872715-62-3Relevant articles and documents
Preparation and application of imidazo aromatic ring compounds
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, (2020/05/02)
The invention provides preparation and application of imidazo aromatic ring compounds, and particularly provides compounds as shown in the following formula I. The definition of each group is as shownin the specification. The compounds have TRK kinase inh
FUSED QUADRACYCLIC COMPOUNDS, COMPOSITIONS AND USES THEREOF
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Paragraph 0394, (2017/08/01)
Provided herein are substituted fused quadracyclic compounds useful as inhibitors of MK2. The invention further provides pharmaceutical compositions of the compounds of the invention. The invention also provides medical uses of substituted fused quadracyclic compounds.
SUBSTITUTED 1-METHYL-1H-QUINOLIN-2-ONES AND 1-METHYL-1H-1,5-NAPHTHYRIDIN-2-ONES AS ANTIBACTERIALS
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Page/Page column 17; 26, (2008/06/13)
Bicyclic nitrogen containing compounds of formula (I) and their use as antibacterials.
NOVEL COMPOUNDS
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Page/Page column 31, (2008/06/13)
This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain substituted pyrrolidines, according to Formula (I) specifically, the invention is di
ANTIBACTERIAL AGENTS
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Page/Page column 104-105, (2010/02/15)
Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
Synthesis and biological activity of novel 1β-Methylcarbapenems with oxyiminopyrrolidinylamide moiety
Lee, Ji Hoon,Lee, Kyung Seok,Kang, Yong Koo,Yoo, Kyung Ho,Shin, Kye Jung,Kim, Dong Chan,Kong, Jae Yang,Lee, Yeonhee,Lee, Sook Ja,Kim, Dong Jin
, p. 4399 - 4403 (2007/10/03)
The synthesis and antibacterial activity of novel 1β- methylcarbapenems 1a-f bearing oxyiminopyrrolidinylamide moiety at C-5 position of pyrrolidine are described. Most compounds exhibited comparable antibacterial activity to meropenem against a wide range of Gram-positive and Gram-negative organisms including Pseudomonas aeruginosa isolates. Of these carbapenems, 1a showed potent and broad spectrum of antibacterial activity and similar stability to DHP-I to meropenem. Against clinical isolates of 40 Gram-negative bacterial species including MDR and ESBL-producing strains, the selected carbapenem 1a possessed excellent in vitro activity except for MDR P. aeruginosa, and was comparable in potency to meropenem.
Discovery of gemifloxacin (Factive, LB20304a): A quinolone of new a generation
Hong, Chang Yong
, p. 41 - 44 (2007/10/03)
Novel quinolone antibacterials, which bear an alkyloxime substituent in the 4-position and an aminomethyl substituent in the 3-position of the pyrrolidine ring, have been designed and synthesized. These fluoroquinolones were found to possess extremely potent antimicrobial activity against Gram-positive organisms including resistant strains such as methicillin-resistant Staphylococcus aureus (MRSA). Among these compounds our development candidate, Gemifloxacin (Factive, LB20304a), showed the best in vivo efficacy and pharmacokinetic profile in animals, as well as good safety pharmacological properties. Gemifloxacin was found to be especially effective against respiratory tract infections that account for over 70% of all infections. With once-a-day dosage, potency against respiratory tract infections such as chronic bronchitis and pneumonia was ensured without any significant side effect. In December 1999, Gemifloxacin filed a NDA for marketing approval to the US Food and Drug Administration. Copyright
Novel fluoroquinolone antibacterial agents containing oxime-substituted (Aminomethyl)pyrrolidines: Synthesis and antibacterial activity of 7-(4- (Aminomethyl)-3-(methoxyimino) pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4- oxo-1,4-dihydro[1,8]naphthyridine-3-carboxylic acid (LB20304)
Hong, Chang Yong,Kim, Young Kwan,Chang, Jay Hyok,Kim, Se Ho,Choi, Hoon,Nam, Do Hyun,Kim, Yong Zu,Kwak, Jin Hwan
, p. 3584 - 3593 (2007/10/03)
New pyrrolidine derivatives, which bear an alkyloxime substituent in the 4-position and an aminomethyl substituent in the 3-position of the pyrrolidine ring, have been synthesized and coupled with various quinolinecarboxylic acids to produce a series of new fluoroquinolone antibacterials. These fluoroquinolones were found to possess potent antimicrobial activity against both Gram-negative and Gram-positive organisms, including methicillin resistant Staphylococcus aureus (MRSA). Variations at the C-8 position of the quinolone nucleus included fluorine, chlorine, nitrogen, methoxy, and hydrogen atom substitution. The activity imparted to the substituted quinolone nucleus by the C-8 substituent was in the order F (C5-NH2) > F (C5-H) > naphthyridine > Cl = OMe = H against Gram-positive organisms. In the case of Gram-negative strains, activity was in the order F (C5-NH2) > naphthyridine = F (C5-H) > H > Cl > OMe. The advantages provided by the newly introduced oxime group of the quinolones were clearly demonstrated by their comparison to a desoximino compound 30. In addition, the oxime moiety greatly improved the pharmacokinetic parameters of the novel quinolones. Among these compounds, compound 20 (LB20304) showed the best in vive efficacy and pharmacokinetic profile in animals, as well as good physical properties. The MICs (μg/mL) of LB20304, compound 30, and ciprofloxacin against several test organisms are as follows: S. aureus 6538p (0.008, 0.031, and 0.13), methicillin resistant S. aureus 241 (4, 16, and 128), Streptococcus epidermidis 887E (0.008, 0.016, and 0.13), methicillin resistant S. epidermidis 178 (4, 32, and 128), Enterococcus faecalis 29212 (0.063, 0.13, and 1), Pseudomonas aeruginosa 1912E (0.25, 0.5, and 0.13), Escherichia coli 3190Y (0.008, 0.016, and 0.008), Enterobacter cloacae P99 (0.008, 0.031, and 0.008), Actinobacter calcoaceticus 15473 (0.063, 0.13, and 0.25). On the basis of these promising results, LB20304 was selected as a candidate for further evaluation.