- AZETIDINE AND SPIROAZETIDINE COMPOUNDS AND USES THEREOF
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The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
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Page/Page column 45; 46; 49-51; 57-58
(2021/12/30)
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- COMPOUND HAVING BET INHIBITORY ACTIVITY AND PREPARATION METHOD AND USE THEREFOR
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The invention relates to the field of pharmaceutical chemistry. Specifically, the present invention relates to a series of BET (bromodomain and extra-terminal domain) inhibitors having a novel structure, particularly inhibitors targeting BRD4 (Bromodomain-containing protein 4), and a preparation method and use therefor. The structure thereof is shown in the following general formula (I). Said compounds or a stereoisomer, racemate, geometric isomer, tautomer, prodrug, hydrate, solvate, or crystal form thereof, or a pharmaceutically acceptable salt thereof, and the pharmaceutical compsosition thereof can be used for the treatment and/or prevention of related diseases mediated by bromodomain proteins.
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Paragraph 0249-0251
(2020/12/22)
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- Structural Studies on 4,5-Disubstituted 2-Aminoimidazole-Based Biofilm Modulators that Suppress Bacterial Resistance to β-Lactams
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A library of 4,5-disubstituted 2-aminoimidazole triazole amide (2-AITA) conjugates has been successfully assembled. Upon biological screening, this class of small molecules was discovered as enhanced biofilm regulators through non-microbicidal mechanisms against methicillin-resistant Staphylococcus aureus (MRSA) and multidrug-resistant Acinetobacter baumannii (MDRAB), with active concentrations in the low micromolar range. The library was also subjected to synergism and resensitization studies with β-lactam antibiotics against MRSA. Lead compounds were identified that suppress the antibiotic resistance of MRSA by working synergistically with oxacillin, a β-lactam antibiotic resistant to penicillinase. A further structure-activity relationship (SAR) study on the parent 2-AITA compound delivered a 2-aminoimidazole diamide (2-AIDA) conjugate with significantly increased synergistic activity with oxacillin against MRSA, decreasing the MIC value of the β-lactam antibiotic by 64-fold. Increased anti-biofilm activity did not necessarily lead to increased suppression of antibiotic resistance, which indicates that biofilm inhibition and resensitization are most likely occurring via distinct mechanisms.
- Su, Zhaoming,Yeagley, Andrew A.,Su, Rui,Peng, Lingling,Melander, Christian
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p. 2030 - 2039
(2013/01/15)
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- RENIN INHIBITORS
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The present invention relates to piperidinyl-based renin inhibitor compounds having the formula containing amino-terminal groups, and their use in treating cardiovascular events and renal insufficiency.
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Page/Page column 30
(2009/07/17)
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- Process for the preparation of aryl-piridyl compounds
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A method is described for the preparation of aryl-pyridine compounds of formula (I) by cross-coupling reaction, promoted by catalytic systems based on palladium or nickel between compounds of formula (II) and (III) in which:—Met represents Mg or Zn,—Y represents Cl, Br, I or acetoxy,—Z represents I, Br, Cl, triflate, sulphonate, phosphate,—R1, R2, R3, R4, which are the same as one another or different, represent hydrogen, a linear and/or branched C1-C4 alkyl, and/or an aryl, and/or a heteroaryl, or R1 and R2 and/or R3 and R4, taken together, form a C3-C8 ring, an aryl and/or a heteroaryl,—A represents —COR5 where R5 represents hydrogen, a linear and/or branched C1-C4 alkyl, and/or an aryl, and/or a heteroaryl, or—A represents —CRs5(OR6)(OR7) where R5 has the meaning described above and R6 and R7, which are the same as one another or different, represent a linear and/or branched C1-C4 alkyl, and/or an aryl, and/or a heteroaryl, or R6 and R7, joined together, represent a C1-C8 alkyl or alkenyl.
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Page/Page column 3
(2008/06/13)
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- PROCESS FOR THE PREPARATION OF PYRIDYL-ARYL-SULPHONIC COMPOUNDS
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A method is described for the preparation of pyridyl-aryl-sulphonic compounds of formula (I), by cross-coupling reaction, promoted by catalytic systems based on palladium or nickel between compounds of formulae (II, III), in which; a) Met represents Mg
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Page/Page column 8
(2010/02/06)
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- PROCESS FOR THE PREPARATION OF ARYL-PIRIDYL COMPOUNDS
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A method is described for the preparation of aryl-pyridine compounds of formula (I) by cross-coupling reaction, promoted by catalytic systems based on palladium or nickel between compounds of formula (II) and (III) in which: - Met represents Mg or Zn, - Y represents C1, Br, I or acetoxy, - Z represents I, Br, Cl, triflate, sulphonate, phosphate, - Rl, R2, R3, R4, which are the same as one another or different, represent hydrogen, a linear and/or branched Cl-C4 alkyl, and/or an aryl, and/or a heteroaryl, or Rl and R2 and/or R3and R4, taken together, form a C3-C8 ring, an aryl and/or a heteroaryl, - A represents -COR5 where R5 represents hydrogen, a linear and/or branched Cl-C4 alkyl, and/or an aryl, and/or a heteroaryl, or - A represents -CRs5(OR6)(OR7) where R5 has the meaning described above and R6 and R7, which are the same as one another or different, represent a linear and/or branched C1-C4 alkyl, and/or an aryl, and/or a heteroaryl, or R6 and R7, joined together, represent a C1-C8 alkyl or alkenyl.
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- PREPARATION OF PYRIDYL GRIGNARD REAGENTS AND CROSS COUPLING REACTIONS WITH SULFOXIDES BEARING AZAHETEROCYCLES
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Pyridyl Grignard reagents were prepared from the corresponding iodopyridine and EtMgBr.New cross coupling reactions of the Grignard reagents with azaheterocycles took place on the sulfinyl sulfur atom to afford biazaheteroaryls.
- Furukawa, Naomichi,Shibutani, Tadao,Fujihara, Hisashi
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p. 5845 - 5848
(2007/10/02)
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- Total synthesis of thienamycin analogs - III. Synthesis of 2-aryl and 2-heteroaryl analogs of theinamycin
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The total syntheses of 2-aryl and 2-heteroaryl carbapen-2-em-3-carboxylic acids with and without a 6-hydroxyethyl side chain, using Wittig cyclization for formation of the bicyclic ring system is described. Antibacterial activity of the compounds synthesized is discussed.
- Cama,Wildonger,Guthikonda,et al.
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p. 2531 - 2549
(2007/10/02)
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