Agents for preventing and treating disorders involving modulation of the RyR receptors
    3.
    发明授权
    Agents for preventing and treating disorders involving modulation of the RyR receptors 有权
    用于预防和治疗涉及RyR受体调节的病症的药剂

    公开(公告)号:US08022058B2

    公开(公告)日:2011-09-20

    申请号:US11212309

    申请日:2005-08-25

    摘要: The present invention provides novel compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells. Such disorders and diseases include, by way of example only, cardiac disorders and diseases, skeletal muscular disorders and diseases, cognitive disorders and diseases, malignant hyperthermia, diabetes, and sudden infant death syndrome. Cardiac disorder and diseases include, but are not limited to, irregular heartbeat disorders and diseases; exercise-induced irregular heartbeat disorders and diseases; sudden cardiac death; exercise-induced sudden cardiac death; congestive heart failure; chronic obstructive pulmonary disease; and high blood pressure. Irregular heartbeat disorders and diseases include and exercise-induced irregular heartbeat disorders and diseases include, but are not limited to, atrial and ventricular arrhythmia; atrial and ventricular fibrillation; atrial and ventricular tachyarrhythmia; atrial and ventricular tachycardia; catecholaminergic polymorphic ventricular tachycardia (CPVT); and exercise-induced variants thereof. Skeletal muscular disorder and diseases include, but are not limited to, skeletal muscle fatigue, exercise-induced skeletal muscle fatigue, muscular dystrophy, bladder disorders, and incontinence. Cognitive disorders and diseases include, but are not limited to, Alzheimer's Disease, forms of memory loss, and age-dependent memory loss.

    摘要翻译: 本发明提供新的式I化合物及其盐,水合物,溶剂合物,络合物和前药。 本发明还提供了合成式I化合物的方法。本发明另外提供包含式I化合物的药物组合物和使用式I药物组合物的方法,以治疗和预防与调节钙的RyR受体相关的疾病和疾病 通道在单元格中起作用。 这样的疾病和疾病仅包括心脏病和疾病,骨骼肌障碍和疾病,认知障碍和疾病,恶性高热,糖尿病和婴儿猝死综合征。 心脏疾病和疾病包括但不限于不规则的心跳障碍和疾病; 运动引起的心律失常和疾病不规律; 心脏猝死; 运动性心源性猝死; 充血性心力衰竭; 慢性阻塞性肺疾病; 和高血压。 不规律的心跳疾病和疾病包括运动诱发的心律失常和疾病的疾病包括但不限于心房和室性心律失常; 心房和心室颤动; 心房和心室快速性心律失常; 心房和室性心动过速; 儿茶酚胺能多态性室性心动过速(CPVT); 和运动诱发的变体。 骨骼肌障碍和疾病包括但不限于骨骼肌疲劳,运动引起的骨骼肌疲劳,肌营养不良,膀胱障碍和失禁。 认知障碍和疾病包括但不限于阿尔茨海默病,记忆丧失的形式和年龄依赖性记忆丧失。

    Agents for preventing and treating disorders involving modulation of the RyR receptors
    4.
    发明授权
    Agents for preventing and treating disorders involving modulation of the RyR receptors 有权
    用于预防和治疗涉及RyR受体调节的病症的药剂

    公开(公告)号:US07704990B2

    公开(公告)日:2010-04-27

    申请号:US11212413

    申请日:2005-08-25

    IPC分类号: C07D281/02 A61K31/554

    摘要: The present invention provides novel compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells. Such disorders and diseases include, by way of example only, cardiac disorders and diseases, skeletal muscular disorders and diseases, cognitive disorders and diseases, malignant hyperthermia, diabetes, and sudden infant death syndrome. Cardiac disorder and diseases include, but are not limited to, irregular heartbeat disorders and diseases; exercise-induced irregular heartbeat disorders and diseases; sudden cardiac death; exercise-induced sudden cardiac death; congestive heart failure; chronic obstructive pulmonary disease; and high blood pressure. Irregular heartbeat disorders and diseases include and exercise-induced irregular heartbeat disorders and diseases include, but are not limited to, atrial and ventricular arrhythmia; atrial and ventricular fibrillation; atrial and ventricular tachyarrhythmia; atrial and ventricular tachycardia; catecholaminergic polymorphic ventricular tachycardia (CPVT); and exercise-induced variants thereof. Skeletal muscular disorder and diseases include, but are not limited to, skeletal muscle fatigue, exercise-induced skeletal muscle fatigue, muscular dystrophy, bladder disorders, and incontinence. Cognitive disorders and diseases include, but are not limited to, Alzheimer's Disease, forms of memory loss, and age-dependent memory loss.

