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Last Updated: October 31, 2020

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Claims for Patent: 9,908,907

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Summary for Patent: 9,908,907
Title:Substituted piperaziniums for the treatment of emesis
Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK.sub.1) receptor. The compounds have the general formula (I): ##STR00001##
Inventor(s): Fadini; Luca (Giubiasco, CH), Manini; Peter (Giubiasco, CH), Pietra; Claudio (Como, IT), Giuliano; Claudio (Como, IT), Lovati; Emanuela (Mendrisio, CH), Cannella; Roberta (Varese, IT), Venturini; Alessio (Varese, IT), Stella; Valentino J (Lawrence, KS)
Assignee: Helsinn Healthcare SA (Lugano/Pazzallo, CH)
Application Number:15/194,984
Patent Claims: 1. A compound of formula (VI): ##STR00051## or a pharmaceutically acceptable salt thereof, wherein: (a) R.sub.2, R.sub.5 and R.sub.6 are each independently hydrogen; (b) m, p and s are each independently zero; and (c) R.sub.200 and R.sub.300 are each independently selected from the group consisting of hydrogen and methyl.

2. A chloride hydrochloride salt of a compound of formula (VI): ##STR00052## wherein: (a) R.sub.2, R.sub.5 and R.sub.6 are each independently hydrogen; (b) m, p and s are each independently zero; and (c) R.sub.200 and R.sub.300 are each independently selected from the group consisting of hydrogen and methyl.

3. A parenteral pharmaceutical composition comprising a compound of formula (I): ##STR00053## or a pharmaceutically acceptable salt thereof, and one or more liquid pharmaceutical excipients.

4. The parenteral composition of claim 3, wherein the parenteral composition further comprises palonosetron, or a pharmaceutically acceptable salt thereof.

5. A parenteral pharmaceutical composition comprising a chloride hydrochloride salt of a compound of formula (I): ##STR00054## and one or more liquid pharmaceutical excipients.

6. The parenteral composition of claim 5, wherein the parenteral composition further comprises palonosetron, or a pharmaceutically acceptable salt thereof.

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