专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US06566355B1 Bicyclic and tricyclic &bgr;-lactams 失效
标题翻译：双环和三环β-内酰胺
公开(公告)号：US06566355B1
公开(公告)日：2003-05-20
申请号：US08420957
申请日：1995-04-12
申请人： Christian Hubschwerlen , Robert Charnas , Ingrid Heinze , Klaus Gubernator
发明人： Christian Hubschwerlen , Robert Charnas , Ingrid Heinze , Klaus Gubernator
IPC分类号： C07D48704
CPC分类号： A61K31/43 , A61K31/545 , C07D487/04 , A61K31/40 , A61K2300/00
摘要： There are described compounds of the formula in which R signifies lower alkoxycarbonyl, lower alkoxy-carbonylamino, the acyl residue of an &agr;- or &bgr;-amino acid or a residue of the general formula Q—X—Y— (a) wherein Q signifies a 3- to 6-membered ring which optionally contains nitrogen, sulfur and/or oxygen and which is optionally bonded with a fused ring, X signifies a direct bond or a linear “spacer” with up to 6 atoms consisting of carbon, nitrogen, oxygen and/or sulfur, of which up to 2 atoms can be nitrogen atoms and 1 atom can be oxygen or sulfur, and Y represents one of the groups —CO—, —CS—, —CONH— and (where X contains neither sulfur nor carbonyl as a terminal component) —SO2—; and in which R1 and R2 together signify a group of the formula wherein A represents hydrogen or a residue which is usable in the 3-position of cephalosporin antibiotics, and in which R3 represents hydrogen, and pharmaceutically compatible salts of these compounds. The products have &bgr;-lactamase inhibiting properties. They are useful in combination with &bgr;-lactam antibiotics in the control of &bgr;-lactamase forming pathogens.
摘要翻译：描述的化合物是R表示低级烷氧基羰基，低级烷氧基 - 羰基氨基，α-或β-氨基酸的酰基残基或通式化合物的残基Q表示3-至6-元环，其任选地含有氮，硫和/或氧，并且其任选地与稠环键合，X表示直接键或具有多至6个碳原子，氮，氧和/或硫原子的直链“间隔”，其中最多2个原子可以是氮原子，1个原子可以是氧或硫，Y表示-CO-，-CS-，-CONH-和（其中X不含硫或羰基作为末端成分）之一的-SO 2 - ; 并且其中R 1和R 2一起表示一组甲酰胺A表示氢或可用于头孢菌素抗生素3位的残基，其中R3表示氢，以及这些化合物的药学上相容的盐。产品具有β β-内酰胺酶抑制性质。它们与β-内酰胺抗生素联合用于控制β-内酰胺酶形成病原体。

2. 发明授权

US6150350A Antimicrobial compositions 失效
标题翻译：抗微生物组合物
公开(公告)号：US6150350A
公开(公告)日：2000-11-21
申请号：US138866
申请日：1998-08-24
申请人： Peter Angehrn , Ingrid Heinze-Krauss , Malcolm Page , Hans G. F. Richter
发明人： Peter Angehrn , Ingrid Heinze-Krauss , Malcolm Page , Hans G. F. Richter
IPC分类号： C07D501/48 , A61K31/00 , A61K31/545 , A61K31/546 , A61K31/79 , A61P31/00 , A61P31/04 , C07D501/54 , C07D501/56 , C07D487/00 , C07D499/00 , C07D501/00
CPC分类号： A61K31/79
摘要： The invention relates to antimicrobial compositions comprising a combination of (1) a therapeutically effective amount of a compound of formula I ##STR1## with (2) a second ingredient selected from carbapenem antibiotics or with .beta.-lactamase inhibitors, to the use of the compositions for producing a medicament for the treatment and prophylaxis of infectious diseases, including MRSA infections, and to pharmaceutical compositions containing the combination.
摘要翻译：本发明涉及抗微生物组合物，其包含（1）治疗有效量的式I化合物与（2）选自碳青霉烯类抗生素或β-内酰胺酶抑制剂的第二种成分的组合，用于制备用于治疗和预防感染性疾病（包括MRSA感染）的药物和含有该组合的药物组合物。

