851883-08-4Relevant academic research and scientific papers
Immunomodulator
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Paragraph 0240-0241; 0245-0247, (2021/02/10)
The invention discloses an immunomodulator, and particularly relates to compounds for inhibiting IL-17A and application of the compounds serving as the immunomodulator in preparation of drugs. The invention discloses an application of a compound shown as a formula I or a stereoisomer thereof in preparing medicines for inhibiting IL-17A, and provides a new choice for clinically screening and/or preparing medicines for treating diseases related to IL-17A activity.
Immunomodulator
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Paragraph 0180-0181; 0191-0193, (2021/02/10)
The invention discloses an immunomodulator, and particularly relates to compounds for inhibiting IL17A and application of the compounds serving as the immunomodulator in preparation of drugs. The invention discloses an application of a compound shown as a formula I or a stereoisomer thereof in preparing medicines for inhibiting IL-17A, and provides a new choice for clinically screening and/or preparing medicines for treating diseases related to IL-17A activity.
Discovery of BAY-985, a Highly Selective TBK1/IKK? Inhibitor
Lefranc, Julien,Schulze, Volker Klaus,Hillig, Roman Christian,Briem, Hans,Prinz, Florian,Mengel, Anne,Heinrich, Tobias,Balint, Jozsef,Rengachari, Srinivasan,Irlbacher, Horst,St?ckigt, Detlef,B?mer, Ulf,Bader, Benjamin,Gradl, Stefan Nikolaus,Nising, Carl Friedrich,Von Nussbaum, Franz,Mumberg, Dominik,Panne, Daniel,Wengner, Antje Margret
supporting information, p. 601 - 612 (2020/02/04)
The serine/threonine kinase TBK1 (TANK-binding kinase 1) and its homologue IKK? are noncanonical members of the inhibitor of the nuclear factor κB (IκB) kinase family. These kinases play important roles in multiple cellular pathways and, in particular, in inflammation. Herein, we describe our investigations on a family of benzimidazoles and the identification of the potent and highly selective TBK1/IKK? inhibitor BAY-985. BAY-985 inhibits the cellular phosphorylation of interferon regulatory factor 3 and displays antiproliferative efficacy in the melanoma cell line SK-MEL-2 but showed only weak antitumor activity in the SK-MEL-2 human melanoma xenograft model.
An organic electroluminescent compounds (by machine translation)
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Paragraph 0059; 0060; 0061, (2018/03/24)
The present invention discloses an organic electroluminescent compounds, such as the formula (I) with or (II) the structure of the shown: Wherein A and Z is independently N or CH; R1 And R2 Are each independently selected from: H, alkyl, cycloalkyl, alkoxy, aromatic, heterocyclic aromatic; R3 - R6 Are each independently selected from: H, cyano, alkyl, cycloalkyl, alkoxy, aromatic, heterocyclic aromatic; R7 And R8 And they are connected together constitute N carbazolyl or C1 - C8 alkyl substituted carbazole-based. The design of the invention a series of boron organic molecule can be used as a light-emitting material used for making the OLED device, which exhibit relatively low driving voltage, high luminous efficiency, high color purity and long service life, has applied to the prospects of AMOLED. (by machine translation)
HETEROARYLBENZIMIDAZOLE COMPOUNDS
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Page/Page column 318, (2017/07/06)
The present invention covers heteroarylbenzimidazole compounds of general formula (I) in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative and/or inflammatory disorders, as a sole agent or in combination with other active ingredients.
IMIDAZOPYRAZINES AND PYRAZOLOPYRIMIDINES AND THEIR USE AS AMPA RECEPTOR MODULATORS
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Page/Page column 97, (2016/12/26)
Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, N-oxides, or solvates thereof, [Formula should be inserted here] Also provided herein are pharmaceutical compositions, comprising compounds of Formula (I), and methods of
METALLO-BETA-LACTAMASE INHIBITORS
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Paragraph 1200, (2016/12/01)
The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
METALLO-BETA-LACTAMASE INHIBITORS
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Page/Page column 65, (2017/04/04)
The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
PHOSPHOINOSITIDE 3-KINASE INHIBITORS WITH ZINC BINDING MOIETY
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Paragraph 0296; 0472, (2016/10/07)
PROBLEM TO BE SOLVED: To provide phosphoinositide 3-kinase inhibitors with a zinc binding moiety. SOLUTION: There is provided a compound represented by formula (I) in the figure. (X is S, O or the like; Y is CH, N or the like; G1 is optionally substituted N or the like; R1 and R2 are each independently H or the like; C is a substituted heterocycle or the like; B is a linear alkyl or the like; Ra and Rb together with the nitrogen atom coupled to them are morpholino or the like; G2 is an indazole ring or the like; q, r and s are independently from 0 to 1, provided that at least one of them is 1; t is from 0 to 1; n is from 0 to 4; and p is from 0 to 2.) COPYRIGHT: (C)2016,JPOandINPIT
NOVEL 3-INDOL SUBSTITUTED DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE
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Page/Page column 102; 103, (2016/01/12)
The present invention relates to compound of Formula (I) or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or HIV, depression, and obesity. The invention also relates to a process for manufacturing compounds of Formula (I).
