Show metadata Hide metadata

(19)

(11)

2 456 280

(13)

(51)

IPC

C07D401/14(2006-01-01)

A61K31/506(2006-01-01)

A61P35/02(2006-01-01)

(21) (22)

Application

2010135782/04, 2010-08-27

(24)

Start date

2010-08-27

(22)

Actual filing date

2010-08-27

(45)

Published

2012-07-20

(72)

Inventor

Ivanov Andrej SergeevichSavost'Janov Sergej VladimirovichShishkov Sergej Viktorovich

(73)

Holder

Obshchestvo S Ogranichennoj Otvetstvennost'Ju

CRYSTALLINE (-MODIFICATION OF 4-[(4-METHYL-1-PIPERAZINYL)METHYL]-N-[4-METHYL-3-[[4-(3-PYRIDINYL)-2-PYRIMIDINYL]-AMINO]-PHENYL] BENZAMIDE METHANESULPHONATE, METHOD FOR PREPARING IT AND BASED PHARMACEUTICAL COMPOSITION Russian patent published in 2012 - IPC C07D401/14 A61K31/506 A61P35/02

Abstract RU 2456280 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a new crystalline η-modification of 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]-amino]-phenyl]benzamide methanesulphonate (having the international nonproprietary name imanitib mesylate), to a method for preparing it and a based pharmaceutical composition. The new modification may be used in pharmaceutical industry and medicine as an antileukemic cytostatic preparation for therapy of cancer. The new crystalline η-modification of imanitib mesylate is characterized by an individual unique set of planar distances (d, Ǻ) and related intensities (l_oτ, %) specified in the patent claim; as well as an endothermic melting effect equal to - (29.9±0.4) J/g at temperature (218.6±0.5)°C and IR-spectra within the ranges 450 to 4000 cm^-1 and 5300 to 14000 cm^-1. The method for preparing the η-modification of imanitib mesylate consists in the fact that an aqueous solution of imanitib mesylate is frozen in a liquid nitrogen medium at rate min. 80 degrees/min that is followed by sublimation dehydration for 22-27 hours.

EFFECT: preparing the new antileukemic cytostatic preparation for therapy of cancer.

3 cl, 8 dwg, 4 ex

Similar patents RU2456280C2

Title	Year	Author	Number
ROENTGEN-AMORPHOUS WATER-FREE MODIFICATION OF 4-[(4-METHYL-1-PIPERAZINYL)METHYL]-N-[4-METHYL-3-[[4-(3-PYRIDINYL)-2-PYRIMIDINYL]-AMINO]-PHENYL]BENZAMIDE OF METHANE SULFONATE AND METHOD OF OBTAINING IT	2008	Shabatin Vladimir Petrovich Morozov Jurij Nikolaevich Sergeev Gleb Borisovich	RU2365587C1
NANOSIZE WEAKLY CRYSTALLINE MODIFICATION OF 4-METHYL-N-[3-(4-METHYLIMIDAZOL-1-YL)-5-(TRIFLUOROMETHYL)PHENYL]-3-[(4-PYRIDIN-3-YLPYRIMIDIN-2-YL)AMINO]BENAZAMIDE HYDROCHLORIDE MONOHYDRATE, METHOD FOR PRODUCTION THEREOF AND PHARMACEUTICAL COMPOSITION BASED THEREON	2013	Malin Aleksandr Aleksandrovich Mikhajlov Oleg Rostislavovich Uvarov Nikolaj Aleksandrovich	RU2551359C1
SALT FORMS OF 4-(4-METHYLPIPERAZINE-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDINE-3-YL)PYRIMIDINE-2-YLAMINO)PHENYL]-BENZAMIDE	2005	Bjurger Khans Mikhaehl' Manli Pol Uill'Jam Mutts Mikhaehl'	RU2375355C2
CRYSTALLINE β-MODIFICATION OF 4-[4-({[4-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]CARBAMOYL}AMINO)PHENOXY]-N-METHYL-PYRIDINE-2-CARBOXAMIDE OF p-TOLUENE SULPHONATE, METHOD FOR PRODUCTION THEREOF AND PHARMACEUTICAL COMPOSITION BASED THEREON	2015	Mikhajlov Oleg Rostislavovich Uvarov Nikolaj Aleksandrovich Malin Aleksandr Aleksandrovich	RU2568638C1
CRYSTAL ANHYDROUS DELTA MODIFICATION OF N-(2-CHLORINE-6-METHYLPHENYLDIAZOMETHANE)-2-[6-[4-(2-HYDROXYETHYL)-1-PIPERAZINYL]-2-METHYL-4-PIRIMIDINYL]AMINO]-5-THIAZOLCARBOXAMIDE, METHOD OF ITS PRODUCTION AND PHARMACEUTICAL COMPOSITION BASED ON IT	2014	Malin Aleksandr Aleksandrovich Mikhajlov Oleg Rostislavovich Uvarov Nikolaj Aleksandrovich	RU2567537C1
SALTS OF 4-METHYL-N-[3-(4-METHYLIMIDAZOLE-1-YL)-5-TRIFLUOROMETHYLPHENYL]-3-(4-PYRIDINE-3-YLPYRIMIDINE-2-YLAMINO)BENZAMIDE	2013	Manli Pol U. Shi Venchun Satton Pol Allen Karpinski Peter Kh. Vu Rain Monne Stefani Brotsio Jerg	RU2605551C2
4-METHYL-N-[3-(4-METHYLIMIDAZOL-1-YL)-5-TRIFLUOROMETHYLPHENYL]-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)BENZAMIDE SALTS	2006	Manli Pol U. Shi Vehn'Chun Satton Pol Allen Karpinski Petr Kh. Vu Rain Monn'E Stefani Brotsio Jerg	RU2483065C2
4-METHYL-[3-(4-METHYLIMIDAZOL-1-YL)-5-TRIFLUOROMETHYLPHENYL]-3-(4-PYRIDIN-3-YLPYRIMIDIN-2-YLAMINO)BENZAMIDE SALTS	2006	Manli Pol U. Shi Vehn'Chun Satton Pol Allen Karpinski Petr Kh. Vu Rain Monn'E Stefani Brotsio Jerg	RU2434864C2
CRYSTALLINE γ-MODIFICATION OF N-{3-CHLORO-4-[(3-FLUOROBENZYL)OXY]PHENYL}-6-[5-({[2-(METHYLSULFONYL)ETHYL]AMINO}METHYL)-2-FURYL]-4-QUINOLINE AMINE OF BIS (4-METHYLBENZENESULFONATE) MONOHYDRATE, METHOD OF ITS PRODUCTION AND PHARMACEUTICAL COMPOSITION BASED THEREON	2016	Mikhajlov Oleg Rostislavovich Uvarov Nikolaj Aleksandrovich Malin Aleksandr Aleksandrovich	RU2603943C1
NOVEL CRYSTALLINE SALT FORM 3-(1,2,4-TRIAZOLO[4,3-A]PYRIDIN-3-YLETHYNYL)-4-METHYL-N-(4-((4-METHYLPIPERAZIN-1-YL)METHYL)-3-TRIFLUOROMETHYLPHENYL) BENZAMIDE FOR MEDICAL APPLICATION	2016	Chilov Germes Grigorevich Titov Ilya Yurevich	RU2652992C2

RU 2 456 280 C2

Authors

Ivanov Andrej Sergeevich

Savost'Janov Sergej Vladimirovich

Shishkov Sergej Viktorovich

Dates

2012-07-20—Published

2010-08-27—Filed