880875-39-8Relevant articles and documents
Synthesis of Diiodinated All-Carbon 3,3′-Diphenyl-1,1′-spirobiindene Derivatives via Cascade Enyne Cyclization and Electrophilic Aromatic Substitution
Li, Quanzhe,Yu, Liuzhu,Wei, Yin,Shi, Min
supporting information, p. 9282 - 9296 (2019/08/12)
A synthetic method for the construction of diiodinated all-carbon spirobiindene derivatives has been developed from the reaction of propargyl alcohol-tethered alkylidenecyclopropanes with iodine. The reaction proceeded through an iodination-initiated cascade intramolecular enyne cyclization and electrophilic aromatic substitution reaction process in 1,2-dichloroethane upon heating, giving desired spirocyclic products in moderate to excellent yields. Further transformation of the obtained products has also been presented.
Palladium-Catalyzed Cascade Reductive and Carbonylative Cyclization of Ortho-Iodo-Tethered Methylenecyclopropanes (MCPs) Using N-Formylsaccharin as CO Source
Fan, Xing,Shi, Min,Wei, Yin
supporting information, p. 5677 - 5683 (2019/11/16)
A palladium-catalyzed reductive and carbonylative cyclization of ortho-iodo-tethered methylenecyclopropanes (MCPs) using N-formylsaccharin as CO source has been developed, affording the desired indanone derivatives in moderate to good yields with high regio- and stereoselectivity and good functional group compatibility.
Catalyst-free geminal aminofluorination of ortho-sulfonamide-tethered alkylidenecyclopropanes via a Wagner-Meerwein rearrangement
Fan, Xing,Wang, Qiang,Wei, Yin,Shi, Min
supporting information, p. 10503 - 10506 (2018/09/21)
A catalyst-free intramolecular geminal aminofluorination of ortho-sulfonamide-tethered alkylidenecyclopropanes has been developed. The reaction proceeded through two SET processes with Selectfluor to give a fluorinated cyclopropylcarbinyl cation and a further Wagner-Meerwein rearrangement to generate a cyclobutyl carbocation, which undergoes intramolecular nucleophilic capture by amide to forge fluorinated cyclobuta[b]indoline derivatives. A polycyclic multi-fluorinated byproduct was also formed through a Ritter-type reaction in some cases.
Cascade Amination/Cyclization/Aromatization Process for the Rapid Construction of [2,3-c]Dihydrocarbazoles and [2,3-c]Carbazoles
Fan, Xing,Yu, Liu-Zhu,Wei, Yin,Shi, Min
supporting information, p. 4476 - 4479 (2017/09/11)
An intramolecular cascade amination/cyclization/aromatization reaction of functionalized alkylidenecyclopropanes has been developed in the presence of silver acetate, affording a variety of [2,3-c]dihydrocarbazoles and [2,3-c]carbazoles in moderate to excellent yields. The mechanistic investigations revealed that this cascade reaction proceeds through a radical initiated process. Moreover, further transformations for the synthesis of eustifoline-D and an OLED exhibit a potential synthetic utility of this method.
Structure-activity relationships and pharmacophore model of a noncompetitive pyrazoline containing class of GluN2C/GluN2D selective antagonists
Acker, Timothy M.,Khatri, Alpa,Vance, Katie M.,Slabber, Cathryn,Bacsa, John,Snyder, James P.,Traynelis, Stephen F.,Liotta, Dennis C.
