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48 条记录 (耗时 0.039 秒)

    Peptides with an insulin-like action
    41.
    发明授权
    Peptides with an insulin-like action 失效
    具有胰岛素样作用的肽

    公开(公告)号：US5622934A

    公开(公告)日：1997-04-22

    申请号：US247394

    申请日：1994-05-23

    申请人： Wendelin Frick ,  G unter M uller ,  Stefan M ullner ,  Gerhard Breipohl

    发明人： Wendelin Frick ,  G unter M uller ,  Stefan M ullner ,  Gerhard Breipohl

    IPC分类号： A61K38/28 ,  A61K38/00 ,  A61P3/08 ,  A61P3/10 ,  C07K5/06 ,  C07K5/065 ,  C07K5/08 ,  C07K5/087 ,  C07K5/093 ,  C07K5/097 ,  C07K7/06 ,  C07K7/08 ,  C07K9/00 ,  A61K38/06

    CPC分类号： C07K9/001 ,  C07K5/0606 ,  C07K5/06078 ,  C07K5/0812 ,  C07K5/0819 ,  C07K5/0821 ,  C07K5/0827 ,  Y02P20/55

    摘要： Peptides with an insulin-like action, of formula I: ##STR1## in which G is a hydrogen atom, an amino add residue, or a monosubstituted or polysubstituted amino acid; D is an amino acid residue, a phosphoamino acid residue, a monosaccharide residue, or a covalent bond; E is --NH--(CH.sub.2).sub.n --NR.sup.5.sub.2, a glycerol residue, or --NH--(CH.sub.2).sub.p --R.sup.6 --R.sup.7 ; R.sup.1 is (C.sub.1 -C.sub.4)-alkyl or .dbd.O; R.sup.2 is a sulfhydryl protecting group, (C.sub.1 -C.sub.3)-alkyl, or a hydrogen atom; R.sup.3 and R.sup.4, independently of one another, are a hydrogen atom or methyl; R.sup.5, each being identical or different, is a hydrogen atom, 1 to 6 monosaccharide residues, or 1 to 6 monosubstituted or polysubstituted monosaccharide residues; R.sup.6 is O PO.sub.4 H, PO.sub.2 H, NHCOO, S or OCOO; R.sup.7 is a hydrogen atom, 1 to 6 monosaccharide residues, or 1 to 6 monosubstituted or polysubstituted monosaccharide residues; w is an integer 1 or 2; their preparation and use for treatment of diabetes mellitus or insulin-independent diabetes.

    摘要翻译： 具有胰岛素样作用的式I的肽：其中G是氢原子，氨基加成残基或单取代或多取代的氨基酸; D是氨基酸残基，磷酸氨基酸残基，单糖残基或共价键; E是-NH-（CH 2）n -NR 52，甘油残基或-NH-（CH 2）p -R 6 -R 7; R1是（C1-C4） - 烷基或= O; R2是巯基保护基，（C1-C3） - 烷基或氢原子; R 3和R 4彼此独立地是氢原子或甲基; R5各自相同或不同，是氢原子，1至6个单糖残基或1至6个单取代或多取代的单糖残基; R6是O PO4H，PO2H，NHCOO，S或OCOO; R7是氢原子，1至6个单糖残基或1至6个单取代或多取代的单糖残基; w是整数1或2; 它们用于治疗糖尿病或胰岛素不依赖性糖尿病的制备和用途。

    Polyamide nucleic acid derivatives and agents, and processes for preparing them
    43.
    发明授权
    Polyamide nucleic acid derivatives and agents, and processes for preparing them 失效
    聚酰胺核酸衍生物和试剂，及其制备方法

    公开(公告)号：US07897346B2

    公开(公告)日：2011-03-01

    申请号：US12474532

    申请日：2009-05-29

    申请人： Eugen Uhlmann ,  Gerhard Breipohl ,  David William Will

    发明人： Eugen Uhlmann ,  Gerhard Breipohl ,  David William Will

    IPC分类号： C12Q1/68 ,  C07H19/04 ,  C07H21/02

    CPC分类号： C07K14/003 ,  A61K38/00 ,  Y10T436/143333

    摘要： The present invention relates to PNA derivatives which carry, at the C terminus, or at both the C and N termini of the PNA backbone, one or more phosphoryl radicals. The phosphoryl radicals carry, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the above-mentioned PNA derivatives and to their use as pharmaceuticals or diagnostic agents.

