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1. 发明授权

US08039639B2 Kinase inhibitors and methods of use thereof 有权
标题翻译：激酶抑制剂及其使用方法
公开(公告)号：US08039639B2
公开(公告)日：2011-10-18
申请号：US13020578
申请日：2011-02-03
申请人： Robert Groneberg , Laurence E. Burges , Darren Harvey , Ellen Laird , Mark C. Munson , James P. Rizzi , Martha Rodriguez , Charles Todd Eary , Daniel John Watson
发明人： Robert Groneberg , Laurence E. Burges , Darren Harvey , Ellen Laird , Mark C. Munson , James P. Rizzi , Martha Rodriguez , Charles Todd Eary , Daniel John Watson
IPC分类号： C07D231/56
CPC分类号： C07D231/40 , C07D231/56
摘要： A compound of Formula II and salts thereof are useful in the preparation of a compound of Formula I and pharmaceutically acceptable salts and prodrugs thereof.
摘要翻译：式II化合物及其盐可用于制备式I化合物及其药学上可接受的盐和前药。

2. 发明申请

US20110124878A1 KINASE INHIBITORS AND METHODS OF USE THEREOF 有权
标题翻译：激酶抑制剂及其使用方法
公开(公告)号：US20110124878A1
公开(公告)日：2011-05-26
申请号：US13020578
申请日：2011-02-03
申请人： Robert Groneberg , Laurence E. Burges , Darren Harvey , Ellen Laird , Mark C. Munson , James P. Rizzi , Martha Rodriguez , Charles Todd Eary , Daniel John Watson
发明人： Robert Groneberg , Laurence E. Burges , Darren Harvey , Ellen Laird , Mark C. Munson , James P. Rizzi , Martha Rodriguez , Charles Todd Eary , Daniel John Watson
IPC分类号： C07D231/56
CPC分类号： C07D231/40 , C07D231/56
摘要： A compound of Formula II and salts thereof are useful in the preparation of a compound of Formula I and pharmaceutically acceptable salts and prodrugs thereof.
摘要翻译：式II化合物及其盐可用于制备式I化合物及其药学上可接受的盐和前药。

3. 发明授权

US08044083B2 Kinase inhibitors and methods of use thereof 有权
标题翻译：激酶抑制剂及其使用方法
公开(公告)号：US08044083B2
公开(公告)日：2011-10-25
申请号：US12161412
申请日：2007-01-26
申请人： Robert Groneberg , Laurence E. Burgess , Darren Harvey , Ellen Laird , Mark C. Munson , James P. Rizzi , Martha Rodriguez , Charles Todd Eary , Daniel John Watson
发明人： Robert Groneberg , Laurence E. Burgess , Darren Harvey , Ellen Laird , Mark C. Munson , James P. Rizzi , Martha Rodriguez , Charles Todd Eary , Daniel John Watson
IPC分类号： A61K31/416 , C07D231/56
CPC分类号： C07D231/40 , C07D231/56
摘要： The compound of Formula (I) and pharmaceutically acceptable salts and prodrugs thereof are useful in the treatment and prevention of various disorders mediated by kinases.
摘要翻译：式（I）化合物及其药学上可接受的盐和前药可用于治疗和预防由激酶介导的各种疾病。

4. 发明申请

US20090023795A1 Kinase Inhibitors And Methods Of Use Thereof 有权
标题翻译：激酶抑制剂及其使用方法
公开(公告)号：US20090023795A1
公开(公告)日：2009-01-22
申请号：US12161412
申请日：2007-01-26
申请人： Robert Groneberg , Laurence E. Burgess , Darren Harvey , Ellen Laird , Mark C. Munson , James P. Rizzi , Martha Rodriguez , Charles Todd Eary , Daniel John Watson
发明人： Robert Groneberg , Laurence E. Burgess , Darren Harvey , Ellen Laird , Mark C. Munson , James P. Rizzi , Martha Rodriguez , Charles Todd Eary , Daniel John Watson
IPC分类号： A61K31/416 , C07D231/54 , A61P29/00 , A61P37/02 , A61P19/08 , A61P35/00 , A61P31/00 , A61P25/00
CPC分类号： C07D231/40 , C07D231/56
摘要： The compound of Formula (I) and pharmaceutically acceptable salts and prodrugs thereof are useful in the treatment and prevention of various disorders mediated by kinases.
摘要翻译：式（I）化合物及其药学上可接受的盐和前药可用于治疗和预防由激酶介导的各种疾病。

