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    Alkyl-4-silylheterocyclic phenols and thiophenols useful as antioxidant agents
    2.
    发明授权
    Alkyl-4-silylheterocyclic phenols and thiophenols useful as antioxidant agents 失效
    烷基-4-甲硅烷基杂环苯酚和可用作抗氧化剂的苯硫酚

    公开(公告)号：US6121463A

    公开(公告)日：2000-09-19

    申请号：US102869

    申请日：1998-06-23

    申请人： Roger A. Parker ,  Michael L. Edwards ,  Mark J. Vaal ,  James E. Matt ,  Kim S. Chen ,  Mark T. Yates ,  Paul S. Wright ,  Steven J. Busch

    发明人： Roger A. Parker ,  Michael L. Edwards ,  Mark J. Vaal ,  James E. Matt ,  Kim S. Chen ,  Mark T. Yates ,  Paul S. Wright ,  Steven J. Busch

    IPC分类号： C07F7/08 ,  C07D327/00 ,  C07D305/00 ,  C07D307/02 ,  C07D333/22

    CPC分类号： C07F7/0814

    摘要： The present invention provides compounds of the formula ##STR1## wherein R is hydrogen or --C(O)--(CH.sub.2).sub.m --Q wherein Q is hydrogen or --COOH and m is an integer 1, 2, 3 or 4;R.sub.1, R.sub.5 and R.sub.6 are independently a C.sub.1 -C.sub.6 alkyl group;R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen or a C.sub.1 -C.sub.6 alkyl group;Z is thio, oxy or a methylene group;A is a C.sub.1 -C.sub.4 alkylene group;X is thio or oxy; andG.sub.1 and G.sub.2 are independently hydrogen, C.sub.1 -C.sub.6 alkyl or --C(O)--(CH.sub.2).sub.n --CH.sub.3 and n is an integer 0, 1, 2 or 3;or a pharmaceutically acceptable salt thereof; useful for the treatment of atherosclerosis and chronic inflammatory disorders; for inhibiting cytokine-induced expression of VCAM-1 and/or ICAM-1; for inhibiting the peroxidation of LDL lipid; for lowering plasma cholesterol; and as anti-oxidant chemical additives useful for preventing oxidative deterioration in organic materials.

    摘要翻译： 本发明提供下式的化合物其中R是氢或-C（O） - （CH 2）m-Q，其中Q是氢或-COOH，m是整数1,2,3或4; R1，R5和R6独立地为C1-C6烷基; R2，R3和R4独立地是氢或C1-C6烷基; Z是硫代，氧基或亚甲基; A是C1-C4亚烷基; X是硫或氧; 且G 1和G 2独立地为氢，C 1 -C 6烷基或-C（O） - （CH 2）n -CH 3，n为整数0,1,2或3; 或其药学上可接受的盐; 可用于治疗动脉粥样硬化和慢性炎症性疾病; 用于抑制VCAM-1和/或ICAM-1的细胞因子诱导的表达; 用于抑制LDL脂质的过氧化; 用于降低血浆胆固醇; 以及用作防止有机材料氧化变质的抗氧化剂。

    Substituted phenols and thiophenols useful as antioxidant agents
    3.
    发明授权
    Substituted phenols and thiophenols useful as antioxidant agents 失效
    用作抗氧化剂的取代的酚和苯酚

    公开(公告)号：US6114572A

    公开(公告)日：2000-09-05

    申请号：US974112

    申请日：1997-11-19

    申请人： Roger A. Parker ,  Paul S. Wright ,  Steven J. Busch ,  Kim S. Chen ,  Mark T. Yates

    发明人： Roger A. Parker ,  Paul S. Wright ,  Steven J. Busch ,  Kim S. Chen ,  Mark T. Yates

    IPC分类号： C07C43/23 ,  C07C69/017 ,  C07C323/20 ,  C07C67/02 ,  A01N31/00 ,  C07C41/00 ,  C07C59/00

    CPC分类号： C07C43/23 ,  C07C323/20 ,  C07C69/017

    摘要： The present invention provides compounds of the formula ##STR1## wherein X is selected from the group consisting of ##STR2## Y is thio, oxy or a methylene group; Z is hydrogen or --C(O)--(CH.sub.2).sub.m --Q wherein Q is hydrogen or --COOH and m is an integer 1, 2, 3 or 4;R.sub.1 is C.sub.1 -C.sub.6 alkyl; andR.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl;or a stereoisomer thereof; useful for the treatment of atherosclerosis and chronic inflammatory disorders; for inhibiting cytokine-induced expression of VCAM-1 and/or ICAM-1; for inhibiting the peroxidation of LDL lipid; for lowering plasma cholesterol; and as anti-oxidant chemical additives useful for preventing oxidative deterioration in organic materials.

