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公开(公告)号:US06358956B1
公开(公告)日:2002-03-19
申请号:US09516750
申请日:2000-03-01
申请人: George D. Hartman , William C. Lumma, Jr. , John T. Sisko , Anthony M. Smith , Thomas J. Tucker , Gerald E. Stokker
发明人: George D. Hartman , William C. Lumma, Jr. , John T. Sisko , Anthony M. Smith , Thomas J. Tucker , Gerald E. Stokker
IPC分类号: A06L31295
CPC分类号: C07D233/64 , C07D401/12 , C07D405/12
摘要: The present invention comprises piperazine-containing compounds which inhibit prenyl-protein transferases, including-farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer.
摘要翻译: 本发明包括抑制异戊烯基 - 蛋白质转移酶的含哌嗪化合物,包括法呢基蛋白转移酶和er牛鞭毛蛋白转移酶I型。这种治疗化合物可用于治疗癌症。
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公开(公告)号:US07115597B2
公开(公告)日:2006-10-03
申请号:US10677687
申请日:2003-10-02
申请人: Mark T. Bilodeau , George D. Hartman , Jacob M. Hoffman, Jr. , John T. Sisko , Peter J. Manley , Anthony M. Smith , Thomas J. Tucker , William C. Lumma, Jr. , Leonard Rodman
发明人: Mark T. Bilodeau , George D. Hartman , Jacob M. Hoffman, Jr. , John T. Sisko , Peter J. Manley , Anthony M. Smith , Thomas J. Tucker , William C. Lumma, Jr. , Leonard Rodman
IPC分类号: C07D417/12 , A61K31/427 , C07D241/04
CPC分类号: C07D403/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D487/04 , C07D487/08 , C07D491/08
摘要: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
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公开(公告)号:US06376496B1
公开(公告)日:2002-04-23
申请号:US09516756
申请日:2000-03-01
申请人: George D. Hartman , William C. Lumma, Jr. , John T. Sisko , Anthony M. Smith , Thomas J. Tucker , Jeffrey M. Bergman
发明人: George D. Hartman , William C. Lumma, Jr. , John T. Sisko , Anthony M. Smith , Thomas J. Tucker , Jeffrey M. Bergman
IPC分类号: C07D40304
CPC分类号: C07D233/64
摘要: The present invention comprises piperazine-containing compounds which inhibit prenyl-protein transferases, including farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer.
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公开(公告)号:US07265134B2
公开(公告)日:2007-09-04
申请号:US10486574
申请日:2002-08-13
申请人: George D. Hartman , Thomas J. Tucker , John T. Sisko , Anthony M. Smith , William C. Lumma, Jr.
发明人: George D. Hartman , Thomas J. Tucker , John T. Sisko , Anthony M. Smith , William C. Lumma, Jr.
IPC分类号: A61K31/426 , A61K31/4535 , C07D417/12 , C07D401/12 , C07D277/38
CPC分类号: C07D417/12 , A61K31/427 , A61K31/4439 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D277/48 , C07D417/14 , A61K2300/00
摘要: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
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公开(公告)号:US06335343B1
公开(公告)日:2002-01-01
申请号:US09516945
申请日:2000-03-01
IPC分类号: A61K31496
CPC分类号: C07D233/64 , C07D403/06
摘要: The present invention comprises piperazine/piperazinone-containing compounds having multicyclic ring system substituents on one of the piperazine/piperazinone nitrogens, which inhibit prenyl-protein transferases, including farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer.
摘要翻译: 本发明包括在哌嗪/哌嗪酮氮之一上具有多环系统取代基的哌嗪/哌嗪酮化合物,其抑制异戊烯基 - 蛋白转移酶,包括法尼基蛋白转移酶和er牛儿基ger牛儿基因型I型转运酶。这种治疗化合物可用于 治疗癌症。
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公开(公告)号:US06355643B1
公开(公告)日:2002-03-12
申请号:US09516757
申请日:2000-03-01
申请人: William C. Lumma , John T. Sisko , Anthony M. Smith , Thomas J. Tucker , Christopher J. Dinsmore , Jeffrey M. Bergman
发明人: William C. Lumma , John T. Sisko , Anthony M. Smith , Thomas J. Tucker , Christopher J. Dinsmore , Jeffrey M. Bergman
IPC分类号: A61K31496
CPC分类号: C07D233/64 , A61K31/496
摘要: The present invention comprises unsubstituted and substituted piperazine-containing compounds having alkanoyl, alkylsulfonyl, alkylamido or alkoxycarbonyl substituents, and having the formula A, which inhibit prenyl-protein transferases. In particular, the invention relates to prenyl-protein transferase inhibitors which are efficacious in vivo as inhibitors of geranylgeranyl-protein transferase type I (GGTase-I) and that inhibit the cellular processing of both the H-Ras protein and the K4B-Ras protein. Such therapeutic compounds are useful in the treatment of cancer.
