US2008021051A1PendingUtilityA1

Phycotoxins and Uses Thereof

43
Assignee: PHYTOTOX LTDPriority: May 7, 2004Filed: May 6, 2005Published: Jan 24, 2008
Est. expiryMay 7, 2024(expired)· nominal 20-yr term from priority
Inventors:Nestor Antonio Lagos Wilson
A61P 9/14A61P 27/02A61P 25/02A61P 25/04A61P 25/00A61P 25/06A61P 29/00A61P 25/08A61P 13/10A61P 19/02A61P 19/00A61P 21/00A61P 17/00A61P 1/04A61P 23/00A61P 1/00A61P 19/10A61P 15/00A61P 21/02A61P 17/02A61K 31/505Y02A50/30
43
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Claims

Abstract

Pharmaceutical compositions comprising tricyclic 3,4-propinoperhydropurines and uses thereof for blocking neuronal transmission which are useful in treating anal fissure and other wounds and muscle disorders are provided. Also provided are methods of treating wounds and muscle disorders by administering the composition of the invention to a muscle or in the vicinity of a muscle either topically or by injection.

Claims

exact text as granted — not AI-modified
1 . A method of treating a patient afflicted with at least one ailment selected from the group consisting of: blepharospasm, strabismus, focal dystonia, hyperhydrosis, urinary bladder relaxation, muscular spasm-related pain, and muscular spasms, comprising the step of administering to a patient in need of such treatment an effective amount of a composition comprising at least one tricyclic 3,4-propinoperhydropurine represented by formula I set forth below:  
     
       
         
         
             
             
         
       
     
     wherein R 1  and R 5  are independently selected from the group consisting of —H and —OH; R 2  and R 3  are independently selected from the group consisting of —H and —SO 3 ; and R 4  is selected from the group consisting of —H, —OH, —COONH 2 , —COONHSO −   3  and —COOCH 3 , with the proviso that either one of R 2  and R 3  must be —OSO −   3 , or R 4  must be —COONHSO −   3 , and a pharmacologically acceptable carrier.  
   
   
       2 . The method of  claim 1 , wherein the composition is injected into a muscle.  
   
   
       3 . The method of  claim 1 , wherein the at least one compound of the formula I is selected from the group consisting of: GTX-1, GTX-2, GTX-3, GTX-4 and GTX-5.  
   
   
       4 . The method of  claim 3 , wherein the composition comprises GTX-2 and GTX-3.  
   
   
       5 . The method of  claim 3 , wherein the effective amount of said composition contains from about 1 to about 5000 units of activity.  
   
   
       6 . The method of  claim 3 , wherein the effective amount of said composition contains from more than 32 to about 1000 units of activity.  
   
   
       7 . The method of  claim 3 , wherein the effective amount of said composition contains from more than 40 to about 1000 units of activity.  
   
   
       8 . The method of  claim 3 , wherein the effective amount of said composition contains from about 50 to about 500 units of activity.  
   
   
       9 . The method of  claim 3 , wherein the effective amount of said composition contains from about 75 to about 200 units of activity.  
   
   
       10 . The method of  claim 3 , wherein said composition further comprises a neurotoxin selected from the group consisting of saxitoxin, neosaxitoxin, decarbamoylsaxitoxin, tetanus toxin, and Botulin A toxin.  
   
   
       11 . The method of  claim 3 , wherein said composition further comprises a local anesthetic.  
   
   
       12 . The method of  claim 11 , wherein the local anesthetic is selected from the group consisting of: benzocaine, tetracaine, mepivacaine, prilocalne, etidocaine, bupivacaine, lidocaine.  
   
   
       13 . The method of  claim 2 , wherein the composition is injected at multiple injection points.  
   
   
       14 . The method of  claim 13 , wherein the location of the multiple injection points is determined, at least in part, based upon a predetermined treatment plan for the specific ailment being treated.  
   
   
       15 . The method of  claim 1 , wherein the composition is applied topically.  
   
   
       16 . The method of  claim 15 , wherein the topical composition comprises from about 0.0001% to about 0.01% by weight of one or more compounds of the formula I, based on the total weight of the composition.  
   
   
       17 . The method of  claim 1 , wherein the composition is applied transdermally.  
   
   
       18 . A method of treating a patient afflicted with at least one ailment selected from the group consisting of: carpal-tunnel syndrome, fibromyalgia, join flare, joint pain, post-operative pain, arthritis, sciatica, tendonitis, neck pain, back pain, hemifacial spasm, hyperfunctional larynx, juvenile cerebral palsy, spasticity, tension headaches, migraine headaches, writer's cramp, tremors, tics, disorders of the upper and lower esophageal sphincter, gastroparesis, hypertrophic pyloric stenosis, hemorrhoids, proctalgia fugax, irritable bowel syndrome, muscular spasms, vasospastic disorders, disorders involving uterine, or bladder spasm, sphincter of Oddi dysfunction, and short-segment Hirschprung's, and bruxism, comprising the step of administering to a patient in need of such treatment an effective amount of a composition comprising at least one tricyclic 3,4-propinoperhydropurine represented by formula I set forth below:  
     
       
         
         
             
             
         
       
     
     wherein R 1  and R 5  are independently selected from the group consisting of —H and —OH; R 2  and R 3  are independently selected from the group consisting of —H and —SO 3 ; and R 4  is selected from the group consisting of —H, —OH, —COONH 2 , —COONHSO −   3  and —COOCH 3 , with the proviso that either one of R 2  and R 3  must be —OSO −   3 , or R 4  must be —COONHSO −   3 , and a pharmacologically acceptable carrier.  
   
