摘要:
The present invention is directed to modulators, such as inhibitors, of JNK isoform 2 (JNK2) or isoform 3 (JNK3) comprising compounds of formula (I) or formula (II) as described herein. Compounds of the invention can be used for treatment of a medical disorder in a patient wherein modulation of JNK3 is medically indicated, such as when the disorder is Parkinsons disease (PD) Alzheimer's disease (AD), Huntington's disease (HD), amyotrophic lateral sclerosis (ALS), multiple sclerosis (MS), myocardial infarction (MI), glaucoma, obesity, diabetes, cancer, rheumatoid arthritis, fibrotic disease, pulmonary fibrosis, kidney disease, liver inflammation, Crohns disease, hearing loss, Prader Willi syndrome, or a condition where modification of feeding behavior is medically indicated.
摘要:
The present invention relates to the new [6+5] fused bicycle derivatives, pharmaceutically acceptable salts or isomers thereof, processes for preparing the same, and pharmaceutical compositions comprising the same. The [6+5] fused bicycle derivatives can antagonize the thrombin receptor and thus may be effectively used for the treatment and prevention of thrombus, platelet aggregation, atherosclerosis, restenosis, blood coagulation, hypertension, arrhythmia, angina pectoris, heart failure, inflammation and cancer when used alone or with other cardiovascular agents.
摘要:
Disclosed herein are novel substituted-lH-quinazoline-2,4-dione derivatives, a preparation method thereof, and a pharmaceutical composition containing the same. The novel substituted- lH-quinazoline-2,4-dione derivatives are excellent in binding affinity and selectivity for 5-HT6 receptors over other receptors, inhibit serotonin(5-HT)-stimulated cAMP accumulation, and disrupt apomorphine(2 mg/kg, i.p.)-induced hyperactivity in rats. Thanks to these effects, the derivatives are useful in the treatment of 5-HT6 receptor-related central nervous system diseases.
摘要翻译:本文公开了新的取代的1H-喹唑啉-2,4-二酮衍生物,其制备方法和含有该取代基的喹唑啉-2,4-二酮衍生物的药物组合物。 新型取代的1H-喹唑啉-2,4-二酮衍生物对5-HT6受体的结合亲和力和其他受体的选择性优于其他受体,抑制5-羟色胺(5-HT)刺激的cAMP积累,并破坏阿扑吗啡(2mg / kg ,ip)诱导大鼠活动过度。 由于这些效果,衍生物可用于治疗5-HT6受体相关的中枢神经系统疾病。
摘要:
A projection television including a light source emitting light; and color wheel including a plurality of color filters provided in front of the light source and transmitting the light from the light source, a driver rotatably driving the plurality of color filters, and a supporter having a first side coupled to the driver and a second side coupled to the plurality of color filters so as to rotatably support the plurality of color filters, the driver being provided in a center portion of the color wheel, the plurality of color filters are provided around an edge of the color wheel being spaced from the driver, and a heat barrier being provided between the driver and the plurality of color filters to prevent heat generated due to the plurality of color filters from being transmitted to the driver. Thus, a projection television having a color filter absorbing heat generated from the light source disposed separately from the driver so as to prevent functional quality of the color wheel from being degraded due to the heat is provided.
摘要:
The present invention is to provide a method and a transdermal drug delivery device for treating erectile dysfunction which comprises a patch (100) containing pharmaceutically active ingredient and being directly applied to the male glans and its support (200) and the rings (30) for compressing the base part of the penis to aid the erection. The patch according to the present invention may be divided into two types, i.e. a cylinder type patch and a multi-reservoir type patch. The transdermal drug delivery patch device of the present invention is painless and safely to use and may be effectively produced and maintained erection of the penis without the adverse side effects and with a high degree of patient acceptability in the case of male impotence.
摘要:
The present invention relates to the new [6+5] fused bicycle derivatives, pharmaceutically acceptable salts or isomers thereof, processes for preparing the same, and pharmaceutical compositions comprising the same. The [6+5] fused bicycle derivatives can antagonize the thrombin receptor and thus may be effectively used for the treatment and prevention of thrombus, platelet aggregation, atherosclerosis, restenosis, blood coagulation, hypertension, arrhythmia, angina pectoris, heart failure, inflammation and cancer when used alone or with other cardiovascular agents.
摘要:
Disclosed herein are a new indole carboxylic acid bispyridyl carboxamide derivative, a preparation method thereof, and a composition for prevention or treatment of obesity, urinary disorders, and CNS disorders, containing the same as an active ingredient. Because the indole carboxylic acid bispyridyl carboxamide derivatives according to the present invention have high affinity for 5-HT 2c receptors, act selectively on the 5-HT 2c receptors, the derivatives rarely have adverse effects caused by other receptors. Because the derivatives effectively inhibit serotonin activity, they may be useful for treatment or prevention of obesity; urinary disorders such as urinary incontinence, premature ejaculation, erectile dysfunction, and prostatic hyperplasia; CNS disorders such as depression, anxiety, concern, panic disorder, epilepsy, obsessive-compulsive disorder, migraine, sleep disorder, withdrawal from drug abuse, Alzheimer's disease, and schizophrenia, associated with 5-HT 2c receptors.
摘要:
Disclosed herein are a new indole carboxylic acid bispyridyl carboxamide derivative, a preparation method thereof, and a composition for prevention or treatment of obesity, urinary disorders, and CNS disorders, containing the same as an active ingredient. Because the indole carboxylic acid bispyridyl carboxamide derivatives according to the present invention have high affinity for 5-HT2c receptors, act selectively on the 5-HT2c receptors, the derivatives rarely have adverse effects caused by other receptors. Because the derivatives effectively inhibit serotonin activity, they may be useful for treatment or prevention of obesity; urinary disorders such as urinary incontinence, premature ejaculation, erectile dysfunction, and prostatic hyperplasia; CNS disorders such as depression, anxiety, concern, panic disorder, epilepsy, obsessive-compulsive disorder, migraine, sleep disorder, withdrawal from drug abuse, Alzheimer's disease, and schizophrenia, associated with 5-HT2c receptors.
摘要:
The present invention relates to compounds of substituted-1,1-dioxo-benzo[1,2,4]thiadiazin-3-ones acting as a 5HT6 receptor antagonist, a preparation method thereof, and a pharmaceutical composition containing the same for treatment of the central nervous system disorders. The compounds of substituted-1,1-dioxo-benzo[1,2,4]thiadiazin-3-ones according to the present invention have excellent binding affinity for the 5HT6 receptor and excellent selectivity for the 5HT6 receptor over other receptors. Also, the compounds reverse a disruption of PPI by apomorphine and don't show rotatod deficit in mice. Therefore the compounds according to the present invention may be valuably used for treatment of a 5HT6 receptor relating disorders.