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

Способ получения производных цефалоспорина или их аддитивных солей с трифторуксусной кислотой

Изобретение касается антибиотиков цефалоспоринового ряда, в частности производных цефалоспорина формулы где Z - 1,3- или 1,4-циклогексилен, или RS - группа -C-S-CK CH7 где К - - С(о)р - Алк - р О или 1; Алк указан выйе; или y,-2-,3-wjm 4-пиперидил,незаме цен- ный или замещенный по атому N пипе- ридил-4-СО или Ш2-Алк-СО, или их аддитивных солей с CFjCOGH, которые могут быть использованы в медицине. Для выявления активности с повышенной антимикробной эффективностью пробив отдельных штаммов микроорганизмов йыли получены новые производные I. Синтез ведут заменой брома в 3- бромметилцефалоспорине на соответствующий заместитель, причем в исходных продуктах все NH - и СООН-группы защищены. Затем защитные группы удаляют и выделяют I в свободном виде или в виде аддитивных солей с CFgCOOH. Соединения I обладают низкой токсичностью и более сильным антимикробным действием, чем известные цефалоспорины, 5 табл. СО N9 00 00 СН ...

Способ получения производных цефалоспорина или их солей и его вариант

... 1. Способ получения производных цефалоспорина общей формулы Н -pHCONH 4 А Д-Нх г СНг-Б-Ве со ОООЕ NH где А - 4-оксифенил или 2-тиенил; R - радикал обшей формулы .он Пг а или н-ув Rt RI где R - 3-пиридиламиногруппа, незамещенная или замещенная аминосульфонилом, 2-фурилметиламинОгруппа , 2 имидазолилметиламиногруппа , незамещенная или замещенная метилом, 2-тиенилметиламиногруппа , незамещенная или замещенная аминосульфонилом , или -пиридилметиламиногруппа; Het - 4-метил-5,6-диоксо-1,2,4триазин-3-ил , 1-винилтетразол-5-ил или группа формулы N-X II (I V I )X2 где Rj - гидроксил, амино, диметиламино , ацетиламино, аминокарбонил , аминокарбониламино , аминосульфонгил, аминосульфониламино, оксисульфониламино , метилсульфонил или группа карбоновой или сульфокислоты; п - 1 или 2, или группа СП (CH2)j,R 2 - этил; Е - водород ,или защитная группа например сложноэфирная, или их солей, если Е - водород, отличающийся тем, что производное 7-аминоцефалоспоранрвой кислоты общей формулы ЯоН. I S J Nj CHrS-Het ...

CEPHALOSPORANSAEUREDERIVATE, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG IN PHARMAZEUTISCHEN ZUBEREITUNGEN

NEW CEPHALOSPORINS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

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.

3-Tetrahydrofuran and tetrohydropyrinol ephynolsporens and analogues.

B-Lactam antibiotics of formula (I) or a salt thereof: wherein R1 is hydrogen, methoxy or formamido; R2 is an acyl group;CO2R3 is a carboxy group or a .carboxylate anion, or R is a readily removable carboxy protecting group; R represents up to four substituents; X is S,SO,S02,0.or CH2; m is 1 or 2;and n is 0, useful in the treatment of bacterial infections in humans and animals.

NOVEL COMPOUNDS

Improvements relative to derivatives of naphtylglycyl-cephalosporines.

New antibiotic compounds derived from the cephalosporines, process of obtaining and pharmaceutical compositions the container.

NOVEL COMPOUNDS

ANTIBIOTIC CEPHALOSPORINDERIVATE, PROCEDURES FOR YOUR PRODUCTION AND PHARMACEUTICAL PREPARATIONS.

PROCEDURE FOR THE PRODUCTION OF NEW N-ACYLAMINO-ALFA-ARYLACETAMIDO-CEPHALOSPORINEN AS WELL AS OF THEIR SALTS

CEPHALOSPORINVERBINDUNGEN, PROCEDURES FOR YOUR PRODUCTION AND THEY ABSTENTION PHARMACEUTICAL PREPARATIONS.

