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1. 发明申请

US20120088749A1 S1P Receptor Modulating Compounds and Use Thereof 审中-公开
标题翻译： S1P受体调节化合物及其用途
公开(公告)号：US20120088749A1
公开(公告)日：2012-04-12
申请号：US13327951
申请日：2011-12-16
申请人： Susana C. Neira , Xiang Yu , Roland Burli , Victor Cee , Brian Lanman
发明人： Susana C. Neira , Xiang Yu , Roland Burli , Victor Cee , Brian Lanman
IPC分类号： A61K31/397 , C07D401/10 , A61K31/4427 , A61P37/06 , A61P29/00 , A61P35/02 , A61P3/10 , A61P25/00 , A61P17/06 , A61P1/04 , A61P1/00 , C07D205/04 , A61P19/04
CPC分类号： C07D205/04 , C07D401/10
摘要： The present invention relates to amides 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 may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.
摘要翻译：本发明涉及具有作为S1P受体调节剂的活性的酰胺和这些化合物用于治疗与不适当的S1P受体活性相关的疾病的用途。这些化合物可用作免疫调节剂，例如用于治疗或预防诸如自身免疫性疾病和相关免疫疾病（包括系统性红斑狼疮），炎症性肠病如克罗恩病和溃疡性结肠炎，I型糖尿病，葡萄膜炎，牛皮癣，重症肌无力，类风湿关节炎，非肾小球性肾病，肝炎，白塞病，肾小球性肾炎，慢性血小板减少性紫癜，溶血性贫血，肝炎和韦格纳肉芽肿; 并处理其他条件。

2. 发明申请

US20090082331A1 S1P RECEPTOR MODULATING COMPOUNDS AND USE THEREOF 失效
标题翻译： S1P受体调节化合物及其用途
公开(公告)号：US20090082331A1
公开(公告)日：2009-03-26
申请号：US12234514
申请日：2008-09-19
申请人： Susana C. Neira , Xiang Yu
发明人： Susana C. Neira , Xiang Yu
IPC分类号： A61K31/397 , C07D205/04 , A61P37/06 , A61P19/02 , A61P3/10 , A61P1/00 , A61P35/02
CPC分类号： C07D205/04 , C07D401/10
摘要： The present invention relates to amides that have activity as SIP receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.
摘要翻译：本发明涉及具有作为SIP受体调节剂的活性的酰胺和这些化合物用于治疗与不适当的S1P受体活性相关的疾病的用途。这些化合物可用作免疫调节剂，例如用于治疗或预防诸如自身免疫性疾病和相关免疫疾病（包括系统性红斑狼疮），炎症性肠病如克罗恩病和溃疡性结肠炎，I型糖尿病，葡萄膜炎，牛皮癣，重症肌无力，类风湿关节炎，非肾小球性肾病，肝炎，白塞病，肾小球性肾炎，慢性血小板减少性紫癜，溶血性贫血，肝炎和韦格纳肉芽肿; 并处理其他条件。

3. 发明授权

US08080542B2 S1P receptor modulating compounds and use thereof 失效
标题翻译： S1P受体调节化合物及其用途
公开(公告)号：US08080542B2
公开(公告)日：2011-12-20
申请号：US12234514
申请日：2008-09-19
申请人： Susana C. Neira , Xiang Yu , Roland Burli , Victor Cee , Brian Lanman
发明人： Susana C. Neira , Xiang Yu , Roland Burli , Victor Cee , Brian Lanman
IPC分类号： A61K31/397 , C07D205/04
CPC分类号： C07D205/04 , C07D401/10
摘要： The present invention relates to amides that have activity as SIP receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.
摘要翻译：本发明涉及具有作为SIP受体调节剂的活性的酰胺和这些化合物用于治疗与不适当的S1P受体活性相关的疾病的用途。这些化合物可用作免疫调节剂，例如用于治疗或预防诸如自身免疫性疾病和相关免疫疾病（包括系统性红斑狼疮），炎症性肠病如克罗恩病和溃疡性结肠炎，I型糖尿病，葡萄膜炎，牛皮癣，重症肌无力，类风湿关节炎，非肾小球性肾病，肝炎，白塞病，肾小球性肾炎，慢性血小板减少性紫癜，溶血性贫血，肝炎和韦格纳肉芽肿; 并处理其他条件。

