| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 1 | 双芳基磺酰胺衍生物 | CN200880108601.7 | 2008-09-18 | CN101808983A | 2010-08-18 | 亨丽埃塔·德姆洛; 乌尔丽克·奥布斯特森德; 坦贾·舒尔兹-加施; 马修·赖特 |
| 本发明涉及式(I)的新型双芳基磺酰胺衍生物，其中R1至R3和Y如说明书和权利要求书中所定义，以及其生理上可接受的盐和酯。这些化合物与LXRα和LXRβ结合，并且可用作药物。 | ||||||
| 2 | 氮杂杂环化合物 | CN201080034913.5 | 2010-07-22 | CN102471338B | 2014-07-02 | A·E·苏顿; N·布鲁格; T·E·理查德森; H·G·范迪维尔; B·R·胡克; R·蓝; J·波特尼克 |
| 本发明提供了式(I)的新的、被取代的氮杂杂环类化合物，它们的制备方法以及它们用于治疗过度增殖性疾病、例如癌症的用途。 | ||||||
| 3 | 荧光标记的配体 | CN200480013905.7 | 2004-03-31 | CN1860364A | 2006-11-08 | M·乔治; S·J·希尔; B·凯拉姆; R·J·米德尔顿 |
| 包含许多通式(I)所示标记非肽配体的库：(LigJL)mL(JTTag)m(JTL(JLLig)m)p，及其盐，它包含一个或多个相同或不同的配体部分Lig，它们各自通过相同或不同的接头L以及相同或不同的连接位点或连接官能团JT和JL连接到一个或多个相同或不同的标记部分Tag；其中，Lig包含GPCR配体，细胞内酶或底物的抑制剂，或者药物转运蛋白的抑制剂；L是单键或者是选自如N、O、S、P的杂原子、支链或直链饱和或不饱和的，并任选包含杂原子的C1－600烃基及其组合的任意接头部分，它们可以是单体、具有2－30个低聚重复单元的低聚物、具有超过30到至多300个聚合重复的聚合物；Tag是任何已知或新的标记底物；m各独立地选自1－3的整数；p是0－3；其特征在于，连接是在包含不同Lig、JL、L、JT和/或－Tag的化合物中的相同或不同的连接位点上，以及在包含相同Lig、JL、L、JT和/或－Tag的化合物中的不同连接位点上；及其制备方法；制备通式(I)所示库化合物或通式(IV)所示前体的方法；由所述库选择通式(I)所示化合物的方法；与其涉及药效性能的信息相关的通式(I)所示的化合物；通式(I)所示的新化合物或者通式(IV)所示的前体；其用途；与此有关的结合或抑制的方法；与此有关的荧光靶的用途；修饰的细胞表面GPCR和表达它的细胞；以及包含通式(I)所示化合物及其靶的试剂盒。 | ||||||
| 4 | 双芳基磺酰胺衍生物 | CN200880108601.7 | 2008-09-18 | CN101808983B | 2013-11-13 | 亨丽埃塔·德姆洛; 乌尔丽克·奥布斯特森德; 坦贾·舒尔兹-加施; 马修·赖特 |
| 本发明涉及式(I)的新型双芳基磺酰胺衍生物，其中R1至R3和Y如说明书和权利要求书中所定义，以及其生理上可接受的盐和酯。这些化合物与LXRα和LXRβ结合，并且可用作药物。 | ||||||
| 5 | 新的氮杂杂环化合物 | CN201080034913.5 | 2010-07-22 | CN102471338A | 2012-05-23 | A·E·苏顿; N·布鲁格; T·E·理查德森; H·G·范迪维尔; B·R·胡克; R·蓝; J·波特尼克 |
| 本发明提供了式(I)的新的、被取代的氮杂杂环类化合物，它们的制备方法以及它们用于治疗过度增殖性疾病、例如癌症的用途。 | ||||||
| 6 | 荧光标记的配体 | CN201010260894.X | 2004-03-31 | CN101962390A | 2011-02-02 | M·乔治; S·J·希尔; B·凯拉姆; R·J·米德尔顿 |
| 本发明涉及荧光标记的配体，提供了一种由如下通式(I)表示的化合物及其盐： (LigJL)mL(JTFl)m(JTL(JLLig)m)p。 | ||||||
| 7 | 荧光标记的配体 | CN200480013905.7 | 2004-03-31 | CN1860364B | 2010-09-29 | M·乔治; S·J·希尔; B·凯拉姆; R·J·米德尔顿 |
| 包含许多通式(I)所示标记非肽配体的库：(Lig JL)mL(JT Tag)m(JTL(JLLig)m)p，及其盐，它包含一个或多个相同或不同的配体部分Lig，它们各自通过相同或不同的接头L以及相同或不同的连接位点或连接官能团JT和JL连接到一个或多个相同或不同的标记部分Tag；其中，Lig包含GPCR配体，细胞内酶或底物的抑制剂，或者药物转运蛋白的抑制剂；L是单键或者是选自如N、O、S、P的杂原子、支链或直链饱和或不饱和的，并任选包含杂原子的C1-600烃基及其组合的任意接头部分，它们可以是单体、具有2-30个低聚重复单元的低聚物、具有超过30到至多300个聚合重复的聚合物；Tag是任何已知或新的标记底物；m各独立地选自1-3的整数；p是0-3；其特征在于，连接是在包含不同Lig、JL、L、JT和/或-Tag的化合物中的相同或不同的连接位点上，以及在包含相同Lig、JL、L、JT和/或-Tag的化合物中的不同连接位点上；及其制备方法；制备通式(I)所示库化合物或通式(IV)所示前体的方法；由所述库选择通式(I)所示化合物的方法；与其涉及药效性能的信息相关的通式(I)所示的化合物；通式(I)所示的新化合物或者通式(IV)所示的前体；其用途；与此有关的结合或抑制的方法；与此有关的荧光靶的用途；修饰的细胞表面GPCR和表达它的细胞；以及包含通式(I)所示化合物及其靶的试剂盒。 | ||||||
| 8 | 联吡啶化合物、过渡金属络合物和使用该过渡金属络合物的共轭芳香族化合物的制造方法 | CN200880101728.6 | 2008-06-18 | CN101772508A | 2010-07-07 | 浅海拓; 神川卓 |
| 式(1)(式中，R1、R2和R3独立地表示可以被取代的碳原子数1～10的烷基等，R4、R5、R6、R7和R8独立地表示氢原子等)所示的联吡啶化合物；使式(1)所示的联吡啶化合物与第9族、第10族或第11族过渡金属化合物接触而得到的过渡金属络合物；和共轭芳香族化合物的制造方法，其特征在于，在该过渡金属络合物的存在下使1个或2个离去基团与芳香环键合的芳香族化合物(A)、和结构与其相同的芳香族化合物(A)或与上述芳香族化合物(A)结构不同且1个或2个离去基团与芳香环键合的芳香族化合物(B)发生反应。 | ||||||
