102297-62-1Relevant articles and documents
TRICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS
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Page/Page column 75-76, (2012/09/10)
The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthama, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases. (I)
KINASE INHIBITORS
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Page/Page column 48-49, (2008/06/13)
The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula I, II, or III or a stereoisomer, tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, I II III wherein X, R1, R2, R3, R31, n, and m have the meaning defined in the claims. In particular, the present invention relates more specifically to ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.
Chalcone derivatives and drugs containing the same
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, (2008/06/13)
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.
Synthesis and structure-activity relationships of carboxylated chalcones: A novel series of CysLT1 (LTD4) receptor antagonists
Zwaagstra, Mari?l E.,Timmerman, Hendrik,Tamura, Masahiro,Tohma, Tsutomu,Wada, Yasushi,Onogi, Kazuhiro,Zhang, Ming-Qiang
, p. 1075 - 1089 (2007/10/03)
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.
Synthesis of (+/-)-Sydonic Acid
Murali, D.,Rao, G. S. Krishna
, p. 156 - 157 (2007/10/02)
A two-step synthesis of sydonic acid (1) makes use of the phenolic acetylbenzoic acid (4) obtained by the regio-selective oxidation of the known 2-acetoxy-4-methylacetophenone (3) by benzyltriethylammonium permanganate (BTAP).Similar BTAP oxidation of the
Benzopyrones. Part 22. Synthesis of New 4-Oxochromene Polycarboxylic Acids
Ellis, Gwynn P.,Hudson, Henrietta V.
, p. 3830 - 3860 (2007/10/02)
The synthesis of the following chromone dicarboxylic acids is described: 4-oxochromene-2,7-dicarboxylic acid, 6-methyl-4-oxochromene-2,8-dicarboxylic acid, 7-hydroxy-4-oxochromene-2,8-dicarboxylic acid, and 4-oxochromene-3,6-dicarboxylic acid. 4-Oxochromene-2,3-dicarboxylic acid 2-ethyl ester has been synthesized as well as 4-oxochromene-2,6,8-tricarboxylic acid.Some derivatives of these acids are described and the relative stability of carboxy groups attached to the chromen-4-one ring system is discussed.