公开(公告)号：US4587047A

公开(公告)日：1986-05-06

申请号：US364352

申请日：1982-04-01

Applicant: Hermann Breuer ,  William A. Slusarchyk ,  Theodor Denzel ,  Uwe D. Treuner

Inventor： Hermann Breuer ,  William A. Slusarchyk ,  Theodor Denzel ,  Uwe D. Treuner

IPC: C07D205/085 ,  C07D521/00 ,  C07D205/08 ,  A61K31/395 ,  C07D401/12 ,  C07D403/12

CPC classification number: C07D231/12 ,  C07D205/085 ,  C07D233/56 ,  C07D249/08

Abstract: Antibacterial activity is exhibited by .beta.-lactams having a ##STR1## substituent in the 1-position and an acylamino substituent in the 3-position wherein Z is oxygen or sulfur, and R is alkyl, alkenyl, alkynyl, substituted alkyl, phenyl, substituted phenyl, a 5,6 or 7-membered heterocycle (R.sub.c), phenylalkyl, (substituted phenyl)alkyl, R.sub.c -alkyl or --NR.sub.a R.sub.b wherein R.sub.a and R.sub.b are the same or different and each is hydrogen, alkyl, substituted alkyl, phenyl, substituted phenyl, phenylalkyl, or (substituted phenyl)alkyl or one of R.sub.a and R.sub.b is hydrogen, alkyl, phenyl, substituted phenyl, phenylalkyl or (substituted phenyl)alkyl and the other is amino, alkanoylamino, arylcarbonylamino, alkoxycarbonylamino, alkylsulfonylamino, alkylamino, dialkylamino, phenylamino, (substituted phenyl)amino, hydroxy, cyano, alkoxy, phenyloxy, (substituted phenyl)oxy, phenylalkoxy, (substituted phenyl)alkoxy, R.sub.c, R.sub.c -alkyl, R.sub.c -alkoxy, alkylsulfonyl, alkylmethyleneamino, phenylmethyleneamino or (substituted phenyl)methyleneamino.

Abstract translation: 在1-位具有取代基的β-内酰胺和3-位上的酰氨基取代基，其中Z是氧或硫，R是烷基，烯基，炔基，取代的烷基，苯基，被取代的抗菌活性表现出抗菌活性 苯基，5,6或7-元杂环（Rc），苯基烷基，（取代的苯基）烷基，R c-烷基或-NR a R b，其中R a和R b相同或不同，各自为氢，烷基，取代的烷基，苯基， 取代的苯基，苯基烷基或（取代的苯基）烷基或Ra和Rb中的一个是氢，烷基，苯基，取代的苯基，苯基烷基或（取代的苯基）烷基，另一个是氨基，烷酰基氨基，芳基羰基氨基，烷氧基羰基氨基，烷基磺酰基氨基，烷基氨基， 二烷基氨基，苯基氨基，（取代苯基）氨基，羟基，氰基，烷氧基，苯氧基，（取代的苯基）氧基，苯基烷氧基，（取代的苯基）烷氧基，Rc，Rc-烷基，Rc-烷氧基，烷基磺酰基，烷基亚甲基氨基，苯基亚甲基氨基或 苯基） 亚乙基氨基。

公开(公告)号：US4551277A

公开(公告)日：1985-11-05

申请号：US550288

申请日：1983-11-09

Applicant: Uwe D. Treuner

Inventor： Uwe D. Treuner

IPC: C07D205/08 ,  C07D205/085 ,  C07D417/12 ,  A61K31/395 ,  C07D401/12 ,  C07D403/12

CPC classification number: C07D417/12 ,  C07D205/085

Abstract: Antibacterial activity is exhibited by (3-acylamino)-2-azetidinones having in the 1-position a group of the formula ##STR1## or a salt or ester thereof wherein R.sub.5 and R.sub.6 are the same or different and each is hydrogen or alkyl.

Abstract translation: 具有1-位的式（3-酰基氨基）-2-氮杂环丁酮的式（III）所示的抗菌活性或其盐或酯，其中R 5和R 6相同或不同，各自为氢或烷基。

公开(公告)号：US4534896A

公开(公告)日：1985-08-13

申请号：US503964

申请日：1983-06-13

Applicant: Uwe D. Treuner ,  Hermann Breuer

Inventor： Uwe D. Treuner ,  Hermann Breuer

IPC: C07D205/08 ,  A61K31/395 ,  A61K31/397 ,  A61P31/04 ,  C07D205/085 ,  C07D417/12

CPC classification number: C07D417/12 ,  C07D205/085

Abstract: Antibacterial activity and .beta.-lactamase inhibitory activity is exhibited by .beta.-lactams having a 3-acylamino substituent and in the 1-position a group having the formula ##STR1## wherein R.sub.5 is hydrogen, methyl or ethyl.

