НОВЫЕ ЛЕКАРСТВЕННЫЕ ВЕЩЕСТВА

Изобретение относится к органической химии и может найти применение в медицине. Описываются соединения или их соли, имеющие следующую общую формулу (I): где A=R-T1-, где R представляет собой радикал лекарственного вещества, такой как определено в формуле изобретения, T1=(CO), О, S, N или NR1c, где R1c представляет собой Н или C1-C5 алкил; В=-ТB -Х2-tBI, где ТB и tBI одинаковы или различны и выбраны из (СО), О, S, N или NR1c, где R1c такой, как определено выше, Х2 представляет собой бивалентную мостиковую группу, такую как соответствующий предшественник В, такой, как определено в формуле изобретения; С представляет собой бивалентный радикал -Tc-Y-, где Тс=(СО), О, S, N или NR1c, где R1c такой, как определено выше, Y имеет значения такие, как представлено в формуле изобретения. Также описывается фармацевтическая композиция на основе соединений формулы (I) для использования в случаях окислительного стресса и/или эндотелиальных дисфункций. Технический результат - получены новые соединения и ...

СПОСОБ ПОЛУЧЕНИЯ АМПИЦИЛЛИНА ТРИГИДРАТА

Способ получения производных 7-/ -(-)-2-АМиНО-2-(п-АцЕТОКСифЕНил- АцЕТАМидО)-3-цЕфЕМ-4-КАРбОНОВОй КиСлОТы

Способ получения кристаллического пивалоилоксиметилового эфира ампициллина

Способ получения 6-метокси- -карбоксипенициллиной или их солей

Способ получения альфа-аминоциклогексадиенилалкиленпенициллинов или альфа-аминоциклогексадиенилалкиленцефалоспоринов

Способ получения сложного 1-этоксикарбонилоксиэтилового эфира 6- @ -(-)-2-амино-2-фенилацетамидо @ пенициллановой кислоты в виде его аддитивной соли с галоидводородной кислотой

Способ получения йодметил 6-/ @ -2-азидо-2-фенилацетамидо/пеницилланоилоксиметил карбоната

СПОСОБ ПОЛУЧЕНИЯ ЙОДМЕТИЛ 6-(В-2-АЗИДО-2-ФЕНИЛАЦЕТАМИДО)-ПЕНИЦИЛЛАНОИПОКСИМЕТИЛ КАРБОНАТА формулы отличающийся тем, что соединение общей формулы /г , QHCH-CONHJ-J-VCH; Нз о - --соом (У) где М - тетрабутиламмоний, подвергают взаимодействию с соединением формулы О , JCHgOCOCHgJ в среде инертного в условиях реакции 9) органического растворителя при тем;о пературе от 0 до комнатной. СП ...

Способ получения кристаллических пенициллановых кислот

Способ получения производных пенициллановой кислоты или их солей

Способ получения производных цефалоспорина или пенициллина

Способ получения бис-эфиров метандиола с пенициллином и 1,1-диоксидом пенициллановой кислоты

СПОСОБ ПОЛУЧЕНИЯ БИС-ЭФИРОВ МЕТАНДИОЛА С ПЕНИЦИЛЛИНОМ И 1,1-ДИОКСИДОМ ПЕНИЦИЛЛАНОВОЙ КИСЛОТЫ формулы Н Н н-сн,-соян -4 ш: . о о сн, Y сн, 5x5- 0 C-l R о где R - фенил или феноксигруппа, отличающийся тем, что соединение формулы Н Н -,, VT Т. V. H,N снз Q --14-- /с-о п о о 0 ri V f«W i vS-s4- 3 т рснз S к-J.,,f.- с-о 0 в о подвергают ацилированию реакционноспособным производным карбоновой кислоты формулы ю N9 ГО R-CH,j-COOH, где R имеет указанные значения 00 при охлаждении в среде инертного растворителя.

BETA-LACTAM-ANTIBIOTIKA.

PHARMAZEUTISCHE VERBINDUNGEN

VERFAHREN ZUR HERSTELLUNG VON HALOGENMETHYL-6-SUBST.-PENICILLANOYLOXYMETHYL-CARBONATEN

Process for 6-(d(-)-alpha-amino-phenylacet- - amido)-penicillanic acid

... 6-APA is acylated with D(-)alpha-aminophenylacetic acid protected by reaction with a beta-keto ester, a beta-dicarboxylic acid or O-nitrophenylsulphenyl chloride in an organic solvent at pH 8-10 at 20-80 degrees C. As the product hydrolysed in aq. acetone pref. at pH 2-3.5, evapd., the residue extd. with an organic solvent, pref. BuOAc and the title product (I) isolated. (I) is a broad spectrum anti-biotic and is produced by a simple procedure without isolation of intermediates.

