公开(公告)号：US20080188485A1

公开(公告)日：2008-08-07

申请号：US12055900

申请日：2008-03-26

申请人： Bahige M. Baroudy ,  John W. Clader ,  Hubert B. Josien ,  Stuart W. McCombie ,  Brian A. McKittrick ,  Michael W. Miller ,  Bernard R. Neustadt ,  Anandan Palani ,  Elizabeth M. Smith ,  Ruo Steensma ,  Jayaram R. Tagat ,  Susan F. Vice ,  Mark A. Laughlin ,  Eric Gilbert ,  Marc A. Labroli

发明人： Bahige M. Baroudy ,  John W. Clader ,  Hubert B. Josien ,  Stuart W. McCombie ,  Brian A. McKittrick ,  Michael W. Miller ,  Bernard R. Neustadt ,  Anandan Palani ,  Elizabeth M. Smith ,  Ruo Steensma ,  Jayaram R. Tagat ,  Susan F. Vice ,  Mark A. Laughlin ,  Eric Gilbert ,  Marc A. Labroli

IPC分类号： A61K31/496 ,  A61P1/00 ,  A61P19/02

CPC分类号： C07D401/06 ,  A61K31/496 ,  A61K45/06 ,  C07D211/58 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D409/06 ,  C07D413/06 ,  A61K2300/00

摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroarylalkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.

摘要翻译： 使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R 1是氢或烷基; R 2是取代的苯基，取代的杂芳基，芴基，二苯甲基或任选取代的苯基或杂芳基烷基; R 3是氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基，苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R 4，R 5和R 7是氢或烷基; R 6是氢，烷基或链烯基; 公开了用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化的新型化合物，以及包含它们的药物组合物 ，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

公开(公告)号：US07384944B2

公开(公告)日：2008-06-10

申请号：US10668862

申请日：2003-09-23

申请人： Bahige M. Baroudy ,  John W. Clader ,  Hubert B. Josien ,  Stuart W. McCombie ,  Brian A. McKittrick ,  Michael W. Miller ,  Bernard R. Neustadt ,  Anandan Palani ,  Elizabeth M. Smith ,  Ruo Steensma ,  Jayaram R. Tagat ,  Susan F. Vice ,  Mark A. Laughlin ,  Eric Gilbert ,  Marc A. Labroli

发明人： Bahige M. Baroudy ,  John W. Clader ,  Hubert B. Josien ,  Stuart W. McCombie ,  Brian A. McKittrick ,  Michael W. Miller ,  Bernard R. Neustadt ,  Anandan Palani ,  Elizabeth M. Smith ,  Ruo Steensma ,  Jayaram R. Tagat ,  Susan F. Vice ,  Mark A. Laughlin ,  Eric Gilbert ,  Marc A. Labroli

IPC分类号： A61K31/497

CPC分类号： C07D401/06 ,  A61K31/496 ,  A61K45/06 ,  C07D211/58 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D409/06 ,  C07D413/06 ,  A61K2300/00

摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.

摘要翻译： 使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R 1是氢或烷基; R 2是取代的苯基，取代的杂芳基，萘基，芴基，二苯基甲基或任选取代的苯基或杂芳基 - 烷基; R 3是氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基，苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R 4，R 5和R 7是氢或烷基; R 6是氢，烷基或链烯基; 公开了用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化的新型化合物，以及包含它们的药物组合物 ，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

公开(公告)号：US06391865B1

公开(公告)日：2002-05-21

申请号：US09562814

申请日：2000-05-01

申请人： Bahige M. Baroudy ,  John W. Clader ,  Hubert B. Josien ,  Stuart W. McCombie ,  Brian A. McKittrick ,  Michael W. Miller ,  Bernard R. Neustadt ,  Anandan Palani ,  Elizabeth M. Smith ,  Ruo Steensma ,  Jayaram R. Tagat ,  Susan F. Vice ,  Eric Gilbert ,  Marc A. Labroli

发明人： Bahige M. Baroudy ,  John W. Clader ,  Hubert B. Josien ,  Stuart W. McCombie ,  Brian A. McKittrick ,  Michael W. Miller ,  Bernard R. Neustadt ,  Anandan Palani ,  Elizabeth M. Smith ,  Ruo Steensma ,  Jayaram R. Tagat ,  Susan F. Vice ,  Eric Gilbert ,  Marc A. Labroli

IPC分类号： A01N5500

CPC分类号： A61K31/496 ,  A61K45/06 ,  C07D211/58 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D409/06 ,  C07D413/06 ,  A61K2300/00

摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.

