- COMPOUNDS AND USES THEREOF
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The present disclosure features compounds useful for the treatment of BAF complex-related disorders.
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Page/Page column 137; 184
(2021/10/15)
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- SMARCA DEGRADERS AND USES THEREOF
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The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same for the modulation of one or more SWI/SNF-related matrix associated actin dependent regulator of chromatin subfamily A (SMARCA) and/or polybromo-1 (PB-1) protein via ubiqitination and/or degradation by compounds. The compounds are bifunctional molecules that link a cereblon-binding moiety to a ligand that binds SMARCA and/or PB1 proteins.
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Paragraph 00928; 00929
(2020/12/30)
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- Azido-Desferrioxamine Siderophores as Functional Click-Chemistry Probes Generated in Culture upon Adding a Diazo-Transfer Reagent
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This work aimed to undertake the in situ conversion of the terminal amine groups of bacterial desferrioxamine (DFO) siderophores, including desferrioxamine B (DFOB), to azide groups to enable downstream click chemistry. Initial studies trialed a precursor-directed biosynthesis (PDB) approach. Supplementing Streptomyces pilosus culture with blunt-end azido/amine non-native substrates designed to replace 1,5-diaminopentane as the native diamine substrate in the terminal amine position of DFOB did not produce azido-DFOB. Addition of the diazo-transfer reagent imidazole-1-sulfonyl azide hydrogen sulfate to spent S. pilosus medium that had been cultured in the presence of 1,4-diaminobutane, as a viable native substrate to expand the suite of native DFO-type siderophores, successfully generated the cognate suite of azido-DFO analogues. CuI-mediated or strain-promoted CuI-free click chemistry reactions between this minimally processed mixture and the appropriate alkyne-bearing biotin reagents produced the cognate suite of 1,4-disubstituted triazole-linked DFO-biotin compounds as potential molecular probes, detected as FeIII-loaded species. The amine-to-azide transformation of amine-bearing natural products in complex mixtures by the direct addition of a diazo-transfer reagent to deliver functional click chemistry reagents adds to the toolbox for chemical proteomics, chemical biology, and drug discovery.
- Gotsbacher, Michael P.,Codd, Rachel
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p. 1433 - 1445
(2020/02/27)
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- Modular RNA regulators and methods
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This disclosure describes modular miRNA regulator molecules and methods of using modular miRNA regulator molecules. Generally, the modular miRNA regulator molecules include a recognition module and an inhibition module. Generally, the recognition module includes a polynucleotide in which at least a portion of the polynucleotide recognizes at least a portion of a preselected pre-miRNA. Generally, the inhibition module includes a moiety that inhibits nuclease processing of the preselected pre-RNA to a mature RNA.
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Page/Page column 22
(2018/10/30)
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- For the treatment of tumor macrocyclic derivatives (by machine translation)
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The invention discloses a method for modulating protein kinase activity, and is used for the treatment or prevention of protein kinase related disorders. Specifically, the invention relates to a method for the treatment of tumor of the macrocyclic derivatives, which belongs to the regulating Anaplastic lymphoma kinase (ALK) active compound, and provides the preparation method of the compound, and the compound used for the treatment or prevention of diseases associated with the ALK pharmaceutical use. (by machine translation)
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Paragraph 0176; 0180-0181
(2017/07/20)
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- Design, radiosynthesis, and evaluation of radiotracers for positron emission tomography imaging of stearoyl-CoA desaturase-1
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Design, radiosynthesis, and biological evaluation of two radiotracers (N-(3-[18F]fluoropropyl)-6-(4-(trifluoromethyl)benzoyl)-piperazin-1-yl)pyridazine-3-carboxamide (18F-FPPPT) and (N-(4-[18F]fluoroaniline)-6-(4-(trifluoromethyl)benzoyl)-piperazin-1-yl)pyridazine-3-carboxamide (18F-FAPPT)) are described for noninvasive assessment of stearoyl-CoA desaturase-1 (SCD-1). The overexpression of SCD-1 in multiple solid tumors associates with poor survival in cancer patients. The two radiotracers,18F-FPPPT and18F-FAPPT, were each prepared in three steps in radiochemical yields of 21% and 3%, respectively. The practicality of imaging SCD-1 with18F-FPPPT was tested in two mouse models bearing xenograft tumors with different levels of SCD-1 expression, which afforded a 1.8-fold uptake difference correspondingly. Our work indicates that it is possible to develop SCD-1 specific imaging probes from previously reported SCD-1 inhibitors.
- Silvers, William C.,Cai, Hancheng,?z, Orhan K.,Sun, Xiankai
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p. 924 - 927
(2016/05/24)
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- SURFACE FUNCTIONALIZED, HOST-GUEST POLYMER NANO-ASSEMBLIES AND METHODS THEREOF
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The invention generally relates to polymer-based nano-structures. More particularly, the invention relates to novel, surface-functionalized, guest-host polymer nano-assemblies and nano-delivery vehicles useful in diverse fields including drug delivery, diagnostics and specialty materials. The nano-assemblies and nano-delivery vehicles of the invention are afforded via simplify and reliable approaches.
