8-cyano-1-cyclopropyl-7-(1s,6s-2,8-diazabicyclo-[4,3,0]-nonane-8-yl)-6- flu oro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid of crystalline modification b and medicinal agent based on thereof eliciting effect against pathogenic microorganisms

FIELD: organic chemistry, medicine.

SUBSTANCE: invention describes 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo-[4.3.0]-nonane-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid of the formula (I):

in the crystalline modification B and a medicinal agent based on thereof that elicits effect against pathogenic microorganisms. Indicated modification of compound of the formula (I) shows stability and insignificant absorption of air moisture ant doesn't convert to another crystalline modification or amorphous form being even in the prolonged storage.

EFFECT: valuable properties of agent.

4 cl, 4 dwg, 6 ex

 

The present invention refers to a crystalline modification 8-cyan-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline-carboxylic acid, more particularly to an 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0] nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-Z-quinoline-carboxylic acid crystalline modification and drug on its basis, with activity against pathogenic bacteria.

8-cyan-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-Z-quinoline-carboxylic acid of the formula (I) will hereinafter be referred to as CCDC.

CCDC is known from DE-A 19 633 805 or WO 97/31001. It is obtained by the reaction of 7-chloro-8-cyan-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinoline-carboxylic acid and (1S,6S)-2,8-diazabicyclo [4.3.0]nonane in a mixture of dimethylformamide and acetonitrile in the presence of a base. After mixing with water CCDC is extracted from water with dichloromethane and by removing the extractant is released. The resulting powder, which is no definite crystalline modification does not show. The powder, on the contrary, for the most part amorphous, and may contain a mixture of different crystalline modifications. If you accidentally get a single crystalline modification, it is not clear how it can be extracted and obtained od of oznacenim way. For the preparation of drugs available, however, the condition that for biologically active substances, which can exist in different crystalline modifications, clearly indicates what kind of crystalline modification of it is used for the production of medicinal substances.

This is partly amorphous powder, method of manufacturing the above was briefly described, in addition, hygroscopic. Amorphous solids, particularly hygroscopic solids, difficult processing in herbal medicines, as they, for example, can detect low bulk density and poor fluidity. In addition, for processing hygroscopic substances require special working tools and devices in order to have reproducible results, for example, in the content of biologically active substances or stability of the produced solid products.

The task of the invention to provide a specific crystalline modification CCDC, which due to their physical properties, in particular properties of crystals, does not show the above-mentioned disadvantages in the manufacture of galenic forms.

The problem is solved by the proposed 8-cyan-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline-carboxylic Ki is lotay (CCDC) of the crystalline modification V, characterized by x-ray-powder diffraction pattern recorded in table reflexes (2θ (2 theta)) high and medium intensity.

Table 1:

X-ray diffractogram of the powder CCDC crystalline modification

2θ (2 theta)

8,91

13,23

14,26

14,40

15,34

17,88

19,70

20,78

21,86

28,13

30.20mm

X-ray diffractogram of the powder CCDC crystalline modifications are also presented in figure 1.

CCDC crystalline modification differs from other forms of CCDC, it is also near future properties. These properties can also be used separately or in conjunction with other parameters to determine the proposed CCDC crystalline modification Century

CCDC crystalline modification differs in that it has a melting point 243-245° With defined using differential thermal analysis (DTA). The characteristic chart DTA presented in figure 2.

CCDC crystal modifications In further differs in that its infrared spectrum, measured in CVG, corresponds to the one given in figure 3.

CCDC crystalline modification differs in that it can be received by one of the following ways. CCDC crystalline modifications To get the reaction of 7-halo-8-cyan-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinoline-carboxylic acid of the formula (I)

where Hal is fluorine or preferably chlorine

and (1S,6S)-2,8-diazabicyclo[4.3.0]nonane of the formula (III)

if necessary in the presence of a base in a mixture of ethanol with a polar aprotic diluent, such as N-organic, dimethylformamide or sulfolane. Or another way is heated CCDC unknown modification with a diluent, such as ethanol, propanol or isopropanol or mixtures of these alcohols with a polar aprotic diluent, such as N-organic, dimethylformamide or sulpholane optionally in the presence of a base, and then the mixture is cooled and CCDC crystal modifications In isolated (separated).

CCDC crystalline modification proved remarkably stable and becomes even during prolonged storage in different crystalline modification or amorphous form. In addition, compared with the amorphous CCDC modification In much less prone to absorb water from the air. For these reasons, it is well suited for the manufacture of tablets and other solid dosage forms. Due to its stability it gives such dosage forms long desired stability during storage. Therefore, the crystalline modification allows a specific and targeted way to make stabilility medicines on the basis of CCDC.

CCDC crystalline modification has an effective activity against pathogenic bacteria in the field of medicine and veterinary medicine. Its wide range of applications corresponds to the range of application of the CCDC.

