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1. 发明授权

US08394795B2 Pyrazole [3, 4-B] pyridine Raf inhibitors 失效
标题翻译：吡唑[3,4-B]吡啶Raf抑制剂
公开(公告)号：US08394795B2
公开(公告)日：2013-03-12
申请号：US12920050
申请日：2009-02-27
申请人： Kateri A. Ahrendt , Alexandre J. Buckmelter , Jason De Meese , Jonas Grina , Joshua D. Hansen , Ellen R. Laird , Paul Lunghofer , David Moreno , Brad Newhouse , Li Ren , Jeongbeob Seo , Hongqi Tian , Steven Mark Wenglowsky , Bainian Feng , Janet Gunzner , Kim Malesky , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Wendy B. Young
发明人： Kateri A. Ahrendt , Alexandre J. Buckmelter , Jason De Meese , Jonas Grina , Joshua D. Hansen , Ellen R. Laird , Paul Lunghofer , David Moreno , Brad Newhouse , Li Ren , Jeongbeob Seo , Hongqi Tian , Steven Mark Wenglowsky , Bainian Feng , Janet Gunzner , Kim Malesky , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Wendy B. Young
IPC分类号： A61K31/535 , A61K31/44 , C07D413/14 , C07D471/04
CPC分类号： C07D471/04 , C07C311/08
摘要： Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
摘要翻译：式I化合物可用于抑制Raf激酶。公开了使用式I化合物和立体异构体，互变异构体，前药和其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

2. 发明申请

US20110092479A1 PYRAZOLE [3, 4-B] PYRIDINE RAF INHIBITORS 失效
标题翻译：吡咯并[3,4-B]吡啶类RAF抑制剂
公开(公告)号：US20110092479A1
公开(公告)日：2011-04-21
申请号：US12920050
申请日：2009-02-27
申请人： Kateri A. Ahrendt , Alexandre J. Buckmelter , Jason De Meese , Jonas Grina , Joshua D. Hansen , Ellen R. Laird , Paul Lunghofer , David Moreno , Brad Newhouse , Li Ren , Jeongbeob Seo , Hongqi Tian , Steven M. Wenglowsky , Bainian Feng , Janet Gunzner , Kim Malesky , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Wendy B. Young
发明人： Kateri A. Ahrendt , Alexandre J. Buckmelter , Jason De Meese , Jonas Grina , Joshua D. Hansen , Ellen R. Laird , Paul Lunghofer , David Moreno , Brad Newhouse , Li Ren , Jeongbeob Seo , Hongqi Tian , Steven M. Wenglowsky , Bainian Feng , Janet Gunzner , Kim Malesky , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Wendy B. Young
IPC分类号： A61K31/437 , C07D471/04 , A61K31/5377 , A61K31/496 , A61P35/00 , A61P35/02 , A61P13/12
CPC分类号： C07D471/04 , C07C311/08
摘要： Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
摘要翻译：式I化合物可用于抑制Raf激酶。公开了使用式I化合物和立体异构体，互变异构体，前药和其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

3. 发明授权

US08338452B2 Raf inhibitor compounds and methods of use thereof 失效
标题翻译： Raf抑制剂化合物及其使用方法
公开(公告)号：US08338452B2
公开(公告)日：2012-12-25
申请号：US12920045
申请日：2009-02-27
申请人： Kateri A. Ahrendt , Alexandre J. Buckmelter , Jonas Grina , Joshua D. Hansen , Ellen R. Laird , David Moreno , Brad Newhouse , Li Ren , Steven M. Wenglowsky , Bainian Feng , Janet Gunzner , Kim Malesky , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Wendy B. Young
发明人： Kateri A. Ahrendt , Alexandre J. Buckmelter , Jonas Grina , Joshua D. Hansen , Ellen R. Laird , David Moreno , Brad Newhouse , Li Ren , Steven M. Wenglowsky , Bainian Feng , Janet Gunzner , Kim Malesky , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Wendy B. Young
IPC分类号： A01N43/42 , A61K31/44 , C07D471/02 , C07D491/02
CPC分类号： C07D471/04 , C07C311/08
摘要： Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
摘要翻译：式（I）的化合物可用于抑制Raf激酶。公开了使用式（I）化合物及其立体异构体，互变异构体，前药和其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