5. 发明授权

US08268871B2 Mitotic kinesin inhibitors and methods of use thereof 有权
标题翻译：有丝分裂驱动蛋白抑制剂及其使用方法
公开(公告)号：US08268871B2
公开(公告)日：2012-09-18
申请号：US12822066
申请日：2010-06-23
申请人： Jeremy Hans , Eli M. Wallace , Qian Zhao , Shelley Allen , Ellen Laird , Joseph P. Lyssikatos , John E. Robinson , Christopher P. Corrette , Robert Kirk DeLisle , Walter C. Voegtli
发明人： Jeremy Hans , Eli M. Wallace , Qian Zhao , Shelley Allen , Ellen Laird , Joseph P. Lyssikatos , John E. Robinson , Christopher P. Corrette , Robert Kirk DeLisle , Walter C. Voegtli
IPC分类号： A61K31/41 , C07D417/04
CPC分类号： C07D513/04 , C07D285/12 , C07D417/04 , C07D417/14 , C07D419/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D497/04 , C07F9/65395
摘要： This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
摘要翻译：本发明涉及有丝分裂驱动蛋白抑制剂，特别是KSP，以及制备这些抑制剂的方法。本发明还提供包含本发明抑制剂的药物组合物和利用抑制剂和药物组合物治疗和预防各种疾病的方法。

6. 发明申请

US20060199826A1 Cyclopropane compounds and pharmaceutical use thereof 失效
标题翻译：环丙烷化合物及其药物用途
公开(公告)号：US20060199826A1
公开(公告)日：2006-09-07
申请号：US11011773
申请日：2004-12-15
申请人： Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole Littmann , Katsutaka Yasue , Steven Andrews , Atushi Sakai , Andrew Fryer , Takafumi Matsuo , Ellen Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
发明人： Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole Littmann , Katsutaka Yasue , Steven Andrews , Atushi Sakai , Andrew Fryer , Takafumi Matsuo , Ellen Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
IPC分类号： A61K31/496 , A61K31/4436 , A61K31/416 , C07D49/02
CPC分类号： C07C311/29 , C07C311/13 , C07C311/20 , C07C311/22 , C07C311/46 , C07C2601/02 , C07C2601/14 , C07C2603/08 , C07C2603/18 , C07C2603/30 , C07D205/04 , C07D207/48 , C07D209/44 , C07D211/58 , C07D211/96 , C07D213/18 , C07D213/65 , C07D213/71 , C07D213/74 , C07D213/81 , C07D213/82 , C07D217/08 , C07D231/12 , C07D233/64 , C07D237/12 , C07D239/22 , C07D243/08 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/107 , C07D277/26 , C07D277/36 , C07D277/82 , C07D295/26 , C07D307/79 , C07D307/91 , C07D333/18 , C07D333/34 , C07D333/36 , C07D333/38 , C07D333/62 , C07D401/04 , C07D409/04 , C07D409/12 , C07D413/04 , C07D417/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X1 is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1-(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有聚集蛋白聚糖蛋白聚糖酶抑制活性和MMP-13抑制活性的化合物，可用作骨关节炎，类风湿性关节炎等的治疗剂，更具体而言，可以使用式（1）的环丙烷化合物：其中R 1 是 - （CH 2）2 -X-（CH 2）n - SUP> 1等，其中m和n相同或不同，并且各自为0至6，X 1是单键等，而A 1， SUP>是取代的C 3-14烃环基等; R 2和R 3相同或不同，并且各自为氢原子， - （CH 2）2 N 其中p和q为 - （CH 2）2 - - - - CH 2 - 相同或不同，并且各自为0至6，X 1为单键等，而A 2为任选取代的C 3-14烷基，烃环等; R 4是-CO 2 R 9等，其中R 9是氢原子等。 ; 和R 20和R 21相同或不同，各自为氢原子， - （CH 2 CH 2）m 12 其中m12和m12（其中m12和m12）相同或不同，各自为0至6，X 12为单键等，R 30为氢原子等; 或其前药或其药学上可接受的盐。

7. 发明授权

US06646737B2 Submicron dimensional calibration standards and methods of manufacture and use 有权
标题翻译：亚微米尺寸校准标准和制造和使用方法
公开(公告)号：US06646737B2
公开(公告)日：2003-11-11
申请号：US09961629
申请日：2001-09-24
申请人： Marco Tortonese , Ian Smith , Ellen Laird , Bradley W. Scheer
发明人： Marco Tortonese , Ian Smith , Ellen Laird , Bradley W. Scheer
IPC分类号： G01R3126
CPC分类号： G01Q40/02 , H01J2237/30444
摘要： A calibration standard which may be used to calibrate lateral dimensional measurement systems is provided. The calibration standard may include a first substrate spaced from a second substrate. In addition, the calibration standard may include at least one layer disposed between the first and second substrates. The layer may have a traceably measured thickness. For example, a thickness of the layer may be traceably measured using any measurement technique in which a measurement system may be calibrated with a standard reference material traceable to a national testing authority. The calibration standard may be cross-sectioned in a direction substantially perpendicular to an upper surface of the first substrate. The cross-sectioned portion of the calibration standard may form a viewing surface of the calibration standard. In this manner, a lateral dimensional artifact of the calibration standard may include the traceably measured thickness of at least the one layer.
摘要翻译：提供了可用于校准横向尺寸测量系统的校准标准。校准标准可以包括与第二衬底间隔开的第一衬底。此外，校准标准可以包括设置在第一和第二基板之间的至少一层。该层可以具有可追溯测量的厚度。例如，可以使用任何测量技术来可追溯地测量该层的厚度，其中可以使用可追溯到国家检测机构的标准参考材料校准测量系统。校准标准可以在基本上垂直于第一衬底的上表面的方向上横截面。校准标准的横截面部分可以形成校准标准的观察表面。以这种方式，校准标准的横向尺寸伪影可以包括至少一层的可追溯测量的厚度。

