- INHIBITORS OF RAF KINASES
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Provided herein are inhibitors of receptor tyrosine kinase effector, RAF, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.
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Paragraph 00297; 00300-00301
(2022/04/03)
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- COMPOUNDS AND USES THEREOF
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The present disclosure features compounds and methods useful for the treatment of BAF complex-related disorders.
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Page/Page column 294
(2021/08/06)
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- ANALOGS OF 2-PRALIDOXIME AS ANTIDOTES AGAINST ORGANOPHOSPHORUS NERVE AGENTS
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Provided herein are compounds useful in treating exposure to an organophosphorus compound, such as a nerve agent, pesticide, or, generally, an acetylcholinesterase inhibitor, such as sarin. Compositions, e.g. pharmaceutical compositions or dosage forms, comprising the compounds also are provided herein. Methods of treating a patient exposed to a nerve agent, pesticide, or, generally, an acetylcholinesterase inhibitor, e.g., an organophosphorus compound, such as sarin, also are provided.
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Paragraph 0079
(2020/02/23)
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- Synthesis method of 2-pyridylaldehyde derivative
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The invention relates to the field of medical intermediates, in particular to a synthesis method of 2-pyridylaldehyde derivative. A synthesis path shown in the formula 1 is adopted, wherein X can be Cl or Br or CF3. Cheap starting raw materials are adopted, the use of hazardous materials which have large toxicity and are easily explosive is avoided, the cost of the product is greatly lowered, popularization and industrialized production are facilitated, and the synthesis method has the advantages of being low in cost, easy to operate, high in yield, easy to industrialize and the like. The formula 1 is shown in the description.
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Paragraph 0067-0068; 0074-0075; 0076-0083
(2018/09/28)
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- 2-Pyridylquinolone antimalarials with improved antimalarial activity and physicochemical properties
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A series of 2-pyridylquinolones has been prepared in 5-7 steps and through lead optimisation, antimalarial activity as low as 12 nM against Plasmodium falciparum (Pf) has been achieved. Compared with previous analogues in this series, selected molecules h
- Charoensutthivarakul, Sitthivut,Hong, W. David,Leung, Suet C.,Gibbons, Peter D.,Bedingfield, Paul T.P.,Nixon, Gemma L.,Lawrenson, Alexandre S.,Berry, Neil G.,Ward, Stephen A.,Biagini, Giancarlo A.,O'Neill, Paul M.
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supporting information
p. 1252 - 1259
(2015/07/15)
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- Human carbonic anhydrase II as host protein for the creation of artificial metalloenzymes: The asymmetric transfer hydrogenation of imines
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In the presence of human carbonic anhydrase II, aryl-sulfonamide-bearing IrCp* pianostool complexes catalyze the asymmetric transfer hydrogenation of imines. Critical cofactor-protein interactions revealed by the X-ray structure of [(η5-Cp*)Ir(pico 4)Cl] 9 WT hCA II were genetically optimized to improve the catalytic performance of the artificial metalloenzyme (68% ee, kcat/KM 6.11 × 10 -3 min-1 mM-1).
- Monnard, Fabien W.,Nogueira, Elisa S.,Heinisch, Tillmann,Schirmer, Tilman,Ward, Thomas R.
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p. 3269 - 3274
(2013/07/26)
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- Tuning of the properties of transition-metal bispidine complexes by variation of the basicity of the aromatic donor groups
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Bispidines (3,7-diazabicyclo[3.3.1]nonanes) as very rigid and highly preorganized ligands find broad application in the field of coordination chemistry, and the redox potentials of their transition-metal complexes are of importance in oxidation reactions by high-valent iron complexes, aziridination catalyzed by copper complexes, and imaging by 64Cu positron emission tomography tracers. Here, we show that the redox potentials and stability constants of the copper(II) complexes of 15 tetradentate bispidines can be varied by substitution of the pyridine rings (variation of the redox potential over ca. 450 mV and of the complex stability over approximately 10 log units). It is also shown that these variations are predictable by the pKa values of the pyridine groups as well as by the Hammett parameters of the substituents, and the density functional theory based energy decomposition analysis also allows one to accurately predict the redox potentials and concomitant complex stability. It is shown that the main contribution emerges from the electrostatic interaction energy, and the partial charges of the pyridine donor groups therefore also correlate with the redox potentials.
- Comba, Peter,Morgen, Michael,Wadepohl, Hubert
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p. 6481 - 6501
(2013/07/19)
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- Synthesis of the pyridinyl analogues of dibenzylideneacetone (pyr-dba) via an improved Claisen-Schmidt condensation, displaying diverse biological activities as curcumin analogues
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An efficient and easy procedure to synthesize the pyridinyl analogues of dibenzylideneacetone (pyr-dba) was developed by the condensation of substituted nicotinaldehyde and acetone in the presence of K2CO3 in toluene-EtOH-H2O solvent system. Structurally diverse pyr-dba, including quinolinyl dba, can be prepared conveniently in moderate to excellent yields under mild conditions with this method. The resulting pyr-dba functioned as the enone analogs of curcumin and efficiently inhibited the activation of NF-κB and the growth of colorectal carcinoma HCT116 p53+/+ cells as well as the HIV-1 IN-LEDGF/p75 interaction. The Royal Society of Chemistry 2012.
- Cao, Bin,Wang, Yong,Ding, Kan,Neamati, Nouri,Long, Ya-Qiu
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experimental part
p. 1239 - 1245
(2012/03/07)
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- 8-SUBSTITUTED QUINOLINES AND RELATED ANALOGS AS SIRTUIN MODULATORS
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Provided herein are 8-substituted quinolines and related analogues as sirtuin-modulating compounds of Structural Formula (I) and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
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Page/Page column 124
(2010/09/18)
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- NEW COMPOUNDS 578
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The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
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Page/Page column 24
(2010/06/13)
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- PYRIDINE DERIVATIVES AS SODIUM CHANNEL BLOCKERS
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Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein; each of R1 to R4 is independently selected from hydrogen and C1-4 alkyl, and each of rings A and B independently is optionally further substi
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Page/Page column 27-28
(2010/11/30)
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- A convenient synthetic route to a useful synthon: 4-bromo-2-pyridinecarboxaldehyde
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We have developed a novel four-step method to synthesise 4-bromo-2-pyridinecarboxaldehyde, from 2-picoline-N-oxide via 4-nitro-2-pyridinecarboxaldehyde, under mild reaction conditions.
- Zaman, Nicolas,Guillot, Régis,Sénéchal-David, Katell,Boillot, Marie-Laure
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body text
p. 7274 - 7275
(2009/04/10)
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- Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for beta-secretase modulation
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The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles
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Page/Page column 12
(2008/06/13)
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- Triazolopyridines. 18.1 nucleophilic substitution reactions on triazolopyridines; a new route to 2,2'-Bipyridines
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The synthesis of some 5-, 6-, and 7-halogenotriazolopyridines is described and their reactions with nucleophiles. The formation or 7,7'-bitriazolopyridines provides a new synthesis of 2,2'-bipyridines.
- Jones, Gurnos,Pitman, Mark A.,Lunt, Edward,Lythgoe, David J.,Abarca, Belen,Ballesteros, Rafael,Elmasnaouy, Mostafa
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p. 8257 - 8268
(2007/10/03)
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