- 3-substituent-5-(substituted aryl)-7-azaindole derivative and application thereof
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The invention discloses a 3-substituent-5-(substituted aryl)-7-azaindole derivative and application thereof. The structural formula of the 3-substituent-5-(substituted aryl)-7-azaindole derivative is shown in the specification, and the 3-substituent-5-(substituted aryl)-7-azaindole derivative has obvious anti-coronavirus activity. In-vitro binding experiments show that the 3-substituent-5-(substituted aryl)-7-azaindole derivative disclosed by the invention generally has relatively strong affinity with a drug target 3CLPro protease of coronavirus, can effectively inhibit the activity of the 3CLPro protease, and is a small molecular ligand for targeted inhibition of 3CLPro.
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- HETEROCYCLIC COMPOUND, PHARMACEUTICAL COMPOSITION COMPRISING SAME, PREPARATION METHOD THEREFOR, AND USE THEREOF
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The present invention relates to a heterocyclic compound, a pharmaceutical composition comprising same, a preparation method therefor, and a use thereof. Specifically, the compound of the present invention is represented by formula (I), and used for preventing or treating a disease or condition related to RET activity.
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Paragraph 0237-0238
(2022/01/01)
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- 1,5,7-TRISUBSTITUTED ISOQUINOLINE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF IN MEDICINES
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The present disclosure relates to 1,5,7-trisubstituted isoquinoline derivatives, their preparation and pharmaceutical use. In particular, the present disclosure discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof. The definitions of the groups in the formula can be found in the specification and claims.
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Paragraph 0230; 0232; 0234
(2020/08/30)
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- Substituted pyridine compound and its method and use thereof
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The invention relates to a novel substitutive pyridine compound, and a pharmaceutically acceptable salt and a pharmaceutical preparation of the substitutive pyridine compound for regulating the activity of protein kinases and regulating signal responses between cells or in the cells. Meanwhile, the invention further relates to a pharmaceutical composition containing the compound provided by the invention, and a method for treating high proliferative diseases of mammals, especially human with the pharmaceutical composition.
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- PYRROLO[3,2-C]PYRIDINE DERIVATIVES AS TLR INHIBITORS
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The present invention provides a heterocyclic compound having a TLR7, TLR9, TLR7/8, TLR7/9 or TLR7/8/9 inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases, inflammatory diseases and the like, in particular, systemic lupus erythematosus, Sjogren's syndrome, rheumatoid arthritis, psoriasis, inflammatory bowel disease and the like. The present invention is a compound represented by the formula (1): wherein each symbol is as described in the specification, or a salt thereof.
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Paragraph 0656; 0658
(2017/01/31)
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- HETEROCYCLIC COMPOUNDS
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The present invention provides a heterocyclic compound a TLR7 and/or TLR9 and/or TLR-7/8/9 and/or TLR-7/8 and/or TLR-7/9 inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases and/or inflammatory diseases and the like, in particular, acute decompensated heart failure, non-alcoholic steatohepatitis (NASH), IgA nephropathy, Duchenne muscular dystrophy (DMD), systemic lupus erythematosus, Sjogren's syndrome, rheumatoid arthritis, psoriasis, inflammatory bowel disease, asthma, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, B-cell malignancies, transplant rejection and graft-versus-host disease, hepatocellular carcinoma (HCC) and the like. The present invention is a compound represented by the formula (1) : wherein each symbol is as described in the specification, or a salt thereof.
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Paragraph 0308; 0309; 0311
(2017/03/21)
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- PYRROLO[3,2-C]PYRIDINE DERIVATIVES AS TLR INHIBITORS
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The present invention provides a heterocyclic compound having a TLR7, TLR9, TLR7/8, TLR7/9 or TLR7/8/9 inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases, inflammatory diseases and the like, in particular, systemic lupus erythematosus, Sjogren's syndrome, rheumatoid arthritis, psoriasis, inflammatory bowel disease and the like. The present invention is a compound represented by the formula (1): wherein each symbol is as described in the specification, or a salt thereof.
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Paragraph 0239
(2016/12/16)
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- PDE 10a Inhibitors for the Treatment of Type II Diabetes
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Disclosed are compounds, compositions and methods for treating Type II diabetes. Such compounds are represented by Formula (I) as follows: wherein R1, R2, L, and Q are defined herein.
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- 3-(PYRAZOLYL)-1H-PYRROLO[2,3-b]PYRIDINE DERIVATIVES AS KINASE INHIBITORS
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The present application relates to novel 3-(pyrazolyl)-lH-pyrrolo[2,3-b]pyridine derivatives of formula (I), as protein kinase inhibitors. The invention particularly relates to compounds of formula (I), preparation of compounds and pharmaceutical compositions thereof. The invention further relates to pharmaceutically acceptable salts and compositions comprising the said novel 3-(pyrazolyl)-lH-pyrrolo[2,3-b]pyridine derivatives and their use in the treatment of various disorders.
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Page/Page column 25; 40
(2014/01/18)
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- Pyridine Derivative and Medicinal Agent
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A main object of the present invention is to provide a novel pyridine derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof. In formula [1], R represents an aryl group or a heteroaryl group, which may be
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Paragraph 0531; 0632
(2013/09/12)
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- Use of small-molecule crystal structures to address solubility in a novel series of g protein coupled receptor 119 agonists: Optimization of a lead and in vivo evaluation
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G protein coupled receptor 119 (GPR119) is viewed as an attractive target for the treatment of type 2 diabetes and other elements of the metabolic syndrome. During a program toward discovering agonists of GPR119, we herein describe optimization of an initial lead compound, 2, into a development candidate, 42. A key challenge in this program of work was the insolubility of the lead compound. Small-molecule crystallography was utilized to understand the intermolecular interactions in the solid state and resulted in a switch from an aryl sulphone to a 3-cyanopyridyl motif. The compound was shown to be effective in wild-type but not knockout animals, confirming that the biological effects were due to GPR119 agonism.
- Scott, James S.,Birch, Alan M.,Brocklehurst, Katy J.,Broo, Anders,Brown, Hayley S.,Butlin, Roger J.,Clarke, David S.,Davidsson, ?jvind,Ertan, Anne,Goldberg, Kristin,Groombridge, Sam D.,Hudson, Julian A.,Laber, David,Leach, Andrew G.,MacFaul, Philip A.,McKerrecher, Darren,Pickup, Adrian,Schofield, Paul,Svensson, Per H.,S?rme, Pernilla,Teague, Joanne
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supporting information; experimental part
p. 5361 - 5379
(2012/08/28)
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