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    Compounds 148
    1.
    发明授权
    Compounds 148 失效
    化合物148

    公开(公告)号：US08119673B2

    公开(公告)日：2012-02-21

    申请号：US12489458

    申请日：2009-06-23

    Applicant: Jonas Brånalt ,  David Gustafsson ,  Ingemar Nilsson ,  Magnus Polla

    Inventor： Jonas Brånalt ,  David Gustafsson ,  Ingemar Nilsson ,  Magnus Polla

    IPC: A61K31/41 ,  C07D257/04

    CPC classification number: C07D403/12 ,  C07D405/14 ,  C07D413/12

    Abstract: This invention relates to novel pharmaceutically useful compounds of formula (I), in particular compounds that are competitive inhibitors of trypsin-like serine proteases, especially thrombin, their use as medicaments, pharmaceutical compositions containing them and synthetic routes to their production.

    Abstract translation: 本发明涉及新的药学上有用的式（I）化合物，特别是作为胰蛋白酶样丝氨酸蛋白酶，特别是凝血酶的竞争性抑制剂，它们作为药物的药物，含有它们的药物组合物和其生产合成途径的化合物。

    Thrombin Inhibiting 2-Oxo-1,2,5,6-Tetrahydropyridine Derivatives
    2.
    发明申请
    Thrombin Inhibiting 2-Oxo-1,2,5,6-Tetrahydropyridine Derivatives 审中-公开
    凝血酶抑制2-氧代-1,2,5,6-四氢吡啶衍生物

    公开(公告)号：US20080207695A1

    公开(公告)日：2008-08-28

    申请号：US11917515

    申请日：2006-06-14

    Applicant: Ingemar Nilsson ,  Magnus Polla

    Inventor： Ingemar Nilsson ,  Magnus Polla

    IPC: A61K31/444 ,  C07D213/73 ,  A61K31/44 ,  A61P7/02 ,  C07D401/12

    CPC classification number: C07D401/14 ,  C07D213/73 ,  C07D213/75

    Abstract: There is provided a compound of formula (I) wherein R1, R2a, R2b, R3a, R3b, R4, R5a, R5b, R6 to R8, A and G have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is beneficial (e.g. conditions, such as thrombo-embolisms, where inhibition of thrombin is required or desired, and/or conditions where anticoagulant therapy is indicated).

    Abstract translation: 提供了式（I）的化合物，其中R 1，R 2，R 2，R 2b，R 3a， R 3b，R 4，R 5a，R 5b，R 6，R 6， A和G具有在说明书中给出的含义，哪些化合物可用作或用作胰蛋白酶样蛋白酶的竞争性抑制剂诸如凝血酶的前药，因此在 特别地，在治疗凝血酶抑制有益的条件（例如需要或期望抑制凝血酶的条件，例如血栓栓塞，和/或指示抗凝治疗的条件）。

    Chemical compounds
    3.
    发明授权
    Chemical compounds 失效
    化合物

    公开(公告)号：US07375121B2

    公开(公告)日：2008-05-20

    申请号：US10489530

    申请日：2002-09-23

    Applicant: Magnus Polla

    Inventor： Magnus Polla

    IPC: A61K31/44 ,  C07D211/72

    CPC classification number: C07F9/6539 ,  C07F9/5765 ,  C07F9/58

    Abstract: The present invention concerns compounds of formula (I), and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases where inhibition of carboxypeptidase U is beneficial. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.

    Abstract translation: 本发明涉及式（I）化合物及其药学上可接受的盐或溶剂化物，或这些盐的溶剂合物，该化合物抑制羧肽酶U，因此可用于预防和治疗羧肽酶U的抑制有益的疾病。 在另外的方面，本发明涉及用于治疗的本发明化合物; 制备这些新化合物的方法; 含有至少一种本发明化合物或其药学上可接受的盐或溶剂合物作为活性成分的药物组合物; 以及活性化合物在制造上述用于医疗用途的药物中的用途。

