公开(公告)号：DE2359402A1

公开(公告)日：1975-06-05

申请号：DE2359402

申请日：1973-11-29

Applicant: HOECHST AG

Inventor： BORMANN DIETER DIPL CHEM DR ,  WORM MANFRED DIPL CHEM DR

IPC: C07D501/04 ,  A61K31/545 ,  C07D20060101 ,  C07D501/18 ,  C07D501/60

公开(公告)号：DE2243242A1

公开(公告)日：1974-03-28

申请号：DE2243242

申请日：1972-09-02

Applicant: HOECHST AG

Inventor： BAUERSCHMIDT EBERHARD DIPL CHE ,  BORMANN DIETER DIPL CHEM DR ,  WORM MANFRED DIPL CHEM DR

IPC: C07D501/04 ,  C07D20060101 ,  C07D501/16 ,  C07D501/18 ,  C07D99/24

公开(公告)号：DE3028198A1

公开(公告)日：1982-02-25

申请号：DE3028198

申请日：1980-07-25

Applicant: HOECHST AG

Inventor： WORM MANFRED DIPL CHEM DR ,  MUTH KARL DIPL CHEM DR

IPC: C07D209/08 ,  C07D211/32 ,  C07D401/06 ,  A61K31/40 ,  A61K31/445

公开(公告)号：DE2651386A1

公开(公告)日：1978-05-18

申请号：DE2651386

申请日：1976-11-11

Applicant: HOECHST AG

Inventor： BORMANN DIETER DIPL CHEM DR ,  KNABE BERND DIPL CHEM DR ,  SCHRINNER ELMAR DR ,  WORM MANFRED DIPL CHEM DR

IPC: A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D271/10 ,  C07D271/107 ,  C07D501/20 ,  C07D519/06

公开(公告)号：DE2641060A1

公开(公告)日：1978-03-16

申请号：DE2641060

申请日：1976-09-11

Applicant: HOECHST AG

Inventor： SCHORR MANFRED DIPL CHEM DR ,  SCHRINNER ELMAR DR ,  WORM MANFRED DIPL CHEM DR ,  SCHMITT WILFRIED

IPC: C07D235/12 ,  C07D235/18 ,  C07D471/04 ,  C07D499/64 ,  C07D501/20 ,  C07D499/70 ,  A61K31/43 ,  A61K31/545

Abstract: Beta-Lactam cpds. of formula (I) and their acceptable salts and esters are new. In (I) X is of formula (H) or (J) R1 is H, opt. substd. alkyl, aryl or heterocyclic gp; R2 and R4 are H or lower alkyl; R3 and R5 are H, halogen, lower alkyl or alkoxy; A is CH or N; B is a single bond or methyleneoxy; C is a single bond, or phenylene; D is a single bond, lower alkylene or oxyalkylene; Y is opt. substd. Ph, opt. substd. monocyclic aromatic heterocyclic gp. or dihydrophenyl; and Z is of formula (K) or (L) E is H, acetoxy of S-G; G is an opt. substd. heterocyclic gp.). Typical cpds. are 6 D-2-(4-(benzimidazol-2-yl)phenoxyacetylamino-2-phenyl-acetylami- no -penicillanic acid and 7 D-2-(2-(4-fluorophenyl)-benzimidazol-5-yl-carbonylamino)-2-phen- ylacetyl-amino -cephalosporanic acid.

公开(公告)号：DE2710902A1

公开(公告)日：1978-09-21

申请号：DE2710902

申请日：1977-03-12

Applicant: HOECHST AG

Inventor： BORMANN DIETER DIPL CHEM DR ,  KNABE BERND DIPL CHEM DR ,  SCHRINNER ELMAR DR ,  WORM MANFRED DIPL CHEM DR

IPC: A61K31/44 ,  A61K31/535 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D277/20 ,  C07D277/38 ,  C07D277/40 ,  C07D463/00 ,  C07D501/20 ,  C07D505/00

Abstract: Cephem derivatives of the formula in which R1 denotes hydrogen or low-molecular alkoxy, R2 denotes hydrogen, optionally substituted alkyl, phthalide or a cation, X denotes sulfur, oxygen or CH2 and A denotes hydrogen, alkoxy, halogen or a group -CH2Y, in which Y represents hydrogen, acyloxy, alkoxy, optionally substituted carbamoyloxy or a group -SR3, in which R3 can represent acyl, alkyl or an optionally substituted 5-membered or 6-membered heterocyclic structure are disclosed as valuable antibiotics which are well suited for combating Gram-positive and in particular Gram-negative infections and also have an unexpectedly good action against penicillinase-forming staphylococci.