摘要翻译： 使用式5的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R 1是氢或烷基; R 2是取代的苯基，取代的杂芳基，萘基，芴基，二苯基甲基或任选取代的苯基 - R 4是氢或烷基; R 6是氢，烷基或链烯基; R 4是氢或烷基; R 3是氢，烷基或烷氧基烷基， 公开了用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化的新型化合物，以及包含它们的药物组合物 ，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

公开(公告)号：US08114879B2

公开(公告)日：2012-02-14

申请号：US12055900

申请日：2008-03-26

申请人： Bahige M. Baroudy ,  John W. Clader ,  Hubert B. Josien ,  Stuart W. McCombie ,  Brian A. McKittrick ,  Michael W. Miller ,  Bernard R. Neustadt ,  Anandan Palani ,  Elizabeth M. Smith ,  Ruo Steensma ,  Jayaram R. Tagat ,  Susan F. Vice ,  Mark A. Laughlin ,  Eric Gilbert ,  Marc A. Labroli

发明人： Bahige M. Baroudy ,  John W. Clader ,  Hubert B. Josien ,  Stuart W. McCombie ,  Brian A. McKittrick ,  Michael W. Miller ,  Bernard R. Neustadt ,  Anandan Palani ,  Elizabeth M. Smith ,  Ruo Steensma ,  Jayaram R. Tagat ,  Susan F. Vice ,  Mark A. Laughlin ,  Eric Gilbert ,  Marc A. Labroli

IPC分类号： A61K31/497 ,  C07D403/00

CPC分类号： C07D401/06 ,  A61K31/496 ,  A61K45/06 ,  C07D211/58 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D409/06 ,  C07D413/06 ,  A61K2300/00

摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.

摘要翻译： 使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R1是氢或烷基; R 2是取代的苯基，取代的杂芳基，芴基，二苯基甲基或任选取代的苯基或杂芳基 - 烷基; R 3是氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基，苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R4，R5和R7是氢或烷基; R6是氢，烷基或烯基; 公开了用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化的新型化合物，以及包含它们的药物组合物 ，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

公开(公告)号：US06689765B2

公开(公告)日：2004-02-10

申请号：US10061011

申请日：2002-01-30

申请人： Bahige M. Baroudy ,  John W. Clader ,  Hubert B. Josien ,  Stuart W. McCombie ,  Brian A. McKittrick ,  Michael W. Miller ,  Bernard R. Neustadt ,  Anandan Palani ,  Elizabeth M. Smith ,  Ruo Steensma ,  Jayaram R. Tagat ,  Susan F. Vice ,  Mark A. Laughlin ,  Eric Gilbert ,  Marc A. Labroli

发明人： Bahige M. Baroudy ,  John W. Clader ,  Hubert B. Josien ,  Stuart W. McCombie ,  Brian A. McKittrick ,  Michael W. Miller ,  Bernard R. Neustadt ,  Anandan Palani ,  Elizabeth M. Smith ,  Ruo Steensma ,  Jayaram R. Tagat ,  Susan F. Vice ,  Mark A. Laughlin ,  Eric Gilbert ,  Marc A. Labroli

IPC分类号： A61K31695

CPC分类号： C07D401/06 ,  A61K31/496 ,  A61K45/06 ,  C07D211/58 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D409/06 ,  C07D413/06 ,  A61K2300/00

摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v, host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.

