- Nitroimidazole compound as well as preparation method and application thereof
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The invention discloses a novel nitroimidazole compound as well as a preparation method and application thereof. The nitroimidazole compound has a general formula (I) shown in the specification.
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Paragraph 0377-0379; 0384-0385
(2021/02/10)
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- CYCLOPROPYLAMINE COMPOUND AS LSD1 INHIBITOR AND USE THEREOF
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Provided is a cyclopropylamine compound as lysine-specific demethylase 1 (LSD1) inhibitor, and a use thereof in preparation of drug for treating diseases associated with LSD1. The cyclopropylamine compound is a compound represented by formula (I), an isomer thereof, and a pharmaceutically acceptable salt thereof.
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Paragraph 0179-0180; 0183
(2021/07/24)
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- Easy-To-Synthesize Spirocyclic Compounds Possess Remarkable in Vivo Activity against Mycobacterium tuberculosis
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Society urgently needs new, effective medicines for the treatment of tuberculosis. To kick-start the required hit-to-lead campaigns, the libraries of pharmaceutical companies have recently been evaluated for starting points. The GlaxoSmithKline (GSK) library yielded many high-quality hits, and the associated data were placed in the public domain to stimulate engagement by the wider community. One such series, the spiro compounds, are described here. The compounds were explored by a combination of traditional in-house research and open source methods. The series benefits from a particularly simple structure and a short associated synthetic chemistry route. Many members of the series displayed striking potency and low toxicity, and highly promising in vivo activity in a mouse model was confirmed with one of the analogues. Ultimately the series was discontinued due to concerns over safety, but the associated data remain public domain, empowering others to resume the series if the perceived deficiencies can be overcome.
- Guardia, Ana,Baiget, Jessica,Cacho, Mónica,Pérez, Arancha,Ortega-Guerra, Montserrat,Nxumalo, Winston,Khanye, Setshaba D.,Rullas, Joaquín,Ortega, Fátima,Jiménez, Elena,Pérez-Herrán, Esther,Fraile-Gabaldón, María Teresa,Esquivias, Jorge,Fernández, Raquel,Porras-De Francisco, Esther,Encinas, Lourdes,Alonso, Marta,Giordano, Ilaria,Rivero, Cristina,Miguel-Siles, Juan,Osende, Javier G.,Badiola, Katrina A.,Rutledge, Peter J.,Todd, Matthew H.,Remui?án, Modesto,Alemparte, Carlos
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p. 11327 - 11340
(2019/01/08)
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- Synthesis of oxaspiropiperidines as a strategy for lowering logD
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The syntheses of four new spiropiperidines designed as polar analogs of methyl 2-(3-azaspiro[5.5]undec-an-9-yl)acetate are described.
- Cernak, Timothy,Dykstra, Kevin,Levorse, Dorothy,Verras, Andreas,Balkovec, James,Nargund, Ravi,DeVita, Robert
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scheme or table
p. 6457 - 6459
(2011/12/22)
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- Cyclohexane derivatives and their use as therapeutic agents
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The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R17, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
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- N-acylsulfonamide apoptosis promoters
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N-Benzoyl arylsulfonamides having the formula are BCL-Xl inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-Xl inhibiting compositions and methods of promoting apoptosis in a mammal.
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- N-Acylsulfonamide apoptosis promoters
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N-Benzoyl arylsulfonamides having the formula Are BCL-X1 inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-X1 inhibiting compositions and methods of promoting apoptosis in a mammal.
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