CAS: 61270-58-4; Cefonicid

上下游产品

(R)-methyl mandelate 7-amino-3-(1-sulfomethyl-1H-1,2,3,4-tetrazol-5-yl)thiomethyl-3-cephem-4-carboxylic acid

📜(R)-(-)-扁桃酸甲酯,(6R-反式)-7-氨基-8-氧代-3-(((1-(磺酸甲基)-1H-四唑-5-基)硫)甲基)-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸置于3G3K Penicillin G Acylase Immobilized On Glyoxyl Agarose体系中,化学反应生成 头孢尼西
参考文献:定点诱变和固定化的耦合用于更高效生物催化剂的合理设计:来自大肠杆菌的固定化 3G3K Pga 的案例
标题:定点诱变和固定化的耦合用于更高效生物催化剂的合理设计:来自大肠杆菌的固定化 3G3K Pga 的案例
摘要:我们研究了通过定点诱变获得的来自大肠杆菌的青霉素 G 酰基转移酶 (Pga) 的固定化 3G3K 突变体的合成性能.3G3K 突变体的特征是由三个赖氨酸与 β 链末端的三个甘氨酸交替组成的标签,之前曾报道过抗生素合成速率和酰化剂水解速率的比率更高. Vs/vh1 值)比野生型酶.通过使用不同的乙醛基支持物(用醛基激活),对 3G3K 突变体进行了新的固定研究.在通过动力学控制的 N-酰化 (Kcna) 合成头孢曼多和头孢尼西的过程中测试了新固定化制剂的催化性能.与商业野生型 Pga 相比,
DOI:10.1002/ejoc.200801204

专利信息

专利号:US-7199128-B2
优先权日:2005-02-02
标题 :8-N-substituted-2H-isothiazolo[5,4-b]quinolizine-3,4-diones and related compounds as antiinfective agents
发明人：BRADBURY BARTON J; WILES JASON ALLAN; DESHPANDE MILIND; WANG QIUPING; HASHIMOTO AKIHIRO; LUCIEN EDLAINE
权利人:ACHILLION PHARMACEUTICALS INC
摘要:The invention provides compounds and salts of Formula I and Formula II: n nwhich possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A 1 , A 8 , R 2 , R 3 , R 5 , R 6 , R 7 , and R 9 are defined herein.n n Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of compounds of Formula I and/or Formula II and one or more other active agents. The invention also provides methods for treating microbial and protozoal infections in animals.

专利号:US-2009012071-A1
优先权日:2007-04-23
标 题 :4-substituted-1h-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2h,9h)-diones and related compounds as anti-infective agents
发明人：BRADBURY BARTON JAMES; DESHPANDE MILIND; HASHIMOTO AKIHIRO; KIM HA YOUNG; LUCIEN EDLAINE; PAIS GODWIN; PUCCI MICHAEL JOHN; WANG QIUPING; WILES JASON ALLAN
权利人:ACHILLION PHARMACEUTICALS INC
摘要:The present invention provides compounds of the formula that possess antimicrobial activity. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity. Particular compounds provided herein are also potent and/or selective inhibitors of microbial DNA synthesis and reproduction. The invention provides anti-microbial compositions, including pharmaceutical compositions, containing a compound of the invention and one or more or more carriers. The invention provides pharmaceutical compositions containing a 4-substituted- 1 H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound as the only active agent or in combination with one or more other active agents. The invention provides methods for treating or preventing microbial infections, preferably animals, by administering an effective amount of a 4-substituted- 1 H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound to an organism suffering from or susceptible to microbial infection. The invention also provides methods of inhibiting microbial growth and survival by applying an effective amount of a 4-substituted- 1 H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound.

专利号:US-8946422-B2
优先权日:2005-07-27
标题:8-methoxy-9H-isothiazolo[5,4-B]quinoline-3,4-diones and related compounds as anti-infective agents
发明人：BRADBURY BARTON JAMES; WILES JASON ALLAN; WANG QIUPING; HASHIMOTO AKHIRO; LUCIEN EDLAINE; PAIS GODWIN CLARENCE GILROY; DESHPANDE MILIND; PUCCI MICHEAL JOHN; KIM HA YOUNG
权利人:BRADBURY BARTON JAMES; WILES JASON ALLAN; WANG QIUPING; HASHIMOTO AKHIRO; LUCIEN EDLAINE; PAIS GODWIN CLARENCE GILROY; DESHPANDE MILIND; PUCCI MICHEAL JOHN; KIM HA YOUNG; ACHILLION PHARMACEUTICALS INC
摘要:The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: Such compounds possess useful antimicrobial activity. The variables R2, R3, R5, R6, R7, and R9 shown in Formula A and B are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

专利号:US-7659399-B2
优先权日:2005-01-05
标 题 :1-thia-2,4a-diaza-cyclopenta[b]napththalene-3,4-diones and related compounds as anti-infective agents
发明人：BRADBURY BARTON JAMES; WILES JASON ALLAN
权利人:ACHILLION PHARMACEUTICALS INC
摘要:The invention provides compounds and salts of Formula I and Formula II: n nwhich possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A 1 , A 8 , R 2 , R 3 , R 5 , R 6 , R 7 , and R 9 are defined herein.n n Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

专利号:EP-1809639-B1
优先权日:2004-11-11
标 题 :8a, 9-dihydro-4a-h-isothiazolo[5,4-b] quinoline-3, 4-diones and related compounds as anti-infective agents
发明人：BRADBURY BARTON JAMES; DESHPANDE MILIND; PUCCI MICHAEL JOHN; WANG QIUPING; WILES JASON ALLAN; SONG YONGSHENG; HASHIMOTO AKIHIRO; LUCIEN EDLAINE
权利人:ACHILLION PHARMACEUTICALS INC
摘要:The invention provides compounds and salts of Formula I and Formula II: which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables n, m, p, R_A, R_B, A₁, R₂, R₃, R₅, R₆, R₇, A₈ and R₉ are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in eukaryotes.