公开(公告)号：US09181260B2

公开(公告)日：2015-11-10

申请号：US14381954

申请日：2013-03-01

Applicant: MOEHS IBERICA S.L.

Inventor： Maria del Carmen Bernabeu Martínez ,  Alicia Dobarro Rodríguez ,  Cristobal Galán Rodríguez

IPC: A61K9/20 ,  A61K9/28 ,  A61K31/155 ,  A61K31/22 ,  A61K31/404 ,  A61K31/4439 ,  A61K31/4985 ,  A61K31/64 ,  A61K45/06 ,  C07D487/04

CPC classification number: C07D487/04 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/28 ,  A61K31/155 ,  A61K31/22 ,  A61K31/404 ,  A61K31/4439 ,  A61K31/4985 ,  A61K31/64 ,  A61K45/06 ,  A61K2300/00

Abstract: A novel crystalline form of sitagliptin sulfate is provided. In addition, a method for obtaining the crystalline form, pharmaceutical compositions comprising the novel crystalline form and the crystalline form for use as a medicament are provided.

Abstract translation: 提供硫酸西他列嗪的新型结晶形式。 此外，提供了获得结晶形式的方法，包含新型结晶形式的药物组合物和用作药物的结晶形式。

公开(公告)号：US20220411382A1

公开(公告)日：2022-12-29

申请号：US17755412

申请日：2020-03-10

Applicant: MOEHS IBERICA, S.L.

Inventor： Roberto BALLETTE ,  Oscar JIMÉNEZ ALONSO ,  Elena GARCÍA GARCÍA ,  Alicia DOBARRO RODRÍGUEZ

IPC: C07D239/553 ,  C07D239/557

Abstract: A new intermediate is useful in the synthesis of elagolix. A process for obtaining the intermediate includes reacting a precursor with iodine monochloride in the presence of an organic solvent. A process for preparing elagolix makes use of the intermediate. The intermediate can be 3-((R)-2-(amino-2-phenylethyl)-1-(2-fluoro-6-trifluoromethylbenzyl)-5-iodo-6-methyl-1H-pyrimidine-2,4-dione or a salt thereof, such as a hydrochloride.

公开(公告)号：US20220402923A1

公开(公告)日：2022-12-22

申请号：US17627275

申请日：2020-07-21

Applicant: MOEHS IBERICA S.L.

Inventor： Carles SÁNCHEZ CASALS ,  Alicia DOBARRO RODRÍGUEZ ,  Sergio CARNEADO MORENO

IPC: C07D487/04

Abstract: The present invention relates to a lyophilization method for obtaining amorphous remimazolam besylate without contamination of crystalline material of said product.

公开(公告)号：US11325911B2

公开(公告)日：2022-05-10

申请号：US16754821

申请日：2018-10-11

Applicant: MOEHS IBERICA, S.L.

Inventor： Carles Sánchez Casals ,  Alicia Dobarro Rodríguez

IPC: C07D487/04 ,  A61P25/20 ,  C07D401/04 ,  C07D413/14

Abstract: The present invention relates to a method for preparing 3-[(4S)-8-bromo-1-methyl-6-(pyridin-2-yl)-4H-imidazo[1,2-a] [1,4]benzodiazepin-4-yl]-propionic acid methyl ester starting from 3-[(3S)-7-bromo-2-oxo-5-(pyridin-2-yl)-2,3-dihydro-1H-[1,4]-benzodiazepin-3-yl] propionic acid methyl ester, and novel compounds useful as intermediates in said method, i.e., (3S)-3-[7-bromo-2-(2,2-dimethoxypropylamino)-5-pyridin-2-yl-3H-benzo[e] [1,4]diazepin-3-yl]propionic acid methyl ester.

公开(公告)号：US11858901B2

公开(公告)日：2024-01-02

申请号：US17755412

申请日：2020-03-10

Applicant: MOEHS IBERICA, S.L.

Inventor： Roberto Ballette ,  Oscar Jiménez Alonso ,  Elena García García ,  Alicia Dobarro Rodríguez

IPC: C07D239/553 ,  C07D239/557

CPC classification number: C07D239/553 ,  C07D239/557

Abstract: A new intermediate is useful in the synthesis of elagolix. A process for obtaining the intermediate includes reacting a precursor with iodine monochloride in the presence of an organic solvent. A process for preparing elagolix makes use of the intermediate. The intermediate can be 3-((R)-2-(amino-2-phenylethyl)-1-(2-fluoro-6-trifluoromethylbenzyl)-5-iodo-6-methyl-1H-pyrimidine-2,4-dione or a salt thereof, such as a hydrochloride.

