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51. 发明申请

US20100298373A1 OXADIAZOLE DERIVATIVES ACTIVE ON SPHINGOSINE-1-PHOSPHATE (SIP) 失效
标题翻译：活性磷酸1-磷酸酯（SIP）的氧杂衍生物
公开(公告)号：US20100298373A1
公开(公告)日：2010-11-25
申请号：US12747188
申请日：2008-12-19
申请人： Jag Paul Heer , Thomas Daniel Heightman
发明人： Jag Paul Heer , Thomas Daniel Heightman
IPC分类号： A61K31/4725 , C07D217/20 , A61P37/00
CPC分类号： C07D217/22 , C07D217/06 , C07D217/16 , C07D413/04 , C07D413/14
摘要： The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
摘要翻译：本发明涉及具有药理活性的新型恶二唑衍生物，其制备方法，含有它们的药物组合物及其在治疗各种病症中的用途。

52. 发明授权

US07691879B2 Isoquinoline potassium channel inhibitors 失效
标题翻译：异喹啉钾通道抑制剂
公开(公告)号：US07691879B2
公开(公告)日：2010-04-06
申请号：US10572342
申请日：2004-09-17
申请人： B. Wesley Trotter , Kausik K. Nanda , Nathan R. Kett , Christopher J. Dinsmore , Gerald S. Ponticello , David A. Claremon
发明人： B. Wesley Trotter , Kausik K. Nanda , Nathan R. Kett , Christopher J. Dinsmore , Gerald S. Ponticello , David A. Claremon
IPC分类号： A61K31/47 , C07D217/00 , C07D217/22
CPC分类号： C07D217/14 , C07D217/16 , C07D401/04
摘要： The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
摘要翻译：本发明涉及具有用作治疗心律失常的钾通道抑制剂的结构（I）的化合物等。

53. 发明申请

US20100048588A1 AMINOCARBONYL-DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE 有权
标题翻译：氨苄青霉素衍生物作为HISTONE脱乙酰壳多糖的新型抑制剂
公开(公告)号：US20100048588A1
公开(公告)日：2010-02-25
申请号：US12360139
申请日：2009-01-27
申请人： Kristof Van Emelen , Hans Louis Jos De Winter , Alexy Borisovich Dyatkin , Marc Gustaaf Celine Verdonck , Lieven Meerpoel , Jimmy Arnold Viviane Van heusden
发明人： Kristof Van Emelen , Hans Louis Jos De Winter , Alexy Borisovich Dyatkin , Marc Gustaaf Celine Verdonck , Lieven Meerpoel , Jimmy Arnold Viviane Van heusden
IPC分类号： A61K31/4965 , C07D241/04
CPC分类号： C07D413/12 , A61K31/40 , A61K31/402 , A61K31/435 , A61K31/4427 , A61K31/454 , A61K31/4545 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D207/09 , C07D207/14 , C07D211/14 , C07D211/58 , C07D213/78 , C07D217/02 , C07D217/04 , C07D217/16 , C07D239/42 , C07D295/155 , C07D295/26 , C07D307/68 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D409/12 , C07D409/14 , C07D413/04 , C07D471/04 , C07D471/10 , C07D513/04 , C12Q1/34 , C12Q1/48
摘要： This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括具有组蛋白脱乙酰酶抑制酶活性的式（I）的新化合物，其中n，R 1，R 2，R 3，R 4，L，Q，X，Y，Z具有定义的含义; 其制剂，含有它们的组合物及其作为药物的用途。

