-
公开(公告)号:US20140221331A1
公开(公告)日:2014-08-07
申请号:US14117742
申请日:2012-05-16
发明人: Nicolas Barraud , Bharat Gangadhar Kardak , Michael John Kelso , Staffan Kjelleberg , Scott Rice
IPC分类号: C07D501/46 , A01N51/00 , A61K31/545 , A61K31/546 , C07D501/42
CPC分类号: C07D501/46 , A01N51/00 , A61K31/545 , A61K31/546 , A61K45/06 , A61K47/55 , C07D501/30 , C07D501/34 , C07D501/42 , C07D501/54 , C07D501/56 , C07D503/18 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/481
摘要: The present invention relates generally to methods and compounds for regulating the release of nitric oxide in the vicinity of biofilm-forming microorganisms to regulate programmed cell death in the microorganisms and thereby promote dispersal of microorganism from biofilms and/or inhibit biofilm formation or development. More particularly, the invention relates to the use of compounds to provide spatial and temporal control over nitric oxide release.
摘要翻译: 本发明一般涉及用于调节生物膜形成微生物附近的一氧化氮释放的方法和化合物,以调节微生物中的程序性细胞死亡,从而促进微生物从生物膜的分散和/或抑制生物膜形成或发育。 更具体地说,本发明涉及使用化合物来提供对一氧化氮释放的空间和时间控制。
-
公开(公告)号:US08188311B2
公开(公告)日:2012-05-29
申请号:US12557030
申请日:2009-09-10
申请人: V. Ravi Chandran
发明人: V. Ravi Chandran
IPC分类号: C07C229/00
CPC分类号: A61K38/12 , A61K38/10 , A61K45/06 , A61K47/542 , C07C229/08 , C07C229/22 , C07C229/26 , C07C229/36 , C07C233/47 , C07C2602/22 , C07D207/33 , C07D209/10 , C07D209/14 , C07D211/34 , C07D211/90 , C07D215/38 , C07D217/26 , C07D223/16 , C07D239/10 , C07D261/20 , C07D265/18 , C07D275/04 , C07D295/185 , C07D311/24 , C07D311/32 , C07D333/58 , C07D401/06 , C07D401/12 , C07D403/10 , C07D405/14 , C07D409/06 , C07D413/06 , C07D473/18 , C07D473/34 , C07D493/04 , C07D493/10 , C07D495/04 , C07D498/06 , C07D498/14 , C07D499/14 , C07D501/22 , C07D501/34 , C07D501/46 , C07D501/56 , C07F9/572 , C07F9/65616
摘要: The present invention is directed to a derivative comprised of an L-Threonine bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. The derivative has the same utility as the drug from which it is made, but it has enhanced therapeutic properties. In fact, the derivatives of the present invention enhance at least one or more therapeutic qualities, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.
摘要翻译: 本发明涉及由与其上具有羟基,氨基,羧基或酰化衍生物的药物或药物结合的L-苏氨酸组成的衍生物。 该衍生物与其制备的药物具有相同的效用,但具有增强的治疗性质。 事实上,本发明的衍生物增强至少一种或多种如本文所定义的治疗质量。 本发明还涉及含有其的药物组合物。
-
公开(公告)号:US07696354B2
公开(公告)日:2010-04-13
申请号:US12100307
申请日:2008-04-09
IPC分类号: C07D277/38
CPC分类号: C07D501/56 , A61K31/546 , C07D501/00
摘要: A compound of the formula: (wherein, T is S, SO or O; X is halogen, CN, carbamoyl optionally substituted with lower alkyl, lower alkyl, lower alkoxy, or lower alkylthio; A is substituted lower alkylene (wherein the substituent is optionally substituted mono lower alkyl, optionally substituted lower alkylidene, or optionally substituted lower alkylene); Z+ is an optionally substituted, a cation and an N atom-containing heterocyclic group), ester, amino-protected compound wherein the amino bonds to a thiazole ring at the 7-position, or pharmaceutically acceptable salt or solvate thereof.
摘要翻译: 下式的化合物:其中T是S,SO或O; X是卤素,CN,任选被低级烷基,低级烷基,低级烷氧基或低级烷硫基取代的氨基甲酰基; A是取代的低级亚烷基(其中取代基是 任选取代的单低级烷基,任选取代的低级亚烷基或任选取代的低级亚烷基); Z +是任选取代的,阳离子和含N原子的杂环基团),酯,氨基保护的化合物,其中氨基与噻唑环 在7-位,或其药学上可接受的盐或溶剂化物。
-
公开(公告)号:US20100004481A1
公开(公告)日:2010-01-07
申请号:US12556968
申请日:2009-09-10
申请人: V. Ravi Chandran
发明人: V. Ravi Chandran
IPC分类号: C07C69/88 , C07C229/00
CPC分类号: A61K38/12 , A61K38/10 , A61K45/06 , A61K47/542 , C07C229/08 , C07C229/22 , C07C229/26 , C07C229/36 , C07C233/47 , C07C2602/22 , C07D207/33 , C07D209/10 , C07D209/14 , C07D211/34 , C07D211/90 , C07D215/38 , C07D217/26 , C07D223/16 , C07D239/10 , C07D261/20 , C07D265/18 , C07D275/04 , C07D295/185 , C07D311/24 , C07D311/32 , C07D333/58 , C07D401/06 , C07D401/12 , C07D403/10 , C07D405/14 , C07D409/06 , C07D413/06 , C07D473/18 , C07D473/34 , C07D493/04 , C07D493/10 , C07D495/04 , C07D498/06 , C07D498/14 , C07D499/14 , C07D501/22 , C07D501/34 , C07D501/46 , C07D501/56 , C07F9/572 , C07F9/65616
摘要: The present invention is directed to a derivative comprised of an L-Threonine bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. The derivative has the same utility as the drug from which it is made, but it has enhanced therapeutic properties. In fact, the derivatives of the present invention enhance at least one or more therapeutic qualities, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.
