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1. 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）。

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

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。

4. 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）。

5. 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）。

6. 发明申请

US20080188666A1 LINEAR PHENYL-SUBSTITUTED INDAZOLES AND INDOLES, A PROCESS FOR THEIR PRODUCTION AND THEIR USE AS ANTI-INFLAMMATORY AGENTS 审中-公开
标题翻译：线性苯基取代的吲哚和吲哚，其生产过程及其作为抗炎剂的用途
公开(公告)号：US20080188666A1
公开(公告)日：2008-08-07
申请号：US11936395
申请日：2007-11-07
申请人： Markus Berger , Hartmut Rehwinkel , Heike Schaecke , Matti Lepisto , Karl Edmann
发明人： Markus Berger , Hartmut Rehwinkel , Heike Schaecke , Matti Lepisto , Karl Edmann
IPC分类号： C07D401/04 , C07D231/56 , C07D209/14
CPC分类号： C07D405/12 , C07D231/56 , C07D401/04 , C07D405/14
摘要： The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.
摘要翻译：本发明涉及式I化合物，其制备方法及其作为抗炎剂的用途。

7. 发明授权

US06962791B2 Treatment or prophylaxis of diseases caused by pilus-forming bacteria 失效
公开(公告)号：US06962791B2
公开(公告)日：2005-11-08
申请号：US09799608
申请日：2001-03-07
申请人： Scott Hultgren , Meta Kuehn , Zheng Xu , Derek Ogg , Mark Harris , Matti Lepisto , Charles Hal Jones , Jan Kihlberg
发明人： Scott Hultgren , Meta Kuehn , Zheng Xu , Derek Ogg , Mark Harris , Matti Lepisto , Charles Hal Jones , Jan Kihlberg
IPC分类号： A61K31/00 , A61K31/70 , C07H1/00 , G01N33/68 , G01N33/569 , A61K39/108 , A61K39/02
CPC分类号： A61K31/7004 , A61K31/00 , A61K31/70 , C07H1/00 , G01N33/68 , G01N2333/195 , G01N2500/10 , G01N2500/20 , Y02A50/481 , Y10S435/849
摘要： Novel methods for the treatment and/or prophylaxis of diseases caused by tissue-adhering bacteria are disclosed. By interacting with periplasmic molecular chaperones it is achieved that the assembly of pili is prevented or inhibited and thereby the infectivity of the bacteria is diminished. Also disclosed are methods for screening for drugs as well as methods for the de novo design of such drugs, methods which rely on novel computer drug modelling methods involving an approximative calculation of binding free energy between macromolecules. Finally, novel pyranosides which are believed to be capable of interacting with periplasmic molecular chaperones are also disclosed.

8. 发明授权

US06420127B1 Compounds and pharmaceutical compositions for the treatment and prophylaxis of bacterial infections 失效
标题翻译：用于治疗和预防细菌感染的化合物和药物组合物
公开(公告)号：US06420127B1
公开(公告)日：2002-07-16
申请号：US08640877
申请日：1996-10-10
申请人： Scott Hultgren , Meta Kuehn , Zheng Xu , Derek Ogg , Mark Harris , Matti Lepisto , Charles Hal Jones , Jan Kihlberg
发明人： Scott Hultgren , Meta Kuehn , Zheng Xu , Derek Ogg , Mark Harris , Matti Lepisto , Charles Hal Jones , Jan Kihlberg
IPC分类号： G01N33569
CPC分类号： A61K31/7004 , A61K31/00 , A61K31/70 , C07H1/00 , G01N33/68 , G01N2333/195 , G01N2500/10 , G01N2500/20 , Y02A50/481 , Y10S435/849
摘要： Novel methods for the treatment and/or prophylaxis of diseases caused by tissue-adhering bacteria are disclosed. By interacting with periplasmic molecular chaperones it is achieved that the assembly of pili is prevented or inhibited and thereby the infectivity of the bacteria is diminished. Also disclosed are methods for screening for drugs as well as methods for the de novo design of such drugs, methods which rely on novel computer drug modelling methods involving an approximative calculation of binding free energy between macromolecules. Finally, novel pyranosides which are believed to be capable of interacting with periplasmic molecular chaperones are also disclosed.
摘要翻译：公开了用于治疗和/或预防由组织粘附细菌引起的疾病的新方法。通过与周质分子伴侣相互作用，可以防止或抑制毛细血管的组装，从而减少细菌的感染性。还公开了用于筛选药物的方法以及用于从头设计这些药物的方法，这些方法依赖于涉及大分子之间的结合自由能的近似计算的新型计算机药物建模方法。最后，还公开了被认为能够与周质分子伴侣相互作用的新型吡喃糖苷。

9. 发明授权

US5009016A Method for on-machine coating-drying of a paper web or the like 失效
标题翻译：纸幅等的机上涂布干燥方法
公开(公告)号：US5009016A
公开(公告)日：1991-04-23
申请号：US381674
申请日：1989-07-14
申请人： Matti LePisto , Reijo Ilmanen , Markku Karlsson , Sauli Laakso
发明人： Matti LePisto , Reijo Ilmanen , Markku Karlsson , Sauli Laakso
IPC分类号： F26B3/30 , D21F5/00 , D21F5/18 , D21H25/06 , F26B3/28 , F26B13/10 , F26B13/20 , F26B20/00
CPC分类号： D21F5/187 , D21F5/002 , D21H25/06 , F26B13/104 , F26B3/283
摘要： A method for contact-free drying of a paper or board web or of any other corresponding continuous web. During drying, both infrared radiation and drying air jets are used. The web is carried by the air jets through the dryer free of contact. The moving web is first passed into an infrared drying gap, in which a drying energy pulse of relatively short duration is directed at the web, the power of the energy pulse being substantially higher than the average drying power of the dryer per unit of area. After the infrared drying gap, the web is immediately passed into an airborne web drying gap wherein the web is supported and dried by means of air jets. Air is brought into the infrared unit, which air having been heated in the infrared unit is passed as replacement air and/or drying air for the airborne web drying unit or units placed after the infrared unit. The air flows to be passed into the infrared unit are passed in connection with the inlet gap of the web to both sides of the web so as to form both accompanying and sealing air jet flows.
摘要翻译： PCT No.PCT / FI87 / 00159 Sec。 371日期：1989年7月14日 102（e）日期1989年7月14日PCT公布1987年11月26日PCT公布。出版物WO89 / 04890 日期1989年6月1日。一种用于纸或纸幅或任何其它相应连续幅材的无接触干燥的方法。在干燥过程中，使用红外辐射和干燥空气射流。网状物由空气喷射器通过干燥器无接触。移动幅材首先被传送到红外干燥间隙中，其中持续时间相对较短的干燥能量脉冲指向幅材，能量脉冲的功率显着高于每单位面积干燥器的平均干燥功率。在红外线干燥间隙之后，纤维网立即进入空气中的纤维网干燥间隙，其中纤维网通过空气喷射被支撑和干燥。空气被引入红外单元中，在红外单元中已被加热的空气作为替换空气和/或干燥空气通过作为放置在红外单元之后的空气干燥单元或单元的干燥空气。将要进入红外线单元的空气流与纤维网的入口间隙连接到幅材的两侧，以便形成伴随和密封的空气喷射流。

10. 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）。

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