- The metal complex, and (meth) acrylic acid ester copolymer of olefin / α - using the same (by machine translation)
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(Meth) acrylic acid ester of a high molecular weight copolymer [a] catalyst. The metal complex represented by the general formula [a] (A). [In the formula, R9 - R13 Hydrogen, a substituent represented by the general formula (B) (R14 And R15 The, are each independently hydrogen or a hydrocarbon group of 1 - 6 carbon atoms which may have a hetero atom, may form a ring together), 6 - 12 carbon atoms with an aryl group, an adamantyl group, OR2 , SR2 , Or N (R2 )2 , Represents. However, R9 - R13 One of the, at least one substituent represented by the general formula (B) 1, 6 - 12 carbon atoms of an aryl group, an adamantyl group, OR2 , SR2 , Or N (R2 )2 In. ]Figure 1 [drawing] (by machine translation)
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Paragraph 0067; 0068; 0071
(2019/11/05)
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- Design, synthesis, and evaluation of A-ring-modified lamellarin N analogues as noncovalent inhibitors of the EGFR T790M/L858R mutant
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A series of A-ring-modified lamellarin N analogues were designed, synthesized, and evaluated as potential noncovalent inhibitors of the EGFR T790M/L858R mutant, a causal factor in the drug-resistant non-small cell lung cancer. Several water-soluble ammonium- or guanidinium-tethered analogues exhibited good kinase inhibitory activities. The most promising analogue, 14f, displayed an excellent inhibitory profile against the T790M/L858R mutant [IC50 (WT) = 31.8 nM; IC50 (T790M/L858R) = 8.9 nM]. The effects of A-ring-substituents on activity were rationalized by docking studies.
- Fukuda, Tsutomu,Umeki, Teppei,Tokushima, Keiji,Xiang, Gao,Yoshida, Yuki,Ishibashi, Fumito,Oku, Yusuke,Nishiya, Naoyuki,Uehara, Yoshimasa,Iwao, Masatomo
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p. 6563 - 6580
(2017/11/17)
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- Hydrogen bonds in phenylboronic acids with polyoxaalkyl substituents at ortho-position
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Phenylboronic acids with polyoxaalkyl substituents at ortho position were synthesized from the corresponding bromides. Structures in solid state, determined by single crystal X-ray diffraction, reveal the presence of inter- and intramolecular hydrogen bonds. Presence of several oxygen atoms in oxaalkyl chains enables the formation of intramolecular hydrogen bonds by B(OH)2 group with different oxygen centers which lead to the formation of bifurcated hydrogen bonds. Investigated compounds were characterized by 1H, 13C, 11B and 17O NMR spectroscopy in solution. Assignment of 1H and 13C signals was made on the basis of HSQC and HMBC spectra. 17O NMR spectra show that in acetonitrile solution hydrogen bonds with solvent molecules are predominant.
- Adamczyk-Wo?niak, Agnieszka,Cyrański, Micha? K.,Dabrowska, Aldona,Gierczyk, B?azej,Klimentowska, Paulina,Schroeder, Grzegorz,Zubrowska, Anna,Sporzyński, Andrzej
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p. 430 - 435
(2009/07/18)
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- Biphenyl derivatives substituted by an aromatic or heteroaromatic radical and pharamaceutical and cosmetic compositions containing same
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“Biphenyl derivatives substituted with an aromatic or heteroaromatic radical, and pharmaceutical and cosmetic compositions containing them” in which: Ar represents an aromatic or a heteroaromatic radical optionally substituted, in particular, with an alkyl or a carboxyl group, R2and R3represent, in particular, H or alkyl, or R2and R3, taken together, form a 5- or 6-membered ring, R4and R5represent, in particular, H or halogen, R6represents, in particular, H or lower alkyl, and the salts of the compounds of formula (I). These compounds can be used in particular in the treatment of dermatological complaints associated with a keratinization disorder, and for combating ageing of the skin.
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- Polymerization of t-butyl vinyl ether mediated by an aluminum Lewis acid-TrF system and its complex structure-tacticity correlation
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A variety of aluminum (aryloxide)s were used with triphenylmethyl fluoride (TrF) initiator for the isoselective cationic polymerization of t-butyl vinyl ether. This contribution discusses the relationship between polymer tacticity and counteranion structure, which changed according to the bulkiness, strength and chirality of the Lewis acid combined with TrF so as to make the ionic pair more interactive in the polymerization process. Newly developed organoaluminum activators, 15 and 22, showed mm = 55-57%, which is a more than 10% increase in mm compared with achiral aluminum compounds.
- Oishi,Yamamoto
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p. 1445 - 1454
(2007/10/03)
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- Benzopyranopyrrole and benzopyranopyridine alpha -1 adrenergic compounds
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The present invention relates to a compound of the formula and the pharmaceutically acceptable salts thereof wherein W is a bicyclic heterocyclic ring system. The compounds are alpha -1 adrenergic antagonists and are useful in the treatment of BPH; also disclosed are alpha -1 antagonist compositions and a method for antagonizing alpha -1 adrenoreceptors and treating BPH.
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