- COMPOUNDS AND METHOD FOR TREATING CYTOKINE RELEASE SYNDROME
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Disclosed herein are embodiments of a method for treating or preventing cytokine release syndrome (CRS). In certain embodiments, the method comprises administering a compound, or a salt, solvate, prodrug or pharmaceutical composition thereof, to a subject experiencing, or at risk of developing, CRS. The compound may be a kinase inhibitor, such as a JAK inhibitor and/or an IRAK inhibitor, and/or the compound may have a structure according to Formulas I, III, IV or VII. And the method may comprise administering the compound to a subject who is has received, is currently receiving, and/or will be receiving a cell therapy.
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Page/Page column 110
(2021/02/12)
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- Research on Controllable Degradation of Novel Sulfonylurea Herbicides in Acidic and Alkaline Soils
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The degradation issue of sulfonylurea (SU) has become one of the biggest challenges that hamper the development and application of this class of herbicides, especially in the alkaline soils of northern China. On the basis of the previous discovery that some substituents on the fifth position of the benzene ring in Chlorsulfuron could hasten its degradation rate, apparently in acidic soil, this work on Metsulfuron-methyl showed more convincing results. Two novel compounds (I-1 and I-2) were designed and synthesized, and they still retained potent herbicidal activity in tests against both dicotyledons and monocotyledons. The half-lives of degradation (DT50) assay revealed that I-1 showed an accelerated degradation rate in acidic soil (pH 5.59). Moreover, we delighted to find that the degradation rate of I-1 was 9-10-fold faster than that of Metsulfuron-methyl and Chlorsulfuron when in alkaline soil (pH 8.46), which has more practical value. This research suggests that a modified structure that has potent herbicidal activity as well as accelerated degradation rate could be realized and this approach may provide a way to improve the residue problem of SUs in farmlands with alkaline soil.
- Zhou, Shaa,Hua, Xue-Wen,Wei, Wei,Gu, Yu-Cheng,Liu, Xiao-Qing,Chen, Jing-Huo,Chen, Ming-Gui,Xie, Yong-Tao,Zhou, Sha,Meng, Xiang-De,Zhang, Yan,Li, Yong-Hong,Wang, Bao-Lei,Song, Hai-Bin,Li, Zheng-Ming
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p. 7661 - 7668
(2017/09/15)
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- A convenient synthesis of 2-methoxycarbonyl-5-iodobenzene sulfonamide
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A convenient and concise synthesis of 2-methyl-5-nitrobenzene sulfonamide can be achieved by sulfochlorination and ammoniation with p-nitrotoluene as raw materials for an 81.2 % yield. 6-Aminosaccharin can be produced via oxidation and reduction in a 64.3
- Cai, Xinhong,Chen, Qiulu,Guan, Jing,Gong, Shunze,Fu, Hao,Xu, Defeng
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p. 1622 - 1624
(2017/05/29)
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- In vitro inhibition effect and structure-activity relationships of some saccharin derivatives on erythrocyte carbonic anhydrase i and II
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In this study, in vitro inhibitory effects of some saccharin derivatives on purified carbonic anhydrase I and II were investigated using CO2 as a substrate. The results showed that all compounds inhibited the hCA I and hCA II enzyme activities. Among the compounds, 6-(p-tolylthiourenyl) saccharin (6m) was found to be the most active one for hCA I activity (IC50 = 13.67 μM) and 6-(m-methoxyphenylurenyl) saccharin (6b) was found to be the most active one for hCA II activity (IC50 = 6.54 μM). Structure-activity relationships (SARs) study showed that, generally, thiourea derivatives (6l - v) inhibited more hCA I and hCA II than urea derivatives (6a-k). All compounds (excluding 6c and 6r) have higher inhibitory activity on hCA II than on hCA I.
- Sonmez, Fatih,Bilen, Cigdem,Sumersan, Sinem,Gencer, Nahit,Isik, Semra,Arslan, Oktay,Kucukislamoglu, Mustafa
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p. 118 - 123
(2014/03/21)
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- TREATMENT FOR VITILIGO
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Compounds I and II, as well as prodrugs, hydrates, solvates, N-oxides, salts and pharmaceutical compositions containing them, are useful for treating vitiligo. In certain embodiments, the compounds are provided in topical compositions.
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- Cyclic secondary sulfonamides: Unusually good inhibitors of cancer-related carbonic anhydrase enzymes
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Carbonic anhydrase IX (CA IX) is a target for hypoxic cancer therapies, and the discovery of CA IX selective ligands is imperative for the development of these agents. Primary sulfonamides are broad specificity inhibitors of CA enzymes, while secondary su
- Moeker, Janina,Peat, Thomas S.,Bornaghi, Laurent F.,Vullo, Daniela,Supuran, Claudiu T.,Poulsen, Sally-Ann
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p. 3522 - 3531
(2014/05/20)
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- COMPOSITION FOR OPHTHALMIC ADMINISTRATION
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Disclosed herein are embodiments of a composition useful for treating and/or preventing dry eye disorders. The disclosed composition comprises components that maintain the composition's chemical and/or physical properties thereby providing a composition suitable for use.