-
公开(公告)号:US07589233B2
公开(公告)日:2009-09-15
申请号:US11442027
申请日:2006-05-26
申请人: V. Ravi Chandran
发明人: V. Ravi Chandran
IPC分类号: C07C229/00
CPC分类号: A61K38/12 , A61K38/10 , A61K45/06 , A61K47/542 , C07C229/08 , C07C229/22 , C07C229/26 , C07C229/36 , C07C233/47 , C07C2602/22 , C07D207/33 , C07D209/10 , C07D209/14 , C07D211/34 , C07D211/90 , C07D215/38 , C07D217/26 , C07D223/16 , C07D239/10 , C07D261/20 , C07D265/18 , C07D275/04 , C07D295/185 , C07D311/24 , C07D311/32 , C07D333/58 , C07D401/06 , C07D401/12 , C07D403/10 , C07D405/14 , C07D409/06 , C07D413/06 , C07D473/18 , C07D473/34 , C07D493/04 , C07D493/10 , C07D495/04 , C07D498/06 , C07D498/14 , C07D499/14 , C07D501/22 , C07D501/34 , C07D501/46 , C07D501/56 , C07F9/572 , C07F9/65616
摘要: The present invention is directed to a derivative comprised of an L-Threonine bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. The derivative has the same utility as the drug from which it is made, but it has enhanced therapeutic properties. In fact, the derivatives of the present invention enhance at least one or more therapeutic qualities, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.
摘要翻译: 本发明涉及由与其上具有羟基,氨基,羧基或酰化衍生物的药物或药物结合的L-苏氨酸组成的衍生物。 该衍生物与其制备的药物具有相同的效用,但具有增强的治疗性质。 事实上,本发明的衍生物增强至少一种或多种如本文所定义的治疗质量。 本发明还涉及含有其的药物组合物。
-
公开(公告)号:US20090111737A1
公开(公告)日:2009-04-30
申请号:US12082666
申请日:2008-04-11
申请人: Burton G. Christensen , Edmund J. Moran , John H. Griffin , J. Kevin Judice , YongQi Mu , John L. Pace , Mathai Mammen , James Aggen
发明人: Burton G. Christensen , Edmund J. Moran , John H. Griffin , J. Kevin Judice , YongQi Mu , John L. Pace , Mathai Mammen , James Aggen
CPC分类号: C07D477/12 , C07D499/32 , C07D499/44 , C07D501/56
摘要: This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands has a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.
摘要翻译: 本发明涉及作为抗菌剂的新型多结合化合物(试剂)。 本发明的多相结合化合物包含2-10个配体,其通过连接体或连接体共价连接,其中所述各单体(即,未连接)状态的所述配体具有结合涉及细胞壁生物合成和代谢的酶的能力 用于合成细菌细胞壁和/或细菌细胞表面的前体因而干扰细胞壁的合成和/或代谢。 特别地,本发明的多相结合化合物包含通过接头或接头共价连接的2-10个配体,其中每个所述配体具有能够结合青霉素结合蛋白的配体结构域,转肽酶,转肽酶的底物, β-内酰胺酶,pencillinase酶,头孢菌素酶,转糖基酶或转糖基酶酶底物; 优选地,配体选自β-内酰胺或糖肽类抗菌剂。
-
公开(公告)号:US20050153950A1
公开(公告)日:2005-07-14
申请号:US10507502
申请日:2003-03-18
IPC分类号: A61K31/546 , A61P31/04 , C07D277/40 , C07D277/46 , C07D277/56 , C07D501/00 , C07D501/50 , C07D519/06 , A61K31/545 , A61K31/5383 , C07D501/14
CPC分类号: C07D501/56 , A61K31/546 , C07D501/00
摘要: A compound of the formula: (wherein, T is S, SO or O; X is halogen, CN, carbamoyl optionally substituted with lower alkyl, lower alkyl, lower alkoxy, or lower alkylthio; A is substituted lower alkylene (wherein the substituent is optionally substituted mono lower alkyl, optionally substituted lower alkylidene, or optionally substituted lower alkylene); Z+ is an optionally substituted, a cation and an N atom-containing heterocyclic group), ester, amino-protected compound wherein the amino bonds to a thiazole ring at the 7-position, or pharmaceutically acceptable salt or solvate thereof.