PROCEDURE FOR the PRODUCTION OF NEW n ACYLAMINO ALFA ARYLACETAMIDo CEPHALOSPORINEN AS WELL AS OF THEIR SALTS

CEPHALOSPORIN-TYPE ANTIBIOTICS AND PROCESS FOR PRODUCING THE SAME

CEPHALOSPORINS, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

CEPHALOSPORIN-TYPE ANTIBIOTICS AND PROCESS FOR PRODUCING THE SAME

M-6-14536C/75 A cephalosporin compound represented by the formula (I) or (I') (I) (I') wherein R1 represents a phenyl group, a 2-thienyl group or a phenoxy group; R2 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms which may be substituted with a phenyl group, an alkoxy group having 1 to 4 carbon atoms or a halogen atom, or a phenyl group which may be substituted with one or two groups selected from the group consisting of a halogen atom, a nitro group, an alkyl group having 1 to 4 carbon atoms and an alkoxy group having 1 to 4 carbon atoms; R3 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms which may be substituted with a monoalkylamino group having 1 to 4 carbon atoms in the alkyl moiety thereof, a dialkylamino group having 1 to 4 carbon atoms in each alkyl moiety thereof, a halogen atom or a phenyl group which may be substituted with one to three groups selected from the group consisting of a halogen atom, a nitro ...

CEPHALOSPORINS, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

NEW CEPHALOSPORINS, PROCESSES FOR THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM Cephalosporins of the formula (I) wherein A is phenyl, 4-hydroxyphenyl, 3,4-dihydroxyphenyl or thienyl; Het is substituted triazin-3-yl or 1-substi-tuted-tetrazol-5-yl; R2 is optionally substituted heterocycyl or heterocyclylmethyl; and E is hydrogen or a protecting group; as well as tautomers and salts thereof. The novel compounds may be prepared by a variety of processes, and formulated into pharmaceutical compositions. They have activity against gram-positive and, particularly, gram-negative bacteria.

PROCEDURE FOR THE PRODUCTION OF NEW CEPHALOSPORINVERBINDUNGEN.

PROCEDURE FOR THE PRODUCTION OF 3 (MORPHOLINOALKOXYIMINOMETHYL) - CEPHEMVERBINDUNGEN.

[...][...] LA [...] DE N-ACYL-AMINO-ALPHA-PHENYL-( [...] ) -ACETAMIDO [...].

PROCEDURE FOR THE PRODUCTION OF NEW CEPHALOSPORANSAEUREDERIVATE.

Method for preparing cefonicid or its medicinal salt and intermediate

The invention provides a method for preparing cephalosporin nixi or its salt and its intermediate. The invention employs alkyl sulfonic acid to replace BF3 used in curretn technique as catalyst for reaction of 1- methanesulfonic acid- 5- mercapto- 1, 2, 3, 4- tetrazole acid or its salt and 7-aminocephalosporanic acid or its salt. It is characterized by reduced cost, decreased energy consumption, less toxic waste gas discharge and apparent economic benefit.

METHOD OF PREPARATION OF the ACID 7-D- (-) A-AMINO-A- (P-HYDROXYPHENYLACETAMIDO) - DESACETOXYCEPHALOSPORANIQUE

NOVEL CEPHALOSPORIN ANTIBIOTICS OF THE GROUP AND METHODS FOR THEIR MANUFACTURE

PRODUCTION OF ANTI-BACTERIAL AGENT

3,7-DISUBSTITUTED-3-CEPHEM-4-CARBOXYLIC ACIDS

CEPHALOSPORINE AND YOUR HOMOLOGOUS ONES, PREPARATIONS AND PHARMAZEUTSICHE PREPARATIONS

ANTIMICROBIAL COMPOSITIONS WHICH VINYLPYRROLIDINON CEPHALOSPORIN DERIVATIVES AND A CARBAPENEMANTIBIOTIKUM OR BETA LACTAMASEINHIBITOR ENTHATEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN N-ACYLAMINO-ALFA-ARYLACETAMIDO-CEPHALOSPORINEN SOWIE VON DEREN SALZEN

