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1. 发明申请

WO2008066789A3 HETEROARYL AMIDE DERIVATIVES 审中-公开
标题翻译：杂芳基酰胺衍生物
公开(公告)号：WO2008066789A3
公开(公告)日：2008-08-21
申请号：PCT/US2007024396
申请日：2007-11-27
申请人： NEUROGEN CORP , HUTCHISON ALAN J , LI HONGBIN , MAO JIANMIN , WUSTROW DAVID J , YUAN JUN , ZHAO HE
发明人： HUTCHISON ALAN J , LI HONGBIN , MAO JIANMIN , WUSTROW DAVID J , YUAN JUN , ZHAO HE
IPC分类号： A01N55/02 , A61K31/555
CPC分类号： C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/113 , C07D519/00
摘要： Heteroaryl amide derivatives are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译：提供具有下式的杂芳基酰胺衍生物：其中变量如本文所述。此类化合物是可用于体内或体外调节特定受体活性的配体，并且特别用于治疗与人，家养伴侣动物和家畜动物中的病理性受体激活相关的病症。提供了用于使用这些化合物来治疗此类病症的药物组合物和方法，以及使用这些配体用于受体定位研究的方法。

2. 发明申请

WO2007133820A2 DIARYL TRIAZOLONES AS CB1 ANTAGONISTS 审中-公开
标题翻译： DIARYL TRIAZOLONES作为CB1拮抗剂
公开(公告)号：WO2007133820A2
公开(公告)日：2007-11-22
申请号：PCT/US2007060599
申请日：2007-01-17
申请人： NEUROGEN CORP , HUTCHISON ALAN J , MAO JIANMIN , MAYNARD GEORGE D , PRINGLE WALLACE C , ZHAO HE , WUSTROW DAVID J
发明人： HUTCHISON ALAN J , MAO JIANMIN , MAYNARD GEORGE D , PRINGLE WALLACE C , ZHAO HE , WUSTROW DAVID J
IPC分类号： A61F9/00
CPC分类号： C07D401/14 , C07D249/12 , C07D401/04 , C07D403/04 , C07D413/14
摘要： Diaryl triazolones of Formula I are provided, in which the variables are as described herein. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using diaryl traizolones of Formula I to treat such disorders are provided, as are methods for using such compounds as ligands for receptor localization studies and various in vitro assays.
摘要翻译：提供式I的二芳基三唑酮，其中变量如本文所述。这些化合物可用于体内或体外调节CB1活性，并且特别可用于治疗对人，家养伴侣动物和家畜中的CB1调节有反应的病症，包括食欲障碍，肥胖症和成瘾性疾病。还提供了使用式I的二芳基特里诺酮来治疗这些疾病的药物组合物和方法，以及使用这些化合物作为受体定位研究的配体和各种体外测定的方法。

3. 发明申请

WO2006113704A3 SUBTITUTED HETEROARYL CB1 ANTAGONISTS 审中-公开
标题翻译：被诱发的异常CB1拮抗剂
公开(公告)号：WO2006113704A3
公开(公告)日：2007-02-08
申请号：PCT/US2006014548
申请日：2006-04-18
申请人： NEUROGEN CORP , YUAN JUN , GUO QIN , ZHAO HE , HU SHAOJING , WHITEHOUSE DARREN , FRINGLE WALLACE , MAO JIANMIN , MAYNARD GEORGE , HAMMER JACK , WUSTROW DAVID , LI HONGBIN
发明人： YUAN JUN , GUO QIN , ZHAO HE , HU SHAOJING , WHITEHOUSE DARREN , FRINGLE WALLACE , MAO JIANMIN , MAYNARD GEORGE , HAMMER JACK , WUSTROW DAVID , LI HONGBIN
IPC分类号： C07D401/04 , A61K31/4965 , A61K31/497 , A61K31/53 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/14 , C07D417/04 , C07D417/14
CPC分类号： C07D403/14 , C07D213/28 , C07D213/61 , C07D213/74 , C07D239/42 , C07D239/54 , C07D241/12 , C07D241/20 , C07D241/24 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14
摘要： Compounds of Formula (I) are provided. In which the variables are as described herein. Such compounds may be used to modulate CBl activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CBl modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such Iigands for receptor localization studies and various in vitro assays.
摘要翻译：提供式（I）的化合物。其中变量如本文所述。这种化合物可用于体内或体外调节CB1活性，并且特别可用于治疗对人类，驯养的伴侣动物和家畜动物中的CB1调节有反应的病症，包括食欲障碍，肥胖症和成瘾性疾病。还提供了使用它们治疗这种病症的药物组合物和方法，以及使用这些液体用于受体定位研究和各种体外测定的方法。

