141699-59-4Relevant articles and documents
SUBSTITUTED AMINOQUINOLONES AS DGKALPHA INHIBITORS FOR IMMUNE ACTIVATION
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Page/Page column 129-130, (2021/06/04)
The present invention covers aminoquinolone compounds of general formula (I) : in which R1, R2, R3, R4, R5, R6, R7, R8, X and n are as defined herein, methods of prepa
Lead Optimization of 3,5-Disubstituted-7-Azaindoles for the Treatment of Human African Trypanosomiasis
Klug, Dana M.,Mavrogiannaki, Eftychia M.,Forbes, Katherine C.,Silva, Lisseth,Diaz-Gonzalez, Rosario,Pérez-Moreno, Guiomar,Ceballos-Pérez, Gloria,Garcia-Hernández, Raquel,Bosch-Navarrete, Cristina,Cordón-Obras, Carlos,Gómez-Li?án, Claudia,Saura, Andreu,Momper, Jeremiah D.,Martinez-Martinez, Maria Santos,Manzano, Pilar,Syed, Ali,El-Sakkary, Nelly,Caffrey, Conor R.,Gamarro, Francisco,Ruiz-Perez, Luis Miguel,Gonzalez Pacanowska, Dolores,Ferrins, Lori,Navarro, Miguel,Pollastri, Michael P.
supporting information, p. 9404 - 9430 (2021/07/25)
Neglected tropical diseases such as human African trypanosomiasis (HAT) are prevalent primarily in tropical climates and among populations living in poverty. Historically, the lack of economic incentive to develop new treatments for these diseases has meant that existing therapeutics have serious shortcomings in terms of safety, efficacy, and administration, and better therapeutics are needed. We now report a series of 3,5-disubstituted-7-azaindoles identified as growth inhibitors of Trypanosoma brucei, the parasite that causes HAT, through a high-throughput screen. We describe the hit-to-lead optimization of this series and the development and preclinical investigation of 29d, a potent antitrypanosomal compound with promising pharmacokinetic (PK) parameters. This compound was ultimately not progressed beyond in vivo PK studies due to its inability to penetrate the blood-brain barrier (BBB), critical for stage 2 HAT treatments.
Synthesis and Characterization of N-(4-(Piperidin-4-ylsulfonyl) phenyl)5-vinylpyrimidin-2-amine
Dong, Jingjing,Feng, Baicheng,Jin, Yan,Lu, Jianqiang,Wang, Tielin
, p. 255 - 258 (2021/08/05)
Target product N-(4-(piperidin-4-ylsulfonyl)phenyl)5-vinylpyrimidin-2- amine (13) was synthesized using 6-oxopyran-3-carbaldehyde (M1) and 4-hydroxypiperidine (M2) as starting materials by a series of nucleophilic substitution and oxidation. Different aci
CXCR2 ANTAGONIST
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Paragraph 0097-0099; 0122-0124, (2020/11/23)
A compound as a CXCR2 antagonist and an application thereof in preparing a drug as a CXCR2 antagonist. In particular, the present invention relates to a compound represented by formula (II) or an isomer or pharmaceutically acceptable salt thereof.
Copper-Catalyzed Cross-Coupling between Alkyl (Pseudo)halides and Bicyclopentyl Grignard Reagents
Andersen, Claire,Bernardelli, Patrick,Cossy, Janine,Daumas, Marc,Ferey, Vincent,Guérinot, Amandine
, (2020/08/05)
The development of a copper-catalyzed cross-coupling between primary and secondary (pseudo)halides and bicyclopentyl Grignard reagents is reported. Highly strained bicyclopentanes can be cross-coupled with a large panel of primary alkyl mesylates and secondary alkyl iodides. The catalytic system is simple and cheap, and the reaction is general and chemoselective.
PYRROLO(PYRAZOLO)PYRIMIDINE DERIVATIVE AS LRRK2 INHIBITOR
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Paragraph 0119-0120, (2020/11/23)
The present invention relates to a pyrrolo(pyrazolo)pyrimidine derivative having efficacy as an LRRK2 inhibitor, a preparation method therefor, and a pharmaceutical composition for preventing or treating degenerative brain diseases, containing the same.
1, 2, 4-OXADIAZOLE DERIVATIVES AND USES THEREOF
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Paragraph 0094, (2020/04/25)
The disclosure provides 1, 2, 4-oxadiazole derivatives useful for stemming bleeding and for treating cancer.
1, 3, 4-OXADIAZOLE DERIVATIVES AND USES THEREOF
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Paragraph 0082, (2020/04/25)
The disclosure provides 1, 3, 4-oxadiazole derivatives useful for stemming bleeding and for treating cancer.
IRAK DEGRADERS AND USES THEREOF
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Paragraph 00962; 002942-002944, (2020/06/19)
The present invention provides compounds, compositions thereof, and methods of using the same.
Pyrrolo[2, 3-d] pyrimidine derivatives containing piperidine as well as preparation and application thereof
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Paragraph 0121; 0124; 0125, (2020/09/16)
The invention relates to a piperidine-containing pyrrolo[2, 3-d] pyrimidine derivative as shown in a general formula I or a general formula II as well as a use method and a preparation method thereof.The invention also relates to a strong JAK kinase inhibition effect of the compound shown in the general formula I or II, the invention also relates to an application of the compound in preparation of medicines for treating and/or preventing diseases caused by abnormal expression of JAK, and particularly relates to application of the compound in preparation of medicines for treating inflammatory/autoimmune diseases, fibrosis and cancers.