WO/2016/116075 METHOD OF ISOLATION OF A MIXTURE OF ENANTIOMERS OF 1-(6-BROMO-2-METHOXYQUINOLIN-3-YL)-4-(DIMETHYLAMINO)-2-(NAPHTHALEN-1-YL)-1-PHENYLBUTAN-2-OL||WO||28.07.2016|
||PCT/CZ2016/000005||ZENTIVA, K.S.||LUSTIG, Petr|
A method of isolation of the E1 and E2 optical isomers, forming an enantiomeric mixture, from a mixture of four optical isomers E1, E2, E3, E4, wherein the enantiomeric mixture of E3 and E4 is first separated from the solution and subsequently the mixture of E1 and E2 is isolated in the form of a base in the mother liquors, wherein E1 is (1R,2S)-1-(6-bromo-2-memoxyqumolm-3-yl)-4-(dimethylamino)-2- (naphthalen-1-yl)-1-phenylbutan-2-ol, E2 is the (1S,2R)-enantiomer of the same compound, and E3 and E4 are the (1R,2R) and (1S,2S) enantiomers, respectively.
WO/2016/116076 NEW POSSIBILITIES OF CHIRAL RESOLUTION OF BEDAQUILINE||WO||28.07.2016|
||PCT/CZ2016/000006||ZENTIVA, K.S.||STEFKO, Martin|
A method of performing isolation and purification of bedaquiline (la) from a mixture of stereoisomers of 6-bromo-2-methoxy-quinolin-3 -yl)-4-dimethylamino-2-( 1 -naphthyl)- 1 - phenyl-butan-2-ol identified as I-rac, being a mixture of the stereoisomers of formulae la, lb, and Il-rac, being a mixture of the stereoisomers of formulae Ila, lib, with any ratio of individual constituents of the mixture, wherein said mixture is dissolved together with derivatives of N-benzoyl-L-aspartic acid Ilia, wherein R1 and R2 independently stand for hydrogen, a primary, secondary or tertiary C1-C4 alkyl, a primary or secondary amide, wherein always at least one of the R1 or R2 symbols stands for hydrogen; and R3 is a C5-C12 aryl, C5-C12 heteroaryl with one or more heteroatoms, which may be further substituted by a halogen, amino group, carbonyl, or carboxyl, or its functional derivative, preferably phenyl, naphthyl, tolyl, or mesytyl, and the resulting salt is recrystallized from a suitable solvent or mixture, which can be ketones, esters, ethers, amides, nitriles or organic acids, alcohols, aliphatic and aromatic hydrocarbons, chlorinated hydrocarbons, water and/or their mixtures.
WO/2016/116077 POLYMER-STABILIZED AMORPHOUS FORMS OF VORTIOXETINE||WO||28.07.2016|
||PCT/CZ2016/000008||ZENTIVA, K.S.||ZVATORA, Pavel|
The present invention relates to an amorphous mixture of vortioxetine of formula I or its hydrobromide salt with a polymer, characterized in that the polymer is selected from derivatives of polyacrylates, polymethacrylates, cellulose or polyvinyls. Also included is a method of preparing said amorphous mixture, comprising dissolution of vortioxetine in the base form or in the hydrobromide salt form and a suitable polymer in a suitable organic solvent, and subsequent removal of the solvent to produce an amorphous mixture. Another method consists in mixing vortioxetine in the base form or in the hydrobromide salt form with a suitable polymer, and subsequent heating of this mixture to produce a melt and than an amorphous mixture.
WO/2016/116073 CHIRAL RESOLUTION OF BEDAQUILINE BY USING CYCLCIC PHOSPHORIC ACIDS||WO||28.07.2016|
||PCT/CZ2016/000003||ZENTIVA, K.S.||ZVATORA, Pavel|
A method of performing isolation and purification of bedaquiline (la) from a mixture of stereoisomers of 6-bromo-2-methoxy-quinolin-3-yl)-4-dimethylamino-2-(l-naphthyl)-l- phenyl-butan-2-ol identified as I-rac, being a mixture of the stereoisomers of formulae la, lb, and II-rac, being a mixture of the stereoisomers of formulae Ila, lib, with any ratio of individual constituents of the mixture, wherein said mixture is dissolved together with derivatives of 1,3 -propanediol hydrogen phosphate of formula IV, wherein R1, R2, and R3 independently stand for hydrogen, a halogen, C1-C6 alkyl, aryl, naphthyl, phenyl and preferably a halogenated phenyl or phenyl substituted in any way, and the resulting salt is crystallized.