    摘要翻译： 本发明提供下式的化合物其中X选自Y是硫代，氧基或亚甲基; Z是氢或-C（O） - （CH 2）m-Q其中Q是氢或-COOH，m是整数1,2,3或4; R1是C1-C6烷基; 并且R 2，R 3和R 4各自独立地为氢或C 1 -C 6烷基; 或其立体异构体; 可用于治疗动脉粥样硬化和慢性炎症性疾病; 用于抑制VCAM-1和/或ICAM-1的细胞因子诱导的表达; 用于抑制LDL脂质的过氧化; 用于降低血浆胆固醇; 以及用作防止有机材料氧化变质的抗氧化剂。

    Method of inhibiting vascular cell adhesion molecule-1 and treating chronic inflammatory diseases with 2, 6-di-alkyl-4-silyl-phenols
    6.
    发明授权
    Method of inhibiting vascular cell adhesion molecule-1 and treating chronic inflammatory diseases with 2, 6-di-alkyl-4-silyl-phenols 失效
    抑制血管细胞粘附分子-1并用2,6-二烷基-4-甲硅烷基苯酚治疗慢性炎性疾病的方法

    公开(公告)号：US5795876A

    公开(公告)日：1998-08-18

    申请号：US824221

    申请日：1997-03-25

    申请人： Paul S. Wright ,  Steven J. Busch

    发明人： Paul S. Wright ,  Steven J. Busch

    IPC分类号： A61K31/695

    CPC分类号： A61K31/695

    摘要： Methods useful for inhibiting VCAM-1 and for treating chronic inflammatory conditions in a patient in need thereof are disclosed comprising administering to the patient effective amounts of a compound of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently a C.sub.1 -C.sub.6 alkyl group; Z is a thio, oxy or methylene group; A is a C.sub.1 -C.sub.4 alkylene group; R.sub.5 is a C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.n --(Ar) wherein n is an integer 0, 1, 2 or 3; and Ar is phenyl or naphthyl unsubstituted or substituted with one to three substituents selected from the group consisting of hydroxy, methoxy, ethoxy, chloro, fluoro or C.sub.1 -C.sub.6 alkyl; are disclosed.

    摘要翻译： 公开了可用于抑制VCAM-1和用于治疗有需要的患者的慢性炎性病症的方法，包括向患者施用有效量的下式化合物（1），其中R1，R2，R3和R4各自为 独立地为C1-C6烷基; Z是硫基，氧基或亚甲基; A是C1-C4亚烷基; R5是C1-C6烷基或 - （CH2）n-（Ar），其中n是整数0,1,2或3; 并且Ar是未取代的或被一至三个选自羟基，甲氧基，乙氧基，氯，氟或C 1 -C 6烷基的取代基取代的苯基或萘基; 被披露。

    Alkyl-4-silyl-phenols and esters thereof as antiatherosclerotic agents
    7.
    发明授权
    Alkyl-4-silyl-phenols and esters thereof as antiatherosclerotic agents 失效
    烷基-4-甲硅烷基 - 苯酚及其酯作为抗动脉粥样硬化剂

    公开(公告)号：US5608095A

    公开(公告)日：1997-03-04

    申请号：US637968

    申请日：1996-04-30

    申请人： Roger A. Parker ,  Michael L. Edwards ,  Mark J. Vaal ,  James E. Matt, Jr. ,  Kim S. Chen ,  Mark T. Yates ,  Paul S. Wright ,  Steven J. Busch

    发明人： Roger A. Parker ,  Michael L. Edwards ,  Mark J. Vaal ,  James E. Matt, Jr. ,  Kim S. Chen ,  Mark T. Yates ,  Paul S. Wright ,  Steven J. Busch

    IPC分类号： A61K31/695 ,  A61P3/06 ,  A61P11/06 ,  A61P19/02 ,  A61P29/00 ,  A61P37/00 ,  A61P43/00 ,  C07F7/08 ,  C07F7/10 ,  C07F7/12 ,  C07F7/18

