公开(公告)号：US06335324B1

公开(公告)日：2002-01-01

申请号：US09458847

申请日：1999-12-13

申请人： Gregory S. Bisacchi ,  William A. Slusarchyk ,  Uwe Treuner ,  James C. Sutton ,  Robert Zahler ,  Steven Seiler ,  David R. Kronenthal ,  Michael E. Randazzo ,  Mark D. Schwinden ,  Zhongmin Xu ,  Zhongping Shi

发明人： Gregory S. Bisacchi ,  William A. Slusarchyk ,  Uwe Treuner ,  James C. Sutton ,  Robert Zahler ,  Steven Seiler ,  David R. Kronenthal ,  Michael E. Randazzo ,  Mark D. Schwinden ,  Zhongmin Xu ,  Zhongping Shi

IPC分类号： C07D4014

CPC分类号： C07D403/12 ,  C07D205/08

摘要： Compounds of the formulas: are disclosed. These compounds inhibit tryptase as well as other enzyme systems or are selective tryptase inhibitors and are useful as antiinflammatory agents particularly in the treatment of chronic asthma.

摘要翻译： 公开了下列化合物： 这些化合物抑制类胰蛋白酶以及其他酶系统或选择性类胰蛋白酶抑制剂，并且可用作抗炎剂，特别是用于治疗慢性哮喘。

公开(公告)号：US4111978A

公开(公告)日：1978-09-05

申请号：US829707

申请日：1977-09-01

申请人： Hermann Breuer ,  Uwe Treuner

发明人： Hermann Breuer ,  Uwe Treuner

IPC分类号： C07D501/20 ,  C07C121/16 ,  C07C121/66

CPC分类号： C07D501/20

摘要： New compounds of the following general formula, and their salts ##STR1## wherein R.sub.1 and R.sub.2 each is hydrogen, lower alkyl, lower alkenyl, phenyl, hydroxyphenyl, chlorophenyl, benzyl, phenethyl, or R.sub.1 and R.sub.2 together complete a cyclopentyl or cyclohexyl group; R.sub.3 is hydrogen, lower alkyl, lower alkenyl, cyclopentyl, cyclohexyl, phenyl, hydroxyphenyl, aminophenyl, chlorophenyl, benzyl, furyl, thienyl, pyrrolidyl or pyridyl; and R.sub.5 is hydrogen or lower alkyl; are intermediates for the production of cephalosporin derivatives.

摘要翻译： 下列通式的新化合物及其盐，其中R 1和R 2各自为氢，低级烷基，低级烯基，苯基，羟基苯基，氯苯基，苄基，苯乙基或R 1和R 2一起完成环戊基或环己基; R3是氢，低级烷基，低级烯基，环戊基，环己基，苯基，羟基苯基，氨基苯基，氯苯基，苄基，呋喃基，噻吩基，吡咯烷基或吡啶基。 R5是氢或低级烷基; 是用于生产头孢菌素衍生物的中间体。

公开(公告)号：US3932396A

公开(公告)日：1976-01-13

申请号：US513676

申请日：1974-10-10

申请人： Hermann Breuer ,  Uwe Treuner

发明人： Hermann Breuer ,  Uwe Treuner

IPC分类号： C07D501/20 ,  C07D501/26 ,  C07D501/36

CPC分类号： C07D501/20

摘要： New cyanomethylthioacetylcephalosporins of the following general formula, and their salts ##SPC1##Wherein R is hydrogen or a salt forming ion of the group consisting of aluminum, alkali metal, alkaline earth metal, lower alkylamine, phenyl-lower alkylamine, N,N'-dibenzylethylenediamine, procaine or lower alkylpiperidine; R.sub.1 and R.sub.2 each is hydrogen, lower alkyl, lower alkenyl, phenyl, hydroxyphenyl, chlorophenyl, benzyl, phenethyl or R.sub.1 and R.sub.2 together complete a cyclopentyl or cyclohexyl group; R.sub.3 is cyclo-lower alkyl, cyclo-lower alkenyl or cyclo-lower alkadienyl; and X is hydrogen, lower alkanoyloxy, lower alkoxy or lower alkylthio.

