Thiazolidinone compounds useful as chemokine inhibitors
    12.
    发明授权
    Thiazolidinone compounds useful as chemokine inhibitors 有权
    可用作趋化因子抑制剂的噻唑烷酮化合物

    公开(公告)号:US06506751B1

    公开(公告)日:2003-01-14

    申请号:US09705219

    申请日:2000-11-02

    IPC分类号: C07D41306

    摘要: Disclosed are compounds of the Formula I wherein: Z is C or nothing, provided that when Z is nothing, R3 and R4 are nothing; A is S, S═O or O═S═O; R1 and R2 are independently hydrogen, lower alkyl, halogen, hydroxy or lower alkoxy, (un)substituted aryl, (un)substituted arylalkyl, (un)substituted heteroaryl or(un)substituted heteroarylakyl; R3 and R4 independently represent hydrogen, lower alkyl, cycloalkyl, aminoalkyl, mono- or dialkylaminoalkyl, (un)substituted aryl or (un)substituted heteroaryl; R5 represents a (un)substituted carbocyclic group containing from 3-7 members, up to two of which members are optionally hetero atoms; or R5 is (CR6R7)—(CH2)n—XR8R9; X is S or N; R6, R7, R8, R9, and n are as defined in the specification. The compounds are useful in the treatment and prevention of the AIDS virus. Intermediates useful in the preparation of the final products, pharmaceutical compositions containing the final products are also taught.

    摘要翻译: 公开了式I的化合物,其中Z为C或无,条件是当Z不为任何时,R 3和R 4不为任何; A为S,S = O或O = S = O; R 1和R 2独立地为氢,低级烷基 ,卤素,羟基或低级烷氧基,(未)取代的芳基,(未)取代的芳基烷基,(未)取代的杂芳基或(未)取代的杂芳基; R3和R4独立地表示氢,低级烷基,环烷基,氨基烷基, ,(un)取代的芳基或(未)取代的杂芳基; R 5表示含有3-7个成员的(未)取代的碳环基,其中至多两个为任意的杂原子; 或R 5是(CR 6 R 7) - (CH 2)n -XR 8 R 9; X是S或N; R 6,R 7,R 8,R 9和n如说明书中所定义。该化合物可用于治疗和预防艾滋病毒。 还教导了用于制备最终产品的中间体,含有最终产品的药物组合物。

    Benzene butyric acids and their derivatives as inhibitors of matrix metalloproteinases
    17.
    发明授权
    Benzene butyric acids and their derivatives as inhibitors of matrix metalloproteinases 失效
    苯丁酸及其衍生物作为基质金属蛋白酶的抑制剂

    公开(公告)号:US06541521B1

    公开(公告)日:2003-04-01

    申请号:US09351549

    申请日:1999-07-12

    IPC分类号: A61K31195

    摘要: Benzene butyric acid compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurysm, heart failure, left ventricular dilation, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, osteoporosis, renal disease, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.

    摘要翻译: 苯丁酸化合物和衍生物以及其制备方法及其药物组合物的描述,其可用作基质金属蛋白酶抑制剂,特别是明胶酶A,胶原酶-3和溶基质溶解素-1以及用于治疗多发性硬化, 动脉粥样硬化斑块破裂,主动脉瘤,心力衰竭,左心室扩张,再狭窄,牙周病,角膜溃疡,烧伤治疗,褥疮溃疡,伤口愈合,癌症,炎症,疼痛,关节炎,骨质疏松症,肾脏疾病或其他自身免疫或炎症 依赖于白细胞或其他激活的迁移细胞的组织侵袭的疾病,急性和慢性神经变性疾病,包括中风,头部创伤,脊髓损伤,阿尔茨海默病,肌萎缩性侧索硬化,脑淀粉样血管病,艾滋病,帕金森病,亨廷顿病,朊病毒疾病, 重症肌无力和Duchenne肌营养不良症。

    Chemokine receptor antagonists
    19.
    发明授权
    Chemokine receptor antagonists 有权
    趋化因子受体拮抗剂

    公开(公告)号:US06316449B1

    公开(公告)日:2001-11-13

    申请号:US09558267

    申请日:2000-04-25

    IPC分类号: A61K31150

    CPC分类号: C07D471/14

    摘要: The instant invention is a series of compounds which are MCP-1 receptor antagonists of Formula I Also included in the invention are intermediates and processes for the preparation of the compounds as well as methods of using the compounds as agents for the treatment of atherosclerosis, chronic and acute inflammatory disease, chronic and acute immune disorders and transplant rejection as well as for preventing infection by HIV, treating infection by HIV, delaying the onset of AIDS, or treating AIDS.

    摘要翻译: 本发明是一系列化合物,其是本发明中包括的式IAl的MCP-1受体拮抗剂,其是中间体和化合物的制备方法,以及使用该化合物作为治疗动脉粥样硬化,慢性和 急性炎症性疾病,慢性和急性免疫疾病和移植排斥以及预防艾滋病毒感染,治疗艾滋病毒感染,延迟艾滋病发作或治疗艾滋病。