公开(公告)号：US4035359A

公开(公告)日：1977-07-12

申请号：US599266

申请日：1975-07-25

申请人： Burton G. Christensen ,  Lovji D. Cama

发明人： Burton G. Christensen ,  Lovji D. Cama

IPC分类号： C07C57/38 ,  C07C57/72 ,  C07D499/00 ,  C07D499/58 ,  C07D499/46

CPC分类号： C07D499/00 ,  C07C57/38 ,  C07C57/72

摘要： Novel 6-methoxy and 6-thioalkyl-6-acylamido-penicillanic acids and their non-toxic pharmaceutically-acceptable salts, esters and amides which are useful as antibiotics. The products are prepared by treating an ester of 6-substituted-6-aminopenicillanic acid with an acylating agent followed by removal of the ester group. Also disclosed are novel intermediates.

摘要翻译： 新的6-甲氧基和6-硫烷基-6-酰氨基 - 青霉烷酸及其无毒的药学上可接受的盐，酯和酰胺，其可用作抗生素。 通过用酰化剂处理6-取代-6-氨基青霉烷酸的酯，然后除去酯基来制备产物。 还公开了新型中间体。

公开(公告)号：US3994885A

公开(公告)日：1976-11-30

申请号：US545451

申请日：1975-01-30

申请人： Gary A. Koppel

发明人： Gary A. Koppel

IPC分类号： C07D499/04 ,  A61K31/43 ,  A61P31/04 ,  C07D20060101 ,  C07D499/00 ,  C07D499/21 ,  C07D499/32 ,  C07D499/44 ,  C07D499/46 ,  C07D499/60 ,  C07D499/62 ,  C07D499/64 ,  C07D499/68 ,  C07D499/70 ,  C07D499/74 ,  C07D499/80 ,  C07D501/20 ,  C07D501/57 ,  C07D501/60 ,  C07D513/20

CPC分类号： C07D501/57 ,  C07D499/00 ,  C07D499/44

摘要： 6-Alkoxylated-6-acylamidopenicillanic acids and 7-alkoxylated-7-acylamidocephalosporin acids and esters thereof, are provided by reacting a 6-acylamidopenicillanic acid ester or a 7-acylamidocephalosporin ester under anhydrous conditions at -90.degree. C. to -15.degree. C. with an alkali metal salt of a lower alkyl alcohol in the presence of an excess of the corresponding alcohol to produce, in situ, the anionic form of the antibiotic which on halogenation with a positive halogen compound, e.g. t-butyl hypochlorite, yields the compound of the invention. Compounds of the invention, e.g. 6-methoxy-6-phenoxyacetamidopenicillanic acid and 7-methoxy-7-[2-(2-thienyl)acetamido]cephalosporanic acid are useful antibiotics.

摘要翻译： 6-烷氧基化-6-酰氨基青霉烷酸和7-烷氧基化-7-酰基酰氨基头孢菌素酸及其酯通过6-酰基氨基青霉烷酸酯或7-酰基酰氨基头孢菌素酯在-90℃至-15℃的无水条件下反应来提供 用低级烷基醇的碱金属盐在过量相应的醇的存在下，原位生成阴离子形式的抗生素，其用正卤素化合物卤化，例如 叔丁基次氯酸盐，得到本发明的化合物。 本发明的化合物，例如 6-甲氧基-6-苯氧基乙酰氨基青霉烷酸和7-甲氧基-7- [2-（2-噻吩基）乙酰氨基]头孢烷酸是有用的抗生素。

