公开(公告)号：US20110059945A1

公开(公告)日：2011-03-10

申请号：US12945572

申请日：2010-11-12

申请人： Ashis K. Saha ,  Nili Schutz ,  Xiang Yu ,  Dilara McCauley ,  Mercedes Lobera ,  Yael Marantz ,  Jian Lin ,  Srinivasa Cheruku ,  Pini Orbach ,  Anurag Sharadendu ,  Robert Christian Penland ,  Kimberley Gannon ,  Sharon Shacham ,  Silvia Noiman ,  Oren Becker

发明人： Ashis K. Saha ,  Nili Schutz ,  Xiang Yu ,  Dilara McCauley ,  Mercedes Lobera ,  Yael Marantz ,  Jian Lin ,  Srinivasa Cheruku ,  Pini Orbach ,  Anurag Sharadendu ,  Robert Christian Penland ,  Kimberley Gannon ,  Sharon Shacham ,  Silvia Noiman ,  Oren Becker

IPC分类号： A61K31/397 ,  A61P37/06 ,  A61P35/00 ,  A61P19/00 ,  A61P3/10 ,  A61P35/04 ,  A61P11/06 ,  A61P9/10 ,  A61P13/12 ,  A61P1/16 ,  A61K31/4525 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/343

CPC分类号： C07D405/10 ,  C07D307/80 ,  C07D307/81 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D417/14

摘要： The present invention relates to compounds of the general formula (I) 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通式（I）的化合物，以及这些化合物用于治疗与不适当的S1P受体活性有关的疾病的用途。 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。

公开(公告)号：US07855193B2

公开(公告)日：2010-12-21

申请号：US11491766

申请日：2006-07-24

申请人： Ashis K. Saha ,  Nili Schutz ,  Xiang Yu ,  Dilara McCauley ,  Mercedes Lobera ,  Yael Marantz ,  Jian Lin ,  Srinivasa R. Cheruku ,  Pini Orbach ,  Anurag Sharadendu ,  Robert Christian Penland ,  Kimberley Gannon ,  Sharon Shacham ,  Silvia Noiman ,  Oren Becker

发明人： Ashis K. Saha ,  Nili Schutz ,  Xiang Yu ,  Dilara McCauley ,  Mercedes Lobera ,  Yael Marantz ,  Jian Lin ,  Srinivasa R. Cheruku ,  Pini Orbach ,  Anurag Sharadendu ,  Robert Christian Penland ,  Kimberley Gannon ,  Sharon Shacham ,  Silvia Noiman ,  Oren Becker

IPC分类号： A61K31/397 ,  A61K31/5377 ,  A61K31/4525 ,  A61K31/4025 ,  A61K31/343 ,  C07D411/06 ,  C07D405/06 ,  C07D205/04 ,  C07D307/80

CPC分类号： C07D405/10 ,  C07D307/80 ,  C07D307/81 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D417/14

摘要： The present invention relates to compounds of the general formula (I) 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通式（I）的化合物，以及这些化合物用于治疗与不适当的S1P受体活性有关的疾病的用途。 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。

公开(公告)号：US20080064677A9

公开(公告)日：2008-03-13

申请号：US11491766

申请日：2006-07-24

申请人： Ashis K. Saha ,  Nili Schutz ,  Anurag Sharadendu ,  Dilara McCauley ,  Mercedes Lobera ,  Yael Marantz ,  Jian Lin ,  Srinivasa Rao Cheruku ,  Pini Orbach ,  Anurag Sharadendu ,  Robert Christian Penland ,  Kimberley Gannon ,  Sharon Shacham ,  Silvia Noiman ,  Oren Becker

发明人： Ashis K. Saha ,  Nili Schutz ,  Anurag Sharadendu ,  Dilara McCauley ,  Mercedes Lobera ,  Yael Marantz ,  Jian Lin ,  Srinivasa Rao Cheruku ,  Pini Orbach ,  Anurag Sharadendu ,  Robert Christian Penland ,  Kimberley Gannon ,  Sharon Shacham ,  Silvia Noiman ,  Oren Becker

