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公开(公告)号：US11529362B2
公开(公告)日：2022-12-20
申请号：US16817683
申请日：2020-03-13
IPC分类号： A61K31/675 , A61K31/496 , A61K9/08 , A61K9/00 , A61K9/19 , A61K47/02 , A61K47/18 , A61K47/26 , A61K31/473 , A61P1/08
摘要： Injectable dosages and formulations of fosnetupitant and pharmaceutically acceptable salts thereof are provided that are efficacious, chemically stable and physiologically balanced for safety and efficacy.
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公开(公告)号：US20180194788A1
公开(公告)日：2018-07-12
申请号：US15874325
申请日：2018-01-18
发明人： Luca Fadini , Peter Manini , Claudio Pietra , Claudio Giuliano , Emanuela Lovati , Roberta Cannella , Alessio Venturini , Valentino J. Stella
IPC分类号： C07F9/6509 , C07D401/04 , C07D213/89 , C07D213/74 , A61K45/06 , A61K31/44 , A61K31/56 , A61K31/496 , A61K31/473 , A61K31/675
CPC分类号： C07F9/650952 , A61K31/44 , A61K31/473 , A61K31/496 , A61K31/56 , A61K31/675 , A61K45/06 , C07D213/74 , C07D213/89 , C07D401/04
摘要： Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK1) receptor. The compounds have the general formula (I):
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公开(公告)号：US20200206249A1
公开(公告)日：2020-07-02
申请号：US16817683
申请日：2020-03-13
IPC分类号： A61K31/675 , A61P1/08 , A61K9/08 , A61K47/26 , A61K47/18 , A61K47/02 , A61K31/496 , A61K31/473 , A61K9/19 , A61K9/00
摘要： Injectable dosages and formulations of fosnetupitant and pharmaceutically acceptable salts thereof are provided that are efficacious, chemically stable and physiologically balanced for safety and efficacy.
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公开(公告)号：US10005803B2
公开(公告)日：2018-06-26
申请号：US15282016
申请日：2016-09-30
发明人： Luca Fadini , Alessio Venturini
IPC分类号： C07F9/6509 , C07F9/09
CPC分类号： C07F9/650952 , C07B2200/13 , C07F9/091 , C07F9/65583
摘要： The present invention provides crystalline forms of the chloride monohydrochloride salt of fosnetupitant, methods of making the crystalline forms, and pharmaceutical dosage forms that make use of the crystalline forms.
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公开(公告)号：US12071421B2
公开(公告)日：2024-08-27
申请号：US17699522
申请日：2022-03-21
发明人： Luca Fadini , Peter Manini , Claudio Pietra , Claudio Giuliano , Emanuela Lovati , Roberta Cannella , Alessio Venturini , Valentino J. Stella
IPC分类号： C07D401/04 , A61K9/00 , A61K31/4178 , A61K31/439 , A61K31/44 , A61K31/473 , A61K31/496 , A61K31/56 , A61K31/573 , A61K31/675 , A61K45/06 , A61P1/08 , A61P13/10 , A61P25/22 , A61P25/24 , C07D213/74 , C07D213/76 , C07D213/89 , C07F9/02 , C07F9/6509
CPC分类号： C07D401/04 , A61K9/0019 , A61K31/4178 , A61K31/439 , A61K31/44 , A61K31/473 , A61K31/496 , A61K31/56 , A61K31/573 , A61K31/675 , A61K45/06 , A61P1/08 , A61P13/10 , A61P25/22 , A61P25/24 , C07D213/74 , C07D213/76 , C07D213/89 , C07F9/025 , C07F9/650952
摘要： 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.
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公开(公告)号：US20170348335A1
公开(公告)日：2017-12-07
申请号：US15611785
申请日：2017-06-02
IPC分类号： A61K31/675 , A61K47/18 , A61K31/496 , A61K9/00 , A61K31/473 , A61K9/19 , A61K47/26 , A61K47/02
CPC分类号： A61K31/675 , A61K9/0019 , A61K9/08 , A61K9/19 , A61K31/473 , A61K31/496 , A61K47/02 , A61K47/183 , A61K47/26 , A61P1/08
摘要： Injectable dosages and formulations of fosnetupitant and pharmaceutically acceptable salts thereof are provided that are efficacious, chemically stable and physiologically balanced for safety and efficacy.
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公开(公告)号：US20150011510A1
公开(公告)日：2015-01-08
申请号：US14360991
申请日：2012-11-28
发明人： Luca Fadini , Peter Manini , Claudio Pietra , Claudio Guiliano , Emanuela Lovati , Roberta Cannella , Alessio Venturini , Valentino J. Stella
IPC分类号： C07D213/89 , A61K31/675 , A61K45/06 , A61K31/496 , C07D213/76 , C07F9/06 , C07D213/72
CPC分类号： C07D213/89 , C07D213/72 , C07D213/74 , C07D213/76 , C07D401/04 , C07F9/062
摘要： Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK1) receptor. The compounds have the general formula (I):
摘要翻译： 公开了用于预防和/或治疗由神经激肽（NK1）受体病理生理介导的疾病的化合物，组合物和方法。 该化合物具有通式（I）：
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公开(公告)号：US20230172953A1
公开(公告)日：2023-06-08
申请号：US17986934
申请日：2022-11-15
IPC分类号： A61K31/675 , A61K9/08 , A61P1/08 , A61K9/00 , A61K9/19 , A61K31/473 , A61K31/496 , A61K47/02 , A61K47/18 , A61K47/26
CPC分类号： A61K31/675 , A61K9/08 , A61P1/08 , A61K9/0019 , A61K9/19 , A61K31/473 , A61K31/496 , A61K47/02 , A61K47/183 , A61K47/26
摘要： Injectable dosages and formulations of fosnetupitant and pharmaceutically acceptable salts thereof are provided that are efficacious, chemically stable and physiologically balanced for safety and efficacy.
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公开(公告)号：US10717721B2
公开(公告)日：2020-07-21
申请号：US16228835
申请日：2018-12-21
发明人： Luca Fadini , Peter Manini , Claudio Pietra , Claudio Giuliano , Emanuela Lovati , Roberta Cannella , Alessio Venturini , Valentino J. Stella
IPC分类号： C07D213/74 , C07D401/04 , A61K31/496 , A61K31/56 , A61K45/06 , C07D213/89 , A61K31/44 , A61K31/473 , A61K31/675 , C07F9/6509 , A61P25/22 , A61P13/10 , A61P25/24 , A61P1/08 , A61K9/00 , A61K31/573
摘要： Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK1) receptor. The compounds have the general formula (I):
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公开(公告)号：US10208073B2
公开(公告)日：2019-02-19
申请号：US15874325
申请日：2018-01-18
发明人： Luca Fadini , Peter Manini , Claudio Pietra , Claudio Giuliano , Emanuela Lovati , Roberta Cannella , Alessio Venturini , Valentino J Stella
IPC分类号： C07D213/74 , C07D453/02 , C07J9/00 , C07F9/6509 , C07D401/04 , A61K31/496 , A61K31/56 , A61K45/06 , C07D213/89 , A61K31/44 , A61K31/473 , A61K31/675
摘要： 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.
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