    摘要翻译: 本发明提供新的式I化合物及其盐,水合物,溶剂合物,络合物和前药。 本发明还提供了合成式I化合物的方法。本发明另外提供包含式I化合物的药物组合物和使用式I药物组合物的方法,以治疗和预防与调节钙的RyR受体相关的疾病和疾病 通道在单元格中起作用。 这样的疾病和疾病仅包括心脏病和疾病,骨骼肌障碍和疾病,认知障碍和疾病,恶性高热,糖尿病和婴儿猝死综合征。 心脏疾病和疾病包括但不限于不规则的心跳障碍和疾病; 运动引起的心律失常和疾病不规律; 心脏猝死; 运动性心源性猝死; 充血性心力衰竭; 慢性阻塞性肺疾病; 和高血压。 不规律的心跳疾病和疾病包括运动诱发的心律失常和疾病的疾病包括但不限于心房和室性心律失常; 心房和心室颤动; 心房和心室快速性心律失常; 心房和室性心动过速; 儿茶酚胺能多态性室性心动过速(CPVT); 和运动诱发的变体。 骨骼肌障碍和疾病包括但不限于骨骼肌疲劳,运动引起的骨骼肌疲劳,肌营养不良,膀胱障碍和失禁。 认知障碍和疾病包括但不限于阿尔茨海默病,记忆丧失的形式和年龄依赖性记忆丧失。

    Agents for preventing and treating disorders involving modulation of the RyR receptors
    5.
    发明申请
    Agents for preventing and treating disorders involving modulation of the RyR receptors 有权
    用于预防和治疗涉及RyR受体调节的病症的药剂

    公开(公告)号:US20070173482A1

    公开(公告)日:2007-07-26

    申请号:US11506285

    申请日:2006-08-17

    IPC分类号: A61K31/675 A61K31/554

    摘要: The present invention provides compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells.

    摘要翻译: 本发明提供式I化合物及其盐,水合物,溶剂合物,络合物和前药。 本发明还提供了合成式I化合物的方法。本发明另外提供包含式I化合物的药物组合物和使用式I药物组合物的方法,以治疗和预防与调节钙的RyR受体相关的疾病和疾病 通道在单元格中起作用。

    Process for preparing benzothiazepines from gamma-aminoalkylbenzenes
    6.
    发明授权
    Process for preparing benzothiazepines from gamma-aminoalkylbenzenes 有权
    从γ-氨基烷基苯制备苯并硫氮杂的方法

    公开(公告)号:US08618282B2

    公开(公告)日:2013-12-31

    申请号:US12397212

    申请日:2009-03-03

    IPC分类号: C07D281/08 C07D281/10

    摘要: The invention provides a process for preparing a 2,3,4,5-tetrahydro[1,4]benzothiazepine of formula: by reacting a [2-(acylaminoethyl)thio]arene of formula with an aldehyde or a multimer thereof, and with an acid. The invention also provides for first reacting the [2-(acylaminoethyl)thio]arene with the aldehyde or multimer thereof and a base to form an [N-hydroxymethyl-2-[acylaminoethyl)thio]arene of formula then treating the [N-hydroxymethyl-2-(acylaminoethyl)thio]arene with the acid to form the 2,3,4,5-tetrahydro[1,4]benzothiazepine.

