FIELD: medicine, pharmaceutics.
SUBSTANCE: present invention refers to purified polymorph IV of a compound of formula Ia characterised by X-ray powder diffraction (XRPD) peaks at 3.8, 7.5, 16.1, 16.5 and 17.1 degrees 2θ (±0.1) derived by X-ray copper K-alpha1-radiation (wave length is equal to 1.5406 angstroms). Besides, the invention refers to two methods of producing said polymorph IV. The first one involve exposure of polymorph II of the compound of formula Ia to at least two heating and cooling cycles within the temperature range 5 to 50°C in the presence of a medium selected from diisopropyl ester and C5-C7alkane or -alkene where said Polymorph II of the compound of formula Ia is characterised by XRPD peaks at 3.5, 6.9, 9.2, 10.4 and 18.0 degrees 20 (±0.1) derived by X-ray copper K-alpha1-radiation (wave length is equal to 1.5406 angstroms). The second method involves making an ethyl acetate solution of the compound of formula 1a where the water content makes less than 3.6 % vol./vol., and adding C5-C7alkane or -alkene to this solution at temperature 20 to 36°C.
EFFECT: preparation of a solid pharmaceutical composition of polymorph IV showing motiline agonist activity, and also developing a method of treating a disturbed gastric molitity by means of polymorph IV.
13 cl, 2 tbl, 23 dwg, 7 ex
Title |
Year |
Author |
Number |
SALTS AND POLYMORPHS OF SUBSTITUTED IMIDAZOPYRIDINYL-AMINOPYRIDINE |
2015 |
- Bates, Craig
- Mao, Jianmin
- Reed, David
|
RU2732125C2 |
POLYMORPHS OF 2-(4-(2-(1-ISOPROPYL-3-METHYL-1H-1,2,4-TRIAZOL-5-YL)-5,6-DIHYDROBENZO[F]IMIDAZO[1,2-D][1,4]OXAZEPIN-9-YL)-1H-PYRAZOL-1-YL)-2-METHYLPROPANAMIDE, METHODS OF PRODUCTION AND PHARMACEUTICAL USES THEREOF |
2014 |
|
RU2658009C2 |
CRYSTALLINE FORMS OF 3-[5-(2-FLUOROPHENYL)-[1,2,4]OXADIAZOL-3-YL]BENZOIC ACID, AND USE THEREOF AND METHODS FOR PREPARING |
2007 |
- Al'Msted Nil G.
- Khvang Piter Seongvoo
- Moon Joung-Choon
|
RU2474577C2 |
METHODS OF PRODUCTION ISOQUINOLINONES AND SOLID FORMS ISOQUINOLINONES |
2012 |
- Zhen Pinda
- Martin Majkl
- Izbester Pol
- Lejn Bendzhamin S.
- Kropp Dzhejson
|
RU2626883C2 |
POLYMORPHOUS AND AMORPHOUS FORMS OF {2-FLUORINE-5-[3-((E)-2-PYRIDINE-2-ILVINYL)-1N-INDAZOLE-6-ILAMINE]PHENYL}AMIDE 2, 5-DIMETHYL-2N-PYRAZOLE-3-CARBONIC ACID |
2005 |
- E Tsjan'
- Zuk Skott Ehdvard
- Oullet Majkl Allen
- Khettinger Donald Nikolas
- Srirangam Dzhajaram Kasturi
- Kanija Robert Stiven
- Saeed Nabil' Lauze
- Uajtlin Mehtt'Ju Dehvid
- Mitchell Mark Brajan
|
RU2324692C1 |
POLYMORPHOUS AND AMORPHOUS FORMS OF (R)-2-HYDROXY-2-METHYL-4-(2,4,5-TRIMETHYL-3,6-DIOXOCYCLOHEXA-1,4-DIENYL)BUTANAMIDE |
2015 |
- Mollard Pol
- Kornel Kristofer R.
- Vesson Kiron E.
- Dzhannusis Piter
- Sachit Shazad
- Mirmekhrabi Makhmud
|
RU2770091C2 |
ROMIDEPSIN SOLID FORMS AND USE THEREOF |
2011 |
- Vrolijk Nikolas
- Khanko Dzhejson
- Endzhers Devid Alan
- Khejdzhen Erik
- Smolenskaya Valeriya
- Stalts Dzheffri Skott
- Naringrekar Vidzhaj Kharishchandra
- Pejkov Viktor Tsatchev
- Foss Villard Rodni
- Darling Nil Lourens
|
RU2607634C2 |
CRYSTALLINE FORM (S)-N-(5-((R)-2-(2,5-DIFLUOROPHENYL)-PYRROLIDIN-1-YL)-PYRAZOLO[1,5-A]PYRIMIDIN-3-YL)-3-HYDROXYPYRROLIDINE-1-CARBOXAMIDE HYDROSULPHATE |
2015 |
- Errigo Alisha B.
- Dzhuengst Derrik
- Shakh Khalid
|
RU2723990C2 |
3-[1,2,3,6-TETRAHYDROPYRIDIN-2-YL]PYRIDINE GLUTARATE OR PHARMACEUTICALLY ACCEPTABLE SOLVATE THEREOF |
2019 |
|
RU2823979C2 |
NOVEL SOLID FORMS (2S,3S,4S,5R,6S)-3,4,5-TRIHYDROXY-6-(((4AR,10AR)-7-HYDROXY-1-PROPYL-1,2,3,4,4A,5,10,10A-OCTAHYDROBENZO[G]QUINOLIN-6-YL)OXY)TETRAHYDRO-2H-PYRAN-2-CARBOXYLIC ACID |
2020 |
- Jensen, Klaus, Gervig
- Jorgensen, Morten
- Dzhukhl, Martin
- Kvaerno, Lisbet
- De Diego, Khejdi, Lopez
- Fredkholt, Karin
- Terkelsen, Frans Dennis
- Frikhed, Tobias Gilling
- Yakobsen, Mikkel Fog
|
RU2820501C2 |