US2008027030A1PendingUtilityA1

Pharmaceutical compositions comprising amifostine and related compounds

63
Assignee: STOGNIEW MARTINPriority: Apr 27, 1998Filed: Feb 8, 2006Published: Jan 31, 2008
Est. expiryApr 27, 2018(expired)· nominal 20-yr term from priority
Inventors:Martin StogniewJean Bourthis
A61K 31/135A61P 17/00A61K 31/19A61K 31/13A61K 31/215A61K 31/54A61P 1/04A61K 31/56A61K 31/66A61K 31/522A61K 31/04A61P 1/00A61K 31/495
63
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Claims

Abstract

The present invention is directed to pharmaceutical compositions comprising amifostine or a related compound and a compound which may be selected from the group consisting of an anesthetic, a corticosteroid, an antihistamine and an anti-inflammatory. The present invention is also directed to methods of treating or protecting tissue of a human from damage associated with radiation and/or chemotherapeutic treatment of cancers by the application of the pharmaceutical compositions.

Claims

exact text as granted — not AI-modified
1 . A pharmaceutical composition comprising: 
 (a) a therapeutically effective amount of at least one compound of formula (I):      R 1 NH(CH 2 ) n NH(CH 2 ) m SR 2   (I)    wherein R 1  is hydrogen, C 5 -C 7  aryl, C 2 -C 7  acyl, or C 1 -C 7  alkyl;    R 2  is hydrogen, PO 3 H 2  or R 3 , wherein R 3  is R 1 NH(CH 2 ) n NH(CH 2 ) m S—; and    n and m are each independently an integer from 1 to 10, or a pharmaceutically acceptable salt, solvate or hydrate thereof; and    (b) a second compound selected from the group consisting of an anesthetic, a corticosteroid, an antihistamine and an anti-inflammatory.    
   
   
       2 . The pharmaceutical composition of  claim 1 , wherein the second compound comprises an anesthetic.  
   
   
       3 . The pharmaceutical composition of  claim 2 , wherein the anesthetic comprises pramoxine, lidocaine, procaine, mepivacaine or a combination thereof.  
   
   
       4 . The pharmaceutical composition of  claim 1 , wherein the second compound comprises a corticosteroid.  
   
   
       5 . The pharmaceutical composition of  claim 4 , wherein the corticosteroid comprises hydrocortisone, hydrocortisone 21-acetate, hydrocortisone 17-valerate, hydrocortisone 17-butyrate, betamethasone valerate, betamethasone diproprionate, triamcinolone acetonide, fluocinonide, clobetasol proprionate or a combination thereof.  
   
   
       6 . The pharmaceutical composition of  claim 1 , wherein the second compound comprises an antihistamine agent.  
   
   
       7 . The pharmaceutical composition of  claim 6 , wherein the antihistamine agent comprises hydroxyzine, diphenhydramine, propranolol, promethazine, vitamin A palmitate or a combination thereof.  
   
   
       8 . The pharmaceutical composition of  claim 1 , wherein the second compound comprises an anti-inflammatory agent.  
   
   
       9 . The pharmaceutical composition of  claim 8 , wherein the anti-inflammatory agent comprises naproxen, ibuprofen, theophylline, cromolyn, albuterol, retinoic acid, 13-cis retinoic acid or a combination thereof.  
   
   
       10 . The pharmaceutical composition of  claim 1  further comprising a pharmaceutically acceptable excipient, carrier or diluent.  
   
   
       11 . The pharmaceutical composition of  claim 1 , wherein R 1  is hydrogen or methyl; R 2  is hydrogen or PO 3 H 2 ; m is 2 or 3; and n is 3.  
   
   
       12 . The pharmaceutical composition of  claim 1 , wherein the compound is amifostine, WR-1065, WR-151326, WR-151327, or WR-33278, or a pharmaceutically acceptable salt, solvate or hydrate thereof.  
   
   
       13 . The pharmaceutical composition of  claim 12 , wherein the compound of formula (I) is amifostine, or a pharmaceutically acceptable salt, solvate or hydrate thereof.  
   