VERFAHREN ZUR HERSTELLUNG DER NEUEN 6-D-(-)-ALFA-AMINO-ALFA-(P-ACETOXYPHENYL-ACETAMIDO)-PENICILLANSAURE

VINYLPYRROLIDINON CEPHALOSPORIN DERIVATIVES

PROCEDURE FOR the PRODUCTION the NEW ONE 6-D (-) - ALFA AMINO ALFA (P-ACETOXYPHENYL-ACETAMIDO) - PENICILLANSAURE

its manufacture and use

CEPHALOSPORINS AND HOMOLOGUES PREPARATIONS AND PHARMACEUTICAL COMPOSITIONS

... ▓▓ B-Lactam antibiotics of formula (I) or a salt thereof,▓wherein R1 is hydrogen, methoxy or formamido; R2 is an acyl group;▓ CO2R3 is a carboxy group or a carboxylate anion, or R3is a readily▓removable carboxy protecting group; R4 represents up to four▓substituents; X is S, SO, SO2, O or CH2; m is 1 0r 2; and n is 0,▓useful in the treatment of bacterial infections in humans and▓animals.▓ ...

PROCESS FOR THE PRODUCTION OF PENICILLINS

The invention provides a novel method for producing phenylglycyl chloride hydrochlorides involving reaction of N-substituted phenylglycines with for example thionyl chloride and then gaseous hydrogen chloride, as well as certain novel starting materials for use in this process and certain end-products thereby produced.

PROCESS FOR PRODUCING ANTIBIOTIC COMPOUNDS DERIVED FROM CEPHALOSPORINS

CEPHALOSPORIN DERIVATIVES, METHODS OF PRODUCTION THEREOF AND PROPHYLACTIC AND THERAPEUTIC AGENTS FOR BACTERIAL INFECTION

Substituted 7-styryl-carbonyloxy-acetamido cephalosporanic

PROCEDURE FOR THE PREPARATION OF NEW REPLACED DERIVATIVES OF 7 (ALFA- (N-HIDROXIACILAMINO))- ACETAMIDO-CEFALOSPORINAS

Beta lactam production

A new process is described for the production of 7-alpha-aminoacyl-cephalosporin free from halogen-containing solvents by acylating 7-amino-ceph-3-em-4-carboxylic acid or a derivative thereof in a halogen-free solvent.

VERFAHREN ZUR HERSTELLUNG VON 7-D-(-)-ALPHA-AMINO-ALPHA-(P-HYDROXYPHENYLACETAMIDO)DESACETOXYCEPHALOSPORANSAEURE

VERFAHREN ZUR HERSTELLUNG VON CEPHALOSPORANSAEUREDERIVATEN

CEPHALOSPORINE UND IHRE HOMOLOGEN, ZUBEREITUNGEN UND PHARMAZEUTSICHE PRÄPARATE

CEPHALOSPORIN-TYPE ANTIBIOTICS AND PROCESS FOR PRODUCING THE SAME

... 1467217 Cephalosporins MEIJI SEIKA KAISHA Ltd 19 June 1975 [20 June 1974] 26071/75 Heading C2C The invention comprises novel antibiotic compounds (I) and (I1) wherein R1 is a phenyl group, a 2-thienyl group or a phenoxy group; R2 is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms which may be substituted with a phenyl group, an alkoxy group having 1 to 4 carbon atoms or a halogen atom, or a phenyl group which may be substituted with one or two groups selected from a halogen atom, a nitro group, an alkyl group having 1 to 4 carbon atoms and an alkoxy group having 1 to 4 carbon atoms; R3 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms which may be substituted with a monoalkylamino group having 1 to 4 carbon atoms in the alkyl moiety thereof, a dialkylamino group having 1 to 4 carbon atoms in each alkyl moiety thereof, a halogen atom or a phenyl group which may be substituted with one to three groups selected from a halogen atom ...

