Helsinn Healthcare Sa

Ocera Therapeutics, Inc.

Ono Pharmaceutical Co., Ltd.

Other

Ono Pharmaceuticals Co., Ltd.

Peter Manini

Stephen William Watt

Keith Anderson

Jim Behling

Christine Henderson Dougan

Attilia Figini

Valentino J Stella

Claudio Pietra

Claudio Giuliano

Alessio Venturini

Luca Fadini

Emanuela Lovati

Roberta Cannella

Silvina Garcia Rubio

Seemon H Pines

Hideyuki Yoshiyama

Eleanor De Groot

Shin-itsu Kuwabe

Takehiko Yanagimachi

Shin-Itsu Kuwabe

Seemon (deceased) Pines

Keith H Anderson

Seemon Pines

Disclosed are compounds including phosphate and N-oxide prodrugs of the NK1 antagonist netupitant, useful in the prevention and/or treatment of diseases including emesis induced by chemotherapy. Also disclosed are methods of making a di-tert-butyl (chloromethyl) phosphate useful in the manufacture of such prodrugs by reacting a dialkylphosphate salt with an acid to obtain the corresponding ester of phosphoric acid, reacting the ester with a quaternary ammonium hydroxide base to form a monobasic salt, and reacting the monobasic salt with chloroiodomethane to form the corresponding chloromethyl dialkyl phosphate.

Process for the synthesis of substituted chloromethyl dialkylphosphates

Fosnetupitant chloride hydrochloride having improved stability, characterized by the following chemical structure: 

Fosnetupitant chloride hydrochloride having improved stability

Disclosed herein are forms of L-ornithine phenyl acetate and methods of making the same. A crystalline form may, in some embodiments, be Forms I, II, III and V, or mixtures thereof. The crystalline forms may be formulated for treating subjects with liver disorders, such as hepatic encephalopathy. Accordingly, some embodiments include formulations and methods of administering L-ornithine phenyl acetate.

L-ornithine phenyl acetate and methods of making thereof

The present invention relates to particulate forms of anamorelin monohydrochloride or a composition comprising anamorelin monohydrochloride having controlled chloride content, preferably isolated in an amorphous and/or fine particulate state, processes for making the particulate forms, and pharmaceutical compositions comprising the particulate forms.

Methods of producing anamorelin hydrochloride having controlled chloride content

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

Substituted piperaziniums for the treatment of emesis

Disclosed is a solution comprising the chloride hydrochloride salt of 4-(5-(2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethylpropanamido)-4-(o-tolyl)pyridin-2-yl)-1-methyl-1-((phosphonooxy)methyl)piperazin-1-ium (fosnetupitant) and palonosetron hydrochloride in combination with dexamethasone and its application in methods for preventing acute and delayed nausea and vomiting in a human patient receiving highly emetogenic cancer chemotherapy.

Solution comprising the chloride hydrochloride salt of 4-(5-(2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethylpropanamido)-4-(o-tolyl)pyridin-2-yl)-1-methyl-1-((phosphonooxy)methyl)piperazin-1-IUM-(fosnetupitant) and palonosetron hydrochloride in combination with dexamethasone as a neurokinin receptor modulator

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Giubiasco, Switzerland

Peter Manini