Morpholine contains secondary amine groups and has all the typical reactive characteristics of secondary amine groups. It can react with inorganic acids to form salts, and react with organic acids to form salts or amides, which can be subjected to alkylation reaction, and can also be reacted with ethylene oxide, ketone or Willgerodt reaction. Morpholine is a six-membered ring containing oxygen and nitrogen, and its alkalinity is much lower than that of its parent piperidine. The marketed morpholine drugs are mainly distributed in the fields of tumors, cardiovascular and cerebrovascular diseases, respiratory system diseases, digestive system diseases, infectious diseases and mental disorders.
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On January 8, 2024, Bayer announced positive top-line results of the pivotal Phase III studies OASIS 1 and 2 evaluating the efficacy and safety of the investigational compound elinzanetant versus placebo. Elinzanetant successfully met all four primary endpoints and all three key secondary endpoints in both studies. Elinzanetant is a first dual neurokinin-1,3 (NK-1,3) receptor antagonist for the non-hormonal treatment of moderate to severe VMS associated with menopause. Elinzanetant may address moderate to severe VMS by modulating a group of estrogen sensitive neurons in the hypothalamus region of the brain (the KNDy neurons) which, with the decrease of estrogen, become hypertrophic and lead to a hyperactivation of the thermoregulatory pathway, consequently disrupting body heat control mechanisms resulting in VMS. Elinzanetant may also decrease sleep disturbances associated with menopause.
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