4. 发明申请

WO2005110416A3 4,5-DISUBSTITUTED-2-ARYL PYRIMIDINES 审中-公开
公开(公告)号：WO2005110416A3
公开(公告)日：2006-04-13
申请号：PCT/US2005015897
申请日：2005-05-06
申请人： NEUROGEN CORP , MAYNARD GEORGE D , GHOSH MANUKA , YUAN JUN , CURRIE KEVIN S , MITCHELL SCOTT , GUO QIN , ZHAO HE
发明人： MAYNARD GEORGE D , GHOSH MANUKA , YUAN JUN , CURRIE KEVIN S , MITCHELL SCOTT , GUO QIN , ZHAO HE
IPC分类号： A61K31/505 , C07D239/26 , C07D239/28 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D417/04 , C07D471/04 , C07D498/04 , A61K31/506 , C07D43/04
CPC分类号： A61K31/505 , C07D239/26 , C07D239/28 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D417/04 , C07D471/04 , C07D498/04
摘要： 4,5-disubstituted-2-arylpyrimidines of Formula (I) and Formula (II) are provided: wherein R 1 , R 2 , R 3 , R 8 , R 9 , A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I and II bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 4,5-disubstituted-2-arylpyrimidines, which are useful as probes for the localization of C5a receptors.
摘要翻译：提供式（I）和式（II）的4,5-二取代-2-芳基嘧啶：其中R 1，R 2，R 3， R 8，R 8，R 9，A和Ar如本文所定义。这些化合物是C5a受体的配体。优选的式I和II化合物以高亲和力结合C5a受体，并在C5a受体上呈现中性拮抗剂或反向活性。本发明还涉及包含这些化合物的药物组合物，以及这些化合物在治疗各种炎性，心血管和免疫系统疾病中的用途。此外，本发明提供标记的4,5-二取代-2-芳基嘧啶，其可用作C5a受体定位的探针。

6. 发明申请

WO0249993A3 HIGH AFFINITY SMALL MOLECULE C5A RECEPTOR MODULATORS 审中-公开
标题翻译：高亲和力小分子C5A受体调节剂
公开(公告)号：WO0249993A3
公开(公告)日：2003-02-20
申请号：PCT/US0026816
申请日：2000-09-29
申请人： NEUROGEN CORP , THURKAUF ANDREW , ZHANG XIAOYAN , HE XIA-SHU , ZHAO HE , PETERSON JOHN , MAYNARD GEORGE , OHLIGER ROBERT
发明人： THURKAUF ANDREW , ZHANG XIAOYAN , HE XIA-SHU , ZHAO HE , PETERSON JOHN , MAYNARD GEORGE , OHLIGER ROBERT
IPC分类号： C12N15/09 , A61K31/165 , A61K31/166 , A61K31/216 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/402 , A61K31/415 , A61K31/4155 , A61K31/417 , A61K31/4178 , A61K31/4184 , A61K31/427 , A61K31/437 , A61K31/44 , A61K31/4418 , A61K31/4439 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/4965 , A61P1/04 , A61P3/10 , A61P7/00 , A61P7/04 , A61P7/06 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P21/04 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/04 , A61P37/02 , A61P37/06 , C07C233/73 , C07D207/32 , C07D207/327 , C07D213/38 , C07D215/12 , C07D217/04 , C07D217/06 , C07D217/14 , C07D217/16 , C07D231/12 , C07D233/54 , C07D233/64 , C07D235/18 , C07D235/30 , C07D317/58 , C07D333/24 , C07D333/28 , C07D333/54 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12 , C07D471/04 , C07D521/00 , C12Q1/02 , C07D215/00 , C07D233/02 , C07D235/02 , C07D317/44 , C07D405/00 , C07D419/00 , C07D471/02
CPC分类号： C07D207/327 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/44 , A61K31/47 , C07D217/04 , C07D231/12 , C07D233/56 , C07D233/64 , C07D249/08 , C07D333/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D471/04
摘要： The invention includes low molecular weight, non-peptidic, non-peptidommetic, organic molecules that can act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also such ligands that can 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 vivo effect; 4) comprise fewer than four or preferably no amide bonds, and 5) capable of habiting leukocyte chemotaxis at nanomolar or sub-nanomolar concentrations. The invention also includes pharmaceutical composition comprising such compounds and the use of such compounds in treating a variety of inflammatory and immune system disorders.
摘要翻译：本发明包括可以充当哺乳动物补体C5a受体的调节剂的低分子量非肽，非肽，有机分子，优选用作高亲和力C5a受体配体的那些，以及可以作为拮抗剂或反向激动剂的这种配体的补体C5a受体。本发明优选的化合物具有一些或全部以下性质，因为它们是：1）结构上的多芳基; 2）结构中的杂芳基; 3）药学上可接受的口服剂量可以提供可检测的体内效应; 4）包含少于四个或优选不存在酰胺键，以及5）能够以纳摩尔或亚纳摩尔浓度吸收白细胞趋化性。本发明还包括包含这些化合物的药物组合物和这些化合物在治疗各种炎性和免疫系统疾病中的用途。