supporting information, p. 6434 - 6456 (2013/09/23)
Here we describe the synthesis and structure-activity relationship for a class of pyrazoline-containing dihydroquinolone negative allosteric modulators of the NMDA receptor that show strong subunit selectivity for GluN2C- and GluN2D-containing receptors over GluN2A- and GluN2B-containing receptors. Several members of this class inhibit NMDA receptor responses in the nanomolar range and are more than 50-fold selective over GluN1/GluN2A and GluN1/GluN2B NMDA receptors, as well as AMPA, kainate, GABA, glycine, nicotinic, serotonin, and purinergic receptors. Analysis of the purified enantiomers of one of the more potent and selective compounds shows that the S-enantiomer is both more potent and more selective than the R-enantiomer. The S-enantiomer had an IC 50 of 0.17-0.22 μM at GluN2D- and GluN2C-containing receptors, respectively, and showed over 70-fold selectivity over other NMDA receptor subunits. The subunit selectivity of this class of compounds should be useful in defining the role of GluN2C- and GluN2D-containing receptors in specific brain circuits in both physiological and pathophysiological conditions.
QUINOLINE DERIVATIVES AS PIK3 INHIBITORS
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Page/Page column 31, (2012/06/01)
Substituted bicyclic heteroaryls having the general formula (I) and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with pl 108 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML), Myelodysplastic syndrome (MDS), myeio-proiiferative diseases (MPD), Chronic Myeloid Leukemia (CML), T-cell Acute Lymphoblastic leukaemia (T-ALL), B-cell Acute Lymphoblastic leukaemia (B-ALL), Non Hodgkins Lymphoma (NHL), B-cell lymphoma and solid tumors, such as breast cancer.
QUINAZOLINONE T-TYPE CALCIUM CHANNEL ANTAGONISTS
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Page/Page column 22-23, (2010/11/23)
The present invention is directed to quinazolinone compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
COMPOUNDS WHICH INCREASE APOLIPOPROTEIN A-1 PRODUCTION AND USES THEREOF IN MEDICINE
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Page/Page column 32, (2010/10/20)
The present invention relates to compounds of formula (I), pharmaceutically acceptable salts thereof, hydrates thereof, solvates thereof, prodrugs thereof and combinations thereof: wherein X represents CH or N; Y represents CH or N; R1 represents H or C1-2alkyl; R2 represents H or C1-4alkyl; R3 represents C1-6alkyl, carbocyclyl, carbocyclylC1-4alkyl, heterocyclyl or heterocyclylC1-4alkyl, wherein any of the carbocyclyl or heterocyclyl groups are optionally substituted by one or two groups selected from: halogen, C1-6alkyl, haloC1-6alkyl, hydroxyC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, nitro, cyano, -COH, -COOH, C1-6alkoxycarbonyl, C1-6alkylcarbonyl, -C(OH)R5R6 (wherein R5 and R6 independently represent H or C1-6alkyl), -(CH2)nNR3aR3b and -O(CH2)pNR3aR3b (wherein n represents 1, 2 or 3, p represents 2 or 3 and R3a and R3b independently represent H, C1-6alkyl or carbocyclylC1-4alkyl, or R3a and R3b together with the interconnecting atoms form a 5 or 6-membered ring which ring optionally contains one or two heteroatoms independently selected from the group consisting of O, S and N); R4 represents H, hydroxy, halo, C 1-6 alkyl, haloC1-6alkyl, hydroxyC1-6alkyl, C2-6alkenyl, C1-6alkoxy, haloC1-6alkoxy, carbocyclyl or heterocyclyl, wherein the carbocyclyl or heterocyclyl group is optionally substituted by one or two groups selected from: halogen, C1-6alkyl, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, nitro and cyano; and provided that the compound is not: 7-chloro-5-phenyl-[1,2,4]triazolo[4,3-a]quinolin-4-amine; 7-chloro-1-methyl-5-phenyl[1,2,4]triazolo[4,3-a]quinolin-4-amine; or 7-chloro-5-(2-chlorophenyl)-1-methyl-{1,2,4]triazolo[4,3-a]quinolin-4-amine. Also disclosed are pharmaceutical compositions containing the compounds and to their use in medicine. The compound exhibit increased apo-A1 production and are useful in the treatment for example a disease or condition caused by raised levels of LDL-cholesterol or by inflammation.