公开(公告)号：US20060069110A1

公开(公告)日：2006-03-30

申请号：US11237513

申请日：2005-09-27

Applicant: Denise Andersen ,  Catherine Chang ,  James Falsey ,  Michael Frohn ,  Fang-Tsao Hong ,  Hongyu Liao ,  Longbin Liu ,  Patricia Lopez ,  Daniel Retz ,  Gilbert Rishton ,  Robert Rzasa ,  Aaron Siegmund ,  Seifu Tadesse ,  Nuria Tamayo ,  Christopher Tegley

Inventor： Denise Andersen ,  Catherine Chang ,  James Falsey ,  Michael Frohn ,  Fang-Tsao Hong ,  Hongyu Liao ,  Longbin Liu ,  Patricia Lopez ,  Daniel Retz ,  Gilbert Rishton ,  Robert Rzasa ,  Aaron Siegmund ,  Seifu Tadesse ,  Nuria Tamayo ,  Christopher Tegley

IPC: A61K31/506 ,  C07D403/14 ,  C07D403/04

CPC classification number: C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14

Abstract: The present invention relates to pyridines, pyrimidines and derivatives thereof, and pharmaceutically acceptable salts thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic β cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.

Abstract translation: 本发明涉及吡啶，嘧啶及其衍生物及其药学上可接受的盐。 还包括治疗炎症，类风湿性关节炎，斑节病，骨质疏松症，多发性骨髓瘤，葡萄膜炎，急性或慢性骨髓性白血病，胰腺β细胞破坏，骨关节炎，类风湿性脊椎炎，痛风性关节炎，炎性肠病，成人呼吸窘迫综合征 （ARDS），牛皮癣，克罗恩病，过敏性鼻炎，溃疡性结肠炎，过敏反应，接触性皮炎，哮喘，肌肉变性，恶病质，赖特综合征，I型糖尿病，II型糖尿病，骨吸收疾病，移植物抗宿主反应，阿尔茨海默病 ，中风，心肌梗塞，缺血再灌注损伤，动脉粥样硬化，脑外伤，多发性硬化，脑疟疾，败血症，败血性休克，中毒性休克综合征，发热，HIV-1，HIV-2，HIV-3，巨细胞病毒 ），流感病毒，腺病毒，哺乳动物中的疱疹病毒或带状疱疹感染，包括给予有效量的如上所述的化合物。

公开(公告)号：US20140378460A1

公开(公告)日：2014-12-25

申请号：US14241026

申请日：2012-08-27

Applicant: Susan M. Catalano ,  Gilbert Rishton ,  Nicholas J. Izzo

Inventor： Susan M. Catalano ,  Gilbert Rishton ,  Nicholas J. Izzo

IPC: C07D235/04 ,  C07C267/00 ,  G01N33/50 ,  C07D317/46 ,  C07D211/22 ,  C07C43/23 ,  C07C211/15 ,  C07C233/91

CPC classification number: C07D235/04 ,  A61K31/135 ,  A61K31/351 ,  A61K31/423 ,  A61K31/454 ,  A61K31/47 ,  A61K31/495 ,  A61K31/5377 ,  C07C43/23 ,  C07C211/15 ,  C07C233/91 ,  C07C267/00 ,  C07D211/22 ,  C07D317/46 ,  G01N33/5058 ,  G01N2333/705 ,  G01N2500/10

Abstract: This invention relates to the use sigma-2 receptor antagonists, and of pharmaceutical compositions comprising such compounds, in methods for inhibiting Abeta-associated synapse loss or synaptic dysfunction in neuronal cells, modulating an Abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with Abeta pathology and more broadly treating with such compounds and compositions neurodegenerative diseases and disorders associated with Abeta pathology. This invention also relates to methods for screening compounds for activity in inhibiting cognitive decline on the basis of their ability to bind to a sigma-2 receptor.

Abstract translation: 本发明涉及使用σ-2受体拮抗剂和包含这些化合物的药物组合物，用于抑制神经元细胞中Abeta相关突触丢失或突触功能障碍的方法，调节神经元细胞中与Abeta相关的膜转运变化，以及治疗 与Abeta病理学相关的认知衰退和用这种化合物和组合物更广泛地治疗与Abeta病理学相关的神经变性疾病和病症。 本发明还涉及用于根据其与σ-2受体结合的能力来筛选化合物抑制认知衰退活性的方法。

公开(公告)号：US20140378473A1

公开(公告)日：2014-12-25

申请号：US14241019

申请日：2012-08-27

Applicant: Susan M. Catalano ,  Gilbert Rishton ,  Nicholas J. Izzo

Inventor： Susan M. Catalano ,  Gilbert Rishton ,  Nicholas J. Izzo

IPC: C07D491/107 ,  C07D295/096 ,  C07D211/22 ,  C07C217/62 ,  C07D209/44

CPC classification number: C07D491/107 ,  C07B2200/07 ,  C07C211/28 ,  C07C211/29 ,  C07C215/54 ,  C07C217/58 ,  C07C217/62 ,  C07C235/60 ,  C07C317/32 ,  C07C2601/10 ,  C07C2602/10 ,  C07D209/44 ,  C07D211/14 ,  C07D211/22 ,  C07D295/08 ,  C07D295/096 ,  C07D319/18 ,  C07D491/10

Abstract: This invention relates to novel diarylamino compounds that bind to the sigma-2 receptor, to pharmaceutical compositions comprising such compounds, and to methods for inhibiting or restoring synapse loss in neuronal cells, modulating a membrane trafficking change in neuronal cells, and treating cognitive decline and neurodegenerative diseases and disorders therewith.

Abstract translation: 本发明涉及结合σ-2受体的新型二芳基氨基化合物，包含这些化合物的药物组合物，以及用于抑制或恢复神经元细胞突触损失，调节神经元细胞中的膜运输变化和治疗认知衰退的方法，以及 神经退行性疾病和疾病。