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公开(公告)号：US06562823B1
公开(公告)日：2003-05-13
申请号：US09719878
申请日：2001-06-28
申请人： Christopher J. Dinsmore , Jeffrey M. Bergman , Samuel L. Graham , Diem N. Nguyen , Gerald E. Stokker , Theresa M. Williams , C. Blair Zartman
发明人： Christopher J. Dinsmore , Jeffrey M. Bergman , Samuel L. Graham , Diem N. Nguyen , Gerald E. Stokker , Theresa M. Williams , C. Blair Zartman
IPC分类号： C07D26700
CPC分类号： C07D498/18
摘要： The present invention is directed to peptidomimetic piperazine-containing macrocyclic 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 - 蛋白质转移酶和致癌基因蛋白Ras的异戊烯基化的含模拟哌嗪的大环化合物。 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：US5661161A
公开(公告)日：1997-08-26
申请号：US527972
申请日：1995-09-14
申请人： Neville J. Anthony , Terrence M. Ciccarone , S. Jane deSolms , Samuel L. Graham , Gerald E. Stokker , Catherine M. Wiscount
发明人： Neville J. Anthony , Terrence M. Ciccarone , S. Jane deSolms , Samuel L. Graham , Gerald E. Stokker , Catherine M. Wiscount
IPC分类号： A61K31/40 , A61K31/4015 , A61K31/415 , A61K31/44 , A61K31/4427 , A61K38/00 , A61P9/00 , A61P9/10 , A61P31/00 , A61P43/00 , C07D207/28 , C07D401/06 , C07D403/06 , C07K5/02 , C07K5/06 , C07K5/08 , C07D207/16
CPC分类号： C07D401/06 , C07D207/28 , C07D403/06 , C07K5/0207 , 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 farnesyl-protein transferase. Furthermore, these CAAX analogues differ from those previously described as inhibitors of farnesyl-protein 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 antoxidation 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类似物抑制法呢基蛋白转移酶。 此外，这些CAAX类似物与先前描述为法呢基 - 蛋白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体内的药代动力学行为方面提供独特的优势，预防硫醇依赖的化学反应，如用内源性硫醇快速无毒化和二硫化物形成，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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公开(公告)号：US06284755B1
公开(公告)日：2001-09-04
申请号：US09456153
申请日：1999-12-07
申请人： S. Jane deSolms , Samuel L. Graham , Anthony W. Shaw , Terrence M. Ciccarone , Gerald E. Stokker
发明人： S. Jane deSolms , Samuel L. Graham , Anthony W. Shaw , Terrence M. Ciccarone , Gerald E. Stokker
IPC分类号： A01N4346
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D413/12 , C07D471/04
摘要： The present invention is directed to azepan-2-one compounds which inhibit prenyl-protein transferase, particularly farnesyl-protein transferase (Ftase), 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，特别是法呢基蛋白转移酶（Ftase）的酪蛋白-2-酮化合物和致癌基因蛋白Ras的异戊烯基化。 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：US5585359A
公开(公告)日：1996-12-17
申请号：US315171
申请日：1994-09-29
IPC分类号： A61K38/55 , A61K38/00 , A61P35/00 , A61P43/00 , C07C229/12 , C07C229/22 , C07C229/24 , C07C229/26 , C07C229/36 , C07C237/12 , C07C255/24 , C07C323/60 , C07K5/06 , C07K5/08 , C07K5/083 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： C07K5/06026 , C07K5/0808 , 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.
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公开(公告)号：US5576293A
公开(公告)日：1996-11-19
申请号：US314987
申请日：1994-09-29
申请人： S. Jane deSolms , Victor M. Garsky , Elizabeth A. Giuliani , Robert P. Gomez , Samuel L. Graham , Gerald E. Stokker , Catherine M. Wiscount
发明人： S. Jane deSolms , Victor M. Garsky , Elizabeth A. Giuliani , Robert P. Gomez , Samuel L. Graham , Gerald E. Stokker , Catherine M. Wiscount
IPC分类号： C07D233/64 , A61K31/35 , A61K31/351 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/425 , A61K31/426 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/47 , A61K38/00 , A61K38/55 , A61P35/00 , A61P43/00 , C07D207/28 , C07D209/18 , C07D211/76 , C07D213/82 , C07D233/54 , C07D233/90 , C07D277/20 , C07D277/56 , C07D309/30 , C07D405/12 , C07D409/12 , C07K5/02 , C07K5/097 , C07K5/117 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： C07D213/82 , C07D207/28 , C07D233/64 , C07D233/90 , C07K5/0207 , C07K5/0821 , C07K5/0825 , C07K5/1024 , 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.
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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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公开(公告)号：US5523456A
公开(公告)日：1996-06-04
申请号：US315046
申请日：1994-09-29
IPC分类号： C07D307/33 , A61K38/55 , A61P35/00 , A61P43/00 , C07C229/14 , C07C237/12 , C07C255/24 , C07C317/48 , C07C323/57 , C07D309/30 , C07D521/00 , C07K5/06 , C07K5/08 , C07C317/02 , C07C317/44
CPC分类号： C07K5/06026
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.
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8.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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