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![Process for preparing {6-[(diethylamino)methyl]naphthalen-2-yl}methyl [4-(hydroxycarbamoyl)phenyl]carbamate having high purity](/abs-image/US/2022/06/09/US20220177421A1/abs.jpg.150x150.jpg)
公开(公告)号：US20220177421A1
公开(公告)日：2022-06-09
申请号：US17435731
申请日：2020-03-05
Applicant: ITALFARMACO SPA
Inventor： Stefano TURCHETTA , Maurizio ZENONI , Elio ULLUCCI , Stefania COCCIOLO , Giorgio BERARDI , Nakia MAULUCCI
IPC: C07C271/28 , C07C269/06 , B01J20/281
Abstract: A process for obtaining {{6-[(diethylamino)methyl]naphthalen-2-yl}methyl [4-(hydroxycarbamoyl)phenyl]carbamate and/or pharmaceutically acceptable salts thereof having high purity is described. This process allows to obtain a product having an amount of any single unknown impurity equal to or less than 0.10%, as well as a product having a purity greater than 99.5%, preferably equal to or greater than 99.6%.
An HPLC method for determining the purity of the product and possible impurities thereof is also described.-
2.发明申请USE OF HISTONE DEACETYLASE INHIBITORS FOR THE CARE OF PHILADELPHIA-NEGATIVE MYELOPROLIFERATIVE SYNDROMES 审中-公开乙酰脱乙酰基酶抑制剂用于治疗儿童肾上腺髓质增生综合征公开(公告)号：US20170049740A1
公开(公告)日：2017-02-23
申请号：US15346926
申请日：2016-11-09
Applicant: ITALFARMACO SPA
Inventor： Tiziano OLDONI , Paolo MASCAGNI , Alessandro RAMBALDI , Tiziano BARBUI
Abstract: The use of substances capable of inhibiting one or more enzymes of the histone deacetylase family (histone deacetylase inhibitors) for the therapeutic treatment of Philadelphia-negative myeloproliferative syndromes (polycythemia vera, essential thrombocythemia or idiopathic myelofibrosis) is described. The dosage of the above-mentioned substances is significantly lower than that normally used for the care of other tumour syndromes and may be from 10 to 150 mg/day/patient.
Abstract translation: 描述了能够抑制组蛋白脱乙酰酶家族的一种或多种酶（组蛋白脱乙酰酶抑制剂）用于费城阴性骨髓增生综合征（真性红细胞增多症，原发性血小板增多症或特发性骨髓纤维化）的治疗性治疗的物质的使用。 上述物质的剂量明显低于通常用于其他肿瘤综合征的治疗剂量，并且可以为10至150mg /天/患者。
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公开(公告)号：US20210128512A1
公开(公告)日：2021-05-06
申请号：US17149794
申请日：2021-01-15
Applicant: ITALFARMACO SPA
Inventor： Tiziano OLDONI , Paolo MASCAGNI , Alessandro RAMBALDI , Tiziano BARBUI
Abstract: Method of treating Philadelphia-negative myeloproliferative syndromes in a patient suffering therefrom by administering to the patient diethyl-[6-(4-hydroxycarbamoyl-phenylcarbamoyloxymethyl)-naphthalen-2-yl-methyl]-ammonium chloride, or other pharmaceutically acceptable salts and/or solvates, in a daily dosage amount of from 50 to 100 mg per patient.
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![Process for preparing {6-[(diethylamino)methyl]naphthalen-2-yl}methyl [4-(hydroxycarbamoyl)phenyl]carbamate having high purity](/abs-image/US/2023/11/02/US20230348368A1/abs.jpg.150x150.jpg)
4.发明公开公开(公告)号：US20230348368A1
公开(公告)日：2023-11-02
申请号：US18338435
申请日：2023-06-21
Applicant: ITALFARMACO SPA
Inventor： Stefano TURCHETTA , Maurio ZENONI , Elio ULLUCCI , Stefania COCCIOLO , Giorgio Berardi , Nakia MAULUCCI
IPC: C07C271/28 , C07C269/06 , B01J20/286 , C07C269/08
CPC classification number: C07C271/28 , C07C269/06 , B01J20/286 , C07C269/08 , G01N2030/027
Abstract: A process for obtaining {{6-[(diethylamino)methyl]naphthalen-2-yl}methyl [4-(hydroxycarbamoyl)phenyl]carbamate and/or pharmaceutically acceptable salts thereof having high purity is described. This process allows to obtain a product having an amount of any single unknown impurity equal to or less than 0.10%, as well as a product having a purity greater than 99.5%, preferably equal to or greater than 99.6%.
