公开(公告)号：US07612078B2

公开(公告)日：2009-11-03

申请号：US11075565

申请日：2005-03-08

申请人： Dale S. Dhanoa ,  Oren Becker ,  Silvia Noiman ,  A. Sekar Reddy ,  Srinivasa R. Cheruku ,  Rosa E. Melendez ,  Anurag Sharadendu ,  Dongli Chen ,  Yael Marantz ,  Sharon Shacham ,  Alexander Heifetz ,  Boaz Inbal ,  Venkitasamy Kesavan ,  Shay Bar-Haim

发明人： Dale S. Dhanoa ,  Oren Becker ,  Silvia Noiman ,  A. Sekar Reddy ,  Srinivasa R. Cheruku ,  Rosa E. Melendez ,  Anurag Sharadendu ,  Dongli Chen ,  Yael Marantz ,  Sharon Shacham ,  Alexander Heifetz ,  Boaz Inbal ,  Venkitasamy Kesavan ,  Shay Bar-Haim

IPC分类号： C07D495/04 ,  A61K31/519 ,  A61P25/06 ,  A61P9/12

CPC分类号： C07D495/04

摘要： The invention relates to 5-HT receptor modulators, particularly 5-HT2B antagonists. Novel piperidinylamino-thieno[2,3-d]pyrimidine compounds represented by Formula I, II and III, and uses thereof for treating conditions including pulmonary arterial hypertension, congestive heart failure, and hypertension.

摘要翻译： 本发明涉及5-HT受体调节剂，特别是5-HT 2B拮抗剂。 由式I，II和III表示的新型哌啶基氨基 - 噻吩并[2,3-d]嘧啶化合物及其用于治疗包括肺动脉高压，充血性心力衰竭和高血压的病症的用途。

公开(公告)号：US07488731B2

公开(公告)日：2009-02-10

申请号：US11782415

申请日：2007-07-24

申请人： Dale S. Dhanoa ,  Dongli Chen ,  Oren Becker ,  Silvia Noiman ,  Srinivasa R. Cheruku ,  Yael Marantz ,  Anurag Sharadendu ,  Sharon Shacham ,  Alexander Heifetz ,  Pradyumna Mohanty ,  Boaz Inbal ,  Merav Fichman ,  Raphael Nudelman ,  Shay Bar-Haim

发明人： Dale S. Dhanoa ,  Dongli Chen ,  Oren Becker ,  Silvia Noiman ,  Srinivasa R. Cheruku ,  Yael Marantz ,  Anurag Sharadendu ,  Sharon Shacham ,  Alexander Heifetz ,  Pradyumna Mohanty ,  Boaz Inbal ,  Merav Fichman ,  Raphael Nudelman ,  Shay Bar-Haim

IPC分类号： A61K31/495 ,  C07D295/13

CPC分类号： C07D213/74 ,  C07D211/96 ,  C07D239/42 ,  C07D295/13 ,  C07D401/12

摘要： The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formula I, and synthesis and uses thereof for treating diseases including those mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as generalized anxiety disorder, ADD/ADHD, neural injury, stroke, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

公开(公告)号：US07491727B2

公开(公告)日：2009-02-17

申请号：US11516345

申请日：2006-09-05

申请人： Dale S. Dhanoa ,  Dongli Chen ,  Oren Becker ,  Silvia Noiman ,  Srinivasa R. Cheruku ,  Yael Marantz ,  Anurag Sharadendu ,  Sharon Shacham ,  Alexander Heifetz ,  Pradyumna Mohanty ,  Boaz Inbal ,  Merav Fichman ,  Raphael Nudelman ,  Shay Bar-Haim

发明人： Dale S. Dhanoa ,  Dongli Chen ,  Oren Becker ,  Silvia Noiman ,  Srinivasa R. Cheruku ,  Yael Marantz ,  Anurag Sharadendu ,  Sharon Shacham ,  Alexander Heifetz ,  Pradyumna Mohanty ,  Boaz Inbal ,  Merav Fichman ,  Raphael Nudelman ,  Shay Bar-Haim

IPC分类号： A61K31/495 ,  A61K31/496

CPC分类号： C07D213/74 ,  C07D211/96 ,  C07D239/42 ,  C07D295/13 ,  C07D401/12

摘要： The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formula I, and synthesis and uses thereof for treating diseases including those mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as generalized anxiety disorder, ADD/ADHD, neural injury, stroke, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

摘要翻译： 本发明涉及5-HT受体激动剂或拮抗剂。 公开了由式I表示的新型芳基哌嗪基磺酰胺化合物及其用于治疗包括由5-HT受体直接或间接介导的疾病的疾病的合成和用途。 这些病症包括中枢神经系统疾病，如广泛性焦虑症，ADD / ADHD，神经损伤，中风和偏头痛。 还包括制备方法和新型中间体及其药物盐。

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：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：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。