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公开(公告)号：US08378100B2
公开(公告)日：2013-02-19
申请号：US12351550
申请日：2009-01-09
IPC分类号： A61K31/675 , A61K31/66 , C07F9/58 , C07F9/28 , A61P35/00
CPC分类号： C07F9/3808 , C07F9/3882
摘要： The present invention provides β-hydroxy phosphonate compounds that are autotaxin inhibitors.
摘要翻译： 本发明提供了自分泌抑素的β-羟基膦酸酯化合物。
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公开(公告)号：US20110106241A1
公开(公告)日：2011-05-05
申请号：US12896881
申请日：2010-10-02
IPC分类号： A61F2/82 , C07C233/78 , A61K31/166 , A61P35/00 , C07D271/06 , A61K31/4245 , A61P11/06 , C07D333/24 , C07D413/04 , A61K31/381 , C07D413/14 , C07D409/14 , C07D413/02 , C07D409/02 , A61P9/00
CPC分类号： C07D413/04 , C07D409/04
摘要： Amidine analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) are provided. The compounds can prevent angiogenesis in tumor cells.
摘要翻译： 提供了可以抑制鞘氨醇激酶1和鞘氨醇激酶2（SphK1和SphK2）活性的脒类似物。 该化合物可以预防肿瘤细胞中的血管生成。
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公开(公告)号：US07820703B2
公开(公告)日：2010-10-26
申请号：US11579658
申请日：2005-05-06
CPC分类号： C07F9/65515 , C07F9/091 , C07F9/094 , C07F9/3891 , C07F9/404 , C07F9/5728 , C07F9/58 , C07F9/6506
摘要： The present invention is directed to compositions comprising lysophosphatidic acid analogs and methods of using such analogs as agonist or antagonists of LPA receptor activity. In addition the invention is directed to LPA receptor agonists that vary in the degree of selectivity at individual LPA receptors (i.e. LPA1, LPA2 and LPA3). More particularly the present invention is directed to LPA analogs wherein the glycerol is replaced with ethanolamine and a variety of substitutions have been linked at the second carbon atom.
摘要翻译： 本发明涉及包含溶血磷脂酸类似物的组合物和使用此类类似物作为LPA受体活性的激动剂或拮抗剂的方法。 此外，本发明涉及LPA受体激动剂，其在各个LPA受体（即LPA1，LPA2和LPA3）上的选择度变化。 更具体地说，本发明涉及LPA类似物，其中甘油被乙醇胺替代，并且多种取代已经在第二个碳原子连接。
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5.发明授权公开(公告)号：US07638637B2
公开(公告)日：2009-12-29
申请号：US10578216
申请日：2004-11-03
IPC分类号： C07D233/61 , C07D277/22 , C07D263/32 , A61K31/4164 , A61K31/421 , A61K31/426
CPC分类号： C07F9/6506
摘要： The present invention relates to S1P analogs that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds have the general structure (I) wherein R11 is C5-C18 alkyl or C5-C18 alkenyl; Q is selected from the group consisting of C3-C6 optionally substituted cycloalkyl, C3-C6 optionally substituted heterocyclic, C3-C6 optionally substituted aryl C3-C6 optionally substituted heteroaryl and; R2 is selected from the group consisting of H, C1-C4 alkyl, (C1-C4 alkyl)OH and (C1-C4 alkyl)NH2; R23 is H or C1-C4 alkyl, and R15 is a phosphonate ester or a phosphate ester or a pharmaceutically acceptable salt or tautomer thereof.