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Paragraph 00108; 00112
(2015/09/28)
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- Regioselective rapid synthesis of fully substituted 1,2,3-triazoles mediated by propargyl cations
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Regioselective rapid triazole syntheses at low temperature are described. Organic azides and propargyl cations generated by acids gave fully substituted 1H-1,2,3-triazoles. Most reactions could be performed in 5 min at not only rt but also -90 C. Both terminal and internal alkynes were acceptable, and the sterically bulky substituents could afford the products smoothly. Various types of three-component coupling reactions were demonstrated, and the presence of allenylaminodiazonium intermediates was indicated.
- Zhang, Huan,Tanimoto, Hiroki,Morimoto, Tsumoru,Nishiyama, Yasuhiro,Kakiuchi, Kiyomi
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supporting information
p. 5222 - 5225
(2013/11/06)
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- ANTIFUNGAL AGENTS
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Compounds and compositions useful as antifungals are provided, as are methods of use and preparation of such compounds and compositions containing such compounds. In some embodiments, the compounds are bifunctional, comprising two active moieties connected by a linking moiety. The compounds of the invention are useful for treating infections by microorganisms.
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Page/Page column 37
(2012/04/23)
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- COMPSITIONS, SYNTHESIS, AND METHODS OF USING QUINOLINE BASED ATYPICAL ANTIPSYCHOTIC AGENTS
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The present invention provides novel quinolinone derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression.
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Page/Page column 30
(2009/01/20)
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- INHIBITORS OF AKT ACTIVITY
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Invented are novel 1 H-imidazo[4,5-c]pyridin-2-yl compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
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Page/Page column 76
(2008/06/13)
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- Camptothecin derivatives
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A camptothecin derivative comprising a compound of the formula ?I!: STR1 wherein R1, R2, R3, R4 and R5 are (A) adjacent two groups combine to form alkylene, or both are H, and one of the remaining three groups is --Xn --Alkm --R6, and the other two are H, alkyl or halogen, or (B) adjacent two groups combine to form alkylene, and one of the carbon atoms of said alkylene group is substituted by --Xn --Alkm --R6, and the remaining three groups are H, alkyl or a halogen, and one or two --CH2 -- of the alkylene in (A) or (B) may optionally be replaced by --O--, --S-- or --NH--, X is --O-- or --NH--, Alk is alkylene, R6 is --NH2, STR2 or --OH, m and n are both 0 or 1, or m is 1 and n is 0, which camptothecin compound is bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof. Said camptothecin derivatives show enhanced antitumor activities but few side effects and are useful as a medicament.
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- S type 2-substituted hydroxy-2-indolidinylbutyric ester compounds and process for preparation thereof
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A process for preparing S type 2-substituted hydroxy-2-indolidinyl-butyric ester compound ?II!: STR1 wherein Ro is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of "R"(in which the nitrogen atom is protected), R1 and R2 are lower alkyl group, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound ?I!: STR2 wherein the symbols are as defined above.
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- Camptothecin derivatives
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A camptothecin derivative comprising a compound of the formula ?I!: STR1 wherein R1 is a substituted or unsubstituted lower alkyl group, X1 is a group of the formula: --NHR2 (R2 is a hydrogen atom or a lower alkyl group) or a group of --OH, and Alk is a straight chain or branched chain alkylene group having optionally an oxygen atom in the chain thereof, bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof. Said camptothecin derivatives show enhanced antitumor activities but few side effects unlike conventional anticancer agents, and hence, these compounds are extremely useful as a medicament.
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- N-[4-(3-aminopropyl)-aminobutyl]-2-(ω-guanidino-fatty-acid-amido)-2-substituted-ethanamide and salt thereof
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N-[4-(3-Aminopropyl)aminobutyl]-2-(ω-guanidino-fatty acid-amido)-2-substituted-ethanamides represented by the general formula STR1 wherein Y represents --(CH2 --CH2 --, --CH=CH or STR2 R represents a hydrogen atom, an alkyl group of 1 to 4 carbon atoms which may have a hydroxyl group as substituent, or a benzyl group, and n is an integer of from 1 to 8, provided that when Y is STR3 and n is 4, R represents the groups other than the hydrogen atom; a salt thereof having antitumor activity in experimental animal tumors and a process for the preparation thereof is provided.
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- N-[4-[(3-aminopropyl)amino]butyl]-2,2-dihydroxyethanamide
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N-[4-[(3-aminopropyl)amino]butyl]-2,2-dihydroxyethanamide is an immunostimulant in animals and an intermediate for synthesis of the antibiotic BMG162-aF2.
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