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公开(公告)号:NZ208064A
公开(公告)日:1987-07-31
申请号:NZ20806484
申请日:1984-05-04
Applicant: HOECHST AG
Inventor: SCHWAB W , DURCKHEIMER W , KIRRSTETTER R , LATTRELL R
IPC: C07D501/04 , A61K31/425 , A61K31/545 , C07D20060101 , C07D501/00 , C07D501/06 , C07D501/38 , C07D501/46 , C07D501/56 , C07D501/57
Abstract: Process for the preparation of cephem compounds of the formula
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公开(公告)号:YU76784A
公开(公告)日:1986-12-31
申请号:YU76784
申请日:1984-04-27
Applicant: HOECHST AG
Inventor: KIRRSTETTER R , LATTRELL R , SCHWAB W
IPC: A61K31/425 , A61K31/545 , C07D20060101 , C07D501/00 , C07D501/04 , C07D501/06 , C07D501/38 , C07D501/46 , C07D501/56 , C07D501/57 , C07D519/00
Abstract: Process for the preparation of cephem compounds of the formula wherein R is optionally substituted aminothiazolyl or amino-1,2,4-thiadiazolyl, A is optionally substituted pyridinium, R1 is hydrogen or methoxy and R2 are special aliphatic substituents, by a nucleophilic replacement in the substituent in 3-position in the presence of tri-C1C4-alkyl iodosilane.
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公开(公告)号:NZ203436A
公开(公告)日:1986-06-11
申请号:NZ20343683
申请日:1983-03-02
Applicant: HOECHST AG
Inventor: LATTRELL R , KIRRSTETTER R , SCHWAB W , DURCKHEIMER W , SEIBERT G
IPC: C07D501/36 , A61K31/545 , A61K31/546 , A61P31/04 , C07D277/20 , C07D501/34 , C07D501/46 , C07D501/00
Abstract: The invention relates to cephem derivatives of the general formula I and their physiologically acceptable acid addition salts, to pharmaceutical formulations active against bacterial infections, to processes for preparing the compounds and formulations, and to the use of the compounds for combating bacterial infections.
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公开(公告)号:NZ206659A
公开(公告)日:1986-11-12
申请号:NZ20665983
申请日:1983-12-21
Applicant: HOECHST AG
Inventor: LATTRELL R , DURCKHEIMER W , KIRRSTETTER R , SCHWAB W , KLESEL N
IPC: A01N20060101 , A01N43/78 , A01N43/86 , A61K20060101 , A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D501/20 , C07D501/46 , C07D501/56 , C07D501/57
Abstract: For the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE 1. Cephem derivatives of the general formula see diagramm : EP0111935,P10,F1 and physiologically acceptable acid addition salts thereof in which R**1 denotes hydrogen, R**2 denotes hydrogen, R**3 denotes C1 -C4 -alkyl optionally substituted by fluorine, A denotes a quinolinium or an isoquinolinium radical, each of which can also be substituted once or twice by C1 -C4 -alkyl and in which the R**3O group is in the syn position. For the Contracting State : AT A process for the preparation of cephem derivatives of the general formula I see diagramm : EP0111935,P11,F1 and physiologically acceptable acid addition salts thereof in which R**1 denotes hydrogen, R**2 denotes hydrogen, R**3 denotes C1 -C4 -alkyl optionally substituted by fluorine, A denotes a quinolinium or an isoquinolinium radical, each of which can also be substituted once or twice by C1 -C4 -alkyl and in which the R**3O group is in the syn position, which comprises a) reacting a compound of the general formula II see diagramm : EP0111935,P11,F2 or salts thereof or a reactive derivative of the compound II in which R**1, R**2 and R**3 have the abovementioned meaning and R**8 denotes an amino group or a protected amino group and R**9 denotes a group which can be replaced by quinoline, isoquinoline or substituted quinolines or isoquinolines corresponding to the radicals A of the formula I, with quinoline, isoquinoline or one of their derivatives, and alpha) splitting off a protective group which is present where appropriate and beta) if necessary, converting the resulting product into a physiologically acceptable acid addition salt, or b) reacting a 7-aminocephen compound of the general formula III see diagramm : EP0111935,P12,F3 or acid addition salts thereof in which R**2 and A have the abovementioned meaning, it also being possible for the amino group to be present in the form of a reactive derivative, with a 2-(2-aminothiazol-4-yl)-2-syn-oximinoacetic acid of the general formula IV see diagramm : EP0111935,P12,F4 in which R**1, R**3 and R**8 have the above meaning, or with an activated derivative of this compound, and alpha) splitting off a protective group which is present where appropriate and beta) if necessary, converting the resulting product into a physiologically acceptable acid addition salt
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公开(公告)号:YU76684A
公开(公告)日:1986-10-31
申请号:YU76684
申请日:1984-04-27
Applicant: HOECHST AG
Inventor: SCHWAB W , DUERCKIEIMER W , KIRRSTETTER R , LATTRELL R
IPC: C07D501/04 , A61K31/425 , A61K31/545 , C07D20060101 , C07D501/00 , C07D501/06 , C07D501/38 , C07D501/46 , C07D501/56 , C07D501/57
Abstract: Process for the preparation of cephem compounds of the formula
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公开(公告)号:NZ208065A
公开(公告)日:1986-10-08
申请号:NZ20806584
申请日:1984-05-04
Applicant: HOECHST AG
Inventor: KIRRSTETTER R , DURCKHEIMER W , LATTRELL R , SCHWAB W
IPC: A61K31/425 , A61K31/545 , C07D20060101 , C07D501/00 , C07D501/04 , C07D501/06 , C07D501/38 , C07D501/46 , C07D501/56 , C07D501/57 , C07D519/00
Abstract: Process for the preparation of cephem compounds of the formula wherein R is optionally substituted aminothiazolyl or amino-1,2,4-thiadiazolyl, A is optionally substituted pyridinium, R1 is hydrogen or methoxy and R2 are special aliphatic substituents, by a nucleophilic replacement in the substituent in 3-position in the presence of tri-C1C4-alkyl iodosilane.