摘要翻译： 本发明涉及具有作为S1P受体调节剂的活性的S1P类似物以及这些化合物用于治疗与不适当S1P受体活性相关的疾病的用途。 所述化合物具有其中R 11为C 5 -C 18烷基或C 5 -C 18烯基的通式结构（I） Q选自C 3 -C 6任选取代的环烷基，C 3 -C 6任选取代的杂环，C 3 -C 6任选取代的芳基C 3 -C 6任选取代的杂芳基; R2选自H，C1-C4烷基，（C1-C4烷基）OH和（C1-C4烷基）NH2; R 23是H或C 1 -C 4烷基，R 15是膦酸酯或磷酸酯或其药学上可接受的盐或互变异构体。
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6.发明申请PHENYL-CYCLOALKYL AND PHENYL-HETEROCYCLIC DERIVATIVES AS S1P RECEPTOR AGONISTS 审中-公开作为S1P受体激动剂的苯丙氨酸和苯基间苯二酚衍生物公开(公告)号：US20090105315A1
公开(公告)日：2009-04-23
申请号：US12195606
申请日：2008-08-21
IPC分类号： C07D271/06 , A61K31/4245 , A61K31/381 , C07D333/04 , A61P37/00 , A61P41/00
CPC分类号： C07D271/06 , C07F9/65318
摘要： Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
摘要翻译： 提供了在一种或多种S1P受体上具有激动剂活性的化合物。 化合物是鞘氨醇类似物，其在磷酸化之后可以作为S1P受体的激动剂。
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公开(公告)号：US20080318901A1
公开(公告)日：2008-12-25
申请号：US11579658
申请日：2005-05-06
IPC分类号： A61K31/661 , C07F9/08 , C07F9/572 , A61K31/665 , A61P17/02 , A61K31/675 , C07F9/6506 , C07F9/655
CPC分类号： C07F9/65515 , C07F9/091 , C07F9/094 , C07F9/3891 , C07F9/404 , C07F9/5728 , C07F9/58 , C07F9/6506
摘要： The present invention is directed to compositions comprising lysophosphatidic acid analogs and methods of using such analogs as agonist or antagonists of LPA receptor activity. In addition the invention is directed to LPA receptor agonists that vary in the degree of selectivity at individual LPA receptors (i.e. LPA1, LPA2 and LPA3). More particularly the present invention is directed to LPA analogs wherein the glycerol is replaced with ethanolamine and a variety of substitutions have been linked at the second carbon atom.
摘要翻译： 本发明涉及包含溶血磷脂酸类似物的组合物和使用此类类似物作为LPA受体活性的激动剂或拮抗剂的方法。 此外，本发明涉及LPA受体激动剂，其在各个LPA受体（即LPA1，LPA2和LPA3）上的选择度变化。 更具体地说，本发明涉及LPA类似物，其中甘油被乙醇胺替代，并且多种取代已经在第二个碳原子连接。
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公开(公告)号：US07241790B2
公开(公告)日：2007-07-10
申请号：US10523337
申请日：2003-07-30
IPC分类号： C07F9/06 , C07D233/61 , A61K31/417
CPC分类号： C07F9/65068 , C07F9/091 , C07F9/094 , C07F9/6506
摘要： The present invention relates to S1P analogs that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds have the general structure of Formula (I) wherein R11 is C5–C18 alkyl or C5–C18 alkenyl; Q is selected from the group consisting of C3–C6 optionally substituted cycloalkyl, C3–C6 optionally substituted heterocyclic, C3–C6 optionally substituted aryl C3–C6 optionally substituted heteroaryl and —NH(CO)—; R2 is selected from the group consisting of H, C1–C4 alkyl, (C1–C4 alkyl)OH and (C1–C4 alkyl)NH2; R23 is H or C1–C4 alkyl, and R15 is selected from the group consisting of hydroxy, phosphonate, and of Formula (II) wherein X and R15 is selected from the group consisting of O and S; or a pharmaceutically acceptable salt or tautomer thereof
摘要翻译： 本发明涉及具有作为S1P受体调节剂的活性的S1P类似物以及这些化合物用于治疗与不适当S1P受体活性相关的疾病的用途。 这些化合物具有式（I）的通式结构，其中R 11是C 5 -C 18烷基或C 5 - C 1 -C 18链烯基; Q选自C 3 -C 6任选取代的环烷基，C 3 -C 6亚烷基，C 3 -C 6 - 任选取代的杂环，C 3 -C 6任选取代的芳基C 3 -C 6 -C 6任选取代的杂芳基和 - NH（CO） - ; R 2选自H，C 1 -C 4烷基，（C 1〜 C 4烷基）OH和（C 1 -C 4烷基）NH 2; R 23是H或C 1 -C 4烷基，R 15选自由以下组成的组： 羟基，膦酸酯和式（II）的化合物，其中X和R 15选自O和S; 或其药学上可接受的盐或互变异构体