3. 发明授权

US5935950A Cephalosporin pyridinium derivatives 失效
标题翻译：头孢菌素吡啶衍生物
公开(公告)号：US5935950A
公开(公告)日：1999-08-10
申请号：US924626
申请日：1997-09-05
申请人： Peter Angehrn , Ingrid Heinze-Krauss , Malcolm Page , Urs Weiss
发明人： Peter Angehrn , Ingrid Heinze-Krauss , Malcolm Page , Urs Weiss
IPC分类号： C07D501/04 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/16 , C07D501/24 , C07D501/56
CPC分类号： C07D501/00 , Y02P20/55
摘要： Compounds of formula I ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, cycloalkyl or acetyl;x is CH or N;n is 0, 1 or 2;m is 0 or 1;R.sup.2 is hydrogen, lower alkyl, .omega.-hydroxy alkyl, benzyl or lower alkyl-heterocyclyl, the benzyl and the heterocyclyl group being unsubstituted or substituted with at least one of the groups amino, cyano, carboxy, halogen, hydroxy, lower alkyl, lower alkoxy or --CONR.sub.2, where R is hydrogen or lower alkyl; or R.sup.2 is --CH.sub.2 CONR.sup.4 R.sup.5 ; whereinR.sup.4, R.sup.5 are each independently hydrogen, .omega.-hydroxy-alkyl, phenyl, benzyl, naphthyl or heterocyclyl, the phenyl, benzyl, naphthyl or heterocyclyl groups being unsubstituted or substituted with at least one of the groups optionally protected hydroxy, halogen, optionally substituted lower alkyl, optionally substituted lower alkoxy, .omega.-hydroxyalkyl or cyano; or R.sup.4 and R.sup.5 form together a group of formula ##STR2## with the proviso that when pyridinium ring A is pyridinium-4-yl, m is 1; as well as readily hydrolysable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts. These compounds are useful as parenteral antibiotics.
摘要翻译：其中R1是氢，低级烷基，环烷基或乙酰基的式Ⅰ化合物; x是CH或N; n为0,1或2; m为0或1; R2是氢，低级烷基，ω-羟基烷基，苄基或低级烷基 - 杂环基，苄基和杂环基是未取代的或被至少一个氨基，氰基，羧基，卤素，羟基，低级烷基，低级烷氧基或-CONR2，其中R是氢或低级烷基; 或R 2为-CH 2 CONR 4 R 5; 其中R 4，R 5各自独立地为氢，ω-羟基 - 烷基，苯基，苄基，萘基或杂环基，苯基，苄基，萘基或杂环基为未取代的或被至少一个选自羟基，卤素，取代的低级烷基，任选取代的低级烷氧基，ω-羟烷基或氰基; 或R 4和R 5一起形成式的基团，条件是当吡啶鎓环A为吡啶鎓-4-基时，m为1; 以及其易水解的酯，所述化合物的药学上可接受的盐和式I化合物的水合物及其酯和盐。这些化合物可用作胃肠外抗生素。

4. 发明授权

US5925632A Derivatives of 3-pyrrolidylidene-2-one-cephalsporines 失效
标题翻译： 3-吡咯烷亚基-2-单头孢菌素的衍生物
公开(公告)号：US5925632A
公开(公告)日：1999-07-20
申请号：US875563
申请日：1997-07-25
申请人： Ingrid Heinze-Krauss , Hans Richter
发明人： Ingrid Heinze-Krauss , Hans Richter
IPC分类号： C07D501/04 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/06 , C07D501/48 , C07D501/56
CPC分类号： C07D501/00 , Y02P20/55
摘要： Compounds of formula (I) ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, aralkyl, cycloalkyl, R.sup.3 CO-- or --C(R.sup.4 R.sup.5)CO.sub.2 R.sup.6 ; where R.sup.4 and R.sup.5 are each independently hydrogen or lower alkyl, or R.sup.4 and R.sup.5 taken together with the carbon atom to which they are attached form a cycloalkyl group; R.sup.3 is hydrogen or lower alkyl and R.sup.6 is hydrogen, lower alkyl, lower alkenyl or a carboxylic acid protecting group;R.sup.2 is isobutyl, 2,2-dimethyl-propyl or cyclohexyl-methyl;n is 0, 1 or 2;X is CH or N;as well as readily hydrolyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts are disclosed. These compounds have valuable antibacterial activity.
摘要翻译： PCT No.PCT / EP96 / 00667 Sec。 371日期1997年7月25日 102（e）日期1997年7月25日PCT提交1996年2月16日PCT公布。公开号WO96 / 26943 日期：1996年9月6日，式（I）化合物，其中R1为氢，低级烷基，芳烷基，环烷基，R3CO-或-C（R4R5）CO2R6; 其中R 4和R 5各自独立地为氢或低级烷基，或者R 4和R 5与它们所连接的碳原子一起形成环烷基; R3是氢或低级烷基，R6是氢，低级烷基，低级烯基或羧酸保护基; R2是异丁基，2,2-二甲基 - 丙基或环己基 - 甲基; n为0,1或2; X是CH或N; 以及其易水解的酯，所述化合物的药学上可接受的盐和式I化合物及其酯和盐的水合物被公开。这些化合物具有有价值的抗菌活性。