公开(公告)号：US3974142A

公开(公告)日：1976-08-10

申请号：US502956

申请日：1974-09-03

申请人： Hans-Bodo Konig ,  Wilfried Schrock ,  Karl-Georg Metzger

发明人： Hans-Bodo Konig ,  Wilfried Schrock ,  Karl-Georg Metzger

IPC分类号： C07D233/38 ,  C07D275/02 ,  C07D333/34 ,  C07D499/00 ,  C07D499/64 ,  C07D499/46

CPC分类号： C07D275/02 ,  C07D233/38 ,  C07D333/34 ,  C07D499/00

摘要： Arylmethyl- and cyclohexenylmethyl- penicillins, substituted on the .alpha.carbon atom of the side chain by a 2,3-disubstituted imidazolidinylcarbamido or a 2,3-disubstituted imidazolidinylthiocarbamido group, or by the corresponding 2,3-disubstituted 1,3-diazacyclohexylcarbamido or thiocarbamido groups are anti-bacterial agents.

摘要翻译： 通过2,3-二取代的咪唑烷基氨基甲酰基或2,3-二取代的咪唑烷基硫代氨基甲酰基取代在侧链的α碳原子上的芳基甲基 - 和环己烯基甲基 - 青霉素，或通过相应的2,3-二取代的1,3-二氮杂环己基氨基甲酰基或 硫代氨基甲酰基是抗菌剂。

公开(公告)号：US3959259A

公开(公告)日：1976-05-25

申请号：US621174

申请日：1975-10-09

申请人： Hermann Breuer

发明人： Hermann Breuer

IPC分类号： C07D271/06 ,  C07D271/07 ,  C07D499/00 ,  C07D499/46 ,  C07D499/76

CPC分类号： C07D271/07 ,  C07D499/00

摘要： 1,2,4-Oxadiazolonylacetyl penicillins and cephalosporins of the general formula ##SPC1##Wherein A is either ##SPC2##R.sub.1 is hydrogen, lower alkyl or phenyl-lower alkyl; R.sub.2 is hydrogen, lower alkyl, phenyl, hydroxyphenyl, thienyl, furyl, or pyridyl; R.sub.3 is hydrogen, lower alkyl, phenyl-lower alkyl, a salt forming ion, trimethylsilyl, benzhydryl, or ##EQU1## R.sub.4 is lower alkyl, phenyl or phenyl-lower alkyl; and X is hydrogen, lower alkoxy, lower alkanoyloxy, lower alkylmercapto, the radical of a nitrogen base, or certain heterocyclic thio moieties; are disclosed. They are useful as antibacterial agents.

摘要翻译： 1,2,4-恶二唑乙酰基青霉素和通式为WHEREIN A的头孢菌素是R 1是氢，低级烷基或苯基 - 低级烷基; R2是氢，低级烷基，苯基，羟基苯基，噻吩基，呋喃基或吡啶基; R3是氢，低级烷基，苯基 - 低级烷基，成盐离子，三甲基甲硅烷基，二苯甲基或O并行-CH 2 -O-C-R 4; R4是低级烷基，苯基或苯基 - 低级烷基; X是氢，低级烷氧基，低级烷酰氧基，低级烷基巯基，氮碱基或某些杂环硫基; 被披露。 它们可用作抗菌剂。

公开(公告)号：US3939149A

公开(公告)日：1976-02-17

申请号：US426188

申请日：1973-12-19

申请人： Hans-Bodo Konig ,  Wilfried Schrock ,  Hans Disselnkotter ,  Karl Georg Metzger

发明人： Hans-Bodo Konig ,  Wilfried Schrock ,  Hans Disselnkotter ,  Karl Georg Metzger

IPC分类号： A61K31/43 ,  C07C275/60 ,  C07D499/64 ,  C07D499/46

CPC分类号： C07D499/64 ,  A61K31/43 ,  C07C275/60 ,  C07D499/68

摘要： 6-(.alpha.-3-Acyl-ureidoacetamido)-penicillanic acids and pharmaceutically acceptable non-toxic salts thereof in which the hydrogen atom of the nitrogen atom present in the 3-position is substituted, are effective against Gram-positive and Gram-negative infections, particularly Klebsiella aerobacter infections.