Abstract translation: 具有3-酰基氨基取代基的β-内酰胺和1-位具有式“IMAGE”的基团，其中R5是氢，甲基或乙基，表现出抗细菌活性和β-内酰胺酶抑制活性。

公开(公告)号：US4501743A

公开(公告)日：1985-02-26

申请号：US588831

申请日：1984-03-12

Applicant: Hermann Breuer ,  Uwe D. Treuner ,  Theodor Denzel

Inventor： Hermann Breuer ,  Uwe D. Treuner ,  Theodor Denzel

IPC: C07D277/20 ,  A61K31/545

CPC classification number: C07D277/20

Abstract: Cephalosporins of the formula ##STR1## wherein R is hydrogen, sodium, potassium or certain ester groups; R.sub.1 is in the .alpha.-configuration and is hydrogen or methoxy; R.sub.2 is hydrogen, ##STR2## X is hydrogen, ##STR3## R.sub.4 is hydrogen or lower alkyl; R.sub.5 is hydrogen, lower alkyl, ##STR4## --(CH.sub.2).sub.n --N--(lower alkyl).sub.2 ; R.sub.6 is hydrogen, sodium, or potassium; n is an integer from 1 to 4; are disclosed. These compounds are useful as anti-bacterial agents.

Abstract translation: 其中R为氢，钠，钾或某些酯基团的式“IMAGE”的头孢菌素; R1为α构型，为氢或甲氧基; R2是氢，X是氢，R4是氢或低级烷基; R5是氢，低级烷基， - （CH2）n-N-（低级烷基）2; R6是氢，钠或钾; n是1至4的整数; 被披露。 这些化合物可用作抗细菌剂。

公开(公告)号：US4171435A

公开(公告)日：1979-10-16

申请号：US495598

申请日：1974-08-08

Applicant: Hermann Breuer ,  Uwe D. Treuner

Inventor： Hermann Breuer ,  Uwe D. Treuner

IPC: A61K31/545 ,  C07D501/20 ,  C07D501/28 ,  C07D501/32 ,  C07D501/34

CPC classification number: C07C321/00

Abstract: [(Thioalkyl)thioacetyl]cephalosporin derivatives of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, tri(lower alkyl)silyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen, lower alkyl, phenyl, thienyl or furyl; R.sub.2 and R.sub.6 each is hydrogen or lower alkyl; R.sub.3 and R.sub.5 each is lower alkyl, phenyl or phenyl-lower alkyl and R.sub.4 is hydrogen, hydroxy or lower alkanoyloxy; are useful as antimicrobial agents.

Abstract translation: 其中R是氢，低级烷基，苯基 - 低级烷基，三（低级烷基）甲硅烷基，成盐离子或基团R 1是氢，低级烷基，（低级烷基）硫代乙酰基]头孢菌素衍生物 烷基，苯基，噻吩基或呋喃基; R2和R6各自为氢或低级烷基; R3和R5各自为低级烷基，苯基或苯基 - 低级烷基，R4为氢，羟基或低级烷酰氧基; 作为抗微生物剂是有用的。

公开(公告)号：US4142045A

公开(公告)日：1979-02-27

申请号：US876789

申请日：1978-02-10

Applicant: Hermann Breuer ,  Uwe D. Treuner

Inventor： Hermann Breuer ,  Uwe D. Treuner

IPC: C07D501/20 ,  C07D501/34 ,  C07D501/36 ,  C07D501/38 ,  C07D501/44

CPC classification number: C07D501/36 ,  C07D501/20

Abstract: Carbamoylalkylureido cephalosporins of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen or methoxy; A is straight or branched chain alkylene of 1 to 6 carbons; R.sub.2 and R.sub.3 are independently selected from hydrogen and straight chain alkyl of 1 to 4 carbons, or R.sub.2 is hydrogen and R.sub.3 is branched chain alkyl of 3 or 4 carbons, phenyl, benzyl or phenethyl, or R.sub.2 and R.sub.3 taken together with N atom to which they are attached form ##STR3## R.sub.4 is hydrogen or lower alkyl; R.sub.5 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.6 is hydrogen or lower alkyl; R.sub.7 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR4## or certain heterothio groups; are disclosed. These compounds are useful as antibacterial agents.

Abstract translation: 其中R为氢，低级烷基，苯基 - 低级烷基，二苯基 - 低级烷基，三（低级烷基）甲硅烷基，三卤代乙基，成盐离子或基团R 1的氨基甲酰基烷基脲基头孢菌素为氢或 甲氧基 A是1至6个碳的直链或支链亚烷基; R2和R3独立地选自氢和1至4个碳的直链烷基，或者R2是氢，R3是3或4个碳的支链烷基，苯基，苄基或苯乙基，或R2和R3与N原子一起 它们是连接的，其中R 4是氢或低级烷基; R5是氢，低级烷基，环烷基，环烯基，环链二烯基，苯基，苯基 - 低级烷基，取代的苯基，取代的苯基 - 低级烷基或某些杂环基; R6是氢或低级烷基; R7是低级烷基; X是氢，低级烷酰氧基，或者某些杂硫基; 被披露。 这些化合物可用作抗菌剂。

