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    • 8. 发明专利
    • Agonistas y composiciones del receptor 5-HT2C y métodos de uso
    • ES2757922T3
    • 2020-04-30
    • ES16721320
    • 2016-04-26
    • ARENA PHARM INC
    • REN ALBERT SSEMPLE GRAEMEZHU XIUWENSAGE CARLETON R
    • C07D487/06A61K31/407A61P25/00
    • Un compuesto seleccionado de los siguientes compuestos, y las sales, hidratos y solvatos farmacéuticamente aceptables de los mismos: N-(2,2-difluoroetil)-7-metil-1,2,3,4,6,7-hexahidro-[1,4]diazepino [6,7,1-hi]indol-8-carboxamida (Compuesto No. 1); (S)-N-(2,2-difluoroetil)-7-metil-1,2,3,4,6,7-hexahidro-[1,4]diazepino [6,7,1-hi]indol-8-carboxamida (Compuesto No. 2); (R)-N-(2,2-difluoroetil)-7-metil-1,2,3,4,6,7-hexahidro-[1,4]diazepino [6,7,1-hi]indol-8-carboxamida (Compuesto No. 3); (S)-N-(2,2-difluoroetil)-7-etil-1,2,3,4,6,7-hexahidro-[1,4]diazepino [6,7,1-hi]indol-8-carboxamida (Compuesto No. 4); (R)-N-(2,2-difluoroetil)-7-etil-1,2,3,4,6,7-hexahidro-[1,4]diazepino [6,7,1-hi]indol-8-carboxamida (Compuesto No. 5); N-(2,2-difluoroetil)-7,7-dimetil-1,2,3,4,6,7-hexahidro-[1,4]diazepino [6,7,1-hi]indol-8-carboxamida (Compuesto No. 6); N-(2,2-difluoroetil)-2,3,4,6-tetrahidro-1H-espiro-[[1,4]diazepino [6,7,1-hi]indol-7,1'-ciclobutano]-8-carboxamida (Compuesto No. 7); (S)-N-(2,2-difluoroetil)-7-(2,2,2-trifluoroetil)-1,2,3,4,6,7-hexahidro-[1,4]diazepino[6,7,1-hi]indol-8-carboxamida (Compuesto No. 8); y (R)-N-(2,2-difluoroetil)-7-(2,2,2-trifluoroetil)-1,2,3,4,6,7-hexahidro-[1,4]diazepino[6,7,1-hi]indol-8-carboxamida (Compuesto No. 9).
    • 10. 发明专利
    • 5-HT2C RECEPTOR AGONISTS AND COMPOSITIONS AND METHODS OF USE
    • CA3002544A1
    • 2016-11-03
    • CA3002544
    • 2016-04-26
    • ARENA PHARM INC
    • REN ALBERT SSEMPLE GRAEMEZHU XIUWENSAGE CARLETON R
    • C07D487/06A61K31/5517A61P25/00
    • Provided in some embodiments are compounds herein. Also provided in some embodiments are methods for weight management, inducing satiety, and decreasing food intake, and for preventing and treating obesity, antipsychotic-induced weight gain, type 2 diabetes, Prader-Willi syndrome, tobacco/nicotine dependence, drug addiction, alcohol addiction, pathological gambling, reward deficiency syndrome, and sex addiction), obsessive-compulsive spectrum disorders and impulse control disorders (including nail-biting and onychophagia), sleep disorders (including insomnia, fragmented sleep architecture, and disturbances of slow-wave sleep), urinary incontinence, psychiatric disorders (including schizophrenia, anorexia nervosa, and bulimia nervosa), Alzheimer disease, sexual dysfunction, erectile dysfunction, epilepsy, movement disorders (including parkinsonism and antipsychotic-induced movement disorder), hypertension, dyslipidemia, nonalcoholic fatty liver disease, obesity-related renal disease, and sleep apnea. Also provided in some embodiments are compositions comprising a compound herein, optionally in combination with a supplemental agent, and methods for reducing the frequency of smoking tobacco in an individual attempting to reduce frequency of smoking tobacco; aiding in the cessation or lessening of use of a tobacco product in an individual attempting to cease or lessen use of a tobacco product; aiding in smoking cessation and preventing associated weight gain; controlling weight gain associated with smoking cessation by an individual attempting to cease smoking tobacco; reducing weight gain associated with smoking cessation by an individual attempting to cease smoking tobacco; treating nicotine dependency, addiction and/or withdrawal in an individual attempting to treat nicotine dependency, addiction and/or withdrawal; or reducing the likelihood of relapse use of nicotine by an individual attempting to cease nicotine use comprising administering a compound herein, optionally in combination with a supplemental agent.