PIVALOYLOXYMETHYL-ALPHA-AMINOBENZYLPENICILLINAT

(ALPHA-CYANAMINO) ACETAMIDO-PENICILLINE UND -CEPHALOSPORINE

VERFAHREN ZUR HERSTELLUNG VON PENICILLINVERBINDUNGEN

VERFAHREN ZUR HERSTELLUNG EINER LOESUNG VON PHARMAZEUTISCH VERWERTBAREM AMPICILLIN-NATRIUM

SS-LACTAM-ANTIBIOTIKA, VERFAHREN ZUR HERSTELLUNG UND IHRE VERWENDUNG ALS ARZNEIMITTEL

NEUE PENICILLINE

PENICILLIN SALTS

... 1365028 Penicillin salts MERCK & CO Inc 13 Nov 1972 [18 Nov 1971 7 Aug 1972] 52374/72 Heading C2A The novel probenecid salt of D-(-)--aminobenzyl-penicillin pivaloyloxymethyl ester is prepared by reacting together in a liquid medium probenecid or a salt thereof and the said penicillin ester or a salt thereof. In the preferred process, the liquid medium is a solvent for the reactants and a non-solvent for the desired product, so that the latter crystallizes out from the reaction medium. This is achieved by using methanol, ethanol, propanol or isopropanol as the medium in which are reacted essentially equimolar amounts of an alkali metal (e.g. potassium) salt of probenecid and a mineral acid (e.g. HCl) salt of the penicillin ester, whereupon the inventive salt crystallizes out and the by-product (KCl) remains in solution. Pharmaceutical antibacterial compositions comprise the said novel salt together with a non- toxic pharmaceutical carrier. The compositions may be in unit dosage solid or ...

PENICILLINS AND PRODUCTION THEREOF

... 1412168 -Alkoxysulphonyl-benzylpenicillins TAKEDA YAKUHIN KOGYO KK 16 Nov 1973 [9 July 1973 13 July 1973] 53279/73 Heading C2C Novel - alkoxysulphonyl - benzylpenicillins of the general formula wherein R is a C 6-14 branched alkyl group, and pharmaceutically acceptable salts thereof are prepared by reacting 6-aminopenicillanic acid or a salt or easily-cleavable ester thereof with an - alkoxysulphonyl - phenylacetic acid of the general formula or a reactive derivative thereof (e.g. the acid chloride, prepared by reacting the acid with thionyl chloride) and, in the case where an easily-cleavable ester of 6-amino penicillanic acid is used, removing the easily-cleavable ester-forming group, followed optionally by salification of the product. Pharmaceutical compositions having antimicrobial activity comprise, as active ingredient, an -alkoxysulphonyl-benzylpenicillin of the first general formula above or a pharmaceutically acceptable salt thereof, together with a physiologically acceptable carrier ...

A-BROMODIETHYL CARBONATE AND ITS USE IN THE PREPARATION OF ANTIBIOTICS

PHARMACEUTICAL INJECTABLE AMOXICILLIN PREPARATION

Materials treatment

An apparatus for use in a process of removing a material from a substrate comprises a separator 2 having a first inlet 6 through which solvent may be added and a second inlet 26 through which the substrate may be introduced, the apparatus being arranged for intimate contact of the solvent with the substrate. The apparatus also comprises units 12, 34 for collecting the solvent charged with the material and for collecting the substrate after the material has been extracted therefrom. Preferably, the separator is a column, in which the pressure may be reduced to below atmospheric pressure. The apparatus may comprise a recirculation system to return the solvent to the first inlet after extraction of the material from the substrate. A process using the apparatus is also disclosed, wherein a C1-C4 fluorinated hydrocarbon is contacted with the substrate to remove the material therefrom.

