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111 条记录 (耗时 0.139 秒)

    Vitamin D analogues having a halogen-or azido- substituted side chain
    82.
    发明授权
    Vitamin D analogues having a halogen-or azido- substituted side chain 失效
    维生素D类似物具有卤素或叠氮基取代的侧链

    公开(公告)号：US5612325A

    公开(公告)日：1997-03-18

    申请号：US367206

    申请日：1995-01-03

    申请人： Kai Hansen ,  Henrik Pedersen

    发明人： Kai Hansen ,  Henrik Pedersen

    IPC分类号： A61K31/59 ,  A61K31/593 ,  A61P3/08 ,  A61P9/12 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07C401/00

    CPC分类号： C07C401/00

    摘要： A compound of formula I ##STR1## wherein R stands for a straight or branched, saturated or unsaturated alkyl group containing from 4 to 12 carbon atoms optionally substituted with a hydroxy group, and possibly containing a ring structure, and in which at least one of the carbon atoms not bearing hydroxyl group is substituted with one or more halogen atoms or an azido group; and prodrugs of I in which one or more of the hydroxy groups are masked as groups which can be reconverted to hydroxy groups in vivo, in pure form or in mixtures. The compounds show antiinflammatory and immunomodulating effects as well as strong activity in inducing differentiation and inhibiting undesirable proliferation of certain cells. The compounds are prepared by oxidizing 1(S),3(R)-bis-(tert-butyldimethylsilyloxy)-20(S)formyl-9,10-seco-pregna-5(E),7(E),10(19)-triene, reducing the resulting product; alkylating the reduction product and then subjecting the alkylated product to triplet-sensitized photoisomerization.

    摘要翻译： PCT No.PCT / DK95 / 00305 Sec。 371日期1995年1月3日 102（e）日期1995年1月3日PCT 1993年9月23日PCT公布。 第WO94 / 07851号公报 日期1994年04月14日一种式I化合物其中R代表任选被羟基取代的含有4至12个碳原子的直链或支链饱和或不饱和烷基，并且可能含有环结构， 其中至少一个不含羟基的碳原子被一个或多个卤素原子或叠氮基取代; 和其中一个或多个羟基被掩蔽为可以在体内，纯形式或混合物中再转化为羟基的基团的I前药。 这些化合物显示出抗炎和免疫调节作用，以及在诱导分化和抑制某些细胞的不期望的增殖方面具有很强的活性。 通过氧化1（S），3（R） - 双 - （叔丁基二甲基甲硅烷氧基）-20（S）甲酰基-9,10-仲孕-5（E），7（E），10（ 19） - 三烯，还原所得产物; 烷基化还原产物，然后使烷基化产物进行三重敏感的光异构化。

    4,5,6,7-Tetrahydroisothiazolo (4,5-c) pyridine derivatives
    84.
    发明授权
    4,5,6,7-Tetrahydroisothiazolo (4,5-c) pyridine derivatives 失效
    4,5,6,7-四氢异噻唑（4,5-c）吡啶衍生物

    公开(公告)号：US4923880A

    公开(公告)日：1990-05-08

    申请号：US322632

    申请日：1989-03-13

    申请人： Povl Krogsgaard-Larsen ,  Erik Falch ,  Henrik Pedersen

    发明人： Povl Krogsgaard-Larsen ,  Erik Falch ,  Henrik Pedersen

    IPC分类号： A61K20060101 ,  A61K31/425 ,  A61K31/435 ,  A61K31/44 ,  A61P25/28 ,  C07D20060101 ,  C07D513/04

    CPC分类号： C07D513/04

    摘要： The present invention relates to novel compounds of the following formula: ##STR1## individual isomers and pharmaceutically acceptable acid addition salts thereof, whereinR.sup.1 is hydrogen, alkyl or phenyl-lower alkyl, in which the phenyl group may be substituted with halogen, lower alkyl or lower alkoxy;R.sup.2 is alkyl, alkenyl, alkynyl, branched or unbranched, with 1-6 carbon atoms inclusive, which group may be optionally substituted with fluoro, hydroxy or phenyl optionally substituted with halogen, trifluoromethyl, lower alkyl, hydroxy or lower alkoxy;R.sup.3 and R.sup.4 are the same or different, and each represents hydrogen, alkyl(1-6 C-atoms), cycloalkyl (3-6 C-atoms), phenyl optionally substituted with halogen trifluoromethyl, lower alkyl, hydroxy or lower alkoxy, or phenyl-lower alkyl, in which the phenyl group may be substituted with halogen, trifluoromethyl, lower alkyl, hydroxy or lower alkoxy.The invention moreover relates to methods for the preparation of the compounds of formula I, to novel intermediates, to pharmaceutical compositions containing same and to methods for the treatment of disorders, caused by malfunction of the acetylcholine (AcCh) or muscarinic system, by administering a non-toxic effective amount of a compound of formula I.