As grounds upon receipt CCDC crystalline modification In applied primarily tertiary amines, trimethylamine, triethylamine, ethyldiethanolamine (strong base), N-methyl-piperidine, N-ethyl-piperidine, N-propyl-piperidine and N-butyl-piperidine. Most preferably the use of triethylamine and ethyldiethanolamine. 1 mol of compound (II) usually take 1-2 mole of base, preferably of 1.1 to 1.5 mol.

Apply a mixture of ethanol and N-methyl-pyrrolidone, dimethylformamide and sulfolane, and the ratio of ethanol:the polar aprotic solvent is from 0.5:1 to 4:1, preferably from 1:1 to 3:1.

The reaction proceeds at normal pressure or at elevated pressures of from 1 to 100 bar, preferably 1-20 bar.

The reaction proceeds at a temperature between 0 and 200° C, preferably between 20 and 150° C.

1 mol of compound (II) usually take 1-2 moles, preferably 1-1,5 mol of compound (III).

CCDC crystal modifications In precipitates from the reaction mixture and can be filtered. Filtered the solid may optionally be purified by washing with ethanol. The initial product of the formula (II) and (III), used for the production of CCDC known (compare DE-A 19633805).

If CCDC unknown modification heated for several hours in one of the diluents such as ethanol, propanol, isopropanol or mixtures of these alcohols with a polar aprotic diluent, such as N-organic, dimethylformamide or sulfolane, then at room temperature precipitated is filtered off the precipitate, wash it with ethanol and then dried. This method of obtaining preferably used as the Foundation of the triethylamine or ethyldiethanolamine (1 mol CCDC about 0.01 and 0.1 mol of base).

X-ray diffractogram of the powder characteristics CCDC crystalline modification was received on the transmission diffractometer STADI-P sensitive detector PSD2) company STOE.

The melting temperature was obtained by means of DTA instrument DSC 820 company Mettler-Toledo. The heating of the sample CCDC crystalline modifications were made to the air in an aluminum crucible with a speed of 10° K/min IR spectrum was obtained on the instrument FTS 60 A firm Biorad by pressing the sample in KBR.

The following examples illustrate the invention without limiting it. Used in the following examples, the solvents and bases are particularly preferred.

Comparative example

A mixture of 3.07 g of 7-chloro-8-cyan-1-cyclopropyl-6-fluoro-1,4-dihydro-oxo-3-quinoline-carboxylic acid, 1.39 g of (1S,6S)-2,8-diazabicyclo[4.3.0]nonane, 2.24 g of 1,4-diazabicyclo[2.2.2]octane (DABCO), 29.5 ml of dimethylformamide and 29.5 ml of acetonitrile is stirred for 16 hours at room temperature. The reaction mixture is evaporated in a rotary vacuum evaporator at a bath temperature of 60° and the remainder was transferred to 10 ml of water. One stripped off (the result) of the solution was adjusted with diluted hydrochloric acid to pH 7 and the precipitated solid precipitate is filtered off. The filtrate is shaken out three times with dichloromethane, was taken in 20 ml of the Organic phase is dried with sodium sulfate, filtered and the filtrate evaporated on a vacuum rotary evaporator at a temperature of the water bath at 60° C. Obtain 2.4 g of a solid substance in a light brown colour, which is characterized depicted in figure 4 x-ray-diffraction pattern of the powder and in accordance with which it is in the bulk is amorphous.

Obtained according to this method, the solid absorbs at a relative humidity equal to 95% (installed by using a saturated aqueous solution above the sediment Na2HPO4×12H2O) within days 17 wt.% water.

Example 1

To 1012 g of 7-chloro-8-cyan-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinoline-carboxylic acid add a mixture of 3300 ml of ethanol, 1980 ml of N-methylpyrrolidone and 534 g diisopropylethylamine. Heated to education is phlegmy and then added dropwise 459 g (18,68)-2,8-diazabicyclo[4.3.0]nonane. After the addition is stirred for further 3 hours at education phlegmy, then cooled to room temperature, filtered the solid and washed it a total of 1800 ml of ethanol.

The resulting substance is suspended in a mixture of 4650 ml of ethanol and 41 g of diisopropylethylamine and heated the reaction mixture for 3 hours with flowing phlegm. Next, the reaction mixture is cooled to room temperature, filtered, the solid is then washed it a total of 1000 ml of ethanol and dried at a temperature of 60-70° in a vacuum drying Cabinet to constant weight. Receive 1130 solid beige color, which is presented on Fig.1 x-ray diffraction the powder diffraction pattern presented in figure 2 diagram DTA presented on Figure 3 IR spectrum.

