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1. 发明授权

US6114572A Substituted phenols and thiophenols useful as antioxidant agents 失效
标题翻译：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。

2. 发明授权

US6121463A Alkyl-4-silylheterocyclic phenols and thiophenols useful as antioxidant agents 失效
标题翻译：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。

3. 发明授权

US6133467A 2,6-di-t-butyl-4-[(dimethyl-4-methoxyphenylsilyl)-methyl-oxy]phenol and 2,6-di-t-butyl-4-[(dimethyl-2-methoxy-phenylsilyl)methyloxy]phenol 失效
标题翻译： 2,6-二叔丁基-4 - [（二甲基-4-甲氧基苯基甲硅烷基） - 甲氧基]苯酚和2,6-二叔丁基-4 - [（二甲基-2-甲氧基 - 苯基甲硅烷基）甲氧基 ]苯酚
公开(公告)号：US6133467A
公开(公告)日：2000-10-17
申请号：US103215
申请日：1998-06-23
申请人： Michael L. Edwards , Mark J. Vaal , Roger A. Parker , James E. Matt , Kim S. Chen , Mark T. Yates
发明人： Michael L. Edwards , Mark J. Vaal , Roger A. Parker , James E. Matt , Kim S. Chen , Mark T. Yates
IPC分类号： C07F7/08 , C07F7/04
CPC分类号： C07F7/0818
摘要： This invention relates to the compounds of 2,6-di-t-butyl-4-[(dimethyl-4-methoxyphenylsilyl)methyloxy]phenol and 2,6-di-t-butyl-4-[(dimethyl-2-methoxyphenylsilyl)methyloxy]phenol, polymorphs thereof and their pharmaceutically acceptable salts, useful as antiatherosclerotic agents.
摘要翻译：本发明涉及2,6-二叔丁基-4 - [（二甲基-4-甲氧基苯基甲硅烷基）甲氧基]苯酚和2,6-二叔丁基-4 - [（二甲基-2-甲氧基苯基甲硅烷基）甲氧基]苯酚，其多晶型物及其药学上可接受的盐，可用作抗动脉粥样硬化剂。

4. 发明授权

US5608095A Alkyl-4-silyl-phenols and esters thereof as antiatherosclerotic agents 失效
标题翻译：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。

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