- 7-azaindole heterocyclic compound and preparation method and application thereof
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The invention belongs to the technical field of 7-azaindole heterocyclic compounds, and discloses a 7-azaindole heterocyclic compound and a preparation method and application thereof. The structure of the compound is shown as a general formula I, a general formula II, a general formula III or a general formula IV (detailed description). The compound can simultaneously have a good effect of inhibiting central nervous excitation on cell and mouse excitation models, and the compound has relatively low neurotoxicity.
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Paragraph 0031-0033; 0042; 0045-0046
(2021/10/05)
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- Discovery and characterization of novel indole and 7-azaindole derivatives as inhibitors of β-amyloid-42 aggregation for the treatment of Alzheimer's disease
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The aggregation of amyloid-β peptides into cytotoxic oligomeric and fibrillary aggregates is believed to be one of the major pathological events in Alzheimer disease. Here we report the design and synthesis of a novel series of indole and 7-azaindole derivatives containing, nitrile, piperidine and N-methyl-piperidine substituents at the 3-position to prevent the pathological self-assembly of amyloid-β. We have further demonstrated that substitution of the azaindole and indole derivatives at the 3 positions is required to obtain compounds with improved physicochemical properties to allow brain penetration.
- Sreenivasachary, Nampally,Kroth, Heiko,Benderitter, Pascal,Hamel, Anne,Varisco, Yvan,Hickman, David T.,Froestl, Wolfgang,Pfeifer, Andrea,Muhs, Andreas
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supporting information
p. 1405 - 1411
(2017/03/08)
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- Novel Compounds for the Treatment of Diseases Associated with Amyloid or Amyloid-Like Proteins
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The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.
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Page/Page column 46
(2011/11/30)
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- AZAINDOLE DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONISTIC ACTIVITY
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The present invention creates an azaindole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further providing a therapeutic agent for treating allergic diseases.
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Page/Page column 37-39
(2008/06/13)
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- Pyrazole-based cathepsin S inhibitors with improved cellular potency
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High potency pyrazole-based noncovalent inhibitors of human cathepsin S (CatS) were developed by modification of the benzo-fused 5-membered ring heterocycles found in earlier series of CatS inhibitors. Although substitutions on this heterocyclic framework
- Wei, Jianmei,Pio, Barbara A.,Cai, Hui,Meduna, Steven P.,Sun, Siquan,Gu, Yin,Jiang, Wen,Thurmond, Robin L.,Karlsson, Lars,Edwards, James P.
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p. 5525 - 5528
(2008/03/11)
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- 3-PIPERIDIN-4-YL-INDOLE ORL-1 RECEPTOR MODULATORS
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The present invention is directed to novel 3-piperidin-4-yl-indole derivatives of formula (I) and forms thereof, wherein X, R1, R2, R3, R4 and R5 are as herein defined, pharmaceutical compositions thereof and use as ORL-1 receptor modulators for treating, preventing or ameliorating ORL-1 receptor mediated disorders and conditions.
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Page/Page column 54
(2008/06/13)
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- AZAINDOLYLPIPERIDINE DERIVATIVES AS ANTIHISTAMINIC AND ANTIALLERGIC AGENTS
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This invention is directed to new potent and selective antagonists of H1 histamine receptors having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.
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Page/Page column 44
(2008/06/13)
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