866638-72-4Relevant academic research and scientific papers
Discovery of a novel indole pharmacophore for the irreversible inhibition of myeloperoxidase (MPO)
Axford, Laura,Cohick, Evan,Dales, Natalie,Deng, Lin,Hamann, Lawrence G.,Harrison, Tyler J.,Hollis-Symynkywicz, Micah,Kecman, Sam,Lee, Lac,Loi, Sally,Marcinkeviciene, Jovita,Marro, Martin L.,Papillon, Julien P. N.,Patnaik, Anup,Patterson, Andrew W.,Regard, Jean B.,Ren, Xianglin
, (2020)
Myeloperoxidase (MPO) activity and subsequent generation of hypochlorous acid has been associated with the killing of host-invading microorganisms (e.g. bacteria, viruses, and fungi). However, during oxidative stress, high MPO activity can damage host tissue and is linked to several chronic inflammatory conditions. Herein, we describe the development of a novel biaryl, indole-pyrazole series of irreversible mechanism-based inhibitors of MPO. Derived from an indole-containing high-throughput screen hit, optimization efforts resulted in potent and selective 6-substituted indoles with good oral bioavailability and in vivo activity.
ANTIBACTERIAL 8-PHENYLAMINO-3-(PYRAZOL-4-YL)IMIDAZO[1,2-A]PYRAZINE DERIVATIVES
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Page/Page column 304-305, (2021/11/06)
The invention provides novel imidazopyrazine derivatives having the general formula (I), wherein X and R3 to R9 are as described herein or pharmaceutically acceptable salts thereof, wherein X and R3 to R9 are as defined herein. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.
NOVEL IMIDAZOPYRAZINE DERIVATIVES
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Page/Page column 51; 197-198, (2021/12/31)
The invention provides novel imidazopyrazine derivatives having the general formula (I), wherein Rx and R3 to R5 are as described herein (formula (I)) or pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.
ALK5 INHIBITORS
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Paragraph 0479; 0672; 0673, (2020/07/07)
The present disclosure provides inhibitors of activin receptor-like kinase 5 (ALK5). Also disclosed are methods to modulate the activity of ALK5 and methods of treatment of disorders mediated by ALK5.
THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Paragraph 1301, (2015/02/18)
Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.
THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Page/Page column 284; 285, (2015/02/02)
Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.
Simple preparations of 4 and 5-iodinated pyrazoles as useful building blocks
Guillou, Sandrine,Bonhomme, Frédéric J.,Ermolenko, Mikhail S.,Janin, Yves L.
experimental part, p. 8451 - 8457 (2011/11/13)
The pyrazole nucleus has recently become a recurrent scaffold in the research fields of CropScience and oncology. We report here the preparation of an array of 4- and 5-iodinated pyrazole derivatives, such as 4-iodo-3-trifluoromethylpyrazole or ethyl 5-io
N1 - ((PYRAZOL-1-YMETHYL) -2-METHYLPHENYL)- PHATALAMIDE DERIVATIVES AND RELATED COMPOUNDS INSECTICIDES
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Page/Page column 73, (2008/06/13)
Novel benzenedicarboxamides of the formula (I) wherein X represents hydrogen, halogen atom, nitro, C1-6alkylsulfonyloxy,C1-6alkylsulfinyl, C1-6alkylsulfenyl or C1-6alkylsulfonyl, R1 represents C1-6alkyl, C1-6alkylthio-C1-6alkyl, C1-6alkylsulfinyl- C1-6alkyl or C1-6 alkylsulfonyl- C1-6alkyl, Y represents halogen or C1-6alkyl, m represents 0 or 1, A represents O, S, SO, SO2, CH2 or CH(CH3), and Q represents a 5- or 6-membered heterocyclic group that contains at least one hetero atom selected from the group consisting of N, O and S and can be optionally substituted; processes for their preparation, their intermediates and their use as insecticides.