   
       19 . The method of  claim 18 , wherein the composition is injected into a muscle.  
   
   
       20 . The method of  claim 18 , wherein the at least one compound of the formula I is selected from the group consisting of: GTX-1, GTX-2, GTX-3, GTX-4 and GTX-5.  
   
   
       21 . The method of  claim 20 , wherein the composition comprises GTX-2 and GTX-3.  
   
   
       22 . The method of  claim 20 , wherein the effective amount of said composition contains from about 1 to about 5000 units of activity.  
   
   
       23 . The method of  claim 20 , wherein the effective amount of said composition contains from more than 32 to about 1000 units of activity.  
   
   
       24 . The method of  claim 20 , wherein the effective amount of said composition contains from more than 40 to about 1000 units of activity.  
   
   
       25 . The method of  claim 20 , wherein the effective amount of said composition contains from about 50 to about 500 units of activity.  
   
   
       26 . The method of  claim 20 , wherein the effective amount of said composition contains from about 75 to about 200 units of activity.  
   
   
       27 . The method of  claim 20 , wherein said composition further comprises a neurotoxin selected from the group consisting of saxitoxin, neosaxitoxin, decarbamoylsaxitoxin, tetanus toxin, and Botulin A toxin.  
   
   
       28 . The method of  claim 20 , wherein said composition further comprises a local anesthetic.  
   
   
       29 . The method of  claim 28 , wherein the local anesthetic is selected from the group consisting of: benzocaine, tetracaine, mepivacaine, prilocalne, etidocaine, bupivacaine, lidocaine.  
   
   
       30 . The method of  claim 18 , wherein the composition is applied topically.  
   
   
       31 . The method of  claim 20 , wherein the topical composition comprises from about 0.0001% to about 0.01% by weight of one or more compounds of the formula I, based on the total weight of the composition.  
   
   
       32 . The method of  claim 19 , wherein the composition is injected at multiple injection points.  
   
   
       33 . The method of  claim 32 , wherein the location of the multiple injection points is determined, at least in part, based upon a predetermined treatment plan for the specific ailment being treated.  
   
   
       34 . The method of  claim 18 , wherein the composition is applied transdermally.  
   
   
       35 . A method of reducing or eliminating wrinkles comprising the step of administering to a patient in need of such treatment an effective amount of a composition comprising at least one tricyclic 3,4-propinoperhydropurine represented by formula I set forth below:  
     
       
         
         
             
             
         
       
     
     wherein R 1  and R 5  are independently selected from the group consisting of —H and —OH; R 2  and R 3  are independently selected from the group consisting of —H and —SO 3 ; and R 4  is selected from the group consisting of —H, —OH, —COONH 2 , —COONHSO −   3  and —COOCH 3 , with the proviso that either one of R 2  and R 3  must be —OSO −   3 , or R 4  must be —COONHSO −   3 , and a pharmacologically acceptable carrier.  
   
   
       36 . The method of  claim 35 , wherein the composition is injected into a muscle.  
   
   
       37 . The method of  claim 35 , wherein the at least one compound of the formula I is selected from the group consisting of: GTX-1, GTX-2, GTX-3, GTX-4 and GTX-5.  
   
   
       38 . The method of  claim 37 , wherein the composition comprises GTX-2 and GTX-3.  
   
   
       39 . The method of  claim 37 , wherein the effective amount of said composition contains from about 1 to about 5000 units of activity.  
   
   
       40 . The method of  claim 37 , wherein the effective amount of said composition contains from more than 32 to about 1000 units of activity.  
   
   
       41 . The method of  claim 37 , wherein the effective amount of said composition contains from more than 40 to about 1000 units of activity.  
   
   
       42 . The method of  claim 37 , wherein the effective amount of said composition contains from about 50 to about 500 units of activity.  
   
   
       43 . The method of  claim 37 , wherein the effective amount of said composition contains from about 75 to about 200 units of activity.  
   
   
       44 . The method of  claim 37 , wherein said composition further comprises a neurotoxin selected from the group consisting of saxitoxin, neosaxitoxin, decarbamoylsaxitoxin, tetanus toxin, and Botulin A toxin.  
   
   
       45 . The method of  claim 37 , wherein said composition further comprises a local anesthetic.  
   
   
       46 . The method of  claim 45 , wherein the local anesthetic is selected from the group consisting of: benzocaine, tetracaine, mepivacaine, prilocalne, etidocaine, bupivacaine, lidocaine.  
   
   
       47 . The method of  claim 35 , wherein the composition is applied topically.  
   
   
       48 . The method of  claim 37 , wherein the topical composition comprises from about 0.0001% to about 0.01% by weight of one or more compounds of the formula I, based on the total weight of the composition.  
   
   
       49 . The method of  claim 36 , wherein the composition is injected at multiple injection points.  
   
   
       50 . The method of  claim 49 , wherein the location of the multiple injection points is determined, at least in part, based upon a predetermined treatment plan for the specific ailment being treated.  
   
   
       51 . The method of  claim 35 , wherein the composition is applied transdermally.

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