7. 发明专利

JP2011219476A HIGH AFFINITY SMALL MOLECULE C5a RECEPTOR MODULATOR 审中-公开
标题翻译：高亲和力小分子C5a受体调节剂
公开(公告)号：JP2011219476A
公开(公告)日：2011-11-04
申请号：JP2011092825
申请日：2011-04-19
申请人： Neurogen Corp , ニューロジェン・コーポレーション
发明人： THURKAUF ANDREW , ZHANG XIAOYAN , HE XIA-SHU , ZHAO HE , PETERSON JOHN , MAYNARD GEORGE , OHLIGER ROBERT
IPC分类号： C07D233/64 , A61K31/417 , A61K31/4178 , A61K31/437 , A61K31/4439 , A61K31/4709 , A61P1/04 , A61P3/10 , A61P3/14 , A61P7/02 , A61P9/10 , A61P11/00 , A61P11/08 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/04 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07B61/00 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D471/04 , C12N15/09 , C12Q1/02
摘要： PROBLEM TO BE SOLVED: To provide low molecular weight, non-peptidic, non-peptidomimetic, organic compounds that can act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also such ligands that can act as antagonists or inverse agonists of complement C5a receptors.SOLUTION: The compound possesses the following properties: (1) a polycyclic aryl structure; (2) a heteroaryl structure; (3) a pharmaceutically acceptable oral dose which can detect an effect in vivo; (4) amide bonds fewer than four or preferably no amide bonds, and (5) inhibitory capacity inhibiting leukocyte chemotaxis at nanomolar, preferably sub-nanomolar concentration. There also are provided pharmaceutical compositions comprising such compounds and the use of such compositions in treating a variety of inflammatory and immune system disorders.
摘要翻译：要解决的问题：提供可用作哺乳动物补体C5a受体调节剂的低分子量，非肽，非拟肽，有机化合物，优选作为高亲和力C5a受体配体的调节剂，以及这些配体，可以作为补体C5a受体的拮抗剂或反向激动剂。化合物具有以下性质：（1）多环芳基结构; （2）杂芳基结构; （3）可以检测体内效果的药学上可接受的口服剂量; （4）酰胺键少于四个或优选不含酰胺键，和（5）抑制能力，抑制纳摩尔，优选亚纳摩尔浓度下的白细胞趋化性。还提供包含这些化合物的药物组合物和这些组合物在治疗各种炎性和免疫系统疾病中的用途。版权所有（C）2012，JPO＆INPIT