Materials treatment

ACRLOXYALKYL ESTER DERIVATIVES OF PENICILLIN AND CEPHALOSPORIN

... 1377573 Penicillin and cephalosporin esters YAMANOUCHI PHARMACEUTICAL CO Ltd 5 April 1972 [5 April 1971 19 April 1971 20 April 1971 11 Aug 1971] 15715/72 Heading C2C Novel acyloxyalkyl esters of ampicillin, cephaloglycin and cephalexin having the general Formula (I) wherein A is a group of formula in which R1 and R2 each represents an unsubstituted or substituted alkyl, cycloalkyl, alkenyl or phenyl group wherein the substituent is a phenyl group, a phenoxy group or a halogen atom or atoms, and R3 is a hydrogen atom or an acetoxy group, and acid addition salts of the said esters, are prepared by esterifying 6-aminopenicillanic acid, 7-aminocephalosporanic acid or 7-aminodesacetoxy-cephalosporanic acid, or an N-acylated derivative of these compounds, by reacting the alkali metal salt thereof with an acyloxyalkyl halide of formula wherein R1 and R2 are as defined above and X is a halogen atom. The resulting ester is then N-acylated by reaction ...

SYNTHETIC PENICILLIN AND PROCESS FOR THE PREPARATION THEREOF

... 1372570 Penicillin esters BRISTOL-MYERS CO 26 Nov 1971 [27 Nov 1970] 55105/71 Heading C2A Novel penicillin esters having the Formula (I) wherein X is hydrogen or a cation, are prepared by either (a) reacting a compound of formula wherein Y and R are each a cation, with a halomethyl pivalate of formula wherein R2 is Cl, Br or I, or its chemical equivalent as an esterifying agent; or (b) reacting a compound of formula with trimethylamine-sulphur trioxide, Reaction (a) is preferably performed in hexamethlphosphortriamide using equimolar quantities of the reactants. Reaction (b) may be carried out in dry methylene chloride using a 10% molar excess of the trimethylamine-sulphur trioxide. The compounds may be converted to their base salts by treatment with a basic compound of the inorganic cation (e.g. Na, Ca, K) Al or NH 4 ) or with an organic base. When such treatment is conducted in aqeous solution, the salt is obtained as the mono- or di-hydrate. Pharmaceutical compositions having ...

IMPROVEMENTS IN OR RELATING TO BETA LACTAM PRODUCTION

Penicillin compounds and methods for the production thereof

Penicillin compounds and methods for the production thereof are described, said penicillin compounds being represented by the formula (I) (I) wherein R1, R2, and R3 each represents hydrogen, a lower alkyl group, a halogen atom, a lower alkoxy group, a hydroxyl group, or a substituted or unsubstituted phenylalkoxy group except that R1, R2, and R3 cannot all represent hydrogen simultaneously; R4 represents hydrogen or a lower alkyl group; and R5 represents hydrogen or a hydroxyl group.

PENICILLINS

PROCESS FOR THE PRODUCTION OF 2-AMINOBENZYLPENICILLIN

... 1286920 Enzymes EISAI KK 10 Aug 1970 [2 Sept 1969] 38472/70 Heading C3H [Also in Division C2] An enzyme preparation capable of N-acylating 6-aminopenicillanic acid with an N-acylating derivative of D-(-)--aminophenylacetic acid to give ampicillin, is prepared by ultra-sonically disrupting cells of Flavobacterium EF 44-102 nov. sp. (ATCC. 21429) in pH 7À5 decimolar phosphate buffer and centrifuging down the cell debris to leave a clear enzyme solution. The enzyme is also capable of N-deacylating ampicillin to 6-aminopenicillanic acid.

Novel substituted 5-(amino-propylidene)-dibenzo[a,d]-cyclohepta[1,4,6]trienes and the manufacture thereof

Novel compounds of formula wherein each of the symbols R represents a lower alkyl group, X and Y each represent a hydrocarbon substituent which, when alkyl, may be joined to one another directly or through an oxygen or nitrogen atom (which nitrogen atom may carry an alkyl, hydroxy or hydroxyalkyl substituent) to form a ring which includes the N-atom to which they are attached, or one of them may form a similar ring with one of the lower alkyl groups which may be attached to the propylidene chain, and Hal represents a 10- or 11-halogen substituent, and wherein the broken lines denote that the groups attached thereby are optional, and acid addition salts thereof, are prepared either by dehydrating the corresponding 5-aminopropyl compound having a hydroxy substituent in the 5-position of the tricyclic system or on the 1-position of the 5-aminopropyl substituent or, where the optional alkyl groups on the propylidene chain are not involved in ring formation, reacting the ...