| 9 | Novel Azaheterocyclic Compounds | US13388690 | 2010-07-22 | US20120277228A1 | 2012-11-01 | Amanda E. Sutton; Nadia Brugger; Thomas E. Richardson; Harold George Vandeveer; Bayard R. Huck; Ruoxi Lan; Justin Potnick |
| The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer. | ||||||
| 10 | Aminopyridine-containing thiourea inhibitors of herpes viruses | US09804510 | 2001-03-12 | US06380243B1 | 2002-04-30 | Jonathan Bloom; Martin DiGrandi; Russell Dushin; Stanley Lang; Bryan O'Hara |
| Compounds of the formula wherein A is heteroaryl; R9-R12 are independently hydrogen, alkyl of 1 to 4 carbon atoms, perhaloalkyl of 1 to 4 carbon atoms, halogen, alkoxy of 1 to 4 carbon atoms, or cyano, or R9 and R10 or R11 and R12 may be taken together to form aryl of 5 to 7 carbon atoms; W is O, NR6, or is absent; G is aryl or heteroaryl; and X is a bond X is a bond, —NH, alkyl of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, thioalkyl of 1 to 6 carbon atoms, alkylamino of 1 to 6 carbon atoms, or (CH)J; and J is alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or benzyl; and n is an integer from 1 to 6; or a pharmaceutical salt thereof, useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus. | ||||||
| 11 | Aminopyridine-containing thiourea inhibitors of herpes viruses | US09444896 | 1999-11-22 | US06262090B1 | 2001-07-17 | Jonathan Bloom; Martin DiGrandi; Russell Dushin; Stanley Lang; Bryan O'Hara |
| Compounds of the formula wherein A is heteroaryl; R9-R12 are independently hydrogen, alkyl of 1 to 4 carbon atoms, perhaloalkyl of 1 to 4 carbon atoms, halogen, alkoxy of 1 to 4 carbon atoms, or cyano, or R9 and R10 or R11 and R12 may be taken together to form aryl of 5 to 7 carbon atoms; W is O, NR6, or is absent; G is aryl or heteroaryl; and X is a bond X is a bond, —NH, alkyl of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, thioalkyl of 1 to 6 carbon atoms, alkylamino of 1 to 6 carbon atoms, or (CH)J; and J is alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or benzyl; and n is an integer from 1 to 6; or a pharmaceutical acceptable salt thereof, useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus. | ||||||
| 12 | MAPK INHIBITORS | US15505942 | 2015-08-25 | US20170266173A1 | 2017-09-21 | Henry Krum; Peter Scammells; Bing Wang; Natalie Vinh; Jamie Simpson; David Chalmers |
| The present invention relates to certain novel substituted thiophene compounds and the finding that they display useful efficacy in the inhibition of the p38α MAPK enzyme. This provides for use of the compounds in various treatment methodologies related to MAPK inhibition, including the treatment of inflammation. | ||||||
| 13 | Bipyridine compound, transition metal complex, and method for production of conjugated aromatic compound using the transition metal complex | US12664960 | 2008-06-18 | US08293905B2 | 2012-10-23 | Taku Asaumi; Takashi Kamikawa |