CEPHALOSPORINE, PROCEDURE FOR YOUR PRODUCTION AND PHARMACEUTICAL PREPARATIONS.

NEW CEPHALOSPORINE, PROCEDURES FOR YOUR PRODUCTION AND THESE CONNECTIONS CONTAINING DRUGS.

CEPHALOSPORIN ESTERS

CEPHALSOPORINS

CEPHALOSPORIN-TYPE ANTIBIOTICS AND PROCESS FOR PRODUCING THE SAME

ANTIBACTERIAL AGENTS

N-ACYLAMINO-'-ARYLACETAMIDO CEPHALOSPORINS

S-1-14918C/75 (F-13883) A cephalosporin derivative of the formula (I), wherein A is a mono- or polycyclic heteroaromatic ring, which contains at least one nitrogen atom as a hetero atom and which may be substituted with one or more substituents; R is a phenyl group substituted with at least one substituent selected from the group consisting of an amino group, a hydroxy group, a ureido group and a hydroxymethyl group; and X is an -OCOCH3 group or an -S-Het group in which Het is a 5- or 6-membered heterocyclic ring containing one to four hetero atoms selected from the group consisting of nitrogen, oxygen and sulfur atoms which may be substituted with one or more substituents, and the nontoxic pharmaceutically acceptable salts thereof which are useful as an antimicrobial and prepared by the reaction of a compound of the formula (II), HO-A-COOH (II) wherein A is as defined above, or a reactive derivative thereof, with a compound of the formula (III), wherein R and X are as defined above, or ...

CEPHALOSPORINS AND HOMOLOGUES, PREPARATIONS AND PHARMACEUTICAL COMPOSITIONS

... 2087967 9201696 PCTABS00010 .beta.-Lactam antibiotics of formula (I) or a salt thereof, wherein R1 is hydrogen, methoxy or formamido; R2 is an acyl group; CO2R3 is a carboxy group or a carboxylate anion, or R3 is a readily removable carboxy protecting group; R4 represents up to four substituents; X is S, SO, SO2, O or CH2; m is 1 or 2; and n is 0, useful in the treatment of bacterial infections in humans and animals.

NOUVEAUX COMPOSES ANTIBIOTIQUES DERIVES DES CEPHALOSPORINES

LA PRESENTE INVENTION CONCERNE DE NOUVELLES CEPHALOSPORINES DE FORMULE: (CF DESSIN DANS BOPI) DANS LAQUELLE:-COOA EST UN RADICAL ACIDE, UN SEL OU UN ESTER FACILEMENT HYDROLYSABLE,-X DESIGNE O OU S,-R ET R DESIGNENT INDEPENDAMMENT H OU ALKYLE INFERIEUR OU FORMENT AVEC L'ATOME DE CARBONE AUQUEL ILS SONT LIES UN NOYAU CYCLOBUTYLE OU CYCLOPENTYLE,-R EST UN RADICAL AMINE,LESDITES CEPHALOSPORINES ETANT SOUS FORME D'ISOMERE PUIS DE MELANGES D'ISOMERES ET EVENTUELLEMENT DE SELS D'AMINES, ELLE CONCERNE EGALEMENT UN PROCEDE DE PREPARATION DE CES CEPHALOSPORINES ET LES MEDICAMENTS ANTIBIOTIQUES QUI EN CONTIENNENT.

