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1. 发明申请

US20080188485A1 PIPERIDINE DERIVATIVES USEFUL AS CCR5 ANTAGONISTS 有权
标题翻译：哌啶衍生物作为CCR5拮抗剂有用
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。

2. 发明授权

US07384944B2 Piperazine derivatives useful as CCR5 antagonists 有权
标题翻译：哌嗪衍生物可用作CCR5拮抗剂
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。

3. 发明授权

US08114879B2 Piperazine derivatives useful as CCR5 antagonists 有权
标题翻译：哌嗪衍生物可用作CCR5拮抗剂
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。

4. 发明授权

US06689765B2 Piperazine derivatives useful as CCR5 antagonists 有权
标题翻译：可用作CCR5拮抗剂的哌嗪衍生物
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。

5. 发明授权

US06391865B1 Piperazine derivatives useful as CCR5 antagonists 有权
标题翻译：哌嗪衍生物可用作CCR5拮抗剂
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。

6. 发明授权

US06387930B1 Piperidine derivatives useful as CCR5 antagonists 有权
标题翻译：哌啶衍生物可用作CCR5拮抗剂
公开(公告)号：US06387930B1
公开(公告)日：2002-05-14
申请号：US09562815
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 , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin
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 , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin
IPC分类号： C07D40104
CPC分类号： C07D401/14 , C07D211/58 , C07D413/14 , C07D417/14
摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein X is —C(R13)2—, —C(R13)(R19)—, —C(O)—, —O—, —NH—, —N(alkyl)—, R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is H, alkyl or alkenyl; R2 is optionally substituted phenyl, phenylalkyl, heteroaryl or heteroarylalkyl, naphthyl, fluorenyl or diphenylmethyl; R3 is optionally substituted phenyl, heteroaryl or naphthyl; R4 is H, alkyl, fluoro-alkyl, cyclopropylmethyl, —CH2CH2OH, —CH2CH2—O-alkyl, —CH2C(O)—O-alkyl, —CH2C(O)NH2, —CH2C(O)—NHalkyl or —CH2C(O)—N(alkyl)2; R19 is optionally substituted phenyl, heteroaryl or naphthyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; and R5, R13, R14, R15 and R16 are hydrogen or alkyl 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X是-C（R 13）2 - ， - C（R 13）（R 19） - ， - C（O） - ， - O - N（烷基） - ，R是任选取代的苯基，吡啶基，噻吩基或萘基; R1是H，烷基或烯基; R2是任选取代的苯基，苯基烷基，杂芳基或杂芳基烷基，萘基，芴基或二苯基甲基; R 3是任选取代的苯基，杂芳基或萘基; R4是H，烷基，氟代烷基，环丙基甲基，-CH2CH2OH，-CH2CH2-O-烷基，-CH2C（O）-O-烷基，-CH2C（O）NH2，-CH2C（O）或-CH 2 C（O）-N（烷基）2; R 19是任选取代的苯基，杂芳基或萘基，环烷基，环烷基烷基或烷氧基烷基; 和R 5，R 13，R 14，R 15和R 16是氢或烷基，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，炎性肠病，特应性皮炎，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。

7. 发明授权

US06602885B2 Piperidine derivatives useful as CCR5 antagonists 有权
标题翻译：哌啶衍生物可用作CCR5拮抗剂
公开(公告)号：US06602885B2
公开(公告)日：2003-08-05
申请号：US10010481
申请日：2001-11-08
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 , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin
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 , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin
IPC分类号： A61K314545
CPC分类号： C07D401/14 , C07D211/58 , C07D413/14 , C07D417/14
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 H, alkyl or alkenyl; R2 is optionally substituted phenyl, phenylalkyl, heteroaryl or heteroarylalkyl, naphthyl, fluorenyl or diphenylmethyl; R3 is optionally substituted phenyl, heteroaryl or naphthyl; R4 is H, alkyl, fluoro-alkyl, cyclopropylmethyl, —CH2CH2OH, —CH2CH2—O-alkyl, —CH2C(O)—O-alkyl, —CH2C(O)NH2, —CH2C(O)—NHalkyl or —CH2C(O)—N(alkyl)2; R19 is optionally substituted phenyl, heteroaryl or naphthyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; and R5, R13, R14, R15 and R16 are hydrogen or alkyl 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H，烷基或烯基; R 2是任选取代的苯基，苯基烷基，杂芳基或杂芳基烷基，萘基，芴基或二苯基甲基; R3是任选取代的苯基，杂芳基或萘基; R 4是H，烷基，氟代烷基，环丙基甲基，-CH 2 CH 2 OH，-CH 2 CH 2 -O-烷基，-CH 2 C（O）-O-烷基，-CH 2 C（O），-CH 2 C（O）-NH烷基或-CH 2 C（O）-N（烷基）2; R 19是任选取代的苯基，杂芳基或萘基，环烷基，环烷基烷基或烷氧基烷基; 和R 5，R 13，R 14，R 15和R 16是氢或烷基，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，炎性肠病，特应性皮炎，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。

8. 发明授权

US06204282B1 Benzimidazole compounds that are vitronectin receptor antagonists 失效
标题翻译：作为玻连蛋白受体拮抗剂的苯并咪唑化合物
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。

9. 发明授权

US5348944A Carboxyalkyl dipeptides 失效
标题翻译：羧甲基二肽
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。

10. 发明授权

US4929641A Mercapto-acylamino acid antihypertensives 失效
标题翻译：巯基 - 酰氨基酸抗高血压药
公开(公告)号：US4929641A
公开(公告)日：1990-05-29
申请号：US192435
申请日：1988-05-11
申请人： Martin F. Haslanger , Bernard R. Neustadt , Elizabeth M. Smith
发明人： Martin F. Haslanger , Bernard R. Neustadt , Elizabeth M. Smith
IPC分类号： C07C323/59 , C07C327/32
CPC分类号： C07C323/59 , C07C327/32
摘要： Novel mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension are disclosed.
摘要翻译：公开了可用于治疗高血压的新型巯基酰基氨基酸和用于治疗高血压的巯基酰基氨基酸和心房利钠因子或血管紧张素转换酶抑制剂的组合。

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