Patents by Inventor Marco Alpegiani

Marco Alpegiani has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Process for the preparation of enzalutamide
    Patent number: 10035776
    Abstract: Disclosed is a process for the preparation of Enzalutamide comprising the reaction (Scheme 2), wherein R can be alkyl, aryl, aryl-alkyl or heterocyclyl.
    Type: Grant
    Filed: May 24, 2016
    Date of Patent: July 31, 2018
    Assignee: Olon S.P.A.
    Inventors: Samuele Frigoli, Davide Longoni, Marco Alpegiani, Claudio Fuganti, Stefano Serra
  • INDUSTRIAL PROCESS FOR THE PREPARATION OF ENZALUTAMIDE
    Publication number: 20180148416
    Abstract: Disclosed is an efficient method of synthesising Enzalutamide, which comprises the cyclisation reaction of isothiocyanate 1 with acid 3 pre-treated with a silylating agent, or reacting 1 and 3 in the presence of a silylating agent.
    Type: Application
    Filed: May 24, 2016
    Publication date: May 31, 2018
    Applicant: Olon S.P.A.
    Inventors: Samuele Frigoli, Davide Longoni, Marco Alpegiani
  • PROCESS FOR THE PREPARATION OF ENZALUTAMIDE
    Publication number: 20180141914
    Abstract: Disclosed is a process for the preparation of Enzalutamide comprising the reaction (Scheme 2), wherein R can be alkyl, aryl, aryl-alkyl or heterocyclyl.
    Type: Application
    Filed: May 24, 2016
    Publication date: May 24, 2018
    Applicant: Olon S.P.A.
    Inventors: Samuele Frigoli, Davide Longoni, Marco Alpegiani, Claudio Fuganti, Stefano Serra
  • Process for the preparation of ospemifene and fispemifene
    Patent number: 9975832
    Abstract: Disclosed is a process for the synthesis of the active ingredients ospemifene and fispemifene which comprises reacting phenol 4 with an alkylating agent X—CH2CH2—Y of formula 7, wherein X is a leaving group and Y is the —(OCH2CH2)nOH group wherein n is zero or 1; or X and Y, taken together, represent an oxygen atom; to give ospemifene or fispemifene of formula 8.
    Type: Grant
    Filed: December 28, 2015
    Date of Patent: May 22, 2018
    Assignee: OLON S.P.A.
    Inventors: Tania Cristiano, Marco Alpegiani
  • PROCESS FOR THE PREPARATION OF OSPEMIFENE AND FISPEMIFENE
    Publication number: 20170342007
    Abstract: Disclosed is a process for the synthesis of the active ingredients ospemifene and fispemifene which comprises reacting phenol 4 with an alkylating agent X—CH2CH2—Y of formula 7, wherein X is a leaving group and Y is the —(OCH2CH2)nOH group wherein n is zero or 1; or X and Y, taken together, represent an oxygen atom; to give ospemifene or fispemifene of formula 8.
    Type: Application
    Filed: December 28, 2015
    Publication date: November 30, 2017
    Inventors: Tania Cristiano, Marco Alpegiani
  • Procedure for the preparation of abiraterone acetate and intermediates thereof
    Patent number: 9630987
    Abstract: Disclosed is a process for the preparation of abiraterone and abiraterone acetate with high yields and purity. A key element of the method is the isolation of a crystalline intermediate that makes the process particularly suitable for implementation on an industrial scale.
    Type: Grant
    Filed: October 27, 2016
    Date of Patent: April 25, 2017
    Assignee: OLON S.P.A.
    Inventors: Tania Cristiano, Marco Alpegiani
  • PROCEDURE FOR THE PREPARATION OF ABIRATERONE ACETATE AND INTERMEDIATES THEREOF
    Publication number: 20170044207
    Abstract: Disclosed is a process for the preparation of abiraterone and abiraterone acetate with high yields and purity. A key element of the method is the isolation of a crystalline intermediate that makes the process particularly suitable for implementation on an industrial scale.
    Type: Application
    Filed: October 27, 2016
    Publication date: February 16, 2017
    Inventors: Tania Cristiano, Marco Alpegiani
  • Procedure for the preparation of abiraterone acetate and intermediates thereof
    Patent number: 9556219
    Abstract: Disclosed is a process for the preparation of abiraterone and abiraterone acetate with high yields and purity. A key element of the method is the isolation of a crystalline intermediate that makes the process particularly suitable for implementation on an industrial scale. There is also provided a process for the production of abiraterone acetate by acetylation of abiraterone in the absence of bases or acetylation catalysts.
