Patents Assigned to Industriale Chimica S.R.L.
  • Patent number: 12077559
    Abstract: The present invention relates to a new process for the synthesis of 3?-hydroxy-5?-pregnan-20-one, commonly known as brexanolone, wherein the corresponding cyclic 20-ketal or cyclic 20-thioketal compound of formula (IV) is deprotected with the use or iodine in an organic solvent: (I).
    Type: Grant
    Filed: October 21, 2019
    Date of Patent: September 3, 2024
    Assignee: INDUSTRIALE CHIMICA S.R.L.
    Inventors: Claudio Delfrate, Davide Rigamonti, Tea Borelli, Roberto Lenna
  • Publication number: 20240199684
    Abstract: The present invention refers to a process for the industrial-scale preparation of 17?-hydroxy-6?,7?; 15?,16?-dimethylene-3-oxo-17?-pregn-4-ene-21-carboxylic acid y-lactone, known by the common name of Drospirenone, in the form of a fine powder without the use of mechanical grinding or micronization techniques. but rather exploiting a double change of crystalline form, from Crystalline Form I to Crystalline Form II and from Crystalline Form II to Crystalline Form I. The invention also refers to the new Crystalline Form II of Drospirenone obtained in the process.
    Type: Application
    Filed: April 8, 2022
    Publication date: June 20, 2024
    Applicant: INDUSTRIALE CHIMICA S.R.L.
    Inventors: Roberto LENNA, Michele BALDRIGHI
  • Patent number: 11840519
    Abstract: The present invention to a process for the preparation of the sodium salt of 4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]-amino]-butanoic acid, compound also known as Elagolix sodium salt, having the formula (I) reported below:
    Type: Grant
    Filed: July 27, 2020
    Date of Patent: December 12, 2023
    Assignee: INDUSTRIALE CHIMICA S.R.L.
    Inventors: Roberto Lenna, Andrea Fasana, Jerry Ortiz
  • Publication number: 20230287036
    Abstract: The present invention relates to a process for preparing (15?,16?,17(?)-Estra-1,3,5(10)-triene -3,15,16,17-tetrol monohydrate, also known as Estetrol monohydrate.
    Type: Application
    Filed: May 17, 2023
    Publication date: September 14, 2023
    Applicant: INDUSTRIALE CHIMICA S.R.L.
    Inventors: Roberto Lenna, Andrea Fasana, Riccardo Lucentini
  • Publication number: 20220348607
    Abstract: The present invention relates to a process for preparing (15?,16?,17?)-Estra-1,3,5(10)-triene-3,15,16,17-tetrol, also known as Estetrol, having the formula shown below:
    Type: Application
    Filed: September 25, 2020
    Publication date: November 3, 2022
    Applicant: INDUSTRIALE CHIMICA S.R.L.
    Inventors: Roberto LENNA, Andrea FASANA, Riccardo LUCENTINI
  • Patent number: 11390645
    Abstract: A process for the synthesis of ?-hydroxy 3-17-(1H-benzimidazol-1-yl)androsta-5,16-diene is described, a compound also known as Galeterone and used in the treatment of prostate cancer, having the formula (6).
    Type: Grant
    Filed: August 8, 2017
    Date of Patent: July 19, 2022
    Assignee: INDUSTRIALE CHIMICA S.R.L.
    Inventors: Francesco Barbieri, Roberto Lenna
  • Publication number: 20210284681
    Abstract: A process for the synthesis of ?-hydroxy 3-17-(1H-benzimidazol-1-yl)androsta-5,16-diene is described, a compound also known as Galeterone and used in the treatment of prostate cancer, having the formula 6).
    Type: Application
    Filed: August 8, 2017
    Publication date: September 16, 2021
    Applicant: INDUSTRIALE CHIMICA S.R.L.
    Inventors: Francesco BARBIERI, Roberto LENNA
  • Patent number: 10189765
    Abstract: The present invention relates to a new process for the synthesis of 17?-hydroxy-des-A-androst-9,10-en-5-one, the compound of the following formula (1), which can be used as an intermediate in the synthesis of retroprogesterones.
    Type: Grant
    Filed: October 28, 2016
    Date of Patent: January 29, 2019
    Assignee: INDUSTRIALE CHIMICA S.R.L.
    Inventors: Roberto Lenna, Roberto Di Brisco
  • Publication number: 20180339956
    Abstract: The present invention relates to a new process for the synthesis of 17?-hydroxy-des-A-androst-9,10-en-5-one, the compound of the following formula (1), which can be used as an intermediate in the synthesis of retroprogesterones.
    Type: Application
    Filed: October 28, 2016
    Publication date: November 29, 2018
    Applicant: INDUSTRIALE CHIMICA S.R.L.
    Inventors: Roberto LENNA, Roberto DI BRISCO
  • Patent number: 9695213
    Abstract: A process is described wherein, by employing 17?-(3-hydroxypropyl)-6?,7?;15?,16?-dimethylene-5?-androstane-3?,5,17?-triol (II) as starting product, in a single stage reaction there is obtained drospirenone, (I), a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic action, that is useful for preparing pharmaceutical compositions with contraceptive action.
    Type: Grant
    Filed: February 20, 2013
    Date of Patent: July 4, 2017
    Assignee: INDUSTRIALE CHIMICA S.R.L.
    Inventors: Roberto Lenna, Johannes Bernardus Maria Rewinkel, Francesco Barbieri, Maria Giovanna Luoni
  • Patent number: 9676815
    Abstract: The present invention relates to a novel process for the synthesis of abiraterone and in particular abiraterone acetate, a compound of formula (I) reported below: having pharmacological activity suitable for slowing down the progression of advanced stage prostate cancer. The process is characterized by the fact that the intermediate triflation step is carried out on prasterone (DHEA) or its 3-acetate using Ar—N(OTf)2 as the triflation reagent, but where Ar is not phenyl, and by the fact that the base used in this step is an alkali metal alcoholate.