   
       14 . The pharmaceutical composition of  claim 1 , wherein the pharmaceutical composition is a cream, lotion, ointment, gel, solution, or suspension.  
   
   
       15 . The pharmaceutical composition of  claim 14 , wherein the pharmaceutical composition is a solution.  
   
   
       16 . The pharmaceutical composition of  claim 15 , wherein the solution further comprises a diluent.  
   
   
       17 . The pharmaceutical composition of  claim 16 , wherein the diluent is water, acetone, ethanol, ethylene glycol, propylene glycol, butane-1,3-diol, isopropyl myristate, isopropyl palmitate, mineral oil or a combination thereof.  
   
   
       18 . The pharmaceutical composition of  claim 17 , wherein the diluent is water.  
   
   
       19 . The pharmaceutical composition of  claim 18 , wherein the water diluent further comprises sodium chloride, potassium chloride, calcium chloride or a combination thereof.  
   
   
       20 . The pharmaceutical composition of  claim 1 , wherein the therapeutically effective amount of the compound of formula (I) is 10-600 mg.  
   
   
       21 . A method of protecting tissue of a human from damage caused by radiation and/or chemotherapeutic treatment, which comprises administering: 
 (a) a therapeutically effective amount of at least one compound of formula (I):      R 1 NH(CH 2 ) n NH(CH 2 ) m SR 2   (I)    wherein R 1  is hydrogen, C 5 -C 7  aryl, C 2 -C 7  acyl, or C 1 -C 7  alkyl;    R 2  is hydrogen, PO 3 H 2  or R 3 , wherein R 3  is R 1 NH(CH 2 ) n NH(CH 2 ) m S—; and    n and m are each independently an integer from 1 to 10, or a pharmaceutically acceptable salt, solvate or hydrate thereof; and    (b) a second compound selected from the group consisting of an anesthetic, a corticosteroid, an antihistamine and an anti-inflammatory.    
   
   
       22 . The method of  claim 21 , wherein the tissue is mucosal, skin or hair tissue.  
   
   
       23 . The method of  claim 21 , wherein the method is for protecting tissue of a human from mucositis caused by radiation and/or chemotherapeutic treatment.  
   
   
       24 . The method of  claim 23 , wherein the method is for protecting tissue of a human from xerostomia caused by radiation and/or chemotherapeutic treatment.  
   
   
       25 . The method of  claim 21 , wherein the compound of formula (I) and the second compound are administered in a single pharmaceutical composition.  
   
   
       26 . The method of  claim 25 , wherein the single pharmaceutical composition is a solution.  
   
   
       27 . The method of  claim 26 , wherein the single pharmaceutical composition is administered by injection.  
   
   
       28 . The method of  claim 21 , wherein the compound of formula (I) and the second compound are administered in separate pharmaceutical compositions.  
   
   
       29 . The method of  claim 21 , wherein the compound of formula (I) and the second compound are administered simultaneously.  
   
   
       30 . The method of  claim 21 , wherein the compound of formula (I) and the second compound are administered separately.  
   
   
       31 . The method of  claim 21 , wherein the therapeutically effective amount of the compound of formula (I) is 10-600 mg.  
   
   
       32 . The method of  claim 31 , wherein the therapeutically effective amount of the compound of formula (I) is 100-300 mg.  
   
   
       33 . The method of  claim 21 , wherein the compound of formula (I) comprises amifostine.  
   
   
       34 . The method of  claim 21 , wherein the second compound comprises an anesthetic.  
   
   
       35 . The method of  claim 34 , wherein the anesthetic comprises pramoxine, lidocaine, procaine, mepivacaine or a combination thereof.  
   
   
       36 . The method of  claim 21 , wherein the second compound comprises a corticosteroid.  
   
   
       37 . The method of  claim 36 , wherein the corticosteroid comprises hydrocortisone, hydrocortisone 21-acetate, hydrocortisone 17-valerate, hydrocortisone 17-butyrate, betamethasone valerate, betamethasone diproprionate, triamcinolone acetonide, fluocinonide, clobetasol proprionate or a combination thereof.  
   
