- Diaromatic vinyl derivative as well as preparation method and application thereof
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The structural formula of the diaromatic vinyl derivative is shown I. In-flight R1 Document CH3 (Methyl) or CD3 (Deuterated methyl). R2 A group selected from C1 - 8 saturated alkoxy or alkylamino, substituted C2
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Paragraph 0066; 0069-0072
(2021/09/29)
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- HETEROARYL-CARBOXYLIC ACIDS AS HISTONE DEMETHYLASE INHIBITORS
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The invention relates to heteroaryl-carboxylic acids as described herein, useful as histone demethylase inhibitors. The invention also relates to pharmaceutical compositions comprising these compounds and to their use in therapy, including e.g., in the treatment of cancer.
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Page/Page column 126
(2018/01/17)
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- PYRROLO[2,3-C]PYRIDINES AS IMAGING AGENTS FOR NEUROFIBRILARY TANGLES
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Pyrrolopyridine compounds of formula (I) or their pharmaceutically acceptable salts are disclosed, which may be suitable for imaging tau aggregates, b-sheet aggregates, beta-amyloid aggregates or alpha- synuclein aggregates, and hence are useful in binding and imaging tau aggregates in Alzheimer's patients. More specifically, the compounds are used as tracers in positron emission tomography (PET) imaging to study tau deposits in brain in vivo to allow diagnosis of Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology. Futher, the compounds are useful for measuring clinical efficacy of therapeutic agents for Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology.
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Page/Page column 114
(2016/01/01)
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- Structure-activity relationships of substituted 1-pyridyl-2-phenyl-1,2- ethanediones: Potent, selective carboxylesterase inhibitors
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Inhibition of intestinal carboxylesterases may allow modification of the pharmacokinetics/pharmacodynamic profile of existing drugs by altering half-life or toxicity. Since previously identified diarylethane-1,2-dione inhibitors are decidedly hydrophobic,
- Young, Brandon M.,Hyatt, Janice L.,Bouck, David C.,Chen, Taosheng,Hanumesh, Parimala,Price, Jeanine,Boyd, Vincent A.,Potter, Philip M.,Webb, Thomas R.
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supporting information; experimental part
p. 8709 - 8715
(2011/02/23)
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- Switchable cucurbituril-bipyridine beacons
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4-Aminobipyridine derivatives form strong inclusion complexes with cucurbit[6]uril, exhibiting remarkably large enhancements in fluorescence intensity and quantum yields. The remarkable complexation-induced pKa shift (ΔpKa =3.3) highlights the strong charge-dipole interaction upon binding. The reversible binding phenomenon can be used for the design of switchable beacons that can be incorporated into cascades of binding networks. This concept is demonstrated herein by three different applications: 1) a switchable fluorescent beacon for chemical sensing of transition metals and other ligands; 2) direct measurement of binding constants between cucurbit[6]uril and various nonfluorescent guest molecules; and 3) quantitative monitoring of biocatalytic reactions and determination of their kinetic parameters. The latter application is illustrated by the hydrolysis of an amide catalyzed by penicillin G acylase and by the elimination reaction of a b-cabamoyloxy ketone catalyzed by aldolase antibody 38C2.
- Sinha, Mantosh K.,Reany, Ofer,Parvari, Galit,Karmakar, Ananta,Keinan, Ehud
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experimental part
p. 9056 - 9067
(2010/10/01)
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- CHEMICAL COMPOUNDS
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Compounds of formula (I) and their pharmaceutically acceptable salts are described: Formula (I). Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
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Page/Page column 58-59
(2010/11/23)
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- Bicyclic heterocycles as cannabinoid receptor modulators
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The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula I: including all prodrugs, pharmaceutically acceptable salts and stereoisomers, R1, R2, R3, R3a, R4, A, B, n, Y and Z are described herein.
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Page/Page column 11
(2008/06/13)
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