Substituted piperaziniums for the treatment of emesis

Patent metadata

Field	Value
Publication number	US-9908907-B2
Application number	US-201615194984-A
Country	US
Kind code	B2
Filing date	Jun 28, 2016
Priority date	Nov 29, 2011
Publication date	Mar 6, 2018
Grant date	Mar 6, 2018

Abstract

Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK 1 ) receptor. The compounds have the general formula (I):

First claim

What is claimed is:

1. A compound of formula (VI):

or a pharmaceutically acceptable salt thereof,
wherein:
(a) R 2 , R 5 and R 6 are each independently hydrogen;
(b) m, p and s are each independently zero; and
(c) R 200 and R 300 are each independently selected from the group consisting of hydrogen and methyl.

2. A chloride hydrochloride salt of a compound of formula (VI):

wherein:
(a) R 2 , R 5 and R 6 are each independently hydrogen;
(b) m, p and s are each independently zero; and
(c) R 200 and R 300 are each independently selected from the group consisting of hydrogen and methyl.

3. A parenteral pharmaceutical composition comprising a compound of formula (I):

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):

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.

Assignees

• Helsinn Healthcare Sa

Inventors

• Fadini Luca
• Manini Peter
• Pietra Claudio
• Giuliano Claudio
• Lovati Emanuela
• Cannella Roberta
• Venturini Alessio
• Stella Valentino J

Classifications

• C07F9/025

  Purification; Separation; Stabilisation; Desodorisation of organo-phosphorus compounds (of natural phosphatides C07F9/103; phosphines C07F9/5095) · CPC title

• C07D213/76

  to which a second hetero atom is attached (nitro radicals C07D213/61) · CPC title

• A61K31/439

  the ring forming part of a bridged ring system, e.g. quinuclidine (8-azabicyclo [3.2.1] octanes A61K31/46) · CPC title

• A61K31/4178

  not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin · CPC title

• C07D213/74

  Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals · CPC title