; A61P; A61P25/00; A61P25/28; A61P39/00; A61P43/00; A61P5/00; A61P5/24; A61P5/32; A61K31/55; C; C07; C07D; C07D409/00; C07D409/02; C07D409/10

Claims Analysis

Total Claims: 8
Claim 1
Independent Claim 54 words
The use of a compound having the formula wherein R¹ and R³ are independently hydrogen, -CH₃, wherein Ar is optionally substituted phenyl; R² is selected from the group consisting of pyrrolidino and piperidino; or a pharmaceutically acceptable salt or solvate thereof, in the preparation of a medicament useful for the inhibition of Alzheimer's disease.
Claim 2
Dependent Claim 13 words
The use of Claim 1 wherein said compound is or its hydrochloride salt.
Claim 3
Dependent Claim 54 words
The use of a compound having the formula wherein R¹ and R³ are independently hydrogen, -CH₃, wherein Ar is optionally substituted phenyl; R² is selected from the group consisting of pyrrolidino and piperidino; or a pharmaceutically acceptable salt or solvate thereof, in the preparation of a medicament useful for increasing TGF-β expression the brain.
Claim 4
Dependent Claim 13 words
The use of Claim 3 wherein said compound is or its hydrochloride salt.
Claim 5
Dependent Claim 57 words
The use of a compound having the formula wherein R¹ and R³ are independently hydrogen, -CH₃, wherein Ar is optionally substituted phenyl; R² is selected from the group consisting of pyrrolidino and piperidino; or a pharmaceutically acceptable salt or solvate thereof, in the preparation of a medicament useful for inhibiting the inflammatory response associated with Alzheimer's Disease.
Claim 6
Dependent Claim 13 words
The use of Claim 5 wherein said compound is or its hydrochloride salt.
Claim 7
Dependent Claim 54 words
The use of a compound having the formula wherein R¹ and R³ are independently hydrogen, -CH₃, wherein Ar is optionally substituted phenyl; R² is selected from the group consisting of pyrrolidino and piperidino; or a pharmaceutically acceptable salt or solvate thereof, in the preparation of a medicament useful for inhibiting β-amyloid peptide mediated neurotoxicity.
Claim 8
Dependent Claim 13 words
The use of Claim 7 wherein said compound is or its hydrochloride salt.

References Cited (Backward Citations)

US4418068A Cited
DE4311870A1 Cited
EP0629697A2 Cited

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