摘要翻译: 下式的化合物:其中T是S,SO或O; X是卤素,CN,任选被低级烷基,低级烷基,低级烷氧基或低级烷硫基取代的氨基甲酰基; A是取代的低级亚烷基(其中取代基是 任选取代的单低级烷基,任选取代的低级亚烷基或任选取代的低级亚烷基); Z +是任选取代的阳离子和含N原子的杂环基),酯,氨基保护的化合物 其中氨基与7-位的噻唑环或其药学上可接受的盐或溶剂化物的键合。
-
公开(公告)号:US20170226126A1
公开(公告)日:2017-08-10
申请号:US15503564
申请日:2015-08-14
IPC分类号: C07D501/56 , C07D501/04 , C07D501/24
CPC分类号: C07D501/56 , C07B2200/13 , C07D501/04 , C07D501/24 , C07D501/54 , Y02P20/55
摘要: Described herein are crystalline forms of a compound of formula (III−), including toluene solvates off A TD-CLE, as well as processes for the preparation thereof and use thereof in the preparation of cephalosporin compounds such as ceftolozane. Provided herein is a crystalline form of a compound of formula (III−): wherein X is CI, Br, or I; and R1 and R2 are each independently an oxygen protecting group; processes for making the crystalline form, and use of said form in the synthesis of antibacterial cephalosporins such as ceftolozane.
-
公开(公告)号:US20170166587A1
公开(公告)日:2017-06-15
申请号:US15369181
申请日:2016-12-05
发明人: Samarendra Nath MAITI , Dai Quoc NGUYEN , Andhe V.N. REDDY , Judy YIP , Chan Minh HA , Rong LING , Rudong SHAN , Madhava Reddy MADALA
IPC分类号: C07D501/56 , C07D501/04 , A61K31/546
CPC分类号: C07D501/56 , A61K31/546 , C07D501/04
摘要: Cephem compounds, pharmaceutically acceptable salts thereof, and methods of using same, wherein the compound has a bicyclic nitrogen-containing aromatic heterocyclic ring as the quaternary ammoniomethyl group at the 3-position and one or both of a terminal amidine residue (substituted or unsubstituted) attached to an aryl or a 5- or 6-membered heteroaryl group (substituted or unsubstituted) which is further attached through a spacer to the free N-atom of the quaternary nitrogen-containing bicyclic ring at the 3-side chain, or a terminal guanidine residue attached to an aryl or a 5- or 6-membered heteroaryl group (substituted or unsubstituted) which is further attached through a spacer to the free N-atom of the quaternary nitrogen-containing bicyclic ring at the 3-side chain.
-
公开(公告)号:US09145425B2
公开(公告)日:2015-09-29
申请号:US13639412
申请日:2011-04-04
申请人: Shinya Hisakawa , Yasushi Hasegawa , Toshiaki Aoki , Hiroki Kusano , Masayuki Sano , Jun Sato , Kenji Yamawaki
发明人: Shinya Hisakawa , Yasushi Hasegawa , Toshiaki Aoki , Hiroki Kusano , Masayuki Sano , Jun Sato , Kenji Yamawaki
IPC分类号: C07D471/08 , C07D501/56 , C07D505/24 , C07D501/46 , C07D519/06
CPC分类号: C07D505/24 , C07D471/08 , C07D501/46 , C07D501/56 , C07D519/06
摘要: This invention provides Cephem compounds having the formula: or an ester, a protected compound at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof, a pharmaceutical composition thereof, and a method for treating a bacterial infectious disease with the compound, the ester, the protected compound, the salt, or the solvate thereof, wherein the symbols in the formula are defined in the specification. The compounds exhibit potent antimicrobial spectrum against a variety of bacteria including Gram negative bacteria and/or Gram positive bacteria, preferably beta-lactamase producing Gram negative bacteria, more preferably, multi-drug resistant microbials, in particular, Class B type metallo-beta-lactamase producing Gram negative bacteria, and still preferably extended-spectrum beta-lactamase (ESBL) producing bacteria. The compounds most preferably do not exhibit cross-resistance against known Cephem drugs or Carbapenem drugs.
摘要翻译: 本发明提供具有下式的Cephem化合物:或酯,7-侧链上的环上的氨基上的被保护的化合物,其药学上可接受的盐或溶剂合物,其药物组合物和 化合物,酯,受保护化合物,盐或其溶剂化物的细菌感染性疾病,其中式中的符号在说明书中定义。 该化合物对各种细菌(包括革兰氏阴性细菌和/或革兰氏阳性细菌,优选β-内酰胺酶产生革兰氏阴性细菌,更优选多药耐药性微生物,特别是B类金属β- 产生革兰氏阴性细菌的内酰胺酶,更优选延长的β-内酰胺酶(ESBL)产生细菌。 该化合物最优选不表现出对已知的Cephem药物或碳青霉烯类药物的抗药性。
-
-
-
-
-
-
-
-
-