FIELD: pharmaceutics.
SUBSTANCE: invention relates to novel crystalline anhydrous modification 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 (lapatinib ditosylate monohydrate), in particular γ-modification, characterized by certain set of diffraction maxima (d, Å) and their intensity (Irelative, %) and certain thermal effects and their temperatures on curve of differential scanning calorimetry, as well as to method of its production and use in pharmaceutical compositions as reversible selective inhibitor of intracellular tyrosine kinase receptor of epidermal growth factor for treating advanced and/or metastatic breast cancer.
EFFECT: increased biological activity.
4 cl, 5 dwg, 3 tbl, 4 ex
Title |
Year |
Author |
Number |
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 |
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 |
CRYSTALLINE ANHYDROUS γ-MODIFICATION OF 4-(3'-CHLOR-4'-FLUORANILINO)-7-METHOXY-6-(3-MORPHOLINOPROPOXY)QUINAZOLINE, METHOD FOR PRODUCING IT AND BASED PHARMACEUTICAL COMPOSITION |
2014 |
- Malin Aleksandr Aleksandrovich
- Mikhajlov Oleg Rostislavovich
- Uvarov Nikolaj Aleksandrovich
|
RU2577518C2 |
CRYSTALLINE β-MODIFICATION OF N-(3-ETHYLPHENYL)-6,7-BIS(2 METHOXYETHOXY)QUINAZOLINE-4-AMINE HYDROCHLORIDE, METHOD FOR PRODUCTION THEREOF AND PHARMACEUTICAL COMPOSITION BASED THEREON |
2015 |
- Mikhajlov Oleg Rostislavovich
- Uvarov Nikolaj Aleksandrovich
- Malin Aleksandr Aleksandrovich
|
RU2610337C1 |
PHARMACEUTICAL COMPOSITION CONTAINING N-[3-CHLOR-4-[(3-FLUOROPHENYL)METHOXY]PHENYL]-6-[5[[[2-(METHYLSULPHONYL)ETHYL]AMINO]METHYL]-2-FURYL]-4-QUINAZOLINAMINE |
2009 |
- Katrin Rimkus
- Frank Muskulus
- Zandra Brjuk
- Jana Pehtts
|
RU2548757C2 |
CRYSTALLINE γ-MODIFICATION (1α,2β,4β,5α,7β)-7-[(HYDROXYDI-2-THIENYLACETYL)OXY]-9,9-DIMETHYL-3-OXA-9-AZONIATRICYCLO[3,3,1,0]NONANE BROMIDE MONOHYDRATE, METHOD OF THEREOF OBTAINING AND THEREOF-BASED PHARMACEUTICAL COMPOSITION |
2015 |
- Mikhajlov Oleg Rostislavovich
- Uvarov Nikolaj Aleksandrovich
- Malin Aleksandr Aleksandrovich
|
RU2567539C1 |
CRYSTALLINE β-MODIFICATION OF 3-(4-AMINO-1-OXO-1,3-DIHYDRO-2H-ISOINDOL-2-YL)-PIPERIDINE-2,6-DIONE, METHOD OF ITS PRODUCTION AND PHARMACEUTICAL COMPOSITION BASED THEREON |
2016 |
- Mikhajlov Oleg Rostislavovich
- Uvarov Nikolaj Aleksandrovich
- Malin Aleksandr Aleksandrovich
|
RU2616976C1 |
CRYSTALLINE ε-MODIFICATION OF N-[2-(DIETHYLAMINO)ETHYL]-5-[(Z)-(5-FLUOR-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE)METHYL]-2,4-DIMETHYL-1H-PYRROL-3-CARBOXAMIDE MALATE, METHOD FOR PRODUCING SAME AND BASED PHARMACEUTICAL COMPOSITION |
2014 |
- Malin Aleksandr Aleksandrovich
- Mikhajlov Oleg Rostislavovich
- Uvarov Nikolaj Aleksandrovich
|
RU2567535C1 |
METHOD OF CANCER TREATMENT |
2005 |
- Berger Mark S.
- Dzhilmer Tona Morgan
- Pandite Arundati Nirmalini
|
RU2361589C2 |