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Carbamoyl cyclohexane derivatives for treating autism spectrum disorder

A technology for autism and derivatives, which is applied in the field of carbamoylcyclohexane derivatives for the treatment of autism spectrum disorders, and can solve problems such as reduced function

Pending Publication Date: 2021-11-19
RICHTER GEDEON NYRT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Further studies reported that 5-hydroxytryptamine 5-HT in the peripheral and brain of ASD patients 2 Type (not specified) receptor function is also reduced (McBride et al., Arch. Gen. Psychiatry 1989, 46, 213-221)

Method used

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  • Carbamoyl cyclohexane derivatives for treating autism spectrum disorder
  • Carbamoyl cyclohexane derivatives for treating autism spectrum disorder
  • Carbamoyl cyclohexane derivatives for treating autism spectrum disorder

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Embodiment Construction

[0024] In one aspect, the present application relates to trans-N-[4-[2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl]cyclohexyl disclosed in WO 2005 / 012266A1 ]-N',N'-dimethylurea hydrochloride (cariprazine) and trans-N-[4-{2-[4-(2,3-dichloro-phenyl)-piperazine -1-yl]-ethyl}-cyclohexyl]-morpholine-4-carboxamide hydrochloride (compound 2). Cariprazine has shown great benefit on ASD symptoms in animal models. These results suggest that cariprazine, its close analogs and derivatives may have therapeutic effects against the symptoms of ASD in human patients.

[0025] In one aspect, the application relates to the use of cariprazine, its salts, close analogs, derivatives, pharmaceutical compositions, metabolites and combinations for the treatment of a condition selected from Asperger's syndrome, Atypical autism (also known as combined mental developmental disorder not otherwise specified; PDD-NOS), Rett syndrome, childhood schizotypal disorder, attention deficit hyperactivity disorde...

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Abstract

The present invention relates to trans-N-[4-[2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl]cyclohexyl]-N',N'-dimethylurea (cariprazine), its salts, close analogs, derivatives, pharmaceutical compositions, metabolites and combinations for use in the treatment of symptoms of autism spectrum disorder in general, and preferably the object of the present invention is to treat one or more symptoms of autism. Furthermore, it was also found that cariprazine, its salts, close analogs, derivatives, pharmaceutical compositions, metabolites and combinations are suitable for treatment of conditions such as Asperger's syndrome, atypical autism (otherwise known as pervasive developmental disorder not otherwise specified; PDD-NOS), Rett syndrome, childhood disintegrative disorder, attention deficit hyperactivity disorder (ADHD) and sensory integration dysfunction.

Description

technical field [0001] The present invention relates to trans-N-[4-[2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl]cyclohexyl] for use in the treatment of symptoms of autism spectrum disorder -N',N'-dimethylurea (cariprazine), salts, close analogs, derivatives, pharmaceutical compositions, metabolites and combinations thereof. Background technique [0002] Autism Spectrum Disorder (ASD) is a complex, very challenging and prevalent neurodevelopmental disorder with a frequency of 1:34-1:77 (average 1 :59) (CDC Morbidity and Mortality Weekly Report Surveillance Summaries, April 27, 2018 / 67(6):1-23 "CDC Morbidity and Mortality Weekly Report Surveillance Summaries, April 27, 2018 / 67(6): 1-23"). According to several epidemiological studies, the median prevalence estimate for ASD in 2012 was 62 / 10,000 (Elsabbagh et al., Autism Res. 2012, 5: 160-179). As such, ASD is today recognized as a global, common, lifelong neurodevelopmental disorder affecting about 1% of children and adult...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61K31/5377A61K45/06A61P25/00
CPCA61K31/496A61K31/5377A61K45/06A61P25/00A61K31/495A61P25/18
Inventor V·罗曼N·阿德哈姆-帕兰吉W·罗杰厄利P·珀-杰杨
Owner RICHTER GEDEON NYRT
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