US2021338674A1PendingUtilityA1

Compounds and pharmaceutical compositions for treating disorders associated with the 5-ht1a and 5-ht2a receptors

Assignee: ACHE LABORATORIOS FARMACEUTICOS SAPriority: Sep 24, 2010Filed: Apr 30, 2021Published: Nov 4, 2021
Est. expirySep 24, 2030(~4.2 yrs left)· nominal 20-yr term from priority
A61P 25/22A61K 31/517C07D 239/88A61P 25/28A61P 25/18A61P 25/00A61K 31/513A61P 15/00A61P 25/30C07D 239/91A61P 43/00C07D 239/90A61P 25/24
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Claims

Abstract

Alkyl-piperazine-phenyl 4 (3H)-quinazolinones compounds of general formula (I) below are provided that are pharmacologicaly active and able to act on the 5-HT1A and 5-HT2A serotonin receptors in a manner that promotes the control, relief or cure of disorders associated with these receptors, and pharmaceutical compositions containing the compounds for the treatment of disorders associated with these receptors. These compounds and their pharmaceutical compositions are useful in the treatment of conditions such as depression, anxiety, phobias, addictions, aggressiveness, impulsiveness, panic, psychotic, eating and sleep disorders, obsessive-compulsive disorder and female sexual dysfunctions, including loss of sexual desire, inhibition of sexual desire and absence of sexual desire, among other disorders associated with these receptors.

Claims

exact text as granted — not AI-modified
1 . A 5-HT1A and 5-HT2A serotonin modulator compound having the formula (I): 
       
         
           
           
               
               
           
         
         wherein: 
         n=2, R1 is hydrogen, and R2 is 2-methoxyphenyl; 
         or pharmaceutically acceptable salts thereof. 
       
     
     
         2 . A pharmaceutical composition comprising the compound according to  claim 1  and a pharmaceutical acceptable excipient. 
     
     
         3 . The pharmaceutical composition according to  claim 2 , wherein the compound in the composition is in an amount sufficient to treat a disorder associated with the 5-HT 1A  and 5-HT 2A  receptors in a patient. 
     
     
         4 . The pharmaceutical composition according to  claim 3 , wherein a dosage of the compound is an amount of from about 0.1 mg to about 1,000 mg. 
     
     
         5 . The pharmaceutical composition according to  claim 4 , wherein the dosage is from about 5 mg to about 500 mg. 
     
     
         6 . The pharmaceutical composition according to  claim 4 , wherein the dosage is from about 1 mg to about 250 mg. 
     
     
         7 . The pharmaceutical composition according to  claim 3 , wherein the composition is in a form that is suitable for administration via a mode selected from the group consisting of oral, parenteral, nasal, rectal, transmucosal, and transdermal administration, 
     
     
         8 . The pharmaceutical composition according to  claim 3 , wherein the disorder associated with the 5-HT 1A  and 5-HT 2A  receptors is selected from the group consisting of depression, anxiety, phobias, panic, addictions, aggressiveness, impulsiveness, eating disorders, sleep disorders, obsessive-compulsive disorder, psychotic disorders, disorders involving the heat regulation mechanism, female sexual dysfunctions, hypoactive sexual desire disorder, sexual aversion disorder, female sexual excitation disorder, and the loss, inhibition or absence of sexual desire.

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