公开(公告)号：US3937699A

公开(公告)日：1976-02-10

申请号：US467823

申请日：1974-05-07

申请人： Tsunehiko Asako ,  Takenobu Soma ,  Hirotomo Masuya ,  Tadatsugu Harukawa ,  Takuichi Miki

发明人： Tsunehiko Asako ,  Takenobu Soma ,  Hirotomo Masuya ,  Tadatsugu Harukawa ,  Takuichi Miki

IPC分类号： C07D499/46 ,  C07D499/66

CPC分类号： C07D501/20 ,  C07D499/64 ,  C07D499/66 ,  C07D501/22 ,  C07D501/32

摘要： 6-(1'-CYCLOHEXENYLGLYCINAMIDO)PENICILLANIC ACID AND SALTS THEREOF, WHICH HAVE BOTH A BROAD SPECTRUM ANTIBACTERIAL ACTION AND STRONG ACTIVITY AGAINST Escherichia coli.

公开(公告)号：US3923789A

公开(公告)日：1975-12-02

申请号：US46122774

申请日：1974-04-15

申请人： BAYER AG

发明人： SCHROCK WILFRIED ,  METZGER KARL-GEORG ,  KONIG HANS-BODO

IPC分类号： C07D499/66 ,  A23K20/195 ,  A61K31/50 ,  A61P31/04 ,  C07D231/08 ,  C07D231/20 ,  C07D499/00 ,  C07D499/12 ,  C07D499/16 ,  C07D499/64 ,  C07D499/68 ,  C07D499/70 ,  C07D499/46

CPC分类号： C07D231/20 ,  C07D231/08 ,  C07D499/00

摘要： A compound of the formula:

OR A PHARMACEUTICALLY ACCEPTABLE NONTOXIC SALT THEREOF WHEREIN R1 is hydrogen, straight or branched chain alkyl of one to five carbon atoms, monoaralkyl of up to eight carbon atoms, monoaryl, substituted monoaryl, or thienyl; A is a moiety of the formula:

wherein R2, R3, R4, R5, R6 and R7 are the same or different and each is hydrogen, straight or branched chain alkyl of one to five carbon atoms, monoaralkyl of up to eight carbon atoms, monoaryl, substituted monoaryl, or thienyl; B is a moiety of the formula:

WHEREIN R8, R9 and R10 are the same or different and each is hydrogen, fluorine, chlorine, bromine, iodine, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulphonyl, sulphamyl, nitro, cyano, di(lower alkyl)amino, lower alkanoylamino, lower alkanoyloxy, lower alkylsulphonylamino, trifluoromethyl or hydroxy; E is oxygen or sulphur; and C* is a carbon atom constituting a center of chirality, ARE USEFUL FOR THEIR ANTIBACTERIAL ACTIVITY.

公开(公告)号：US3891635A

公开(公告)日：1975-06-24

申请号：US19548271

申请日：1971-11-03

申请人： KONINKLIJKE GIST SPIRITUS

发明人： HENNIGER PETER WOLFGANG ,  SMID PETER MAX

IPC分类号： C07D499/04 ,  A61K31/431 ,  A61K31/546 ,  A61P31/04 ,  C07D261/08 ,  C07D499/00 ,  C07D499/44 ,  C07D499/46 ,  C07D499/58 ,  C07D499/70 ,  C07D499/72 ,  C07D501/04 ,  C07D501/20 ,  C07D501/22 ,  C07D501/34 ,  C07D501/46 ,  C07D99/24

