Helsinn Healthcare Sa

Turboden, S.p.a.

Other

Turboden S.r.l.

Anacardio Ab

Claudio Pietra

Claudio Giuliano

Silvina Garcia Rubio

Valentino J Stella

Peter Manini

Alessio Venturini

Luca Fadini

Emanuela Lovati

Roberta Cannella

Angelo Guainazzi

Roberto Bini

Antoine Daina

Mario Gaia

Zhigang Li

Marielle Martinez-Loi

Mauro Perseghini

Davide Colombo

Sergio Cantoreggi

Andrea Duvia

Lars Lund

Alberto Bernareggi

The new compound 3-(1-(2,3-dichloro-4-methoxyphenyl)ethyl)-1-methyl-1-(1,3,3-trimethylpiperidin-4-yl)urea monohydrochloride salt has a high capability to permeate through the blood-brain barrier and to display, at central nervous system level, a consistent ghrelin agonist activity; the compound is effective in the treatment and/or prevention of a medical condition mediated by the ghrelin receptor in the central nervous system. In particular, in experimental tests, the compound has shown high efficacy in the treatment of neurotoxic damage, with a useful combined pattern of neuroprotective effects both at central and peripheral level. The compound is further useful in the treatment of conditions which require a reduction of the heart rate. The compound is pharmacologically active at low to moderate doses, thus showing a favourable therapeutic index.

Centrally-active ghrelin agonist and medical uses thereof

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

The new compound 3-(1-(2,3-dichloro-4-methoxyphenyl) ethyl)-1-methyl-1-(1,3, 3-trimethylpiperidin-4-yl)urea monohydrochloride salt has a high capability to permeate through the blood-brain barrier and to display, at central nervous system level, a consistent ghrelin agonist activity; the compound is effective in the treatment and/or prevention of a medical condition mediated by the ghrelin receptor in the central nervous system. In particular, in experimental tests, the compound has shown high efficacy in the treatment of neurotoxic damage, with a useful combined pattern of neuroprotective effects both at central and peripheral level. The compound is further useful in the treatment of conditions which require a reduction of the heart rate. The compound is pharmacologically active at low to moderate doses, thus showing a favourable therapeutic index.

An organic Rankine cycle system with cascade cycles provided with a first organic Rankine cycle which operates at high temperature, in which a first organic working fluid carries out a heat exchange with a hot source fluid and a second organic Rankine cycle which operates at a temperature lower than the temperature of the first organic Rankine cycle and in which a second organic working fluid carries out a heat exchange with the same hot source. The evaporator of the first organic Rankine cycle is fed by the entire flow rate of the hot source fluid, while the evaporator and the preheater of the second organic Rankine cycle are fed by a first partial flow of the hot source fluid, the remaining second partial flow of the hot source fluid being used to partially carry out the preheating of the organic working fluid of the first organic Rankine cycle.

Cascade organic Rankine cycle plant

Provided are various embodiments relating to fumarate salt of (R)-3-(1-(2,3-dichloro-4-(pyrazin-2-yl)phenyl)-2,2,2-trifluoroethyl)-1-methyl-1-(1-methylpiperidin-4-yl) urea, and methods of producing and using the same to treat conditions and disorders associated with an increase of ghrelin level, such as food abuse, alcohol addiction, and other disorders (e.g., Prader-Willi syndrome). Also provided are various embodiments relating to crystalline HM04 free base, different crystalline forms of HM04 fumarate salt, and methods of producing the same.

Fumarate salt of (R)-3-(1-(2,3-dichloro-4-(pyrazin-2-yl)phenyl)-2,2,2-trifluoroethyl)-1-methyl-1-(1-methylpiperidin-4-yl)urea, methods of preparation, and uses thereof

A cascade organic Rankine cycle plant comprising a hot source, at least a first high temperature organic Rankine cycle and a second low temperature organic Rankine cycle, said cycles comprising at least one preheater, at least one vaporizer, at least one turbine, at least one condenser, wherein the hot source first supplies a vaporizer of the high temperature cycle, then the vaporizer of the low temperature cycle and finally it is divided into two flows which supply a first preheater of the high temperature cycle and a preheater of the low temperature cycle. The first high-temperature organic Rankine cycle comprises a further vaporizer operating at an intermediate pressure between the vaporizer pressure of the high temperature cycle and the vaporizer pressure of the low temperature cycle.

Optimized cascade organic Rankine cycle

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

Fosnetupitant chloride hydrochloride having improved stability

Fumarate salt of (R)-3-(1-(2,3-dichloro-4-(pyrazin-2-yl)phenyl)-2,2,2- trifluoroethyl)-1-methyl-1-(1-methylpiperidin-4-yl) urea, methods of preparation, and uses thereof

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 are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the ghrelin receptor. The compounds have the general Formula I: or pharmaceutically acceptable salts thereof.

Substituted asymmetric ureas as modulators of ghrelin receptor activity

Benzenesulfonyl-asymmetric ureas are provided for the treatment of conditions modulated by the ghrelin receptor.

Benzenesulfonyl-asymmetric ureas and medical uses thereof

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

Asymmetric ureas and medical uses thereof

An embodiment of the present invention is a method of controlling an Organic Rankine Cycle system, the system comprising at least one feed pump (), at least one heat exchanger (), an expansion turbine () and a condenser (), the organic Rankine Cycle comprising a feeding phase of an organic working fluid, a heating and vaporization phase of the same working fluid, an expansion and condensation phase of the same working fluid, wherein said method controls an adjusted variable (X), which is a function of an overheating of the organic fluid, by means of a controller () that acts by varying a control variable (Y), which is a parameter of the organic fluid in its liquid phase, and wherein the adjusted variable (X) is a temperature difference (&#x394;T) between a current temperature of the organic fluid in vapor phase at the turbine inlet and a temperature threshold (Tlim), under which the expansion phase involves the formation of a liquid phase of the organic fluid.

Control method for an organic rankine cycle

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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Como, Italy

Claudio Pietra