公开(公告)号：US4128723A

公开(公告)日：1978-12-05

申请号：US883602

申请日：1978-03-06

Applicant: Hermann Breuer ,  Uwe D. Treuner

Inventor： Hermann Breuer ,  Uwe D. Treuner

IPC: C07D333/24 ,  C07D501/20 ,  C07D501/36 ,  C07D501/32 ,  C07D501/46

CPC classification number: C07D333/24

Abstract: Cyanoalkylureido cephalosporins of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen or methoxy; A is straight or branched chain alkylene or ##STR3## R.sub.2 is phenyl, 2-thienyl, or 3-thienyl; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.5 is hydrogen or lower alkyl; R.sub.6 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR4## or certain heterothio groups; are disclosed. These compounds are useful as antibacterial agents.

Abstract translation: 其中R为氢，低级烷基，苯基 - 低级烷基，二苯基 - 低级烷基，三（低级烷基）甲硅烷基，三卤代乙基，形成成盐离子或基团R 1的氰基烷基脲基头孢菌素为氢或 甲氧基 A是直链或支链亚烷基或者R 2是苯基，2-噻吩基或3-噻吩基; R3是氢或低级烷基; R4是氢，低级烷基，环烷基，环烯基，环链二烯基，苯基，苯基 - 低级烷基，取代的苯基，取代的苯基 - 低级烷基或某些杂环基; R5是氢或低级烷基; R6是低级烷基; X是氢，低级烷酰氧基，或者某些杂硫基; 被披露。 这些化合物可用作抗菌剂。

公开(公告)号：US4113943A

公开(公告)日：1978-09-12

申请号：US776400

申请日：1977-03-10

Applicant: Uwe D. Treuner ,  Hermann Breuer

Inventor： Uwe D. Treuner ,  Hermann Breuer

IPC: C07D307/54 ,  C07D333/24 ,  C07D501/36

CPC classification number: C07C255/00 ,  C07D307/54 ,  C07D333/24

Abstract: 7.beta.-[(2-Amino-1,2-dioxoethyl)amino]acyl cephalosporins of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl or a salt forming ion; R.sub.1 is hydrogen, lower alkyl, saturated or unsaturated cycloalkyl, phenyl, phenyl-lower alkyl, substituted phenyl or certain heterocyclic groups; R.sub.2 is hydrogen or methoxy; R.sub.3 is hydrogen, lower alkyl or cycloalkyl; and X is hydrogen, lower alkanoyloxy, carbamoyloxy, lower alkoxy, lower alkylthio ##STR2## or certain heterothio groups, are useful as antibacterial agents.

公开(公告)号：US4110535A

公开(公告)日：1978-08-29

申请号：US715018

申请日：1976-08-16

Applicant: Hermann Breuer ,  Uwe D. Treuner

Inventor： Hermann Breuer ,  Uwe D. Treuner

IPC: C07D333/24 ,  C07D501/36

CPC classification number: C07D333/24

Abstract: Ureido cephalosporin derivatives of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl or phenyl-lower alkyl, or certain heterocyclic groups; R.sub.2 is hydrogen or lower alkyl; R.sub.3 is hydrogen or methoxy; R.sub.4 is hydrogen, halogen, lower alkyl, or lower alkoxy; R.sub.5 is hydrogen or lower alkyl; R.sub.6 is lower alkyl, phenyl, or phenyl-lower alkyl; are disclosed. These compounds are useful as antibacterial agents.

公开(公告)号：US4100344A

公开(公告)日：1978-07-11

申请号：US776151

申请日：1977-03-10

Applicant: Hermann Breuer ,  Uwe D. Treuner

Inventor： Hermann Breuer ,  Uwe D. Treuner

IPC: C07D501/36

CPC classification number: C07D501/36

Abstract: Alkenyl and alkinylureido cephalosporins of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen or methoxy; R.sub.2 is lower alkenyl or alkinyl, R.sub.3 is hydrogen or lower alkyl; R.sub.4 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.5 is hydrogen or lower alkyl; R.sub.6 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR3## OR CERTAIN HETEROTHIO GROUPS; ARE DISCLOSED. These compounds are useful as antibacterial agents.

Abstract translation: 其中R是氢，低级烷基，苯基 - 低级烷基，二苯基 - 低级烷基，三（低级烷基）甲硅烷基，三卤代乙基，成盐离子或基团R1的烯基和炔基脲基头孢菌素 氢或甲氧基; R2是低级烯基或炔基，R3是氢或低级烷基; R4是氢，低级烷基，环烷基，环烯基，环链二烯基，苯基，苯基 - 低级烷基，取代的苯基，取代的苯基 - 低级烷基或某些杂环基; R5是氢或低级烷基; R6是低级烷基; X是氢，低级烷酰氧基，或者某些异味基团; 被披露 这些化合物可用作抗菌剂。