BILASTIN CRYSTALLINE FORMS AND THEIR PRODUCTION METHODS Russian patent published in 2022 - IPC C07D401/04 A61K31/454 A61P37/08 

Abstract RU 2772222 C2

FIELD: organic chemistry.

SUBSTANCE: invention relates to the field of organic chemistry, namely to a method for the production of a hydrated crystalline Eta-form of 4-[2-[4-[1-(2-ethoxyethyl)-1H-benzimidazole-2-yl]-1-piperidinyl)ethyl]-α,α-dimethyl-benzenacetic acid (bilastin). The method includes following stages: i) bilastin is dissolved in a mixture of water and acetonitrile at a temperature from 40 to 70°C; ii) a solution obtained at the stage i) is cooled to a temperature from 25 to 50°C; iii) a crystallization germ in the form of a hydrated crystalline Eta-form is introduced into a solution obtained at the stage ii), and the resulting solution is cooled to a temperature from 0 to 30°C for a time period necessary for crystallization; and iv) a crystalline form obtained at the stage iii) is dried at a reduced pressure at a temperature from 25 to 40°C until the water content is from 3.5 to 4% by weight, which is calculated by the Karl-Fischer method. The hydrated crystalline Eta-form of bilastin has an X-ray diffractogram that includes characteristic peaks at 8.4; 9.6; 12.2; 13.2; 15.1 and 19.2±0.2 degrees 2-theta, measured using an X-ray diffractometer with Cu-Kα radiation (1.5418 Å).

EFFECT: method is developed for the production of a hydrated crystalline Eta-form of bilastin with good physical and mechanical properties, such as stability and compressibility that allow for its easy use for the production of pharmaceutical compositions.

2 cl, 32 dwg, 2 tbl, 10 ex

Similar patents RU2772222C2

Title Year Author Number
CRYSTALLINE FORM AND METHOD OF CLEANING SAME 2011
  • Beljaev Aleksandr
  • Lermont Devid Aleksander
  • Brodbelt Brajan
  • Albert Ekaterina
  • Andres Patrisija
RU2604734C2
POLYMORPH OF (4-HYDROXYCARBAMOYLPHENYL)CARBAMINIC ACID (6-DIETHYLAMINOMETHYL-2-NAPHTHALENYL)METHYL ETHER HYDROCHLORIDE 2010
  • Turketta Stefano
  • Dzenoni Mauritsio
RU2552354C2
CRYSTAL COMPOUNDS 2016
  • Mckinney, Anthony Alexander
  • Bymaster, Franklin
  • Piskorski, Walter
  • Fleitz, Fred J.
  • Yang, Yonglai
  • Engers, David A.
  • Smolenskaya, Valeriya
  • Kusukuntla, Venkat
RU2789672C2
CRYSTALLINE FORMS OF THE TLR7/TLR8 INHIBITOR 2019
  • Bieri, Nicole
  • Kordikowski, Andreas
  • Li, Bin
  • Lustenberger, Philipp
  • Ramos, Rita
  • Sethuraman, Vijay
  • Zhang, Sisi
RU2792005C2
SOLID FORMS OF 3-(5-AMINO-2-METHYL-4-OXO-4H-QUINAZOLIN-3-YL)PIPERIDINE-2,6-DIONE DERIVATIVES AND THEIR PHARMACEUTICAL COMPOSITIONS AND USE 2012
  • Myuller Dzhordzh V.
  • Man Khon-Vakh
  • Koen Bendzhamin M.
  • Li In
  • Syuj Dzhin
  • Leong Uillyam V.
RU2611007C2
POLYMORPHIC FORM OF SODIUM HYODEOXYCHOLATE (NAHDC) AND PREPARATION PROCESS THEREOF 2014
  • Galdi Gianluca
  • Sacco Paolo
  • Ferrari Valeria
RU2669785C2
NOVEL CRYSTALLINE FORMS OF SODIUM SALT OF (4-{4-[5-(6-TRIFLUOROMETHYL-PYRIDIN-3-YLAMINO)PYRIDIN-2-YL]PHENYL}CYCLOHEXYL) ACETIC ACID 2011
RU2612556C2
AMINE SOLVATE OF SODIUM GLUCOSE OPENER OF SODIUM GLUCOSE OPENER AND METHOD FOR PRODUCTION THEREOF AND USE THEREOF 2017
  • Zhang Lei
  • Wang Yuan
RU2710230C1
METHOD OF PRODUCING N-[5-(3,5-DIFTORBENZIL)-1H-INDAZOLE-3-YL]-4-(4-METHYLPIPERAZINE-1-YL)-2-(TETRAHYDROPYRAN-4-YLAMINO)BENZAMIDE 2013
  • Barbudzhan Natale Alvaro
  • Forino Romualdo
  • Orsini Paolo
RU2602071C2
FORM IV OF IVABRADINE HYDROCHLORIDE 2012
  • Prohens Lopez Rafel
  • Puigjaner Vallet Cristina
  • Barbas Canero Rafael
  • Del Rio Pericacho Jose Luis
  • Marti Via Josep
RU2619121C2

RU 2 772 222 C2

Authors

Del Rio Pericacho, Jose Luis

Puigjaner Vallet, Maria Cristina

Prohens Lopez, Rafael

Arredondo Martinez, Yolanda Esther

Dates

2022-05-18Published

2016-07-22Filed