Cytoprotective benzofuran derivatives
    22.
    发明授权
    Cytoprotective benzofuran derivatives 失效
    细胞保护性苯并呋喃衍生物

    公开(公告)号:US06653346B1

    公开(公告)日:2003-11-25

    申请号:US10361141

    申请日:2003-02-06

    申请人: Bing Wang Jian Chen

    发明人: Bing Wang Jian Chen

    IPC分类号: A61K3134

    摘要: Cytoprotective compounds, many of which are benzofuran derivatives are useful in the treatment of certain ischemic or inflammatory conditions, including but not limited to stroke, myocardial infarction, congestive heart failure, and skin disorders characterized by inflammation or oxidative damage. They are also useful in the manufacture of pharmaceutical and cosmetic formulations for the treatment of such conditions.

    摘要翻译: 其中许多是苯并呋喃衍生物的细胞保护化合物可用于治疗某些缺血性或炎症性疾病,包括但不限于中风,心肌梗死,充血性心力衰竭和以炎症或氧化损伤为特征的皮肤病症。 它们也可用于制备用于治疗这些病症的药物和化妆品制剂。

    Aromatic heterocycle compounds having HIV integrase inhibiting activities
    24.
    发明授权
    Aromatic heterocycle compounds having HIV integrase inhibiting activities 失效
    具有HIV整合酶抑制活性的芳族杂环化合物

    公开(公告)号:US06620841B1

    公开(公告)日:2003-09-16

    申请号:US09857632

    申请日:2001-06-07

    IPC分类号: A61K3134

    摘要: A compound of the formula (I): wherein X is hydroxy, protected hydroxy or optionally substituted amino; Y is —COORA wherein RA is hydrogen or ester residue, —CONRBRC wherein RB and RC each is independently hydrogen or amide residue, optionally substituted aryl or optionally substituted heteroaryl; and A1 is optionally substituted heteroaryl; provided that a compound wherein Y and/or A1 is optionally substituted indol-3-yl is excluded, a tautomer, a prodrug, a pharmaceutically acceptable salt or a hydrate thereof has an inhibitory activity against an integrase.

    摘要翻译: 式(I)的化合物:其中X是羟基,保护的羟基或任选取代的氨基; Y是-COORA,其中RA是氢或酯残基,-CONRBRC,其中RB和RC各自独立地是氢或酰胺残基,任选取代的芳基或任选取代的杂芳基; 并且A 1是任选取代的杂芳基; 不包括其中Y和/或A 1为任选取代的吲哚-3-基的化合物,其互变异构体,前药,药学上可接受的盐或其水合物对整合酶具有抑制活性。

    Method for delivering ascorbic acid and acetone to the dermal layer of the skin
    25.
    发明授权
    Method for delivering ascorbic acid and acetone to the dermal layer of the skin 有权
    将抗坏血酸和丙酮输送到皮肤真皮层的方法

    公开(公告)号:US06602906B1

    公开(公告)日:2003-08-05

    申请号:US09683994

    申请日:2002-03-09

    IPC分类号: A61K3134

    摘要: The present invention provides a more efficient method of delivering therapeutically effective amounts of ascorbic acid and acetone to the dermal layer of the skin via the topical application of 5,6-O-isopropylidene L-ascorbic acid. This invention further provides a stable, cosmetically acceptable vehicle in which the 5,6-O-isopropylidene L-ascorbic acid can be applied to the skin.

    摘要翻译: 本发明提供了通过局部施用5,6-O-异亚丙基L-抗坏血酸将治疗有效量的抗坏血酸和丙酮递送至皮肤真皮层的更有效的方法。 本发明还提供一种稳定的化妆品可接受的载体,其中可以将5,6-O-异亚丙基L-抗坏血酸施用于皮肤。

    Method for treatment of aging or damage skin

    公开(公告)号:US06444699B1

    公开(公告)日:2002-09-03

    申请号:US09732385

    申请日:2000-12-07

    IPC分类号: A61K3134

    摘要: An ascorbic acid-based composition and related method for the treatment of aging or photo-damaged skin is disclosed. The composition includes water and ascorbic acid, at least a portion of which has generally been pretreated by being dissolved under relatively high temperature and concentration conditions. The composition typically includes at least about 5.0% (w/v) ascorbic acid and may advantageously be formulated to have a pH above 3.5. Generally, the composition also includes non-toxic zinc salt, tyrosine compound, and/or pharmaceutically acceptable carrier. In addition, the composition may include an anti-inflammatory compound, such as aminosugar and/or sulfur-containing anti-inflammatory compound. The topical composition may be in the form of a serum, a hydrophilic lotion, an ointment, a cream, or a gel.

