- Compound for inhibiting EGFR kinase as well as preparation method and application thereof
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The invention provides a compound as shown in a general formula (I) and pharmaceutically acceptable salt thereof as well as a preparation method and application of the compound. The compound can selectively inhibit the activity of an EGFR (epidermal growt
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Paragraph 0040; 0074-0076
(2021/01/12)
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- Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model
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Histone deacetylase 6 (HDAC6) is a promising therapeutic target for the treatment of neurodegenerative disorders. SW-100 (1a), a phenylhydroxamate-based HDAC6 inhibitor (HDAC6i) bearing a tetrahydroquinoline (THQ) capping group, is a highly potent and sel
- Shen, Sida,Picci, Cristina,Ustinova, Kseniya,Benoy, Veronick,Kutil, Zsófia,Zhang, Guiping,Tavares, Maurício T.,Pavlí?ek, Ji?í,Zimprich, Chad A.,Robers, Matthew B.,Van Den Bosch, Ludo,Ba?inka, Cyril,Langley, Brett,Kozikowski, Alan P.
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p. 4810 - 4840
(2021/05/07)
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- Ruthenium-catalyzed intramolecular arene C(sp2)-H amidation for synthesis of 3,4-dihydroquinolin-2(1 H)-ones
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We report the [Ru(p-cymene)(l-proline)Cl] ([Ru1])-catalyzed cyclization of 1,4,2-dioxazol-5-ones to form dihydroquinoline-2-ones in excellent yields with excellent regioselectivity via a formal intramolecular arene C(sp2)-H amidation. The reactions of the 2- and 4-substituted aryl dioxazolones proceeds initially through spirolactamization via electrophilic amidation at the arene site, which is para or ortho to the substituent. A Hammett correlation study showed that the spirolactamization is likely to occur by electrophilic nitrenoid attack at the arene, which is characterized by a negative ρ value of -0.73.
- Au, Chi-Ming,Ling, Cho-Hon,Sun, Wenlong,Yu, Wing-Yiu
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supporting information
p. 3310 - 3314
(2021/05/29)
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- TETRAHYDROQUINOLINE SUBSTITUTED HYDROXAMIC ACIDS AS SELECTIVE HISTONE DEACETYLASE 6 INHIBITORS
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Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, tr
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Paragraph 0183; 0185
(2017/09/08)
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- COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES
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The present invention provides compounds of formula I: [INSERT FORMULA HERE] or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease, such as malaria, caused by a Plasmodium parasite.
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Page/Page column 140; 141
(2014/06/11)
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- Regiodivergent access to five- and six-membered benzo-fused lactams: Ru-catalyzed olefin hydrocarbamoylation
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We report herein a new strategy of the Ru-catalyzed intramolecular olefin hydrocarbamoylation for the regiodivergent synthesis of five- and six-membered benzo-fused lactams starting from N-(2-alkenylphenyl)formamides. Using a combined catalyst of Ru3
- Li, Bin,Park, Yoonsu,Chang, Sukbok
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supporting information
p. 1125 - 1131
(2014/02/14)
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- NOVEL HETEROCYCLIC CARBOXAMIDES AS M1 AGONISTS
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The present invention relates to novel M1 agonistic compounds of formula (I) and their use in the treatment of cognitive impairment associated i.a. with schizophrenia and in the treatment of other diseases mediated by the muscarinic M1 receptor.
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Page/Page column 58-59
(2009/10/21)
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- Novel approach to 3,4-dihydro-2(1H)-quinolinone derivatives via cyclopropane ring expansion
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N-(1'-Alkoxy)cyclopropyl-2-haloanilines are transformed to 3,4-dihydro-2(1H)-quinolinones via palladium-catalyzed cyclopropane ring expansion. The reaction tolerates a variety of functional groups such as ester, nitrile, ether, and ketone group
- Tsuritani, Takayuki,Yamamoto, Yuhei,Kawasaki, Masashi,Mase, Toshiaki
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supporting information; experimental part
p. 1043 - 1045
(2009/09/05)
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- The tandem reaction combining radical and ionic processes: an efficient approach to substituted 3,4-dihydroquinolin-2-ones
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3,4-Dihydroquinolin-2-ones are of great importance in the areas of pharmaceuticals. However, the direct intramolecular radical cyclizations of the corresponding amide compounds favor 5-exo products 2. Reports on the radical cyclization reactions producing
- Zhou, Wang,Zhang, Liangren,Jiao, Ning
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experimental part
p. 1982 - 1987
(2009/08/07)
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- TETRAHYDROQUINOLINE, INDOLINE, AND RELATED ANILINE DERIVATIVES OF HETEROCYCLE-FUSED BENZODIOXAN METHYLAMINES
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The present invention relates to a compound of the formula: or an enantiomer, diastereomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, useful as modulators of 5 -HTi A receptor activity and/or serotonin reuptake. These compounds are useful in treating nervous system disorders, such as anxiety-related disorders, cognition-related disorders, depression, schizophrenia, or sexual dysfunction and related illnesses.
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Page/Page column 62
(2008/06/13)
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- A Facile Regioselective Aromatic Fluorination of N-Aryl-N-hydroxyamides with Diethylaminosulfur Trifluoride (DAST)
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Treatment of N-aryl-N-hydroxyamides with diethylaminosulfur trifluoride (DAST) under conventional reaction conditions results in removal of the hydroxy function and introduction of a fluorine atom at the para position of the aromatic ring, in high yield.
- Kikugawa, Yasuo,Matsumoto, Kazuhiro,Mitsui, Kimiyo,Sakamoto, Takeshi
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p. 921 - 922
(2007/10/02)
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- Heterocyclic aldose reductase inhibitors and methods of using them
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The invention relates to new compounds of the formula: STR1 Aldose reductase inhibitors. Treatment of certain complications of diabetes.
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