IP Library Granted Patent US 8,895,586
Granted Patent B2
US 8,895,586 · App. 13/864,381 · Granted Nov 25, 2014

Methods of treating 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)
C07D213/74A61K31/44C07D213/89C07D401/04A61K31/496A61K31/56A61K45/06
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Quick Facts
Patent No.
US 8,895,586
App. No.
13/864,381
Granted
Nov 25, 2014
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 (25)

1. A method of treating emesis in a patient in need thereof, comprising administering to said patient a therapeutically effective amount of the following compound:

or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein said emesis comprises chemotherapy-induced nausea and vomiting, radiotherapy-induced nausea and vomiting, or post-operative nausea and vomiting.

3. The method of claim 1 , wherein said emesis is induced by moderately emetogenic chemotherapy.

4. The method of claim 1 , wherein said emesis is induced by highly emetogenic chemotherapy.

5. The method of claim 1 , wherein said emesis is acute and delayed emesis induced by moderately or highly emetogenic chemotherapy.

6. The method of claim 1 , wherein said compound is administered via injection.

7. The method of claim 1 , wherein said compound is administered at a dosage of from 10 to 200 mg.

8. The method of claim 1 , further comprising administering palonosetron or a pharmaceutically acceptable salt thereof.

9. The method of claim 1 , further comprising administering palonosetron or a pharmaceutically acceptable salt thereof and dexamethasone.

10. A method of treating emesis in a patient in need thereof, comprising administering to said patient via injection a therapeutically effective amount of the following compound:

or a pharmaceutically acceptable salt thereof.

11. The method of claim 10 , wherein said emesis comprises chemotherapy-induced nausea and vomiting.

12. The method of claim 10 , wherein said emesis is acute and delayed emesis induced by moderately or highly emetogenic chemotherapy.

13. The method of claim 10 , wherein said compound is administered via injection at a dosage of from 10 to 200 mg.

14. A method of treating emesis in a patient in need thereof, comprising administering to said patient a therapeutically effective amount of the following compound:

in combination with palonosetron or a pharmaceutically acceptable salt thereof and dexamethasone.

15. The method of claim 14 , wherein said emesis comprises chemotherapy-induced nausea and vomiting.

16. The method of claim 14 , wherein said compound is administered via injection.

17. The method of claim 14 , wherein said compound is administered via injection at a dosage of from 10 to 200 mg.

18. A method of treating emesis in a patient in need thereof, comprising administering to said patient a therapeutically effective amount of the following compound:

or a pharmaceutically acceptable salt thereof.

19. The method of claim 18 , wherein said compound is administered via injection.

20. The method of claim 18 , wherein said compound is administered at a dosage of from 10 to 200 mg.

21. The method of claim 18 , further comprising administering 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 Jan 2, 2018
From: FADINI, LUCA; MANINI, PETER; PIETRA, CLAUDIO; GIULIANO, CLAUDIO; LOVATI, EMANUELA; CANNELLA, ROBERTA; VENTURINI, ALESSIO; STELLA, VALENTINO J; BRAGLIA, RICCARDO
To: HELSINN HEALTHCARE SA
Reel/Frame 044519/0821 →
Continuity (3)
Division 13478361 · May 23, 2012
Provisional Application 61564537 · Nov 29, 2011
Related Publication 20130231315A1 · Sep 5, 2013