Claims for Patent: 10,717,721

Summary for Patent: 10,717,721

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 (NK1) receptor. The compounds have the general formula (I):
Inventor(s):	Luca Fadini, Peter Manini, Claudio Pietra, Claudio Giuliano, Emanuela Lovati, Roberta Cannella, Alessio Venturini, Valentino J. Stella
Assignee:	Helsinn Healthcare SA
Application Number:	US16/228,835
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,717,721
Patent Claims:	1. A compound of formula (VI): or a pharmaceutically acceptable salt thereof, wherein: each R1 is independently hydrogen, halogen, alkyl, alkylNR101R102, alkenyl,—C(O)R101, —C(O)NR101R102, —C(O)OR101, —NR101R102, —NR101C(O)R102, —OR101, —SR101, —S(O)2R102, —S(O)2NR101R102, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl, wherein the alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl are each optionally substituted with one or more independently selected R103 substituents; each R2 is independently hydrogen, halogen, alkyl, alkylNR101R102, alkenyl,—C(O)R101, —C(O)NR101R102, —C(O)OR101, —NR101R102, —NR101C(O)R102, —OR101, —SR101, —S(O)2R102, —S(O)2NR101R102, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl, wherein the alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl are each optionally substituted with one or more independently selected R103 substituents; R5 is hydrogen, halogen, alkyl, alkylNR101R102, alkenyl,—C(O)R101, —C(O)NR101R102, —C(O)OR101, —NR101R102, —NR101C(O)R102, —OR101, —SR101, —S(O)2R102, —S(O)2NR101R102, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl, wherein the alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl are each optionally substituted with one or more independently selected R103 substituents; R6 is hydrogen, halogen, alkyl, alkylNR101R102, alkenyl,—C(O)R101, —C(O)NR101R102, —C(O)OR101, —NR101R102, —NR101C(O)R102, —OR101, —SR101, —S(O)2R102, —S(O)2NR101R102, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl, wherein the alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl are each optionally substituted with one or more independently selected R103 substituents; each R7 is independently hydrogen, halogen, alkyl, alkenyl, amino, —OR104, or cycloalkyl, wherein the alkyl, alkenyl, amino and cycloalkyl are each optionally substituted with one or more independently selected R103 substituents; R200 is hydrogen, alkyl, or cycloalkyl, wherein the alkyl and cycloalkyl are each optionally substituted with one or more independently selected R103 substituents; R300 is hydrogen, alkyl, or cycloalkyl, wherein the alkyl and cycloalkyl are each optionally substituted with one or more independently selected R103 substituents; R101 is hydrogen, halogen, cyano, nitro, oxide, alkyl, alkenyl, —C(O)OR104, —C(O)NR104R105, —C(O)OR104, —NR104R105, —NR104C(O)R105, —NR104 S(O)2R105, —OR104, —SR104, —S(O)2NR104R105, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl, wherein the alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl are each optionally substituted with one or more independently selected R103 substituents; R102 is hydrogen, halogen, cyano, nitro, oxide, alkyl, alkenyl, —C(O)OR104, —C(O)NR104R105, —C(O)OR104, —NR104R105, —NR104C(O)R105, —NR104 S(O)2R105, —OR104, —SR104, —S(O)2NR104R105, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl, wherein the alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl are each optionally substituted with one or more independently selected R103 substituents; or R101and R102, together with the atoms to which they are attached, form a fused or non-fused monocyclic, bicyclic or tricyclic carbocyclic or heterocyclic ring, which is optionally and independently substituted with one or more independently selected R103 substituents; each R103 is independently halogen, cyano, nitro, oxide, alkyl, alkenyl, —C(O)OR104, —C(O)NR104R105, —C(O)OR104, —NR104R105, —NR104C(O)R105, —NR104 S(O)2R105, —OR104, —SR104, —S(O)2NR104R105, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; R104 is hydrogen, halogen, cyano, nitro, oxide, alkyl, hydroxyalkyl, alkoxyalkyl, heterocycloalkylalkyl, arylalkyl, heteroarylalkyl, alkenyl, amino, hydroxy, alkoxy, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; R105 is hydrogen, halogen, cyano, nitro, oxide, alkyl, hydroxyalkyl, alkoxyalkyl, heterocycloalkylalkyl, arylalkyl, heteroarylalkyl, alkenyl, amino, hydroxy, alkoxy, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; m is 0, 1, 2, 3, or 4; each p is independently 0 or 1; and s is 0, 1, 2, 3, or 4; with a proviso that if a non-pyridine N-Oxide is present on the compound of formula (VI), then the total number of N-Oxides on the compound of formula (VI) is greater than one. 2. A compound selected from the group consisting of: or a pharmaceutically acceptable salt thereof.