    Thrombin Inhibiting 2,4-Dioxo-3,4-Dihydropyrimidine Derivatives
    6.
    发明申请
    Thrombin Inhibiting 2,4-Dioxo-3,4-Dihydropyrimidine Derivatives 审中-公开
    凝血酶抑制2,4-二氧代-3,4-二氢嘧啶衍生物

    公开(公告)号：US20080214589A1

    公开(公告)日：2008-09-04

    申请号：US11917512

    申请日：2006-06-14

    Applicant: Ingemar Nilsson ,  Magnus Polla

    Inventor： Ingemar Nilsson ,  Magnus Polla

    IPC: A61K31/506 ,  C07D407/14

    CPC classification number: C07D239/545 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14

    Abstract: There is provided a compound of formula I wherein R1 to R5, A, G, L and X have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is beneficial (e.g. conditions, such as thrombo-embolisms, where inhibition of thrombin is required or desired, and/or conditions where anticoagulant therapy is indicated).

    Abstract translation: 提供式I化合物，其中R 1至R 5，A，G，L和X具有说明书中给出的含义，该化合物可用作或或 可用作胰蛋白酶样蛋白酶的竞争性抑制剂如凝血酶的前药，因此特别是在治疗凝血酶抑制是有益的条件（例如血栓栓塞，其中凝血酶抑制为 需要或期望，和/或表示抗凝治疗的条件）。

    2,5-disubstituted 3-mercaptopentanoic acid
    7.
    发明授权
    2,5-disubstituted 3-mercaptopentanoic acid 失效
    2,5-二取代的3-巯基戊酸

    公开(公告)号：US07572817B2

    公开(公告)日：2009-08-11

    申请号：US10517713

    申请日：2003-06-10

    Applicant: Magnus Polla

    Inventor： Magnus Polla

    IPC: A61K31/44 ,  A61K31/425 ,  A61K31/38 ,  A61K31/36 ,  C07D217/00 ,  C07D213/72 ,  C07D207/00 ,  C07D487/02 ,  C07D277/00 ,  C07D239/00 ,  C07D241/04 ,  C07D223/00

    CPC classification number: C07D211/34 ,  C07D213/73 ,  C07D277/40 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06

    Abstract: The present invention concerns compounds of formula (I), and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases where inhibition of carboxypeptidase U is beneficial. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.

    Abstract translation: 本发明涉及式（I）化合物及其药学上可接受的盐或溶剂化物，或这些盐的溶剂合物，该化合物抑制羧肽酶U，因此可用于预防和治疗羧肽酶U的抑制有益的疾病。 在另外的方面，本发明涉及用于治疗的本发明化合物; 制备这些新化合物的方法; 含有至少一种本发明化合物或其药学上可接受的盐或溶剂合物作为活性成分的药物组合物; 以及活性化合物在制造上述用于医疗用途的药物中的用途。

    Phosphinyloxy, oxime and carboxylic acid derivatives which are useful as carboxypeptidase U inhibitors
    8.
    发明申请
    Phosphinyloxy, oxime and carboxylic acid derivatives which are useful as carboxypeptidase U inhibitors 失效
    可用作羧肽酶U抑制剂的磷酰氧基，肟和羧酸衍生物

    公开(公告)号：US20060079484A1

    公开(公告)日：2006-04-13

    申请号：US11293060

    申请日：2005-12-02

    Applicant: Marcel Linschoten ,  Magnus Polla

    Inventor： Marcel Linschoten ,  Magnus Polla

    IPC: C07F5/02 ,  A61K31/69 ,  A61K31/675

    CPC classification number: A61K38/57 ,  A61K2300/00

    Abstract: The present invention relates to compounds of Formula I, and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases associated with carboxypeptidase U. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.

    Abstract translation: 本发明涉及式I化合物及其药学上可接受的盐或溶剂合物，或这些盐的溶剂化物，该化合物抑制羧肽酶U，因此可用于预防和治疗与羧肽酶U相关的疾病。在另外的方面， 本发明涉及用于治疗的本发明化合物; 制备这些新化合物的方法; 含有至少一种本发明化合物或其药学上可接受的盐或溶剂合物作为活性成分的药物组合物; 以及活性化合物在制造上述用于医疗用途的药物中的用途。

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