摘要:
The present invention relates to compounds of the formula I A—B—D—E—F—G (I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.
摘要:
Novel oligonucleotide analogs of the formula [I] are described, ##STR1## in which A, B, D, G, L, P, Q, Q', R.sup.5, R.sup.6, X, Y, Z and n are as defined in the description, which have useful physical, biological and pharmacological properties, as well as a process for their preparation. Their application relates to use as inhibitors of gene expression (antisense oligonucleotides, ribozymes, sense oligonucleotides and triplex-forming oligonucleotides), as probes for the detection of nucleic acids and as auxiliaries in molecular biology.
摘要:
Oligonucleotides of the formula:5'-(CAP)-(Oligo)-(CAP)-3'are disclosed where (oligo) is a nucleotide sequence of from 10 to 40 nucleotides in length, and CAP is G.sub.m, where m is an integer of from zero to ten, the two CAP's which are present in the molecule can be defined independently of each other and must be different in the case where m is zero at the 5' or 3' end and the end of the oligo sequence is other than guanine. The oligonucleotides can be synthesized chemically. The oligonucleotides are used to diagnose or treat cancer, restenosis, a disease caused by a virus, a disease affected by integrins or cell-cell adhesion receptor or a disease triggered by diffusible factors.
摘要:
The invention relates to compounds of the formula I ##STR1## where R.sup.1 is H, alkyl, acyl, aryl, or a phosphate residue; R.sup.2 is H, OH, alkoxy, NH.sub.2, or halogen; B is a base customary in nucleotide chemistry; a is O or CH.sub.2 ; n is an integer from 1 to 100; W=O, S or Se; V=O, S, or NH; Y=O, S, NH, or CH.sub.2 ; Y'=O, S, NH, or alkylene; X=OH or SH; U=OH, SH, SeH, alkyl, alkoxy, aryl, aryloxy, or amine, and Z=OH, SH, SeH, an optionally substituted radical from the group comprising alkyl, aryl, heteroaryl, alkoxy, or amino, or a group which favors intracellular uptake or serves as the label of a DNA probe or attacks the target nucleic acid during hybridization, where if Z=OH, SH, CH.sub.3, or OC.sub.2 H.sub.5, at least one of the groups X, Y, Y', V, or W is not OH or O or R.sup.1 is not H; a process for their preparation and their use as inhibitors of gene expression, as probes for detecting nucleic acids and as aids in molecular biology.
摘要翻译:本发明涉及式Ⅰ化合物,其中R1是H,烷基,酰基,芳基或磷酸酯残基; R2是H,OH,烷氧基,NH2或卤素; B是核苷酸化学中常规的基础; a是O或CH2; n为1〜100的整数, W = O,S或Se; V = O,S或NH; Y = O,S,NH或CH 2; Y'= O,S,NH或亚烷基; X = OH或SH; U = OH,SH,SeH,烷基,烷氧基,芳基,芳氧基或胺,Z = OH,SH,SeH,任选取代的基团,其包含烷基,芳基,杂芳基,烷氧基或氨基, 其有利于细胞内吸收或用作DNA探针的标记或在杂交期间攻击靶核酸,其中如果Z = OH,SH,CH 3或OC 2 H 5,X,Y,Y',V, 或W不是OH或O或R 1不是H; 其制备方法及其作为基因表达抑制剂的用途,作为检测核酸的探针和分子生物学的辅助工具。
摘要:
Novel oligonucleotide analogs of the formulae I and II ##STR1## in which A, B, D, R.sup.1, R.sup.2, T, U, V, W, X, Y, Z, a, b, m, m', n and n' have the meanings stated in the description, with valuable physical, biological and pharmacological properties, and a process for the preparation thereof are described. Application thereof relates to the use as inhibitors of gene expression (antisense oligonucleotides, ribozymes, sense oligonucleotides and triplex forming oligonucleotides), as probes for detecting nucleic acids and as aids in molecular biology.
摘要:
The present invention relates to a compound of the formula ##STR1## in which A, Q, R.sup.2, R.sup.3 and R.sup.4, and also the corresponding, asterisked radicals, are defined as indicated in the description, to a process for their preparation, and also to their use for inhibiting retroviral proteases.
摘要:
A process for the preparation of .alpha.- or .alpha.,.alpha.'-substituted derivatives of the bis(aminomethyl)phosphinic acid of the formula I and their acid or basic salts, ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 are defined as in the description, wherein a bis(aminomethyl)phosphinate is converted into the corresponding bisimine, which is alkylated by R.sup.2 and R.sup.3 in the .alpha.- and/or .alpha.,.alpha.'-position after reaction with a base, and is converted into a compound of the formula I by subsequent treatment with an acid.