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35 条记录 (耗时 0.053 秒)

    Sulfonyl urea and carbamate ACAT inhibitors
    22.
    发明授权
    Sulfonyl urea and carbamate ACAT inhibitors 失效
    磺酰脲和氨基甲酸酯ACAT抑制剂

    公开(公告)号：US5981595A

    公开(公告)日：1999-11-09

    申请号：US85657

    申请日：1993-07-01

    申请人： Joseph Armand Picard ,  William Howard Roark ,  Bruce David Roth

    发明人： Joseph Armand Picard ,  William Howard Roark ,  Bruce David Roth

    IPC分类号： C07C311/53 ,  C07C311/55 ,  A61K31/175

    CPC分类号： C07C311/53 ,  C07C311/55

    摘要： A pharmaceutically useful compound which lowers blood cholesterol levels having the formula ##STR1## wherein X is oxygen or --NH--; Ar is phenyl, substituted phenyl, naphthyl or substituted naphthyl; R.sub.1 is hydrogen, lower alkyl or benzyl; and R.sub.2 is a straight or branched alkyl group having from 5 to 17 carbon atoms which may be substituted on the 1-carbon position with methyl, ethyl, phenyl, or substituted phenyl, or a cycloalkyl group having from 3 to 8 carbon atoms.

    摘要翻译： 一种降低具有下式的血液胆固醇水平的药学上有用的化合物，其中X是氧或-NH-; Ar是苯基，取代的苯基，萘基或取代的萘基; R1是氢，低级烷基或苄基; 并且R 2是具有5至17个碳原子的直链或支链烷基，其可以在1-碳位上被甲基，乙基，苯基或取代的苯基或具有3至8个碳原子的环烷基取代。

    Fluorine-substituted biphenyl butyric acids and their derivatives as inhibitors of matrix metalloproteinases
    25.
    发明授权
    Fluorine-substituted biphenyl butyric acids and their derivatives as inhibitors of matrix metalloproteinases 失效
    氟取代的联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：US06169103A

    公开(公告)日：2001-01-02

    申请号：US09256714

    申请日：1999-02-24

    申请人： Claude Forsey Purchase, Jr. ,  Bruce David Roth ,  Gerald Paul Schielke ,  Lary Craswell Walker ,  Andrew David White

    发明人： Claude Forsey Purchase, Jr. ,  Bruce David Roth ,  Gerald Paul Schielke ,  Lary Craswell Walker ,  Andrew David White

    IPC分类号： A61K3140

    CPC分类号： C07C327/58 ,  A61K31/275 ,  A61K31/40 ,  C07C251/48 ,  C07C255/64

    摘要： Fluorine-substituted biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, stromelysin-1, and collagenase-3, and for the treatment of atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, osteoporosis, multiple sclerosis, renal disease, and 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： 描述了氟取代的联苯基丁酸化合物和衍生物以及用于制备的酸法和其药物组合物，其可用作基质金属蛋白酶抑制剂，特别是明胶酶A，溶基质溶质素-1和胶原酶-3，并且对于 治疗动脉粥样硬化斑块破裂，主动脉瘤，心力衰竭，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，多发性硬化，肾脏疾病和其他自身免疫或 依赖于白细胞或其他活化的迁移细胞的组织侵袭的炎性病症，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的肌营养不良症。

    Pyrazolone derivatives as MCP-1 antagonists
    26.
    发明授权
    Pyrazolone derivatives as MCP-1 antagonists 失效
    吡唑酮衍生物作为MCP-1拮抗剂

    公开(公告)号：US06011052A

    公开(公告)日：2000-01-04

    申请号：US845729

    申请日：1997-04-25

    申请人： Janak Khimchand Padia ,  Bruce David Roth ,  John Edward Strode ,  Bharat Kalidas Trivedi

    发明人： Janak Khimchand Padia ,  Bruce David Roth ,  John Edward Strode ,  Bharat Kalidas Trivedi