摘要翻译： 使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R 1是氢或烷基; R 2是取代的苯基，取代的杂芳基，萘基，芴基， 苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R 4，R 5，R 5和R 5独立地选自氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基， R 7为氢或烷基; R 6为氢，烷基或烯基;用于治疗HIV，实体器官移植排斥，移植物v，宿主病，关节炎，类风湿性关节炎，炎性肠病，特应性皮炎， 公开了牛皮癣，哮喘，过敏或多发性硬化，以及新化合物，包含它们的药物组合物，以及本发明的CCR5拮抗剂与用于治疗 可用于治疗炎性疾病的HIV或药物。

公开(公告)号：US07256186B2

公开(公告)日：2007-08-14

申请号：US10941440

申请日：2004-09-15

申请人： Dimitri A. Pissarntiski ,  Hubert B. Josien ,  Elizabeth M. Smith ,  John W. Clader ,  Theodros Asberom ,  Tao Guo ,  Douglas W. Hobbs

发明人： Dimitri A. Pissarntiski ,  Hubert B. Josien ,  Elizabeth M. Smith ,  John W. Clader ,  Theodros Asberom ,  Tao Guo ,  Douglas W. Hobbs

IPC分类号： C07D211/08 ,  C07D207/46 ,  C07D205/00 ,  C07D279/00 ,  A01N43/00

CPC分类号： C07D401/14 ,  C07D211/96 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D451/06 ,  C07D471/04 ,  C07D471/10 ,  C07D491/10

摘要： This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —XC(O)Y, alkylene-XC(O)Y, cycloalkylene-X—C(O)—Y, —CH—X—C(O)—NR3—Y or —CH—X—C(O)—Y, wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.

摘要翻译： 本发明公开了下式的新型γ分泌酶抑制剂：其中：R 1是取代的芳基或取代的杂芳基; R 2是R 1基团，烷基，-XC（O）Y，亚烷基-XC（O）Y，亚环烷基-XC（O）-Y，-CH -XC（O）-NR 3 -Y或-CH-XC（O）-Y，其中X和Y如本文所定义; 每个R 3和R 3各自独立地为H或烷基; R 11是芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基，芳基杂环烷基或烷氧基烷基。 还公开了使用一种或多种本发明化合物治疗阿尔茨海默病的方法。

公开(公告)号：US07208602B2

公开(公告)日：2007-04-24

申请号：US10358898

申请日：2003-02-05

申请人： Dmitri A. Pissarnitski ,  Hubert B. Josien ,  Elizabeth M. Smith ,  John W. Clader ,  Theodros Asberom ,  Tao Guo ,  Douglas W. Hobbs

发明人： Dmitri A. Pissarnitski ,  Hubert B. Josien ,  Elizabeth M. Smith ,  John W. Clader ,  Theodros Asberom ,  Tao Guo ,  Douglas W. Hobbs

IPC分类号： C07D211/08 ,  C07D207/46 ,  C07D205/00 ,  C07D279/00 ,  A01N43/00

CPC分类号： C07D401/12 ,  C07D211/96 ,  C07D401/14 ,  C07D409/12 ,  C07D471/10

摘要： This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —X(CO)Y, or alkylene-X(CO)Y wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.

摘要翻译： 本发明公开了下式的新型γ分泌酶抑制剂：其中：R 1是取代的芳基或取代的杂芳基; R 2是R 1基团，烷基，-X（CO）Y或亚烷基-X（CO）Y，其中X和Y如本文所定义; 每个R 3和R 3各自独立地为H或烷基; R 11是芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基，芳基杂环烷基或烷氧基烷基。 还公开了使用一种或多种本发明化合物治疗阿尔茨海默病的方法。

公开(公告)号：US07884080B2

公开(公告)日：2011-02-08

申请号：US11854754

申请日：2007-09-13

申请人： Robert G. Aslanian ,  Chad E. Bennett ,  Duane A. Burnett ,  Tin-Yau Chan ,  Eugenia Y. Kiselgof ,  Chad E. Knutson ,  Joel M. Harris ,  Brian A. McKittrick ,  Anandan Palani ,  Elizabeth M. Smith ,  Henry M. Vaccaro ,  Dong Xiao ,  Hyunjin M. Kim