Obtained according to this method, the solid absorbs at a relative humidity equal to 95% (installed by using a saturated aqueous solution above the sediment Na2HPO4×12H2O) within a day about 1 wt.% water.

Example 2

A mixture of 4.6 g of 7-chloro-8-cyan-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinoline-carboxylic acid, 15 ml of ethanol, 9 ml of N-methylpyrrolidine and 1.9 g of N-triethylamine is heated to education back phlegmy. Was added dropwise of 2.08 g of (1S,6S)-2,8-diazabicyclo[4.3.0]nonane and paramesh the offer, then 3 hours at education phlegmy. Upon cooling to room temperature the solid is filtered off and washed with a total of 10 ml of ethanol and dried to constant weight. Get 5,23 g solid beige color, DTA chart which corresponds to the modification of the Century

Example 3

A mixture of 4.6 g of 7-chloro-8-cyan-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinoline-carboxylic acid, 15 ml of ethanol, 9 ml of N-methylpyrrolidine and 2.12 g of N-ethylpiperidine heated to education back phlegmy. Was added dropwise of 2.08 g of (1S,6S)-2,8-diazabicyclo[4.3.0] nonane and then stirred 3 hours at education phlegmy. Upon cooling to room temperature the solid is filtered off and washed with a total of 10 ml of ethanol and dried to constant weight. Get 5,1 g solid beige color, DTA chart which corresponds to the modification of the Century

Example 4

A mixture of 9.2 g of 7-chloro-8-cyan-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinoline-carboxylic acid, 30 ml of ethanol, 18 ml of dimethylformamide and 4,85 g diisopropylethylamine heated to education back phlegmy. Was added dropwise to 4.17 g of (1S,6S)-2,8-diazabicyclo[4.3.0] nonane and then stirred 3 hours at education phlegmy. Upon cooling to room temperature the solid is filtered off and washed with a total of 20 ml of ethanol and dried to constant weight. Get 11 grams of solid beige color is the DTA chart which corresponds to the modification of the Century

Example 5

A mixture of 9.2 g of 7-chloro-8-cyan-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinoline-carboxylic acid, 30 ml of ethanol, 18 ml of sulfolane and 4,85 g diisopropylethylamine heated to education back phlegmy. Was added dropwise to 4.17 g of (1S,6S)-2,8-diazabicyclo[4.3.0]nonane and then stirred 3 hours at education phlegmy. Upon cooling to room temperature the solid is filtered off and washed with a total of 20 ml of ethanol and dried to constant weight. Obtain 10.8 g of a solid substance beige, DTA chart which corresponds to the modification of the Century

Example 6

0.5 g of a solid substance of comparative example are suspended in 3 ml of ethanol. The reaction mixture is heated for 3 hours with the formation of reverse phlegmy, the solid is filtered off and dried. X-ray powder diffractogram corresponds to the modification of the Century

1. 8-cyan-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline-carboxylic acid (CCDC) of the crystalline modification V, with x-ray diffraction the diffraction pattern of the powder with the following reflexes (2 theta) with high and medium intensity.

2θ (2 theta)

8,91

13,23

14,26

14,40

15,34

17,88

19,70

20,78

21,86

28,13

30,0

2. 8-cyan-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline-carboxylic acid (CCDC) of crystalline modification according to claim 1, having defined using DTA melting temperature 243-245°C.

3. 8-cyan-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline-carboxylic acid (CCDC) of crystalline modification according to claim 1 or 2, obtained by the interaction of 7-halo-8-cyan-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinoline-carboxylic acid of formula (II)

where

Hal is fluorine or preferably chlorine

with (1S,6S)-2,8-diazabicyclo[4.3.0]nananom formula (III)

if necessary in the presence of a base in an environment of ethanol in the mixture with a polar aprotic diluent, such as N-organic, dimethylformamide and sulfolane, or by heating CCDC unknown modification in the environment of a diluent, such as ethanol, propanol or isopropanol, or mixtures of these alcohols with a polar aprotic diluent, such as N-organic, dimethylformamide and sulfolane, optionally in the presence of a base, cooling the mixture and separating CCDC in the form of a crystalline modification of the Century

4. Drug with activity against pathogenic bacteria, characterized by the fact that h is about it contains along with the usual excipients and fillers CCDC modification In one of claims 1 to 3.



 

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SUBSTANCE: invention describes 8-cyano-1-cyclopropyl-7-(1S,6S)-2,8-diazabicyclo-[4.3.0]-nonane-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid of the formula (I): with the crystalline modification A and a drug eliciting effect against pathogenic microorganisms. The prepared crystalline modification shows stability and doesn't transform to another crystalline modification or amorphous form being even at prolonged storage.

EFFECT: improved and valuable properties of compound.

4 cl, 4 dwg, 6 ex

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EFFECT: improved and valuable properties of compound.

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