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公开(公告)号:YU45965B
公开(公告)日:1992-12-21
申请号:YU76684
申请日:1984-04-27
Applicant: HOECHST AG
Inventor: SCHWAB W , DUERCKHEIMER W , KIRRSTETTER R , LATTRELL R
IPC: C07D501/04 , A61K31/425 , A61K31/545 , C07D20060101 , C07D501/00 , C07D501/06 , C07D501/38 , C07D501/46 , C07D501/56 , C07D501/57
Abstract: POSTOPEK ZA PRIPRAVO CEFEMSKIH SPOJIN, s splošno formulo kjer pomeni R tiazolilni ostanek ali 1,2,4-tiadiazolilni ostanek v katerih stoji R3 za vodik in B za amino skupino, in kjer pomeni R1 vodik, R2 metilno skupino, A kinolinijev ostanek , izokinolinijev ostanek metilkinolinijev ostanek ali priridinijev ostanek , ciklopenteno-ali ciklohekseno-piridinijev ostanek ali metilpiridinijev ostanek in v kateri stoji skupina R2-O v sin legi, označen s tem, da spojino s splošno formulo II kjer ima R1 v formuli I navedeni pomen, R7 pomeni skupino, ki se da zamenjati s tisto bazo, ki ustreza ostankom A v formuli I in R8 stoji za vodik ali zaščitno skupino za amino, presnovimo v aprotonskem topilu pri temperaturah med +10 in +80В° C z bazo, ki je osnova v formuli I definiranega ostanka A, in v prisotnosti tri-C1-C4-alkiljodosilana, pri čemer dodamo bazo v stehiometrični množini ali do dvajsetkratnem prebitku, ob tvorbi spojine s splošno formulo III, v kateri imajo R1, R8 in A zgoraj navedeni pomen, in a) v danem primeru prisono zaščitno skupino za amino odcepimo in b) spojino III, kjer pomeni R8 vodik, bodisi kot tako ali v obliki reakcijsko sposobnega derivata presnovimo z 2-sin-oksiminoocetno kislino s splošno formulo IV kjer imata R in R2 navedeni pomen, ali z derivatom te spojine, aktiviranim na karbonilni skupini. Prijava vsebuje še 1 odvisen zahtevek i 1 neovisen zahtevek.
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公开(公告)号:YU45966B
公开(公告)日:1992-12-21
申请号:YU76784
申请日:1984-04-27
Applicant: HOECHST AG
Inventor: KIRRSTETTER R , LATTRELL R , SCHWAB W , DUERCKHEIMER W
IPC: A61K31/425 , A61K31/545 , C07D20060101 , C07D501/00 , C07D501/04 , C07D501/06 , C07D501/38 , C07D501/46 , C07D501/56 , C07D501/57 , C07D519/00
Abstract: POSTOPEK ZA PRIPRAVO CEFEMSKIH SPOJIN, s splošno formulo I kjer pomeni R tiazolilni ostanek ali 1,2,4-tiadiazolilni ostanek v katerih stojita R3 za vodik ali halogen in B za v danem primeru substituirano amino skupino, in kjer pomeni R1 vodik, R2 nižji alkil, karboksi-nižjialkil, A kinilinijev ali izokinolinijev ostanek ki sta lahko tudi enkrat substituirana z metilom, ali fenantridinijev ostanek ali priridinijev ostanek ki je lahko enkrat ali dvakrat, enako ali različno substituiran z nižjim alkilom, ki je lahko substituiran s sulfo ali metoksi, pri čemer sta lahko 2 alkilni skupini, ki stojita v legi orto, tudi sklenjeni v tri- ali tetrametilenski obroč, v katerem je lahko en obročni ogljikov atom tudi nadomešćen z atomom kisika ali žvepla in v katerem se nadalje lahko nahaja še ena dvojna vez, z metoksi, s halogenom, s fenilom ali s karbamoilom, in v kateri stoji skupina R2O v sin legi, označen s tem, da spojino s splošno formulo II ali njene soli, jer imajo R, R2, R2 pomen, naveden v formuli I, in R7 pomeni skupino, ki se jo da zamenjati s tisto bazo, ki ustreza ostankom A formule I, presnovimo v aprotonskem topilu pri temperaturah med +10 in +80В° C s to bazo v prisotnosti tri-C1-C4-alkiljodosilana, pri čemer dodamo bazo v stehiometrični množini ali do dvajsetkratnem prebitku, in a) v danem primeru prisotno zaščitno skupino odcepimo in b) po potrebi dobljeni produkt prevedemo v fiziološko prenesljivo kislinsko adicijsko sol. Prijava vsebuje še 1 ovisen zahtevek i 1 neovisen zahtevek.
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