Substituted 7-styryl-carbonyloxy-acetamido cephalosporanic

METHOD OF PREPARATION OF the ACID 7-D- (-) A-AMINO-A- (P-HYDROXYPHENYLACETAMIDO) - DESACETOXYCEPHALOSPORANIQUE

Cephalosporin esters

CEPHALOSPORINES

CEPHALOSPORIN DERIVATIVES, PROCESS AND THEIR PREPARATION, AND PROPHYLACTIC AND TREATING AGENT AGAINST BACTERIAL INFECTION

Cephalosporin derivatives represented by the general formula (I), wherein R1 represents an alpha-, beta- or gamma-amino acid residue (bonded through an ester bond) whose amino group is optionally susbstituted by a lower alkyl group, R2 represents a l-alkanoyl-oxyalkyl group, a l-alkoxycarbonyloxyalkyl group, a phthalidyl group or a 5-methyl-1, 3-dioxolen-2-on-4-ylmethyl group, R3 represents a carbamoyloxymethyl group optionally substituted by a lower alkyl group, or a heterocyclic thiomethyl group optionally substituted by a suitable substituent, and R4 represents a hydrogen atom or a hydroxy group, and non-toxic salts thereof are rapidly absorbed in blood by oral administration to exhibit an excellent antibacterial effect, thus useful as an oral prophylactic and treating agent against bacterial infection.

Process for the production of penicillins

The invention provides a novel method for producing phenylglycyl chloride hydrochlorides involving reaction of N-substituted phenylglycines with for example thionyl chloride and then gaseous hydrogen chloride, as well as certain novel starting materials for use in this process and certain end-products thereby produced.

CEPHALOSPORINS AND HOMOLOGUES, PREPARATIONS AND PHARMACEUTICAL COMPOSITIONS

... beta-Lactam antibiotics of formula (I) or a salt thereof, wherein R1 is hydrogen, methoxy or formamido; R2 is an acyl group; CO2R3 is a carboxy group or a carboxylate anion, or R3 is a readily removable carboxy protecting group; R4 represents up to four substituents; X is S, SO, SO2, O or CH2; m is 1 or 2; and n is 0, useful in the treatment of bacterial infections in humans and animals.

Способ получения 7-д-(-)-2формилокси-2-(4ацилоксифенилацетамидо)-цефалоспорановых кислот или их солей

Способ получения производных цефалоспорина в виде их аддитивных солей с соляной кислотой

Изобретение касается гетероциклических соединений, в частности антибиотиков иефалоспоринового ряда (ЦС) общей формулы СН -СНS-Шо II I с N-ClCOOR l C-R быть использованы в медицине. Для выявления лучшей акшвности у соединений указанного ряда был разработан способ синтеза ЦС. Получение ЦС ведут из соответствующего цефалоспори- на, где R - Н, и соединения X-R., где X - галоид, при охлаждении (-15 С) в среде Инертного органического растворителя с последующей обработкой этанольньм раствором НС и вьпелением аддитилной соли ПС. Испытания ПС покапывают антим1ткробное действие с л чтим гидролизом и яьтодом из организма . 2 табл. (У) ...

Способ получения 7- -/-/- -амино- -(п-оксифенилацетамидо)-дезацетоксицефалоспорановой кислоты, или ее гидрата или ее соли

Cephalosporine, Verfahren zu ihrer Herstellung und pharmazeutische Präparate.

IMPROVEMENTS WITH REFERENCE TO THE PRODUCTION OF BETA LAKTAME

PROCEDURE FOR the PRODUCTION the NEW ONE 6-D (-) - ALFA AMINO ALFA (P-ACETOXYPHENYL-ACETAMIDO) - PENICILLANSAURE

3-%MORPHOLINOALKOXYIMINOMETHYL<CEPHEM COMPOUNDS

ANTIMICROBIAL COMPOSITION

The invention relates to antimicrobial compositions comprising a combination of vinyl-pyrrolidinone cephalosporin derivatives of the general formula I (see formula I) with carbapenem antibiotics or with .beta.-lactamase inhibitors, to the use of the compositions for producing a medicament for the treatment and prophylaxis of infectious diseases, including MRSA infections, and to pharmaceutical compositions containing the combination.

