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    • 9. 发明授权
    • Indolylmaleimide derivatives
    • 吲哚马来酰亚胺衍生物
    • US07534808B2
    • 2009-05-19
    • US12034675
    • 2008-02-21
    • Jean-Pierre EvenouPeter Von MattJürgen WagnerGerhard Zenke
    • Jean-Pierre EvenouPeter Von MattJürgen WagnerGerhard Zenke
    • A61K31/404
    • A61K31/496C07D401/14C07D403/04C07D403/14
    • Provided are compounds of Formula (I), which are useful in the treatment and/or prevention of diseases or disorders mediated by T lymphocytes and/or PKC, e.g. acute or chronic rejection of organ or tissue allo- or xenografts, graft versus host diseases, atherosclerosis, vascular occlusion due to vascular injury such as angioplasty, restenosis, obesity, syndrome X, impaired glucose tolerance, polycystic ovary syndrome, hypertension, heart failure, chronic obstructive pulmonary disease, CNS diseases such as Alzheimer disease or amyotrophic lateral sclerosis, cancer, infectious diseases such as AIDS, septic shock or adult respiratory distress syndrome, ischemia/reperfusion injury e.g. myocardial infraction, stroke, gut ischemia, renal failure or hemorrhage shock, or traumatic shock, e.g. traumatic brain injury. The compounds of (I) are also useful in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders or autoimmune diseases e.g. rheumatoid arthritis, osteoarthritis, systemic lupus erythematosus, Hashimoto's thyroidis, multiple sclerosis, myasthenia gravis, diabetes type I or II and the disorders associated therewith, e.g. angiopathy, diabetic proliferative retinopathy, diabetic macular edema, nephropathy, neuropathy and dawn phenomenon, respiratory diseases such as asthma or inflammatory lung injury, inflammatory liver injury, inflammatory glomerular injury, cutaneous manifestations of immunologically-mediated disorders or illnesses, inflammatory and hyperproliferative skin diseases (such as psoriasis, atopic dermatitis, allergic contact dermatitis, irritant contact dermatitis and further eczematous dermatitises, seborrhoeic dermatitis), inflammatory eye diseases, e.g. Sjoegren's syndrome, keratoconjunctivitis or uveitis, inflammatory bowel disease, Crohn's disease or ulcerative colitis.
    • 提供式(I)的化合物,其可用于治疗和/或预防由T淋巴细胞和/或PKC介导的疾病或病症,例如, 器官或组织异种移植物的急性或慢性排斥,移植物抗宿主病,动脉粥样硬化,血管损伤引起的血管闭塞,如血管成形术,再狭窄,肥胖症,综合征X,葡萄糖耐量降低,多囊卵巢综合征,高血压,心力衰竭, 慢性阻塞性肺疾病,中枢神经系统疾病如阿尔茨海默病或肌萎缩性侧索硬化,癌症,艾滋病感染性疾病,败血性休克或成人呼吸窘迫综合征,缺血/再灌注损伤 心肌梗死,中风,肠缺血,肾功能衰竭或出血性休克或创伤性休克,例如, 创伤性脑损伤。 (I)的化合物还可用于治疗和/或预防T细胞介导的急性或慢性炎性疾病或病症或自身免疫疾病,例如, 类风湿关节炎,骨关节炎,系统性红斑狼疮,桥本氏症,多发性硬化症,重症肌无力,I型或II型糖尿病及其相关疾病,例如。 血管病,糖尿病性增生性视网膜病变,糖尿病性黄斑水肿,肾病,神经病和黎明现象,呼吸系统疾病如哮喘或炎性肺损伤,炎症性肝损伤,炎性肾小球损伤,免疫介导的疾病或疾病的皮肤表现,炎性和过度增生性皮肤病 (如牛皮癣,特应性皮炎,过敏性接触性皮炎,刺激性接触性皮炎和进一步的湿疹性皮肤病,脂溢性皮炎),炎症性眼病 Sjoegren综合征,角膜结膜炎或葡萄膜炎,炎症性肠病,克罗恩病或溃疡性结肠炎。
