US2011301154A1PendingUtilityA1

Sigma receptors ligands with anti-apoptotic and/or pro-apoptotic properties, over cellular mechanisms, exhibiting prototypical cytoprotective and also anticancer activity

Assignee: VAMVAKIDES ALEXANDREPriority: Feb 26, 2009Filed: Feb 17, 2010Published: Dec 8, 2011
Est. expiryFeb 26, 2029(~2.6 yrs left)· nominal 20-yr term from priority
A61P 35/04A61P 35/00A61P 31/12A61K 31/4453A61K 31/64A61K 31/5415A61K 31/44A61K 31/137A61K 31/445A61K 31/495A61P 29/00A61K 31/343A61K 31/5377A61K 31/4525A61K 31/431A61K 31/341A61K 31/13A61K 31/365
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Claims

Abstract

The present invention involves new and original sigma receptors Ligands: (Mono-or dialkylaminoalkyl)-γ-butyro-lactones, their analogues aminotetrahydroturanes, the (1-adamantyl) benzene alkylamines, the N,N Dialkyl α-[(adamantyl-1)ben-zyloxy-2] alkylamines and the 3-cyclopentyl adamantyl-amines or alkylamines or-alkyl phenylamines, their enantiomers or di-astereoisomers, their pharmaceutically acceptable salts and Quinacrine Me-thylene blue, Astemizole and their relative analogues with pro-apoptotic and/or anti-apoptotic properties over cellular biochemical mechanisms, with prototypical anti-cancer, an-timetastatic and antiviral activities associated with antagonism of the neuropatic pain and, at very low doses, with cytoprotectve and cytoregenerative activity against the cytodegenerative diseases.

Claims

exact text as granted — not AI-modified
1 - 8 . (canceled) 
     
     
         9 . A method of using sigma(σ) receptor ligands, said method comprising the steps of:
 providing a compound comprising a sigma(σ)-receptor ligands and a sigma(σ) ligands generics, said sigma(σ) ligands generics being selected from the group consisting of Quinacrine, analogues of Quinacrine, Methylene blue, analogues of Methylene blue, Astemizole, and analogues of Astemizole; and 
 using said compound for preparation of pharmaceuticals with anticancer, antimetastatic and antiviral activity associated with analgesic properties. 
 
     
     
         10 . The method according to  claim 9 , wherein said sigma(σ)-receptor ligands being selected from the group consisting of (mono- or di-alkylaminoalkyl)-γ-butyrolactones), aminotetrahydrofuranes, enantiomers or diastereoisomers of aminotetrahydrofuranes, (1-adamantyl) benzene alkylamines, enantiomers or diastereoisomers of (1-adamantyl) benzene alkylamines, N,N di-alkyl α-[(adamantyl-1) benzyloxy-2] alkylamines, enantiomers or diastereoisomers of N,N di-alkyl α-[(adamantyl-1) benzyloxy-2] alkylamines, 3-cyclopentyl adamantyl-amines or -alkylamines or -alkyl phenylamines, enantiomers or diastereoisomers of 3-cyclopentyl adamantyl-amines or -alkylamines or -alkyl phenylamines, and their pharmaceutically acceptable salts. 
     
     
         11 . The method according to  claim 10 , wherein said compound further comprising at least one pharmaceutically acceptable excipient. 
     
     
         12 . A method of using sigma(σ) receptor ligands, said method comprising the steps of:
 providing a compound comprising a sigma(σ)-receptor ligands and a sigma(σ) ligands generics, said sigma(σ) ligands generics being selected from the group consisting of Quinacrine, analogues of Quinacrine, Methylene blue, analogues of Methylene blue, Astemizole, and analogues of Astemizole; and 
 using said compound for preparation of pharmaceuticals with analgesic activity against neuropathic pain. 
 
     
     
         13 . The method according to  claim 12 , wherein said sigma(σ)-receptor ligands being selected from the group consisting of (mono- or di-alkylaminoalkyl)-γ-butyrolactones), aminotetrahydrofuranes, enantiomers or diastereoisomers of aminotetrahydrofuranes, (1-adamantyl) benzene alkylamines, enantiomers or diastereoisomers of (1-adamantyl) benzene alkylamines, N,N di-alkyl α-[(adamantyl-1) benzyloxy-2] alkylamines, enantiomers or diastereoisomers of N,N di-alkyl α-[(adamantyl-1) benzyloxy-2] alkylamines, 3-cyclopentyl adamantyl-amines or -alkylamines or -alkyl phenylamines, enantiomers or diastereoisomers of 3-cyclopentyl adamantyl-amines or -alkylamines or -alkyl phenylamines, and their pharmaceutically acceptable salts. 
     
     
         14 . The method according to  claim 13 , wherein said compound further comprising at least one pharmaceutically acceptable excipient. 
     
     
         15 . A method of using sigma(σ) receptor ligands, said method comprising the steps of:
 providing a compound comprising a sigma(σ)-receptor ligands and a sigma(σ) ligands generics, said sigma(σ) ligands generics being selected from the group consisting of Quinacrine, analogues of Quinacrine, Methylene blue, analogues of Methylene blue, Astemizole, and analogues of Astemizole; and 
 using said compound for preparation of pharmaceuticals selected from the group consisting of pharmaceuticals acting synergistically with clinically used anticancer drugs and antagonizing neuropathic pain induced by the anticancer drugs, pharmaceuticals with cytoprotective activity against pathogenesis of cytodegenerative diseases, pharmaceuticals with cytoprotective and cytoregenerative activity, and pharmaceuticals with protective activity against the pathogenesis of inflammatory and neuropathic pain. 
 
     
     
         16 . The method according to  claim 15 , wherein said sigma(σ)-receptor ligands being selected from the group consisting of (mono- or di-alkylaminoalkyl)-γ-butyrolactones), aminotetrahydrofuranes, enantiomers or diastereoisomers of aminotetrahydrofuranes, (1-adamantyl) benzene alkylamines, enantiomers or diastereoisomers of (1-adamantyl) benzene alkylamines, N,N di-alkyl α-[(adamantyl-1) benzyloxy-2] alkylamines, enantiomers or diastereoisomers of N,N di-alkyl α-[(adamantyl-1) benzyloxy-2] alkylamines, 3-cyclopentyl adamantyl-amines or -alkylamines or -alkyl phenylamines, enantiomers or diastereoisomers of 3-cyclopentyl adamantyl-amines or -alkylamines or -alkyl phenylamines, and their pharmaceutically acceptable salts. 
     
     
         17 . The method according to  claim 16 , wherein said compound further comprising at least one pharmaceutically acceptable excipient.

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