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
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
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
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).
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).
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.
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.
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
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.
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.
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
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
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
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.
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
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
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
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.
Abstract: A process is described for preparing budesonide which comprises the steps of: a) preparing an aqueous hydrochloric acid solution; b) reacting 16?-hydroxyprednisolone and butyraldehyde within the solution prepared in step a), in an inert atmosphere; c) quenching the reaction of step b) with water. The process of the invention enables the ratio between the A and B epimers of budesonide to be controlled.
Abstract: A process is described for preparing, exclusively by chemical way, 21-hydroxy steroids having progestinic activity, said process having a high stereochemical control at C-21 position.
Type:
Grant
Filed:
October 20, 2005
Date of Patent:
January 11, 2011
Assignee:
Industriale Chimica S.R.L.
Inventors:
Francesca Costantino, Roberto Lenna, Maria Julieta Comin, Javier Ramirez, Juan Bautista Rodriguez