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公开(公告)号：US06518424B1
公开(公告)日：2003-02-11
申请号：US09438103
申请日：1999-11-10
IPC分类号： C07D23924
CPC分类号： C07D239/36 , C07D239/42
摘要： Substituted pyrimidines that have the general structure: in which the symbol R1 represents a C1-C6 alkyl, C1-C6 alkoxy or halogen atom; R2 represents a phenyl group, substituted phenyl group, benzyl moiety, substituted benzyl moiety, C3-C7 cycloalkyl, or substituted C3-C7 cycloalkyl; R3 represents a hydrogen or C1-C6 alkyl group, R4 represents —H, —OH, —N3 or —NHCOCH3; and R5 represents H are provided. These compounds have activity as inhibitors of phospholipase A2, and are useful in treating disorders mediated by phospholipase A2.
摘要翻译： 具有一般结构的取代的嘧啶：其中符号R1表示C1-C6烷基，C1-C6烷氧基或卤素原子; R 2表示苯基，取代的苯基，苄基部分，取代的苄基部分，C 3 -C 7环烷基或取代的C 3 -C 7环烷基; R 3表示氢或C 1 -C 6烷基，R 4表示-H，-OH，-N 3或-NHCOCH 3; 并且R5表示H。 这些化合物作为磷脂酶A2的抑制剂具有活性，可用于治疗由磷脂酶A2介导的病症。
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公开(公告)号：US5866318A
公开(公告)日：1999-02-02
申请号：US476463
申请日：1995-06-07
IPC分类号： A61K31/63 , A61K31/635 , C07C311/39 , C07C311/46 , C07C317/44 , C07C323/52 , C07D209/24 , C07D213/56 , C07D231/12 , C07D233/54 , C07D277/30 , C07D307/54 , C07D333/28 , C07D333/60 , C07F9/40 , C12Q1/34 , G01N33/50 , C12Q1/00 , C12N5/06 , C12Q1/68
CPC分类号： G01N33/5058 , A61K31/63 , A61K31/635 , C07C311/39 , C07C311/46 , C07C317/44 , C07C323/52 , C07D209/24 , C07D213/56 , C07D231/12 , C07D233/64 , C07D277/30 , C07D307/54 , C07D333/28 , C07D333/60 , C07F9/4006 , C12Q1/34 , G01N33/5008 , G01N33/5014 , G01N33/502 , C07C2101/18 , G01N2333/918 , G01N2500/00 , G01N2510/00
摘要： The invention is drawn to a method for identifying agents that inhibit neural degeneration by administering to cell populations consisting essentially of neurons or cells from neuronal cell lines, where these cells are exposed to an apoptotic stimulus other than APP gene products, an agent, where it is determined whether the agent inhibits neural degeneration.
摘要翻译： 本发明涉及用于鉴定抑制神经变性的药剂的方法，所述药物通过对基本上由神经元细胞组成的神经元或细胞组成的细胞群施用，其中这些细胞暴露于除APP基因产物之外的凋亡刺激物，其中它们 确定该药物是否抑制神经变性。
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3.发明授权Dipeptide and related compounds which inhibit leukocyte adhesion mediated by VLA-4 失效抑制由VLA-4介导的白细胞粘附的二肽和相关化合物公开(公告)号：US07288526B2
公开(公告)日：2007-10-30
申请号：US10119238
申请日：2002-04-08
申请人： Eugene D. Thorsett , Christopher M. Semko , Michael A. Pleiss , Louis John Lombardo , Francine S. Grant , Darren B. Dressen , Michael S. Dappen
发明人： Eugene D. Thorsett , Christopher M. Semko , Michael A. Pleiss , Louis John Lombardo , Francine S. Grant , Darren B. Dressen , Michael S. Dappen
IPC分类号： C07K5/06
CPC分类号： C07K5/06026 , A61K38/00 , C07K5/06104 , C07K5/06139 , C07K5/06165
摘要： Disclosed are compounds which bind VLA-4. Certain of these compounds aslo inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