5. 发明授权

US5510343A Bicyclic and tricyclic .beta.-lactams 失效
公开(公告)号：US5510343A
公开(公告)日：1996-04-23
申请号：US474207
申请日：1995-06-07
申请人： Robert Charnas , Klaus Gubernator , Ingrid Heinze , Christian Hubschwerlen
发明人： Robert Charnas , Klaus Gubernator , Ingrid Heinze , Christian Hubschwerlen
IPC分类号： A61K31/40 , A61K31/397 , A61K31/43 , A61K31/435 , A61K31/545 , A61P31/04 , A61P43/00 , B01J8/12 , C07D471/16 , C07D487/04 , C07D487/16 , C12N9/99 , A61K31/445
CPC分类号： A61K31/43 , A61K31/545 , C07D487/04
摘要： There are described compounds of the formula ##STR1## in which R signifies lower alkoxycarbonyl, lower alkoxycarbonylamino, the acyl residue of an .alpha.- or .beta.-amino acid or a residue of the general formulaQ--X--Y-- (a)wherein Q signifies a 3- to 6-membered ring which optionally contains nitrogen, sulphur and/or oxygen and which is optionally bonded with a fused ring, X signifies a direct bond or a linear "spacer" with up to 6 atoms consisting of carbon, nitrogen, oxygen and/or sulphur, of which up to 2 atoms can be nitrogen atoms and 1 atom can be oxygen or sulphur, and Y represents one of the groups --CO--, --CS--, --CONH-- and (where X contains neither sulphur nor carbonyl as a terminal component) --SO.sub.2 --;and in which R.sup.1 signifies hydrogen, halogen, carbamoyloxy, lower alkanoyloxy or a group of the formula --S--Het, wherein Het represents a 5- or 6-membered heteroaromatic group containing nitrogen, sulphur and/or oxygen, and R.sup.2 represents the sulpho group --SO.sub.3 H or R.sup.1 and R.sup.2 together signify a group of the formula ##STR2## wherein A represents hydrogen or a residue which is usable in the 3-position of cephalosporin antibiotics, and in which R.sup.3 represents hydrogen or R.sup.1 and R.sup.3 together represent a group of the formula.dbd.CH--R.sup.a (c)wherein R.sup.a signifies one of the groups--COR.sup.b (c.sup.1)--CH.sub.2 --OCOR.sup.c (c.sup.2)--CH.sub.2 --NR.sup.d R.sup.e (c.sup.3)--CH.sub.2 --S--Het (c.sup.4)in which R.sup.b represents lower alkoxy or amino, R.sup.c represents lower alkyl, phenyl or amino, R.sup.d and R.sup.e each independently represent hydrogen or lower alkyl or R.sup.d and R.sup.e together with the N atom to which they are attached represent a 5- or 6-membered N-heterocycle which optionally contains a further nitrogen, oxygen or sulphur atom and Het represents a 5- or 6-membered heteroaromatic group containing nitrogen, sulphur and/or oxygen,and pharmaceutically compatible salts of these compounds.The products have .beta.-lactamase inhibiting properties. They are useful in combination with .beta.-lactam antibiotics in the control of .beta.-lactamase forming pathogens.