An HPLC method for determining the purity of the product and possible impurities thereof is also described.-
5.发明申请USE OF HISTONE DEACETYLASE INHIBITORS FOR THE CARE OF PHILADELPHIA-NEGATIVE MYELOPROLIFERATIVE SYNDROMES 审中-公开乙酰脱乙酰基酶抑制剂用于治疗儿童肾上腺髓质增生综合征公开(公告)号：US20140039059A1
公开(公告)日：2014-02-06
申请号：US14047391
申请日：2013-10-07
Applicant: ITALFARMACO SPA
Inventor： Tiziano Oldoni , Paolo Mascagni , Alessandro Rambaldi , Tiziano Barbui
IPC: A61K31/167 , A61K45/06
Abstract: The use of substances capable of inhibiting one or more enzymes of the histone deacetylase family (histone deacetylase inhibitors) for the therapeutic treatment of Philadelphia-negative myeloproliferative syndromes (polycythemia vera, essential thrombocythemia or idiopathic myelofibrosis) is described. The dosage of the above-mentioned substances is significantly lower than that normally used for the care of other tumour syndromes and may be from 10 to 150 mg/day/patient.
Abstract translation: 描述了能够抑制组蛋白脱乙酰酶家族的一种或多种酶（组蛋白脱乙酰酶抑制剂）用于费城阴性骨髓增生综合征（真性红细胞增多症，原发性血小板增多症或特发性骨髓纤维化）的治疗性治疗的物质的使用。 上述物质的剂量明显低于通常用于其他肿瘤综合征的治疗剂量，并且可以为10至150mg /天/患者。
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Patent Agency Ranking
公开(公告)号：US20250057913A1
公开(公告)日：2025-02-20
申请号：US18721923
申请日：2022-12-22
Applicant: ITALFARMACO SPA
Inventor： Daniela MODENA , Giovanni SANDRONE , Andrea STEVENAZZI , Christian STEINKÜHLER , Natalia S. PELLEGATA , Stefan SCHULZ
Abstract: The present invention relates to the use of the compound of formula (I) or the pharmaceutically acceptable salts and/or solvates thereof in the treatment of SSTR3 expressing tumors, selected from non-functioning pituitary adenomas (NFPAs) or other neuroendocrine-related malignancies, selected from pancreatic tumors, pheochromocytomas, paragangliomas, lung carcinoids or breast cancer. More specifically, the present invention provides to the use of pharmaceutical compositions comprising the compound of formula (I) or the pharmaceutically acceptable salts and/or solvates thereof and at least one physiologically acceptable excipient in the treatment of a patient affected by SSTR3 expressing tumors, selected from non-functioning pituitary adenomas (NFPAs) or other neuroendocrine-related malignancies, selected from pancreatic tumors, pheochromocytomas, paragangliomas, lung carcinoids or breast cancer.
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公开(公告)号：US10688047B2
公开(公告)日：2020-06-23
申请号：US15770443
申请日：2016-10-28
Applicant: ITALFARMACO SPA
Inventor： Giuseppe Colombo , Roberta Artico , Paolo Mascagni , Maria Valmen Monzani , Silvia Puccianti
IPC: A61K9/00 , A61K47/10 , A61K9/10 , A61K47/26 , A61K31/167 , A61P7/02 , A61P21/00 , A61P19/02 , A61P35/02 , A61K31/325 , A61K47/02 , A61K47/12 , A61K47/36
Abstract: Physically and chemically stable oral liquid formulations of Givinostat (Diethyl-[6-(4-hydroxycarbamoyl-phenylcarbamoyloxymethyl)-naphthalen-2-yl-methyl]-ammonium chloride) are disclosed, together with methods for the preparation thereof. Such oral formulations are in the form of aqueous suspensions and contain Givinostat and/or pharmaceutically acceptable salts and/or derivatives thereof, at least a wetting agent and/or at least a density-imparting agent. Such formulations are suitable for oral administration for systemic therapeutic action.