| A bipyridine compound represented by the formula (1): wherein R1, R2 and R3 each independently represent a C1-C10 alkyl group which may be substituted etc., and R4, R5, R6, R7 and R8 each independently represent a hydrogen atom etc., a transition metal complex obtained by contacting a bipyridine compound represented by the formula (1) with a compound of a transition metal belonging to Group 9, 10 or 11, and a method for production of a conjugated aromatic compound comprising reacting an aromatic compound (A) wherein one or two leaving groups are bonded to an aromatic ring with an aromatic compound (A) having the same structure as that of the above-mentioned aromatic compound (A) or an aromatic compound (B) being structurally different from the above-mentioned aromatic compound (A) and having one or two leaving groups bonded to an aromatic ring, in the presence of the transition metal complex. | ||||||
| 14 | Biaryl sulfonamide derivatives | US12211835 | 2008-09-17 | US08039493B2 | 2011-10-18 | Henrietta Dehmlow; Ulrike Obst Sander; Tanja Schulz-Gasch; Matthew Wright |
| The invention is concerned with novel biaryl sulfonamide derivatives of formula (I) wherein R1 to R3 and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments. | ||||||
| 15 | BIPYRIDINE COMPOUND, TRANSITION METAL COMPLEX, AND METHOD FOR PRODUCTION OF CONJUGATED AROMATIC COMPOUND USING THE TRANSITION METAL COMPLEX | US12664960 | 2008-06-18 | US20100184978A1 | 2010-07-22 | Taku Asaumi; Takashi Kamikawa |
| A bipyridine compound represented by the formula (1): wherein R1, R2 and R3 each independently represent a C1-C10 alkyl group which may be substituted etc., and R4, R5, R6, R7 and R8 each independently represent a hydrogen atom etc., a transition metal complex obtained by contacting a bipyridine compound represented by the formula (1) with a compound of a transition metal belonging to Group 9, 10 or 11, and a method for production of a conjugated aromatic compound comprising reacting an aromatic compound (A) wherein one or two leaving groups are bonded to an aromatic ring with an aromatic compound (A) having the same structure as that of the above-mentioned aromatic compound (A) or an aromatic compound (B) being structurally different from the above-mentioned aromatic compound (A) and having one or two leaving groups bonded to an aromatic ring, in the presence of the transition metal complex. | ||||||
| 16 | Aminopyridine-containing thiourea inhibitors of herpes viruses | US09804510 | 2001-03-12 | US20020026055A1 | 2002-02-28 | Jonathan Bloom; Martin DiGrandi; Russell Dushin; Stanley Lang; Bryan O'Hara |