4. 发明申请

US20110224248A1 AZAQUINOLONES THAT INHIBIT PROLYL HYDROXYLASE 有权
标题翻译：抑制丙酸羟化酶的AZAQUINOLONES
公开(公告)号：US20110224248A1
公开(公告)日：2011-09-15
申请号：US13109877
申请日：2011-05-17
申请人： Jennifer R. Allen , Roland Burli , Marian C. Bryan , Guo-Qiang Cao , Susana C. Neira , Anthony B. Reed
发明人： Jennifer R. Allen , Roland Burli , Marian C. Bryan , Guo-Qiang Cao , Susana C. Neira , Anthony B. Reed
IPC分类号： A61K31/4375 , C07D471/04 , C07D215/22 , A61K31/4704 , A61P7/06 , A61P9/12 , A61P3/10 , A61P35/00 , A61P29/00 , C12N5/071 , A61P9/10 , A61P43/00
CPC分类号： C07D471/04 , C07D215/22 , C07D405/04 , C07D409/04
摘要： Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
摘要翻译：式I化合物是HIF脯氨酰羟化酶的有用抑制剂。式I的化合物具有以下结构：其中本文提供变量的定义。

5. 发明授权

US07842685B2 S1P1 receptor agonists and use thereof 有权
标题翻译： S1P1受体激动剂及其用途
公开(公告)号：US07842685B2
公开(公告)日：2010-11-30
申请号：US12456687
申请日：2009-06-18
申请人： Victor J. Cee , Michael J. Frohn , Brian Alan Lanman , Susana C. Neira , Anthony B. Reed , Kelvin K. C. Sham
发明人： Victor J. Cee , Michael J. Frohn , Brian Alan Lanman , Susana C. Neira , Anthony B. Reed , Kelvin K. C. Sham
IPC分类号： A61K31/397 , A61K31/4365 , C07D513/04
CPC分类号： C07D513/04 , A61K9/2018 , A61K9/2059 , A61K9/48
摘要： The present invention relates to compounds of Formula (I): that are have activity as S1P receptor modulating agents, more specifically to specifically compounds that are S1P1 receptor agonists. The invention also related to the use of such compounds to treat diseases associated with inappropriate S1P1 receptor activity such as autoimmune diseases.
摘要翻译：本发明涉及式（I）化合物：其具有作为S1P受体调节剂的活性，更具体地涉及作为S1P1受体激动剂的具体化合物。本发明还涉及使用这些化合物来治疗与不适当的S1P1受体活性相关的疾病，例如自身免疫性疾病。

6. 发明授权

US07728130B2 Quinolone based compounds exhibiting prolyl hydroxylase inhibitory activity 有权
标题翻译：喹诺酮类化合物显示脯氨酰羟化酶抑制活性
公开(公告)号：US07728130B2
公开(公告)日：2010-06-01
申请号：US11635683
申请日：2006-12-08
申请人： Jennifer R. Allen , Kaustav Biswas , Roland Burli , Jennifer Dao , Michael J. Frohn , Jennifer E. Golden , Randall W. Hungate , Robert Kurzeja , Stephanie J. Mercede , Kristine M. Muller , Susana C. Neira , Tanya A. N. Peterkin , Christopher M. Tegley , Violeta Yu
发明人： Jennifer R. Allen , Kaustav Biswas , Roland Burli , Jennifer Dao , Michael J. Frohn , Jennifer E. Golden , Randall W. Hungate , Robert Kurzeja , Stephanie J. Mercede , Kristine M. Muller , Susana C. Neira , Tanya A. N. Peterkin , Christopher M. Tegley , Violeta Yu
IPC分类号： C07D413/00
CPC分类号： C07D215/22 , C07D215/56 , C07D401/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , G01N33/542
摘要： This invention relates to new quinolone based compounds that exhibit prolyl hydroxylase inhibitory activity. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one quinolone based compound. This invention further involves assays for the detection of a hydroxyproline residue in a HIF molecule.
摘要翻译：本发明涉及显示脯氨酰羟化酶抑制活性的新型喹诺酮类化合物。本发明还涉及通过向受试者施用至少一种基于喹诺酮的化合物来增加受试者中HIF水平或活性或治疗与受试者中HIF水平或活性相关的病症的方法。本发明还涉及用于检测HIF分子中的羟脯氨酸残基的测定法。

7. 发明申请

US20090156605A1 Quinolones and azaquinolones that inhbit prolyl hydroxylase 有权
标题翻译：喹诺酮和氮杂喹啉酮，其吸收脯氨酰羟化酶
公开(公告)号：US20090156605A1
公开(公告)日：2009-06-18
申请号：US12148179
申请日：2008-04-16
申请人： Jennifer R. Allen , Roland Burli , Marian C. Bryan , Guo-Qiang Cao , Susana C. Neira , Anthony B. Reed
发明人： Jennifer R. Allen , Roland Burli , Marian C. Bryan , Guo-Qiang Cao , Susana C. Neira , Anthony B. Reed
IPC分类号： A61K31/5025 , C07D471/04 , A61K31/4375 , A61K31/4704 , C07D215/20 , C12N5/06
CPC分类号： C07D471/04 , C07D215/22 , C07D405/04 , C07D409/04
摘要： Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
摘要翻译：式I化合物是HIF脯氨酰羟化酶的有用抑制剂。式I的化合物具有以下结构：其中本文提供变量的定义。