SUBSTITUTED PENICILLANIC ACIDS

... 1476981 6 - (D) - (-) - - amino - - (pacetoxyphenylacetamido)penicillanic acid BRISTOL MYERS CO 19 March 1975 [5 June 1974 19 Nov 1974] 24848/74 and 50016/74 Heading C2C The invention comprises the title compound [substantially free from L-(+ )-isomer], and its pharmaceutically acceptable salts. In examples, this compound is prepared by reacting aminopenicillanic acid or its trimethylsilyl ester with the acid chloride hydrochloride, of D-(-)-p-acetoxyphenylglycine, and (where applicable) hydrolysing the intermediate trimethylsilyl ester of the product. The title compound may be treated in aqueous solution with an esterase to give the p-hydroxyphenyl analogue. Therapeutic compositions having antibacterial activity, and which may be administered orally or parenterally, comprise either the title compound, or the p-hydroxyphenyl analogue which has been prepared from it.

PROCESS FOR THE PREPARATION OF SODIUM AMOXYCILLIN

PROCESS OF PREPARING A SOLID PREPARATION OF A PENICILLIN DERIVATIVE

PROCESS FOR THE PREPARATION OF SODIUM AMOXYCILLIN

PIPERAZINYLBENZOHETEROCYCLIC COMPOUNDS

PENICILLINS

6-(A-HETEROCYCLYLCARBONYL AMINO-ACETAMIDO)-PENICILLINS AND COMPOSITIONS CONTAINING THEM

Penicillins

Method of preparation of only one ampicilline ester salt pivaloyloxymethylic.

Method of preparation of a new agent antibactérien.

Process of stabilization of agents of halogenation phosphite of triaryle-halogen.

Method of preparation of new penicillins.

Method of preparation of a new acid penicillanic and new industrial product.

Process for the preparation of penicillin esters.

Derived pénam and their preparation.

New methods of preparation of penicillin and their use.

VERFAHREN ZUR HERSTELLUNG VON D(-)-ALFA-AMINO-P-HYDROXYBENZYLPENICILLIN

MEANS TO THE FAERBEN OF KERATINFASERN

PROCEDURE FOR THE PRODUCTION OF NEW PENICILLIN DERIVATIVES

PROCEDURE FOR THE PRODUCTION OF FIRM ONE 6 (D-ALPHA - AMINO P HYDROXYPHENYLACETAMIDO) - PENICILLAN SAEURENATRIUMSALZ

PROCEDURE FOR THE PRODUCTION OF NEW BETA LACTAM - CONNECTIONS

PROCEDURE FOR THE PRODUCTION OF NEW PENICILLIN DERIVATIVES

PROCEDURE FOR THE PRODUCTION OF P-HYDROXY-ALPHA - AMINOBENZYLPENICILLIN

PROCEDURE FOR THE PRODUCTION OF NEW PENICILLIN DERIVATIVES

VERFAHREN ZUR HERSTELLUNG VON 6-(D-(-)-ALPHA-(4- ETHYL-2,3-DIOXO-1-PIPERAZINOCARBONYLAMINO)- PHENYLAZETAMIDO)-PENICILLANSAEURE

A process for the preparation-of 6-D-( alpha )-4-ethyl-2,3-dioxo-1 -piperazinylcarbonylamino)- alpha -phenylacetamido-penicillanic acid which allows easy recovery of the reaction product in high yield and purity comprises acylating ampicillin with 4-ethyl-2,3-dioxopiperazinylcarbonyl chloride in an aqueous/organic solvent medium which is a chlorinated aliphatic hydrocarbon medium, reaction taking place in the presence of a base with 4 to 6 ml of the chlorinated aliphatic hydrocarbon being present for each gram of the starting ampicillin and being followed by separation off of the organic phase, cooling of the aqueous phase to a temperature of not more than 10 DEG C, and acidification of the aqueous phase.

