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：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：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：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：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：US20100152141A1

公开(公告)日：2010-06-17

申请号：US12306301

申请日：2007-06-26

申请人： Kimberley Gannon ,  Sharon Shacham

发明人： Kimberley Gannon ,  Sharon Shacham

IPC分类号： A61K31/66 ,  A61K31/495 ,  A61K31/55 ,  A61P25/28

CPC分类号： A61K45/06 ,  A61K31/495

摘要： The invention relates to 5-HT6 receptor modulators. Compositions comprising arylamine compounds and acetylcholinesterase inhibitors and use of these compositions are disclosed. Such uses include e.g., the treatment, modulation and/or prevention of Alzheimer's disease and memory disorders, and psychological disorders such as schizophrenia, are disclosed.

摘要翻译： 本发明涉及5-HT6受体调节剂。 公开了包含芳基胺化合物和乙酰胆碱酯酶抑制剂的组合物以及这些组合物的用途。 这样的用途包括例如阿尔茨海默病和记忆障碍的治疗，调节和/或预防以及心理障碍如精神分裂症。

公开(公告)号：US20100280050A1

公开(公告)日：2010-11-04

申请号：US12676454

申请日：2008-09-04

申请人： Kimberley Gannon ,  Ohilip B. Graham

发明人： Kimberley Gannon ,  Ohilip B. Graham

IPC分类号： A61K31/519 ,  A61P43/00

CPC分类号： A61K31/519

摘要： The invention provides a method of treating or preventing fibrosis in a subject by administering a 5-HT modulator, e.g., a 5-HT2B modulator. In particular embodiments, the 5-HT modulator is a piperidinylamino-thieno[2,3-d]pyrimidine compound.

摘要翻译： 本发明提供通过施用5-HT调节剂例如5-HT 2B调节剂治疗或预防受试者的纤维化的方法。 在具体实施方案中，5-HT调节剂是哌啶基氨基 - 噻吩并[2,3-d]嘧啶化合物。