- INDANE DERIVATIVES FOR USE IN THE TREATMENT OF BACTERIAL INFECTION
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The invention relates to a compound which is an indane according to Formula (I), or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, L, M, ?, n, p, and q are as defined herein. The compounds are useful in the treatment of antibacterial infection either as stand alone antibiotics, or in combination with further antibiotics.
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Paragraph 0187-0189
(2020/04/09)
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- A concise approach to benzoic acid derivatives bearing an α,β-unsaturated ketone substituent: Synthesis of methyl taboganate
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A concise route to benzoic acid derivatives bearing an α,β- unsaturated ketone moiety and its application to the synthesis of the natural product methyl taboganate (1) is described. The methodology is based on the addition of a Grignard reagent to an appr
- Detsi, Anastasia,Roussis, Vassilios,Tsotinis, Andrew,Roussakis, Christos,Calogeropoulou, Theodora
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p. 3131 - 3135
(2007/10/03)
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- Chalcone derivatives and drugs containing the same
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PCT No. PCT/JP97/01652 Sec. 371 Date Nov. 17, 1998 Sec. 102(e) Date Nov. 17, 1998 PCT Filed May 16, 1997 PCT Pub. No. WO97/44306 PCT Pub. Date Nov. 27, 1997This invention relates to chalcone derivatives represented by the following formula (1): wherein A represents a phenyl group, a quinolyl group or the like, W represents a vinylene group or the like, and R1 to R5 each independently represent a carboxyl, cyano, alkyloxycarbonyl or like group, or salts of the chalcone derivatives, and also to drugs containing them as effective ingredients. These compounds have excellent cys-LT receptor antagonism, and are useful as antiallergic agents or the like.
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- Synthesis and structure-activity relationships of carboxylated chalcones: A novel series of CysLT1 (LTD4) receptor antagonists
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The synthesis and CysLT1 antagonistic activities of a new series of 2- , 3-, and 4-(2-quinolinylmethoxy)- and 3- and 4-[2-(2-quinolinyl)ethenyl]- substituted, 2'-, 3'-, 4'-, or 5'-carboxylated chalcones are described. Structure-activity relationship studies indicate a preference for the presence of a negatively charged (acidic) moiety, although in some cases nitrile or ester analogues also exhibit moderate activity. The quinoline moiety may be substituted at either the 3- or the 4-position. Replacement of this heterocycle by other aromatic groups results in compounds with comparable affinities [2-(7-chloroquinoline), 1-(1-methyl-2-benzimidazole), or 1-(2-benzothiazole)] or substantially lower activities [1-(1- ethoxyethyl)-2-benzimidazole, 2-naphthyl, or phenyl]. The quinoline and chalcone moieties may be connected by either an ethenyl or a methoxy spacer. The acidic moiety at the chalcone B ring may be attached to the 2'-, 3'-, 4'- , or 5'-position, for both the 3- and 4-substituted chalcones. There are no general patterns to specify which substitution positions gave the most potent compounds. The series contains several potent CysLT1 receptor antagonists, with K(D) values approaching the nanomolar range, as measured by the displacement of [3H]LTD4 from guinea pig lung membranes. Antagonism of LTD4-induced contraction of guinea pig ileum, the inhibition of antigen- induced contraction of guinea pig trachea in vitro, and the inhibition of LTD4-induced increase of vascular permeability in vivo are determined for chalcones with high CysLT1 receptor affinities (K(D) values below 0.1μM). 2'-Hydroxy-4-(2-quinolinylmethoxy)-5'-(5-tetrazolyl)chalcone (14, VUF 4819) showed good activity in both in vitro and in vivo assays and has been selected for further evaluation.
- Zwaagstra, Mari?l E.,Timmerman, Hendrik,Tamura, Masahiro,Tohma, Tsutomu,Wada, Yasushi,Onogi, Kazuhiro,Zhang, Ming-Qiang
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p. 1075 - 1089
(2007/10/03)
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- Alkyliron and Alkylcobalt Reagents, VIII. - Alkyl-Iron(II) Compounds as Reagents and Catalysts for the Transformation of Acyl Chlorides into Ketones
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Me2Fe, Bu2Fe, Me3FeLi, or Bu3FeLi - prepared in situ by reduction of FeCl3 to FeCl2 and subsequent alkylation with MeLi, MeMgBr, BuLi, or BuMgBr - are useful reagents for the conversion of acyl chlorides into ketones.The system (RMgX + catalytic amount of FeCl3) react like the FeII reagents with acyl chlorides to give ketones even at -65 deg C.Competition experiments with benzoyl chloride/2-methoxybenzoyl chloride show that the selectivity increases (competition constants Kk = 9.9, 10.7, 10.9, 15.0, ca. 110) in the sequence MeFeCl, Me2Fe, Me3Fe(MgBr), Me4Fe(MgBr)2, and catalytic system (MeMgBr + 2.5 mol percent FeCl3) (= 2, 3, 4, 5, and 40MeMgBr per 1 FeCl3, respectively).A new hypothesis on the nature of the active catalyst is discussed. Key Words: Organoiron compounds / Iron catalysts / Ketone synthesis
- Kauffmann, Thomas,Voss, Karl-Uwe,Neiteler, Gabriele
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p. 1453 - 1460
(2007/10/02)
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