WO/2016/116078 METHOD OF THREE-DIMENSIONAL SCANNING USING FLUORESCENCE INDUCED BY ELECTROMAGNETIC RADIATION AND A DEVICE FOR EXECUTING THIS METHOD||WO||28.07.2016|
||PCT/CZ2016/000009||PIXEL R&D S.R.O.||UHER, Josef|
For volumetric analysis of the elemental composition of a measured sample (3) the method of three-dimensional scanning is executing using fluorescence induced by electromagnetic radiation, in which the primary beam (1) of electromagnetic radiation is flattened and is directed at the measured sample (3) in which it irradiates the measured area (6). From the measured area (6) there exits fluorescence radiation, which is almost completely shielded by the shielding means (7) to a secondary beam (9), which is released towards the shielded detector (4) through the permeable area (8) formed in the shielding means (7). The secondary beam (9) projects the image of the measured area (6) onto the shielded detector (4), which records the data of the measured area (6) and subsequently uses the data to obtain an elemental composition of the measured sample (3), including the distribution of concentration of elements in the sample volume.
WO/2016/116072 METHOD OF PREPARATION OF BARLEY WITH AN INCREASED DROUGHT RESISTANCE||WO||28.07.2016|
||PCT/CZ2015/000005||UNIVERZITA PALACKEHO V OLOMOUCI||POSPISILOVA, Hana|
The invention provides a method of preparation of barley plants resistant to drought, wherein a nucleotide sequence is inserted into the barley genome, said nucleotide sequence containing a sequence with at least 80% identity to the sequence of the gene AtCKX1 from the plant Arabidopsis thaliana. The invention further provides an expression cassette which contains promoter-AtCKX1-terminator, and use of this expression cassette for the preparation of barley plants showing resistance to drought.
WO/2016/116074 A METHOD OF PRODUCING HIGHLY PURE RILPIVIRINE AND ITS SALTS||WO||28.07.2016|
||PCT/CZ2016/000004||ZENTIVA, K.S.||HAJICEK, Josef|
A method of preparing Rilpivirine of formula I, or a suitable salt thereof, comprising a reaction of a hydrogen halide of the aniline derivative of formula II with chloropyrimidine of formula III in methyl isobutyl ketone and in the presence of a polar additive.
WO/2016/112882 MACROMOLECULAR CONJUGATES FOR ISOLATION, IMMOBILIZATION AND VISUALIZATION OF PROTEINS||WO||21.07.2016|
||PCT/CZ2016/050002||USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I.||SACHA, Pavel|
Macromolecular conjugates for isolation, immobilization and visualization of proteins The invention provides a synthetic macromolecular conjugate for selective interaction with proteins, comprising a synthetic copolymer, and at least one binding group and at least one further group selected from an affinity tag and an imaging probe, said at least one binding group and at least one further group being bound via covalent bond to said synthetic copolymer. The macromolecular conjugate is suitable in particular for identification, visualization, quantification or isolation of proteins and/or cells. HPMA copolymer, i.e.poly(HPMA-co-Ma-β-Ala-TT), a copolymer prepared by conventional solution radical polymerization or controlled radical copolymerization (e.g. RAFT copolymerization, reversible addition-fragmentation chain-transfer) of N-(2- hydroxypropyl)methacrylamide (HPMA) and 3-(3-methacrylamidopropanoyl)thiazolidine-2-thione (Ma-P-Ala-TT) can be preferably used as the basic copolymer.
WO/2016/112878 ELECTRONIC GERMICIDAL DEVICE||WO||21.07.2016|
||PCT/CZ2015/000002||ČERMÁK, Mojmír||ČERMÁK, Mojmír|
In the electronic germicidal device comprising a source of pulsed voltage and a pair of electrodes to be applied on the treated tissue the electrodes (8, 9) placed on a plastic film form at least partially a system of parallel or concentric lines with opposite polarity of the neighbouring electrodes (8, 9).
WO/2016/112879 CRYSTALLINE MODIFICATION 2 OF (3/R)-3-AMINO-1-[3-(TRIFLUOROMETHYL)-6,8-DIHYDRO-5H-[1,2,4]TRIAZOLO[4,3-α]PYRAZIN-7-YL]-4-(2,4,5-TRIFLUOROPHENYL)BUTAN-1-ONE L-TARTRATE||WO||21.07.2016|
||PCT/CZ2016/000001||ZENTIVA, K.S.||RICHTER, Jindrich|
Crystalline Modification 2 of Sitagliptin L-tartrate salt, exhibiting the following characteristic diffraction peaks: 5.83; 15.63; 17.73; 25.58; 26.44 ± 0.2° 2-theta. (Formula)