SUBSTITUTED PHENYLPIPERIDINES WITH SEROTONINERGIC ACTIVITY AND ENHANCED THERAPEUTIC PROPERTIES
    42.
    发明申请
    SUBSTITUTED PHENYLPIPERIDINES WITH SEROTONINERGIC ACTIVITY AND ENHANCED THERAPEUTIC PROPERTIES 审中-公开
    具有丝氨酸活性和增强治疗性质的替代苯基哌啶

    公开(公告)号:US20110130424A1

    公开(公告)日:2011-06-02

    申请号:US12916894

    申请日:2010-11-01

    CPC分类号: C07D405/12

    摘要: Chemical syntheses and medical uses of novel inhibitors of the uptake of monoamine neurotransmitters and pharmaceutically acceptable salts and prodrugs thereof, for the treatment and/or management of psychotropic disorders, anxiety disorder, generalized anxiety disorder, depression, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, hot flashes, senile dementia, migraine, hepatopulmonary syndrome, chronic pain, nociceptive pain, neuropathic pain, painful diabetic retinopathy, bipolar depression, obstructive sleep apnea, psychiatric disorders, premenstrual dysphoric disorder, social phobia, social anxiety disorder, urinary incontinence, anorexia, bulimia nervosa, obesity, ischemia, head injury, calcium overload in brain cells, drug dependence, and/or premature ejaculation are described.

    摘要翻译: 用于治疗和/或治疗精神病症,焦虑障碍,广泛性焦虑症,抑郁症,创伤后应激障碍,强迫症的单胺神经递质及其药学上可接受的盐和前药的新型抑制剂的化学合成和医学用途, 强迫症,恐慌症,热潮红,老年痴呆,偏头痛,肝肺综合征,慢性疼痛,伤害性疼痛,神经性疼痛,疼痛性糖尿病性视网膜病变,双相抑郁症,阻塞性睡眠呼吸暂停,精神疾病,经前焦虑症,社交恐惧症,社交焦虑症 ,尿失禁,厌食症,神经性贪食症,肥胖症,局部缺血,头部损伤,脑细胞中的钙超载,药物依赖性和/或早泄。

    SUBSTITUTED PDE5 INHIBITORS
    43.
    发明申请
    SUBSTITUTED PDE5 INHIBITORS 审中-公开
    取代PDE5抑制剂

    公开(公告)号:US20100234388A1

    公开(公告)日:2010-09-16

    申请号:US12303720

    申请日:2007-06-08

    CPC分类号: C07D471/14 C07B2200/05

    摘要: Provided herein are substituted PDE5 inhibitors of Formula (1), and processes of preparation and pharmaceutical compositions thereof. Also provided are methods of their use for the treatment and/or management of hypertension, erectile dysfunction, and/or the inability to maintain improved erectile function. The compounds are deuterated tadalafil derivatives.

    摘要翻译: 本文提供了式(1)的取代的PDE5抑制剂及其制备方法及其药物组合物。 还提供了它们用于治疗和/或治疗高血压,勃起功能障碍和/或不能维持改善的勃起功能的方法。 化合物是氘化的他达拉非衍生物。

    PREPARATION AND UTILITY OF HMG-COA REDUCTASE INHIBITORS
    45.
    发明申请
    PREPARATION AND UTILITY OF HMG-COA REDUCTASE INHIBITORS 审中-公开
    HMG-COA还原抑制剂的制备和应用

    公开(公告)号:US20100137244A1

    公开(公告)日:2010-06-03

    申请号:US12373228

    申请日:2007-07-12

    CPC分类号: C07D309/30

    摘要: Chemical syntheses and medical uses of novel modulators of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase and diastereomeric mixtures of isomers, individual diastereomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, the chemical synthesis thereof, and the medical use of such compounds for the treatment and/or management of hypercholesterolemia, dyslipidemia, coronary artery disease, atherosclerosis, metabolic syndrome, a hyperproliferative disease such as colorectal cancer, prostate cancer, and melanoma, a neurodegenerative disease such as cerebral ischemia, Alzheimer's disease, and Parkinson's disease are described.

    摘要翻译: 3-羟基-3-甲基戊二酰辅酶A(HMG-CoA)还原酶和异构体的非对映异构体混合物,其各自的非对映异构体,药学上可接受的盐,溶剂合物或前药的新型调节剂的化学合成和医学用途,其化学合成和 用于治疗和/或治疗高胆固醇血症,血脂异常,冠状动脉疾病,动脉粥样硬化,代谢综合征,过度增殖性疾病如结肠直肠癌,前列腺癌和黑素瘤的医学用途,神经变性疾病如脑缺血,阿尔茨海默病 ,帕金森氏病。

    METHODS OF REDUCTION OF INTERPATIENT VARIABILITY
    48.
    发明申请
    METHODS OF REDUCTION OF INTERPATIENT VARIABILITY 审中-公开
    减少互补性变异的方法

    公开(公告)号:US20100076087A1

    公开(公告)日:2010-03-25

    申请号:US12422834

    申请日:2009-04-13

    IPC分类号: A61K31/137 A61P25/24

    摘要: Disclosed herein are methods for the reduction of inter-patient variability of a drug, such as in one or more parameters including half-life (t1/2), maximum plasma concentration (Cmax), time at maximal plasma concentration (Tmax), area under the time-versus-concentration curve (AUC). Also provided are methods of reducing side effects associated with drugs.

    摘要翻译: 本文公开了用于减少药物的患者间变异性的方法,例如在包括半衰期(t1 / 2),最大血浆浓度(Cmax),最大血浆浓度(Tmax)时间),面积 在时间 - 浓度曲线(AUC)下。 还提供减少与药物相关的副作用的方法。