- NEW BRAF INHIBITORS AS PARADOX BREAKERS
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The invention provides a novel compound having the general formula (I) (I) wherein R1-R3 and X are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.
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Page/Page column 43-44
(2021/06/22)
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- Sulfonamide derivatives of cis-imidazolines as potent p53-MDM2/MDMX protein-protein interaction inhibitors
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p53-MDM2/MDMX interaction inhibitors represent the prospective agents for targeted anticancer therapy in tumors expressing wild-type p53 protein. Imidazoline-based MDM2-targeted inhibitors of such type, nutlins, contain halogen-substituted phenyl rings, w
- Bazanov, Daniil R.,Kopeina, Gelina S.,Lozinskaya, Natalia A.,Maksutova, Anita I.,Pervushin, Nikolay V.,Savin, Egor V.,Sosonyuk, Sergey E.,Tsymliakov, Michael D.
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p. 2216 - 2227
(2021/10/14)
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- S(vi) in three-component sulfonamide synthesis: Use of sulfuric chloride as a linchpin in palladium-catalyzed Suzuki-Miyaura coupling
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Sulfuric chloride is used as the source of the -SO2- group in a palladium-catalyzed three-component synthesis of sulfonamides. Suzuki-Miyaura coupling between the in situ generated sulfamoyl chlorides and boronic acids gives rise to diverse sulfonamides in moderate to high yields with excellent reaction selectivity. Although this transformation is not workable for primary amines or anilines, the results show high functional group tolerance. With the solving of the desulfonylation problem and utilization of cheap and easily accessible sulfuric chloride as the source of sulfur dioxide, redox-neutral three-component synthesis of sulfonamides is first achieved. This journal is
- Wang, Xuefeng,Yang, Min,Ye, Shengqing,Kuang, Yunyan,Wu, Jie
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p. 6437 - 6441
(2021/05/19)
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- Triazole compounds and their use in agriculture (by machine translation)
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The present invention provides a triazole compound and its application in agriculture; in particular, the invention provides compounds of formula (A) indicated by the compound and its preparation method; the composition containing these compounds and preparation and their use as fungicides; wherein R1 , R2 , R3 , W, R4 , R5 , R6 , R7 , R8 , R9 , Ra , Rb And in the event of x has the meanings given by the invention. (by machine translation)
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Paragraph 0438; 0439; 0440; 0442; 0444
(2018/11/04)
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- Hit-to-Lead Optimization of a Novel Class of Potent, Broad-Spectrum Trypanosomacides
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The parasitic trypanosomes Trypanosoma brucei and T. cruzi are responsible for significant human suffering in the form of human African trypanosomiasis (HAT) and Chagas disease. Drugs currently available to treat these neglected diseases leave much to be
- Russell, Stephanie,Rahmani, Rapha?l,Jones, Amy J.,Newson, Harriet L.,Neilde, Kevin,Cotillo, Ignacio,Rahmani Khajouei, Marzieh,Ferrins, Lori,Qureishi, Sana,Nguyen, Nghi,Martinez-Martinez, Maria S.,Weaver, Donald F.,Kaiser, Marcel,Riley, Jennifer,Thomas, John,De Rycker, Manu,Read, Kevin D.,Flematti, Gavin R.,Ryan, Eileen,Tanghe, Scott,Rodriguez, Ana,Charman, Susan A.,Kessler, Albane,Avery, Vicky M.,Baell, Jonathan B.,Piggott, Matthew J.
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p. 9686 - 9720
(2016/11/19)
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- Quinoline-based compound and selective androgen receptor agonist comprising the same
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Provided are a novel quinoline-based compound, a pharmaceutical composition containing the quinoline-based compound, and a method for producing the quinoline-based compound. The quinoline-based compound acts on an androgen receptor to increase activities of the androgen receptor, and thus can be favorably used as an agent for treating and preventing diseases or conditions, in which the increased activities of the androgen can lead to improvement of symptoms or the responsiveness to treatment, for example, various hormone-related diseases of the male or female, muscle-wasting disease, osteoporosis, and the like.COPYRIGHT KIPO 2016
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Paragraph 0505-0507; 0515-0517
(2016/10/08)
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- Inhibitors of HCV NS5B polymerase: Synthesis and structure-activity relationships of N-alkyl-4-hydroxyquinolon-3-yl-benzothiadiazine sulfamides
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Substituted N-alkyl-4-hydroxyquinolon-3-yl-benzothiadiazine sulfamides were investigated as inhibitors of genotype 1 HCV polymerase. Structure-activity relationship patterns for this class of compounds are discussed.
- Chris Krueger,Madigan, Darold L.,Jiang, Wen W.,Kati, Warren M.,Liu, Dachun,Liu, Yaya,Maring, Clarence J.,Masse, Sherie,McDaniel, Keith F.,Middleton, Tim,Mo, Hongmei,Molla, Akhteruzzaman,Montgomery, Debra,Pratt, John K.,Rockway, Todd W.,Zhang, Rong,Kempf, Dale J.
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p. 3367 - 3370
(2007/10/03)
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- GAMMA-SECRETASE INHIBITORS
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Compounds of formula: (I) are potent inhibitors of gamma-secretase and hence find use in treatment or prevention of diseases associated with deposition of β-amyloid.
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Page/Page column 22
(2008/06/13)
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