摘要:
The present invention is related to substituted amine derivatives I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such piperazine derivatives of carbazole. Said substituted amine derivatives are efficient modulators, in particular inhibitors, of the Bax function and/or activation. The present invention is furthermore related to novel substituted amine derivatives as well as methods of their preparation. A 1 and A 2 are selected independently from each other from the group consisting of -C(O)- and -SO 2 -. R a , R b , R 0 , R 1 and R 2 are as the application.
摘要翻译:本发明涉及特别用作药物活性化合物的取代胺衍生物I以及含有咔唑类哌嗪衍生物的药物制剂。 所述取代的胺衍生物是Bax功能和/或活化的有效调节剂,特别是抑制剂。 本发明还涉及新型取代的胺衍生物及其制备方法。 A 1和A 2彼此独立地选自-C(O) - 和-SO 2 - 。 R a,R b,R o,R 1和R 2是应用。
摘要:
Novel tripeptide compounds having excellent HIV protease inhibitory activites and represented by general formula (I), pharmacologically acceptable salts thereof, and anti-AIDS drugs containing the same as the active ingredient. An example of the compounds is (R)-N-(2-methylbenzyl)-3-{(2S, 3S)-3-[N-(2-chromonecarbonyl)-L-asparaginyl]amino-2-hydroxy-4-phenylbutanoyl}-5, 5-dimethyl-1, 3-thiazolidine-4-carboxamide.
摘要:
Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
摘要:
An organic compound is provided which contains at least one nitric oxide donor group and at least one group being, or being adapted to be converted in vivo to a free sulfhydryl group. A preferred compound contains at least one sulfhydryl group, either in the reduced -SH form or in the oxidized -S-S-disulfide form.
摘要:
N-Acyl Pyrrozidines and N-Acyl Thiazolidines of the general formula:
wherein, Z represents a methylene group or a sulfur atom, their non-toxic salts or hydrates. The compounds possess an inhibitory activity on propyl endopeptidase, and therefore are usefull for the prevention and/or treatment of amnesia.
摘要:
An arylalkanoylamine derivative represented by general formula (I), excellent in a prolyl endopeptidase inhibitory action and resistances to hypoxia and amnesia; and a drug for improving mneme, cerebral circulation and cerebral metabolism, containing the same as the active ingredient, wherein A represents indanyl, indenyl, 1,2,3,4-tetrahydronaphthalenyl or benzofuranyl; m is an integer of 0 to 5; Z represents hydroxymethyl, formyl, nitrile, hydroxyiminomethyl, semicarbazonomethyl or dialkoxymethyl and X and Y may be the same or different from each other and each represents methylene or sulfur, provided that the case where A represents indanyl, indenyl or 1,2,3,4-tetrahydronaphthalenyl, X and Y represent both methylene, and Z represents hydroxymethyl or formyl is excluded.
摘要:
Nitrates organiques, leurs procédés de préparation ainsi que leur utilisation dans le traitement de maladies vasculaires et notamment dans le traitement de l'angor. Lesdits nitrates répondent à la formule I suivante : R-CO-(A) n -Y-B dans laquelle : R représente notamment un reste soufré et un résidu d'aminoacide soufré ; A représente notamment un groupe CH₂ ou un acide aminé substitué ; n est égal à 0 ou 1 ou supérieur à 1 ; Y représente un atome d'oxygène ou un groupe NH et B représente notamment un reste dianhydro 1,4:3,6 hexitol mono-nitrate, un reste itol nitrate, un reste d'inositol. Lesdits nitrates organiques sont préparés en faisant réagir :
I. soit un thioacide de type R-COOH, dans lequel R a la même signification que ci-dessus avec un dérivé de formule II : (A) n -Y-B, dans laquelle A, Y, B et n ont la même signification que ci-dessus, II. soit un dérivé de formule III : R-CO-(A) n , dans laquelle R, A et n ont la même signification que ci-dessus, avec un dérivé de formule Y-B, dans laquelle Y et B ont la même signification que ci-dessus, dans un solvant approprié et dans des conditions non épimérisantes.
摘要翻译:有机硝酸盐,处理它们的制备以及它们在血管疾病的治疗和治疗心绞痛特别喜欢。 所述硝酸盐对应于下列式I:R-CO-(A)NYB(I>其中:-R darstellt爱尤其是含硫残渣和含硫的氨基酸残基; A darstellt爱尤其是CH 2基团或一个substituiertem 氨基酸; n是等于0或1或大于1; Y darstellt到氧原子或NH基团和B在darstellt尤其是1,4:3,6-双脱水己糖醇单硝酸酯,硝酸-itol残余物,和肌醇残基 一,无论是对R-COOH II型,其中R具有与上述相同的含义,与下式的衍生物的硫代酸:(A)NYB,其中A,Y,所述有机硝酸酯是由反应制备 ,B和n具有与上述相同的含义,或式II的衍生物III:R-CO-(O)N,其中R,A和n具有与上述相同的含义,与式YB的衍生物, 其中Y和B具有相同的含义如上,在合适的溶剂和nonepimerising条件下进行。
摘要:
Cyclic amino-thioacetal amides of formula I wherein X is O, S, p is 1 or 2, R and R₁ are optionally esterified hydrogen or carboxy, A is a single bond, methylene or ethylene, m is zero or 1, n is an integer 1 to 7 and y is a imidazole or β-pyridylmethyl residue as well as intermediates for preparation thereof, Compounds I have valuable therapeutic properties.