6. 发明授权

US5804577A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5804577A
公开(公告)日：1998-09-08
申请号：US708161
申请日：1996-08-27
申请人： Paul Hebeisen , Ingrid Heinze-Krauss , Hans Richter , Valeri Runtz , Henri Stalder , Urs Weiss , George Petros Yiannikouros
发明人： Paul Hebeisen , Ingrid Heinze-Krauss , Hans Richter , Valeri Runtz , Henri Stalder , Urs Weiss , George Petros Yiannikouros
IPC分类号： C07D501/24 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/56 , C07D501/34
CPC分类号： C07D501/00
摘要： The present invention relates to compounds of formula I ##STR1## wherein R.sup.1 is a group selected from 2-, 3-, and 4-hydroxyphenyl, 3-nitrophenyl, and 3-fluoro-4-hydroxyphenyl; as well as readily hydroyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts.
摘要翻译：本发明涉及式Ⅰ化合物，其中R1是选自2-，3-和4-羟基苯基，3-硝基苯基和3-氟-4-羟基苯基的基团; 以及其易水解的酯，所述化合物的药学上可接受的盐和式I化合物的水合物及其酯和盐。

7. 发明授权

US5712268A Compositions of tricyclic .beta.-lactams and uses thereof 失效
标题翻译：三环β-内酰胺的组合物及其用途
公开(公告)号：US5712268A
公开(公告)日：1998-01-27
申请号：US420385
申请日：1995-04-12
申请人： Christian Hubschwerlen , Robert Charnas , Ingrid Heinze , Klaus Gubernator
发明人： Christian Hubschwerlen , Robert Charnas , Ingrid Heinze , Klaus Gubernator
IPC分类号： A61K31/43 , A61K31/545 , B01J8/12 , C07D471/16 , C07D487/04 , A61K31/395 , A61K31/40
CPC分类号： C07D487/04 , A61K31/43 , A61K31/545 , B01J8/12
摘要： There are described pharmaceutical compositions comprising (a) compounds of the formula ##STR1## in which R signifies lower alkoxycarbonyl, lower alkoxy-carbonylamino, the acyl residue of an .alpha.- or .beta.-amino acid or a residue of the general formula Q--X--Y-- (a) wherein Q signifies a 3- to 6-membered ring which optionally contains nitrogen, sulphur and/or oxygen and which is optionally bonded with a fused ring, X signifies a direct bond or a linear "spacer" with up to 6 atoms consisting of carbon, nitrogen, oxygen and/or sulphur, of which up to 2 atoms can be nitrogen atoms and 1 atom can be oxygen or sulphur, and Y represents one of the groups --CO--, --CS--, --CONH-- and (where X contains neither sulphur nor carbonyl as a terminal component) --SO.sub.2 --; and in which R.sup.1 and R.sup.2 together signify a group of the formula ##STR2## wherein A represents hydrogen or a residue which is usable in the 3-position of cephalosporin antibiotics, and in which R.sub.3 represents hydrogen, or their pharmaceutically compatible salts; and (b) a therapeutically effective amount of a .beta.-lactam antibiotic or their pharmaceutically compatible salts; and a pharmaceutically acceptable carrier. The combination is useful in the control or prevention of illnesses caused by .beta.-lactamase forming pathogens.
摘要翻译：描述了药物组合物，其包含（a）式I化合物，其中R表示低级烷氧基羰基，低级烷氧基 - 羰基氨基，α-或β-氨基酸的酰基残基或通式Q-XY的残基 - （a）其中Q表示3至6元环，其任选地含有氮，硫和/或氧，并且其任选地与稠环键合，X表示直接键或具有多达6个的直链键或直链“间隔” 由碳，氮，氧和/或硫组成的原子，其中最多2个原子可以是氮原子和1个原子可以是氧或硫，Y代表-CO-，-CS-，-CONH- 和（其中X不含硫或羰基作为末端成分）-SO2-; 并且其中R 1和R 2一起表示一组式（B）其中A表示氢或可用于头孢菌素抗生素3位的残基，其中R 3表示氢，或其药学上相容的盐 ; 和（b）治疗有效量的β-内酰胺抗生素或其药学上相容的盐; 和药学上可接受的载体。该组合可用于控制或预防由β-内酰胺酶形成的病原体引起的疾病。