4. 发明申请

US20110110889A1 RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF 失效
标题翻译： RAF抑制剂化合物及其使用方法
公开(公告)号：US20110110889A1
公开(公告)日：2011-05-12
申请号：US12920045
申请日：2009-02-27
申请人： Kateri A. Ahrendt et al. , Alexander J. Buckmelter , Jonas Grina , Joshua D. Hansen , Ellen R. Laird , David Moreno , Brad Newhouse , Li Ren , Steven M. Wenglowsky , Bainian Feng , Janet Gunzner , Kim Malesky , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Wendy B. Young
发明人： Kateri A. Ahrendt et al. , Alexander J. Buckmelter , Jonas Grina , Joshua D. Hansen , Ellen R. Laird , David Moreno , Brad Newhouse , Li Ren , Steven M. Wenglowsky , Bainian Feng , Janet Gunzner , Kim Malesky , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Wendy B. Young
IPC分类号： A61K38/21 , C07D471/04 , C07D401/10 , C07D401/02 , A61K31/437 , A61K31/5377 , A61K31/497 , A61K39/395 , A61P35/00
CPC分类号： C07D471/04 , C07C311/08
摘要： Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
摘要翻译：式（I）的化合物可用于抑制Raf激酶。公开了使用式（I）化合物及其立体异构体，互变异构体，前药和其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

5. 发明授权

US06251620B1 Three dimensional structure of a ZAP tyrosine protein kinase fragment and modeling methods 失效
标题翻译： ZAP酪氨酸蛋白激酶片段的三维结构和建模方法
公开(公告)号：US06251620B1
公开(公告)日：2001-06-26
申请号：US08975040
申请日：1997-11-18
申请人： Marcos H. Hatada , Xiaode Lu , Ellen R. Laird , Jennifer L. Karas , Mark J. Zoller , Dennis A. Holt
发明人： Marcos H. Hatada , Xiaode Lu , Ellen R. Laird , Jennifer L. Karas , Mark J. Zoller , Dennis A. Holt
IPC分类号： C12Q148
CPC分类号： C12N9/1205
摘要： The invention relates to human ZAP-70, and in particular, to the region of ZAP-70 containing the tandem Src homology-2 (“SH2”) domains, to crystalline forms thereof, liganded or unliganded, which are particularly useful for the determination of the three-dimensional structure of the protein. The three dimensional structure of the tandem SH2 region of ZAP provides information useful for the design of pharmaceutical compositions which inhibit the biological function of ZAP and other members of the ZAP family of SH2 domain-containing proteins, particularly those biological functions mediated by molecular interactions involving one or both SH2 domains.
摘要翻译：本发明涉及人ZAP-70，特别涉及含有串联Src同源性-2（“SH2”）结构域的ZAP-70区域，其结构形式为配体或非配体，其特别可用于测定的蛋白质的三维结构。 ZAP的串联SH2区域的三维结构提供了有用的药物组合物的设计信息，该药物组合物抑制ZAP和包含SH2结构域的蛋白质的ZAP家族的其他成员的生物学功能，特别是那些通过分子相互作用介导的那些生物学功能一个或两个SH2结构域。

6. 发明授权

US07351825B2 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：US07351825B2
公开(公告)日：2008-04-01
申请号：US11011773
申请日：2004-12-15
申请人： Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafumi Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
发明人： Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafumi Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
IPC分类号： C07D265/00 , C07D295/00 , C07D237/00 , C07D409/00 , C07D411/00 , C07D217/00 , C07D211/00 , C07D213/00 , C07D271/00 , C07D413/00 , C07D498/00 , C07D277/00 , C07D257/00 , C07D233/00 , C07D231/00 , C07D207/00 , C07D333/00 , C07D307/00 , C07D303/00 , C07D309/00 , C07D311/00
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, X 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为单键等，而A 1为取代的C _{3-14个烃环基等; 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