Crystalline (6r,7r)-7-{2-(5-amino-[1,2,4]thiadiazol-3-yl)-2-[(z)-trityloxyimino]-acetylamino}-3-[(r)-1'-tert-butoxycarbonyl-2-oxo-[1,3']bipyrrolidinyl-(3e)-ylidenemethyl]-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid benzhydryl ester

A solid DMSO solvate of a compound of formula (I) is described, which is a useful intermediate for preparing the broad spectrum antibiotics Ceftobiprole and Ceftobiprole Medocaril.

Cephalosporin esters

3-CEPHEM-4-CARBOXYLIC 3,7-DISUBSTITUTED AND THEIR USE AS ANTIBACTERIAL AGENTS

CRYSTALLINE (6R,7R)-7-｛2-(5-AMINO-[1,2,4]THIADIAZOL-3-YL)-2-[(Z)-TRITYLOXYIMINO]-ACETYLAMINO｝-3-[(R)-1'-TERT-BUTOXYCARBONYL-2-OXO-[1,3']BIPYRROLIDINYL-(3E)-YLIDENEMETHYL]-8-OXO-5-THIA-1-AZA-BICYCLO[4.2.0]OCT-2-ENE-2-CARBOXYLIC ACID BENZHYDRYL ESTER； ITS MANUFACTURE AND USE

CEPHALOSPORIN DERIVATIVES, ITS USE, PROCEDURE TO PREPARE THEM, A PHARMACEUTICAL PREPARATION THAT CONTAINS SUCH USEFUL DERIVATIVE AND COMPOUNDS TO PREPARE THESE DERIVATIVES

Derivados de cefalosporina de la fórmula general (I), en donde: R1 es un grupo elegido entre 2-,3- y 4-hidroxifenilo, 2- y 3-metoxifenilo, 4-carboxifenilo, 4-carbamoilfenilo, 3-trifluorometilfenilo, 2- y 3-fluoro-fenilo, 3-nitrofenilo,3-fluoro-4- hidroxifenilo, 2-fluoro-4-hidroxifenilo, 3-fluoro-2-hidroxifenilo, 3-,4-dihidroxi-fenilo, bencilo, -CHR-fenilo, 3-hidroxibencilo, 4-amino-bencilo, 2-, 3- y 4-fluorobencilo, 2-, 3- y 4-metoxibencilo, 4-nitrobencilo, 4-carboxibencilo,4-trifluorometi lbencilo, 1-naftilo y 2-naftilo, estando todos los sustituyentes hidroxilo, amino, carboxilo y carbamoiloopcionalmente sustituidos, o es piridinilo mono-sustituido por halógeno, pirimidilo, piracinilo di sustituido por alquiloinferior, pirida cinilo mono-sustituido por halógeno, piperidinilo en donde el grupo amino puede estar sustituido por un grupo acilo, tiadiazolilo, oxotetrahidrofuranilo, tiofenilomono-sustituido por alcoxicarbonil inferior o carbamoilo,tetrazolil-alquilo i nferior, tetrahidrofuranil-alquil ...

FORFARANDE FOR FRAMSTELLNING AV 7-D-(-)-ALFA-AMINO-ALFA(P-HYDROXIFENYLACETAMIDO)DESACETOXICEFALOSPORANSYRA

FORFARANDE FOR FRAMSTELLNING AV ANTIBIOTIKA AV CEFALOSPORINTYP.