IPC分类号： A61K31/452 ,  A61K31/397 ,  C07D405/02

CPC分类号： C07D405/10 ,  C07D307/80 ,  C07D307/81 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D417/14

摘要： The present invention relates to compounds of the general formula (I) 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, Behcet'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通式（I）的化合物，以及这些化合物用于治疗与不适当的S1P受体活性有关的疾病的用途。 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，贝切特氏病，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。

公开(公告)号：US20070173487A1

公开(公告)日：2007-07-26

申请号：US11491766

申请日：2006-07-24

申请人： Ashis K. Saha ,  Nili Schutz ,  Anurag Sharadendu ,  Dilara McCauley ,  Mercedes Lobera ,  Yael Marantz ,  Jian Lin ,  Srinivasa Rao Cheruku ,  Pini Orbach ,  Anurag Sharadendu ,  Robert Christian Penland ,  Kimberley Gannon ,  Sharon Shacham ,  Silvia Noiman ,  Oren Becker

发明人： Ashis K. Saha ,  Nili Schutz ,  Anurag Sharadendu ,  Dilara McCauley ,  Mercedes Lobera ,  Yael Marantz ,  Jian Lin ,  Srinivasa Rao Cheruku ,  Pini Orbach ,  Anurag Sharadendu ,  Robert Christian Penland ,  Kimberley Gannon ,  Sharon Shacham ,  Silvia Noiman ,  Oren Becker

IPC分类号： A61K31/452 ,  A61K31/397 ,  C07D405/02

CPC分类号： C07D405/10 ,  C07D307/80 ,  C07D307/81 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D417/14

摘要： The present invention relates to compounds of the general formula (I) 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, Behcet'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通式（I）的化合物，以及这些化合物用于治疗与不适当的S1P受体活性有关的疾病的用途。 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，贝切特氏病，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。

公开(公告)号：US20080027036A1

公开(公告)日：2008-01-31

申请号：US11726351

申请日：2007-03-21

申请人： Roland Burli ,  Victor Cee ,  Jennifer Golden ,  Brian Lanman ,  Susana Neira ,  Ashis Saha ,  Nili Schutz ,  Xiang Yu ,  Dilara McCauley ,  Mercedes Lobera ,  Yael Marantz ,  Jian Lin ,  Srinivasa Cheruku ,  Pini Orbach ,  Anurag Sharadendu ,  Robert Penland ,  Kimberley Gannon ,  Sharon Shacham ,  Silvia Noiman ,  Oren Becker ,  Zhaoda Zhang

发明人： Roland Burli ,  Victor Cee ,  Jennifer Golden ,  Brian Lanman ,  Susana Neira ,  Ashis Saha ,  Nili Schutz ,  Xiang Yu ,  Dilara McCauley ,  Mercedes Lobera ,  Yael Marantz ,  Jian Lin ,  Srinivasa Cheruku ,  Pini Orbach ,  Anurag Sharadendu ,  Robert Penland ,  Kimberley Gannon ,  Sharon Shacham ,  Silvia Noiman ,  Oren Becker ,  Zhaoda Zhang

IPC分类号： A61K31/397 ,  A61K31/343 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/47 ,  A61K31/5377 ,  A61P1/00 ,  A61P19/02 ,  A61P29/00 ,  A61P3/10 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07D205/12 ,  C07D213/00 ,  C07D217/00 ,  C07D221/00 ,  C07D235/02 ,  C07D239/70 ,  C07D257/04 ,  C07D263/52 ,  C07D277/00 ,  C07D295/00 ,  C07D307/77

CPC分类号： C07D307/79 ,  C07D307/80 ,  C07D307/81 ,  C07D403/10 ,  C07D405/04 ,  C07D405/10 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048

