摘要:
The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.
摘要:
Novel phenylindene derivatives of the present invention are represented by the following formula: wherein the dotted lines indicate optional bonds;
R 1 is hydrogen, halogen, lower alkyl, lower alkoxy, hydroxymethyl, lower alkoxymethyl, cyano, trifluoromethyl, lower alkylthio or lower alkylsulfonyl; R 2 is halogen, lower alkyl or trlfluoromethyl; and R 3 is hydrogen, alkyl or alkenyl (straight or branched chain with C 1 -C 6 inclusive) optionally substituted with one or two hydroxy groups, any hydroxy group present being optionally esterified with an aliphatic carboxylic acid having from two to twenty-four carbon atoms inclusive, or R 3 is wherein Z ist NR 4 , 0 or S, where R 4 is H or lower alkyl, and W is 0 or S, as well as pharmaceutically acceptable acid addition salts of the compounds of Formula I.
The phenylindene derivatives of Formula I have Interesting pharmacodynamic properties indicating strong antipsychotic activity. Methods for the preparation of said derivatives are also described, as well as novel intermediates, wich are useful in the methods.
摘要翻译:本发明的新型苯基茚衍生物由下式表示:... ...其中虚线表示任选的键; R 1是氢,卤素,低级烷基,低级烷氧基,羟甲基,低级烷氧基甲基,氰基, 三氟甲基,低级烷硫基或低级烷基磺酰基; R 2是卤素,低级烷基或三氟甲基; 和R 3是任选被一个或两个羟基取代的氢,烷基或烯基(具有C 1 -C 6的直链或支链),任何存在的羟基任选地被具有二至二十二个碳原子的脂族羧酸酯化, 4个碳原子,或者R 3为... CHEM,其中Z为NR 4,O或S,其中R 4为H或低级烷基,W为O或S,以及药学上 式I化合物的可接受的酸加成盐。式I的苯基茚衍生物具有表现出强抗精神病活性的有趣的药效学性质。 还描述了制备所述衍生物的方法,以及在该方法中有用的新型中间体。
摘要:
This invention relates to the novel use of sulfonamide squaramides in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
摘要:
Cyclic diamine compounds represented by the general formula (1), acid-addition salts thereof, or hydrates of both, and medicines containing the compounds, salts or hydrates: (1) [wherein R1 and R2 are each hydrogen or methoxy, with the proviso that when R2 is hydrogen, R1 is methoxy, while when R2 is methoxy, R1 is hydrogen; A is oxygen, sulfur, CH=CH, CH=N, or NR3 (wherein R3 is hydrogen, lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, aryl, or aryl-lower alkyl); B is nitrogen, CH, or CR4 (wherein R4 is hydrogen, lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, aryl, or aryl-lower alkyl); m is a number of 1 or 2; and n is a number of 1 to 5]. The above compounds, salts and hydrates exhibit inhibitory activity against cell adhesion and are useful as drugs for allergy, asthma, rheumatic diseases, arteriosclerosis, inflammation, and so on.
摘要:
L'invention a pour objet de nouveaux dérivés de paraphénylènediamine à groupement cyclique diaza substitué par un radical cationique, les compositions tinctoriales les contenant ainsi que le procédé de teinture de fibres kératiniques à partir de ces compositions. La présente invention permet en particulier d'obtenir une coloration des fibres kératiniques chromatique, puissante, peu sélective et tenace. dans laquelle
a est compris entre 0 et 4, étant entendu que lorsque a est supérieur ou égal à 2 alors les radicaux R 1 peuvent être identiques ou différents, b est compris entre 0 et 4, étant entendu que lorsque b est supérieur ou égal à 2 alors les radicaux R 4 peuvent être identiques ou différents, c est 0 ou 1, R 1 représente un atome d'halogène; une chaîne hydrocarbonée en C 1 -C 8 , aliphatique ou alicyclique, saturée ou insaturée, un ou plusieurs atomes de carbone pouvant être remplacés par un ou plusieurs atomes d'oxygène, d'azote, de silicium, de soufre ou un groupement SO 2 ; un radical onium Z; le radical R 1 ne comportant pas de liaison peroxyde, ni de radicaux diazo, nitro ou nitroso, R 2 représente un radical onium Z.
摘要:
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
摘要:
Novel phenylindene derivatives of the present invention are represented by the following formula: wherein the dotted lines indicate optional bonds; R 1 is hydrogen, halogen, lower alkyl, lower alkoxy, hydroxymethyl, lower alkoxymethyl, cyano, trifluoromethyl, lower alkylthio or lower alkylsulfonyl; R 2 is halogen, lower alkyl or trlfluoromethyl; and R 3 is hydrogen, alkyl or alkenyl (straight or branched chain with C 1 -C 6 inclusive) optionally substituted with one or two hydroxy groups, any hydroxy group present being optionally esterified with an aliphatic carboxylic acid having from two to twenty-four carbon atoms inclusive, or R 3 is wherein Z ist NR 4 , 0 or S, where R 4 is H or lower alkyl, and W is 0 or S, as well as pharmaceutically acceptable acid addition salts of the compounds of Formula I. The phenylindene derivatives of Formula I have Interesting pharmacodynamic properties indicating strong antipsychotic activity. Methods for the preparation of said derivatives are also described, as well as novel intermediates, wich are useful in the methods.