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1. 发明申请

US20090124607A1 Novel Bicyclic Sulfonamides for Use as Glucocorticoid Receptor Modulators in the Treatment of Inflammatory Diseases 审中-公开
标题翻译：用作糖皮质激素受体调节剂治疗炎症性疾病的新型双环磺酰胺
公开(公告)号：US20090124607A1
公开(公告)日：2009-05-14
申请号：US12090442
申请日：2006-10-18
申请人： Hakan Bladh , Jan Dahmen , Thomas Hansson , Krister Henriksson , Matti Lepisto , Stinabritt Nilsson
发明人： Hakan Bladh , Jan Dahmen , Thomas Hansson , Krister Henriksson , Matti Lepisto , Stinabritt Nilsson
IPC分类号： A61K31/55 , C07D231/56 , A61K31/416 , C07D401/02 , A61K31/4439 , A61K31/437 , A61P29/00 , C07D239/24 , A61K31/506 , C07D487/02 , A61K31/519
CPC分类号： C07D231/56 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D407/14 , C07D487/04
摘要： Compounds of formula (I): or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).
摘要翻译：式（I）化合物或其药学上可接受的盐; 包含它们的组合物，其制备方法及其在药物治疗中的用途（例如调节温血动物中的糖皮质激素受体）。

2. 发明申请

US20080214641A1 Chemical compounds 572 失效
标题翻译：化合物572
公开(公告)号：US20080214641A1
公开(公告)日：2008-09-04
申请号：US12005066
申请日：2007-12-20
申请人： Markus Berger , Jan Dahmen , Karl Edman , Anders Eriksson , Balint Gabos , Thomas Hansson , Martin Hemmerling , Krister Henriksson , Svetlana Ivanova , Matti Lepisto , Darren McKerrecher , Magnus Munck af Rosenschold , Stinabritt Nilsson , Hartmut Rehwinkel , Camilla Taflin
发明人： Markus Berger , Jan Dahmen , Karl Edman , Anders Eriksson , Balint Gabos , Thomas Hansson , Martin Hemmerling , Krister Henriksson , Svetlana Ivanova , Matti Lepisto , Darren McKerrecher , Magnus Munck af Rosenschold , Stinabritt Nilsson , Hartmut Rehwinkel , Camilla Taflin
IPC分类号： A61K31/416 , C07D231/56 , A61P29/00
CPC分类号： C07D231/56 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04
摘要： Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments
摘要翻译：式（I）化合物：本发明涉及新的吲唑基酯或酰胺衍生物，包含这些衍生物的药物组合物，制备这种新衍生物的方法以及使用这些衍生物作为药物

3. 发明授权

US08030340B2 Indazolyl sulphonamide derivatives useful as glucocorticoid modulators 失效
标题翻译：用作糖皮质激素调节剂的吲唑基磺酰胺衍生物
公开(公告)号：US08030340B2
公开(公告)日：2011-10-04
申请号：US11986555
申请日：2007-11-21
申请人： Markus Berger , Lena Bergstrom , Jan Dahmen , Anders Eriksson , Balint Gabos , Martin Hemmerling , Krister Henriksson , Svetlana Ivanova , Matti Lepisto , Stinabritt Nilsson , Camilla Taflin , Hartmut Rehwinkel , Darren McKerrecher
发明人： Markus Berger , Lena Bergstrom , Jan Dahmen , Anders Eriksson , Balint Gabos , Martin Hemmerling , Krister Henriksson , Svetlana Ivanova , Matti Lepisto , Stinabritt Nilsson , Camilla Taflin , Hartmut Rehwinkel , Darren McKerrecher
IPC分类号： A01N43/56
CPC分类号： C07D231/56 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D413/12
摘要： Compounds of formula (I): or a pharmaceutically acceptable salt thereof, compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).
摘要翻译：式（I）化合物或其药学上可接受的盐; 包含它们的组合物，其制备方法及其在药物治疗中的用途（例如调节温血动物中的糖皮质激素受体）。

