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41. 发明授权

US3989696A 3-Heterothio[(oxyalkyl)thioacetyl]cephalosporin derivatives 失效
标题翻译： 3-异硫脲{8（氧烷基）硫代乙酰基{9头孢菌素衍生物
公开(公告)号：US3989696A
公开(公告)日：1976-11-02
申请号：US573677
申请日：1975-05-01
申请人： Hermann Breuer , Uwe D. Treuner
发明人： Hermann Breuer , Uwe D. Treuner
IPC分类号： C07D501/36 , C07D501/50 , C07D501/54
CPC分类号： C07C323/00
摘要： 3-Heterothio[(oxyalkyl)thioacetyl] cephalosporin derivatives which have the formula ##EQU1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, tri (lower alkyl) silyl, a salt forming ion, or the group ##EQU2## 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 is lower alkyl, phenyl or phenyl-lower alkyl; and R.sub.4 is a five- or six-member nitrogen and/or sulfur or oxygen-containing ring system; are useful as antibacterial agents.
摘要翻译：具有式R2R1S || R3-O-CH-S-CH-CO-NH-CH-CHCH2的3-异硫代[（氧代烷基）硫代乙酰基]头孢菌素衍生物|| C-NC-CH2-S-R4平行角 OC | COOR，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R6O |平行-CH-OC-R5; R 1是氢，低级烷基，苯基，噻吩基或呋喃基; R2和R6各自为氢或低级烷基; R3和R5是低级烷基，苯基或苯基 - 低级烷基; 并且R 4是五或六元氮和/或硫或含氧环系; 作为抗菌剂是有用的。

42. 发明授权

US06642252B2 Acid derivatives useful as serine protease inhibitors 有权
标题翻译：用作丝氨酸蛋白酶抑制剂的酸衍生物
公开(公告)号：US06642252B2
公开(公告)日：2003-11-04
申请号：US10052927
申请日：2001-11-07
申请人： Gregory S. Bisacchi , James C. Sutton , William A. Slusarchyk , Uwe D. Treuner , Guohua Zhao , Daniel L. Cheney , Yan Shi , Shung C. Wu
发明人： Gregory S. Bisacchi , James C. Sutton , William A. Slusarchyk , Uwe D. Treuner , Guohua Zhao , Daniel L. Cheney , Yan Shi , Shung C. Wu
IPC分类号： C07D40102
CPC分类号： C07D401/12 , A61K45/06 , C07B2200/07 , C07C257/18 , C07D207/16 , C07D211/60 , C07D223/06
摘要： Compounds having the formula (I), are useful as serine protease inhibitors, more particularly inhibitors of Factors VIIa, IXa, Xa, and/or XIa, wherein ring B is phenyl or pyridyl, W is preferably C(═O)NR4R5, L is a linker group, X2 comprises nitrogen or carbon, Z is an optionally-substituted monocyclic or bicyclic ring system, and R1, R2, R3, R4, R5 and R6 are as defined in the specification.
摘要翻译：具有式（I）的化合物可用作丝氨酸蛋白酶抑制剂，更具体地可用作因子VIIa，IXa，Xa和/或XIa的抑制剂，其中环B是苯基或吡啶基，W优选为C（= O）NR 4 R 5，L 是连接基团，X 2包括氮或碳，Z是任选取代的单环或双环环系，R1，R2，R3，R4，R5和R6如说明书中所定义。

43. 发明授权

US5290929A Heteroaryl derivatives of monocyclic beta-lactam antibiotics 失效
标题翻译：单环β-内酰胺抗生素的杂芳基衍生物
公开(公告)号：US5290929A
公开(公告)日：1994-03-01
申请号：US941600
申请日：1992-09-08
申请人： William H. Koster , Joseph E. Sundeen , Henner Straub , Peter Ermann , Uwe D. Treuner , Kent Amsberry , Michael Fakes , Sailesh A. Varia
发明人： William H. Koster , Joseph E. Sundeen , Henner Straub , Peter Ermann , Uwe D. Treuner , Kent Amsberry , Michael Fakes , Sailesh A. Varia
IPC分类号： C07C211/50 , A61K31/495 , A61K31/498 , A61P31/04 , C07C217/84 , C07C217/86 , C07C251/38 , C07C271/66 , C07D20060101 , C07D241/42 , C07D241/44 , C07D241/52 , C07D417/14 , C07D491/04 , C07D491/056 , C07F9/40 , C07F9/6509
CPC分类号： C07D241/52 , C07C217/86 , C07C271/66 , C07D241/44 , C07D417/14 , C07D491/04 , C07F9/650994 , Y02P20/55
摘要： Antibacterial activity is exhibited by novel compounds having the formula ##STR1## where R.sub.1, R.sub.2, and M are as defined herein and X is --(CH.sub.2).sub.n -- wherein n is 0, 1, 2, 3 or 4 or CR.sub.3 R.sub.4 wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen, --CH.sub.3 or --C.sub.2 H.sub.5 or R.sub.3 and R.sub.4 taken together with the carbon atom to which they are attached form a 3, 4, 5, 6 or 7-membered cycloalkyl ring.
摘要翻译：具有式（IMAGE）1的新化合物表现出抗菌活性，其中R 1，R 2和M如本文所定义，X为 - （CH 2）n - ，其中n为0,1,2,3或4或CR 3 R 4，其中R 3 和R 4相同或不同，各自为氢，-CH 3或-C 2 H 5或R 3和R 4与它们所连接的碳原子一起形成3,4,5,6或7元环烷基环。