    1,2,3-Triazole and tetrazole substituted piperidine or tetrahydropyridine compounds useful as acetylcholine agonists
    85.
    发明授权
    1,2,3-Triazole and tetrazole substituted piperidine or tetrahydropyridine compounds useful as acetylcholine agonists 失效
    可用作乙酰胆碱激动剂的1,2,3-三唑和四唑取代的哌啶或四氢吡啶化合物

    公开(公告)号：US4866077A

    公开(公告)日：1989-09-12

    申请号：US209994

    申请日：1988-06-22

    申请人： Klaus P. Bogeso ,  Klaus G. Jensen ,  Ejner K. Moltzen ,  Henrik Pedersen

    发明人： Klaus P. Bogeso ,  Klaus G. Jensen ,  Ejner K. Moltzen ,  Henrik Pedersen

    IPC分类号： A61K31/4427 ,  A61K31/445 ,  A61P21/00 ,  A61P25/02 ,  A61P25/28 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04

    CPC分类号： C07D401/04 ,  C07D413/04 ,  C07D417/04

    摘要： The present invention relates to novel compounds of the following formula, where the dotted line designates an optional bond: ##STR1## wherein "het" designates a five membered heterocyclic ring which may include 1 or 2 double bonds and 1-4 heteroatoms selected from nitrogen, oxygen or sulphur, provided that "het" may not designate a 1,2,4- or 1,3,4-oxadiazole;R.sup.1 is selected from hydrogen, lower alkyl, optionally substituted with phenyl which may be substituted with halogen, lower alkyl, or lower alkoxy, or a group R.sup.6 --CO--NH--CH.sub.2 -- or R.sup.6 --O--CO--, wherein R.sup.6 is lower alkyl, branched or unbranched, or phenyl optionally substituted with halogen, trifluoromethyl, lower alkyl, hydroxy, lower alkoxy, or lower acyloxy;R.sup.2 and R.sup.3 are the same or different, each representing hydrogen, lower alkyl, cycloalkyl (3-6 C-atoms), lower alkenyl, lower alkadienyl, lower alkynyl, optionally substituted with hydroxy, halogen or phenyl, in which the phenyl group may be substituted with halogen, trifluoromethyl, lower alkyl, hydroxy or lower alkoxy; R.sup.2 and R.sup.3 may further, respectively, be selected from trifluoromethyl or phenyl optionally substituted with halogen, trifluoromethyl, lower alkyl, hydroxy, lower alkoxy or lower acyloxy, or R.sup.2 and R.sup.3 may, respectively, be a group OR.sup.7 or SR.sup.7 wherein R.sup.7 is defined as R.sup.2 or R.sup.3, andif "het" includes 2 or more carbon atoms, R.sup.4 and R.sup.5 are the same or different, and each is defined as R.sup.2 or R.sup.3, and if "het" includes only one carbon atom, there is only one substituent, R.sup.4, on the heterocyclic ring, and R.sup.4 is defined as R.sup.2 or R.sup.3,as well as individual stereo isomers and pharmaceutically acceptable acid addition salts thereof.The invention moreover relates to methods for the preparation of the compounds of formula I, to novel intermediates, to pharmaceutical compositions containing same and to methods for the treatment of disorders, caused by malfunction of the acetylcholine (AcCh) or muscarinic system, by administering a non-toxic effective amount of a compound of formula I.

    MHC peptide complexes and uses thereof in infectious diseases
    89.
    发明授权
    MHC peptide complexes and uses thereof in infectious diseases 有权
    MHC肽复合物及其在感染性疾病中的应用

    公开(公告)号：US08268964B2

    公开(公告)日：2012-09-18

    申请号：US12619039

    申请日：2009-11-16

    申请人： Jørgen Schøller ,  Henrik Pedersen ,  Liselotte Brix

    发明人： Jørgen Schøller ,  Henrik Pedersen ,  Liselotte Brix

    IPC分类号： C07K1/00 ,  C07K14/00 ,  C07K17/00 ,  C07K16/00 ,  A61K38/16

    CPC分类号： C07K14/70539 ,  A61K38/00 ,  A61K47/61 ,  A61K47/6425 ,  A61K49/1896 ,  G01N33/56905 ,  G01N33/56911 ,  G01N33/56972 ,  G01N33/56977 ,  G01N33/574 ,  G01N2333/70539 ,  G01N2800/24 ,  Y02A50/401 ,  Y02A50/55 ,  Y02A50/57 ,  Y02A50/58

    摘要： Novel compounds carrying ligands capable of binding to counter receptors on relevant target cells are disclosed. The compounds possess a number of advantageous features, rendering them very suitable for a wide range of applications, including use as detection systems, detection of relevant target cells as well as a number of other methods. In particular, novel MHC complexes comprising one or more MHC molecules are disclosed. The affinity and specificity of the MHC-peptide complexes are surprisingly high. The possibility of presenting to the target cells a plurality of MHC-peptide complexes makes the MHC complexes according to the present invention an extremely powerful tool e.g. in the field of therapy and diagnosis. The invention generally relates to the field of therapy, including therapeutic methods and therapeutic compositions. Also comprised by the present invention is the sample-mounted use of MHC complexes and MHC multimers.

    摘要翻译： 公开了携带能够结合相关靶细胞上的对受体的配体的新型化合物。 这些化合物具有许多有利的特征，使得它们非常适用于广泛的应用，包括用作检测系统，相关靶细胞的检测以及许多其它方法。 特别地，公开了包含一种或多种MHC分子的新型MHC复合物。 MHC-肽复合物的亲和性和特异性惊人地高。 向靶细胞呈递多个MHC-肽复合物的可能性使得根据本发明的MHC复合物成为非常强大的工具，例如， 在治疗和诊断领域。 本发明一般涉及治疗领域，包括治疗方法和治疗组合物。 本发明还包括MHC复合物和MHC多聚体的样品安装用途。