4. 发明申请

US20080207721A1 Chemical compounds 失效
标题翻译：化合物
公开(公告)号：US20080207721A1
公开(公告)日：2008-08-28
申请号：US11986555
申请日：2007-11-21
申请人： Markus Berger , Lena Bergstrom , Jan Dahmen , Anders Eriksson , Balint Gabos , Martin Hemmerling , Krister Henriksson , Svetlana Ivanova , Matti Lepisto , Stinabritt Nilsson , Camilla Taflin , Darren McKerrecher , Hartmut Rehwinkel
发明人： Markus Berger , Lena Bergstrom , Jan Dahmen , Anders Eriksson , Balint Gabos , Martin Hemmerling , Krister Henriksson , Svetlana Ivanova , Matti Lepisto , Stinabritt Nilsson , Camilla Taflin , Darren McKerrecher , Hartmut Rehwinkel
IPC分类号： A61K31/416 , C07D231/56
CPC分类号： C07D231/56 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D413/12
摘要： Compounds of formula (I): or a pharmaceutically acceptable salt thereof, compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).
摘要翻译：式（I）化合物或其药学上可接受的盐，包含它们的组合物，其制备方法及其在药物治疗中的用途（例如调节温血动物中的糖皮质激素受体）。

5. 发明申请

US20090093485A1 Novel Sulphonamide Derivatives as Glucocorticoid Receptor Modulators for the Treatment of Inflammatory Diseases 审中-公开
标题翻译：新型磺酰胺衍生物作为用于治疗炎性疾病的糖皮质激素受体调节剂
公开(公告)号：US20090093485A1
公开(公告)日：2009-04-09
申请号：US11718214
申请日：2005-10-26
申请人： Hakan Bladh , Krister Henriksson , Vijaykumar Hulikal , Matti Lepisto
发明人： Hakan Bladh , Krister Henriksson , Vijaykumar Hulikal , Matti Lepisto
IPC分类号： A61K31/53 , C07D215/38 , A61K31/47 , C07D307/78 , A61K31/343 , C07D209/04 , A61K31/404 , C07C311/15 , A61K31/18 , C07D277/20 , A61K31/426 , C07D239/24 , A61K31/505 , C07D213/02 , A61K31/44 , C07D405/02 , A61K31/443 , C07D251/02 , C07D239/72 , A61K31/517 , A61P29/00
CPC分类号： C07D409/04 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/29 , C07C311/46 , C07C317/36 , C07D209/08 , C07D209/16 , C07D213/30 , C07D213/42 , C07D213/65 , C07D213/70 , C07D213/76 , C07D215/20 , C07D215/233 , C07D215/26 , C07D215/36 , C07D215/38 , C07D215/44 , C07D217/02 , C07D231/18 , C07D233/54 , C07D239/47 , C07D239/88 , C07D251/52 , C07D277/46 , C07D307/68 , C07D307/80 , C07D317/64 , C07D333/34 , C07D333/62 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).
摘要翻译：式（I）化合物或其药学上可接受的盐; 包含它们的组合物，其制备方法及其在药物治疗中的用途（例如调节温血动物中的糖皮质激素受体）。

6. 发明申请

US20060035938A1 2-Pyridone derivatives as inhibitors of neutrophile elastase 审中-公开
标题翻译： 2-吡啶酮衍生物作为嗜中性粒细胞弹性蛋白酶抑制剂
公开(公告)号：US20060035938A1
公开(公告)日：2006-02-16
申请号：US10534720
申请日：2003-11-11
申请人： Hakan Bladh , Tomas Klingstedt , Joakim Larsson , Karolina Lawitz , Matti Lepisto , Hans Lonn , Grigorios Nikitidis
发明人： Hakan Bladh , Tomas Klingstedt , Joakim Larsson , Karolina Lawitz , Matti Lepisto , Hans Lonn , Grigorios Nikitidis
IPC分类号： C07D211/72 , A61K31/4412
CPC分类号： C07D213/64 , C07D213/82 , C07D239/557 , C07D241/24 , C07D413/12
摘要： There are provided novel compounds of formula (I) wherein R1?, R4?. R5?, G1?, G2?, X, L, Y1?, Y2? and n are as defined in the Specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors or neutrophil elastase.
摘要翻译：提供新的式（I）化合物，其中R 1？R 4？文件=“US20060035938A1-20060216-P00900.TIF”alt =“custom character”img-content =“character”img-id =“custom-character-00003”he =“2.46mm” 格式=“tif”/> 5 ?, G 1？G 2 ?, X，L，Y 1 ?, Y 2？和n如本说明书和光学异构体，外消旋体和互变异构体及其药学上可接受的盐所定义; 以及其制备方法，含有它们的组合物及其在治疗中的用途。化合物是抑制剂或嗜中性粒细胞弹性蛋白酶。

