- FLUORINE-CONTAINING COMPOUND AND ANTI-CANCER MEDICAL USE THEREOF
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The present invention provides a fluorine-containing compound shown in Formula II/III and its anti-cancer medical use.
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Paragraph 0071; 0169-0170
(2022/04/03)
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- COMPOUNDS FOR THE TREATMENT OF ONCOVIRUS INDUCED CANCER AND METHODS OF USE THEREOF
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The pesent invention relates to compounds of formula (I) pharmaceutically-acceptable salts, hydrates, solvates, or stereoisomers thereof and their use for the prevention and treatment of oncovirus induced cancer in a subject.
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Page/Page column 129-131
(2020/10/21)
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- INHIBITORS OF NOTCH SIGNALLING PATHWAY AND USE THEREOF IN TREATMENT OF CANCERS
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The present invention relates to new inhibitors of Notch signalling pathway and its use in the treatment and/or prevention of cancers.
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Page/Page column 153
(2020/10/21)
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- Amine compound inhibiting SSAO/VAP-1 and application thereof in medicine
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The invention relates to an amine compound for inhibiting semicarbazide-sensitive amine oxidase (SSAO) and/or vascular adhesion protein 1 (VAP-1) and medicinal application thereof, and further relatesto a pharmaceutical composition containing the compound
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Paragraph 0467; 0468; 0469; 0470
(2019/02/04)
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- Synthesis of 6-Arylpyridin-3-ols by Oxidative Rearrangement of (5-Arylfurfuryl)amines
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The synthesis of 6-arylpyridin-3-ols and their 2,4-dibrominated analogues has been achieved by the oxidative rearrangement of (5-arylfurfuryl)amines. The desired arylpyridols were obtained in good to high yields, and the reactions were shown to be suitable for preparation on a gram scale.
- Fürst, Michael C. D.,Sauer, Caroline S.,Moriyama, Takaaki,Kamimura, Akio,Heinrich, Markus R.
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p. 3051 - 3055
(2016/07/12)
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- Repositioning Antitubercular 6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]oxazoles for Neglected Tropical Diseases: Structure-Activity Studies on a Preclinical Candidate for Visceral Leishmaniasis
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6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]oxazole derivatives were initially studied for tuberculosis within a backup program for the clinical trial agent pretomanid (PA-824). Phenotypic screening of representative examples against kinetoplastid diseases unexpectedly led to the identification of DNDI-VL-2098 as a potential first-in-class drug candidate for visceral leishmaniasis (VL). Additional work was then conducted to delineate its essential structural features, aiming to improve solubility and safety without compromising activity against VL. While the 4-nitroimidazole portion was specifically required, several modifications to the aryloxy side chain were well-tolerated e.g., exchange of the linking oxygen for nitrogen (or piperazine), biaryl extension, and replacement of phenyl rings by pyridine. Several less lipophilic analogues displayed improved aqueous solubility, particularly at low pH, although stability toward liver microsomes was highly variable. Upon evaluation in a mouse model of acute Leishmania donovani infection, one phenylpyridine derivative (37) stood out, providing efficacy surpassing that of the original preclinical lead.
- Thompson, Andrew M.,O'Connor, Patrick D.,Blaser, Adrian,Yardley, Vanessa,Maes, Louis,Gupta, Suman,Launay, Delphine,Martin, Denis,Franzblau, Scott G.,Wan, Baojie,Wang, Yuehong,Ma, Zhenkun,Denny, William A.
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p. 2530 - 2550
(2016/04/10)
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- Pyrrolidines
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This invention relates to a class of pyrrolidine compounds of formula (I), and pharmaceutically acceptable derivatives thereof, to their use in medicine, to compositions containing them, and to processes for their preparation. It also relates to intermedi
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Page/Page column 40
(2010/06/11)
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- Heteroaryl-substituted carboxamides and use thereof for the stimulation of the expression of NO synthase
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The present invention relates to heteroaryl-substituted carboxamides of the formula I, in which Het, A, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxi
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Page/Page column 71-72
(2008/12/06)
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