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 R1denotes hydrogen or methyl and R2denotes 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 R1and R2have 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 R1denotes methyl.

3. Connection under item 1 or 2, where R2denotes 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 I

where R1denotes hydrogen or methyl;

R2denotes hydrogen or lower alkanoyl,

as well as their physiologically acceptable acid additive salts, characterized in that the compound of General formula II

where R1and R2have 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 R1and, 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.

 

Same patents:
The invention relates to the field of medicine

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

< / BR>
where A represents NH group, and thus C=O-group or A - C=O-group and thus NH-group, R1HE band, L-clavesilla group of the formula (II)

< / BR>
or together with R2is a ketone; R2is hydrogen or together with R1represents a ketone; R3is hydrogen or C1-C4-alcoolica group, and pharmaceutically acceptable salts of the accession of organic and inorganic acids

The invention relates to a derivative of 9-O-benzodithiophene erythromycin And formula (III), where Y1and Y2represent hydrogen atoms or trimethylsilyl group, or its crystalline MES, which are used as intermediate compounds for the synthesis of clarithromycin

The 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 C1-C10-alkyl, C3alkenyl,3-quinil, etc
The 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

The invention relates to new thiazole derivative of the formula (I) in which R1denotes a group of formula (a)-(d), where R2denotes a group of formula (II), R3denotes hydrogen, alkyl, cycloalkyl, and so on; R4denotes alkyl, phenyl, heteroaryl; R5and R6each independently of one another denote hydrogen, heteroaryl; R7and R8each independently of one another denotes hydrogen, or R7and R8together with the N atoms to which they are linked, form a 5-6-membered heterocycle; R9denotes hydrogen, alkyl, cycloalkyl; R10denotes 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 R1denotes-NH2; 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 is

The invention relates to new thiazole derivative of the formula (I) in which R1denotes a group of formula (a)-(d), where R2denotes a group of formula (II), R3denotes hydrogen, alkyl, cycloalkyl, and so on; R4denotes alkyl, phenyl, heteroaryl; R5and R6each independently of one another denote hydrogen, heteroaryl; R7and R8each independently of one another denotes hydrogen, or R7and R8together with the N atoms to which they are linked, form a 5-6-membered heterocycle; R9denotes hydrogen, alkyl, cycloalkyl; R10denotes 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 R1denotes-NH2; 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 is

The invention relates to new thiazole derivative of the formula (I) in which R1denotes a group of formula (a)-(d), where R2denotes a group of formula (II), R3denotes hydrogen, alkyl, cycloalkyl, and so on; R4denotes alkyl, phenyl, heteroaryl; R5and R6each independently of one another denote hydrogen, heteroaryl; R7and R8each independently of one another denotes hydrogen, or R7and R8together with the N atoms to which they are linked, form a 5-6-membered heterocycle; R9denotes hydrogen, alkyl, cycloalkyl; R10denotes 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 R1denotes-NH2; 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 is

The invention relates to new derivatives of phenyl - and aminobenzenesulfonamide formula

< / BR>
where a denotes (R1SO2NR2-), (R3R60NSO2NR2-); X represents-NH-, -CH2- or-OCH2-; Y represents 2-imidazoline, 2-oxazoline or 4-imidazole; R1means (NISS

The invention relates to medicine, dermatology

The invention relates to medicine, in particular to plants with nephrolithiasis action, and can be used for the treatment and prevention of urolithiasis

The invention relates to medicine, namely to veterinary medicine, and can be used for ointments and their subsequent application in the treatment of infected wounds

The invention relates to medicine, in particular to urology and Nephrology, and for the treatment of acute purulent pyelonephritis
The invention relates to medicine, in particular to the gynecologist, and can be used for the treatment of obesity
The invention relates to medicine, in particular to Nephrology, and can be used for treatment and subsequent prevention of chronic infections of the urinary system in children
The invention relates to the field of medicine
Up!