US06696464B2 Triazolo-pyridines anti-inflammatory compounds 失效
标题翻译：三唑并吡啶抗炎化合物
公开(公告)号：US06696464B2
公开(公告)日：2004-02-24
申请号：US10094760
申请日：2002-03-11
申请人： Kim F. McClure , Michael A. Letavic , Mark A. Dombroski , Allen J. Duplantier , Ellen R. Laird
发明人： Kim F. McClure , Michael A. Letavic , Mark A. Dombroski , Allen J. Duplantier , Ellen R. Laird
IPC分类号： A61K3144
CPC分类号： C07D471/04
摘要： The present invention relates to novel triazolo-pyridines of the formula I wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen; R2 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents; R3 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents; s is an integer from 0-5; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
摘要翻译：本发明涉及式I的新型三唑并 - 吡啶，其中Het是含有一至二个选自氮，硫和氧的杂原子的任选取代的五元杂环，其中至少一个所述杂原子必须是氮; R 2，选自氢，（C 1 -C 6）烷基或其它合适的取代基; R 3选自氢，（C 1 -C 6）烷基或其它合适的取代基; s是0的整数 -5;用于制备的中间体，含有它们的药物组合物及其药物用途。本发明的化合物是MAP激酶的有效抑制剂，优选p38激酶。它们可用于治疗炎症，骨关节炎，类风湿性关节炎，癌症，中风或心脏病发作中的再灌注或缺血，自身免疫疾病和其他疾病。

8. 发明授权

US6114361A 5-oxo-pyrrolidine-2-carboxylic acid hydroxamide derivatives 失效
标题翻译： 5-氧代 - 吡咯烷-2-甲酸羟基酰胺衍生物
公开(公告)号：US6114361A
公开(公告)日：2000-09-05
申请号：US429937
申请日：1999-10-29
申请人： Ralph P. Robinson , Ellen R. Laird
发明人： Ralph P. Robinson , Ellen R. Laird
IPC分类号： C07D207/277 , A61K31/4015 , A61K31/4439 , A61P1/00 , A61P1/02 , A61P1/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/06 , A61P25/16 , A61P25/24 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/18 , A61P35/00 , A61P35/04 , A61P37/02 , A61P37/08 , A61P43/00 , C07D207/12 , C07D207/16 , C07D207/28 , C07D401/04
CPC分类号： C07D207/28 , Y02P20/55
摘要： The present invention relates to a compound of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 are as defined above, to pharmaceutical compositions and methods of treatment.
摘要翻译：本发明涉及药物组合物和治疗方法，其中R1，R2，R3如上定义。

9. 发明申请

US20100105894A1 Cyclopropane compounds and pharmaceutical use thereof 审中-公开
标题翻译：环丙烷化合物及其药物用途
公开(公告)号：US20100105894A1
公开(公告)日：2010-04-29
申请号：US12457391
申请日：2009-06-09
申请人： Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafuml Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
发明人： Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafuml Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
IPC分类号： C07D243/08 , C07C229/02 , C07C307/00 , C07D409/02 , C07D231/10 , C07D401/02 , C07D261/06 , C07D333/34 , C07D241/04 , C07D271/06 , C07D257/04 , C07D295/00 , C07D215/14 , C07D205/04 , C07D413/02 , C07D241/36 , C07D413/14 , C07D223/14
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, X 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）所示的环丙烷化合物：其中，R 1为 - （CH 2 ）m-X-（CH 2）n -Al等，其中m和n相同或不同，各自为0〜6，X为单键等，而A1为取代的C3-14烃环基，等等。; R2和R3相同或不同，各自为氢原子， - （CH2）p-X1-（CH2）q-A2等，其中p和q相同或不同，各自为0至6，X1 是单键等，A2是任选取代的C 3-14烃环基等; R4是-CO 2 R 9等，其中R9是氢原子等; 和R 20和R 21相同或不同，各自为氢原子， - （CH 2）m 12 -X 12 - （CH 2）m 12 -R 30等，其中m12和m12相同或不同，各自为0至6， X12为单键等，R30为氢原子等; 或其前药或其药学上可接受的盐。

10. 发明申请

US20120270803A1 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：US20120270803A1
公开(公告)日：2012-10-25
申请号：US13538698
申请日：2012-06-29
申请人： Jeremy Hans , Eli M. Wallace , Qian Zhao , Joseph P. Lyssikatos , Thomas D. Aicher , Ellen R. Laird , John Robinson , Shelley Allen
发明人： Jeremy Hans , Eli M. Wallace , Qian Zhao , Joseph P. Lyssikatos , Thomas D. Aicher , Ellen R. Laird , John Robinson , Shelley Allen
IPC分类号： A61K31/433 , A61K31/4439 , A61K38/55 , A61P35/02 , A61P35/00
CPC分类号： C07D285/12 , C07D271/107 , C07D401/12 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07F9/201 , C07F9/65392
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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