7. 发明申请

US20100021940A1 Method for Determining the Activity of a Protease in a Sample 审中-公开
标题翻译：测定样品中蛋白酶活性的方法
公开(公告)号：US20100021940A1
公开(公告)日：2010-01-28
申请号：US12296568
申请日：2007-04-11
申请人： Anders Blomgren , Anders Eriksson , Thomas Hansson , Keith Jolley , Matti Lepisto , Karin Von Wachenfeldt
发明人： Anders Blomgren , Anders Eriksson , Thomas Hansson , Keith Jolley , Matti Lepisto , Karin Von Wachenfeldt
IPC分类号： C12Q1/37 , G01N33/573 , C07K2/00 , C07C205/00
CPC分类号： C12Q1/37 , G01N2333/96486 , G01N2500/00 , G01N2800/122
摘要： There is provided a method for determining the activity of a protease in a sample. The method comprises (i) admixing said sample with a substrate, wherein the substrate has the formula (1a) wherein: R1 is a hydrocarbyl group; R2 is a first peptide moiety; R3 is a second peptide moiety and X is selected from the group consisting of O, S and NH; Y1 is a suitable substituent; Y2 is a suitable substituent; and (ii) determining the activity of said protease by detecting the presence of a reporter having the formula H—X—R1, wherein: X is selected from the group consisting of O, S and NH; R1 is a hydrocarbyl group. The substrate and reporter are useful for determining the efficacy of protease-modulators and candidate protease-modulators and in the diagnosis of a disease or disorder in a subject.
摘要翻译：提供了测定样品中蛋白酶活性的方法。该方法包括（i）将所述样品与基底混合，其中基底具有式（1a），其中：R1是烃基; R2是第一个肽部分; R3是第二肽部分，X选自O，S和NH; Y1是合适的取代基; Y2是合适的取代基; 和（ii）通过检测存在具有式H-X-R1的报告基来确定所述蛋白酶的活性，其中：X选自O，S和NH; R1是烃基。底物和报告物可用于确定蛋白酶调节剂和候选蛋白酶调节剂的功效以及受试者中疾病或病症的诊断。

8. 发明授权

US06337342B1 Bis-aryl or heteroaryl indoles 失效
标题翻译：双芳基或杂芳基吲哚
公开(公告)号：US06337342B1
公开(公告)日：2002-01-08
申请号：US09230710
申请日：1999-01-29
申请人： Kostas Karabelas , Matti Lepisto , Peter Sjö
发明人： Kostas Karabelas , Matti Lepisto , Peter Sjö
IPC分类号： A61K314152
CPC分类号： C07D403/04 , C07D403/14 , C07D409/14 , C07D471/04
摘要： The present invention relates to compounds of formula (I): wherein: Ar is an optionally substituted aromatic or heteroaromatic group, R1 is H, C1-6alkyl, CF3, phenyl, benzyl, carboC1-6alkoxy, carbamoyl, or methyl(N—C1-6alkylcarbamoyl) R2 is H, C1-6alkyl, aminoC1-6alkyl, hydroxyC1-6alkyl, (mono- or di- C1-6alkyl)aminoC1-6alkyl, (aminoC1-3alkylphenyl)C1-3alkyl, amidinothio C1-6alkyl, R3 is H or C1-6alkoxy, R4 is H or together with R2, forms an annulated ring which may be substituted by hydroxyC1-3alkyl or amidinothio C1-3alkyl, or aminoC1-3alkyl; and pharmaceutically acceptable salts thereof; and the use of such compounds in medical therapies.
摘要翻译：本发明涉及式（I）的化合物：其中：Ar是任选取代的芳族或杂芳族基团，R 1是H，C 1-6烷基，CF 3，苯基，苄基，C 1 -C 6烷氧基，氨基甲酰基或甲基（N-C 1 （烷基氨基甲酰基）R 2是H，C 1-6烷基，氨基C 1-6烷基，羟基C 1-6烷基，（单 - 或二 - C 1-6烷基）氨基C 1-6烷基，（氨基C 1-3烷基苯基）C 1-3烷基，脒基硫代C 1-6烷基，R 3是H 或C 1-6烷氧基，R 4是H或与R 2一起形成可以被羟基C 1-3烷基或脒基C 1-3烷基或氨基C 1-3烷基取代的环状环;及其药学上可接受的盐;以及这些化合物在医学上的用途疗法。

