公开(公告)号：US06642252B2

公开(公告)日：2003-11-04

申请号：US10052927

申请日：2001-11-07

Applicant: Gregory S. Bisacchi ,  James C. Sutton ,  William A. Slusarchyk ,  Uwe D. Treuner ,  Guohua Zhao ,  Daniel L. Cheney ,  Yan Shi ,  Shung C. Wu

Inventor： Gregory S. Bisacchi ,  James C. Sutton ,  William A. Slusarchyk ,  Uwe D. Treuner ,  Guohua Zhao ,  Daniel L. Cheney ,  Yan Shi ,  Shung C. Wu

IPC: C07D40102

CPC classification number: C07D401/12 ,  A61K45/06 ,  C07B2200/07 ,  C07C257/18 ,  C07D207/16 ,  C07D211/60 ,  C07D223/06

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US5290929A

公开(公告)日：1994-03-01

申请号：US941600

申请日：1992-09-08

Applicant: William H. Koster ,  Joseph E. Sundeen ,  Henner Straub ,  Peter Ermann ,  Uwe D. Treuner ,  Kent Amsberry ,  Michael Fakes ,  Sailesh A. Varia

Inventor： William H. Koster ,  Joseph E. Sundeen ,  Henner Straub ,  Peter Ermann ,  Uwe D. Treuner ,  Kent Amsberry ,  Michael Fakes ,  Sailesh A. Varia

IPC: 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 classification number: C07D241/52 ,  C07C217/86 ,  C07C271/66 ,  C07D241/44 ,  C07D417/14 ,  C07D491/04 ,  C07F9/650994 ,  Y02P20/55

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US5112968A

公开(公告)日：1992-05-12

申请号：US386070

申请日：1989-07-28

Applicant: Uwe D. Treuner

Inventor： Uwe D. Treuner

IPC: C07D417/04 ,  C07D417/14

CPC classification number: C07D417/04 ,  C07D417/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US4499016A

公开(公告)日：1985-02-12

申请号：US290648

申请日：1981-08-06

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

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

IPC: C07D205/08 ,  A61K31/397 ,  A61K31/425 ,  A61K31/505 ,  A61P31/04 ,  C07D205/085 ,  C07D403/12 ,  C07D417/12 ,  C07F7/10 ,  A61K31/395

CPC classification number: C07D403/12 ,  C07D205/085 ,  C07D417/12 ,  C07F7/10

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US4217348A

公开(公告)日：1980-08-12

申请号：US946479

申请日：1978-09-28

Applicant: Uwe D. Treuner ,  Hermann Breuer

Inventor： Uwe D. Treuner ,  Hermann Breuer

IPC: C07D263/26 ,  C07D501/20 ,  A61K31/545 ,  C07D501/34 ,  C07D501/36 ,  C07D501/46

CPC classification number: C07D263/26

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, 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.

Abstract translation: 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。

公开(公告)号：US4128724A

公开(公告)日：1978-12-05

申请号：US868781

申请日：1978-01-12

Applicant: Hermann Breuer ,  Uwe D. Treuner

Inventor： Hermann Breuer ,  Uwe D. Treuner

IPC: C07D333/24 ,  C07D501/20 ,  C07D501/36 ,  C07D501/32 ,  C07D501/56

CPC classification number: C07D333/24

Abstract: New .alpha.-hydrazinocarbonylamino cephalosporins which have the formula ##STR1## are useful as antimicrobial agents.

Abstract translation: 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。

公开(公告)号：US4096329A

公开(公告)日：1978-06-20

申请号：US765037

申请日：1977-02-02

Applicant: Hermann Breuer ,  Uwe D. Treuner

Inventor： Hermann Breuer ,  Uwe D. Treuner

IPC: A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D333/24 ,  C07D501/20 ,  C07D501/36

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。

公开(公告)号：US4077956A

公开(公告)日：1978-03-07

申请号：US718748

申请日：1976-08-30

Applicant: Uwe D. Treuner

Inventor： Uwe D. Treuner

IPC: C07D231/16 ,  C07D231/38 ,  C07D487/14

CPC classification number: C07D487/14 ,  C07D231/16 ,  C07D231/38

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US4063019A

公开(公告)日：1977-12-13

申请号：US671788

申请日：1976-03-30

Applicant: Hermann Breuer ,  Uwe D. Treuner

Inventor： Hermann Breuer ,  Uwe D. Treuner

IPC: A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D233/80 ,  C07D333/24 ,  C07D501/20 ,  C07D501/36

CPC classification number: C07D333/24 ,  C07D233/80

Abstract: [[[(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.

Abstract translation: 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。

公开(公告)号：US4053474A

公开(公告)日：1977-10-11

申请号：US678832

申请日：1976-04-21

Applicant: Uwe D. Treuner ,  Hermann Breuer

Inventor： Uwe D. Treuner ,  Hermann Breuer

IPC: A61K31/505 ,  A61K31/535 ,  A61P29/00 ,  C07D231/38 ,  C07D487/04 ,  C07D487/14 ,  A61K31/415 ,  C07D401/14 ,  C07D403/14

CPC classification number: C07D231/38 ,  C07D487/04 ,  C07D487/14 ,  Y10S514/87

Abstract: New pyrazolo[4,3-e][1,2,4]triazolo[4,3-c]pyrimidines have the general formula ##STR1## They are useful as antiinflammatory agents.

Abstract translation: 新的吡唑并[4,3-e] [1,2,4]三唑并[4,3-c]嘧啶具有通式它们可用作抗炎剂。