摘要翻译: 本发明包括具有烷酰基,烷基磺酰基,烷基酰氨基或烷氧基羰基取代基的未取代和取代的含哌嗪化合物,并且具有抑制异戊烯基 - 蛋白质转移酶的式A。 特别地,本发明涉及在体内作为er牛儿基ger牛蛋白转移酶I型(GGTase-I)抑制剂有效的异戊烯基 - 蛋白转移酶抑制剂,并且抑制H-Ras蛋白和K4B-Ras蛋白两者的细胞加工 。 这些治疗化合物可用于治疗癌症。
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公开(公告)号:US20090124603A1
公开(公告)日:2009-05-14
申请号:US12225506
申请日:2007-03-27
IPC分类号: A61K31/5513 , C07D243/08
CPC分类号: C07D417/04 , C07D401/04 , C07D403/04 , C07D413/04 , C07D413/14
摘要: The present invention is directed to diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
摘要翻译: 本发明涉及作为食欲肽受体的拮抗剂的二氮杂环庚烷化合物,其可用于治疗或预防涉及食欲肽受体的神经和精神病症和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及食欲肽受体的疾病中的用途。
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公开(公告)号:US20090030043A1
公开(公告)日:2009-01-29
申请号:US12223356
申请日:2007-01-29
IPC分类号: A61K31/444 , C07D401/14
CPC分类号: C07D213/74
摘要: The present invention relates to tetraaryl methyl amine compounds and derivatives thereof having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
摘要翻译: 本发明涉及具有用作治疗心律失常的钾通道抑制剂的结构(I)的四芳基甲胺化合物及其衍生物等。
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公开(公告)号:US4947424A
公开(公告)日:1990-08-07
申请号:US424032
申请日:1989-10-19
IPC分类号: H04M1/2745
CPC分类号: H04M1/2745
摘要: A shutter mechanism for a telephone directory that stores telephone numbers to be dialed. The directory has physical spaces for the entry of descriptive labels (e.g. names). The shutter mechanism has a first planar surface for providing these physical spaces. It has a second planar surface overlying the first surface. The second surface is divided into alternating opaque and transparent sections such that the surface having the names can be moved underneath the second surface such that the names can be hidden by the opaque sections or revealed by the transparent sections.
摘要翻译: 一种用于存储要拨打的电话号码的电话簿的快门机构。 该目录具有用于描述性标签(例如名称)的输入的物理空间。 快门机构具有用于提供这些物理空间的第一平面。 它具有覆盖第一表面的第二平面。 第二表面被分成交替的不透明部分和透明部分,使得具有名称的表面可以在第二表面下方移动,使得名称可以被不透明部分隐藏或被透明部分透露。
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公开(公告)号:US5691323A
公开(公告)日:1997-11-25
申请号:US440153
申请日:1995-05-12
申请人: Wayne J. Thompson , Michael F. Sugrue , Richard W. Ransom , Pierre J. Mallorga , Ian M. Bell , Anthony M. Smith
发明人: Wayne J. Thompson , Michael F. Sugrue , Richard W. Ransom , Pierre J. Mallorga , Ian M. Bell , Anthony M. Smith
IPC分类号: C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , A61K31/38 , A61K31/34 , C07D403/14
CPC分类号: C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12
摘要: Compounds, 1,3-dihydro-1-{1-�piperidin-4-yl!piperidin-4-yl}-2H-benzimidazol-2-ones and 1,3-dihydro-1-{4-amino-1-cyclohexyl}-2H-benzimidazol-2-ones and derivatives thereof, their preparation, method of use and pharmaceutical compositions are described. These compounds are endowed with antimuscarinic activity and are useful in the treatment and/or prevention of myopia (commonly known as nearsightedness).
摘要翻译: 化合物,1,3-二氢-1- {1- [哌啶-4-基]哌啶-4-基} -2H-苯并咪唑-2-酮和1,3-二氢-1- {4-氨基-1- 环己基} -2H-苯并咪唑-2-酮及其衍生物,其制备方法,使用方法和药物组合物。 这些化合物具有抗毒蕈碱活性,可用于治疗和/或预防近视(俗称近视)。
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