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11. 发明授权

US06448257B1 Compounds and methods to treat cardiac failure and other disorders 有权
标题翻译：治疗心力衰竭和其他疾病的化合物和方法
公开(公告)号：US06448257B1
公开(公告)日：2002-09-10
申请号：US09535316
申请日：2000-03-24
申请人： Babu J. Mavunkel , David Y. Liu , George F. Schreiner , John A. Lewicki
发明人： Babu J. Mavunkel , David Y. Liu , George F. Schreiner , John A. Lewicki
IPC分类号： A61K31437
CPC分类号： C07D209/08 , C07D209/24 , C07D235/06 , C07D401/06 , C07D401/14 , C07D403/06 , C07D471/04
摘要： Compounds of the formula: wherein the dotted line represents an optional bond; and the pharmaceutically acceptable salts thereof, wherein X1 is an alkyl bridge optionally containing an O, S, or N heteroatom that forms an aliphatic 5-7 membered ring and is optionally substituted by one or more of halo, OR, SR, NR2, RCO, COOR, CONR2, OOCR, or NROCR where R is H or alkyl (1-6C), or by one or more CN or═O, or by one or more aliphatic or aromatic 5- or 6-membered rings optionally containing 1-2 heteroatoms; R1 is wherein X2 is CO or an isostere thereof; m is 0 or 1; Y is optionally substituted alkyl, optionally substituted aryl, or optionally substituted arylalkyl or two Y taken together may form an alkylene (2-3C) bridge; n is 0-4; Z1 is CH or N; X3 is CH or CHR where R is H or alkyl (1-6C), or an isostere thereof; and Ar, R2 and R3 are as defined in the specification. These compounds are selective inhibitors of p38&agr; kinase.
摘要翻译：下式的化合物：其中虚线表示任选的键;及其药学上可接受的盐，其中X 1是任选地含有O，S或N杂原子的烷基桥，其形成脂族5-7元环并任选被取代其中R是H或烷基（1-6C），或一个或多个CN或= O，或一个或多个卤素，OR，SR，NR 2，RCO，COOR，CONR 2，OOCR或NROCR 任选含有1-2个杂原子的脂族或芳族五元或六元环; R 1是其中X 2是CO或其等价物; m是0或1; Y是任选取代的烷基，任选取代的芳基或任选取代的芳基烷基或两个Y 一起可以形成亚烷基（2-3C）桥; n为0-4; Z1为CH或N; X3为CH或CHR，其中R为H或烷基（1-6C）或其等同体; 并且Ar，R 2和R 3如本说明书中所定义。这些化合物是p38alpha激酶的选择性抑制剂。

12. 发明授权

US06130235A Compounds and methods to treat cardiac failure and other disorders 有权
标题翻译：治疗心力衰竭和其他疾病的化合物和方法
公开(公告)号：US06130235A
公开(公告)日：2000-10-10
申请号：US128137
申请日：1998-08-03
申请人： Babu J. Mavunkel , John A. Lewicki , David Y. Liu , George F. Schreiner
发明人： Babu J. Mavunkel , John A. Lewicki , David Y. Liu , George F. Schreiner
IPC分类号： C07D209/08 , C07D235/06 , C07D401/06 , C07D401/14 , C07D403/06 , A61K31/445
CPC分类号： C07D209/08 , C07D235/06 , C07D401/06 , C07D401/14 , C07D403/06
摘要： The invention is directed to compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein Ar.sup.1 is indole, benzimidazole, or benzotriazole, optionally substituted with lower alkyl (1-4C), halo, or lower alkoxy (1-4C);X.sup.1 is CO or an isostere thereof;Y is optionally substituted alkyl, optionally substituted aryl, or optionally substituted arylalkyl;n is 0 or 1;Z is CH or N;X.sup.2 is CH, CH.sub.2 or an isostere thereof; andAr.sup.2 consists of one or two phenyl moieties directly coupled to X.sup.2 and optionally substituted by halo, nitro, alkyl (1-6C), CN or CF.sub.3, or by RCO, COOR, CONR.sub.2, NR.sub.2, OR or SR, wherein R is H or alkyl (1-6C) or by phenyl, itself optionally substituted by the foregoing substituents;with the proviso that if Z is N, X.sup.1 is CO, and Ar.sup.1 is indole, Ar.sup.1 must be coupled to X.sup.1 through the 2-, 5-, 6- or 7-position.These compounds are useful in the treatment of conditions associated with inflammation. In addition, the above compounds and other compounds described herein are useful in treating conditions associated with cardiac failure.
摘要翻译：本发明涉及下式的化合物及其药学上可接受的盐，其中Ar 1是任选被低级烷基（1-4C），卤素或低级烷氧基（1-4C）取代的吲哚，苯并咪唑或苯并三唑; X1是CO或其等离子体; Y是任选取代的烷基，任选取代的芳基或任选取代的芳基烷基; n为0或1; Z是CH或N; X 2是CH，CH 2或其等价物; 并且Ar 2由直接与X 2连接并任选被卤素，硝基，烷基（1-6C），CN或CF 3或RCO，COOR，CONR2，NR2，OR或SR取代的一个或两个苯基部分组成，其中R为H 或烷基（1-6C）或苯基，其本身任选被上述取代基取代; 条件是如果Z是N，则X1是CO，Ar1是吲哚，Ar1必须通过2-，5-，6-或7-位与X1连接。这些化合物可用于治疗与炎症相关的病症。此外，本文所述的上述化合物和其它化合物可用于治疗与心力衰竭相关的病症。

