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1. 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。

2. 发明授权

US07122559B2 Phenylglycine derivatives useful as serine protease inhibitors 有权
标题翻译：用作丝氨酸蛋白酶抑制剂的苯基甘氨酸衍生物
公开(公告)号：US07122559B2
公开(公告)日：2006-10-17
申请号：US10775923
申请日：2004-02-10
申请人： Peter W. Glunz , Gregory S. Bisacchi , George C. Morton , Alexandra A. Holubec , E. Scott Priestley , Xiaojun Zhang , Uwe D. Treuner
发明人： Peter W. Glunz , Gregory S. Bisacchi , George C. Morton , Alexandra A. Holubec , E. Scott Priestley , Xiaojun Zhang , Uwe D. Treuner
IPC分类号： A61K31/472 , C07D217/22
CPC分类号： C07D231/56 , C07C311/51 , C07D217/02 , C07D217/06 , C07D217/22 , C07D233/36 , C07D235/30 , C07D239/94 , C07D261/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Compounds having the formula (I), or a stereoisomer or pharmaceutically-acceptable salt, or hydrate thereof, are useful as factor VIIa inhibitors, wherein X is —NR6S(O)pR16; W is hydrogen or —(CR7R8)q—W1; W1 is hydrogen or a bond with R6; Z is a 5-membered heteroaryl group, a five to six membered heterocyclo or cycloalkyl group, a 9 to 10 membered bicyclic aryl or heteroaryl, or a six membered aryl or heteroaryl, and R1, R2, R3, R6, R7, and R16 are as defined in the specification.
摘要翻译：具有式（I）的化合物或其立体异构体或药学上可接受的盐或其水合物可用作因子VIIa抑制剂，其中X为-NR 6 S（O） 16＆lt; 16＆gt; W是氢或 - （CR 7 R 8）。 W 1是氢或与R 6的键; Z是5元杂芳基，5至6元杂环基或环烷基，9至10元双环芳基或杂芳基，或6元芳基或杂芳基，R 1，R 2， R 2，R 3，R 6，R 7和R 16均为在规范中定义。

3. 发明授权

US4587047A 2-oxo-1-[[(substituted sulfonyl)amino]-carbonyl]azetidines 失效
标题翻译： 2-氧代-1 - [[（取代的磺酰基）氨基]羰基]氮杂环丁烷
公开(公告)号：US4587047A
公开(公告)日：1986-05-06
申请号：US364352
申请日：1982-04-01
申请人： Hermann Breuer , William A. Slusarchyk , Theodor Denzel , Uwe D. Treuner
发明人： Hermann Breuer , William A. Slusarchyk , Theodor Denzel , Uwe D. Treuner
IPC分类号： C07D205/085 , C07D521/00 , C07D205/08 , A61K31/395 , C07D401/12 , C07D403/12
CPC分类号： C07D231/12 , C07D205/085 , C07D233/56 , C07D249/08
摘要： 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.
摘要翻译：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。

4. 发明授权

US5248790A Aminoalkylphosphonic acid esters of natural 4-methoxy-5-methyl-pyran-3-ol and derivatives thereof 失效
标题翻译：天然4-甲氧基-5-甲基 - 吡喃-3-醇及其衍生物的氨基烷基膦酸酯
公开(公告)号：US5248790A
公开(公告)日：1993-09-28
申请号：US906776
申请日：1992-06-30
申请人： Uwe D. Treuner
发明人： Uwe D. Treuner
IPC分类号： A01N57/24 , C07F9/655
CPC分类号： A01N57/24 , C07F9/6552
摘要： Antibiotic substances having the general formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined herein.
摘要翻译：具有通式 I的抗生素物质，其中R1，R2和R3如本文所定义。

5. 发明授权

US4801705A 2-oxo-1-(((substituted sulfonyl)amino)-carbonyl)azetidines 失效
标题翻译： 2-氧代-1 - （（（取代的磺酰基）氨基） - 羰基）氮杂环丁烷
公开(公告)号：US4801705A
公开(公告)日：1989-01-31
申请号：US877599
申请日：1986-06-23
申请人： Hermann Breuer , Jakob-Matthias Drossard , Peter H. Ermann , Henner Straub , Uwe D. Treuner
发明人： Hermann Breuer , Jakob-Matthias Drossard , Peter H. Ermann , Henner Straub , Uwe D. Treuner
IPC分类号： A61K31/395 , A61K31/397 , A61K31/495 , A61P31/04 , C07D205/08 , C07D205/085 , C07D403/12 , C07D417/12 , C07D417/14 , A61K31/415
CPC分类号： C07D417/12 , C07D417/14
摘要： Antibacterial activity is exhibited by .beta.-lactams having a 3-acylamino substituent and having in the 1-position an activating group of the formula ##STR1## wherein R is