8. 发明申请

WO2006119703A3 LASER COORDINATE DRILLING MACHINE 审中-公开
标题翻译：激光坐标钻机
公开(公告)号：WO2006119703A3
公开(公告)日：2007-01-11
申请号：PCT/CN2006000932
申请日：2006-05-10
申请人： ZHAO HE , RUI BO
发明人： ZHAO HE , RUI BO
IPC分类号： B23B49/00 , B23Q17/22
CPC分类号： B23B49/00 , B23Q17/2404 , B23Q17/2423
摘要： A laser coordinate drilling machine comprises a base, a stand, a headstock and two planar laser beam generators, etc. The laser beam generators are mounted on the stand or the headstock directly or through one or two fixers. The midline of one generator is located on the fore-and-aft central plane of the spindle and the midline of the other generator is located on the right-and-left central plane of the spindle. The two generators are mounted downwards or aslant with respect to the spindle. The generated planar laser beams are superposed with the fore-and-aft and right-and-left central planes. Said laser beam generator comprises a laser generator, which can generate straight beam, and a lens for broadening the beam that is mounted in front of the laser generator. Due to the lenses, the two laser beams can form integrated X-Y rectangular coordinates, which includes X-axis, Y-axis and their scales and characters on the table. The drilling machine can position rapidly and exactly the place of the drilling hole and can adjust the position of the work quantificationally on the basis of the rectangular coordinates. It is so convenient and rapid that it can be applied widely on the drilling machine, the drilling and milling machine and other machines for boring hole.
摘要翻译：激光坐标钻机包括基座，支架，主轴箱和两个平面激光束发生器等。激光束发生器直接或通过一个或两个固定器安装在支架或主轴箱上。一个发电机的中线位于主轴的前后中心平面上，另一台发电机的中线位于主轴的左右中心平面上。两个发电机相对于主轴向下或向下安装。产生的平面激光束与前后左右中心平面叠加。所述激光束发生器包括可产生直射束的激光发生器和用于使安装在激光发生器前面的光束变宽的透镜。由于这些镜头，两个激光束可以形成X-Y直角坐标，包括X轴，Y轴及其刻度和字符在桌子上。钻机可以快速，准确地定位钻孔的位置，并可以根据直角坐标定量调整工件的位置。这样方便快捷，可广泛应用于钻孔机，钻铣床等钻孔机。

9. 发明申请

WO2005023806A2 HETEROARYL FUSED PYRIDINES, PYRAZINES AND PYRIMIDINES AS CRF1 RECEPTOR LIGANDS 审中-公开
标题翻译：作为CRF1受体配体的异氟烷基吡啶，吡咯烷和吡咯烷
公开(公告)号：WO2005023806A2
公开(公告)日：2005-03-17
申请号：PCT/US2004028899
申请日：2004-09-03
申请人： NEUROGEN CORP , AVENTIS PHARMA INC
发明人： GE PING , HORVATH RAYMOND F , ZHANG LU YAN , YAMAGUCHI YASUCHIKA , KAISER BERND , ZHANG XUECHUN , ZHANG SUOMING , ZHAO HE , JOHN STANLY , MOORCROFT NEIL , SHUTSKE GREG
IPC分类号： A61K31/437 , A61K31/4375 , A61K31/4985 , C07D471/04 , C07D487/04 , C07D519/00 , C07D471/00
CPC分类号： C07D471/04 , C07D487/04
摘要： Substituted heteroaryl fused pyridine, pyrazine, and pyrimidine compounds that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
摘要翻译：提供了作为CRF 1受体的选择性调节剂的取代的杂芳基稠合的吡啶，吡嗪和嘧啶化合物。这些化合物可用于治疗许多中枢神经系统和周围疾病，特别是压力，焦虑，抑郁，心血管疾病和进食障碍。还提供了治疗这种疾病以及包装的药物组合物的方法。本发明的化合物也可用作CRF受体定位的探针，并且作为用于CRF受体结合的测定中的标准物。给出了在受体定位研究中使用化合物的方法。

10. 发明公开

EP1745033A4 4,5-DISUBSTITUTED-2-ARYL PYRIMIDINES 审中-公开
标题翻译： 4.5二取代的2-芳基嘧啶类
公开(公告)号：EP1745033A4
公开(公告)日：2009-08-26
申请号：EP05746687
申请日：2005-05-06
申请人： NEUROGEN CORP
发明人： MAYNARD GEORGE D , GHOSH MANUKA , YUAN JUN , CURRIE KEVIN S , MITCHELL SCOTT , GUO QIN , ZHAO HE
IPC分类号： C07D401/04 , A61K31/505 , A61K31/506 , C07D239/26 , C07D239/28 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D417/04 , C07D471/04 , C07D498/04
CPC分类号： A61K31/505 , C07D239/26 , C07D239/28 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D417/04 , C07D471/04 , C07D498/04
摘要： 4,5-disubstituted-2-arylpyrimidines of Formula (I) and Formula (II) are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I and II bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 4,5-disubstituted-2-arylpyrimidines, which are useful as probes for the localization of C5a receptors.

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