54. 发明申请

US20090247757A1 LIGANDS, THEIR PREPARATION AND USES THEREOF IN ASYMMETRIC REACTIONS 失效
标题翻译：配体，它们的制备及其在不对称反应中的用途
公开(公告)号：US20090247757A1
公开(公告)日：2009-10-01
申请号：US12267285
申请日：2008-11-07
申请人： Chao-Jun Li , Jianqing Feng
发明人： Chao-Jun Li , Jianqing Feng
IPC分类号： C07D217/02
CPC分类号： C07D217/12 , C07D217/04 , C07D217/16
摘要： Novel chemical agents are described herein. More a ligand of general Formula I: wherein R1, R2, R3 and R4, are independently selected from the group consisting of hydrogen, halogen, hydroxy, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C1-C10 alkoxy, C1-C10 alkylthio, C(O)R5, C(O)OR5, C(O)NHR5, Si(R5)3, benzyl and aryl; X is selected from the group consisting of Cl, Br, I, OR6, O-Prot, OPR6, P(R6)2, NHR6, N(R6)2, NHCSNHR6, NHCONHR6 and SR6; and R5 and R6 are independently selected from the group consisting of hydrogen, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1-10 alkoxy, phenyl, and aryl. These ligands are useful in asymmetric reactions as well as in asymmetric synthesis of molecules of biological interest.
摘要翻译：本文描述了新的化学试剂。更多的通式I的配体：其中R 1，R 2，R 3和R 4独立地选自氢，卤素，羟基，C 1 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基，C 1 -C 10烷氧基，C 1 -C 10烷硫基，C（O）R 5，C（O）OR 5，C（O）NHR 5，Si（R 5）3，苄基和芳基; X选自Cl，Br，I，OR6，O-Prot，OPR6，P（R6）2，NHR6，N（R6）2，NHCSNHR6，NHCONHR6和SR6; R 5和R 6独立地选自氢，C 1-10烷基，C 2-10烯基，C 2-10炔基，C 1-10烷氧基，苯基和芳基。这些配体可用于不对称反应以及不对称合成生物学上的分子。

55. 发明申请

US20090227558A1 AMINO-DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE 审中-公开
标题翻译：氨基衍生物作为组蛋白脱乙酰酶的新型抑制剂
公开(公告)号：US20090227558A1
公开(公告)日：2009-09-10
申请号：US12429838
申请日：2009-04-24
申请人： Patrick Rene Angibaud , Kristof Van Emelen , Virginie Sophie Poncelet , Bruno Roux
发明人： Patrick Rene Angibaud , Kristof Van Emelen , Virginie Sophie Poncelet , Bruno Roux
IPC分类号： A61K31/397 , C07D213/02 , A61K31/4545 , C12Q1/34 , C07D239/02 , A61K31/506 , C07D413/02 , A61K31/5377 , A61P35/00
CPC分类号： C07D413/12 , A61K31/40 , A61K31/402 , A61K31/435 , A61K31/4427 , A61K31/454 , A61K31/4545 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D207/09 , C07D207/14 , C07D211/14 , C07D211/58 , C07D213/78 , C07D217/02 , C07D217/04 , C07D217/16 , C07D239/42 , C07D295/155 , C07D295/26 , C07D307/68 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D409/12 , C07D409/14 , C07D413/04 , C07D471/04 , C07D471/10 , C07D513/04 , C12Q1/34 , C12Q1/48
摘要： This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括其中n，m，t，R1，R2，L，Q，X，Y，Z并具有定义的含有组蛋白脱乙酰酶抑制酶活性的式（I）化合物; 其制剂，含有它们的组合物及其作为药物的用途。

56. 发明申请

US20080176896A1 Modulators of cellular adhesion 有权
公开(公告)号：US20080176896A1
公开(公告)日：2008-07-24
申请号：US11978388
申请日：2007-10-29
申请人： Wang Shen , Kenneth Barr , Johan D. Oslob , Min Zhong
发明人： Wang Shen , Kenneth Barr , Johan D. Oslob , Min Zhong
IPC分类号： A61K31/47 , A61P37/00 , C07D217/00
CPC分类号： A61K31/4725 , A61K31/472 , A61K31/506 , A61K31/517 , A61K45/06 , C04B35/632 , C07D217/06 , C07D217/16 , C07D217/26 , C07D231/56 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14
摘要： The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).

57. 发明申请

US20080139610A1 Derivatives of 4-(n-azacycloalkyl) anilides as potassium channel modulators 有权
标题翻译： 4-（正 - 氮杂环烷基）苯胺的衍生物作为钾通道调节剂
公开(公告)号：US20080139610A1
公开(公告)日：2008-06-12
申请号：US11894877
申请日：2007-08-22
申请人： Jean-Michel Vernier , Martha Alicia De La Rosa , Huanming Chen , Jim Zhen Wu , Gary Lee Larson , Ian Wayne Cheney
发明人： Jean-Michel Vernier , Martha Alicia De La Rosa , Huanming Chen , Jim Zhen Wu , Gary Lee Larson , Ian Wayne Cheney
IPC分类号： A61K31/472 , A61P25/00 , C07D217/12
CPC分类号： C07D217/14 , C07D217/16
摘要： This invention provides a compound of formula IA where X═O or S; Y is O or S; q=1 or 0; and other substituents are defined herein. Such compounds can affect the opening of, or otherwise modulate, voltage-gated potassium channels. They are potentially useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.
摘要翻译：本发明提供式IA化合物，其中X-O或S; Y为O或S; q = 1或0 和其它取代基在本文中定义。这种化合物可影响电压门控钾通道的开启或以其他方式调节。它们可用于治疗和预防受到钾离子通道活化或调节影响的疾病和病症。一种这样的病症是癫痫发作。

