公开(公告)号：US20200239477A1

公开(公告)日：2020-07-30

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 ,  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：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.

公开(公告)号：WO2019020790A1

公开(公告)日：2019-01-31

申请号：PCT/EP2018/070414

申请日：2018-07-27

Applicant: MOEHS IBERICA S.L.

Inventor： SÁNCHEZ CASALS, Carles ,  DOBARRO RODRÍGUEZ, Alicia

IPC: C07D401/04 ,  C07D487/04 ,  C07D213/56

Abstract: The present invention relates to a method for preparing 3-[(3S)-7- bromo-2-oxo-5-(pyridin-2-yl)-2,3-dihydro-IH-[l,4]-benzodiazepin-3-yl] propionic acid methyl ester from (2-amino-5-bromo-phenyl)-pyridin-2- yl-methanone. The present invention also relates to new compounds useful as intermediates in that 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：WO2021013826A1

公开(公告)日：2021-01-28

申请号：PCT/EP2020/070528

申请日：2020-07-21

Applicant: MOEHS IBERICA, S.L.

Inventor： SÁNCHEZ CASALS, Carles ,  DOBARRO RODRÍGUEZ, Alicia

IPC: C07D487/04 ,  A61K31/5517

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：WO2020169643A1

公开(公告)日：2020-08-27

申请号：PCT/EP2020/054308

申请日：2020-02-19

Applicant: MOEHS IBERICA, S.L.

Inventor： BERNABEU MARTÍNEZ, María del Carmen ,  JIMÉNEZ ALONSO, Oscar ,  DOBARRO RODRÍGUEZ, Alicia

IPC: C07J9/00 ,  C07J17/00 ,  C07J51/00

Abstract: The present invention relates to the diethylamine salt of 3a- tetrahydropyranyloxy-6a-ethyl-7a-hydroxy-53-cholanic acid (I), which is a new intermediate in the synthesis of obeticholic acid, to the use of said diethylamine salt in the synthesis of said obeticholic acid, as well as to the method of obtaining this new salt.

公开(公告)号：WO2021001350A1

公开(公告)日：2021-01-07

申请号：PCT/EP2020/068358

申请日：2020-06-30

Applicant: MOEHS IBERICA, S.L.

Inventor： ARE, Celeste ,  SÁNCHEZ CASALS, Carles ,  DOBARRO RODRÍGUEZ, Alicia

IPC: C07D401/06 ,  A61K31/444 ,  A61P25/06

Abstract: The present invention relates to a new intermediate, (2,2-dimethyl-N-[6-(1-methyl-piperidin-4-carbonyl)-pyridin-2-yl]-propanamide) useful in the synthesis of lasmiditan, to a method for obtaining same, to the use of said intermediate for preparing lasmiditan, to a method for preparing lasmiditan making use of said intermediate, and to a method for preparing an intermediate ((6-amino-pyridin-2-yl)-(1-methyl-piperidin-4-yl)-methanone) from (2,2-dimethyl-N-[6-(1-methyl-piperidin-4-carbonyl)-pyridin-2-yl]-propanamide).

公开(公告)号：WO2019158550A1

公开(公告)日：2019-08-22

申请号：PCT/EP2019/053484

申请日：2019-02-13

Applicant: MOEHS IBERICA, S.L.

Inventor： GARCÍA GARCÍA, Elena ,  DOBARRO RODRÍGUEZ, Alicia

IPC: C07D213/75 ,  C07D513/04

Abstract: The present invention relates to a method for preparing tert-butyl N- ((1R,2S,5S)-2-((2-((5-chloropyridin-2-yl)amino)-2-oxoacetyl)amino) -5-(dimethylcarbamoyl)cyclohexyl)carbamate of formula (I), or a salt or solvate thereof,characterized in that it comprises the steps of a) mixing tert-butyl N-((1R,2S,5S)-2-amino-5-(dimethylcarbamoyl) cyclohexyl)carbamate of formula (A) with ethyl 2-((5-chloropyridin-2- yl)amino)-2-oxoacetate of formula (B) in an organic solvent; b) mixing a base with the resulting mixture of step (a); and c) stirring the mixture obtained in step (b). The method substantially facilitates the obtention of the compound of formula (I), leading to a reduction in the viscosity of the reaction medium and improving product yield and/or product purity. Formulae (I), (B), (A).

公开(公告)号：WO2013128000A1

公开(公告)日：2013-09-06

申请号：PCT/EP2013/054164

申请日：2013-03-01

Applicant: MOEHS IBERICA S.L.

Inventor： BERNABEU MARTÍNEZ, María del Carmen ,  DOBARRO RODRÍGUEZ, Alicia ,  GALÁN RODRÍGUEZ, Cristobal

IPC: C07D487/04 ,  A61K31/4985 ,  A61P3/08

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: The present invention relates to a novel crystalline form of sitagliptin sulfate, to a method for obtaining it, to pharmaceutical compositions comprising the novel crystalline form and to said crystalline form for use as a medicament.

Abstract translation: 本发明涉及硫酸西他列霉的新型结晶形式，其获得方法为包含新型结晶形式和所述结晶形式用作药物的药物组合物。