US2023321041A1PendingUtilityA1

Blend containing carbamate compound for prevention, mitigation, or treatment of schizophrenia

Assignee: SK BIOPHARMACEUTICALS CO LTDPriority: Nov 14, 2017Filed: Jun 15, 2023Published: Oct 12, 2023
Est. expiryNov 14, 2037(~11.3 yrs left)· nominal 20-yr term from priority
A61K 31/554A61K 31/519A61K 31/551A61K 31/454A61K 31/5513A61K 31/55A61K 31/41A61K 31/496A61P 25/18A61K 31/16A61K 2300/00
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Claims

Abstract

The present invention relates to a blend for prevention, mitigation, or treatment of schizophrenia, the blend containing a carbamate compound of chemical formula 1, or a pharmaceutically acceptable salt, solvate, or hydrate thereof and, more specifically, to a blend and a pharmaceutical composition each containing a carbamate compound of chemical formula 1 and aripiprazole, and to a use thereof for treating schizophrenia.

Claims

exact text as granted — not AI-modified
1 . A combination for the prevention, alleviation or treatment of schizophrenia, comprising (a) a carbamate compound of the following Formula 1, or a pharmaceutically acceptable salt, solvate or hydrate thereof; and (b) aripiprazole, or a pharmaceutically acceptable salt, solvate or hydrate thereof: 
       
         
           
           
               
               
           
         
         wherein, 
         R 1  and R 2  are each independently selected from the group consisting of hydrogen, halogen, C 1 -C 8  alkyl, halo-C 1 -C 8  alkyl, C 1 -C 8  thioalkoxy and C 1 -C 8  alkoxy; and 
         one of A 1  and A 2  is CH, and the other is N. 
       
     
     
         2 - 22 . (canceled) 
     
     
         23 . A composition comprising (a) a carbamate compound of the following Formula 1, or a pharmaceutically acceptable salt, solvate or hydrate thereof; (b) an antipsycotic agent selected from the group consisting of haloperidol, chlorpromazine, aripiprazole, asenapine, clozapine, iloperidone, olanzapine, lurasidone, paliperidone, quetiapine, risperidone, ziprasidone, and a pharmaceutically acceptable salt, solvate or hydrate thereof; and (c) a pharmaceutically acceptable carrier: 
       
         
           
           
               
               
           
         
         wherein, 
         R 1  and R 2  are each independently selected from the group consisting of hydrogen, halogen, C 1 -C 8  alkyl, halo-C 1 -C 8  alkyl, C 1 -C 8  thioalkoxy and C 1 -C 8  alkoxy; and 
         one of A 1  and A 2  is CH, and the other is N. 
       
     
     
         24 . The composition according to  claim 23 , wherein the antipsycotic agent is selected from the group consisting of haloperidol, chlorpromazine, and a pharmaceutically acceptable salt, solvate or hydrate thereof. 
     
     
         25 . The composition according to  claim 23 , wherein the antipsycotic agent is selected from the group consisting of aripiprazole, asenapine, clozapine, iloperidone, olanzapine, lurasidone, paliperidone, quetiapine, risperidone, ziprasidone, and a pharmaceutically acceptable salt, solvate or hydrate thereof. 
     
     
         26 . The composition according to  claim 23 , wherein R 1  and R 2  are each independently selected from the group consisting of hydrogen, halogen and C 1 -C 8  alkyl. 
     
     
         27 . The composition according to  claim 23 , wherein the carbamate compound of Formula 1 is carbamic acid (R)-1-(2-chlorophenyl)-2-tetrazol-2-yl-ethyl ester of the following Formula 2: 
       
         
           
           
               
               
           
         
       
     
     
         28 . The composition according to  claim 23 , which comprises the compound of Formula 1 in an amount of 12.5 mg to 500 mg based on the free form. 
     
     
         29 . The composition according to  claim 23 , wherein the pharmaceutically acceptable carrier is selected from fillers, antioxidants, buffers, bacteriostats, dispersants, adsorbents, surfactants, binders, preservatives, disintegrants, sweeteners, flavors, glidants, release-controlling agents, wetting agents, stabilizers, suspending agents, and lubricants. 
     
     
         30 . The composition according to  claim 23 , which the pharmaceutically acceptable carrier is selected from saline, sterile water, Ringer's solution, buffered saline, dextrose solution, maltodextrin solution, glycerol, ethanol and mixtures thereof. 
     
     
         31 . The composition according to  claim 29 , wherein the fillers are selected from group consisting of dextrose, sucrose, maltose, lactose, corn starch, mannitol, sorbitol, maltitol, erythritol, xylitol, dextrin, maltodextrin, microcrystalline cellulose, and mixtures thereof. 
     
     
         32 . The composition according to  claim 29 , wherein the antioxidants are selected from group consisting of tocopherol, ascorbic acid, and gallate. 
     
     
         33 . The composition according to  claim 29 , wherein the buffer is citric acid monohydrate. 
     
     
         34 . The composition according to  claim 29 , wherein the surfactants are selected from group consisting of sodium laurate, sodium lauryl sulfate, sodium dodecanesulfonate, sodium oleyl sulfate, benzalkonium chloride, alkyltrimethyl ammonium bromide, glyceryl monooleate, polyoxyethylene dried sorbitan fatty acid ester, polyvinyl alcohol, dried sorbitan S and mixtures thereof. 
     
     
         35 . The composition according to  claim 29 , wherein the binders are selected from group consisting of povidone, copovidone, methylcellulose, hydroxymethylcellulose, hydroxypropylmethylcellulose, hydroxypropylcellulose, hydroxyethylcellulose, gelatin, gum, sucrose, starch or mixtures thereof. 
     
     
         36 . The composition according to  claim 29 , wherein the preservatives are selected from group consisting of benzoic acid, sodium benzoate, benzyl alcohol, butylated hydroxyanisole, butylated hydroxytoluene, chlorbutol, gallate, hydroxybenzoate, EDTA, and mixtures thereof. 
     
     
         37 . The composition according to  claim 29 , wherein the disintegrants are selected from group consisting of sodium starch glycolate, cross-linked polyvinylpyrrolidone, cross-linked carboxymethylcellulose, starch, microcrystalline cellulose, and mixtures thereof. 
     
     
         38 . The composition according to  claim 29 , wherein the glidants are colloidal silicon dioxide. 
     
     
         39 . The composition according to  claim 29 , wherein the release-controlling agents are selected from group consisting of hydroxypropyl methylcellulose, polyethylene oxide, carbomer, pH-independent polymers such as alginic acid, pH-dependent polymers, and mixtures thereof. 
     
     
         40 . The composition according to  claim 29 , wherein the wetting agents are selected from group consisting of hypromellose, polysorbate 20, polysorbate 80, lecithin, polyoxyethylene- and polyoxypropylene ether, sodium deoxycholate, and mixtures thereof. 
     
     
         41 . The composition according to  claim 29 , wherein the suspending agents are selected from group consisting of microcrystalline cellulose, methyl cellulose, sodium carboxymethyl cellulose, hydroxypropyl methyl cellulose, polyvinylpyrrolidone, alginate, chitosan, dextran, gelatin, polyethylene glycol, polyoxyethylene- and polyoxypropylene ether, and mixtures thereof. 
     
     
         42 . The composition according to  claim 29 , wherein the lubricants are selected from group consisting of magnesium stearate, stearic acid, talc, glyceride wax, and mixtures thereof. 
     
     
         43 . A method for preventing, alleviating or treating schizophrenia, comprising:
 administering to a subject in need thereof the composition of  claim 23 .

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