9. 发明申请

US20070219217A1 Triazolone Derivatives as Mmp Inhibitors for the Treatment of Asthma and Copd 审中-公开
标题翻译：三唑酮衍生物作为治疗哮喘和复发的Mmp抑制剂
公开(公告)号：US20070219217A1
公开(公告)日：2007-09-20
申请号：US10593543
申请日：2005-03-29
申请人： Anders Eriksson , Matti Lepisto
发明人： Anders Eriksson , Matti Lepisto
IPC分类号： A61K31/4196 , A61K31/445 , A61K31/496 , C07D249/08 , C07D401/00 , C07D403/00
CPC分类号： C07D249/12 , C07D401/12 , C07D401/14 , C07D417/14 , C07D491/10
摘要： The invention provides compounds of formula (I): wherein R1, R2, R3, R4, R5, X, Y, L, G1 and m have the meanings defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.
摘要翻译：本发明提供式（I）化合物：其中R 1，R 2，R 3，R 4， R 5，X，Y，L，G 1和m具有本说明书中定义的含义; 其准备过程; 含有它们的药物组合物; 制备药物组合物的方法; 及其在治疗中的应用。

10. 发明授权

US4932140A Arrangement of pressure nozzles for the treatment of webs 失效
标题翻译：用于处理腹板的压力喷嘴的布置
公开(公告)号：US4932140A
公开(公告)日：1990-06-12
申请号：US358362
申请日：1989-05-03
申请人： Matti Lepisto
发明人： Matti Lepisto
IPC分类号： B65H20/14 , D21F5/18 , F26B13/20
CPC分类号： D21F5/188 , F26B13/104
摘要： An arrangement of pressure nozzles intended for the treatment of webs comprises a nozzle box. The nozzle box has a carrying face (16) placed facing the web, two nozzle slots (17,18) that blow towards each other being provided in connection with the carrying face, these nozzle slots being placed in the outer part of the space defined by the inner walls (14,15) and the outer walls (20,21) of the nozzle box. The arrangement of nozzles is asymmetric relative to the perpendicular center plane (A--A) of its pressurized carrying face (16). The arrangement of nozzles has a first nozzle slot (18), which is placed relative the carrying face (16) in such a way that the gas jet (v.sub.1) blown out of the nozzle slot follows and remains in contact with the curved carrying face (16) up to the area between the nozzle slots (17,18). The arrangement of nozzles includes a second nozzle slot (17), which is placed within the area of the edge of the curved guide face (14,R.sub.2) placed in its connection or, in the gas flow direction (v.sub.2), before the edge. The ratio of the width of the second nozzle slot (18) to the curve radius (R.sub.2) of its guide face (14) is chosen so, with the flow rates (v.sub.2) of the second nozzle generally occurring, that the gas flow is separated from the curved (R.sub.2) guide face of the second nozzle, before the carrying face area proper between the first and the second nozzle slot (17,18), or in the edge portion of this area.
摘要翻译： PCT No.PCT / FI88 / 00155 Sec。 371日期：1989年5月3日 102（e）日期1989年5月3日PCT提交1988年9月23日PCT公布。公开号WO89 / 02953 日本1989年4月6日。用于处理腹板的压力喷嘴的布置包括喷嘴箱。喷嘴箱具有面向腹板放置的承载面（16），与承载面相连接设置的彼此相对的两个喷嘴槽（17,18），这些喷嘴槽被放置在限定的空间的外部通过喷嘴箱的内壁（14,15）和外壁（20,21）。喷嘴的布置相对于其加压承载面（16）的垂直中心平面（A-A）是不对称的。喷嘴的布置具有第一喷嘴狭槽（18），其相对于承载面（16）放置，使得从喷嘴槽吹出的气体射流（v1）与弯曲的承载面保持接触（16）直到喷嘴槽（17,18）之间的区域。喷嘴的布置包括第二喷嘴槽（17），该第二喷嘴槽（17）被放置在弯曲导向面（14，R2）的边缘的区域内，或者沿气体流动方向（v2），在边缘。选择第二喷嘴狭槽（18）的宽度与其导向面（14）的曲线半径（R2）的比率，使得第二喷嘴的流速（v2）通常发生，气流为在第一和第二喷嘴槽（17,18）之间的承载面积区域中，或者在该区域的边缘部分中，与第二喷嘴的弯曲（R2）引导面分离。

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