    • 10. 发明授权
    • Indolylmaleimide derivatives
    • 吲哚马来酰亚胺衍生物
    • US07358253B2
    • 2008-04-15
    • US11546690
    • 2006-10-12
    • Jean-Pierre EvenouPeter Von MattJürgen WagnerGerhard Zenke
    • Jean-Pierre EvenouPeter Von MattJürgen WagnerGerhard Zenke
    • A61K31/496
    • A61K31/496C07D401/14C07D403/04C07D403/14
    • Provided are compounds of formula (I) which are useful in the treatment and/or prevention of diseases or disorders mediated by T lymphocytes and/or PKC, e.g. acute or chronic rejection of organ or tissue allo- or xenografts, graft versus host diseases, atherosclerosis, vascular occlusion due to vascular injury such as angioplasty, restenosis, obesity, syndrome X, impaired glucose tolerance, polycystic ovary syndrome, hypertension, heart failure, chronic obstructive pulmonary disease, CNS diseases such as Alzheimer disease or amyotrophic lateral sclerosis, cancer, infectious diseases such as AIDS, septic shock or adult respiratory distress syndrome, ischemia/reperfusion injury e.g. myocardial infarction, stroke, gut ischemia, renal failure or hemorrhage shock, or traumatic shock, e.g. traumatic brain injury. The compounds of formula I are also useful in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory disease or disorders or autoimmune diseases e.g. rheumatoid arthritis, osteoarthritis, systemic lupus erythematosus, Hashimotos thyroidis, multiple sclerosis, myasthenia gravis, diabetes type I or II and the disorders associated therewith, e.g. angiopathy, diabetic proliferative retinopathy, diabetic macular edema, nephropathy, neuropathy and dawn phenomenon, respiratory diseases such as asthma or inflammatory lung injury, inflammatory liver injury, inflammatory glomerular injury, cutaneous manifestations of immunologically-mediated disorders or illnesses, inflammatory and hyperproliferative skin diseases (such as psoriasis, atopic dermatitis, allergic contract dermatitis, irritant contact dermatitis and further eczematous dermatitises, seborrhoeic dermatitis), inflammatory eye diseases, e.g. Sjoegren's syndrome, keratoconjunctivitis or uveitis, inflammatory bowel disease, Crohn's disease or ulcerative colitis.
    • 提供式(I)化合物,其可用于治疗和/或预防由T淋巴细胞和/或PKC介导的疾病或病症,例如, 器官或组织异种移植物的急性或慢性排斥,移植物抗宿主病,动脉粥样硬化,血管损伤引起的血管闭塞,如血管成形术,再狭窄,肥胖症,综合征X,葡萄糖耐量降低,多囊卵巢综合征,高血压,心力衰竭, 慢性阻塞性肺疾病,中枢神经系统疾病如阿尔茨海默病或肌萎缩性侧索硬化,癌症,艾滋病感染性疾病,败血性休克或成人呼吸窘迫综合征,缺血/再灌注损伤 心肌梗塞,中风,肠缺血,肾功能衰竭或出血性休克,或创伤性休克,例如。 创伤性脑损伤。 式I化合物还可用于治疗和/或预防T细胞介导的急性或慢性炎性疾病或病症或自身免疫疾病,例如, 类风湿性关节炎,骨关节炎,系统性红斑狼疮,甲状腺桥本体,多发性硬化症,重症肌无力,I型或II型糖尿病及其相关疾病。 血管病,糖尿病性增生性视网膜病变,糖尿病性黄斑水肿,肾病,神经病和黎明现象,呼吸系统疾病如哮喘或炎性肺损伤,炎症性肝损伤,炎性肾小球损伤,免疫介导的疾病或疾病的皮肤表现,炎性和过度增生性皮肤病 (如银屑病,特应性皮炎,过敏性契约性皮炎,刺激性接触性皮炎和进一步的湿疹性皮肤病,脂溢性皮炎),炎症性眼病 Sjoegren综合征,角膜结膜炎或葡萄膜炎,炎症性肠病,克罗恩病或溃疡性结肠炎。