Способ получения производных цефалоспорина в виде их аддитивных солей с галоидводородными кислотами

Изобретение касается производных цефалоспорина, в частности соединений в D конфигурации общей формулы I n-R4-C H4- ;H(OR)-C(0)-WH-X (l), где X - группа -ОН -C-S -Ср RI (COOR,)CRj, связанный через сложноэфирную связь оста;ток (-f к - или v-аминокислоты, где Шо- группа может быть замещена « л /.. -Ч 1 R J, - 1 - (низший алканоилокси)-С: , -С -апкил; 1-(низший карбокснкар- бонш1окси)-С -С2-алкил; фталндил или 5-метил-1,3,-дирксолен-2-он-4-илме- тил; ЕЗ -(1-метил-1Н-тетразол-5-ш1 тиометил ; (5-метил-1,3,4-тиадиазол- -2-ил)тиометил ; (3-оксипиридазин- -6-ил)тиометил ; (1,3,4-тиадиазол- -2-ил)тиометил ; (1Н-1,2,3-триазол- -5-ил)тиометил или t(1,2,3-тиaди aзoл-5-ил)тиoмeтил ; R - Н, OK, в виде их аддитивных солей с галоид- водородными кислотами, которые могут быть использованы в медицине как лекарственные средства. Для выявления -активности среди производных це- фалоспоринов были получены новые I. Их синтез ведут из соответствующего оксипроизводного цефалоспорина и кислоты общей формулы R -COOH ...

CEPHALOSPORIN-DERIVATE

IMPROVEMENTS IN OR RELATING TO BETA LACTAM PRODUCTION

Cephalosporins and homologues, preparations and pharmaceutical compositions

ANTIBACTERIAL AGENTS

This specification discloses certain novel .alpha.-amino- or .alpha.-formyl-.alpha.-(p-acyloxyphenyl)acetamidocephalosporanic acids which are useful as antibacterial agents, and methods of making them. The novel cephalosporin derivatives of this invention comprise the D-(-) compounds of the formula I wherein Y is hydrogen or S-Het, in which Het represents a 5 or 6 membered heterocyclic ring containing 1 to 4 atoms selected from N, O or S, said heterocyclic ring being optionally substituted by C1-C4 alkyl which may be optionally substituted by a carboxylic acid group or hydroxy, or alkoxyalkyl of up to 4 carbon atoms; R is hydrogen, C1-C10 alkyl optionally substituted by carboxylic acid, or phenyl optionally substituted by C1-C4 alkyl, halogen, nitro, amino or trifluoromethyl; R1 is hydrogen, hydroxy, C1-C4 alkyl, C1-C4 alkoxy or halogen, and pharmaceutically acceptable salts thereof, when substantially free of the L-(+) isomer, and the D-(-) compounds of the formula I(a) I(a) wherein Y ...

PROCESS FOR PRODUCING ANTIBIOTIC COMPOUNDS DERIVED FROM CEPHALOSPORINS

The present invention relates to a process for producing antibiotic compounds derived from cephalosporins having formula ; (I) in which: . The COOA group at the 4 position is an acid radical, or an alkaline or alkaline-earth salt or an amino acid or amine salt, for example triethylamine or ethanolamines, or an easily hydrolyzable or metabolically labile and pharmaceutically acceptable ester radical. X denotes an oxygen atom or a sulfur atom n is zero or 1. R1 and R2 each denote independently hydrogen or a lower alkyl group, preferably a methyl group, or R1 and R2 taken together with the carbon atom to which they are linked form a cyclobutyl or cyclopentyl nucleus. B is the residue of a primary or secondary amine, said process consists of acylating 4-tertiobutyl-l-S-oxide 7-amino-3-bromomethyl 3-cepheme carboxylate (II) with the acid(IlI) to obtain the compound (IV) described in European patent application 60745 and of adding to compound (IV) an acid B-(CH2)n-COOH or B(CH2)nCOSH.

CEPHALOSPORIN DERIVATIVES, METHODS OF PRODUCTION THEREOF AND PROPHYLACTIC AND THERAPEUTIC AGENTS FOR BACTERIAL INFECTION

A cephalosporin derivative of the general formula (I) wherein R1 is an .alpha.=, .beta.- or .gamma.-amino acid residue (bonded by the ester linkage), which may optionally be substituted by one or two lower alkyl groups at the amino group thereof, R2 is an 1-alkanoyloxyalkyl, 1-alkoxycarbonyloxyalkyl, phthalidyl or 5-methyl-1,3-dioxolen-2-on-4-ylmethyl group, R3 is a carbamoyloxymethyl group, which may optionally be substituted by one or two lower alkyl groups, or a heterocyclothiomethyl group, which may optionally be substituted by one or more appropriate substituents, and R4 is a hydrogen atom or a hydroxy group, or its non-toxic salt are found to be useful as orally administrable antibiotics having broad antimicrobial activities against both grampositive and gram-negative bacteria.