44. 发明授权

US5112968A Monobactam hydrazide derivatives 失效
标题翻译：单链酰肼衍生物
公开(公告)号：US5112968A
公开(公告)日：1992-05-12
申请号：US386070
申请日：1989-07-28
申请人： Uwe D. Treuner
发明人： Uwe D. Treuner
IPC分类号： C07D417/04 , C07D417/14
CPC分类号： C07D417/04 , C07D417/14
摘要： Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof which possess antibacterial activity.R.sub.s is a substituted hydroxy pyridone of the formulae: ##STR2## wherein Y.sub.1 is CH.sub.2 X; COOR.sub.6 ; CONR.sub.7 R.sub.8 ; OH; OCH.sub.2 R.sub.9 ; CHF.sub.2 ; CHO; CH.dbd.N--OR.sub.10 ; CH.dbd.CH--R.sub.11 ; CN; CH.dbd.N--NHR.sub.12, and Y.sub.2 is hydrogen; COOH; CONH.sub.2 ; CN; CSNH.sub.2 ; COO lower alkyl; CONR.sub.7 /R.sub.8.
摘要翻译：具有式（I）的化合物及其药学上可接受的盐具有抗菌活性。 Rs是下式的取代羟基吡啶酮：其中Y 1是CH 2 X; COOR6; CONR7R8; 哦; OCH2R9; CHF2; CHO; CH = N-OR10; CH = CH-R11; CN; CH = N-NHR 12，Y2为氢; COOH; CONH2; CN; CSNH2; COO低级烷基; CONR7 / R8。

45. 发明授权

US4499016A 2-Oxo-1-[(acylamino)sulfonyl]azetidines 失效
标题翻译： 2-氧代-1 - [（酰氨基）磺酰基]氮杂环丁烷
公开(公告)号：US4499016A
公开(公告)日：1985-02-12
申请号：US290648
申请日：1981-08-06
申请人： Hermann Breuer , Theodor Denzel , Uwe D. Treuner
发明人： Hermann Breuer , Theodor Denzel , Uwe D. Treuner
IPC分类号： C07D205/08 , A61K31/397 , A61K31/425 , A61K31/505 , A61P31/04 , C07D205/085 , C07D403/12 , C07D417/12 , C07F7/10 , A61K31/395
CPC分类号： C07D403/12 , C07D205/085 , C07D417/12 , C07F7/10
摘要： Antibacterial activity is exhibited by .beta.-lactams having an --SO.sub.2 --NH--C--R substituent in the 1-position and an acylamino substituent in the 3-position wherein R is alkyl, phenyl, substituted phenyl, phenylalkyl, (substituted phenyl)alkyl, alkoxy, phenyloxy, (substituted phenyl)oxy, phenylalkoxy, or (substituted phenyl)alkoxy.
摘要翻译：在1-位上具有-SO2-NH-CR取代基的β-内酰胺和3-位的酰氨基取代基，其中R是烷基，苯基，取代的苯基，苯基烷基，（取代的苯基）烷基，烷氧基，苯氧基，（取代苯基）氧基，苯基烷氧基或（取代的苯基）烷氧基。

46. 发明授权

US4217348A Cephalosporins having an oxazolidonyloxamido substituted acyl sidechain 失效
标题翻译：头孢菌素具有恶唑烷二硫酰氨基取代的酰基侧链
公开(公告)号：US4217348A
公开(公告)日：1980-08-12
申请号：US946479
申请日：1978-09-28
申请人： Uwe D. Treuner , Hermann Breuer
发明人： Uwe D. Treuner , Hermann Breuer
IPC分类号： C07D263/26 , C07D501/20 , A61K31/545 , C07D501/34 , C07D501/36 , C07D501/46
CPC分类号： C07D263/26
摘要： 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, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, substituted or unsubstituted phenyl, benzyl, phenethyl, thienyl, furyl, or pyridyl, or 2-amino-4-thiazolyl; X is --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, ##STR2## R.sub.3 is hydrogen, ##STR3## --O--lower alkyl, or certain substituted or unsubstituted heterothio groups; are disclosed. These compounds possess useful antibacterial activity.
摘要翻译：其中R是氢，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，低级烷基，环烷基，环烯基，环烷二烯基，取代或未取代的苯基，苄基，苯乙基，噻吩基，呋喃基或吡啶基，或2-氨基-4-噻唑基; X是-CH 2 - ， - CH 2 -CH 2 - ， - R 3是氢， - 低级烷基或某些取代或未取代的杂硫基; 被披露。这些化合物具有有效的抗菌活性。