13. 发明授权

US08314059B2 Diabetic nephropathy therapies 有权
标题翻译：糖尿病肾病治疗
公开(公告)号：US08314059B2
公开(公告)日：2012-11-20
申请号：US12802373
申请日：2010-06-03
申请人： Allan Flyvbjerg , Guangjie Guo , David Y. Liu , Thomas B. Neff , Noelynn A. Oliver , William R. Usinger , Qingjian Wang
发明人： Allan Flyvbjerg , Guangjie Guo , David Y. Liu , Thomas B. Neff , Noelynn A. Oliver , William R. Usinger , Qingjian Wang
IPC分类号： A61K38/00 , A61K38/17
CPC分类号： A61K38/556 , A61K31/00 , A61K39/395 , A61K2039/505 , C07K16/22 , A61K2300/00
摘要： The present invention relates to methods and compounds for treating specific early stage aspects and late stage aspects of diabetic nephropathy. Methods and compounds for treating various physiological features associated with early stage and with late stage diabetic nephropathy are also provided.
摘要翻译：本发明涉及用于治疗糖尿病肾病的特异性早期方面和晚期方面的方法和化合物。还提供了用于治疗与早期和晚期糖尿病肾病相关的各种生理特征的方法和化合物。

14. 发明授权

US07268139B2 Methods of promoting osteogenesis 有权
标题翻译：促进成骨的方法
公开(公告)号：US07268139B2
公开(公告)日：2007-09-11
申请号：US10651934
申请日：2003-08-29
申请人： Andrew A. Protter , David Y. Liu , Patrick O'Connor
发明人： Andrew A. Protter , David Y. Liu , Patrick O'Connor
IPC分类号： A61K31/497 , A61K31/445 , A61K31/415 , A61K31/38 , A61K31/385
CPC分类号： A61K31/404 , A61K31/4164 , A61K31/4174 , A61K31/4178 , A61K31/445 , A61K31/454 , A61K31/496 , A61K31/501 , A61K31/517 , A61K31/53
摘要： The invention is directed to methods of bone healing by administering a p38 MAP kinase inhibitor. The invention is directed to methods of treating bone fractures, bone diseases, bone grafting, especially enhancing bone healing following facial reconstruction, maxillary reconstruction, mandibular reconstruction or tooth extraction, enhancing long bone extension, enhancing prosthetic ingrowth, and increasing bone synostosis by administering a p38 MAP kinase inhibitor.
摘要翻译：本发明涉及通过施用p38MAP激酶抑制剂的骨愈合方法。本发明涉及治疗骨折，骨疾病，骨移植，特别是增强面部重建后的骨愈合，上颌骨重建，下颌骨重建或拔牙，增强长骨延伸，增强假体向内生长以及增加骨愈合的方法，通过施用 p38 MAP激酶抑制剂。

15. 发明申请

US20120039882A1 Vascular Disease Therapies 审中-公开
标题翻译：血管疾病治疗
公开(公告)号：US20120039882A1
公开(公告)日：2012-02-16
申请号：US13279086
申请日：2011-10-21
申请人： Ingrid Langsetmo Parobok , Christopher T. Jacob , David Y. Liu
发明人： Ingrid Langsetmo Parobok , Christopher T. Jacob , David Y. Liu
IPC分类号： A61K39/395 , A61P9/00 , A61K31/713 , A61K31/7088 , A61K31/7105
CPC分类号： C07K16/22 , A61K2039/505
摘要： The present invention relates to methods and agents for treating impaired vascular and cardiac function. Methods and agents for treating various physiological and pathological features associated with vascular dysfunction and cardiac dysfunction are also provided.
摘要翻译：本发明涉及治疗血管和心脏功能受损的方法和试剂。还提供了用于治疗与血管功能障碍和心脏功能障碍相关的各种生理和病理特征的方法和试剂。

16. 发明申请

US20080254487A1 Connective Tissue Growth Factor Signaling 审中-公开
标题翻译：结缔组织生长因子信号传导
公开(公告)号：US20080254487A1
公开(公告)日：2008-10-16
申请号：US10586318
申请日：2005-01-14
申请人： Stephen J. Klaus , David Y. Liu , Irina Aizman
发明人： Stephen J. Klaus , David Y. Liu , Irina Aizman
IPC分类号： G01N33/566 , C07H3/00 , C12Q1/02
CPC分类号： G01N33/74 , A61K31/737 , G01N2500/02
摘要： The present invention provides compounds and agents that modulate CTGF-mediated cell adhesion and/or binding of CTGF to cells. The invention further provides assays that may be used to identify additional modulators of CTGF-mediated cell adhesion and CTGF binding to cells, and assays that may be used to identify compounds or agents that modulate interaction of CTGF with HSPGs.
摘要翻译：本发明提供调节CTGF介导的细胞粘附和/或CTGF与细胞结合的化合物和试剂。本发明进一步提供可用于鉴定CTGF介导的细胞粘附和CTGF与细胞结合的其它调节剂的测定法，以及可用于鉴定调节CTGF与HSPG相互作用的化合物或试剂的测定法。

