US2002187990A1PendingUtilityA1

Compositions and methods for the treatment of anorectal disorders

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Assignee: CELLEGY PHARMA INCPriority: Dec 14, 1998Filed: Jul 17, 2002Published: Dec 12, 2002
Est. expiryDec 14, 2018(expired)· nominal 20-yr term from priority
Inventors:Thomas P. ParksVivien MakJung-Chung LeeCharles Lee
A61K 9/0031A61K 31/21A61K 31/513A61K 31/52A61K 31/505A61K 31/522A61K 31/198A61K 31/519
57
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Claims

Abstract

Compositions and methods for the treatment of anorectal disorders are provided in which certain combinations of NO donors, PDE inhibitors, superoxide (O 2 − ) scavengers, β-adrenergic agonists, cAMP-dependent protein kinase activators, α 1 -adrenergic antagonists, L-type Ca 2+ channel blockers, estrogens, ATP-sensitive K + channel activators and smooth muscle relaxants are used.

Claims

exact text as granted — not AI-modified
What is claimed is:  
     
         1 . A composition for the treatment of an anorectal disorder, and for controlling the pain associated therewith, said composition comprising at least one internal anal sphincter relaxing agent selected from the group consisting of NO donors, phosphodiesterase type II inhibitors, phosphodiesterase type IV inhibitors, phosphodiesterase type V inhibitors, nonspecific phosphodiesterase inhibitors, superoxide scavengers, β-adrenergic agonists, cAMP-dependent protein kinase activators, α 1 -cadrenergic antagonists, estrogens, ATP-sensitive K +  channel activators, adenosine receptor antagonists, and smooth muscle relaxants, with a pharmaceutically acceptable carrier.  
     
     
         2 . A composition in accordance with  claim 1 , wherein said composition comprises a first agent which is a NO donor selected from the group consisting of nitroglycerin, L-arginine, SNAP, GSNO and SIN-1, and a second agent that is an adrenergic receptor antagonist.  
     
     
         3 . A composition in accordance with  claim 1 , wherein said carrier is formulated for local application.  
     
     
         4 . A composition according to  claim 1 , wherein said composition comprises a first relaxing agent that is a NO donor selected from the group consisting of nitroglycerin, L-arginine, SNAP, GSNO and SIN-1 and a second agent that is a β 2 -adrenergic agonist.  
     
     
         5 . A composition according to  claim 4 , wherein said β 2 -adrenergic agonist is salbutamol or terbutaline.  
     
     
         6 . A composition in accordance with  claim 1 , wherein said composition comprises a first relaxing agent which is a NO donor selected from the group consisting of nitroglycerin, L-arginine, SNAP, GSNO and SIN-1 and a second agent that is an ATP sensitive K +  channel activator.  
     
     
         7 . A composition in accordance with  claim 6 , wherein said second agent is minoxidil or diazoxide.  
     
     
         8 . A composition in accordance with  claim 1 , wherein said composition comprises a first relaxing agent which is a NO donor selected from the group consisting of nitroglycerin, L-arginine, SNAP, GSNO and SIN-1 and a second agent that is an adenosine receptor antagonist.  
     
     
         9 . A composition in accordance with  claim 8 , wherein said second agent is theophylline or dyphylline.  
     
     
         10 . A composition according to  claim 1 , comprising an adenosine receptor antagonist.  
     
     
         11 . A composition according to  claim 10 , wherein said antagonist is theophylline or dyphylline.  
     
     
         12 . A composition according to  claim 1 , comprising a ATP sensitive K +  channel opener.  
     
     
         13 . A composition according to  claim 12 , wherein said opener is minoxidil or diazoxide.  
     
     
         14 . A composition according to  claim 1 , wherein said composition comprises a β 2 -adrenergic agonist.  
     
     
         15 . A composition according to  claim 14 , wherein said β 2 -adrenergic agonist is salbutamol or terbutaline.  
     
     
         16 . A method of treating an anorectal disorder, and for controlling the pain associated therewith, the method comprising administering to a subject in need of such treatment a therapeutically effective amount of a composition that comprises at least one internal anal sphincter relaxing agent selected from the group consisting of NO donors, phosphodiesterase type II inhibitors, phosphodiesterase type IV inhibitors, phosphodiesterase type V inhibitors, nonspecific phosphodiesterase inhibitors, superoxide scavengers, β-adrenergic agonists, cAMP-dependent protein kinase activators, α 1 -adrenergic antagonists, estrogens, L-type Ca 2+  channel blockers, ATP-sensitive K +  channel activators, adenosine receptor antagonists and smooth muscle relaxants.  
     
     
         17 . A method in accordance with  claim 16 , wherein said composition comprises a first agent which is a NO donor selected from the group consisting of nitroglycerin, L-arginine, SNAP, GSNO and SIN-1, and a second agent that is an adrenergic receptor antagonist.  
     
     
         18 . A method in accordance with  claim 16 , wherein said administering is by local application.  
     
     
         19 . A method according to  claim 16 , wherein said composition comprises a first relaxing agent that is a NO donor selected from the group consisting of nitroglycerin, L-arginine, SNAP, GSNO and SIN-1 and a second agent that is a β 2 -adrenergic agonist.  
     
     
         20 . A method according to  claim 19 , wherein said β 2 -adrenergic agonist is salbutamol or terbutaline.  
     
     
         21 . A method in accordance with  claim 16 , wherein said composition comprises a first relaxing agent which is a NO donor selected from the group consisting of nitroglycerin, L-arginine, SNAP, GSNO and SIN-1 and a second agent that is an ATP sensitive K +  channel activator.  
     
     
         22 . A method in accordance with  claim 21 , wherein said second agent is minoxidil or diazoxide.  
     
     
         23 . A method in accordance with  claim 16 , wherein said composition comprises a first relaxing agent which is a NO donor selected from the group consisting of nitroglycerin, L-arginine, SNAP, GSNO and SIN-1 and a second agent that is an adenosine receptor antagonist.  
     
     
         24 . A method in accordance with  claim 23 , wherein said second agent is theophylline or dyphylline.  
     
     
         25 . A method according to  claim 16 , wherein said composition comprises an adenosine receptor antagonist.  
     
     
         26 . A method according to  claim 25 , wherein said antagonist is theophylline or dyphylline.  
     
     
         27 . A method according to  claim 16 , wherein said composition comprises a ATP sensitive K +  channel opener.  
     
     
         28 . A method according to  claim 28 , wherein said activator is minoxidil or diazoxide.  
     
     
         29 . A method according to  claim 16 , wherein said composition comprises a β 2 -adrenergic agonist.  
     
     
         30 . A method according to  claim 29 , wherein said β 2 -adrenergic agonist is salbutamol or terbutaline.  
     
     
         31 . A method in accordance with  claim 16 , wherein said anorectal disorder is an anal fissure.  
     
     
         32 . A method of  claim 16 , wherein said composition comprises a terbutaline or salbutamol.  
     
     
         33 . A method of  claim 16 , wherein said composition comprises theophylline or diphylline.  
     
     
         34 . A method of  claim 16 , wherein said composition comprises minoxidil or diazoxide.

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