    摘要翻译： 本发明涉及在C末端或在PNA主链的C和N末端携带一个或多个磷酰基的PNA衍生物。 磷酰基在适当的情况下携带一个或多个标记基团，用于交联的基团，促进细胞内摄取的基团，或增加PNA衍生物对核酸的结合亲和力的基团。 本发明还涉及制备上述PNA衍生物的方法及其作为药物或诊断剂的用途。

    Polyamide-oligonucleotide derivatives, their preparation and use
    44.
    发明授权
    Polyamide-oligonucleotide derivatives, their preparation and use 失效
    聚酰胺 - 寡核苷酸衍生物，其制备和用途

    公开(公告)号：US06919441B2

    公开(公告)日：2005-07-19

    申请号：US09793146

    申请日：2001-02-27

    申请人： Eugen Uhlmann ,  Gerhard Breipohl

    发明人： Eugen Uhlmann ,  Gerhard Breipohl

    IPC分类号： A61K47/48 ,  C07H21/00 ,  C07K14/00 ,  C07H21/02 ,  C07H21/04

    CPC分类号： C07H21/00 ,  A61K47/59 ,  A61K47/595 ,  A61K47/60 ,  A61K47/605 ,  C07K14/003

    摘要： The invention provides polyamide-oligonucleotide derivatives of the formula: F[(DNA-Li)q(PNA-Li)r(DNA-Li)s(PNA)t]xF′. In the formula, q, r, s, and t are, independently of one another, zero or 1, where the total of two or more adjacent q, r, s, and t is greater than or equal to 2; and x is 1 to 20. In the formula, DNA is a nucleic acid such as DNA or RNA or a known derivative thereof. Li is a covalent linkage between DNA and PNA, where the covalent linkage comprises a bond or an organic radical with at least one atom from the series consisting of C, N, O, or S. PNA is a polyamide structure which contains at least one nucleotide base that is different from thymine. F and F′ are end groups and/or are linked together by a covalent bond. The invention also provides physiologically tolerated salts of the above formula. The invention further provides a process for preparation of the polyamide-oligonucleotide derivatives of the invention as well as their use as pharmaceuticals, as gene probes, and as primers.

    摘要翻译： 本发明提供下式的聚酰胺 - 寡核苷酸衍生物：<？in-line-formula description =“In-line Formulas”end =“lead”→F [（DNA-Li） -Li）R（N-L）（PNA）t X'F'。<βin -line-formula description =“在线公式”end =“tail”？>在公式中，q，r，s和t彼此独立地为零或1，其中两个或更多相邻的 q，r，s和t大于或等于2; 并且x为1至20.在该式中，DNA是DNA或RNA等核酸或其已知衍生物。 Li是DNA和PNA之间的共价连接，其中共价连接包含与C，N，O或S组成的系列中的至少一个原子的键或有机基团.PNA是含有至少一个 与胸腺嘧啶不同的核苷酸碱基。 F和F'是端基和/或通过共价键连接在一起。 本发明还提供了上述式的生理上耐受的盐。 本发明还提供了制备本发明的聚酰胺 - 寡核苷酸衍生物的方法以及它们作为药物，作为基因探针和引物的用途。

    1,4,5,6-tetrahydropyrimidine derivative as a vitronectin inhibitor
    45.
    发明授权
    1,4,5,6-tetrahydropyrimidine derivative as a vitronectin inhibitor 有权
    1,4,5,6-四氢嘧啶衍生物作为玻连蛋白抑制剂

    公开(公告)号：US06900318B1

    公开(公告)日：2005-05-31

    申请号：US10031121

    申请日：2000-07-08

    申请人： Gerhard Breipohl ,  Anuschirwam Peyman ,  Theodor Wollmann

    发明人： Gerhard Breipohl ,  Anuschirwam Peyman ,  Theodor Wollmann

    IPC分类号： A61K31/505 ,  A61P1/02 ,  A61P3/10 ,  A61P3/14 ,  A61P5/24 ,  A61P9/00 ,  A61P9/10 ,  A61P13/12 ,  A61P17/06 ,  A61P19/00 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P29/00 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07D239/16 ,  C07D239/42

    CPC分类号： C07D239/42 ,  C07D239/16

    摘要： The present invention relates to ethyl (2S)-2-(naphthalene-1-sulfonylamino)-3-(4-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)ethyl)benzoylamino)propionate hemifumarate of formula (I), and to a process for its preparation comprising reacting 4-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)ethyl)benzoic acid or a derivative thereof and ethyl (2S)-3-amino-2-(naphthalene-1-sulfonylamino)propionate. The compound of formula (I) is a valuable pharmaceutical which can be used, for example, in the treatment or prophylaxis of diseases which can be influenced by inhibiting the vitronectin receptor, in particular of bone diseases such as osteoporosis. The invention furthermore relates to chemical intermediates useful for the preparation of the compound of formula (I).

    摘要翻译： 本发明涉及（2S）-2-（萘-1-磺酰基氨基）-3-（4-（2-（1,4,5,6-四氢嘧啶-2-基氨基甲酰基）乙基）苯甲酰氨基）丙酸乙酯半富马酸乙酯 （I）化合物及其制备方法，包括使4-（2-（1,4,5,6-四氢嘧啶-2-基氨基甲酰基）乙基）苯甲酸或其衍生物与（2S）-3- 氨基-2-（萘-1-磺酰基氨基）丙酸酯。 式（I）化合物是一种有价值的药物，其可用于例如治疗或预防可通过抑制玻连蛋白受体，特别是骨疾病例如骨质疏松症而受影响的疾病。 本发明还涉及可用于制备式（I）化合物的化学中间体。