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1. 发明申请

US20090012087A1 New Aza-Bicyclohexane Compounds Useful As Inhibitors Of Thrombin 审中-公开
标题翻译：新的氮杂双环己烷化合物可用作凝血酶抑制剂
公开(公告)号：US20090012087A1
公开(公告)日：2009-01-08
申请号：US12166407
申请日：2008-07-02
申请人： Jonas Branalt , Ingemar Nilsson , Magnus Polla
发明人： Jonas Branalt , Ingemar Nilsson , Magnus Polla
IPC分类号： A61K31/5377 , C07D403/08 , A61K31/41 , A61K31/4709 , C07D401/14 , C07D413/14
CPC分类号： C07D403/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： 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.
摘要翻译：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。

2. 发明申请

US20080214589A1 Thrombin Inhibiting 2,4-Dioxo-3,4-Dihydropyrimidine Derivatives 审中-公开
标题翻译：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
申请人： Ingemar Nilsson , Magnus Polla
发明人： Ingemar Nilsson , Magnus Polla
IPC分类号： A61K31/506 , C07D407/14
CPC分类号： C07D239/545 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14
摘要： 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).
摘要翻译：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）。

3. 发明授权

US08119673B2 Compounds 148 失效
标题翻译：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
申请人： Jonas Brånalt , David Gustafsson , Ingemar Nilsson , Magnus Polla
发明人： Jonas Brånalt , David Gustafsson , Ingemar Nilsson , Magnus Polla
IPC分类号： A61K31/41 , C07D257/04
CPC分类号： C07D403/12 , C07D405/14 , C07D413/12
摘要： 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.
摘要翻译：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。

4. 发明申请

US20080207695A1 Thrombin Inhibiting 2-Oxo-1,2,5,6-Tetrahydropyridine Derivatives 审中-公开
标题翻译：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
申请人： Ingemar Nilsson , Magnus Polla
发明人： Ingemar Nilsson , Magnus Polla
IPC分类号： A61K31/444 , C07D213/73 , A61K31/44 , A61P7/02 , C07D401/12
CPC分类号： C07D401/14 , C07D213/73 , C07D213/75
摘要： 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).
摘要翻译：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）。

5. 发明授权

US07375121B2 Chemical compounds 失效
标题翻译：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
申请人： Magnus Polla
发明人： Magnus Polla
IPC分类号： A61K31/44 , C07D211/72
CPC分类号： C07F9/6539 , C07F9/5765 , C07F9/58
摘要： 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.
摘要翻译：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。

6. 发明授权

US06291475B1 Bispidine antiarrhythmic compounds 失效
标题翻译：二甲苯抗心律失常药
公开(公告)号：US06291475B1
公开(公告)日：2001-09-18
申请号：US09214756
申请日：1999-01-12
申请人： Christer Alstermark , Annika Björe , Magnus Björsne , Marianne Frantsi , Torbjörn Halvarsson , Kurt-Jürgen Hoffmann , Eva-Lotte Lindstedt , Magnus Polla , Gert Strandlund
发明人： Christer Alstermark , Annika Björe , Magnus Björsne , Marianne Frantsi , Torbjörn Halvarsson , Kurt-Jürgen Hoffmann , Eva-Lotte Lindstedt , Magnus Polla , Gert Strandlund
IPC分类号： A61K31439
CPC分类号： C07D471/08
摘要： There is provided a compound of formula I, wherein R1, R2, R9, R10, R11, R12, X, A and B have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.
摘要翻译：提供式I化合物，其中R 1，R 2，R 9，R 10，R 11，R 12，X，A和B具有在描述中给出的含义，其可用于预防和治疗心律失常，特别是心房和室性心律失常。

7. 发明授权

US07572817B2 2,5-disubstituted 3-mercaptopentanoic acid 失效
标题翻译： 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
申请人： Magnus Polla
发明人： Magnus Polla
IPC分类号： 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分类号： C07D211/34 , C07D213/73 , C07D277/40 , C07D401/06 , C07D405/06 , C07D409/06
摘要： 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.
摘要翻译：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。

8. 发明申请

US20060079484A1 Phosphinyloxy, oxime and carboxylic acid derivatives which are useful as carboxypeptidase U inhibitors 失效
标题翻译：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
申请人： Marcel Linschoten , Magnus Polla
发明人： Marcel Linschoten , Magnus Polla
IPC分类号： C07F5/02 , A61K31/69 , A61K31/675
CPC分类号： A61K38/57 , A61K2300/00
摘要： 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.
摘要翻译：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。

9. 发明授权

US06974800B1 Formulations comprising an inhibitor of carboxypeptidase U and A thrombin inhibitor 失效
标题翻译：包含羧肽酶U和A凝血酶抑制剂的抑制剂的制剂
公开(公告)号：US06974800B1
公开(公告)日：2005-12-13
申请号：US09600659
申请日：2000-05-03
申请人： Tommy Abrahamsson , Viveca Nerme , Magnus Polla
发明人： Tommy Abrahamsson , Viveca Nerme , Magnus Polla
IPC分类号： A61K45/00 , A61K31/095 , A61K31/155 , A61K31/44 , A61K38/00 , A61K38/55 , A61K38/57 , A61P7/02 , A61P9/00 , A61P43/00 , C07K5/06
CPC分类号： A61K38/57 , A61K31/095 , A61K2300/00
摘要： The present invention relates to pharmaceutical formulations of an inhibitor of carboxypeptidase U (CPU) and a thrombin inhibitor in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier, as well as a kit of parts, a method for treatment and use of the formulations for the treatment of a condition in which inhibition of CPU and/or inhibition of thrombin are required or desired.
摘要翻译：本发明涉及与药学上可接受的佐剂，稀释剂或载体混合的羧肽酶U（CPU）和凝血酶抑制剂的抑制剂的药物制剂，以及一组试剂盒，一种治疗和使用该制剂的方法治疗需要或期望抑制CPU和/或抑制凝血酶的病症。

10. 发明申请

US20050176780A1 2,5-disubstituted 3-mercaptopentanoic acid 失效
标题翻译： 2,5-二取代的3-巯基戊酸
公开(公告)号：US20050176780A1
公开(公告)日：2005-08-11
申请号：US10517713
申请日：2003-06-10
申请人： Magnus Polla
发明人： Magnus Polla
IPC分类号： C07D277/20 , A61K31/426 , A61K31/427 , A61K31/435 , A61K31/439 , A61K31/44 , A61K31/506 , A61P1/16 , A61P7/02 , A61P9/10 , A61P11/00 , A61P17/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07D211/34 , C07D213/73 , C07D213/74 , C07D213/76 , C07D221/22 , C07D277/40 , C07D277/42 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , A61K31/403
CPC分类号： C07D211/34 , C07D213/73 , C07D277/40 , C07D401/06 , C07D405/06 , C07D409/06
摘要： 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.
摘要翻译：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。

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