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1.发明申请2-AMINOIMIDAZOLE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 有权用于治疗阿尔茨海默病的2-氨基咪唑β-分泌酶抑制剂公开(公告)号：US20110034483A1
公开(公告)日：2011-02-10
申请号：US12919277
申请日：2009-02-18
申请人： Ivory D. Hills , Craig A. Coburn , Samuel L. Graham , Keith P. Moore , Philippe G. Nantermet , Hemaka A. Rajapakse , Shawn J. Stachel , Hong Zhu
发明人： Ivory D. Hills , Craig A. Coburn , Samuel L. Graham , Keith P. Moore , Philippe G. Nantermet , Hemaka A. Rajapakse , Shawn J. Stachel , Hong Zhu
IPC分类号： A61K31/506 , C07D233/88 , A61K31/4174 , C07D403/10 , A61K31/4178 , C07D403/06 , C07D413/10 , A61K31/42 , C07D401/10 , A61K31/4439 , A61K31/422 , A61P25/28
CPC分类号： C07D233/88 , C07D401/04 , C07D401/06 , C07D401/08 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D405/06 , C07D405/10 , C07D409/10 , C07D413/10
摘要： The present invention is directed to 2-aminoimidazole compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并可用于治疗其中涉及β-分泌酶的疾病如阿尔茨海默病的式（I）的2-氨基咪唑化合物。 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治疗涉及β-分泌酶的疾病中的用途。
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公开(公告)号：US07205293B2
公开(公告)日：2007-04-17
申请号：US10547228
申请日：2004-03-10
IPC分类号： C07D403/12 , A61K31/55 , A61P25/06
CPC分类号： C07D403/12 , C07D235/02
摘要： The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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 CGRP is involved.
摘要翻译： 本发明涉及作为CGRP受体的拮抗剂的化合物，其可用于治疗或预防涉及CGRP的疾病，例如头痛，偏头痛和丛集性头痛。 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CGRP的疾病中的用途。
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公开(公告)号：US5852010A
公开(公告)日：1998-12-22
申请号：US823920
申请日：1997-03-25
IPC分类号： C07D243/24 , C07D403/12 , A61K31/395
CPC分类号： C07D403/12 , C07D243/24
摘要： The present invention is directed to substituted benozdiazepine compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
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公开(公告)号：US5753650A
公开(公告)日：1998-05-19
申请号：US737191
申请日：1996-11-06
IPC分类号： C07D243/24 , A61K31/55 , A61K31/551 , A61K38/00 , A61P35/00 , A61P43/00 , C07K5/06 , C07D243/14
CPC分类号： C07K5/0606 , A61K38/00
摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer, which compound has the structure; ##STR1## or a pharmaceutically acceptable salt or disulfide thereof and wherein the variables are as defined in the specification.
摘要翻译： PCT No.PCT / US95 / 06286 Sec。 371日期：1996年11月6日 102（e）日期1996年11月6日PCT提交1995年5月16日PCT公布。 公开号WO95 / 32191 日期：1995年11月30日本发明涉及抑制法呢基蛋白转移酶（FTase）和癌基因蛋白Ras的法呢基化的化合物。 本发明还涉及含有本发明化合物的化学治疗组合物和抑制法呢基蛋白转移酶和治疗癌症的方法，该化合物具有结构; 或其药学上可接受的盐或二硫化物，其中变量如本说明书中所定义。
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公开(公告)号：US5652257A
公开(公告)日：1997-07-29
申请号：US526244
申请日：1995-09-21
申请人： Neville J. Anthony , S. Jane deSolms , Robert P. Gomez , Samuel L. Graham , John H. Hutchinson , Gerald E. Stokker
发明人： Neville J. Anthony , S. Jane deSolms , Robert P. Gomez , Samuel L. Graham , John H. Hutchinson , Gerald E. Stokker
IPC分类号： A61K38/00 , C07D233/54 , C07K5/02 , C07K5/06 , C07K5/062 , A61K31/415 , C07D233/02 , C07D233/04 , C07D233/30
CPC分类号： C07D233/64 , C07K5/0205 , C07K5/06026 , A61K38/00
摘要： The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit the farnesylation of Ras. Furthermore, these CAAX analogues differ from those previously described as inhibitors of Ras farnesyl transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.
