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1. 发明授权

US06677376B1 Non-peptidic cyclophilin binding compounds and their use 失效
标题翻译：非肽亲环蛋白结合化合物及其用途
公开(公告)号：US06677376B1
公开(公告)日：2004-01-13
申请号：US09656898
申请日：2000-09-07
申请人： Gregory S. Hamilton , Joseph P. Steiner , Mark J. Vaal , Chi Choi , Ling Wei
发明人： Gregory S. Hamilton , Joseph P. Steiner , Mark J. Vaal , Chi Choi , Ling Wei
IPC分类号： A61K3118
CPC分类号： C07C275/28 , A61K31/17 , C07C275/30 , C07C275/40 , C07C275/42 , C07C311/21 , C07C323/62 , C07C2601/14
摘要： The invention relates to non-peptidic compounds that possess bioactive properties, such as the ability to protect neuronal cells from otherwise lethal treatments or the ability to promote the growth or regeneration of neuronal cells. In part, the invention provides compounds that interact with or bind to a cyclophilin and compounds that have activity towards neuronal cells. Methods for using the compounds, such as administering them to cells or animals or using them to treat neurodegenerative conditions, are specifically included.
摘要翻译：本发明涉及具有生物活性的非肽类化合物，例如保护神经细胞免受其他致死性治疗或促进神经元细胞生长或再生的能力。部分地，本发明提供了与亲环蛋白相互作用或结合的化合物和对神经元细胞具有活性的化合物。具体包括使用化合物的方法，例如将其施用于细胞或动物或用于治疗神经变性病症。

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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