Claims for Patent: 9,403,772

Summary for Patent: 9,403,772

Title:	4-(5-(2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethylpropanamido)-4-(o-tol- yl)pyridin-2-yl)-1-methyl-1-((phosphonooxy)methyl)piperazin-1-ium as a neurokinin receptor modulator
Abstract:	Compounds and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK.sub.1) receptor, based on 4-(5-(2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethylpropanamido)-4-(o-to- lyl)3yridine-2-yl)-1-methyl-1-((phosphonooxy)methyl)piperazin-1-ium and pharmaceutically acceptable salts thereof.
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:	14/360,991
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,403,772
Patent Claims:	1. A pharmaceutically acceptable salt of a compound of formula GA1: ##STR00038## 2. A method of treating emesis, bladder dysfunction, depression or anxiety in a patient, comprising administering to said patient in need thereof a therapeutically effective amount of a compound of formula GA1: ##STR00039## or a pharmaceutically acceptable salt thereof. 3. The method of claim 2, wherein the patient is a human. 4. The method of claim 2, wherein said compound, or pharmaceutically acceptable salt thereof, is intravenously administered at a dosage of from 10 mg to 200 mg. 5. The method of claim 2, wherein said emesis comprises chemotherapy induced nausea and vomiting, radiation therapy induced nausea and vomiting, or post-operative nausea and vomiting. 6. The method of claim 2, wherein said emesis is induced by moderately or highly emetogenic chemotherapy. 7. The method of claim 2, wherein said emesis is acute and delayed emesis induced by moderately or highly emetogenic chemotherapy. 8. The method of claim 2, wherein said emesis is acute and delayed emesis induced by moderately or highly emetogenic chemotherapy, further comprising administering ondansetron, palonosetron, granisetron or tropisetron, or a pharmaceutically acceptable salt thereof and a corticosteroid. 9. A method for making a compound of formula GA1: ##STR00040## comprising (a) reacting 2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1- -yl)-4-(o-tolyl)pyridin-3-yl)propanamide with chloromethyl di-tert-butyl phosphate in the presence of a polar aprotic solvent; and (b) isolating the compound of formula GA1. 10. The method of claim 9, wherein step (a) is carried out in the presence of an iodide salt and in the absence of a proton scavenger. 11. The method of claim 9, wherein step (a) is carried out in the absence of air and oxygen. 12. A method for stabilizing a compound of formula GA1: ##STR00041## comprising contacting the compound with two equivalents of hydrochloric acid. 13. The method of claim 12, wherein the hydrochloric acid is 4M hydrochloric acid. 14. A compound having the following formula: ##STR00042##