摘要翻译： 本发明包括通过体内法尼基化修饰的蛋白Ras的CAAX基序的类似物。 这些CAAX类似物抑制Ras的法呢基化。 此外，这些CAAX类似物与先前描述为Ras法呢基转移酶抑制剂的不同之处在于它们不具有硫醇部分。 缺乏硫醇在改善动物药代动力学行为方面提供独特的优势，防止硫醇依赖的化学反应，如快速自身氧化和内源性硫醇形成二硫键，并减少全身毒性。 本发明还包含含有这些法呢基转移酶抑制剂的化疗组合物及其生产方法。
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6.发明授权2-Sulfamoyl-1H-indole derivatives for the treatment of elevated intraocular pressure 失效2-氨基磺酰基-1H-吲哚衍生物，用于治疗眼内压升高
公开(公告)号：US4840963A
公开(公告)日：1989-06-20
申请号：US679431
申请日：1984-12-07
IPC分类号： C07D209/08 , C07D209/30
CPC分类号： C07D209/08 , C07D209/30
摘要： Novel 2-sulfamoyl-1H-indoles and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in pharmaceutical compositions designed for systemic or topical ophthalmic administration.
摘要翻译： 显示出新的2-氨磺酰基-1H-吲哚及其衍生物可用于治疗设计用于全身或局部眼科给药的药物组合物中的眼内压升高。
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7.发明授权Elevated intraocular pressure lowering benzo-[b]-thiophene-2-sulfonamide derivatives, compositions, and method of use therefor 失效升高的眼压降低苯并[b] - 噻吩-2-磺酰胺衍生物，组合物及其使用方法
公开(公告)号：US4668697A
公开(公告)日：1987-05-26
申请号：US600695
申请日：1984-04-16
IPC分类号： C07D333/54 , C07D333/62 , C07D333/70 , C07D409/04 , C07D409/12 , C07F9/6553 , A61K31/38
CPC分类号： C07D333/54 , C07C309/00 , C07C323/00 , C07D333/62 , C07D333/70 , C07D409/04 , C07D409/12 , C07F9/655354
摘要： Novel 2-sulfamoylbenzo[b]thiophenes and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in compositions including ophthalmic drops and inserts.
摘要翻译： 显示新的2-氨磺酰基苯并[b]噻吩及其衍生物可用于治疗组合物中升高的眼内压，包括滴眼剂和插入物。
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8.发明授权2-Sulfamoylbenzo[b]furan derivatives for the treatment of elevated intraocular pressure 失效2-磺酰氨基苯并[b]呋喃衍生物，用于治疗眼内压升高
公开(公告)号：US4544667A
公开(公告)日：1985-10-01
申请号：US578463
申请日：1984-02-09
IPC分类号： A61K31/34 , A61K31/343 , A61K31/42 , A61K31/66 , A61K31/665 , A61P27/02 , C07D307/82 , C07D407/12 , C07D413/12 , C07F9/09 , C07F9/655
CPC分类号： C07D307/82 , C07F9/65517
摘要： Novel 2-sulfamoylbenzo[b]furans and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in compositions including opthalmic drops and inserts.
摘要翻译： 显示新的2-氨磺酰苯并[b]呋喃及其衍生物可用于治疗组合物中升高的眼内压，包括眼药水和插入物。
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公开(公告)号：US06333335B1
公开(公告)日：2001-12-25
申请号：US09609205
申请日：2000-06-30
IPC分类号： A61K31437
CPC分类号： C07D471/04
摘要： The present invention is directed to tetrahydro-imidazopyridinyl compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
摘要翻译： 本发明涉及抑制异戊烯基 - 蛋白质转移酶和癌基因蛋白Ras的异戊烯化的四氢 - 咪唑并吡啶基化合物。 本发明还涉及含有本发明化合物的化疗组合物和抑制异戊烯基 - 蛋白质转移酶和癌基因蛋白Ras的异戊烯化的方法。
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公开(公告)号：US5817678A
公开(公告)日：1998-10-06
申请号：US749254
申请日：1996-11-15
IPC分类号： C07D233/24 , C07D401/12 , A61K31/445
CPC分类号： C07D233/24 , C07D401/12
摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
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