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1. 发明授权

US06548265B2 Treatment or prophylaxis of diseases caused by pilus-forming bacteria 失效
公开(公告)号：US06548265B2
公开(公告)日：2003-04-15
申请号：US09799576
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： 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.

2. 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.

3. 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。

4. 发明授权

US07025971B2 Treatment or prophylaxis of diseases caused by pilus-forming bacteria 失效
公开(公告)号：US07025971B2
公开(公告)日：2006-04-11
申请号：US09798932
申请日：2001-03-06
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： A61K39/10 , A61K39/02 , A61K39/108 , G01N33/569
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.

5. 发明授权

US06872542B1 Treatment or prophylaxis of diseases caused by pilus-forming bacteria 失效
标题翻译：治疗或预防由菌毛形成细菌引起的疾病
公开(公告)号：US06872542B1
公开(公告)日：2005-03-29
申请号：US09799584
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 , G01N33/554 , A61K39/38 , A61K39/395 , A61K39/40 , A61K49/00
CPC分类号： G01N33/68 , A61K31/00 , A61K31/70 , A61K31/7004 , C07H1/00 , G01N2333/195 , G01N2500/10 , G01N2500/20
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。

6. 发明授权

US06596504B2 Treatment of prophylaxis of diseases caused by pilus-forming bacteria 失效
标题翻译：治疗由菌毛形成细菌引起的疾病的预防
公开(公告)号：US06596504B2
公开(公告)日：2003-07-22
申请号：US09799540
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： A61K3902
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。

7. 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）。

8. 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

9. 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。

10. 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。

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