5628-61-5Relevant articles and documents
SGK1 INHIBITORS FOR THE PROPHYLAXIS AND/OR THERAPY OF VIRAL DISEASES AND/OR CARCINOMAS
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Page/Page column 4, (2011/04/18)
The present invention relates to a compound of the formula I, Ia and Ib, and its pharmaceutically usable tautomers, salts, stereoisomers and the enantiomers, including mixtures thereof in all ratios. The present invention furthermore also relates to compounds of the formula II for the prophylaxis and/or treatment of viral diseases and/or carcinomas, in which R1, R2 each, independently of one another, denote H, CHO or acetyl, R3, R4, R5, R6, R7, R8, R9, R10, R11 each, independently of one another, denote H, A, OSO2A, Hal, NO2, OR12, N(R12)2, CN, O—COA, —[C(R12)2]nCOOR12, O—[C(R12)2]oCOOR12, SO3H, —[C(R12)2]nAr, —CO—Ar, O—[C(R12)2]nAr, —[C(R12)2]nHet, —[C(R12)2]nC≡CH, O—[C(R12)2]nC≡CH, —[C(R12)2]nCON(R12)2, —[C(R12)2]nCONR12N(R12)2, O—[C(R12)2]nCON(R12)2, O—[C(R12)2]oCONR12N(R12)2, NR12COA, NR12CON(R12)2, NR12SO2A, N(SO2A)2, COR12, S(O)mAr, SO2NR12 or S(O)mA, R3 and R4 together also denote CH═CH—CH═CH, R3 and R4, R7 and R8 or R8 and R9 together also denote alkylene having 3, 4 or 5 C atoms, in which one or two CH2 groups may be replaced by oxygen, A denotes unbranched or branched alkyl having 1-6 C atoms, in which 1-7 H atoms may be replaced by F, or cyclic alkyl having 3-7 C atoms, Ar denotes phenyl, naphthyl or biphenyl, each of which is unsubstituted or mono-, di- or trisubstituted by Hal, A, OR12, N(R12)2, NO2, CN, phenyl, CON(R12)2, NR12COA, NR12CON(R12)2, NR12SO2A, COR12, SO2N(R12)2, S(O)mA, —[C(R12)2]n—COOR12 and/or —O[C(R12)2]o—COOR12, Het denotes a mono- or bicyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms, which may be mono-, di- or trisubstituted by Hal, A; OR12, N(R12)2, NO2, CN, COOR12, CON(R12)2, NR12COA, NR12SO2A, COR12, SO2NR12, S(O)mA, ═S, ═NR12 and/or ═O (carbonyl oxygen), R12 denotes H or A, Ha1 denotes F, Cl, Br or I, m denotes O, 1 or 2, n denotes O, 1, 2 or 3, o denotes 1, 2 or 3, for the prophylaxis and/or treatment of viral diseases and/or carcinomas, and their pharmaceutically usable tautomers, salts, stereoisomers and the enantiomers, including mixtures thereof in all ratios.
CARBOXYLIC ACID COMPOUNDS AND MEDICINAL COMPOSITIONS CONTAINING THE SAME AS THE ACTIVE INGREDIENT
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Page/Page column 41, (2008/06/13)
A compound represented by formula (I) wherein the symbols in the formula are the same meanings as those in specification, salts thereof, solvates thereof, or prodrugs thereof binds to DP receptor and shows antagonistic activity for DP receptor. Thus, it is useful for prevention and/or treatment of diseases such as allergic disease (e.g., allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, urticaria, eczema, diseases accompanied by itch (e.g., atopic dermatitis and urticaria), diseases (e.g., cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (e.g., scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy ulcerative colitis, etc. Since it specifically binds to DP receptor and binds weakly to other prostaglandins receptors, they can be pharmaceuticals having little side effect.
Steroid 5α-reductase: Comparative study of mechanism of inhibition by nonsteroids ONO-3805 and LY191704
Harris, Georgianna S.,Ellsworth, Kenneth,Witzel, Bruce E.,Tolman, Richard L.
, p. 386 - 400 (2007/10/03)
Two nonsteroids, ONO-3805 and LY191704, were evaluated as inhibitors of the human and rat 5α-reductases (5αR). ONO-3805 was prepared in a 12-step convergent synthesis. This compound is a potent inhibitor of the human and rat 5αRs, with more potent inhibition seen against the rat enzymes. The inhibition patterns of this compound were best fit to an uncompetitive model which suggests binding in a ternary complex with enzyme and NADP+. Apparent K(i) values of 27, 31, 1, and 0.5 nM versus testosterone were obtained with human type 1, human type 2, rat type 1, and rat type 2 5αR, respectively. Multiple inhibition studies with ONO-3805 and NADP+ support synergistic binding of these two inhibitors with all isozymes. LY191704 was also evaluated as an inhibitor of the human and rat 5αRs. This compound is a selective, competitive inhibitor of human type 1 5αR. Poor inhibition was observed with human type 2 and rat types 1 and 2 5αR.