PROCEDURE FOR THE PRODUCTION OF A POWDER WITH A CONTENT OF MIKROVERKAPSELTEM AMPICILLIN ESTER ACID ADDITION SALT

PROCEDURE FOR THE PRODUCTION OF NEW OF PENICILLIN DERIVATIVES

VERFAHREN ZUR HERSTELLUNG VON NEUEM ALPHA- (4-OXO-4H-THIOPYRAN-3-YL) CARBOXAMIDO -P- HYDROXYBENZYLPENICILLIN

VERFAHREN ZUR HERSTELLUNG NEUER PENICILLINDERIVATE

VERFAHREN ZUR HERSTELLUNG VON NEUEN PENICILLINEN

VERFAHREN ZUR HERSTELLUNG VON FESTEM 6-(D-ALPHA -AMINO-P-HYDROXYPHENYLACETAMIDO)-PENICILLAN- SAEURENATRIUMSALZ

VERFAHREN ZUR HERSTELLUNG VON NEUEN PENICILLAN- SAEUREDERIVATE

VERFAHREN ZUR HERSTELLUNG DER NEUEN 6- (D-2- (3-HYDROXYPYRIDAZIN-4-CARBONAMIDO)-2- (P-HYDROXYPHENYL)-ACETAMIDO)-PENICILLANSAURE UND IHRER SALZE

VERFAHREN ZUR HERSTELLUNG VON P-HYDROXY-ALPHA- -AMINOBENZYLPENICILLIN

VERFAHREN ZUR HERSTELLUNG VON PENICILLIN- UND CEPHALOSPORINDERIVATEN

VERFAHREN ZUR HERSTELLUNG NEUER PENICILLINE UND IHRER SALZE

PROCEDURE FOR the PRODUCTION AGAIN ALFA (4-OXO-4H-THIOPYRAN-3-YL) CARBOXAMIDO P HYDROXYBENZYLPENICILLIN

PROCEDURE FOR THE PRODUCTION OF NEW ONES BETA LACTAMANTIBIOTICA

PROCEDURE FOR THE PRODUCTION HALFSYNTHETIC PENICILLIN DERIVATIVES

PROCEDURE FOR THE PRODUCTION OF THE NEW OF CRYSTALLINE ONE PIVALOYLOXYMETHYL D (-) - ALFA AMINOBENZYLPENICILLINATS

PROCEDURE FOR THE PRODUCTION OF NEW PENICILLINEN

PROCEDURE FOR THE PRODUCTION OF AMINOPENICILLINEN

PROCEDURE FOR PRODUCTION OF ALPHA AMINO BENZYLE PENICILLIN

PROCEDURE FOR THE PRODUCTION OF NEW PENICILLIN DERIVATIVES

PROCEDURE FOR THE PRODUCTION OF ANTIBACTERIAL CONNECTIONS

PROCEDURE FOR THE PRODUCTION OF A POWDER WITH A CONTENT OF MIKROVERKAPSELTEM AMPICILLIN ESTER ACID ADDITION SALT

PROCEDURE FOR THE PRODUCTION OF NEW PENICILLIN DERIVATIVES

PROCEDURE FOR the PRODUCTION of the NEW ONES 6 - (D-2 (3-HYDROXYPYRIDAZIN-4-CARBONAMIDO) - 2 (P-HYDROXYPHENYL) - ACETAMIDO) - PENICILLANSAURE AND YOUR SALTS

PROCEDURE FOR THE PRODUCTION OF STERILE BETA LACTAM ANTIBIOTICS

PHARMACEUTICAL CONNECTIONS

PROCEDURE FOR THE PRODUCTION OF NEW PENICILLINE

PROCEDURE FOR THE PRODUCTION OF NEW PENICILLINEN

PROCEDURE FOR THE PRODUCTION OF NEW DERIVATIVES OF THE PENAM-3-CARBONSAEURE AND CEPHEM-4-CARBONSAEURE

PROCEDURE FOR the PRODUCTION OF 6AMINOPENICILLANS [URE-1,1-DIOXID AND ITS SALTS.

NEW 6ALPHA-METHOXY-PENICILLINE, YOUR SALTS, PROCEDURES FOR YOUR PRODUCTION AND THESE CONNECTIONS CONTAINING DRUGS.

BETA LACTAM ANTIBIOTICS, PROCEDURES FOR THE PRODUCTION AND YOUR USE AS DRUGS.

VERFAHREN ZUR HERSTELLUNG VON NEUEN PENAMCARBONSAEURE-DERIVATEN

VERFAHREN ZUR HERSTELLUNG VON FURO-(3,4-C)PYRIDINDERIVATEN

PROCEDURE FOR THE PRODUCTION OF NEW PENICILLINEN

PROCEDURE FOR THE PRODUCTION OF NEW BETA LACTAMS - CONNECTIONS