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Paragraph 0086; 0087
(2014/08/06)
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- FURO[3,2-d]PYRIMIDINE COMPOUNDS
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The present invention is directed to novel compounds of Formula (I), pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof wherein the variables are defined as herein. The compounds of Formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.
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- New saccharin derivatives as tyrosinase inhibitors
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A newly series of 6-(phenylurenyl/thiourenyl) saccharin (6a-y) derivatives were synthesized and their inhibitory effects on the diphenolase activity of banana tyrosinase were evaluated. A 70-fold purification of the enzyme with 6.85% yield was achieved by using a Sepharose 4B-l-tyrosine-p-amino benzoic acid affinity column. The result showed that all the synthesized compounds inhibited the tyrosinase enzyme activity. Among the compounds synthesized, 6-(3-iodophenylthiourenyl) saccharin (6s) was found to be most active one (Ki = 3.95 μM) and the inhibition kinetics analyzed by Lineweaver-Burk double reciprocal plots revealed that compound 6s was a competitive inhibitor. Structure-activity relationships study showed that generally, most of the 6-(phenylthiourenyl) saccharin derivatives (6m-y) exhibited higher inhibitory activity than 6-(phenylurenyl) saccharin derivatives (6a-l). An electron-withdrawing group at 3-position of phenylurenyl-ring increased in activity and the halogen series at 3-position of phenylthiourenyl-ring showed a qualitative relationship for higher inhibitory activity with increasing size and polarizability. We also calculated HOMO-LUMO energy levels and dipole moments of some selected the synthesized compounds (6a, 6h, 6m and 6s) using Gaussian software.
- Gener, Nahit,Demir, Dudu,Sonmez, Fatih,Kucukislamoglu, Mustafa
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p. 2811 - 2821
(2012/06/29)
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- TREATMENT FOR DISCOID LUPUS
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Compounds I and II as well as salts and pharmaceutical compositions containing them are useful for treating diseases and/or disorders of the skin, such as cutaneous lupus, for example acute cutaneous lupus erythematosus, subacute cutaneous lupus erythematosus, or discoid lupus erythematosus. In certain embodiments, the compounds are provided in topical compositions.
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- Synthesis of some bisnitrosaccharins
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Method for synthesis of previously unknown bisnitrosaccharins from 6-nitrosaccharin under the action of bishalide compounds in polar aprotic solvents in the presence of anhydrous potassium carbonate is suggested. Pleiades Publishing, Ltd., 2012.
- Tagiev,Kazaz,Anyl
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p. 1581 - 1585
(2013/02/23)
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- A highly selective space-folded photo-induced electron transfer fluorescent probe for carbonic anhydrase isozymes IX and its applications for biological imaging
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The first highly selective and sensitive fluorescent probe Z1 for detection of carbonic anhydrase IX (CA IX) over isoforms CA I and CA II was developed. As demonstrated, Z1 worked effectively in both enzymatic systems and living hypoxia cells.
- Zhang, Shenyi,Yang, Chunmei,Lu, Weiqiang,Huang, Jin,Zhu, Weiping,Li, Honglin,Xu, Yufang,Qian, Xuhong
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supporting information; experimental part
p. 8301 - 8303
(2011/09/14)
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- COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY
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Compounds I and II as well as salts and pharmaceutical compositions containing them are useful for treating diseases and/or disorders of the eye.
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Page/Page column 11
(2011/02/25)
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- PYRIMDINE COMPOUNDS USEFUL AS KINASE INHIBITORS
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A compound of formula (I) or a salt or solvate thereof: Formula (1) compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such mono-anilino pyrimidine derivative
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Page/Page column 166-167
(2010/11/30)
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- Synthesis of (bis)sulfonic acid, (bis)benzamides as follicle-stimulating hormone (FSH) antagonists.
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Screening efforts identified (bis)sulfonic acid, (bis)benzamides (1-3) as compounds that interact with the follicle stimulating-hormone receptor (FSHR) and inhibit FSH-stimulated cAMP accumulation with IC(50) values in the low micromolar range. Structure-activity relationship studies using novel analogues of 1-3 revealed that two phenylsulfonic acid moieties were necessary for activity and that the carbon-carbon double bond of the stilbene sub-series was the optimum spacer connecting these groups. Selected analogues (2, 14, and 50) were also able to block FSHR-dependent estradiol production in rat primary ovarian granulosa cells and progesterone secretion in a clonal mouse adrenal Y1 cell line. IC(50) values for these compounds in these assays were in the low micromolar range. Optimization of the benzoic acid side chains of 1-3 led to gains in selectivity versus activity at the thyroid stimulating hormone (TSH) receptor (TSHR). For instance, while stilbene (bis)sulfonic acid congener 2 was only 10-fold selective for FSHR over TSHR, analogue 50 with an IC(50) value of 0.9 microM in the FSHR-cAMP assay was essentially inactive at 30 microM in the TSHR-cAMP assay.
- Wrobel, Jay,Green, Daniel,Jetter, James,Kao, Wenling,Rogers, John,Perez, M Claudia,Hardenburg, Jill,Deecher, Darlene C,Lopez, Francisco J,Arey, Brian J,Shen, Emily S
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p. 639 - 656
(2007/10/03)
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