6. 发明授权

US4762922A 2-oxo-1-[[(substituted sulfonyl)amino]-carbonyl]azetidines 失效
标题翻译： 2-氧代-1 - [[（取代的磺酰基）氨基]羰基]氮杂环丁烷
公开(公告)号：US4762922A
公开(公告)日：1988-08-09
申请号：US70286
申请日：1987-07-01
申请人： Hermann Breuer , Uwe D. Treuner
发明人： Hermann Breuer , Uwe D. Treuner
IPC分类号： C07D401/14 , A61K31/44 , A61K31/4427 , A61P31/04 , C07D401/12 , C07D417/14 , A61K31/395 , A61K31/425
CPC分类号： C07D401/12 , C07D417/14
摘要： Antibacterial activity is exhibited by 2-azetidinones having a 3-acylamino substituent and having an activating group in the 1-position of the formula ##STR1## wherein R is ##STR2## A.sub.1 is --NH-- or ##STR3## A.sub.2 is ##STR4## or --CH.dbd.CH--.
摘要翻译：具有3-酰基氨基取代基的2-氮杂环丁酮和具有式Ia的1位的具有活化基团的抗菌活性表现为其中R为“IMA”或“IMA”> A1为-NH-或 A2 是 + TR 或-CH = CH-。

7. 发明授权

US4128716A 4-Halo derivatives of pyrazolo[1,5-a]-quinoxaline-3-carboxylic acids and esters 失效
标题翻译：吡唑并[8,1-a {9-喹喔啉-3-羧酸和酯的4-卤素衍生物
公开(公告)号：US4128716A
公开(公告)日：1978-12-05
申请号：US833104
申请日：1977-09-13
申请人： Uwe D. Treuner
发明人： Uwe D. Treuner
IPC分类号： C07D231/14 , C07D487/04 , A61K31/495
CPC分类号： C07D487/04 , C07D231/14
摘要： New 4-halo derivatives of pyrazolo[1,5-a]quinoxaline-3-carboxylic acid, esters and their salts have the formula ##STR1## R.sub.1 is hydrogen, lower alkyl or a salt forming ion; R.sub.2 is hydrogen, lower alkyl, halogen or lower alkoxy; and X is halogen.The new compounds are useful as intermediates and as anti-inflammatory agents.
摘要翻译：吡唑并[1,5-a]喹喔啉-3-羧酸的新4-卤代衍生物，酯及其盐具有下式：R1是氢，低级烷基或成盐离子; R2是氢，低级烷基，卤素或低级烷氧基; X为卤素。

8. 发明授权

US4127716A 3-HETEROTHIOMETHYL UREIDO CEPHALOSPORINS 失效
标题翻译： 3-HETEROTHOMETHYL UREIDO CEPHALOSPORINS
公开(公告)号：US4127716A
公开(公告)日：1978-11-28
申请号：US764134
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： C07D307/54 , C07D333/24 , C07D501/36 , C07D501/56 , A61K31/545 , C07D501/54
CPC分类号： C07D333/24 , C07D307/54
摘要： L-Isomer compounds of the formula ##STR1## wherein R.sub.1 is phenyl, thienyl or furyl; R.sub.4 represents certain heterocyclic groups; R.sub.3 is hydrogen, lower alkyl, phenyl-lower alkyl, substituted phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)stannyl, tri(lower alkyl)silyl, a salt forming ion, or the group ##STR2## wherein R is lower alkyl, phenyl, phenyl-lower alkyl, or substituted phenyl and phenyl-lower alkyl are disclosed. These compounds are useful as antibacterial agents.
摘要翻译：其中R1是苯基，噻吩基或呋喃基的式（Ⅰ）的L-异构体化合物; R4表示某些杂环基; R3是氢，低级烷基，苯基 - 低级烷基，取代的苯基 - 低级烷基，二苯基 - 低级烷基，三（低级烷基）甲锡烷基，三（低级烷基）甲硅烷基，成盐离子或基团，其中R 是低级烷基，苯基，苯基 - 低级烷基或取代的苯基和苯基 - 低级烷基。这些化合物可用作抗菌剂。

9. 发明授权

US4100345A 3-(Carbamoyl)pyridino derivatives of 7a-methoxy ureidocephalosporins 失效
标题翻译： 7-甲氧基脲基头孢菌素的3-（氨基甲酰基）吡啶衍生物
公开(公告)号：US4100345A
公开(公告)日：1978-07-11
申请号：US761914
申请日：1977-01-24
申请人： Hermann Breuer , Uwe D. Treuner
发明人： Hermann Breuer , Uwe D. Treuner
IPC分类号： C07D333/24 , C07D501/38 , C07D501/44 , C07D501/40
CPC分类号： C07D333/24
摘要： Ureido cephalosporin derivatives of the formula ##STR1## wherein R.sub.1 is hydrogen or methoxy; R.sub.2 is hydrogen or lower alkyl; R.sub.3 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl; or certain heterocyclic groups; are disclosed. These compounds are useful as antibacterial agents.
摘要翻译：其中R1是氢或甲氧基的式“IMAGE”的脲基头孢菌素衍生物; R2是氢或低级烷基; R3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; 或某些杂环基团; 被披露。这些化合物可用作抗菌剂。

10. 发明授权

US4093801A [[[(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：US4093801A
公开(公告)日：1978-06-06
申请号：US819648
申请日：1977-07-27
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 , C07D501/34 , C07D501/46
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, substitutted 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，环低级烯基，环低级亚烷基，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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