8. 发明授权

US08030346B2 Heterocyclic quinolone derivatives that inhibit prolyl hydroxylase activity 有权
标题翻译：抑制脯氨酰羟化酶活性的杂环喹诺酮衍生物
公开(公告)号：US08030346B2
公开(公告)日：2011-10-04
申请号：US12150675
申请日：2008-04-29
申请人： Jennifer R. Allen , Roland Burli , Michael J. Frohn , Randall W. Hungate , Susana C. Neira , Anthony B. Reed
发明人： Jennifer R. Allen , Roland Burli , Michael J. Frohn , Randall W. Hungate , Susana C. Neira , Anthony B. Reed
IPC分类号： A61K31/385 , A01N43/42 , A01N43/78 , C07D221/22 , C07D515/02
CPC分类号： A61K31/4365 , A61K31/437 , C07D495/04 , C07D513/04
摘要： Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
摘要翻译：式I化合物是HIF脯氨酰羟化酶的有用抑制剂。式I的化合物具有以下结构：其中本文提供变量的定义。

9. 发明授权

US08017626B2 Quinolone based compounds exhibiting, prolyl hydroxylase inhibitory activity, and compositions, and uses thereof 有权
标题翻译：喹诺酮类化合物，表现出脯氨酰羟化酶抑制活性，组合物及其用途
公开(公告)号：US08017626B2
公开(公告)日：2011-09-13
申请号：US12703496
申请日：2010-02-10
申请人： Jennifer R. Allen , Kaustav Biswas , Roland Burli , Jennifer Dao , Michael J. Frohn , Jennifer E. Golden , Randall W. Hungate , Robert Kurzeja , Stephanie J. Mercede , Kristine M. Muller , Susana C. Neira , Tanya A. N. Peterkin , Christopher M. Tegley , Violeta Yu
发明人： Jennifer R. Allen , Kaustav Biswas , Roland Burli , Jennifer Dao , Michael J. Frohn , Jennifer E. Golden , Randall W. Hungate , Robert Kurzeja , Stephanie J. Mercede , Kristine M. Muller , Susana C. Neira , Tanya A. N. Peterkin , Christopher M. Tegley , Violeta Yu
IPC分类号： A61K31/4704 , C07D215/56
CPC分类号： C07D215/22 , C07D215/56 , C07D401/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , G01N33/542
摘要： This invention relates to new quinolone based compounds that exhibit prolyl hydroxylase inhibitory activity. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one quinolone based compound. This invention further involves assays for the detection of a hydroxyproline residue in a HIF molecule.
摘要翻译：本发明涉及显示脯氨酰羟化酶抑制活性的新型喹诺酮类化合物。本发明还涉及通过向受试者施用至少一种基于喹诺酮的化合物来增加受试者中HIF水平或活性或治疗与受试者中HIF水平或活性相关的病症的方法。本发明还涉及用于检测HIF分子中的羟脯氨酸残基的测定法。

10. 发明授权

US08012968B2 Quinolone based compounds exhibiting prolyl hydroxylase inhibitory activity, and compositions, and uses thereof 有权
标题翻译：具有脯氨酰羟化酶抑制活性的喹诺酮类化合物及其组合物及其用途
公开(公告)号：US08012968B2
公开(公告)日：2011-09-06
申请号：US12703716
申请日：2010-02-10
申请人： Jennifer R. Allen , Kaustav Biswas , Roland Burli , Jennifer Dao , Michael J. Frohn , Jennifer E. Golden , Randall W. Hungate , Robert Kurzeja , Stephanie J. Mercede , Kristine M. Muller , Susana C. Neira , Tanya A. N. Peterkin , Christopher M. Tegley , Violeta Yu
发明人： Jennifer R. Allen , Kaustav Biswas , Roland Burli , Jennifer Dao , Michael J. Frohn , Jennifer E. Golden , Randall W. Hungate , Robert Kurzeja , Stephanie J. Mercede , Kristine M. Muller , Susana C. Neira , Tanya A. N. Peterkin , Christopher M. Tegley , Violeta Yu
IPC分类号： A61K31/5377 , A61K31/501 , A61K31/506 , A61K31/4704
CPC分类号： C07D215/22 , C07D215/56 , C07D401/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , G01N33/542
摘要： This invention relates to new quinolone based compounds that exhibit prolyl hydroxylase inhibitory activity. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one quinolone based compound. This invention further involves assays for the detection of a hydroxyproline residue in a HIF molecule.
摘要翻译：本发明涉及显示脯氨酰羟化酶抑制活性的新型喹诺酮类化合物。本发明还涉及通过向受试者施用至少一种基于喹诺酮的化合物来增加受试者中HIF水平或活性或治疗与受试者中HIF水平或活性相关的病症的方法。本发明还涉及用于检测HIF分子中的羟脯氨酸残基的测定法。

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