公开(公告)号：US20120322827A1

公开(公告)日：2012-12-20

申请号：US13522051

申请日：2011-01-13

Applicant: Erkan Baloglu ,  Shomir Ghosh ,  Mercedes Lobera ,  Darby Schmidt

Inventor： Erkan Baloglu ,  Shomir Ghosh ,  Mercedes Lobera ,  Darby Schmidt

IPC: A61K31/4245 ,  C07D413/12 ,  A61K31/4196 ,  A61K31/422 ,  C07D409/12 ,  C07D413/14 ,  A61K31/454

CPC classification number: C07D413/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, n and L are as defined herein, and methods of making and using the same.

Abstract translation: 公开了具有下式的化合物：其中X1，X2，X3，R1，R2，R3，R4，Y，A，n和L如本文所定义，以及制备和使用它们的方法。

公开(公告)号：US07982040B2

公开(公告)日：2011-07-19

申请号：US12343818

申请日：2008-12-24

Applicant: Dale S. Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Pradyumna Mohanty ,  Dongli Chen ,  Mercedes Lobera ,  Laurence Wu ,  Yael Marantz ,  Boaz Inbal ,  Alexander Heifetz ,  Shay Bar-Haim ,  Sharon Shacham

Inventor： Dale S. Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Pradyumna Mohanty ,  Dongli Chen ,  Mercedes Lobera ,  Laurence Wu ,  Yael Marantz ,  Boaz Inbal ,  Alexander Heifetz ,  Shay Bar-Haim ,  Sharon Shacham

IPC: C07D221/02 ,  C07D515/02

CPC classification number: C07D495/04

Abstract: The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

Abstract translation: 本发明涉及5-HT受体激动剂和部分激动剂。 公开了由式I表示的新型噻吩并吡啶酮化合物及其用于治疗由5-HT受体直接或间接介导的疾病的合成和用途。 这些病症包括阿尔茨海默病，认知障碍，肠易激综合征，恶心，呕吐，呕吐，运动失调，胃食管反流病，非溃疡性消化不良，抑郁症，焦虑症，尿失禁，偏头痛，心律失常，心房颤动，缺血性卒中，胃炎，胃排空障碍 ，喂食障碍，胃肠道疾病，便秘，勃起功能障碍和呼吸抑制。 还包括制备方法和新型中间体及其药物盐。

公开(公告)号：US07968538B2

公开(公告)日：2011-06-28

申请号：US11340079

申请日：2006-01-25

Applicant: Oren Becker ,  Rosa Melendez ,  Yael Marantz ,  Anurag Sharadendu ,  Merav Fichman ,  Mercedes Lobera ,  Hanoch Senderowitz ,  Srinivasa Rao Cheruku ,  Silvia Noiman ,  Xiang Y. Yu ,  Sharon Shacham ,  Laurence Wu ,  Ashis Saha ,  Pini Orbach ,  Dale S. Dhanoa

Inventor： Oren Becker ,  Rosa Melendez ,  Yael Marantz ,  Anurag Sharadendu ,  Merav Fichman ,  Mercedes Lobera ,  Hanoch Senderowitz ,  Srinivasa Rao Cheruku ,  Silvia Noiman ,  Xiang Y. Yu ,  Sharon Shacham ,  Laurence Wu ,  Ashis Saha ,  Pini Orbach ,  Dale S. Dhanoa

IPC: C07D295/135 ,  A61K31/451

CPC classification number: C07D295/135 ,  C07D207/14 ,  C07D211/58 ,  C07D243/08 ,  C07D311/68 ,  C07D317/62 ,  C07D319/18 ,  C07D333/66 ,  C07D405/12

Abstract: The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.

Abstract translation: 本发明涉及5-HT 6受体拮抗剂。 新型芳基胺化合物和这些化合物及其药物组合物的用途，例如用于治疗，调节和/或预防与5-羟色胺作用相关的生理条件，例如治疗肥胖症和肥胖相关疾病，例如心血管疾病，消化系统 疾病，呼吸系统疾病，癌症和II型糖尿病; 和精神分裂症等心理障碍。

公开(公告)号：US20060084805A1

公开(公告)日：2006-04-20

申请号：US11269042

申请日：2005-11-08

Applicant: Dale Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Pradyumna Mohanty ,  Dongli Chen ,  Mercedes Lobera ,  Laurence Wu ,  Yael Marantz ,  Boaz Inbal ,  Alexander Heifetz ,  Shay Bar-Haim ,  Sharon Shacham

Inventor： Dale Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Pradyumna Mohanty ,  Dongli Chen ,  Mercedes Lobera ,  Laurence Wu ,  Yael Marantz ,  Boaz Inbal ,  Alexander Heifetz ,  Shay Bar-Haim ,  Sharon Shacham

