I sent an email to IR and Anavex last week asking for clarity on the scope of the below patent. It mentions melanoma in the claims, but not within the body of the patent. The body of the patent addresses more of the MoA regarding Sigma receptors and cell stress, etc. So was hoping it covered a broader scope.
IR did respond that they had forwarded my email to the company for a response.
United States Patent 9,180,106
Vamvakides November 10, 2015
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Sigma receptors ligands with anti-apoptotic and/or pro-apoptotic properties, over cellular mechanisms, exhibiting prototypical cytoprotective and also anti-cancer activity
Abstract
The present invention involves new and original sigma receptors ligands: (Mono- or dialkylaminoalkyl)-.gamma.-butyrolactones, their analogues aminotetrahydroturanes, the (1-adamantyl)benzene alkylamines, the N,N Dialkyl .alpha.-[(adamantyl-1)benzyloxy-2]alkylamines and the 3-cyclopentyl adamantyl-amines or alkylamines or -alkyl phenylamines, their enantiomers or diastereoisomers, their pharmaceutically acceptable salts and Quinacrine Me-thylene blue, Asteinizole and their relative analogues with pro-apoptotic and/or anti-apoptotic properties over cellular biochemical mechanisms, with prototypical anti-cancer, antimetastatic and antiviral activities associated with antagonism of the neuropatic pain and, at very low doses, with cytoprotective and cytoregenerative activity against the cytodegenerative diseases.
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Inventors: Vamvakides; Alexandre (Ymittos Attiki, GR)
Applicant: Name City State Country Type
Anavex Life Sciences Corp.
New York
NY
US
Assignee: Anavex Life Sciences Corp. (New York, NY)
Family ID: 42083964
Appl. No.: 14/205,637
Filed: March 12, 2014
The invention claimed is:
1. A method of treating melanoma in a subject comprising administering in a subject in need thereof a therapeutic amount of a first compound shown here ##STR00001## and a therapeutic amount of a second compound selected from the group consisting of quinacrine, methylene blue, or astemizole.
2. The method of claim 1 wherein the second compound is quinicrine.
3. The method of claim 1 wherein the second compound is methylene blue.
4. The method of claim 1 wherein the second compound is astemazole.
5. A method of treating melanoma in a subject comprising administering in a subject in need thereof a therapeutic amount of a first compound shown here ##STR00002## and a therapeutic amount of a second compound selected from the group consisting of quinacrine, methylene blue, or astemizole.
6. The method of claim 5 wherein the second compound is quinicrine.
7. The method of claim 5 wherein the second compound is methylene blue.
8. The method of claim 5 wherein the second compound is astemazole.
9. A method of treating melanoma in a subject comprising administering in a subject in need thereof a therapeutic amount of a first compound shown here ##STR00003## and a therapeutic amount of a second compound selected from the group consisting of quinacrine, methylene blue, or astemizole.
10. The method of claim 9 wherein the second compound is quinicrine.
11. The method of claim 9 wherein the second compound is methylene blue.
12. The method of claim 9 wherein the second compound is astemazole.
13. A method of treating melanoma in a subject comprising administering in a subject in need thereof a therapeutic amount of a first compound shown here ##STR00004## and a therapeutic amount of a second compound selected from the group consisting of quinacrine, methylene blue, or astemizole.
14. The method of claim 13 wherein the second compound is quinicrine.
15. The method of claim 13 wherein the second compound is methylene blue.
16. The method of claim 13 wherein the second compound is astemazole.
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Description
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BACKGROUND OF THE INVENTION
Field of the Invention
The present invention relates to sigma(a) receptors ligands with anti-apoptotic and/or pro-apoptotic properties for use in connection with exhibiting prototypical cytoprotective properties associated with cytoregenerative activity developed by antagonism of the endoplasmic reticulum stress (ER stress) via activation of the sigma receptors in the connecting membrane between ER and mitochondrion.
SUMMARY OF THE INVENTION
In view of the foregoing disadvantages inherent in the prior art, the present invention provides an improved sigma(a) receptor ligands and method for using, and overcomes the above-mentioned disadvantages and drawbacks of the prior art. As such, the general purpose of the present invention, which will be described subsequently in greater detail, is to provide a new and improved sigma(a) receptor ligands and method which has all the advantages of the prior art mentioned heretofore and many novel features that result in a sigma(a) receptor ligands which is not anticipated, rendered obvious, suggested, or even implied by the prior art, either alone or in any combination thereof.
To attain this, the present invention essentially comprises a method for using a compound including sigma(a)-receptor ligands and a sigma(a) ligands generics. The method includes the providing of a compound having a sigma(a)-receptor ligands and a sigma(a) ligands generics, wherein the sigma(a) ligands generics is selected from Quinacrine, analogues of Quinacrine, Methylene blue, analogues of Methylene blue, Astemizole, and analogues of Astemizole. Then method further includes using the composition for the preparation of pharmaceuticals.
The pharmaceuticals have anticancer, antimetastatic and antiviral activity associated with analgesic properties.
The sigma(a)-receptor ligands may also be selected from (mono- or dialkylaminoalkyl)-y-butyrolactones), aminotetrahydrofuranes, enantiomers or diastereoisomers of aminotetrahydrofuranes, (1-adamantyl)benzene alkylamines, enantiomers or diastereoisomers of (1-adamantyl)benzene alkylamines, N,N di-alkyl a[(adamantyl-1)benzyloxy-2]alkylamines, enantiomers or diastereoisomers of N,N dialkyl a-[(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.
There has thus been outlined, rather broadly, the more important features of the invention in order that the detailed description thereof that follows may be better understood and in order that the present contribution to the art may be better appreciated.
The invention may also include the preparation of pharmaceuticals having analgesic activity against neuropathic pain, 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. There are, of course, additional features of the invention that will be described hereinafter and which will form the subject matter of the claims attached.
Numerous objects, features and advantages of the present invention will be readily apparent to those of ordinary skill in the art upon a reading of the following detailed description of present, but nonetheless illustrative, embodiments of the present invention. In this respect, before explaining the current embodiment of the invention in detail, it is to be understood that the invention is not limited in its application to the details of construction and to the arrangements of the components set forth in the following description or illustrated in the drawings. The invention is capable of other embodiments and of being practiced and carried out in various ways. Also, it is to be understood that the phraseology and terminology employed herein are for the purpose of descriptions and should not be regarded as limiting.
As such, those skilled in the art will appreciate that the conception, upon which this disclosure is based, may readily be utilized as a basis for the designing of other structures, methods and systems for carrying out the several purposes of the present invention. It is important, therefore, that the claims be regarded as including such equivalent constructions insofar as they do not depart from the spirit and scope of the present invention.
AI
