- KETONE INHIBITORS OF LYSINE GINGIPAIN
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The present invention provides compounds according to Formula (I) as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.
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Paragraph 0407
(2018/04/12)
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- NOVEL OXAZOLIDINONE DERIVATIVE AND MEDICAL COMPOSITION CONTAINING SAME
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Disclosed is a novel oxazolidinone derivative represented by Formula 1 above, in particular, a novel oxazolidinone compound having a cyclic amidoxime or cyclic amidrazone group. In Formula 1, R and Q are the same as defined in the detailed description. In addition, disclosed is a pharmaceutical composition for an antibiotic which includes the novel oxazolidinone derivative of Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an active ingredient. The novel oxazolidinone derivative, the prodrug thereof, the hydrate thereof, the solvate thereof, the isomer thereof, and the pharmaceutically acceptable salt thereof have broad antibacterial spectrum against resistant bacteria, low toxicity and strong antibacterial effects against Gram-positive and Gram-negative bacteria and thus may be effectively used as antibiotics.
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Paragraph 0175-0177
(2014/07/08)
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- NOVEL OXAZOLIDINONE DERIVATIVE AND MEDICAL COMPOSITION CONTAINING SAME
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Disclosed is a novel oxazolidinone derivative represented by Formula 1 above, in particular, a novel oxazolidinone compound having a cyclic amidoxime or cyclic amidrazone group. In Formula 1, R and Q are the same as defined in the detailed description. In addition, disclosed is a pharmaceutical composition for an antibiotic which includes the novel oxazolidinone derivative of Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an active ingredient. The novel oxazolidinone derivative, the prodrug thereof, the hydrate thereof, the solvate thereof, the isomer thereof, and the pharmaceutically acceptable salt thereof have broad antibacterial spectrum against resistant bacteria, low toxicity and strong antibacterial effects against Gram-positive and Gram-negative bacteria and thus may be effectively used as antibiotics.
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Paragraph 0164-0167
(2014/02/16)
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- Development of a safe, scalable process for the preparation of an oxaisoxazolidinone
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This report describes the development and scale up of the synthesis of oxaisoxazolidinone 1, a significant synthon in the synthesis of the MRSA development compound AZD5847. Studies were carried out to ensure a short-term, risk based preparation of 9 on a 5 L scale with a solid isolation procedure and a safe, long-term manufacturing process for both 1 and 9 through extensive hazards evaluation.
- Santhosh,Kshirsagar, Yogesh M.,Venkatesan,Hazra, Debasis,Kindel, Jnaneshwara,Sridharan,Ennis, David,Howells, Garnet E.,Stefinovic, Marijan,Manjunatha, Sulur G.,Nambiar, Sudhir
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p. 1802 - 1806
(2015/02/19)
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- Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent
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A series of novel substituted pyridyl phenyl oxazolidinone analogues were synthesized and their structure-activity relationship (SAR) was investigated based on in vitro and in vivo antibacterial activities. The minimum inhibitory concentrations (MICs) of the synthesized compounds against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE) ranged from 0.12 to 2.0 μg/mL, and against Haemophilus influenzae (Hi) from 2.0 to 8.0 μg/mL. Compared to linezolid, only four compounds (11, 12, 21 and 29) showed higher in vitro antibacterial activities and better in vivo protective effects in mice. To improve the aqueous solubility, various prodrugs of compound 11 (DA-7157), which exerted a potency that was enhanced by 2-8-fold compared to that of linezolid, were synthesized. Among the prodrugs, the phosphate compound 42 exhibited excellent aqueous solubility (>50 mg/mL in DW) and good pharmacokinetic profiles, along with better in vivo efficacy than linezolid. This compound 42 is currently undergoing clinical trials with the brand name Torezolid.
- Im, Weon Bin,Choi, Sun Ho,Park, Ju-Young,Choi, Sung Hak,Finn, John,Yoon, Sung-Hwa
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experimental part
p. 1027 - 1039
(2011/04/17)
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- NOVEL ANTIBACTERIAL COMPOUNDS
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The invention relates to novel chimeric antibiotics of formula (I) Wherein R1 is CH2NHCOR5, heteroarylmethyl, heteroaryloxymethyl or heteroarylaminomethyl; R2 is H, OH, OSO3H, OPO3H2, OCH2OPO3H2, OCOCH2CH2COOH, OCOR6; R3 is H or halogen; R4 is (C1-C3)alkyl, (C1-C3)haloalkyl or cycloalkyl; R5 is alkyl or haloalkyl; and R6 is the residue of a naturally occurring amino acid or of dimethylaminoglycine. These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).
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Page/Page column 82
(2010/11/25)
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- Imidazolo-5-YL-2anilino-pyrimidines as agents for the inhibition of the cell proliffration
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Compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, p, q, and n are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man.
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Page/Page column 37
(2010/02/05)
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- NOVEL FLORFENICOL-TYPE ANTIBIOTICS
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The present invention relates to novel florfenicol compounds having the chemical structure: wherein the compounds are useful for the treatment and/or prevention of bacterial infections in a broad range of patients such as, without limitation, birds, fish, shellfish and mammals
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- Antimicrobial thiadiazinone derivatives and their application for treatment of bacterial infections
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The present invention provides certain thiadiazinone derivatives of oxazolidinones of the following formula I: or pharmaceutically acceptable salts thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use,
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- Isoxazolone compounds useful in treating diseases associated with unwanted cytokine activity
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Isoxazolone compounds having the generic structure: are used to treat disease associated with unwanted cytokine activity, including rheumatoid arthritis, osteoarthritis, diabetes, HIV/AIDS, inflammatory bowel disease, Crohn's disease, ulcerative colitis,
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- DERIVATIVES OF 4- (IMIDAZOL-5-YL)-2-(4-SULFOANILINO) PYRIMIDINE WITH CDK INHIBITORY ACTIVITY
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Compounds of the formula (I): wherein R1, R2, R3, R4, R5 and p are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man.
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Page/Page column 69
(2008/06/13)
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- Compounds having GABA like activity, and use of same in tissue irrigating solutions
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Compounds which enhance the efficiency of the corneal endothelial fluid pump thereby promoting normal corneal function and deturgescence of swollen corneas, and methods for the compounds' synthesis are described. In addition, surgical irrigating solutions
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- Action de l'hydroxyuree sur les esters α-acetyleniques
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Hydroxyurea, in its oxanion form NH2-CO-NHO(1-), reacts in basic medium by a 1,4-addition to α-acetylenic esters leading to the E and Z ethylenic β-ureidoxy esters isomers.The E isomer can be isolated and identified from reaction with ethyl tetrolate and ethyl propiolate.The Z isomer undergoes cyclisation in situ to give the 2-carboxamido-5-methyl-3-isoxazolone.With phenyl propiolate, the 3-hydroxy-5-phenyl isoxazole is directly obtained without isolation of the intermediate N-carboxamido derivative.In the case of ethyl propiolate two cyclic compounds are obtained: 3-hydroxyisoxazole and 2-N-carboxamido-5-ethoxy-3-isoxazolidinone.The formation of the former is due to the in situ cyclisation of the Z isomer.The isolation of the latter compound can be explained by solvent addition to the E β-ureidoxyacrylate intermadiate in a Michael addition followed by cyclisation.
- Lassalvy, Christiane,Petrus, Clement,Petrus, Francoise
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p. 175 - 180
(2007/10/02)
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