346691-23-4Relevant academic research and scientific papers
PIPERIDINE-2, 6-DIONE DERIVATIVES WHICH BIND TO CEREBLON, AND METHODS OF USE THEREOF
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Page/Page column 94-95, (2021/06/04)
The present invention provides novel compounds which bind to cereblon, and methods of use thereof. The compounds are represented by Formulas (I) and (II), below: (I) wherein Rx is selected from (Ia), (Ib), (Ic) and (Id); (II) wherein Ry is selected from (IIa), (IIb), (IIc) and (IId).
Benzimidazole-2-piperazine compound, its pharmaceutical composition and its preparation and use
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Paragraph 0385; 0388; 0389, (2016/10/20)
The invention relates to a benzimidazole-2-piperazine derivative and a preparing method and application of the benzimidazole-2-piperazine derivative in medicine, in particular to a novel benzimidazole-2-piperazine derivative shown in the general formula (I), a preparing method of the derivative, a pharmaceutical composition containing the derivative and application of the derivative serving as a therapeutic agent, especially serving as a poly (ADP-ribose) polymerase (PARP) inhibitor. In the general formula (I), R refers to hydrogen or halogen, G refers to carbonyl or methylene, m is 1-2, n is 1-3, and Q refers to hydrogen or C1-C4 alkyl. When X is methylene and Y is NR1 or methylene, X is NR1; R1 refers to hydrogen, C1-C6 alkyl, benzyl, COR2 or SO2R2; R2 refers to the following groups which are not substituted or groups substituted by 1-3 substituent groups, including C1-C6 alkyl, C3-C8 naphthenic base, phenyl, benzyl, naphthyl and C5-C10 aromatic heterocycle base, heterocycle in the C5-C10 aromatic heterocycle base comprises 1-3 heteroatoms selected from N, O and S, and the substituent groups are selected from the following atoms or groups of C1-C6 alkyl, C1-C6 alkoxy, halogen, amidogen, nitryl, sulfydryl, hydroxyl, cyanogroup and trifluoromethyl. The general formula (I) is shown in the specification.
2,5-diazabicyclo [2.2.1] iieptanes and method of preparation, pharmaceutical compositions thereof and its application in medicine
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Paragraph 0214; 0216; 0219; 01220, (2016/11/28)
The present invention relates to a class of 2,5-diazabicyclo[2.2.1]heptane derivatives and a preparation thereof, pharmaceutical compositions of the 2,5-diazabicyclo[2.2.1]heptane derivatives, and medical uses of the 2,5-diazabicyclo[2.2.1]heptane derivat
A novel series of benzimidazole NR2B-selective NMDA receptor antagonists
Davies, David J.,Crowe, Matthew,Lucas, Nolwenn,Quinn, Joanna,Miller, David D.,Pritchard, Sara,Grose, David,Bettini, Ezio,Calcinaghi, Novella,Virginio, Caterina,Abberley, Lee,Goldsmith, Paul,Michel, Anton D.,Chessell, Iain P.,Kew, James N.C.,Miller, Neil D.,Gunthorpe, Martin J.
scheme or table, p. 2620 - 2623 (2012/05/05)
A series of novel benzimidazoles are discussed as NR2B-selective N-methyl-d-aspartate (NMDA) receptor antagonists. High throughput screening (HTS) efforts identified a number of potent and selective NR2B antagonists such as 1. Exploration of the substituents around the core of this template identified a number of compounds with high potency for NR2B (pIC50 >7) and good selectivity against the NR2A subunit (pIC50 2+ and radioligand binding studies. These agents offer potential for the development of therapeutics for a range of nervous system disorders including chronic pain, neurodegeneration, migraine and major depression.
Prolyl Hydroxylase Inhibitors
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Page/Page column 12, (2010/12/29)
The invention described herein relates to certain quinoxaline-5-carboxamide derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.
PROLYL HYDROXYLASE INHIBITORS
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Page/Page column 16, (2009/12/05)
The invention described herein relates to certain benzimidazol-4-ylcarboxamide derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one