    Type: Grant
    Filed: July 23, 2014
    Date of Patent: June 13, 2017
    Assignee: INDUSTRIALE CHIMICA S.R.L.
    Inventors: Roberto Lenna, Riccardo Di Brisco
  • Patent number: 9650410
    Abstract: The present invention relates to a novel process for the synthesis of abiraterone, and in particular of abiraterone acetate, compound of formula (I) reported below: N O (I) which has pharmacological activity useful for slowing down the progression of prostate cancer at an advanced stage. The process is characterized by an intermediate step wherein DHEA-acetate is triflated using Ar—N(OTf)2 as the triflation reagent.
    Type: Grant
    Filed: July 29, 2013
    Date of Patent: May 16, 2017
    Assignee: INDUSTRIALE CHIMICA S.R.L.
    Inventors: Roberto Lenna, Riccardo Di Brisco
  • Patent number: 9562068
    Abstract: An improved process for the preparation of intermediate (V) through the elimination of a molecule of water from intermediate (IV) is described. Intermediate (V) is a key molecule for the synthesis of eplerenone, a synthetic steroid with pharmacological activity used in the treatment of chronic pathological conditions, including hypertension.
    Type: Grant
    Filed: October 16, 2015
    Date of Patent: February 7, 2017
    Assignee: INDUSTRIALE CHIMICA, S.r.l.
    Inventors: Roberto Lenna, Riccardo Di Brisco, Francesco Barbieri
  • Patent number: 9556220
    Abstract: A process is disclosed wherein, using either 17a-(3-hydroxypropyl)-6p,7p;15p,16p-dimethylene-5p-androstane-3p,5,17p-triol (II) or 3?,5^ïI^?^-6?,7?;15?,16?-dimethylene-5?,17?-pregnane-21,17-carbolactone (III) as starting material, through a single-step reaction it is obtained drospirenone (I), a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic activity, useful for preparing pharmaceutical compositions with contraceptive action.
    Type: Grant
    Filed: April 12, 2013
    Date of Patent: January 31, 2017
    Assignee: INDUSTRIALE CHIMICA S.R.L.
    Inventors: Roberto Lenna, Francesco Barbieri, Maria Giovanna Luoni, Monica Noseda
  • Patent number: 9422326
    Abstract: There is described a process for the industrial synthesis of 11-methylene-18-methyl-estr-4-en-3,17-dione, a compound having the structure formula (I) depicted below: (Formula I) (I) useful as intermediate compound in the synthesis of the progestin compounds Desogestrel and Etonogestrel.
    Type: Grant
    Filed: September 3, 2013
    Date of Patent: August 23, 2016
    Assignee: INDUSTRIALE CHIMICA S.r.l.
    Inventors: Roberto Lenna, Edoardo Mariani, Andrea Vanossi
  • Patent number: 9394334
    Abstract: It is described of a process for the preparation of drospirenone, the compound of formula 1 shown below, a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic activity, useful for preparing pharmaceutical compositions having contraceptive action, starting from 17?-(3-hydroxypropyl)-6?,7?;15?,16?-dimethylene-5?-androstane-3?,5,17?-triol.
    Type: Grant
    Filed: November 21, 2012
    Date of Patent: July 19, 2016
    Assignee: INDUSTRIALE CHIMICA S.R.L.
    Inventors: Roberto Lenna, Andrea Vanossi
  • Patent number: 8933061
    Abstract: A process is described, comprising the oxidation of 17?-(3-hydroxypropyl)-6?,7?,15?,16?-dimethylen-5?-androstan-3?,5,17?-triol, for the preparation of drospirenone, a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic activity, useful for preparing pharmaceutical compositions with contraceptive action.
    Type: Grant
    Filed: July 19, 2012
    Date of Patent: January 13, 2015
    Assignee: Industriale Chimica S.r.l.
    Inventors: Roberto Lenna, Francesco Barbieri, Daniele Giudici
  • Publication number: 20130030169
    Abstract: A process is described, comprising the oxidation of 17?-(3-hydroxypropyl)-6?,7?,15?,16?-dimethylen-5?-androstan-3?,5,17?-triol, for the preparation of drospirenone, a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic activity, useful for preparing pharmaceutical compositions with contraceptive action.
    Type: Application
    Filed: July 19, 2012
    Publication date: January 31, 2013
    Applicant: INDUSTRIALE CHIMICA, S.R.L.
    Inventors: Roberto Lenna, Francesco Barbieri, Daniele Giudici
  • Patent number: 8242291
    Abstract: A process is described for the preparation on an industrial scale of N-[2-(8S)-1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl]ethyl]propionamide, ramelteon, having the structure illustrated below:
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: August 14, 2012
    Assignee: Industriale Chimica S.r.L.
    Inventors: Roberto Lenna, Cristina Ghidoli, Luigi Panza
  • Patent number: 8227596
    Abstract: A process is described for the preparation of drospirenone, a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic activity, useful for preparing pharmaceutical compositions with contraceptive action by the oxidation of 17?-(3-hydroxypropyl)-6?,7?,15?, 16?-dimethylene-5?-androstane-3?,5,17?-triol.
    Type: Grant
    Filed: August 4, 2010
    Date of Patent: July 24, 2012
    Assignee: Industriale Chimica S.R.L.
    Inventors: Francesca Costantino, Roberto Lenna, Silvia Piuri