   
       38 . The method of  claim 21 , wherein the second compound comprises an antihistamine agent.  
   
   
       39 . The method of  claim 38 , wherein the antihistamine agent comprises hydroxyzine, diphenhydramine, propranolol, promethazine, vitamin A palmitate or a combination thereof.  
   
   
       40 . The method of  claim 21 , wherein the second compound comprises an anti-inflammatory agent.  
   
   
       41 . The method of  claim 40 , wherein the anti-inflammatory agent comprises naproxen, ibuprofen, theophylline, cromolyn, albuterol, retinoic acid, 13-cis retinoic acid or a combination thereof.  
   
   
       42 . A method of treating damaged tissue of a human caused by radiation and/or chemotherapeutic treatment, which comprises administering: 
 (a) a therapeutically effective amount of at least one compound of formula (I):      R 1 NH(CH 2 ) n NH(CH 2 ) m SR 2   (I)    wherein R 1  is hydrogen, C 5 -C 7  aryl, C 2 -C 7  acyl, or C 1 -C 7  alkyl;    R 2  is hydrogen, PO 3 H 2  or R 3 , wherein R 3  is R 1 NH(CH 2 ) n NH(CH 2 ) m S—; and    n and m are each independently an integer from 1 to 10, or a pharmaceutically acceptable salt, solvate or hydrate thereof; and    (b) a second compound selected from the group consisting of an anesthetic, a corticosteroid, an antihistamine and an anti-inflammatory.    
   
   
       43 . The method of  claim 42 , wherein the tissue is mucosal, skin or hair tissue.  
   
   
       44 . The method of  claim 42 , wherein the method is for treating mucositis.  
   
   
       45 . The method of  claim 42 , wherein the method is for treating xerostomia.  
   
   
       46 . The method of  claim 42 , wherein the compound of formula (I) and the second compound are administered in a single pharmaceutical composition.  
   
   
       47 . The method of  claim 46 , wherein the single pharmaceutical composition is a solution.  
   
   
       48 . The method of  claim 47 , wherein the single pharmaceutical composition is administered by injection.  
   
   
       49 . The method of  claim 42 , wherein the compound of formula (I) and the second compound are administered in separate pharmaceutical compositions.  
   
   
       50 . The method of  claim 42 , wherein the compound of formula (I) and the second compound are administered simultaneously.  
   
   
       51 . The method of  claim 42 , wherein the compound of formula (I) and the second compound are administered separately.  
   
   
       52 . The method of  claim 42 , wherein the therapeutically effective amount of the compound of formula (I) is 10-600 mg.  
   
   
       53 . The method of  claim 52 , wherein the therapeutically effective amount of the compound of formula (I) is 100-300 mg.  
   
   
       54 . The method of  claim 42 , wherein the compound of formula (I) comprises amifostine.  
   
   
       55 . The method of  claim 42 , wherein the second compound comprises an anesthetic.  
   
   
       56 . The method of  claim 55 , wherein the anesthetic comprises pramoxine, lidocaine, procaine, mepivacaine or a combination thereof.  
   
   
       57 . The method of  claim 42 , wherein the second compound comprises a corticosteroid.  
   
   
       58 . The method of  claim 57 , wherein the corticosteroid comprises hydrocortisone, hydrocortisone 21-acetate, hydrocortisone 17-valerate, hydrocortisone 17-butyrate, betamethasone valerate, betamethasone diproprionate, triamcinolone acetonide, fluocinonide, clobetasol proprionate or a combination thereof.  
   
   
       59 . The method of  claim 42 , wherein the second compound comprises an antihistamine agent.  
   
   
       60 . The method of  claim 59 , wherein the antihistamine agent comprises hydroxyzine, diphenhydramine, propranolol, promethazine, vitamin A palmitate or a combination thereof.  
   
   
       61 . The method of  claim 42 , wherein the second compound comprises an anti-inflammatory agent.  
   
   
       62 . The method of  claim 61 , wherein the anti-inflammatory agent comprises naproxen, ibuprofen, theophylline, cromolyn, albuterol, retinoic acid, 13-cis retinoic acid or a combination thereof.

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