58. 发明授权

US07371762B2 3-substituted 6,7-dihydroxytetrahydroisoquinoline derivatives for use as antibacterial agents 失效
标题翻译： 3-取代的6,7-二羟基四氢异喹啉衍生物，用作抗菌剂
公开(公告)号：US07371762B2
公开(公告)日：2008-05-13
申请号：US10487877
申请日：2002-08-09
申请人： Kaspar Burri , Laurent Schmitt , Khalid Islam
发明人： Kaspar Burri , Laurent Schmitt , Khalid Islam
IPC分类号： C07D217/12 , A61K31/47
CPC分类号： C07D217/02 , C07D217/12 , C07D217/14 , C07D217/16
摘要： The invention relates to novel tetrahydroisoquinoline derivatives of general formula I and theirs use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and their use as anti-infectives, wherein R1, R2 and R3 are as defined in claim 1.
摘要翻译：本发明涉及通式Ⅰ的新型四氢异喹啉衍生物及其在药物组合物的制备中用作活性成分。本发明还涉及包括制备化合物的方法，含有一种或多种这些化合物的药物组合物及其作为抗感染剂的用途的相关方面，其中R 1，R 2， SUP＆gt;和R 3＆gt;如权利要求1所定义。

59. 发明授权

US07314938B2 Modulators of cellular adhesion 有权
标题翻译：细胞粘附的调节剂
公开(公告)号：US07314938B2
公开(公告)日：2008-01-01
申请号：US10982463
申请日：2004-11-05
申请人： Wang Shen , Kenneth Barr , Johan D. Oslob , Min Zhong
发明人： Wang Shen , Kenneth Barr , Johan D. Oslob , Min Zhong
IPC分类号： C07D217/14 , A61K31/166
CPC分类号： A61K31/4725 , A61K31/472 , A61K31/506 , A61K31/517 , A61K45/06 , C04B35/632 , C07D217/06 , C07D217/16 , C07D217/26 , C07D231/56 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14
摘要： The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).
摘要翻译：本发明提供具有式（I）的化合物及其药学上可接受的衍生物，其中R 1 -R 4，n，p，A，B，D，E， L和AR 1如本文所述的一般类型和亚类所述，并且另外提供其药物组合物及其用于治疗由CD11 / CD18家族介导的细胞粘附的疾病的方法分子（如LFA-1）。

60. 发明授权

US07271270B2 High affinity small molecule C5a receptor modulators 失效
公开(公告)号：US07271270B2
公开(公告)日：2007-09-18
申请号：US10853731
申请日：2004-05-24
申请人： Andrew Thurkauf , Xiao-shu He , He Zhao
发明人： Andrew Thurkauf , Xiao-shu He , He Zhao
IPC分类号： C07D235/02 , C07D233/00
CPC分类号： C07D207/327 , C07C233/11 , C07C233/22 , C07C233/65 , C07C233/66 , C07C233/73 , C07C233/78 , C07C235/46 , C07C235/48 , C07C235/54 , C07C235/60 , C07C235/62 , C07C235/66 , C07C237/20 , C07C323/62 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2603/18 , C07D213/38 , C07D213/82 , C07D215/12 , C07D217/04 , C07D217/06 , C07D217/14 , C07D217/16 , C07D231/12 , C07D233/64 , C07D233/68 , C07D235/02 , C07D235/14 , C07D235/18 , C07D317/58 , C07D333/24 , C07D333/28 , C07D333/54 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12 , C07D471/04
摘要： This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as antagonists or inverse agonists of complement C5a receptors. Preferred compounds of the invention possess some or all of the following properties in that they are: 1) multi-aryl in structure, 2) heteroaryl in structure, 3) a pharmaceutically acceptable oral dose can provide a detectable in vitro effect, 4) comprise fewer than four or preferably no amide bonds, and 5) capable of inhibiting leukocyte chemotaxis at nanomolar or sub-nanomolar concentrations.This invention also relates to pharmaceutical compositions comprising such compounds and the use of such compounds in treating a variety of inflammatory and immune system disorders. Additionally, this invention relates to the use such compounds as probes for the localization of C5a receptors.

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