公开(公告)号：US20230092143A1

公开(公告)日：2023-03-23

申请号：US17814815

申请日：2022-07-25

Applicant: MOEHS IBERICA, S.L.

Inventor： Abdeslam AKHATOU ,  Alicia DOBARRO RODRÍGUEZ

IPC: C07D401/12 ,  C07C201/14 ,  C07D239/34 ,  C07D239/36

Abstract: A method is for the synthesis of 2,4-dimethylpyrimidin-5-ol, which can be used as an intermediate compound in the synthesis of Lemborexant. The method includes reacting a nitrophenyl compound with N,N-dimethylformamide diethyl acetal.

公开(公告)号：US11236064B2

公开(公告)日：2022-02-01

申请号：US16634448

申请日：2018-07-27

Applicant: Moehs Iberica S.L.

Inventor： Carles Sánchez Casals ,  Alicia Dobarro Rodríguez

IPC: C07D401/04 ,  C07D213/50 ,  C07D487/04

Abstract: The present disclosure relates to a method for preparing 3-[(3S)-7-bromo-2-oxo-5-(pyridin-2-yl)-2,3-dihydro-1H-[1,4]-benzodiazepin-3-yl] propionic acid methyl ester from (2-amino-5-bromo-phenyl)-pyridin-2-yl-methanone. Also disclosed are compounds useful as intermediates in the method, methyl (4S)-4-amino-5-[4-bromo-2-(pyridin-2-carbonyl)anilino]-5-oxo-pentanoate hydrobromide salt and methyl (4S)-4-(benzyloxycarbonylamino)-5-[4-bromo-2-(pyridin-2-carbonyl)anilino]-5-oxo-pentanoate.

公开(公告)号：US20240391878A1

公开(公告)日：2024-11-28

申请号：US18657572

申请日：2024-05-07

Applicant: MOEHS IBERICA, S.L.

Inventor： Ronnie Andrés MIRANDA ,  Albert COROMINAS ,  Isabel LLOVERAS ,  Juan Pablo BAYÓN RUEDA

IPC: C07D233/60 ,  B01J31/22 ,  C07D233/58

Abstract: A method is for preparing dexmedetomidine ((S)-4-(1-(2,3-dimethylphenyl)ethyl)-1H-imidazole) or a pharmaceutically acceptable salt and/or solvate thereof via the asymmetric hydrogenation of a methylene derivative. Methods for preparing tert-butyl (S)-4-(1-(2,3-dimethylphenyl)ethyl)-1H-imidazole-1-carboxylate or a pharmaceutically acceptable salt and/or solvate thereof are vuseful in the preparation of dexmedetomidine or its salts. The catalyst can be rhodium (I) bis(2,5-norbornadiene)tetrafluoroborate (IVa) in the method.

公开(公告)号：US11891375B2

公开(公告)日：2024-02-06

申请号：US17814815

申请日：2022-07-25

Applicant: MOEHS IBERICA, S.L.

Inventor： Abdeslam Akhatou ,  Alicia Dobarro Rodríguez

IPC: C07D401/12 ,  C07C201/14 ,  C07D239/34 ,  C07D239/36

CPC classification number: C07D401/12 ,  C07C201/14 ,  C07D239/34 ,  C07D239/36 ,  C07B2200/13

Abstract: A method is for the synthesis of 2,4-dimethylpyrimidin-5-ol, which can be used as an intermediate compound in the synthesis of Lemborexant. The method includes reacting a nitrophenyl compound with N,N-dimethylformamide diethyl acetal.

公开(公告)号：US20210139452A1

公开(公告)日：2021-05-13

申请号：US16634448

申请日：2018-07-27

Applicant: Moehs Iberica S.L.

Inventor： Carles Sánchez Casals ,  Alicia Dobarro Rodríguez

IPC: C07D401/04 ,  C07D487/04 ,  C07D213/50

Abstract: The present disclosure relates to a method for preparing 3-[(3S)-7-bromo-2-oxo-5-(pyridin-2-yl)-2,3-dihydro-1H-[1,4]-benzodiazepin-3-yl] propionic acid methyl ester from (2-amino-5-bromo-phenyl)-pyridin-2-yl-methanone. Also disclosed are compounds useful as intermediates in the method, methyl (4S)-4-amino-5-[4-bromo-2-(pyridin-2-carbonyl)anilino]-5-oxo-pentanoate hydrobromide salt and methyl (4S)-4-(benzyloxycarbonylamino)-5-[4-bromo-2-(pyridin-2-carbonyl)anilino]-5-oxo-pentanoate.