8. 发明授权

US06294668B1 Vinylpyrrolidinone cephalosporin derivatives 失效
公开(公告)号：US06294668B1
公开(公告)日：2001-09-25
申请号：US08964640
申请日：1997-11-05
申请人： Peter Angehrn , Ingrid Heinze-Krauss , Hans G. F. Richter
发明人： Peter Angehrn , Ingrid Heinze-Krauss , Hans G. F. Richter
IPC分类号： C07D50124
CPC分类号： C07D501/00 , Y02P20/55
摘要： The present invention relates to cephalosporin derivatives of the general formula where R1 is halogen, lower alkyl, phenyl, benzyl, styryl, naphthyl or heterocyclyl; the lower alkyl, phenyl, benzyl, styryl, naphthyl and heterocyclyl being optionally substituted by at least one of halogen, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkoxy, optionally substituted phenyl, amino, lower alkylamino, di-lower alkylamino, carboxy, lower alkylcarboxy, carbamoyl or lower alkylcarbamoyl; R4, R5 independently are hydrogen, lower alkyl or phenyl; X is S, O, NH or CH2; n is 0,1 or 2; m is 0 or 1; s is 0 or 1; R2 is hydrogen, hydroxy, —CH2—CONHR6, lower alkyl-Qr, cycloalkyl-Qr, lower alkoxy, lower alkenyl, cycloalkenyl-Qr, lower alkynyl, aralkyl-Qr, aryl-Qr, aryloxy, aralkoxy, a heterocyclic ring or a heterocyclyl-Qr, the lower alkyl, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aralkyl, aryl, aryloxy, aralkoxy and the heterocyclic ring may be substituted with at least one group selected from carboxy, amino, nitro, cyano, —SO2NHR6, optionally fluoro substituted lower alkyl, lower alkoxy, hydroxy, halogen, —CONR6R7, —CH2CONR6R7, —N(R7)COOR8, R7CO—, R7OCO—, R7COO —, —C(R7R9)CO2R8, —C(R7R9)CONR7R10, wherein R6 is hydrogen, lower alkyl, cycloalkyl or aryl; R7 and R9 are independently hydrogen or lower alkyl; R8 is hydrogen, lower alkyl, lower alkenyl or a carboxylic acid protecting group; and R10 is hydrogen, &ohgr;hydroxy-alkyl, phenyl, naphthyl or heterocyclyl, the phenyl, naphthyl or heterocyclyl being unsubstituted or substituted with at least one of the groups of optionally protected hydroxy, halogen, optionally substituted lower alkyl or &ohgr;-hydroxyalkyl, optionally substituted lower alkoxy and/or cyano, or R7 and R10 form together group of formula Q is —CHR—, —CO— or —SO2—; r is 0 or 1; R is hydrogen or lower alkyl; and R3 is hydroxy, —O−, lower-alkoxy, or —OM and M represents an alkali metal; as well as readily hydrolyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts, as well as the preparation of such compounds, their use for the treatment of infectious diseases and pharmaceutical preparations containing such compounds.

9. 发明授权

US5981519A Vinyl-pyrrolidinone cephalosporins 失效
标题翻译：乙烯基 - 吡咯烷酮头孢菌素
公开(公告)号：US5981519A
公开(公告)日：1999-11-09
申请号：US986549
申请日：1997-12-08
申请人： Peter Angehrn , Paul Hebeisen , Ingrid Heinze-Krauss , Malcolm Page , Valerie Runtz
发明人： Peter Angehrn , Paul Hebeisen , Ingrid Heinze-Krauss , Malcolm Page , Valerie Runtz
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D417/12 , C07D501/00 , C07D501/04 , C07D501/06 , C07D501/24 , C07D501/34 , C07D501/56 , C07F9/572 , C07F9/6558
CPC分类号： C07D417/12 , C07D501/00 , C07F9/5726 , C07F9/65583 , Y02P20/55
摘要： The present invention relates to compounds having the formula ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are as defined herein as well as readily hydrolyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts. These compounds have valuable pharmacological activity for the treatment and prophylaxis of infectious diseases, especially those caused by methicillin resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa.
摘要翻译：本发明涉及具有下式的化合物：其中X，R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所定义，以及其易水解的酯，所述化合物的药学上可接受的盐和化合物的水合物配方Ⅰ及其酯和盐。这些化合物具有有价值的药理活性，用于治疗和预防感染性疾病，特别是由耐甲氧西林金黄色葡萄球菌（MRSA）和铜绿假单胞菌引起的那些。