IPC: C07D498/02

CPC classification number: C07D495/04

Abstract: The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

公开(公告)号：US20050256153A1

公开(公告)日：2005-11-17

申请号：US10955434

申请日：2004-09-30

Applicant: Dale Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Pradyumna Mohanty ,  Dongli Chen ,  Mercedes Lobera ,  Laurence Wu ,  Yael Marantz ,  Boaz Inbal ,  Alexander Heifetz ,  Shay Bar-Haim ,  Sharon Shacham

Inventor： Dale Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Pradyumna Mohanty ,  Dongli Chen ,  Mercedes Lobera ,  Laurence Wu ,  Yael Marantz ,  Boaz Inbal ,  Alexander Heifetz ,  Shay Bar-Haim ,  Sharon Shacham

IPC: A61K31/4743 ,  C07D495/04 ,  C07D498/02

CPC classification number: C07D495/04

Abstract: The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

Abstract translation: 本发明涉及5-HT受体激动剂和部分激动剂。 公开了由式I表示的新型噻吩并吡啶酮化合物及其用于治疗由5-HT受体直接或间接介导的疾病的合成和用途。 这些病症包括阿尔茨海默病，认知障碍，肠易激综合征，恶心，呕吐，呕吐，运动失调，胃食管反流病，非溃疡性消化不良，抑郁症，焦虑症，尿失禁，偏头痛，心律失常，心房颤动，缺血性卒中，胃炎，胃排空障碍 ，喂食障碍，胃肠道疾病，便秘，勃起功能障碍和呼吸抑制。 还包括制备方法和新型中间体及其药物盐。

公开(公告)号：US20140155419A1

公开(公告)日：2014-06-05

申请号：US14235481

申请日：2012-07-27

Applicant: Erkan Baloglu ,  Shomir Ghosh ,  Mercedes Lobera ,  Darby R. Schmidt

Inventor： Erkan Baloglu ,  Shomir Ghosh ,  Mercedes Lobera ,  Darby R. Schmidt

IPC: C07D239/52 ,  C07D213/40 ,  C07D239/26 ,  C07D213/30

CPC classification number: C07D239/52 ,  C07C235/34 ,  C07D213/30 ,  C07D213/38 ,  C07D213/40 ,  C07D213/65 ,  C07D239/26 ,  C07D239/36 ,  C07D239/54 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12

Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORγ.

公开(公告)号：US08114894B2

公开(公告)日：2012-02-14

申请号：US12630468

申请日：2009-12-03

Applicant: Shomir Ghosh ,  Gali Golan ,  Boaz Inbal ,  Vincent Jacques ,  Mercedes Lobera

Inventor： Shomir Ghosh ,  Gali Golan ,  Boaz Inbal ,  Vincent Jacques ,  Mercedes Lobera

IPC: A61K31/404 ,  C07D401/12

CPC classification number: C07D209/24 ,  C07D401/12 ,  C07D471/04

Abstract: Disclosed herein are compounds that may be modulators of 5-HT receptors, and methods of making and using same.

Abstract translation: 本文公开了可以是5-HT受体的调节剂的化合物，以及制备和使用它们的方法。

公开(公告)号：US07855193B2

公开(公告)日：2010-12-21

申请号：US11491766

申请日：2006-07-24

Applicant: 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

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

CPC classification number: C07D405/10 ,  C07D307/80 ,  C07D307/81 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D417/14

Abstract: 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.

Abstract translation: 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：US07407966B2

公开(公告)日：2008-08-05

申请号：US10960769

申请日：2004-10-07

Applicant: Dale S. Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Laurence Wu ,  Mercedes Lobera ,  Pradyumna Mohanty ,  Yael Marantz ,  Boaz Inbal ,  Sharon Shacham ,  Dongli Chen

Inventor： Dale S. Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Laurence Wu ,  Mercedes Lobera ,  Pradyumna Mohanty ,  Yael Marantz ,  Boaz Inbal ,  Sharon Shacham ,  Dongli Chen

IPC: A01N43/42 ,  C07D471/02

CPC classification number: C07D495/04

Abstract: The invention relates to 5-HT4 receptor agonists and partial agonists. Thienopyridinone compounds and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT4 receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, Parkinson's disease, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, and nonulcer dyspepsia. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

Abstract translation: 本发明涉及5-HT 4受体激动剂和部分激动剂。 公开了噻吩并吡啶酮化合物及其用于治疗由5-HT 4受体直接或间接介导的疾病的合成及其用途。 这些病症包括阿尔茨海默氏病，认知障碍，肠易激综合征，帕金森病，恶心，呕吐，呕吐，运动失调，胃食管反流病和非溃疡性消化不良。 还包括制备方法和新型中间体及其药物盐。

公开(公告)号：US20080064677A9

公开(公告)日：2008-03-13

申请号：US11491766

申请日：2006-07-24

Applicant: 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

Inventor： 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: A61K31/452 ,  A61K31/397 ,  C07D405/02

CPC classification number: C07D405/10 ,  C07D307/80 ,  C07D307/81 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D417/14

Abstract: 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.

Abstract translation: 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。