    摘要翻译: 本发明提供了制备下式的2,3,4,5-四氢[1,4]苯并硫氮杂的方法:通过使式的[2-(酰基氨基乙基)硫代]芳烃或其多聚体与 酸。 本发明还提供了使[2-(酰基氨基乙基)硫代]芳烃与其醛或多聚体和碱反应以形成式的[N-羟甲基-2- [酰氨基乙基]硫代]芳烃,然后将[N- 羟基甲基-2-(酰氨基乙基)硫代]芳烃与酸形成2,3,4,5-四氢[1,4]苯并硫氮杂。

    Agents for preventing and treating disorders involving modulation of the RyR receptors
    8.
    发明授权
    Agents for preventing and treating disorders involving modulation of the RyR receptors 有权
    用于预防和治疗涉及RyR受体调节的病症的药剂

    公开(公告)号:US07879840B2

    公开(公告)日:2011-02-01

    申请号:US11506285

    申请日:2006-08-17

    摘要: The present invention provides compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells.

    摘要翻译: 本发明提供式I化合物及其盐,水合物,溶剂合物,络合物和前药。 本发明还提供了合成式I化合物的方法。本发明另外提供包含式I化合物的药物组合物和使用式I药物组合物的方法,以治疗和预防与调节钙的RyR受体相关的疾病和疾病 通道在单元格中起作用。

    Anti-arrythmic and heart failure drugs that target the leak in the ryanodine receptor (RyR2)
    9.
    发明授权
    Anti-arrythmic and heart failure drugs that target the leak in the ryanodine receptor (RyR2) 失效
    针对雷诺地尔受体(RyR2)泄漏的抗心律失常药物和心力衰竭药物

    公开(公告)号:US07544678B2

    公开(公告)日:2009-06-09

    申请号:US11088058

    申请日:2005-03-23

    摘要: The present invention provides novel 1,4-benzothiazepine intermediates and derivatives, methods for synthesizing same, and methods for assaying same. The present invention also provides methods for using these novel compounds to limit or prevent a decrease in the level of RyR2-bound FKBP12.6 in a subject; to prevent exercise-induced sudden cardiac death in a subject; and to treat or prevent heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia in a subject. The present invention further provides methods for identifying an agent that enhances binding of RyR2 and FKBP12.6, and agents identified by these methods. Additionally, the present invention provides methods for identifying agents for use in treating or preventing heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia, and in preventing exercise-induced sudden cardiac death. Also provided are agents identified by such methods.

    摘要翻译: 本发明提供新的1,4-苯并硫氮杂中间体及其衍生物,其合成方法及其测定方法。 本发明还提供了使用这些新化合物来限制或防止受试者中RyR2结合的FKBP12.6水平降低的方法; 以防止受试者运动性心源性猝死; 并且治疗或预防受试者的心力衰竭,心房颤动或运动引起的心律失常。 本发明还提供用于鉴定增强RyR2和FKBP12.6的结合的试剂以及通过这些方法鉴定的试剂的方法。 此外,本发明提供用于鉴定用于治疗或预防心力衰竭,心房颤动或运动诱导的心律失常以及预防运动性心源性猝死的药剂的方法。 还提供了通过这种方法鉴定的药剂。

    Compounds and their preparation for the treatment of Alzheimer's disease by inhibiting beta-amyloid peptide production
    10.
    发明申请
    Compounds and their preparation for the treatment of Alzheimer's disease by inhibiting beta-amyloid peptide production 审中-公开
    化合物及其通过抑制β-淀粉样蛋白肽生产治疗阿尔茨海默氏病的制剂

    公开(公告)号:US20060014704A1

    公开(公告)日:2006-01-19

    申请号:US10961346

    申请日:2004-10-07

    IPC分类号: C07J17/00 A61K31/704

    CPC分类号: C07J17/00 C07J9/00

    摘要: The present invention provides novel ginsenoside compounds, compositions (e.g. pharmaceutical compositions) comprising the ginsenoside compounds, and methods for the synthesis of these ginsenoside compounds. Additionally, the present invention provides methods for inhibiting beta-amyloid peptide production and methods for treating or preventing a pathological condition, particularly, neurodegeneration diseases (e.g. Alzheimer's disease), using these ginsenoside compounds.

    摘要翻译: 本发明提供新型人参皂苷化合物,包含人参皂苷化合物的组合物(例如药物组合物),以及合成这些人参皂甙化合物的方法。 此外,本发明提供了使用这些人参皂苷化合物抑制β-淀粉样蛋白肽生产的方法和用于治疗或预防病理状况,特别是神经变性疾病(例如阿尔茨海默氏病)的方法。