17. 发明申请

US20070293575A1 Compounds and methods for treatment of cancer-related anemia 审中-公开
标题翻译：用于治疗癌症相关性贫血的化合物和方法
公开(公告)号：US20070293575A1
公开(公告)日：2007-12-20
申请号：US11455202
申请日：2006-06-15
申请人： Todd W. Seeley , David Y. Liu , Stephen J. Klaus
发明人： Todd W. Seeley , David Y. Liu , Stephen J. Klaus
IPC分类号： A61K31/198
CPC分类号： A61K31/47
摘要： The invention relates to methods and compounds for treating anemia of cancer. In particular, methods for treating anemia of cancer in a subject having cancer, and methods for increasing reticulocytes, increasing hemoglobin, increasing hematocrit, and increasing red blood cell count in subjects having anemia of cancer, wherein such subjects are refractory to treatment with recombinant human erythropoietin (EPO) are encompassed herein.
摘要翻译：本发明涉及治疗癌症贫血的方法和化合物。特别地，在具有癌症的受试者中治疗癌症的贫血的方法和增加网织红细胞的方法，增加血红蛋白，增加血细胞比容，以及增加患有贫血的受试者的红细胞计数，其中这些受试者对重组人治疗是难以治疗的红细胞生成素（EPO）包括在本文中。

18. 发明授权

US08530404B2 Compounds and methods for treatment of cancer 有权
标题翻译：化合物和治疗癌症的方法
公开(公告)号：US08530404B2
公开(公告)日：2013-09-10
申请号：US11455199
申请日：2006-06-15
申请人： Todd W. Seeley , David Y. Liu , Stephen J. Klaus
发明人： Todd W. Seeley , David Y. Liu , Stephen J. Klaus
IPC分类号： A01N61/00
CPC分类号： A61K31/4745 , A61K31/00 , A61K31/19 , A61K31/195 , A61K31/63 , A61K38/16
摘要： The invention relates to methods and compounds for treating or preventing cancer. Methods for treating or preventing cancer, for inhibiting tumor growth, reducing tumor volume, inhibiting tumor progression, inhibiting metastasis, and improving survival are provided herein.
摘要翻译：本发明涉及治疗或预防癌症的方法和化合物。本文提供了治疗或预防癌症，抑制肿瘤生长，减少肿瘤体积，抑制肿瘤进展，抑制转移和改善生存的方法。

19. 发明授权

US08088381B2 Methods of treatment of cardiovascular disease using anti-CTGF agents 有权
标题翻译：使用抗CTGF药物治疗心血管疾病的方法
公开(公告)号：US08088381B2
公开(公告)日：2012-01-03
申请号：US11418624
申请日：2006-05-05
申请人： Ingrid Langsetmo Parobok , Christopher T. Jacob , David Y. Liu
发明人： Ingrid Langsetmo Parobok , Christopher T. Jacob , David Y. Liu
IPC分类号： A61K39/395 , G01N33/49
CPC分类号： C07K16/22 , A61K2039/505
摘要： The present invention relates to methods for treating impaired cardiac function. Methods for treating various physiological and pathological features associated with cardiac dysfunction by administering an agent that inhibits the expression or activity of connective tissue growth factor (CTGF) are provided.
摘要翻译：本发明涉及治疗心脏功能受损的方法。提供了通过施用抑制结缔组织生长因子（CTGF）的表达或活性的药物来治疗与心脏功能障碍相关的各种生理和病理特征的方法。

20. 发明申请

US20110015223A1 Compounds and methods for treatment of cancer-related anemia 审中-公开
标题翻译：用于治疗癌症相关性贫血的化合物和方法
公开(公告)号：US20110015223A1
公开(公告)日：2011-01-20
申请号：US12806589
申请日：2010-08-16
申请人： Todd W. Seeley , David Y. Liu , Stephen J. Klaus
发明人： Todd W. Seeley , David Y. Liu , Stephen J. Klaus
IPC分类号： A61K31/472 , A61P7/06
CPC分类号： A61K31/47
摘要： The invention relates to methods and compounds for treating anemia of cancer. In particular, methods for treating anemia of cancer in a subject having cancer, and methods for increasing reticulocytes, increasing hemoglobin, increasing hematocrit, and increasing red blood cell count in subjects having anemia of cancer, wherein such subjects are refractory to treatment with recombinant human erythropoietin (EPO) are encompassed herein.
摘要翻译：本发明涉及治疗癌症贫血的方法和化合物。特别地，在具有癌症的受试者中治疗癌症的贫血的方法和增加网织红细胞的方法，增加血红蛋白，增加血细胞比容，以及增加患有贫血的受试者的红细胞计数，其中这些受试者对重组人治疗是难以治疗的红细胞生成素（EPO）包括在本文中。

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