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    • 54. 发明申请
    • SUBSTITUTED-2-IMIDAZOLES
    • 取代的2-IMIDAZOLES
    • US20080113980A1
    • 2008-05-15
    • US11931246
    • 2007-10-31
    • Guido GalleyKatrin Groebke ZbindenRoger NorcrossHenri Stalder
    • Guido GalleyKatrin Groebke ZbindenRoger NorcrossHenri Stalder
    • A61K31/538A61K31/4178C07D403/02C07D413/02
    • C07D413/06C07D401/06C07D403/06
    • The present invention relates to compounds of formula I wherein R1 is selected from the group consisting of hydrogen and lower alkyl; each R2 is independently selected from the group consisting of hydrogen and lower alkyl; each R3 is independently selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, phenyloxy, benzyloxy, halogen and lower alkyl substituted by halogen; X is selected from the group consisting of —CH2—, —CH— and —O—; Y is selected from the group consisting of —CH2—, —CH— and a bond with the proviso that, when X is —O—, Y may not be a bond; Z is selected from the group consisting of —CH2— and —CH—; m is 0, 1 or 2; and n is 0, 1 or 2; and to pharmaceutically-acceptable acid addition salts of such compounds. The invention relates also to processes for preparing such compounds, compositions comprising such a compound or a pharmaceutically-acceptable acid addition salt thereof, and a method of treating a disease or disorder in a patient comprising administering such a compound, or pharmaceutically-acceptable acid addition salt thereof, to a patient in need of such treatment.
    • 本发明涉及式I化合物,其中R 1选自氢和低级烷基; 每个R 2独立地选自氢和低级烷基; 每个R 3独立地选自氢,低级烷基,低级烷氧基,苯氧基,苄氧基,卤素和被卤素取代的低级烷基; X选自-CH 2 - , - CH-和-O-; Y选自-CH 2 - , - CH-和键,条件是当X是-O-时,Y可以不是键; Z选自-CH 2 - 和-CH-; m为0,1或2; 且n为0,1或2; 以及这些化合物的药学上可接受的酸加成盐。 本发明还涉及制备这种化合物的方法,包含这种化合物或其药学上可接受的酸加成盐的组合物,以及治疗患者疾病或病症的方法,包括给予这种化合物或药学上可接受的酸加成 其盐,需要这种治疗的患者。
    • 55. 发明申请
    • Methods for treating CNS disorders with 4-imidazole derivatives
    • 用4-咪唑衍生物治疗CNS障碍的方法
    • US20070197622A1
    • 2007-08-23
    • US11655539
    • 2007-01-19
    • Guido GalleyKatrin Groebke ZbindenMarius HoenerRoger NorcrossHenri Stalder
    • Guido GalleyKatrin Groebke ZbindenMarius HoenerRoger NorcrossHenri Stalder
    • A61K31/415C07D233/56
    • C07D233/64C07D405/06
    • The present invention relates to methods for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R, Ar, R1, R1′, R2, and n are as defined in the specification and to their pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms. The invention also relates to novel compounds of formula I, compositions containing them, and methods for their preparation.
    • 本发明涉及治疗抑郁症,焦虑障碍,双相情感障碍,注意力缺陷多动障碍,应激相关障碍,精神病性精神病,如帕金森病,神经变性疾病如阿尔茨海默病,癫痫,偏头痛, 高血压,药物滥用和代谢障碍如进食障碍,糖尿病,糖尿病并发症,肥胖症,血脂异常,能量消耗和同化障碍,体温平衡紊乱和失调,睡眠和昼夜节律紊乱以及心血管疾病,其包括给予 个体治疗有效量的式I化合物,其中R,Ar,R 1,R 1,R 2,R 2和n 在本说明书中以及其药学活性盐,外消旋混合物,对映异构体,光学异构体和互变异构体形式中所定义。 本发明还涉及式I的新化合物,含有它们的组合物及其制备方法。
    • 60. 发明授权
    • 2-aminooxazolines as TAAR1 ligands
    • 2-氨基恶唑啉作为TAAR1配体
    • US08604061B2
    • 2013-12-10
    • US13426736
    • 2012-03-22
    • Guido GalleyKatrin Groebke ZbindenRoger NorcrossHenri Stalder
    • Guido GalleyKatrin Groebke ZbindenRoger NorcrossHenri Stalder
    • A01N43/40A61K31/44C07D413/00
    • C07D263/28C07D413/04C07D413/06C07D413/12C07F7/0812
    • The invention relates to compounds of formula I wherein X, Y, R1, R2, and n are as defined herein or to a pharmaceutically suitable acid addition salt thereof. The invention also relates to pharmaceutical compositions containing such compounds and methods for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases include depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
    • 本发明涉及其中X,Y,R 1,R 2和n如本文所定义或其药学上合适的酸加成盐的式I化合物。 本发明还涉及含有这些化合物的药物组合物和用于治疗与微量胺相关受体的生物功能相关的疾病的方法,所述疾病包括抑郁症,焦虑障碍,双相情感障碍,注意缺陷多动障碍,应激相关疾病, 精神病,精神分裂症,神经系统疾病,帕金森病,神经变性疾病,阿尔茨海默病,癫痫,偏头痛,药物滥用和代谢紊乱,进食障碍,糖尿病,糖尿病并发症,肥胖症,血脂异常,能量消耗和同化障碍, 体温稳态,睡眠障碍和昼夜节律,以及心血管疾病。