- HMOX1 inducers
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The present invention is related to compounds of structure (I) as heme oxygenase 1 (HMOX 1) inducers. The present invention is also related a method of controlling the activity or the amount, or both the activity and the amount, of heme-oxygenase 1 in a mammalian subject. The definitions of the variables are provided herein.
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Page/Page column 70
(2020/09/18)
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- HETEROCYCLIC COMPOUND
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The present invention relates to a compound represented by the formula (I), which is useful as an agent for the prophylaxis or treatment of epilepsy, neurodegenerative disease and the like. In the formula (I), each symbol is as defined in the specification.
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- Synthesis and in vitro antimycobacterial and isocitrate lyase inhibition properties of novel 2-methoxy-2′-hydroxybenzanilides, their thioxo analogues and benzoxazoles
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A new series of 2-methoxy-2′-hydroxybenzanilide derivatives and their thioxo analogues have been synthesised and characterised by IR, NMR and elemental analysis. These compounds were investigated for their in vitro antimycobacterial activities against Mycobacterium tuberculosis 331/88, Mycobacterium avium 330/88, Mycobacterium kansasii 235/80, clinically isolated M. kansasii 6509/96 and the ability to act as in vitro isocitrate lyase inhibitors. The best ICL inhibitors were two compounds from the thiobenzanilide group (8f, 8m), which exhibited an inhibition potential that was equal to the standard compound, 3-nitropropionic acid. In addition, the best antimycobacterial properties were exhibited by benzanilide derivatives 6h, 6k and 6l with 5-Cl and 4′ or 5′ Cl/Br substitution. For all the thiobenzanilide derivatives tested, two conformers were observed in the NMR spectra, which is most likely due to the hindered rotation of the C-N bond.
- Kozic, Ján,Novotná, Eva,Volková, Marie,Stola?íková, Ji?ina,Trejtnar, Franti?ek,Wsól, Vladimír,Vin?ová, Jarmila
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p. 108 - 119
(2013/01/15)
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- Non-steroidal dissociated glucocorticoid agonists: Indoles as A-ring mimetics and function-regulating pharmacophores
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We report a SAR of non-steroidal glucocorticoid mimetics that utilize indoles as A-ring mimetics. Detailed SAR is discussed with a focus on improving PR and MR selectivity, GR agonism, and in vitro dissociation profile. SAR analysis led to compound (R)-33 which showed high PR and MR selectivity, potent agonist activity, and reduced transactivation activity in the MMTV and aromatase assays. The compound is equipotent to prednisolone in the LPS-TNF model of inflammation. In mouse CIA, at 30 mg/kg compound (R)-33 inhibited disease progression with an efficacy similar to the 3 mg/kg dose of prednisolone.
- Betageri, Raj,Gilmore, Thomas,Kuzmich, Daniel,Kirrane, Thomas M.,Bentzien, J?rg,Wiedenmayer, Dieter,Bekkali, Younes,Regan, John,Berry, Angela,Latli, Bachir,Kukulka, Alison J.,Fadra, Tazmeen N.,Nelson, Richard M.,Goldrick, Susan,Zuvela-Jelaska, Ljiljana,Souza, Don,Pelletier, Josephine,Dinallo, Roger,Panzenbeck, Mark,Torcellini, Carol,Lee, Heewon,Pack, Edward,Harcken, Christian,Nabozny, Gerald,Thomson, David S.
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scheme or table
p. 6842 - 6851
(2011/12/22)
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- Syntheses and bioactivity of o- or p-trifluoromethylphenyl phosphates
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o- and p-Trifluoromethylphenyl phosphates designed as mechanism-based phosphotyrosine phosphatase inactivators have been prepared. Some of them show herbicidal activities.
- Zhou, Xinming,He, Yantao,Wang, Miao,Ding, Yixiang
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scheme or table
p. 651 - 659
(2009/11/30)
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- Trifluoromethyltriphenodioxazine: Air-stable and high-performance n-type semiconductor
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(Chemical Equation Presented) Two trifluoromethyltriphenodioxazines were efficiently synthesized as active materials for n-type organic field-effect transistors, and their optical and electrochemical properties were characterized. Air-stable and high-performance thin film transistors based on the two compounds were fabricated.
- Di, Chong-An,Li, Jing,Yu, Gui,Xiao, Yi,Guo, Yunlong,Liu, Yunqi,Qian, Xuhong,Zhu, Daoben
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supporting information; experimental part
p. 3025 - 3028
(2009/05/07)
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- Palladium-catalyzed C-O bond formation: direct synthesis of phenols and aryl/alkyl ethers from activated aryl halides
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A simple and efficient palladium-catalyzed carbon-oxygen bond formation is reported. The palladium-tri-tert-butylphosphine complex was found to be effective in converting haloarenes to corresponding substituted phenols. This methodology offers a direct transformation of aryl halides to phenols, as well as the straightforward application to generate a wide variety of diaryl or alkyl/aryl ethers.
- Chen, Guoshu,Chan, Albert S.C.,Kwong, Fuk Yee
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p. 473 - 476
(2008/02/03)
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- A General Procedure for the Fluorodenitration of Aromatic Substrates
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The synthesis of several fluoroaromatic compounds by a new procedure of fluorodenitration of nitroarenes is reported.The methodology is based on the principle that the nitrite ion, generated during the fluorodenitration processes and responsible for most of the undesired side reactions, can be trapped with a suitable reagent, e.g., phthaloyl difluoride or tetrafluorophthaloyl difluoride.The yields of fluoro compounds thus obtained are good to excellent, and the procedure is of general application.
- Maggini, Michele,Passudetti, Margherita,Gonzales-Trueba, Guadalupe,Prato, Maurizio,Quintily, Ugo,Scorrano, Gianfranco
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p. 6406 - 6411
(2007/10/02)
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- Phenylamine substituted on amine with a benzo(oxa, thia or di) azole group
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The invention concerns novel diarylamine derivatives of formula I STR1 wherein φ is chosen from STR2 The compounds are herbicides and in further embodiments the invention provides herbicidal compositions containing as active ingredient a compound of formula I, a process for severely damaging or killing unwanted plants by applying to the plants or to the growth medium of the plants an effective amount of a compound of formula I, processes for the preparation of compounds of formula I and intermediates useful in the preparation of compounds of formula I.
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- Process for the preparation of trifluoromethylphenols
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A process for the preparation of a trifluoromethylphenol or the corresponding alkoxy compound which comprises contacting a halogenobenzotrifluoride of the formula STR1 in which X denotes halogen, R1, R2 and R3 denote hydrogen, trifluoromethyl or a substituent which promotes the replacement of X by a hydroxyl group and Y denotes hydrogen, a halogen or alkoxy, at least one of the substituents R1, R2 and R3 representing a trifluoromethyl group and at least one of them representing a substituent which promotes the replacement of the radical X by a hydroxyl group, with an excess aqueous alkali metal hydroxide in an alcoholic solution in the presence of a quaternary onium salt.
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- Benzoxazine carboxamides
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3,4-Dihydro-N-(2-propenyl)-2H-1,4-benzoxazine-2-carboxamides, useful as lipogenesis inhibitors in mammals.
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- Lipogenesis control by esters of benzoxazinecarboxylic acids
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Lipogenesis in mammals is inhibited by esters of 3,4-dihydro-2H-1,4-benzoxazine-2-carboxylic acids.
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