- METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION
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Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods to recover wild-type function to p53 mutants. The compounds of the present invention can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.
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Paragraph 0869
(2021/04/02)
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- CARBOXAMIDE DERIVATIVE
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An SGLT inhibitor comprising a compound of the formula: (|) wherein the ring A is an optionally substituted ring; R1 is an optionally substituted hydrocarbon group, etc.; each of R2 and R3 independently is a hydrogen atom, an optionally substituted hydrocarbon group, etc.; R4 is an optionally substituted hydrocarbon group, etc.; and X is a bivalent chain group whose main chain consists of 1 to 6 atoms. This SGLT inhibitor is useful as a preventive/therapeutic agent for diabetes mellitus, obesity, hypertension, hyperlipemia, etc.
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Page/Page column 71
(2010/11/08)
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- Aminopolycarboxylic acids and derivatives thereof
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There are provided chelating agents particularly useful for the preparation of diagnostic and therapeutic agents for magnetic resonance imaging, scintigraphy, ultrasound imaging, radiotherapy and heavy metal detoxification, said agents being compounds of formula I wherein n and m are 2, 3 or 4; and A, X, R1 and Z are as defined in the specification.
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- Aminopolycarboxylic acids and derivatives thereof
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There are provided chelating agents particularly useful for the preparations of diagnostic and therapeutic agents for magnetic resonance imaging, scintigraphy, ultrasound imaging, radiotherapy and heavy metal detoxification, said agents being compounds of formula X--CHR1 --NZ--(CHR1)n --A--(CHR1)m --NZ--CHR1 --X wherein (each of the groups Z is a group --CHR1 X or the groups Z together are a group --(CHR1)q --A'--(CHR1)r --, where A' is an oxygen or sulphur atom or a group --N--Y; A is a group --N--Y or A--(CHR1)m -- represents a carbon-nitrogen bond or, when the groups Z together are a group --(CHR1)q --A'--(CHR1)r --, A may also represent an oxygen or sulphur atom; each Y, which may be the same or different, is a group --(CHR1)p --N(CHR1 X)2 or a group --CHR1 X; each X, which may be the same or different, is a carboxyl group or a derivative thereof or a group R1 ; each R1, which may be the same or different, is a hydrogen atom, a hydroxyalkyl group or an optionally hydroxylated alkoxy or alkoxyalkyl group; n, m, p, q and r are each 2, 3 or 4; with the provisos that at least two nitrogens carry a --CHR1 X moiety wherein X is a carboxyl group or a derivative thereof, that each --CHR1 X moiety is other than a methyl group, and that unless A' is oxygen or sulphur or A is N--(CHR1)p --N(CHR1 X)2 at least one R1 is other than hydrogen) and salts thereof.
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- A novel method for the synthesis of 9-[[2-hydroxy-1-(aminomethyl)ethoxy]methyl]guanine. A potential antiviral agent
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9-[[2-Hydroxy-1-(aminomethyl)ethoxy]methyl]guanine (1a), an amino analogue of 9-[[2-hydroxy-1-(hydroxymethyl)-ethoxy]methyl]guanine (I) which is a potent antiviral agent, has been synthesized via a multistep-synthesis.
- Liu,Kuzmich,Lin
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p. 613 - 616
(2007/10/02)
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