51206-40-7Relevant articles and documents
1,4-SUBSTITUTED ISOQUINOLINE INHIBITORS OF KEAP1/NRF2 PROTEIN-PROTEIN INTERACTION
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Paragraph 0073, (2019/10/29)
Disclosed herein are compounds that can act as inhibitors of the Kelch-like ECH- associated protein 1/nuclear factor (erythroid-derived 2)-like 2 ("KEAP1/NRF2") protein- protein interaction, and methods of using the compounds to treat and prevent diseases and disorders, such as COPD, multiple sclerosis, and diabetes, and in the promotion of wound healing. The compounds described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: formula (I), wherein the substituents are as described.
Replacement of a Naphthalene Scaffold in Kelch-like ECH-Associated Protein 1 (KEAP1)/Nuclear Factor (Erythroid-derived 2)-like 2 (NRF2) Inhibitors
Richardson, Benjamin G.,Jain, Atul D.,Potteti, Haranatha R.,Lazzara, Phillip R.,David, Brian P.,Tamatam, Chandra R.,Choma, Ewelina,Skowron, Kornelia,Dye, Katherine,Siddiqui, Zamia,Wang, Yue-Ting,Krunic, Aleksej,Reddy, Sekhar P.,Moore, Terry W.
, p. 8029 - 8047 (2018/09/12)
Activators of nuclear factor-erythroid 2-related factor 2 (NRF2) could lead to promising therapeutics for prevention and treatment of oxidative stress and inflammatory disorders. Ubiquitination and subsequent degradation of the transcription factor NRF2 is mediated by Kelch-like ECH-associated protein-1 (KEAP1). Inhibition of the KEAP1/NRF2 interaction with small molecules leads to NRF2 activation. Previously, we and others described naphthalene-based NRF2 activators, but the 1,4-diaminonaphthalene scaffold may not represent a drug-like scaffold. Paying particular attention to aqueous solubility, metabolic stability, potency, and mutagenicity, we modified a previously known, naphthalene-based nonelectrophilic NRF2 activator to give a series of non-naphthalene and heterocyclic scaffolds. We found that, compared to previously reported naphthalene-based compounds, a 1,4-isoquinoline scaffold provides a better mutagenic profile without sacrificing potency, stability, or solubility.
LIGHT-EMITTING COMPOSITION
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Page/Page column 38, (2017/07/06)
Light-Emitting Compound A composition comprising a light-emitting compound having a peak wavelength of at least 650 nm and a material comprising a group of formula (I): wherein Ar1, Ar2 and Ar3 in each occurrence are indep
A highly practical and convenient halogenation of fused heterocyclic N-oxides
Wang, Dong,Wang, Yuxi,Zhao, Junjie,Li, Linna,Miao, Longfei,Wang, Dong,Sun, Hua,Yu, Peng
, p. 5762 - 5768 (2016/08/30)
A novel, simple and practical method for the regioselective halogenation of fused heterocyclic N-oxides has been developed. It employs Vilsmeier reagent, generated in situ by POX3and DMF, as both the activating agent and the nucleophilic halide source. The method is amenable across a broad range of substrates, including quinolines, isoquinolines and the diazine N-oxides, possessing a variety of substitution patterns. Furthermore, all of the reagents associated are cheap and easy to obtain. The potential extension of this method to a one-pot oxidation/halogenation sequence that obviates the need for isolation of the N-oxide intermediates is also presented.
NOVEL COMPOUNDS AS ANTAGONISTS OR INVERSE AGONISTS FOR OPIOID RECEPTORS
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Page/Page column 97, (2010/09/07)
This invention relates to novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy.
SUBSTITUTED PYRIDINES AND PYRIDAZINES WITH ANGIOGENESIS INHIBITING ACTIVITY
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Page/Page column 32, (2009/03/07)
Substituted pyridines and pyridazines having angiogenesis inhibiting activity and generalized structural formula (I) wherein the ring containing A, B, D, E, and L is phenyl or a nitrogen-containing heterocycle; groups X and Y may be any of a variety of defined linking units; R and R may be defined independent substituents or together may be a ring-defining bridge; ring J may be an aryl, pyridyl, or cycloalkyl group; and G groups may be any of a variety of defined substituents. Pharmaceutical compositions containing these materials, and methods of treating a mammal having a condition characterized by abnormal angiogenesis or hyperpermeability processes using these materials are also disclosed.
COMPOUNDS FOR TREATING PULMONARY HYPERTENSION
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Page/Page column 51, (2008/06/13)
The present invention relates to pharmaceutical compositions and combinations for treating, preventing or managing pulmonary hypertension comprising small molecule heterocyclic pharmaceuticals, and more particularly, substituted pyridines and pyridazines optionally combined with at least one additional therapeutic agent.
Substituted pyridines and pyridazines with angiogenesis inhibiting activity
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Page column 43, (2010/02/05)
Substituted pyridazines having angiogenesis inhibiting activity and the generalized structural formula wherein the ring containing A, B, D, E, and L is phenyl or a nitrogen-containing heterocycle; groups X and Y may be any of a variety of defined linking units; R1and R2may be defined independent substituents or together may be a ring-defining bridge; ring J may be an aryl, pyridyl, or cycloalkyl group; and G groups may be any of a variety of defined substituents. Pharmaceutical compositions containing these materials, and methods of treating a mammal having a condition characterized by abnormal angiogenesis or hyperpermiability processes using these materials are also disclosed.
FUNGAL CELL WALL SYNTHESIS GENE
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, (2008/06/13)
A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed.Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved.
3-substituted-aminomethyl cephalosporin derivatives
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, (2008/06/13)
A cephalosporin derivative of the formula I: STR1 in which X is S, O, CH2 or SO, R1 is (optionally-substituted)imidazol-2-yl or one of the C-7 acyl groups known in the cephalosporin art, R2 is hydrogen or methoxy, R3 is carboxy or a biodegradable ester thereof and --R4 is of the formula XII, XIII or XIV: STR2 in which R32-R40 inclusive are as defined in the specification; and the salts thereof. Pharmaceutical compositions, methods of manufacture and intermediates are also described.