摘要： The present invention relates to compounds of the general formula (I) 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通式（I）的化合物，以及这些化合物用于治疗与不适当的S1P受体活性有关的疾病的用途。 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。

公开(公告)号：US20110212940A1

公开(公告)日：2011-09-01

申请号：US13034895

申请日：2011-02-25

申请人： Roland Burli ,  Victor J. Cee ,  Jennifer Golden ,  Brian Alan Lanman ,  Susana Neira ,  Ashis Saha ,  Nili Schutz ,  Xiang Yu ,  Dilara McCauley ,  Mercedes Lobera ,  Yael Marantz ,  Jian Lin ,  Srinivasa R. Cheruku ,  Pini Orbach ,  Anurag Sharadendu ,  Robert C. Penland ,  Kimberley Gannon ,  Sharon Shacham ,  Silvia Noiman ,  Oren Becker ,  Zhaoda Zhang

发明人： Roland Burli ,  Victor J. Cee ,  Jennifer Golden ,  Brian Alan Lanman ,  Susana Neira ,  Ashis Saha ,  Nili Schutz ,  Xiang Yu ,  Dilara McCauley ,  Mercedes Lobera ,  Yael Marantz ,  Jian Lin ,  Srinivasa R. Cheruku ,  Pini Orbach ,  Anurag Sharadendu ,  Robert C. Penland ,  Kimberley Gannon ,  Sharon Shacham ,  Silvia Noiman ,  Oren Becker ,  Zhaoda Zhang

IPC分类号： A61K31/397 ,  C07D405/10 ,  A61K31/4525 ,  C07D405/14 ,  A61K31/443 ,  C07D413/14 ,  A61K31/427 ,  C07D409/14 ,  A61K31/4725 ,  A61K31/4025 ,  C07D307/80 ,  A61K31/343 ,  A61K31/5377 ,  C07D413/10 ,  A61K31/41 ,  A61P35/00 ,  A61P37/06 ,  A61P29/00 ,  A61P3/10 ,  A61P25/00 ,  A61P17/06 ,  A61P35/02 ,  A61P11/00 ,  A61P11/06 ,  A61P17/02 ,  A61P9/00 ,  A61P9/10 ,  A61P13/12 ,  A61P1/16 ,  A61P7/06

CPC分类号： C07D307/79 ,  C07D307/80 ,  C07D307/81 ,  C07D403/10 ,  C07D405/04 ,  C07D405/10 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048

摘要： The present invention relates to compounds of the general formula (I) 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.

公开(公告)号：US07919519B2

公开(公告)日：2011-04-05

申请号：US11726351

申请日：2007-03-21

申请人： Roland Burli ,  Victor J. Cee ,  Jennifer Golden ,  Brian Alan Lanman ,  Susana Neira ,  Ashis Saha ,  Nili Schutz ,  Xiang Yu ,  Dilara McCauley ,  Mercedes Lobera ,  Yael Marantz ,  Jian Lin ,  Srinivasa R. Cheruku ,  Pini Orbach ,  Anurag Sharadendu ,  Robert C. Penland ,  Kimberley Gannon ,  Sharon Shacham ,  Silvia Noiman ,  Oren Becker ,  Zhaoda Zhang

发明人： Roland Burli ,  Victor J. Cee ,  Jennifer Golden ,  Brian Alan Lanman ,  Susana Neira ,  Ashis Saha ,  Nili Schutz ,  Xiang Yu ,  Dilara McCauley ,  Mercedes Lobera ,  Yael Marantz ,  Jian Lin ,  Srinivasa R. Cheruku ,  Pini Orbach ,  Anurag Sharadendu ,  Robert C. Penland ,  Kimberley Gannon ,  Sharon Shacham ,  Silvia Noiman ,  Oren Becker ,  Zhaoda Zhang

