1,2,3-Triazole and tetrazole substituted piperidine or
tetrahydropyridine compounds useful as acetylcholine agonists
    2.
    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

    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

    公开(公告)号:US10336808B2

    公开(公告)日:2019-07-02

    申请号:US13482472

    申请日:2012-05-29

    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.

    MHC PEPTIDE COMPLEXES AND USES THEREOF IN INFECTIOUS DISEASES
    9.
    发明申请
    MHC PEPTIDE COMPLEXES AND USES THEREOF IN INFECTIOUS DISEASES 审中-公开
    MHC肽复合物及其在感染性疾病中的应用

    公开(公告)号:US20120264161A1

    公开(公告)日:2012-10-18

    申请号:US13482472

    申请日:2012-05-29

    IPC分类号: C07K19/00 C12N5/0783 C12Q1/02

    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。

    Fungal lypolytic and amylase enzyme composition and methods using the same
    10.
    发明授权
    Fungal lypolytic and amylase enzyme composition and methods using the same 有权
    真菌溶血酶和淀粉酶组成及使用方法

    公开(公告)号:US08012732B2

    公开(公告)日:2011-09-06

    申请号:US12552572

    申请日:2009-09-02

    摘要: A fungal wild-type lipolytic enzyme having a higher ratio of activity on polar lipids compared with triglycerides, wherein the enzyme preferably has a phospholipid:triglyceride activity ratio of at least 4. Preferably, the lipolytic enzyme according to the present invention has a glycolipid:triglyceride hydrolyzing activity ratio of at least 1.5. In one embodiment, the fungal lipolytic enzyme according to the present invention comprises an amino acid sequence as shown in SEQ ID NO: 1 or SEQ ID No. 2 or SEQ ID No. 4 or SEQ ID No. 6 or an amino acid sequence which has at least 90% identity thereto. The present invention further encompasses a nucleic acid encoding a fungal lipolytic enzyme, which nucleic acid is selected from the group consisting of: (a) a nucleic acid comprising a nucleotide shown in SEQ ID No. 3, SEQ ID No. 5 or SEQ ID No. 7; (b) a nucleic acid which is related to the nucleotide sequence of SEQ ID No. 3, SEQ ID No. 5 or SEQ ID No. 7 by the degeneration of the genetic code; and (c) nucleic acid comprising a nucleotide sequence which has at least 90% identity with the nucleotide sequence shown in SEQ ID No. 3, SEQ ID No. 5 or SEQ ID No. 7.

    摘要翻译: 与甘油三酯相比,极性脂质活性比例更高的真菌野生型脂肪分解酶,其中所述酶优选具有至少为4的磷脂:甘油三酯活性比。优选地,根据本发明的脂肪分解酶具有糖脂: 甘油三酯水解活性比至少为1.5。 在一个实施方案中,根据本发明的真菌脂肪分解酶包含如SEQ ID NO:1或SEQ ID No.2或SEQ ID No.4或SEQ ID No.6所示的氨基酸序列或氨基酸序列, 与其具有至少90%的同一性。 本发明还包括编码真菌脂肪分解酶的核酸,该核酸选自:(a)包含SEQ ID No.3,SEQ ID No.5或SEQ ID No.5所示核苷酸的核酸 第7号 (b)通过遗传密码的退化与SEQ ID No.3,SEQ ID No.5或SEQ ID No.7的核苷酸序列有关的核酸; 和(c)核酸,其包含与SEQ ID No.3,SEQ ID No.5或SEQ ID No.7所示的核苷酸序列具有至少90%同一性的核苷酸序列。