    CPC分类号： C07F7/0818

    摘要： This invention relates to compounds of the formula ##STR1## wherein R.sub.1 and R.sub.6 are each independently C.sub.1 -C.sub.6 alkyl;R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl;R is hydrogen or --C(O)--(CH.sub.2).sub.m --Q wherein Q is hydrogen or --COOH and m is an integer 1, 2, 3 or 4;Z is a thio, oxy or methylene group;A is a C.sub.1 -C.sub.4 alkylene group;R.sub.5 and R.sub.7 are each independently a C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.n --(Ar) wherein n is an integer 0, 1, 2 or 3; and Ar is phenyl or naphthyl unsubstituted or substituted with one to three substituents selected from the group consisting of hydroxy, methoxy, ethoxy, halogen, trifluoromethyl, C.sub.1 -C.sub.6 alkyl, or --NR.sub.8 R.sub.9, wherein R.sub.8 and R.sub.9 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl; with the proviso that when R.sub.2 and at least one of R.sub.5 or R.sub.7 is C.sub.1 -C.sub.6 alkyl, and Ar is not substituted with trifluoromethyl or --NR.sub.8 R.sub.9, then R is --C(O)--(CH.sub.2).sub.m --Q; or a pharmaceutically acceptable salt thereof; useful for the treatment of atherosclerosis and chronic inflammatory disorders; for inhibiting cytokine-induced expression of VCAM-1 and/or ICAM-1; for inhibiting the peroxidation of LDL lipid; for lowering plasma cholesterol; and as antioxidant chemical additives useful for preventing oxidative deterioration in organic materials.

    摘要翻译： 本发明涉及式（1）的化合物，其中R 1和R 6各自独立地为C 1 -C 6烷基; R2，R3和R4各自独立地为氢或C1-C6烷基; R是氢或-C（O） - （CH 2）m-Q其中Q是氢或-COOH，m是整数1,2,3或4; Z是硫基，氧基或亚甲基; A是C1-C4亚烷基; R 5和R 7各自独立地为C 1 -C 6烷基或 - （CH 2）n - （Ar），其中n为整数0,1,2或3; 并且Ar是未取代的或被一至三个选自羟基，甲氧基，乙氧基，卤素，三氟甲基，C 1 -C 6烷基或-NR 8 R 9的取代基取代的苯基或萘基，其中R 8和R 9各自独立地为氢或C1- C6烷基; 条件是当R 2和R 5或R 7中的至少一个是C 1 -C 6烷基，并且Ar不被三氟甲基或-NR 8 R 9取代时，则R是-C（O） - （CH 2）m -Q; 或其药学上可接受的盐; 可用于治疗动脉粥样硬化和慢性炎症性疾病; 用于抑制VCAM-1和/或ICAM-1的细胞因子诱导的表达; 用于抑制LDL脂质的过氧化; 用于降低血浆胆固醇; 以及用作防止有机材料氧化变质的抗氧化剂添加剂。

    Antiangiogenic oligomers
    8.
    发明授权
    Antiangiogenic oligomers 失效
    抗血管生成寡聚体

    公开(公告)号：US5593664A

    公开(公告)日：1997-01-14

    申请号：US379466

    申请日：1995-04-05

    申请人： Paul S. Wright ,  Alan J. Bitonti

    发明人： Paul S. Wright ,  Alan J. Bitonti

    IPC分类号： A61K31/66 ,  A61K31/165 ,  A61K31/17 ,  A61K31/185 ,  A61K31/195 ,  A61K31/74 ,  A61K31/785 ,  A61K31/795 ,  A61K31/80 ,  A61P9/00 ,  A61P35/00 ,  A61P43/00 ,  C07C235/84 ,  C07C275/40 ,  C07F9/38 ,  C08G18/32 ,  C08G18/76 ,  C08G18/77 ,  C08G69/32 ,  C08G73/00

    CPC分类号： A61K31/185 ,  A61K31/785 ,  A61K31/795 ,  A61K31/80 ,  Y10S514/93

    摘要： The present invention relates to the use of certain anionic polyamide and polyurea oligomers for inhibiting angiogenesis, and for their use in treating diseases associated with angiogenesis. These oligomers have a number average molecular weight (M.sub.n) less than 10,000, comprise recurring units coupled by carbonyl linking moieties and have predominantly linear geometry such that regular spacing between anionic groups exists in an aqueous medium. The oligomers also have a preferably linear backbone and be be in their salt form, preferably wherein the salt is pharmaceutically acceptable.

    摘要翻译： PCT No.PCT / US93 / 06792 Sec。 371日期1995年04月5日 102（e）日期1995年4月5日PCT提交1993年7月20日PCT公布。 出版物WO94 / 04165 日期：1994年3月3日本发明涉及某些阴离子聚酰胺和聚脲低聚物用于抑制血管发生的用途，并且用于治疗与血管发生相关的疾病。 这些低聚物的数均分子量（Mn）小于10,000，包括通过羰基连接部分偶联的重复单元，并且主要具有线性几何形状，使得阴离子基团之间的规则间距存在于水性介质中。 低聚物还具有优选的线性主链并且为其盐形式，优选其中该盐是药学上可接受的。