    IPC分类号： C07D231/46 ,  C07D231/50 ,  C07D471/04 ,  A61K31/415 ,  C07D231/06 ,  C07D231/14 ,  C07D231/16

    CPC分类号： C07D471/04 ,  C07D231/46 ,  C07D231/50

    摘要： Pyrazolone derivatives of Formula I or a pharmaceutically acceptable salt thereof are MCP-1 antagonists and are thus useful in the treatment of inflammatory diseases or conditions, atherosclerosis, restenosis, and immune disorders such as arthritis and transplant rejection ##STR1## where: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 can be independently H,C.sub.1-20 alkyl,C.sub.5-7 cycloalkyl,--(CH.sub.2).sub.n NR.sub.6 R.sub.7--(CH.sub.2).sub.0-6 CONR.sub.6 R.sub.7,--(CH.sub.2).sub.n OH or--(CH.sub.2).sub.0-6 CO.sub.2 R.sub.11,biphenyl,aryl of from 6 to 10 carbon atoms, oraryl of from 6 to 10 carbon atoms substituted up to 3 times by halogen, --CN, lower alkyl of from 1-4 carbon atoms, --OH, nitro, --SO.sub.2 H, SO.sub.2 lower alkyl,--SO.sub.2 NR.sub.6 R.sub.7 lower alkoxy--C0.sub.2 R.sub.11,--CONR.sub.6 R.sub.7,--NR.sub.6 R.sub.7 or CH.sub.2 OH.

    摘要翻译： 式I的吡唑酮衍生物或其药学上可接受的盐是MCP-1拮抗剂，因此可用于治疗炎性疾病或病症，动脉粥样硬化，再狭窄和免疫疾病如关节炎和移植排斥反应，其中：R1，R2，R3， R4，R5可以独立地是H，C1-20烷基，C5-7环烷​​基， - （CH2）nNR6R7 - （CH2）0-6CONR6R7， - （CH2）nOH或 - （CH2）0-6CO2R11， 6至10个碳原子，或6至10个碳原子的芳基被卤素取代3次，-CN，1-4个碳原子的低级烷基，-OH，硝基，-SO 2 H，SO 2低级烷基，-SO 2 NR 6 R 7 低级烷氧基-C02R11，-CONR6R7，-NR6R7或CH2OH。

    Phosphonamide ACAT inhibitors
    29.
    发明授权
    Phosphonamide ACAT inhibitors 失效
    磷酰胺ACAT抑制剂

    公开(公告)号：US5807846A

    公开(公告)日：1998-09-15

    申请号：US881483

    申请日：1997-06-24

    申请人： William Howard Roark ,  Bruce David Roth

    发明人： William Howard Roark ,  Bruce David Roth

    IPC分类号： C07F9/24 ,  C07F9/44 ,  A61K31/66

    CPC分类号： A61K31/664 ,  C07F9/2487 ,  C07F9/4492 ,  Y10S514/824

    摘要： The present invention is directed to compounds useful for the regulation of cholesterol of Formula I, methods for using them and pharmaceutical compositions thereof, ##STR1## wherein Ar and Ar.sup.1 are each independently selected from unsubstituted or substituted phenyl which substituents are from 1-5 in number and are each independently selected from alkyl, alkoxy, hydroxy, halogen, nitro, trifluoromethyl, COOH, and COOalkyl; X is --NH--, --O--, --S--, or --(CH.sub.2).sub.0-4 --, and R is hydrogen, alkyl, or phenyl.

    摘要翻译： 本发明涉及可用于调节式I的胆固醇的化合物，其使用方法及其药物组合物，其中Ar和Ar1各自独立地选自未取代或取代的苯基，该取代基为1-5 各自独立地选自烷基，烷氧基，羟基，卤素，硝基，三氟甲基，COOH和COO烷基; X是-NH-，-O - ， - S-或 - （CH 2）0-4-，R是氢，烷基或苯基。