    Type: Grant
    Filed: January 27, 2015
    Date of Patent: January 31, 2017
    Assignee: OLON S.P.A.
    Inventors: Tania Cristiano, Marco Alpegiani
  • PROCEDURE FOR THE PREPARATION OF ABIRATERONE ACETATE AND INTERMEDIATES THEREOF
    Publication number: 20160347786
    Abstract: Disclosed is a process for the preparation of abiraterone and abiraterone acetate with high yields and purity. A key element of the method is the isolation of a crystalline intermediate that makes the process particularly suitable for implementation on an industrial scale. There is also provided a process for the production of abiraterone acetate by acetylation of abiraterone in the absence of bases or acetylation catalysts.
    Type: Application
    Filed: January 27, 2015
    Publication date: December 1, 2016
    Inventors: Tania CRISTIANO, Marco ALPEGIANI
  • Crystalline salts of asenapine
    Patent number: 9447109
    Abstract: Disclosed is asenapine phosphate of formula (I) and its enantiomer (I) which can be used to prepare asenapine maleate. Further disclosed is a monoclinic crystalline form of asenapine maleate.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: September 20, 2016
    Assignee: OLON S.P.A.
    Inventors: Samuele Frigoli, Davide Longoni, Tamara Danelli, Marco Alpegiani
  • Process for the purification of abiraterone acetate
    Patent number: 9340571
    Abstract: The invention relates to a process for the purification of crude abiraterone acetate by treatment with polymer resins in aqueous solvent. The purified product is recovered by simple concentration and filtration.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: May 17, 2016
    Assignee: OLON S.P.A.
    Inventors: Marco Alpegiani, Tania Cristiano, Eugenio Cucchetti
  • Process for the preparation of unsaturated trifluoromethanesulfonate steroid derivatives
    Patent number: 9315541
    Abstract: Disclosed is a method for the conversion of a compound of formula 3 to a compound of formula 4, wherein R is an acetyl group or an alcohol-protecting group. The process involves reacting 3 with a triflating agent in the presence of a nicotinate (3-pyridinecarboxylate) of a C1-C4 alcohol, preferably methyl nicotinate (methyl 3-pyridinecarboxylate) or ethyl nicotinate (ethyl 3-pyridinecarboxylate), to give 4. The method can be conveniently used in a process for the preparation of Abiraterone or Abiraterone acetate.
    Type: Grant
    Filed: May 15, 2015
    Date of Patent: April 19, 2016
    Assignee: OLON S.P.A.
    Inventors: Marco Alpegiani, Tania Cristiano
  • PROCESS FOR THE PURIFICATION OF ABIRATERONE ACETATE
    Publication number: 20160052958
    Abstract: The invention relates to a process for the purification of crude abiraterone acetate by treatment with polymer resins in aqueous solvent. The purified product is recovered by simple concentration and filtration.
    Type: Application
    Filed: October 21, 2013
    Publication date: February 25, 2016
    Inventors: Marco Alpegiani, Tania Cristiano, Eugenio Cucchetti
  • PROCESS FOR THE PREPARATION OF UNSATURATED TRIFLUOROMETHANESULFONATE STEROID DERIVATIVES
    Publication number: 20150337007
    Abstract: Disclosed is a method for the conversion of a compound of formula 3 to a compound of formula 4, wherein R is an acetyl group or an alcohol-protecting group. The process involves reacting 3 with a triflating agent in the presence of a nicotinate (3-pyridinecarboxylate) of a C1-C4 alcohol, preferably methyl nicotinate (methyl 3-pyridinecarboxylate) or ethyl nicotinate (ethyl 3-pyridinecarboxylate), to give 4. The method can be conveniently used in a process for the preparation of Abiraterone or Abiraterone acetate.
    Type: Application
    Filed: May 15, 2015
    Publication date: November 26, 2015
    Inventors: Marco Alpegiani, Tania Cristiano
  • Crystalline (6R,7R)-7-{2-(5-amino-[1,2,4] thiadiazol-3-yl)-2-[(Z)-trityloxyimino]-acetylamino}-3-[(R)-1?-tert-butoxycarbonyl-2-oxo-[1,3?]bipyrrolidinyl-(3E)-ylidenemethyl]-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid benzhydryl ester; its manufacture and use
    Patent number: 9163034
    Abstract: A solid DMSO solvate of a compound of formula (I) is described, which is a useful intermediate for preparing the broad spectrum antibiotics Ceftobiprole and Ceftobiprole Medocaril.