IPC分类号： A61K31/404 ,  A61K31/381 ,  A61K31/343 ,  C07D209/12 ,  C07D333/56 ,  C07D307/80

CPC分类号： C07D307/79 ,  C07D307/80 ,  C07D307/81 ,  C07D403/10 ,  C07D405/04 ,  C07D405/10 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048

摘要： The present invention relates to compounds of the general formula (I) 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通式（I）的化合物，以及这些化合物用于治疗与不适当的S1P受体活性有关的疾病的用途。 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。

公开(公告)号：US20080015177A1

公开(公告)日：2008-01-17

申请号：US11726356

申请日：2007-03-21

申请人： Ashis Saha ,  Xiang Yu ,  Mercedes Lobera ,  Jian Lin ,  Srinivasa Cheruku ,  Oren Becker ,  Yael Marantz ,  Nili Schutz

发明人： Ashis Saha ,  Xiang Yu ,  Mercedes Lobera ,  Jian Lin ,  Srinivasa Cheruku ,  Oren Becker ,  Yael Marantz ,  Nili Schutz

IPC分类号： A61K31/397 ,  A61P1/00 ,  A61P19/02 ,  A61P29/00 ,  A61P3/10 ,  A61P35/00 ,  A61P37/00 ,  C07D233/02

CPC分类号： C07D403/10

摘要： The present invention relates to compounds that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. In certain embodiments, the compounds of the invention relate to aryl oxoimidazolidinyls.

摘要翻译： 本发明涉及具有作为S1P受体调节剂的活性的化合物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。 在某些实施方案中，本发明的化合物涉及芳基氧代咪唑烷基。

公开(公告)号：US20100317649A1

公开(公告)日：2010-12-16

申请号：US12862631

申请日：2010-08-24

申请人： Ashis Saha ,  Xiang Yu ,  Mercedes Lobera ,  Jian Lin ,  Srinivasa R. Cheruku ,  Oren Becker ,  Yael Marantz ,  Nili Schutz

发明人： Ashis Saha ,  Xiang Yu ,  Mercedes Lobera ,  Jian Lin ,  Srinivasa R. Cheruku ,  Oren Becker ,  Yael Marantz ,  Nili Schutz

IPC分类号： A61K31/4178 ,  A61P37/06 ,  A61P35/00 ,  A61P11/00 ,  A61P29/00 ,  A61P3/10 ,  A61P17/06 ,  A61P1/04 ,  A61P1/00 ,  A61P11/06 ,  A61P9/10

CPC分类号： C07D403/10

摘要： The present invention relates to compounds that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. In certain embodiments, the compounds of the invention relate to aryl oxoimidazolidinyls.

摘要翻译： 本发明涉及具有作为S1P受体调节剂的活性的化合物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。 在某些实施方案中，本发明的化合物涉及芳基氧代咪唑烷基。

公开(公告)号：US07790707B2

公开(公告)日：2010-09-07

申请号：US11726356

申请日：2007-03-21

申请人： Ashis Saha ,  Xiang Yu ,  Mercedes Lobera ,  Jian Lin ,  Srinivasa R. Cheruku ,  Oren Becker ,  Yael Marantz ,  Nili Schutz

发明人： Ashis Saha ,  Xiang Yu ,  Mercedes Lobera ,  Jian Lin ,  Srinivasa R. Cheruku ,  Oren Becker ,  Yael Marantz ,  Nili Schutz

IPC分类号： A61K31/397 ,  A61K31/4166 ,  C07D205/04 ,  C07D403/02 ,  C07D403/06

CPC分类号： C07D403/10

摘要： The present invention relates to compounds that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. In certain embodiments, the compounds of the invention relate to aryl oxoimidazolidinyls.

摘要翻译： 本发明涉及具有作为S1P受体调节剂的活性的化合物以及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。 在某些实施方案中，本发明的化合物涉及芳基氧代咪唑烷基。