IP Library Granted Patent US 9,908,907
Granted Patent B2
US 9,908,907 · App. 15/194,984 · Granted Mar 6, 2018

Substituted piperaziniums for the treatment of emesis

Inventors: Luca Fadini (Giubiasco, CH); Peter Manini (Giubiasco, CH); Claudio Pietra (Como, IT); Claudio Giuliano (Como, IT); Emanuela Lovati (Mendrisio, CH); Roberta Cannella (Varese, IT); Alessio Venturini (Varese, IT); Valentino J Stella (Lawrence, KS)
Assignee: Helsinn Healthcare SA
C07F9/650952A61K31/44A61K31/473A61K31/496A61K31/56A61K31/675A61K45/06C07D213/74C07D213/89C07D401/04
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Quick Facts
Patent No.
US 9,908,907
App. No.
15/194,984
Granted
Mar 6, 2018
Kind
B2
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):

Claims (17)

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.

Assignments (3)
RELEASE OF SECURITY INTEREST Recorded Sep 20, 2023
From: HAMILTON SA LLC
To: HELSINN HEALTHCARE SA; HELSINN THERAPEUTICS (U.S.), INC.; HELSINN BIREX PHARMACEUTICALS LIMITED
Reel/Frame 064961/0567 →
SECURITY INTEREST Recorded Dec 30, 2022
From: HELSINN HEALTHCARE SA; HELSINN THERAPEUTICS (U.S.), INC.; HELSINN BIREX PHARMACEUTICALS LIMITED
To: HAMILTON SA LLC
Reel/Frame 062254/0888 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 6, 2017
From: FADINI, LUCA; MANINI, PETER; PIETRA, CLAUDIO; GIULIANO, CLAUDIO; LOVATI, EMANUELA; CANNELLA, ROBERTA; VENTURINI, ALESSIO; STELLA, VALENTINO J
To: HELSINN HEALTHCARE SA
Reel/Frame 044045/0666 →
Continuity (4)
Continuation 14360991
Continuation In Part 13478361 · May 23, 2012
Provisional Application 61564537 · Nov 29, 2011
Related Publication 20170050993A1 · Feb 23, 2017