8. 发明申请

US20130131039A1 5,7-SUBSTITUTED-IMIDAZO[1,2-C]PYRIMIDINES AS INHIBITORS OF JAK KINASES 有权
标题翻译：作为JAK KINASES的抑制剂的5,7-取代的咪唑并[1,2-C]吡啶
公开(公告)号：US20130131039A1
公开(公告)日：2013-05-23
申请号：US13640099
申请日：2011-04-11
申请人： Laurence E. Burgess , Mark Laurence Boys , Robert D. Groneberg , Darren M. Harvey , Timothy Kercher , Christopher F. Kraser , Ellen Laird , Eugene Tarlton , Qian Zhao , Lily Huang
发明人： Laurence E. Burgess , Mark Laurence Boys , Robert D. Groneberg , Darren M. Harvey , Timothy Kercher , Christopher F. Kraser , Ellen Laird , Eugene Tarlton , Qian Zhao , Lily Huang
IPC分类号： C07D487/04 , C07D498/04
CPC分类号： C07D487/04 , C07D498/04
摘要： Compounds of Formula I: (Formula should be inserted here) and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, R7, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
摘要翻译：式I化合物（此处应该插入式）及其其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，X 1和X 2具有本说明书中给出的含义的立体异构体及其药学上可接受的盐和溶剂化物是抑制剂的一种或多种JAK激酶，并且可用于治疗自身免疫性疾病，炎性疾病，移植器官，组织和细胞的排斥，以及血液系统疾病和恶性肿瘤及其并发症。

9. 发明申请

US20130109656A1 MITOTIC KINESIN INHIBITORS AND METHODS OF USE THEREOF 有权
公开(公告)号：US20130109656A1
公开(公告)日：2013-05-02
申请号：US13586355
申请日：2012-08-15
申请人： Jeremy Hans , Eli M. Wallace , Qian Zhao , Shelley Allen , Ellen Laird , Joseph P. Lyssikatos , John E. Robinson , Christopher P. Corrette , Robert Kirk DeLisle , Walter C. Voegtli
发明人： Jeremy Hans , Eli M. Wallace , Qian Zhao , Shelley Allen , Ellen Laird , Joseph P. Lyssikatos , John E. Robinson , Christopher P. Corrette , Robert Kirk DeLisle , Walter C. Voegtli
IPC分类号： C07F9/6539 , C07D419/04 , C07D513/04 , C07D417/04
CPC分类号： C07D513/04 , C07D285/12 , C07D417/04 , C07D417/14 , C07D419/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D497/04 , C07F9/65395
摘要： This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.

10. 发明授权

US07795282B2 Mitotic kinesin inhibitors and methods of use thereof 有权
标题翻译：有丝分裂驱动蛋白抑制剂及其使用方法
公开(公告)号：US07795282B2
公开(公告)日：2010-09-14
申请号：US11415455
申请日：2006-05-01
申请人： Jeremy Hans , Eli M. Wallace , Qian Zhao , Shelley Allen , Ellen Laird , Joseph P. Lyssikatos , John E. Robinson , Christopher P. Corrette , Robert Kirk DeLisle , Walter C. Voegtli
发明人： Jeremy Hans , Eli M. Wallace , Qian Zhao , Shelley Allen , Ellen Laird , Joseph P. Lyssikatos , John E. Robinson , Christopher P. Corrette , Robert Kirk DeLisle , Walter C. Voegtli
IPC分类号： A61K31/41 , C07D285/14
CPC分类号： C07D513/04 , C07D285/12 , C07D417/04 , C07D417/14 , C07D419/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D497/04 , C07F9/65395
摘要： This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
摘要翻译：本发明涉及有丝分裂驱动蛋白抑制剂，特别是KSP，以及制备这些抑制剂的方法。本发明还提供包含本发明抑制剂的药物组合物和利用抑制剂和药物组合物治疗和预防各种疾病的方法。

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