47. 发明授权

US4128724A Hydrazinocarbonylamino cephalosporins 失效
标题翻译：肼基氨基头孢菌素
公开(公告)号：US4128724A
公开(公告)日：1978-12-05
申请号：US868781
申请日：1978-01-12
申请人： Hermann Breuer , Uwe D. Treuner
发明人： Hermann Breuer , Uwe D. Treuner
IPC分类号： C07D333/24 , C07D501/20 , C07D501/36 , C07D501/32 , C07D501/56
CPC分类号： C07D333/24
摘要： New .alpha.-hydrazinocarbonylamino cephalosporins which have the formula ##STR1## are useful as antimicrobial agents.
摘要翻译：具有式“IMAGE”的新的α-肼基羰基氨基头孢菌素可用作抗微生物剂。

48. 发明授权

US4096329A 7-Cyanoalkylureido 3 heterocylic thio methyl cephalosporins 失效
标题翻译： 7-氰基烷基脲基3杂环硫代甲基头孢菌素
公开(公告)号：US4096329A
公开(公告)日：1978-06-20
申请号：US765037
申请日：1977-02-02
申请人： Hermann Breuer , Uwe D. Treuner
发明人： Hermann Breuer , Uwe D. Treuner
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D333/24 , C07D501/20 , C07D501/36
CPC分类号： C07D333/24
摘要： 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.
摘要翻译：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，形成成盐离子或基团R 1的氰基烷基脲基头孢菌素是氢或甲氧基 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。

49. 发明授权

US4077956A 5-Substituted derivatives of dipyrazolo[1,5-a:4',3'-e]pyrazine-6-carboxylic acids and esters 失效
标题翻译： 5-取代的二吡唑并[4,5-a：4 {40,3 {40e {9吡嗪-6-羧酸和酯
公开(公告)号：US4077956A
公开(公告)日：1978-03-07
申请号：US718748
申请日：1976-08-30
申请人： Uwe D. Treuner
发明人： Uwe D. Treuner
IPC分类号： C07D231/16 , C07D231/38 , C07D487/14
CPC分类号： C07D487/14 , C07D231/16 , C07D231/38
摘要： New 5-substituted derivatives of dipyrazolo[1,5-a:4',3'-e]pyrazine-6-carboxylic acid, esters and their salts have the formula ##STR1## R.sup.1 is hydrogen, lower alkyl or phenyl-lower alkylene; R.sup.2 and R.sup.3 each is hydrogen or lower alkyl; X is oxygen or sulfur; and R.sup.4 is hydrogen, lower alkyl, phenyl-lower alkylene or amino-lower alkylene.The new compounds are useful as anti-inflammatory agents and immunosuppressive agents.
摘要翻译：二吡唑并[1,5-a：4'，3'-e]吡嗪-6-羧酸的新的5-取代的衍生物，其酯及其盐具有下式R1是氢，低级烷基或苯基 - 低级亚烷基 ; R2和R3各自为氢或低级烷基; X是氧或硫; 和R4是氢，低级烷基，苯基 - 低级亚烷基或氨基 - 低级亚烷基。

50. 发明授权

US4063019A [[[(2,4-Dioxo-1-imidazolidinyl)amino]carbonyl]amino]-acetylcephalosporin derivatives 失效
标题翻译： {8 {8（2,4-二氧代-1-咪唑啉基）氨基{9羰基{9氨基{9-乙酰头孢菌素衍生物
公开(公告)号：US4063019A
公开(公告)日：1977-12-13
申请号：US671788
申请日：1976-03-30
申请人： Hermann Breuer , Uwe D. Treuner
发明人： Hermann Breuer , Uwe D. Treuner
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D233/80 , C07D333/24 , C07D501/20 , C07D501/36
CPC分类号： C07D333/24 , C07D233/80
摘要： [[[(2,4-Dioxo-1-imidazolidinyl)amino]carbonyl]amino]-acetylcephalosporin derivatives having 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, R.sub.3 and R.sub.5 each is hydrogen or lower alkyl; R.sub.4 is hydrogen, lower alkyl, cyclo-lower alkyl, cyclo-lower alkenyl, cyclo-lower alkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.6 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR3## or certain heterothio groups; are useful as antibacterial agents.
摘要翻译：具有下式的[[[（2,4-二氧代-1-咪唑烷基）氨基]羰基]氨基] - 乙酰头孢菌素衍生物其中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R 1是氢或甲氧基; R2，R3和R5各自为氢或低级烷基; R4是氢，低级烷基，环低级烷基，环低级链烯基，环低级链烯基，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是低级烷基; X是氢，低级烷酰氧基，或者某些杂硫基; 作为抗菌剂是有用的。

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