摘要:
The invention relates to compound of the formula I in which the substituents are as defined in the specification; in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.
摘要:
The present invention relates to compounds of formula (I): wherein R1 is hydroxy, C1-4 alkoxy, amino, C1-4 alkyl-amino, di C1-4alkylamino, benzyloxy or C2-C7 alkanoyl, R2 is C1-4 alkyl, C1-4 alkoxy, C1-4 alkoxy C1-4alkoxy, CF3, halogen, C1-4alkylamino, di C1-4alkylamino, di C1-4 alkylamino C1-4 alkoxy or N—C1-4 alkoxy C1-4 alkyl-N—C1-4 alkylamino, N—C1-4 alkyl-piperazinyl, morpholinyl or pyrrolidinyl-C1-4 alkoxy, wherein the C1-4 alkyl radicals in R2 are optionally further substituted by C1-4 alkyl, halogen, cyano, amino, alkoxy or alkylthio, X is N or O, Y is N, O or CH, Z is N or CH, and W is N or CH, provided that (a) R1 is not hydroxy or C1-4 alkoxy when R2 is CF3, X is O, Y is CH, Z is N and W is CH, (b) R1 is not hydroxy or C1-4 alkoxy when R2 is CF3 or chloro, X is N, Y is O, Z is CH and W is CH, (c) R1 is not hydroxy when R2 is CF3, X is O, Y is N, Z is CH and W is CH and (d) X and Y are not simultaneously O, the salts thereof; their preparation, their use and pharmaceutical compositions containing them.
摘要:
Provided are substituted quinazolin-4-one compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein R1, R2, R3, R5, R6 and L are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the class I PI3K kinases.
摘要:
The invention relates to compound of the formula I in which R1 represents an optionally substituted aryl group or an optionally substituted heteroaryl group; R2 represents hydrogen or a substituent different from hydrogen; R3 represents an optionally substituted aryl group, cycloalkyl group, heteroaryl group, heterocyclyl group; X1 represents O, S, NR4, CR42; X2 represents O, S, NR4, CR42; X3 represents O, S, NR4, CR42; X4 represents O, S, NR4, CR42; R4 represents hydrogen or a substituent different from hydrogen; R5 represents hydrogen or alkyl; Y represents O or S; m represents 0, 1, 2 or 3; n represents 0, 1, 2 or 3 in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.
摘要翻译:本发明涉及式I化合物,其中R 1表示任选取代的芳基或任选取代的杂芳基; R2代表氢或不同于氢的取代基; R 3表示任选取代的芳基,环烷基,杂芳基,杂环基; X1表示O,S,NR4,CR42; X2表示O,S,NR4,CR42; X3表示O,S,NR4,CR42; X 4表示O,S,NR 4,CR 42; R4表示氢或不同于氢的取代基; R5代表氢或烷基; Y表示O或S; m表示0,1,2或3; n表示游离碱形式或酸加成盐形式的0,1,2或3; 作为其制备,用作药物和包含它的药物。
摘要:
The present invention relates to novel benzo[1,2,5]oxadiazoles and benzo[1,2,5]thiadiazoles of formula (I) wherein X is O or S, R1 is 5-(2-fluoro-ethylamino)-thiazol-2-yl, 5-(2-18F-ethylamino)-thiazol-2-yl or a group of formula (a) wherein Y is CH or N, R2 is NHCH3, NH11CH3, N(CH3)11CH3, N(CH3)2, N(11CH3)2, NH(CH2)nF, NH(CH2)n18F, N(CH3)(CH2)nF, N(CH3)—(CH2)n18F, O—(CH2)nF, O—(CH2)n18F, CONH(CH2)nF or CONH(CH2)n18F (n being in each case 2 to 4) and R3 is hydroxy, (C1-4)alkoxy, hydrogen or nitro, in free base or acid addition salt form; their preparation, their use as markers in diagnosis and compositions containing them.
摘要:
The present invention relates to compounds of formula (I): wherein R1 is hydroxy, C1-4 alkoxy, amino, C1-4 alkyl-amino, di C1-4alkylamino, benzyloxy or C2-C7 alkanoyl, R2 is C1-4 alkyl, C1-4 alkoxy, C1-4 alkoxy C1-4alkoxy, CF3, halogen, C1-4alkylamino, di C1-4alkylamino, di C1-4 alkylamino C1-4 alkoxy or N—C1-4 alkoxy C1-4 alkyl-N—C1-4 alkylamino, N—C1-4 alkyl-piperazinyl, morpholinyl or pyrrolidinyl-C1-4 alkoxy, wherein the C1-4 alkyl radicals in R2 are optionally further substituted by C1-4 alkyl, halogen, cyano, amino, alkoxy or alkylthio, X is N or O, Y is N, O or CH, Z is N or CH, and W is N or CH, provided that (a) R1 is not hydroxy or C1-4 alkoxy when R2 is CF3, X is O, Y is CH, Z is N and W is CH, (b) R1 is not hydroxy or C1-4 alkoxy when R2 is CF3 or chloro, X is N, Y is O, Z is CH and W is CH, (c) R1 is not hydroxy when R2 is CF3, X is O, Y is N, Z is CH and W is CH and (d) X and Y are not simultaneously O, the salts thereof; their preparation, their use and pharmaceutical compositions containing them.
摘要:
The present invention provides novel α-O-linked glycoconjugates such as α-O-linked glycopeptides, as well convergent methods for synthesis thereof. The general preparative approach is exemplified by the synthesis of the mucin motif commonly found on epithelial tumor cell surfaces. The present invention further provides compositions and methods of treating cancer using the α-O-linked glycoconjugates.
摘要:
The present invention provides novel &agr;-O-linked glycoconjugates such as &agr;-O-linked glycopeptides, as well convergent methods for synthesis thereof. The general preparative approach is exemplified by the synthesis of the mucin motif commonly found on epithelial tumor cell surfaces. The present invention further provides compositions and methods of treating cancer using the &agr;-O-linked glycoconjugates.