10. 发明授权

US5939410A 1-carba-(dethia)-cephalosporin derivatives 失效
标题翻译： 1-卡巴（dethia） - 头孢菌素衍生物
公开(公告)号：US5939410A
公开(公告)日：1999-08-17
申请号：US929248
申请日：1997-09-10
申请人： Peter Angehrn , Paul Hebeisen , Ingrid Heinze-Krauss , Malcolm Page
发明人： Peter Angehrn , Paul Hebeisen , Ingrid Heinze-Krauss , Malcolm Page
IPC分类号： C07D463/14 , A61K31/435 , A61K31/4353 , A61K31/445 , A61K31/4545 , A61P31/04 , C07D463/00
CPC分类号： C07D463/22 , Y02P20/55
摘要： Compounds of formula I whereinR.sup.1 is hydrogen, lower alkyl which is unsubstituted or substituted by fluoro, aralkyl, cycloalkyl, --COR.sup.4 or --C(R.sup.5 R.sup.6)CO.sub.2 R.sup.7 --C(R.sup.5 R.sup.6)CONHR.sup.7 ; where R.sup.5 and R.sup.6 are each independently hydrogen or lower alkyl, or R.sup.5 and R.sup.6 taken together form a cycloalkyl group; R.sup.4 is hydrogen or lower alkyl and R.sup.7 is hydrogen, lower alkyl, lower alkenyl or a carboxylic acid protecting group;R.sup.2 is hydrogen, hydroxy, lower alkyl-Q.sub.m, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aralkyl-Q.sub.m, aryl-Q.sub.m, aryloxy, aralkoxy, a heterocyclic ring or heterocyclyl lower alkyl, the lower alkyl, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aralkyl, aryl, aryloxy, aralkoxy and the heterocyclic ring being unsubstituted or substituted with at least one group selected from carboxy, amino, nitro, cyano, lower alkyl which is unsubstituted or substituted by fluoro, lower alkoxy, hydroxy, halogen, --COR.sup.6, --C(R.sup.5 R.sup.6)CO.sub.2 R.sup.7, --C(R.sup.5 R.sup.6)CONR.sup.5 R.sup.8, --CONR.sup.5 R.sup.6, --N(R.sup.6)COOR.sup.10, R.sup.6 OCO-- or R.sup.6 COO-- where R.sup.5 and R.sup.6 are hydrogen or lower alkyl; R.sup.7 is hydrogen, lower alkyl, lower alkenyl or a carboxylic acid protecting group; R.sup.8 is hydrogen, lower alkyl or phenyl which is unsubstituted or substituted with at least one halogen, hydroxy, amino, lower alkyl, or lower alkoxy; R.sup.10 is lower alkyl, lower alkenyl or a carboxylic acid protecting group;Q is --CHR--, --CO-- or --SO.sub.2 --;R is hydrogen or lower alkyl;R.sup.3 is hydroxy, --O--, lower alkoxy, --OM and M represents an alkali metal;m is 0 or 1;n is 0, 1 or 2;x is CH or Nas well as readily hydrolysable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts are provided. These compounds have valuable antiinfective properties.
摘要翻译：式I化合物，其中R 1是氢，未被取代或被氟取代的低级烷基，芳烷基，环烷基，-COR 4或-C（R 5 R 6）CO 2 R 7 -C（R 5 R 6）CONHR 7; 其中R 5和R 6各自独立地为氢或低级烷基，或者R 5和R 6一起形成环烷基; R4是氢或低级烷基，R7是氢，低级烷基，低级烯基或羧酸保护基; R2是氢，羟基，低级烷基-Qm，环烷基，低级烷氧基，低级烯基，环烯基，低级炔基，芳烷基-Qm，芳基-Qm，芳氧基，芳烷氧基，杂环或杂环基低级烷基，低级烷基，环烷基，低级烷氧基，低级烯基，环烯基，低级炔基，芳烷基，芳基，芳氧基，芳烷氧基，杂环是未取代的或被至少一个选自羧基，氨基，硝基，氰基，未被取代或被氟取代的低级烷基，低级烷氧基，羟基，卤素，-COR6，-C（R5R6）CO2R7，-C（R5R6）CONR5R8，-CONR5R6，-N（R6）COOR10，R6OCO-或R6COO-，其中R5和R6是氢或低级烷基; R7是氢，低级烷基，低级烯基或羧酸保护基; R8是氢，低级烷基或未取代的或被至少一个卤素，羟基，氨基，低级烷基或低级烷氧基取代的苯基; R 10为低级烷基，低级烯基或羧酸保护基; Q是-CHR-，-CO-或-SO 2 - ; R是氢或低级烷基; R3是羟基，-O-，低级烷氧基，-OM，M代表碱金属; m为0或1; n为0,1或2; x是CH或N，以及其易水解的酯，所述化合物的药学上可接受的盐和式I化合物的水合物及其酯和盐。这些化合物具有有价值的抗感染性。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式