Therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders
    121.
    发明授权
    Therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders 失效
    用于治疗癌症,代谢疾病和皮肤病症的治疗剂

    公开(公告)号:US07572816B2

    公开(公告)日:2009-08-11

    申请号:US10514383

    申请日:2004-07-21

    CPC分类号: C07D233/72 C07D277/34

    摘要: The present invention is directed to compounds having the structure wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells. The invention also discloses pharmaceutical compositions and methods of treatment of disease in mammals

    摘要翻译: 本发明涉及具有其中R 1,R 2,R 3,R 4,R 5和m如本文所定义的结构的化合物。 本发明的化合物是用于治疗哺乳动物受试者的癌症,代谢疾病和皮肤病症的新型治疗剂。 这些化合物也是基因表达的有用调节剂。 它们通过干扰某些细胞信号转导级联发挥其活性。 因此,本发明的化合物也可用于调节由各种激素或细胞因子控制或调节的细胞分化和细胞周期过程。 特别地,本发明涉及诱导癌细胞凋亡的化合物,因此可用于治疗或预防癌症,包括晚期癌症和癌前细胞。 本发明还公开了哺乳动物疾病的药物组合物和治疗方法

    SUBSTITUTED PHENETHYLAMINES WITH SEROTONINERGIC AND/OR NOREPINEPHRINERGIC ACTIVITY
    122.
    发明申请
    SUBSTITUTED PHENETHYLAMINES WITH SEROTONINERGIC AND/OR NOREPINEPHRINERGIC ACTIVITY 有权
    具有丝氨酸和/或非诺贝宁活性的取代的苯乙烯

    公开(公告)号:US20090018207A1

    公开(公告)日:2009-01-15

    申请号:US12234236

    申请日:2008-09-19

    IPC分类号: A61K31/135 C07C211/27

    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 PYRROLIDINES
    123.
    发明申请
    SUBSTITUTED PYRROLIDINES 审中-公开
    取代吡咯烷酮

    公开(公告)号:US20090005431A1

    公开(公告)日:2009-01-01

    申请号:US12164918

    申请日:2008-06-30

    CPC分类号: C07D405/06

    摘要: Disclosed herein are substituted pyrrolidine-based muscarinic receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

    摘要翻译: 本文公开了式I的取代的吡咯烷类毒蕈碱受体调节剂,其制备方法,其药物组合物及其使用方法。

    Therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders
    125.
    发明授权
    Therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders 有权
    用于治疗癌症,代谢疾病和皮肤病症的治疗剂

    公开(公告)号:US07468462B2

    公开(公告)日:2008-12-23

    申请号:US11592009

    申请日:2006-11-01

    申请人: Sepehr Sarshar

    发明人: Sepehr Sarshar

    摘要: The present invention is directed to novel compounds according to formulae wherein R1, R2, R3 and R4 are as defined herein. The invention also discloses methods of preparation, pharmaceutical compositions, and methods of disease treatment utilizing pharmaceutical compositions comprising these compounds. The compounds of this invention are novel therapeutic agents for the treatment of cancer, diabetes, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. The invention also discloses pharmaceutical compositions and methods of treatment of disease in mammals.

    摘要翻译: 本发明涉及下式的新化合物,其中R 1,R 2,R 3和R 4如本文所定义。 本发明还公开了使用包含这些化合物的药物组合物的制备方法,药物组合物和疾病治疗方法。 本发明的化合物是用于治疗哺乳动物受试者中的癌症,糖尿病,代谢疾病和皮肤病症的新型治疗剂。 这些化合物也是基因表达的有用调节剂。 它们通过干扰某些细胞信号转导级联发挥其活性。 因此,本发明的化合物也可用于调节由各种激素或细胞因子控制或调节的细胞分化和细胞周期过程。 本发明还公开了哺乳动物疾病的药物组合物和治疗方法。

    PREPARATION AND UTILITY OF SUBSTITUTED CARBOXYLIC ACID COMPOUNDS
    129.
    发明申请
    PREPARATION AND UTILITY OF SUBSTITUTED CARBOXYLIC ACID COMPOUNDS 审中-公开
    取代的羧酸化合物的制备和应用

    公开(公告)号:US20070276042A1

    公开(公告)日:2007-11-29

    申请号:US11752238

    申请日:2007-05-22

    IPC分类号: A61K31/192 C07C57/30

    摘要: The present disclosure is directed to modulators of cyclooxygenase (COX) enzymes and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the medical use of such compounds for the treatment and/or management of the severity and duration of non-specific pain, tension-type pain, headache, migraine, lower back pain, sciatica, dental pain, muscular pain, pain associated with acute soft tissue injuries, bursitis, tendonitis, lumbago, periarthritis, tennis elbow, sprains, strains, muscular problems associated with sports injuries, muscular problems associated with accidents, period pain, primary dysmenorrhoea, acute sore throat pain, osteoarthritis, rheumatoid arthritis, cancer, any disorder requiring analgesic response, any disorder requiring anti-inflammatory response, any disorder requiring antipyretic response, any conditions mediated by cyclooxygenase, cystic fibrosis, dementia, Alzheimer's disease, and/or conditions mediated by levels of β-amyloid are described.

    摘要翻译: 本公开涉及环氧合酶(COX)酶及其药学上可接受的盐和前药的调节剂,其化学合成以及这些化合物用于治疗和/或治疗非特异性疼痛的严重性和持续时间的医学用途 ,紧张型疼痛,头痛,偏头痛,下背痛,坐骨神经痛,牙痛,肌肉疼痛,与急性软组织损伤相关的疼痛,滑囊炎,腱炎,腰痛,关节炎,网球肘,扭伤,应变,与运动相关的肌肉问题 伤害,与事故相关的肌肉问题,周期性疼痛,原发性痛经,急性喉痛,骨关节炎,类风湿性关节炎,癌症,需要镇痛反应的任何疾病,需要抗炎反应的任何疾病,需要解热反应的任何病症,任何由 环氧合酶,囊性纤维化,痴呆,阿尔茨海默病和/或由β-戊基水平介导的病症 描述了oid。

    Substituted phenylpiperidines with serotoninergic activity and enhanced therapeutic properties
    130.
    发明申请
    Substituted phenylpiperidines with serotoninergic activity and enhanced therapeutic properties 审中-公开
    取代的苯基哌啶与5-羟色胺能活性和增强的治疗性质

    公开(公告)号:US20070112031A1

    公开(公告)日:2007-05-17

    申请号:US11598572

    申请日:2006-11-13

    IPC分类号: A61K31/452 C07D405/02

    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。