    Sulfonyl urea derivatives and their use in the control of interleukin-1 activity
    28.
    发明授权
    Sulfonyl urea derivatives and their use in the control of interleukin-1 activity 失效
    磺酰脲衍生物及其在控制白细胞介素-1活性中的应用

    公开(公告)号:US06433009B1

    公开(公告)日:2002-08-13

    申请号:US09703142

    申请日:2000-10-31

    IPC分类号: A61K3134

    摘要: A compound of the formula wherein R1 and R2 are as defined above, useful in the treatment and condition selected from the group consisting of meningitis and salpingitis, septic shock, disseminated intravascular coagulation, and/or adult respiratory distress syndrome, acute or chronic inflammation, arthritis, cholangitis, colitis, encephalitis, endocarditis, glomerulonephritis, hepatitis, myocarditis, pancreatitis, pericarditis, reperfusion injury, vasculitis, acute and delayed hypersensitivity, graft rejection, and graft-versus-host disease, auto-immune diseases including Type 1 diabetes mellitus and multiple sclerosis, periodonate diseases, interstitial pulmonary fibrosis, cirrhosis, systemic sclerosis, keloid formation, tumors which produce IL-1 as an autocrine growth factor, cachexia, Alzheimers disease, percussion injury, depression, atherosclerosis, osteoporosis in a mammal, including a human.

    摘要翻译: 化合物R1和R2如上所定义,可用于治疗和选自脑膜炎和输卵管炎,败血性休克,弥散性血管内凝血和/或成人呼吸窘迫综合征,急性或慢性炎症,关节炎 ,胆管炎,结肠炎,脑炎,心内膜炎,肾小球性肾炎,肝炎,心肌炎,胰腺炎,心包炎,再灌注损伤,血管炎,急性和迟发型超敏反应,移植排斥反应和移植物抗宿主病,自身免疫疾病包括1型糖尿病和 多发性硬化,牙周病,间质性肺纤维化,肝硬化,全身性硬化症,瘢痕疙瘩形成,产生作为自分泌生长因子的IL-1的肿瘤,恶病质,阿尔茨海默病,打击乐器损伤,抑郁症,动脉粥样硬化,哺乳动物包括人类的骨质疏松症 。

    Muscarinic receptor agonists
    30.
    发明授权
    Muscarinic receptor agonists 失效
    毒蕈碱受体激动剂

    公开(公告)号:US06211204B1

    公开(公告)日:2001-04-03

    申请号:US09483334

    申请日:2000-01-14

    IPC分类号: A61K3134

    CPC分类号: C07D417/14

    摘要: A compound of Formula (I): wherein R is independently selected from (CH2)9−12, (CH2CH2)2O, (CH2CH2)3O2, (CH2CH2)4O3, (CH2CH2)5O4, (CH2CH2)6O5 or (CH2CH2CH2)3O2; or an acid addition salt or hydrate thereof. The compounds, with improved water solubility, have unusually high affinity for muscarinic receptors, and exhibit agonist activity useful in the treatment of neurological and other disorders, in which stimulating cholinergic activity is desirable.

    摘要翻译: 式(I)化合物:其中R独立地选自(CH 2)9-12,(CH 2 CH 2)2 O,(CH 2 CH 2)3 O 2,(CH 2 CH 2)4 O 3,(CH 2 CH 2)5O 4,(CH 2 CH 2) ; 或其酸加成盐或其水合物。 具有改善的水溶性的化合物对毒蕈碱受体具有非常高的亲和力,并且表现出可用于治疗刺激胆碱能活性的神经和其他疾病的激动剂活性。