发明人： Robert G. Aslanian ,  Chad E. Bennett ,  Duane A. Burnett ,  Tin-Yau Chan ,  Eugenia Y. Kiselgof ,  Chad E. Knutson ,  Joel M. Harris ,  Brian A. McKittrick ,  Anandan Palani ,  Elizabeth M. Smith ,  Henry M. Vaccaro ,  Dong Xiao ,  Hyunjin M. Kim

IPC分类号： C07D471/10 ,  A61K31/397 ,  A61P3/06 ,  A61P3/10

CPC分类号： C07D471/10

摘要： The present invention relates to Azetidinone Derivatives of structural formula 1: and compositions comprising an Azetidinone Derivative and methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering to a patient an effective amount of an Azetidinone Derivative.

摘要翻译： 本发明涉及结构式1的氮杂环丁酮衍生物和包含氮杂环丁酮衍生物的组合物和用于治疗或预防脂质代谢紊乱，疼痛，糖尿病，血管病症，脱髓鞘或非酒精性脂肪性肝病的方法，包括给予患者 有效量的氮杂环丁酮衍生物。

公开(公告)号：US06204282B1

公开(公告)日：2001-03-20

申请号：US09450235

申请日：1999-11-29

申请人： Bernard R. Neustadt ,  Elizabeth M. Smith

发明人： Bernard R. Neustadt ,  Elizabeth M. Smith

IPC分类号： A61K314184

CPC分类号： C07D235/14

摘要： The present invention provides compounds having the formula wherein n, p, q and r are each independently selected from 0 or 1; a, b, c, and d each independently represents a carbon or nitrogen atom, with the proviso that no more than two of a, b, c, and d are nitrogen atoms; Y and Y1 each independently represents 1-4 optional substituents selected from alkyl, alkoxy, halo, —CF3, and —C(O)OH; R1, R2, R3 and R4 are as defined herein; R5, R6, R7, R8, R9, R10, R11 and R12 are independently selected from H or C1-C3 alkyl; and wherein are positioned meta or para relative to each other; or a biolabile ester thereof, or a pharmaceutically acceptable salt thereof. Also provided are methods of using these compounds for treating vitronectin-mediated disorders, e.g., cancer, retinopathy, artherosclerosis, vascular restenosis, and osteoporosis.

摘要翻译： 本发明提供了具有式n，p，q和r各自独立地选自0或1的化合物; a，b，c和d各自独立地表示碳原子或氮原子，条件是不大于2个 a，b，c和d是氮原子; Y和Y1各自独立地表示1-4个选自烷基，烷氧基，卤素，-CF 3和-C（O）OH的任选取代基; R 1，R 2，R 3和R 4是 如本文所定义; R 5，R 6，R 7，R 8，R 9，R 10，R 11和R 12独立地选自H或C 1 -C 3烷基;并且其中相对于彼此定位为间位或对位;或其不可生物酯， 其可接受的盐。 还提供了使用这些化合物治疗玻连蛋白介导的病症例如癌症，视网膜病变，动脉粥样硬化，血管再狭窄和骨质疏松症的方法。

公开(公告)号：US5348944A

公开(公告)日：1994-09-20

申请号：US261815

申请日：1988-04-04

申请人： Elijah H. Gold ,  Bernard R. Neustadt ,  Elizabeth M. Smith

发明人： Elijah H. Gold ,  Bernard R. Neustadt ,  Elizabeth M. Smith

IPC分类号： A61K38/00 ,  C07K5/02 ,  A61K37/02 ,  C07K5/06

CPC分类号： C07K5/0222 ,  A61K38/00

摘要： Compounds of the formula ##STR1## useful as antihypertensive agents are disclosed.

摘要翻译： 公开了可用作抗高血压药的式“IMAGE”的化合物。