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8.发明授权Use of histone deacetylase inhibitors for the care of philadelphia-negative myeloproliferative syndromes 有权组蛋白脱乙酰酶抑制剂用于照顾费城阴性骨髓增生综合征公开(公告)号：US09522127B2
公开(公告)日：2016-12-20
申请号：US14047391
申请日：2013-10-07
Applicant: ITALFARMACO SPA
Inventor： Tiziano Oldoni , Paolo Mascagni , Alessandro Rambaldi , Tiziano Barbui
IPC: A61K31/00 , A61K31/16 , A61K31/167 , A61K45/06 , A61K31/18
Abstract: Method of treating Philadelphia-negative myeloproliferative syndromes in a patient suffering from such syndromes. The method is carried out by administering to the patient diethyl-[6-(4-hydroxycarbamoyl-phenylcarbamoyloxymethyl)-naphthalen-2-yl -methyl]-ammonium chloride, or other pharmaceutically acceptable salts and/or solvates, in a daily dosage amount of from 10 to 150 mg per patient.
Abstract translation: 在患有这种综合征的患者中治疗费城阴性骨髓增生综合征的方法。 该方法通过以日剂量给予患者二乙基 - [6-（4-羟基氨基甲酰基 - 苯基氨基甲酰氧基甲基） - 萘-2-基 - 甲基] - 氯化铵或其他药学上可接受的盐和/或溶剂合物 每位患者10至150mg。
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公开(公告)号：US20250011878A1
公开(公告)日：2025-01-09
申请号：US18711937
申请日：2022-11-22
Applicant: ITALFARMACO SPA
Inventor： Gianluca FOSSATI , Chiara RIPAMONTI , Christian STEINKÜHLER
IPC: C12Q1/6886
Abstract: The present invention relates a method based on mRNA biomarkers that can be used to define the efficacious dose and/or the biological activity of inhibitors of histone deacetylase 6 (HDAC6), such as the compound N-hydroxy-4-((5-(thiophen-2-yl)-1H-tetrazol-1-yl)methyl) benzamide, during the clinical treatment of patients affected by cancer. More in particular, the invention refers to the analysis of the gene expression's variation of specific biomarkers in human monocytes, as “gene expression signatures”, in a method to evaluate the clinical efficacy of HDAC6 inhibitors, such as the compound N-hydroxy-4-((5-(thiophen-2-yl)-1H-tetrazol-1-yl)methyl)benzamide.
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![Process for preparing {6-[(diethylamino)methyl]naphthalen-2-yl}methyl [4-(hydroxycarbamoyl)phenyl]carbamate having high purity](/abs-image/US/2024/10/29/US12129224B2/abs.jpg.150x150.jpg)
公开(公告)号：US12129224B2
公开(公告)日：2024-10-29
申请号：US17435731
申请日：2020-03-05
Applicant: ITALFARMACO SPA
Inventor： Stefano Turchetta , Maurizio Zenoni , Elio Ullucci , Stefania Cocciolo , Giorgio Berardi , Nakia Maulucci
IPC: C07C271/28 , B01J20/286 , C07C269/06 , C07C269/08 , G01N30/02
CPC classification number: C07C271/28 , B01J20/286 , C07C269/06 , C07C269/08 , G01N2030/027 , C07C269/06 , C07C271/28 , C07C269/08 , C07C271/28
Abstract: A process for obtaining {{6-[(diethylamino)methyl]naphthalen-2-yl}methyl[4-(hydroxycarbamoyl)phenyl]carbamate and/or pharmaceutically acceptable salts thereof having high purity is described. This process allows to obtain a product having an amount of any single unknown impurity equal to or less than 0.10%, as well as a product having a purity greater than 99.5%, preferably equal to or greater than 99.6%.
An HPLC method for determining the purity of the product and possible impurities thereof is also described.
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