# Derivatives of 11-acetyl-12,13-dioxabicyclo [8.2.1] tridecane, a method of receiving and containing these compounds medicines

The invention relates to a derivative of (2R, 3S, 4S, 5R, 6R, 10R,11R)-2,4,6,8,10-pentamethyl-11-acetyl-12,13-dioxabicyclo[8.2.1] tridec-8-EN-1-it General formula (I), where R

^{1}denotes hydrogen or methyl and R

^{2}denotes hydrogen or (NISS. )alkyl, and their physiologically acceptable acid additive salts. The method of obtaining the compounds according to the invention involves the oxidative cleavage of the glycol in the side 2',3'-dihydroxyphenyl-2-strong chain in position 11 cyclic structures of the compounds of formula (II), where R

^{1}and R

^{2}have the above values. Also proposed drug suitable for treatment of disorders of motility in the gastrointestinal tract, gastroparesis, impaired gastric emptying, gastroesophagal outflow and/or dyspepsia, containing an effective amount of the compounds according to the invention and pharmaceutical excipients and/or carriers. 3 S. and 2 C.p. f-crystals, 1 PL.Description text in facsimile form (see graphic part).

Claims

1. Derivatives (2R,3S,4S,5R,6R,10R,11R)-2,4,6,8,10-pentamethyl-11-acetyl-12,13-dioxabicyclo[8.2.1]tridec-8-ene 1-it will oboznachaet hydrogen or lower alkanoyl,as well as their physiologically acceptable acid salt additive.2. Connection on p. 1, where R^{1}denotes methyl.3. Connection under item 1 or 2, where R

^{2}denotes hydrogen.4. Drug suitable for treatment of disorders of motility in the gastrointestinal tract, gastroparesis, impaired gastric emptying, gastroesophagal outflow and/or dyspepsia and containing an effective amount of the compounds on p. 1 and a conventional pharmaceutical excipients and /or carriers.5. The method of obtaining derivatives of (2R,3S,4S,5R,6R,10R,11R)-2,4,6,8,10-pentamethyl-11-acetyl-12,13-dioxabicyclo-[8.2.1]-tridec-8-EN-1-it General formula Iwhere R

^{1}denotes hydrogen or methyl;R

^{2}denotes hydrogen or lower alkanoyl,as well as their physiologically acceptable acid additive salts, characterized in that the compound of General formula IIwhere R

^{1}and R

^{2}have the above values,2,3-dihydroxyphenyl-2-ilen side chain in the 11-position of the cyclic core structure is transferred by oxidative cleavage of the glycol acetyl side chain, and, if necessary, in the resulting compound of formula I, methyl, otscheplaut metal residue R

^{1}and, if necessary, available the compounds of formula I translate in their stable acid additive salt or acid salt additive is transferred into the free compounds of formula I.

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The invention relates to the field of medicine

The invention relates to compounds represented by the General formula (I)

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where A represents NH group, and thus C=O-group or A - C=O-group and thus NH-group, R

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or together with R

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where A represents NH group, and thus C=O-group or A - C=O-group and thus NH-group, R

^{1}HE band, L-clavesilla group of the formula (II)< / BR>

or together with R

^{2}is a ketone; R^{2}is hydrogen or together with R^{1}represents a ketone; R^{3}is hydrogen or C_{1}-C_{4}-alcoolica group, and pharmaceutically acceptable salts of the accession of organic and inorganic acidsThe invention relates to a derivative of 9-O-benzodithiophene erythromycin And formula (III), where Y

_{1}and Y_{2}represent hydrogen atoms or trimethylsilyl group, or its crystalline MES, which are used as intermediate compounds for the synthesis of clarithromycinThe invention relates to an improved process for the preparation of the hydrochloride of the oxime erythromycin A (I)

The invention relates to a derivative of erythromycin General formula (II), (III), (IV) and (V), where R is a substituted C

_{1}-C_{10}-alkyl, C_{3}alkenyl,_{3}-quinil, etcThe invention relates to the production of antibiotics, namely the technology of water-soluble salts of erythromycin, erythromycin phosphate

The invention relates to derivatives [(1'R), 2R, 3S, 4S, 5R, 6R, 9R, 11R, 12R, 14R] -11-(1'-hydroxypropyl)-2,4,6,8,11,14-HEXAMETHYL-10,13,15-trioxadecyl [9.2.1.1

Derivatives of thiazole, method for their production and pharmaceutical composition based on them // 2218337

The invention relates to new thiazole derivative of the formula (I) in which R

^{1}denotes a group of formula (a)-(d), where R^{2}denotes a group of formula (II), R^{3}denotes hydrogen, alkyl, cycloalkyl, and so on; R^{4}denotes alkyl, phenyl, heteroaryl; R^{5}and R^{6}each independently of one another denote hydrogen, heteroaryl; R^{7}and R^{8}each independently of one another denotes hydrogen, or R^{7}and R^{8}together with the N atoms to which they are linked, form a 5-6-membered heterocycle; R^{9}denotes hydrogen, alkyl, cycloalkyl; R^{10}denotes phenyl, benzyl, and so on; And denotes a carbonyl or sulfonyl; In denotes hydrogen; and m each represents zero or a positive number from zero to 2, but not equal to zero when R^{1}denotes-NH_{2}; b denotes a number from zero to 4; C, d, f, g, k, l and m each independently of one another denotes zero or 1, so that each of the C, f and g cannot simultaneously denote zero and thus m does not denote zero when f or g represents 1; q represents zero or 1, and each k and l also denotes zero, when i denotes zero; e denotes a number from zero to 3; h represents a number from zero to 5; j denotes a number from zero to 2; and the sum isDerivatives of thiazole, method for their production and pharmaceutical composition based on them // 2218337

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^{1}denotes a group of formula (a)-(d), where R^{2}denotes a group of formula (II), R^{3}denotes hydrogen, alkyl, cycloalkyl, and so on; R^{4}denotes alkyl, phenyl, heteroaryl; R^{5}and R^{6}each independently of one another denote hydrogen, heteroaryl; R^{7}and R^{8}each independently of one another denotes hydrogen, or R^{7}and R^{8}together with the N atoms to which they are linked, form a 5-6-membered heterocycle; R^{9}denotes hydrogen, alkyl, cycloalkyl; R^{10}denotes phenyl, benzyl, and so on; And denotes a carbonyl or sulfonyl; In denotes hydrogen; and m each represents zero or a positive number from zero to 2, but not equal to zero when R^{1}denotes-NH_{2}; b denotes a number from zero to 4; C, d, f, g, k, l and m each independently of one another denotes zero or 1, so that each of the C, f and g cannot simultaneously denote zero and thus m does not denote zero when f or g represents 1; q represents zero or 1, and each k and l also denotes zero, when i denotes zero; e denotes a number from zero to 3; h represents a number from zero to 5; j denotes a number from zero to 2; and the sum isDerivatives of thiazole, method for their production and pharmaceutical composition based on them // 2218337

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where a denotes (R

< / BR>

where a denotes (R

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