| Compounds of the formula 1 wherein A is heteroaryl; R9-R12 are independently hydrogen, alkyl of 1 to 4 carbon atoms, perhaloalkyl of 1 to 4 carbon atoms, halogen, alkoxy of 1 to 4 carbon atoms, or cyano, or R, and R10 or R11 and R12 may be taken together to form aryl of 5 to 7 carbon atoms; W is O, NR, or is absent; G is aryl or heteroaryl; and X is a bond X is a bond, nullNH, alkyl of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, thioalkyl of 1 to 6 carbon atoms, alkylamino of 1 to 6 carbon atoms, or (CH)J; and J is alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or benzyl; and n is an integer from 1 to 6; or a pharmaceutical salt thereof, useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus. | ||||||
| 17 | Fluorescently tagged ligand | JP2011158396 | 2011-07-19 | JP2012006935A | 2012-01-12 | GEORGE MICHAEL; HILL STEPHEN JOHN; KELLAM BARRIE; MIDDLETON RICHARD JOHN |
| PROBLEM TO BE SOLVED: To provide a library of tagged non-peptide ligands comprising one or a plurality of ligand moieties each linked to one or a plurality of different tag moieties.SOLUTION: The library comprises a plurality of tagged ligands of formula (I): (LigJ)L(JTag)(JL(JLig)). The library further comprises one or a plurality of same or different ligand moieties Lig each linked to one or a plurality of same or different tag moieties Tag via same or different linker moieties L and same or different linking site or linking functionality Jand J. In the formula (I), Lig comprises a G-protein coupled receptor ligand, an inhibitor of an intracellular enzyme or a substrate or inhibitor of a drug transporter; and L is a single bond or is any linking moiety selected from a heteroatom such as N, O, S, P. | ||||||
| 18 | Bipyridine compound, transition metal complex, and method for producing conjugated aromatic compound using the complex | JP2008158938 | 2008-06-18 | JP2009023996A | 2009-02-05 | ASAUMI HIROSHI; KAMIKAWA TAKU |
| <P>PROBLEM TO BE SOLVED: To provide a bipyridine compound, a transition metal complex, and a method for producing a conjugated aromatic compound using the complex. <P>SOLUTION: A bipyridine compound represented by formula (1) is disclosed (in the formula, R<SP>1</SP>, R<SP>2</SP>, and R<SP>3</SP>each independently represents a 1-10C alkyl group that may be substituted, a 1-5C alkoxy group that may be substituted, or a 6-10C aryl group that may be substituted; and R<SP>4</SP>, R<SP>5</SP>, R<SP>6</SP>, R<SP>7</SP>and R<SP>8</SP>each independently represents a hydrogen atom or a 1-3C alkyl group that may be substituted). <P>COPYRIGHT: (C)2009,JPO&INPIT | ||||||
| 19 | BIPYRIDINE COMPOUND, TRANSITION METAL COMPLEX, AND METHOD FOR PRODUCTION OF CONJUGATED AROMATIC COMPOUND USING THE TRANSITION METAL COMPLEX | EP08765824 | 2008-06-18 | EP2172470A4 | 2011-08-31 | ASAUMI TAKU; KAMIKAWA TAKASHI |
| 20 | BIARYL SULFONAMIDE DERIVATIVES | EP08804356.7 | 2008-09-18 | EP2205556A2 | 2010-07-14 | DEHMLOW, Henrietta; OBST SANDER, Ulrike; SCHULZ-GASCH, Tanja; WRIGHT, Matthew |
| The invention is concerned with novel biaryl sulfonamide derivatives of formula (I) wherein R1 to R3 and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments. | ||||||
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