摘要翻译： 新的具有以下通式的氰甲基硫代乙酰头孢菌素及其盐，其中R为氢或由铝，碱金属，碱土金属，低级烷基胺，苯基 - 低级烷基胺，N，N'-二苄基乙二胺，普鲁卡因 或低级烷基哌啶; R 1和R 2各自为氢，低级烷基，低级烯基，苯基，羟基苯基，氯苯基，苄基，苯乙基或R 1和R 2一起形成环戊基或环己基; R3是环低级烷基，环低级烯基或环 - 低级亚烷基; X为氢，低级烷酰氧基，低级烷氧基或低级烷硫基。

公开(公告)号：US3932397A

公开(公告)日：1976-01-13

申请号：US513677

申请日：1974-10-10

申请人： Hermann Breuer ,  Uwe Treuner

发明人： Hermann Breuer ,  Uwe Treuner

IPC分类号： C07D501/24 ,  C07D501/28 ,  C07D501/36

CPC分类号： C07D501/20

摘要： New cyanomethylthioacetylcephalosporins of the following general formula, and their salts ##SPC1##Wherein R is hydrogen or a salt forming ion of the group consisting of aluminum, alkali metal, alkaline earth metal, lower alkylamine, phenyl-lower alkylamine, N,N'-dibenzylethylenediamine, procaine or lower alkylpiperidine; R.sub.1 and R.sub.2 each is hydrogen, lower alkyl, lower alkenyl, phenyl, hydroxyphenyl, chlorophenyl, benzyl, phenethyl, or R.sub.1 and R.sub.2 together complete a cyclopentyl or cyclohexyl group; R.sub.3 is hydrogen, lower alkyl or lower alkenyl; and X is lower alkoxy or lower alkylthio; are useful as antibacterial agents.

摘要翻译： 新的具有以下通式的氰甲基硫代乙酰头孢菌素及其盐，其中R为氢或由铝，碱金属，碱土金属，低级烷基胺，苯基 - 低级烷基胺，N，N'-二苄基乙二胺，普鲁卡因 或低级烷基哌啶; R 1和R 2各自为氢，低级烷基，低级烯基，苯基，羟基苯基，氯苯基，苄基，苯乙基或R 1和R 2一起形成环戊基或环己基; R3是氢，低级烷基或低级烯基; X为低级烷氧基或低级烷硫基; 作为抗菌剂是有用的。

公开(公告)号：US4086422A

公开(公告)日：1978-04-25

申请号：US714420

申请日：1976-08-16

申请人： Hermann Breuer ,  Uwe Treuner

发明人： Hermann Breuer ,  Uwe Treuner

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

CPC分类号： C07D501/36 ,  C07D501/20

摘要： Carbamoyalkylureido 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.

摘要翻译： 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R1为氢或碳原子数为1的碳原子数1〜8的烷硫基烷基脲基头孢菌素 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：US3944546A

公开(公告)日：1976-03-16

申请号：US513675

申请日：1974-10-10

申请人： Hermann Breuer ,  Uwe Treuner

发明人： Hermann Breuer ,  Uwe Treuner

IPC分类号： C07D501/20

CPC分类号： C07D501/20

摘要： New cyanomethylthioacetylcephalosporins of the following general formula, and their salts ##EQU1## wherein R is hydrogen or a salt forming ion of the group consisting of aluminum, alkali metal, alkaline earth metal, lower alkylamine, phenyl-lower alkylamine, N,N-dibenzylethylenediamine, procaine or lower alkylpiperidine; R.sub.1 and R.sub.2 each is hydrogen, lower alkyl, lower alkenyl, phenyl, hydroxyphenyl, chlorophenyl, benzyl, phenethyl, or R.sub.1 and R.sub.2 together complete a cyclopentyl or cyclohexyl group; R.sub.3 is phenyl, substituted phenyl or thienyl, said phenyl substituents being halogen, lower alkyl, amino or lower alkoxy; and X is hydrogen, lower alkoxy, lower alkylthio or lower alkanoyloxy; are useful as antibacterial agents.

摘要翻译： 新的具有下列通式的氰基甲基硫代乙酰头孢菌素及其盐R3OS | PARALLEL ANGLE CH-C-NH-CH-CHCH2 ||||||||C-NC-CH2X R1-C-CN PARALLEL ANGLE |OC || R2| COOR其中R是氢或由铝，碱金属，碱土金属，低级烷基胺，苯基 - 低级烷基胺，N，N-二苄基乙二胺，普鲁卡因或低级烷基哌啶组成的组的成盐离子; R 1和R 2各自为氢，低级烷基，低级烯基，苯基，羟基苯基，氯苯基，苄基，苯乙基或R 1和R 2一起形成环戊基或环己基; R3是苯基，取代的苯基或噻吩基，所述苯基取代基是卤素，低级烷基，氨基或低级烷氧基; X为氢，低级烷氧基，低级烷硫基或低级烷酰氧基; 作为抗菌剂是有用的。