CPC分类号： C07D261/08 ,  C07D499/00

摘要： Novel heterocyclic amides of the formula

WHEREIN R is selected from the group consisting of lower alkyl and aryl optionally substituted with at least one member of the group consisting of chlorine, fluorine, nitro, amino and lower alkyl and a tertiary alkyl group, R1 is selected from the group consisting of hydrogen, lower alkyl, carboxyl, lower alkoxycarbonyl, an alkali metal, alkaline earth metal or amine salt of carboxyl, a carbamyl, cyano, an amino and chlorine, R2 is selected from the group consisting of hydrogen, cyano, halogen, an amino, lower aralkoxycarbonylamino, lower alkyl, carboxyl esterified with lower alkyl, aryl or aralkyl and carbamoyl optionally substituted on the nitrogen atom with lower alkyl or a phenyl and Q is selected from the group consisting of

X is selected from the group consisting of hydrogen, hydroxy and lower alkanoyloxy and U is selected from the group consisting of amido forming groups or a group OY, wherein Y is selected from the group consisting of hydrogen, salt forming groups, and ester forming groups, or COOY and CH2X together form a lactone or lactam, having antibacterial properties, their preparation and novel intermediates thereof.

摘要翻译： 式WHEREIN R的新型杂环酰胺选自由任选被氯，氟，硝基，氨基和低级烷基和叔烷基中的至少一个成员取代的低级烷基和芳基，选择R1 由氢，低级烷基，羧基，低级烷氧基羰基，羧基的碱金属，碱土金属或胺盐组成的组，氨基甲酰基，氰基，氨基和氯，R2选自氢，氰基， 卤素，氨基，低级芳烷氧基羰基氨基，低级烷基，被低级烷基，芳基或芳烷基酯化的羧基和在氮原子上被低级烷基或苯基取代的氨基甲酰基，Q选自X选自 的氢，羟基和低级烷酰氧基，U选自酰氨基形成基团或基团OY，其中Y选自hy 氢，成盐基团和酯形成基团，或COOY和CH2X一起形成具有抗菌性质的内酯或内酰胺，其制备及其新型中间体。

公开(公告)号：US3891628A

公开(公告)日：1975-06-24

申请号：US26278672

申请日：1972-06-14

申请人： KONINKLIJKE GIST SPIRITUS

发明人： SMID PETER MAX ,  KALTER JAN

IPC分类号： C07D261/18 ,  C07D499/00 ,  C07D499/46 ,  C07D499/76 ,  C07D501/20 ,  C07D501/22 ,  C07D501/34 ,  C07D99/16 ,  C07D99/24

CPC分类号： C07D261/18 ,  C07D499/00 ,  Y02P20/55

摘要： A new process for the preparation of penicillins and cephalosporins with a heterocyclic side chain, to novel products so obtained and to pharmaceutical compositions containing them, and to a new process for the preparation of penicillin and cephalosporin derivatives useful as intermediates in the aforesaid process.

摘要翻译： 用于制备具有杂环侧链的青霉素和头孢菌素的新方法，如此获得的新产品和含有它们的药物组合物的新方法，以及用于制备用作上述方法中的中间体的青霉素和头孢菌素衍生物的新方法。

公开(公告)号：US3873524A

公开(公告)日：1975-03-25

申请号：US42040873

申请日：1973-11-30

申请人： AMERICAN HOME PROD

发明人： SELLSTEDT JOHN H ,  TELLER DANIEL M ,  GUINOSSO CHARLES J

IPC分类号： C07D499/00 ,  C07D499/46 ,  C07D99/14

CPC分类号： C07D499/00

摘要： Derivatives of 4-oxo-5-thiazolino and thiazolidine-5ylideneacetamidopenicillanic acid of potent anti-bacterial activity are produced by acylating 6-aminopenicillanic acid with derivatives of 4-oxo-5-thiazolinylideneacetic acid or 4-oxo-5thiazolidinylideneacetic acid in the presence of a condensing agent directly or after conversion of the -ylideneacetic acid to an acid halide.

摘要翻译： 4-氧代-5-噻唑烷基乙酸或4-氧代-5-噻唑烷基亚乙基乙酸的衍生物，通过将6-氨基青霉烷酸酰化 在缩合剂存在下直接或在将亚乙基乙酸转化成酰卤之后。