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公开(公告)号:US06277989B1
公开(公告)日:2001-08-21
申请号:US09525034
申请日:2000-03-14
申请人: Sarvajit Chakravarty , Sundeep Dugar , John J. Perumattam , George F. Schreiner , David Y. Liu , John A. Lewicki
发明人: Sarvajit Chakravarty , Sundeep Dugar , John J. Perumattam , George F. Schreiner , David Y. Liu , John A. Lewicki
IPC分类号: C07D23942
CPC分类号: C07D401/12 , A61K31/519 , C07D239/94 , C07D471/04
摘要: The invention is directed to methods to inhibit TGF-&bgr; and/or p38-&agr; kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar′ is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.
摘要翻译: 本发明涉及使用下式的化合物或其药学上可接受的盐抑制TGF-β和/或p38-α激酶的方法,其中R3是不干扰取代基;每个Z是CR2或N,其中环中不超过两个Z位置 A是N,并且其中环A中的两个相邻Z位不能是N;每个R2独立地是非干扰取代基; L是连接基; n是0或1; 并且Ar'是任选被1-3个非干扰取代基取代的环状脂族,环状杂脂族,芳族或杂芳族部分的残基。
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公开(公告)号:US06184226B2
公开(公告)日:2001-02-06
申请号:US09141916
申请日:1998-08-28
申请人: Sarvajit Chakravarty , John J. Perumattam , George F. Schreiner , David Y. Liu , John A. Lewicki
发明人: Sarvajit Chakravarty , John J. Perumattam , George F. Schreiner , David Y. Liu , John A. Lewicki
IPC分类号: A01N5500
CPC分类号: C07D401/12 , A61K31/519 , C07D239/94 , C07D471/04
摘要: The invention describes compounds of the formula and the pharmaceutically acceptable salts thereof and the pharmaceutically acceptable salts thereof wherein each R2 is independently a noninterfering substituent; m is an integer of 0-4; Z is CH or N; R1 is H, alkyl (1-6C) or arylalkyl optionally substituted on the aryl group with 1-3 substituents independently selected from alkyl (1-6C), halo, OR, NR2, SR, —OOCR, —NROCR, RCO, —COOR, —CONR2, —SO2NR2, CN, CF3, and NO2, wherein each R is independently H or lower alkyl (1-4C); n is 0, 1 or 2; Ar is phenyl, pyridyl, indolyl, or pyrimidyl, each optionally substituted with a group selected from the group consisting of optionally substituted alkyl (1-6C), halo, OR, NR2, SR, —OOCR, —NROCR, RCO, —COOR, —CONR2, SO2NR2, CN, CF3, and NO2, wherein each R is independently H or lower alkyl (1-4C); and R3 is a branched or cyclic alkyl group (5-7C) or is phenyl optionally substituted with 1-2 substituents which substituents are selected from the group consisting of alkyl (1-6C), halo, OR, NR2, SR, —OOCR, —NROCR, RCO, —COOR, —CONR2, —SO2NR2, CN, CF3, and NO2, wherein each R is independently H or lower alkyl (1-4C) which are useful as antiinflammatories and in treating cardiac disorders.
摘要翻译: 本发明描述了下式的化合物及其药学上可接受的盐及其药学上可接受的盐,其中R2各自独立地为非干扰性取代基; m为0-4的整数; Z为CH或N; R 1为H,烷基(1-6C) (1-6C),卤素,OR,NR2,SR,-OOCR,-NROCR,RCO,-COOR,-CONR2,-SO2NR2,CN等的任选取代的芳基, CF 3和NO 2,其中每个R独立地为H或低级烷基(1-4C); n为0,1或2; Ar为苯基,吡啶基,吲哚基或嘧啶基,各自任选被选自以下的基团取代: 任选取代的烷基(1-6C),卤素,OR,NR2,SR,-OOCR,-NROCR,RCO,-COOR,-CONR2,SO2NR2,CN,CF3和NO2,其中每个R独立地为H或低级烷基 (1-4C); 和R 3是支链或环状烷基(5-7C),或是任选被1-2个取代基取代的苯基,所述取代基选自烷基(1-6C),卤素,OR,NR2,SR,-OOCR, -NROCR,RCO,-COOR,-CONR2,-SO2NR2,CN,CF3和NO2,其中每个R独立地为H或可用作抗炎剂和治疗心脏疾病的低级烷基(1-4C)。
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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。
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14.
公开(公告)号:US08088381B2
公开(公告)日:2012-01-03
申请号:US11418624
申请日:2006-05-05
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。
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15.
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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公开(公告)号:US20100291098A1
公开(公告)日:2010-11-18
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: A61K39/395 , A61P13/12
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。
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17.
公开(公告)号:US20100204269A1
公开(公告)日:2010-08-12
申请号:US12798856
申请日:2010-04-13
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
CPC分类号: A61K45/06 , A61K31/472
摘要: The invention relates to methods and compounds for treating chemotherapy-induced anemia. In particular, methods for treating chemotherapy-induced anemia in subjects refractory to treatment with recombinant human erythropoietin are encompassed herein.
摘要翻译: 本发明涉及治疗化疗诱发性贫血的方法和化合物。 特别地,本文包括在用重组人促红细胞生成素治疗难治的受试者中治疗化疗诱导的贫血的方法。
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公开(公告)号:US07713986B2
公开(公告)日:2010-05-11
申请号:US11455200
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: A61K31/505
CPC分类号: A61K45/06 , A61K31/472
摘要: The invention relates to methods and compounds for treating chemotherapy-induced anemia. In particular, methods for treating chemotherapy-induced anemia in subjects refractory to treatment with recombinant human erythropoietin are encompassed herein.
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公开(公告)号:US07345045B2
公开(公告)日:2008-03-18
申请号:US11053121
申请日:2005-02-07
申请人: Sarvajit Chakravarty , Sundeep Dugar , John J. Perumattam , George F. Schreiner , David Y. Liu , John A. Lewicki
发明人: Sarvajit Chakravarty , Sundeep Dugar , John J. Perumattam , George F. Schreiner , David Y. Liu , John A. Lewicki
IPC分类号: A61K31/4375 , C07D471/04
CPC分类号: C07D401/12 , A61K31/519 , C07D239/94 , C07D471/04
摘要: The invention is directed to methods to inhibit TGF-β and/or p38-α kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar′ is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.
摘要翻译: 本发明涉及使用下式的化合物或其药学上可接受的盐抑制TGF-β和/或p38-α激酶的方法,其中R 3是非干扰性取代基; 每个Z是CR 2或N,其中环A中不超过两个Z位是N,并且其中环A中的两个相邻Z位不能是N; 每个R 2独立地是非干扰取代基; L是连接体; n为0或1; 并且Ar'是任选被1-3个非干扰取代基取代的环脂族,环状杂脂族,芳族或杂芳族部分的残基。
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20.
公开(公告)号:US20070292433A1
公开(公告)日:2007-12-20
申请号:US11455200
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: A61K39/395 , A61K38/46 , A61K31/7072 , A61K31/704 , A61K31/66 , A61K31/56 , A61K31/525 , A61K31/522 , A61K31/454 , A61K31/337
CPC分类号: A61K45/06 , A61K31/472
摘要: The invention relates to methods and compounds for treating chemotherapy-induced anemia. In particular, methods for treating chemotherapy-induced anemia in subjects refractory to treatment with recombinant human erythropoietin are encompassed herein.
摘要翻译: 本发明涉及治疗化疗诱发性贫血的方法和化合物。 特别地,本文包括在用重组人促红细胞生成素治疗难治的受试者中治疗化疗诱导的贫血的方法。
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