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公开(公告)号：US20110130432A1
公开(公告)日：2011-06-02
申请号：US13000637
申请日：2009-06-22
Applicant: Jonas Branalt , David Gustafsson , Ingemar Nilsson , Magnus Polla
Inventor： Jonas Branalt , David Gustafsson , Ingemar Nilsson , Magnus Polla
IPC: A61K31/422 , C07D257/04 , C07D261/02 , A61K31/41 , A61P7/02
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. Formula (I)
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。 式（I）
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公开(公告)号：US20090318517A1
公开(公告)日：2009-12-24
申请号：US12489458
申请日：2009-06-23
Applicant: Jonas Branalt , David Gustafsson , Ingemar Nilsson , Magnus Polla
Inventor： Jonas Branalt , David Gustafsson , Ingemar Nilsson , Magnus Polla
IPC: A61K31/4155 , C07D403/12 , A61K31/41 , A61P7/00 , A61P7/02
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: 本发明涉及新颖的药学上有用的式（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。
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Patent Agency Ranking
13.发明授权公开(公告)号：US07423012B2
公开(公告)日：2008-09-09
申请号：US11293060
申请日：2005-12-02
Applicant: Marcel Linschoten , Magnus Polla
Inventor： Marcel Linschoten , Magnus Polla
IPC: A61K31/44 , A61P7/02 , C07D211/08 , C07D211/20 , C07D213/72
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.
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公开(公告)号：US20080139607A1
公开(公告)日：2008-06-12
申请号：US11930232
申请日：2007-10-31
Applicant: Fredrik Almqvist , Erik Chorell , Pralay Das , Hans Emtenas , Ola Fjellstrom , Mickael Mogemark , Magnus Polla , Veronica Aberg
Inventor： Fredrik Almqvist , Erik Chorell , Pralay Das , Hans Emtenas , Ola Fjellstrom , Mickael Mogemark , Magnus Polla , Veronica Aberg
IPC: A61K31/4365 , C07D471/04 , C07D211/76 , A61K31/4412 , A61P9/10 , A61P9/00 , A61P11/00 , A61P35/00
CPC classification number: C07D513/04 , C07D213/64
Abstract: The present invention relates to new compounds of formula (I), (II), or (III) wherein R1, R2, R3, R4, R5 and W are as defined herein, and methods of using the compounds to inhibit PAI-1 and to treat PAI-1 related disorders.
Abstract translation: 本发明涉及新的式（I），（II）或（III）化合物，其中R 1，R 2，R 3， R 4，R 5和W如本文所定义，以及使用该化合物抑制PAI-1并治疗PAI-1相关疾病的方法。
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15.发明授权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：US07354895B1
公开(公告)日：2008-04-08
申请号：US09600660
申请日：2000-05-03
Applicant: Marcel Linschoten , Magnus Polla
Inventor： Marcel Linschoten , Magnus Polla
IPC: C07D211/08 , C07D211/20 , C07D213/72 , A61K31/44 , A61K7/02
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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16.发明申请Use of Cyclic Anabaenopeptin-type Peptides for the Treatment of a Condition Wherein Inhibition of Carboxypeptidase U is Beneficial, Novel Anabaenopeptin Derivatives and Intermediates Thereof 审中-公开循环阿那贝品肽型肽用于治疗羧肽酶U的抑制作用的新方法，新型的阿那巴多肽衍生物及其中间体公开(公告)号：US20080039376A1
公开(公告)日：2008-02-14
申请号：US10578022
申请日：2004-10-28
Applicant: Petter Bjorquist , Malcolm Buchanan , Marc Campitelli , Anthony Carroll , Edward Hyde , Juliette Neve , Ron Quinn , Magnus Polla
Inventor： Petter Bjorquist , Malcolm Buchanan , Marc Campitelli , Anthony Carroll , Edward Hyde , Juliette Neve , Ron Quinn , Magnus Polla
Abstract: The use of a compound of formula (I): in a method of manufacturing a medicament for the treatment or prophylaxis of a condition wherein inhibition of carboxypeptidase U is beneficial; specified compounds of formula (I) and compositions comprising a compound of formula (I) and a pharmaceutically acceptable adjuvant, diluent or carrier.
Abstract translation: 式（I）化合物在制备用于治疗或预防羧肽酶U的抑制有益的病症的药物的制备方法中的用途; 指定的式（I）化合物和包含式（I）化合物和药学上可接受的佐剂，稀释剂或载体的组合物。
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公开(公告)号：US07071175B1
公开(公告)日：2006-07-04
申请号：US09600661
申请日：2000-05-03
Applicant: Marcel Linschoten , Magnus Polla
Inventor： Marcel Linschoten , Magnus Polla
IPC: C07D213/72 , C07D213/74 , A61K31/44 , A61P7/02
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; 制备这种新化合物的方法：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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