公开(公告)号：DE2634082A1

公开(公告)日：1978-02-02

申请号：DE2634082

申请日：1976-07-29

Applicant: HOECHST AG

Inventor： BORMANN DIETER DIPL CHEM DR ,  KNABE BERND DIPL CHEM DR ,  SCHRINNER ELMAR DR ,  WORM MANFRED DIPL CHEM DR

IPC: C07D20060101 ,  C07D501/20

Abstract: Cephalosporins of formula (I): (where n = 0 or 1, R1-3 are H or 1-5C alkyl but not 4-5C alkyl when n = 1, R4 is H, opt. substd. alkyl, phthalidyl or a cation, R5 is H or 1-3C alkyl A is H, alkoxy, halogen, or CH2Y, Y is H, acyloxy, alkoxy, opt. substd. pyridinium, opt. substd. carbamoyloxy or SR6, R6 is acyl, alkyl or an opt. substd. 5- or 6-membered heterocycle opt. fused with a 5- or 6-membered aromatic ring) are novel. Cpds. (I) are antibiotics active against Gram-positive and -negative bacteria, including penicillinase-producing Staphylococci. A typical cpd. is 7-(3-butenylamino)-cephalosporanic acid. In an example, this is prepd. from 3-butenoic acid and 7-aminocephalosporanic acid.

公开(公告)号：DE2626418A1

公开(公告)日：1977-12-22

申请号：DE2626418

申请日：1976-06-12

Applicant: HOECHST AG

Inventor： BORMANN DIETER DIPL CHEM DR ,  KNABE BERND DIPL CHEM DR ,  SCHRINNER ELMAR DR ,  WORM MANFRED DIPL CHEM DR

IPC: A61K31/43 ,  A61K31/545 ,  C07D499/48 ,  C07D501/20

Abstract: Beta-Lactam derivs. of formula (I) are new. In (I) n = 1-4, Z = C(CH3)2 or -CH2.C(A)=R = H, opt. substd. alkyl, phthalide residue or a cation. A = H, alkoxy, halo or CH2Y. Y = H, acyloxy, alkoxy, opt. substd. pyridinium, opt. substd. carbamoyl (in which the substits. may complete a ring) or SR1. R1 = acyl, alkyl, or an opt. substd. 5 or 6 membered heterocycle which may be fused to a 5 or 6 membered aromatic ring. (I) are antibiotics effective against Gram positive and negative bacteria including penicillinase-producing Staphylococci. They are administered in usual oral or pref. parenteral formulations. In an example, 7-(3,3,3-trifluoropropionylamino)cephalosporanic acid was prepd. from 7-ACA and 3,3,3-trifluoropropionyl chloride.

公开(公告)号：DE2316541A1

公开(公告)日：1974-10-24

申请号：DE2316541

申请日：1973-04-03

Applicant: HOECHST AG

Inventor： SCHORR MANFRED DIPL CHEM DR ,  WORM MANFRED DIPL CHEM DR ,  SCHRINNER ELMAR DR

IPC: C07D501/00 ,  C07D501/22 ,  C07D99/24

Abstract: Title compds are of formula I: (where R', R2 and R3=H or 1-5C alkyl, or R1 + R2 tog. = opt. subst. alkylene; R4=1-5C alkyl or 3-7C cycloalkyl opt. contg a heteroatom; X=NH or a single bond; A= opt. subst. phenylene or thienyl; and Y = O or a single bond. I are prepd. by acylating a 7-aminoceph-3-em carboxylic acid, salt or ester, with a suitably activated acid deriv.

公开(公告)号：DE2651395A1

公开(公告)日：1978-05-18

申请号：DE2651395

申请日：1976-11-11

Applicant: HOECHST AG

Inventor： BORMANN DIETER DIPL CHEM DR ,  KNABE BERND DIPL CHEM DR ,  SCHRINNER ELMAR DR ,  WORM MANFRED DIPL CHEM DR

IPC: A61K31/545 ,  C07D501/20

Abstract: Cephalosporins of formula (I): (where n = 0 or 1, R1-3 are H or 1-5C alkyl but not 4-5C alkyl when n = 1, R4 is H, opt. substd. alkyl, phthalidyl or a cation, R5 is H or 1-3C alkyl A is H, alkoxy, halogen, or CH2Y, Y is H, acyloxy, alkoxy, opt. substd. pyridinium, opt. substd. carbamoyloxy or SR6, R6 is acyl, alkyl or an opt. substd. 5- or 6-membered heterocycle opt. fused with a 5- or 6-membered aromatic ring) are novel. Cpds. (I) are antibiotics active against Gram-positive and -negative bacteria, including penicillinase-producing Staphylococci. A typical cpd. is 7-(3-butenylamino)-cephalosporanic acid. In an example, this is prepd. from 3-butenoic acid and 7-aminocephalosporanic acid.