32380-69-1Relevant academic research and scientific papers
Solid Supports for the Synthesis of 3′-Aminooxy Deoxy- or Ribo-oligonucleotides and Their 3′-Conjugation by Oxime Ligation
No?l, Mathieu,Clément-Blanc, Céline,Meyer, Albert,Vasseur, Jean-Jacques,Morvan, Fran?ois
, p. 14854 - 14860 (2019)
Mono- and triethylene glycol aminooxy derivatives were reacted with levulinic acid, protected with dimethoxytrityl, and immobilized on solid support. The resulting solid supports were used for elongation of oligonucleotides. Then, a mild ammonia treatment was applied to remove the oligonucleotide protecting groups, followed by a treatment with 50 mM methoxyamine at pH 4.2, releasing the 3′-aminooxy oligonucleotides by an oxime exchange reaction. The resulting 3′-aminooxy deoxy- or ribo-oligonucleotides were conjugated to various ketones and aldehydes with high efficiency by oxime ligation.
Synthesis of (2,4)Pyridinophanes
Dhanak, Dashyant,Reese, Colin B.
, p. 2829 - 2832 (1987)
The (2,4)pyridinophane derivatives have been prepared by treating 4,5,6,7,8,9-hexahydro-1H-cyclo-octapyrrole (5b) with dichloro- and dibromo-carbene, respectively.The respective yields of compounds (11a) and (11b) obtained were modest and poor.
INDENE DERIVATIVES USEFUL IN TREATING PAIN AND INFLAMMATION
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Page/Page column 240, (2019/10/29)
Compounds of formula (I) wherein, R1, R2, R3, R4a, R4b and R5 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solv
Discovery of Novel Pyridone-Conjugated Monosulfactams as Potent and Broad-Spectrum Antibiotics for Multidrug-Resistant Gram-Negative Infections
Tan, Liang,Tao, Yunliang,Wang, Ting,Zou, Feng,Zhang, Shuhua,Kou, Qunhuan,Niu, Ao,Chen, Qian,Chu, Wenjing,Chen, Xiaoyan,Wang, Haidong,Yang, Yushe
supporting information, p. 2669 - 2684 (2017/04/21)
Conjugating a siderophore to an antibiotic is a promising strategy to overcome the permeability-mediated resistance of Gram-negative pathogens. On the basis of the structure of BAL30072, novel pyridone-conjugated monosulfactams incorporating diverse substituents into the methylene linker between the 1,3-dihydroxypyridin-4(1H)-one and the aminothiazole oxime were designed and synthesized. Structure-activity relationship studies revealed that a variety of substituents were tolerated, with isopropyl (compound 12c) and methylthiomethyl (compound 16a) showing the best efficacy against multidrug-resistant (MDR) Gram-negative pathogens. In addition, compound 12c exhibits a good free fraction rate in an in vitro human plasma protein binding test, along with a low clearance and favorable plasma exposure in vivo. In a murine systemic infection model with MDR Klebsiella pneumoniae, compound 12c shows an ED50 of 10.20 mg/kg. Taken together, the results indicate that compound 12c is a promising drug candidate for the treatment of serious infections caused by MDR Gram-negative pathogens.
METHOD OF TREATING CANCER WITH A COMBINATION OF BENZYLIDENEGUANIDINE DERIVATIVES AND CHEMOTHERAPEUTIC AGENT.
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Page/Page column 51-52, (2017/03/08)
The present invention relates to a composition for use in treating a glioma or ameliorating the effects of a glioma, particularly glioblastoma, wherein said composition comprises a first active agent selected from the group consisting of a compound of for
BICYCLIC ARYL MONOBACTAM COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF BACTERIAL INFECTIONS
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Page/Page column 86, (2017/09/27)
The present invention relates to bicyclic aryl monobactam compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein A1, L, M, W, X, Y, Z, RX and Rz are as defined herein. The present invention also relates to compositions which comprise a bicyclic aryl monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of one or more beta-lactamase inhibitor compounds.
NOVEL CRYSTAL FORM OF 3,4-DIFLUORO-2-(2-FLUORO-4-IODO-PHENYL AMINO)-N-(2-HYDROXY-ETHOXY)-5-(3-OXO-[1,2]OXAZINAN-2-YLMETHYL)-BENZAMIDE
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Paragraph 0039; 0051; 0052; 0053, (2016/10/09)
PROBLEM TO BE SOLVED: To provide an active pharmaceutical ingredient that is useful as MEK inhibitors and is stable physicochemically. SOLUTION: The present invention provides an educt I-type crystal of 3,4-difluoro-2-(2-fluoro-4-iodo-phenyl amino)-n-(2-hydroxy-ethoxy)-5-(3-oxo-[1,2]oxazinan-2-ylmethyl)-benzamide, having peaks with diffraction angles expressed by 2θ of 14.9, 16.9 and 23.1° (±0.2°) in a powder X-ray diffraction pattern measured using Cu Kα(1.54060?) as an X-ray source. SELECTED DRAWING: None COPYRIGHT: (C)2016,JPOandINPIT
NANOPARTICLES FOR DRUG DELIVERY
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Page/Page column 53, (2016/04/20)
The invention provides therapeutic magnetic nanoparticles containing a therapeutic agent connected to a magnetic nanoparticle core through a stable functional group and a linker that can be induced to release the therapeutic agent from the core, through h
O-ALKYL-BENZYLIDENEGUANIDINE DERIVATIVES AND THERAPEUTIC USE FOR THE TREATMENT OF DISORDERS ASSOCIATED AN ACCUMULATION OF MISFOLDED PROTEINS
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Page/Page column 65, (2016/01/25)
The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof Formula (I), and its uses to treat a disorder associated with protein misfolding stress and in particular with an accumulation of m
The composite body deproteinizing chitosanoligosaccharide-
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Page/Page column 87, (2016/10/09)
Provided herein are conjugates comprising a protein and an oligosaccharide of one of Formulae I-VI. Also provided herein are pharmaceutical compositions comprising such conjugates. Further provided herein are methods of treating a lysosomal storage disorder in a mammal by administration of an oligosaccharide-glycoprotein conjugate.