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公开(公告)号：US5612470A
公开(公告)日：1997-03-18
申请号：US947672
申请日：1992-09-18
IPC分类号： G01N33/53 , A61K38/00 , C07K1/113 , C07K1/22 , C07K14/575 , C07K14/60 , C07K14/61 , C07K14/655 , C07K14/705 , C07K14/72 , C07K17/02 , C12N15/12 , G01N33/52 , G01N33/74
CPC分类号： C07K14/60 , C07K14/723 , G01N33/74 , A61K38/00 , G01N2333/60 , G01N2333/726
摘要： Growth hormone releasing hormone (GHRH) receptor binding has been characterized using a unique binding assay utilizing iodinated GHRH probes. Photoaffinity GHRH probes have been constructed which allow for photolabeling and characterization of the receptor. In addition, high affinity biotinylated GHRH analogs have been constructed. Solubilization of GHRH-R/GHRH complexes and extraction of specifically bound GHRH using a mild detergent solution, followed by affinity chromotography, leads to a substantially purified GHRH-R isolate. Electrophoretic treatment of the GHRH-R isolate produces GHRH-R of sufficient purity to conduct sequencing of the receptor. Cloning of a gene encoding for polypeptides (protein or fragments thereof) having GHRH-R activity is accomplished using a bacterial host, and the cloned gene is expressed in a mammalian cell line.
摘要翻译： 生长激素释放激素（GHRH）受体结合已经通过使用碘化GHRH探针的独特结合测定来表征。 已经构建了能够对受体进行光贴标和表征的光亲和性GHRH探针。 此外，已经构建了高亲和力的生物素化GHRH类似物。 GHRH-R / GHRH复合物的溶解和使用温和洗涤剂溶液提取特异性结合的GHRH，随后进行亲和层析，得到基本纯化的GHRH-R分离物。 GHRH-R分离物的电泳处理产生足够纯度的GHRH-R以进行受体的测序。 使用细菌宿主完成编码具有GHRH-R活性的多肽（蛋白质或其片段）的基因的克隆，并且克隆的基因在哺乳动物细胞系中表达。
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公开(公告)号：US5591641A
公开(公告)日：1997-01-07
申请号：US946232
申请日：1992-09-15
IPC分类号： G01N33/53 , A61K38/00 , A61K38/25 , C07K1/113 , C07K1/22 , C07K14/575 , C07K14/60 , C07K14/61 , C07K14/655 , C07K14/705 , C07K14/72 , C07K17/02 , C12P21/02 , G01N33/52 , G01N33/74 , C12N15/12
CPC分类号： C07K14/60 , C07K14/723 , G01N33/74 , A61K38/00 , G01N2333/60 , G01N2333/726
摘要： Growth hormone releasing hormone (GHRH) receptor binding has been characterized using a unique binding assay utilizing iodinated GHRH probes. Photoaffinity GHRH probes have been constructed which allow for photolabeling and characterization of the receptor. In addition, high affinity biotinylated GHRH analogs have been constructed. Solubilization of GHRH-R/GHRH complexes and extraction of specifically bound GHRH using a mild detergent solution, followed by affinity chromotography, leads to a substantially purified GHRH-R isolate. Electrophoretic treatment of the GHRH-R isolate produces GHRH-R of sufficient purity to conduct sequencing of the receptor. Cloning of a gene encoding for polypeptides (protein or fragments thereof) having GHRH-R activity is accomplished using a bacterial host, and the cloned gene is expressed in a mammalian cell line.
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