    Type: Grant
    Filed: September 15, 2014
    Date of Patent: October 20, 2015
    Assignee: BASILEA PHARMACEUTICA AG
    Inventors: Marco Alpegiani, Jr., Walter Cabri, Markus Heubes, Davide Longoni, Michael Schleimer
  • CRYSTALLINE (6R,7R)-7--3- [(R)-1'-TERT-BUTOXYCARBONYL-2-OXO-[1,3']BIPYRROLIDINYL-(3E)-YLIDENEMETHYL]-8-OXO-5-THIA-1-AZA-BICYCLO[4.2.0] OCT-2-ENE-2-CARBOXYLIC ACID BENZHYDRYL ESTER; ITS MANUFACTURE AND USE
    Publication number: 20150005491
    Abstract: A solid DMSO solvate of a compound of formula (I) is described, which is a useful intermediate for preparing the broad spectrum antibiotics Ceftobiprole and Ceftobiprole Medocaril.
    Type: Application
    Filed: September 15, 2014
    Publication date: January 1, 2015
    Applicant: Basilea Pharmaceutica AG
    Inventors: Marco Alpegiani, JR., Walter Cabri, Markus Heubes, Davide Longoni, Michael Schleimer
  • Crystalline (6R,7R)-7-{2-(5-amino-[1,2,4] thiadiazol-3-yl)-2-[(Z)-trityloxyimino]-acetylamino}-3-[(R)-1?-tert-butoxycarbonyl-2-oxo-[1,3?]bipyrrolidinyl-(3E)-ylidenemethyl]-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid benzhydryl ester; its manufacture and use
    Patent number: 8865697
    Abstract: A solid DMSO solvate of a compound of formula (I) is described, which is a useful intermediate for preparing the broad spectrum antibiotics Ceftobiprole and Ceftobiprole Medocaril.
    Type: Grant
    Filed: April 14, 2009
    Date of Patent: October 21, 2014
    Assignee: Basilea Pharmaceutica AG
    Inventors: Marco Alpegiani, Walter Cabri, Markus Heubes, Davide Longoni, Michael Schleimer
  • CRYSTALLINE SALTS OF ASENAPINE
    Publication number: 20140051741
    Abstract: Disclosed is asenapine phosphate of formula (I) and its enantiomer (I) which can be used to prepare asenapine maleate. Further disclosed is a monoclinic crystalline form of asenapine maleate.
    Type: Application
    Filed: April 30, 2012
    Publication date: February 20, 2014
    Applicant: OLON SPA
    Inventors: Samuele Frigoli, Davide Longoni, Tamara Danelli, Marco Alpegiani
  • Crystalline irinotecan hydrochloride and methods for its preparation
    Patent number: 8247426
    Abstract: Disclosed is a crystalline form of irinotecan hydrochloride (I) and processes for the preparation thereof from crude irinotecan hydrochloride or another polymorphic form of irinotecan. Said crystalline form is particularly suitable for industrial use, because it is easily filtered and possesses characteristics of high stability and purity.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: August 21, 2012
    Assignee: Antibioticos S.p.A.
    Inventors: Giovanni Pozzi, Paolo Ghetti, Gaetano Balsamo, Ettore Negri, Marco Alpegiani, Angelo Bedeschi, Roberta Pizzocaro
  • Stereoselective process and crystalline forms of a camptothecin
    Patent number: 8124769
    Abstract: A stereoselective process for preparing 7-[(E)-t-butyloxyiminomethyl]-camptothecin (also known as gimatecan) is herein disclosed. With the addition of further dissolution and precipitation steps carried out in appropriate different solvent mixtures, four new crystalline forms of gimatecan are also obtainable by using the same stereoselective process.
    Type: Grant
    Filed: August 17, 2010
    Date of Patent: February 28, 2012
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Paolo Carminati, Maria Ornella Tinti, Mauro Marzi, Fabrizio Giorgi, Walter Cabri, Marco Alpegiani, Domenico Vergani, Paolo Ghetti