NOVEL CEPHALOSPORIN ANTIBIOTICS OF THE GROUP AND METHODS FOR THEIR MANUFACTURE

NOVEL (A-(N-ACYLAMINO) A-ARYL ACETAMIDO) -7 CEPHALOSPORINS, PARTICULARLY USEFUL AS ANTIMICROBIALS, AND THEIR PREPARATION

CEPHALOSPORINS AND HOMOLOGUES, PREPARATIONS AND PHARMACEUTICAL COMPOSITIONS

... beta-Lactam antibiotics of formula (I) or a salt thereof, wherein R1 is hydrogen, methoxy or formamido; R2 is an acyl group; CO2R3 is a carboxy group or a carboxylate anion, or R3 is a readily removable carboxy protecting group; R4 represents up to four substituents; X is S, SO, SO2, O or CH2; m is 1 or 2; and n is 0, useful in the treatment of bacterial infections in humans and animals.

Crystalline (6R,7R)-7-{2-(5-amino-[1,2,4] thiadiazol-3-yl)-2-[(Z)-trityloxyimino]-acetylamino}-3-[(R)-1-tert-butoxycarbonyl-2-oxo-[1,3]bipyrrolidinyl-(3E)-ylidenemethyl]-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid benzhydryl ester; its manufacture and use

A solid DMSO solvate of a compound of formula (I) is described, which is a useful intermediate for preparing the broad spectrum antibiotics Ceftobiprole and Ceftobiprole Medocaril.

Intermediates in the synthesis of cephalosporin compounds

Described herein are crystalline forms of a compound of formula (III′), including toluene solvates of TATD-CLE, as well as processes for the preparation thereof and use thereof in the preparation of cephalosporin compounds such as ceftolozane.

ANTIBIOTIKA VOM CEPHALOSPORINTYP, VERFAHREN ZU IHRER HERSTELLUNG UND ARZNEIMITTEL

Vinylpyrrolidone cephalosporin derivatives

Antimicrobial composition

3-(Morpholinoalkoxyiminomethyl)cephem compounds

7-DI-SUBSTITUTED-ACETAMIDS-CEPHEM

VINYLPYRROLIDINON CEPHALOSPORIN DERIVATIVES

The present invention relates to cephalosporin derivatives of the general formula (see fig. I) where R1 is halogen, lower alkyl, phenyl, benzyl, styryl, naphthyl or heterocyclyl; the lower alkyl, phenyl, benzyl, styryl, naphthyl and heterocyclyl being optionally substituted by at least one of halogen, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkoxy, optionally substituted phenyl, amino, lower alkylamino, di-lower alkylamino, carboxy, lower alkylcarboxy, carbamoyl or lower alkylcarbamoyl; R4, R5 independently are hydrogen, lower alkyl or phenyl; X is S, O, NH or CH2; n is 0, 1 or 2; m is 0 or 1; s is 0 or 1; R2 is hydrogen, hydroxy, -CH2-CONHR6, lower alkyl-Qr, cycloalkyl-Qr, lower alkoxy, lower alkenyl, cycloalkenyl-Qr, lower alkynyl, aralkyl-Qr, aryl-Qr, aryloxy, aralkoxy, a heterocyclic ring or a heterocyclyl-Qr, the lower alkyl, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aralkyl, aryl, aryloxy, aralkoxy and the heterocyclic ...

NEW COMPOSE ANTIBIOTIC DERIVED FROM THE CEPHALOSPORINES