摘要翻译： 公开了结合VLA-4的化合物。 这些化合物中的某些化合物抑制白细胞粘附，特别是由VLA-4介导的白细胞粘附。 这样的化合物可用于治疗哺乳动物患者，例如人类例如哮喘，阿尔茨海默氏病，动脉粥样硬化，艾滋病痴呆，糖尿病，炎性肠病，类风湿性关节炎，组织移植，肿瘤转移和心肌缺血等炎性疾病。 化合物也可以用于治疗炎性脑疾病如多发性硬化症。
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4.发明授权Identification of phospholipase A2 inhibitors in A.beta. peptide-mediated neurodegenerative disease 失效鉴定Aβ肽介导的神经变性疾病中磷脂酶A2抑制剂
公开(公告)号：US5707821A
公开(公告)日：1998-01-13
申请号：US476464
申请日：1995-06-07
IPC分类号： A61K31/63 , A61K31/635 , C07C311/39 , C07C311/46 , C07C317/44 , C07C323/52 , C07D209/24 , C07D213/56 , C07D231/12 , C07D233/54 , C07D277/30 , C07D307/54 , C07D333/28 , C07D333/60 , C07F9/40 , C12Q1/34 , G01N33/50 , A61K00/00
CPC分类号： G01N33/5058 , A61K31/63 , A61K31/635 , C07C311/39 , C07C311/46 , C07C317/44 , C07C323/52 , C07D209/24 , C07D213/56 , C07D231/12 , C07D233/64 , C07D277/30 , C07D307/54 , C07D333/28 , C07D333/60 , C07F9/4006 , C12Q1/34 , G01N33/5008 , G01N33/5014 , G01N33/502 , G01N33/5044 , C07C2101/18 , G01N2333/918 , G01N2500/00
摘要： The invention provides methods and compositions for treating neurodegeneration in mammalian cells by administering a phospholipase A2 inhibitor.
摘要翻译： 本发明提供了通过施用磷脂酶A2抑制剂来治疗哺乳动物细胞中神经变性的方法和组合物。
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5.发明授权Sulfonylquinoxalone derivatives and related compounds as bradykinin antagonists 失效磺酰喹诺酮衍生物和相关化合物作为缓激肽拮抗剂公开(公告)号：US07635775B2
公开(公告)日：2009-12-22
申请号：US11429656
申请日：2006-05-05
申请人： Francine S. Grant , Sarah Bartulis , Louis Brogley , Michael S. Dappen , Ramesh Kasar , Mohammed A. Khan , Martin Neitzel , Michael A. Pleiss , Eugene D. Thorsett , John Tucker , Michael Ye , Jon E. Hawkinson
发明人： Francine S. Grant , Sarah Bartulis , Louis Brogley , Michael S. Dappen , Ramesh Kasar , Mohammed A. Khan , Martin Neitzel , Michael A. Pleiss , Eugene D. Thorsett , John Tucker , Michael Ye , Jon E. Hawkinson
IPC分类号： A61K31/498 , C07D241/50 , A61P11/06 , A61P25/06 , A61P25/02
CPC分类号： C07D401/14 , C07D241/44 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Disclosed are sulfonylquinoxalone acetamide derivatives useful as bradykinin antagonists.
摘要翻译： 公开了用作缓激肽拮抗剂的磺酰基喹喔啉乙酰胺衍生物。
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公开(公告)号：US06559127B1
公开(公告)日：2003-05-06
申请号：US09127533
申请日：1998-07-31
申请人： Michael S. Dappen , Darren B. Dressen , Francine S. Grant , Michael A. Pleiss , Cynthia Y. Robinson , Dimitrios Sarantakis , Eugene D. Thorsett
发明人： Michael S. Dappen , Darren B. Dressen , Francine S. Grant , Michael A. Pleiss , Cynthia Y. Robinson , Dimitrios Sarantakis , Eugene D. Thorsett
IPC分类号： C07K506
CPC分类号： C07K5/06069 , A61K38/00 , C07K5/06026 , C07K5/06121
摘要： Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
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公开(公告)号：US07166580B2
公开(公告)日：2007-01-23
申请号：US10266889
申请日：2002-10-07
申请人： Michael S. Dappen , Darren B. Dressen , Francine S. Grant , Michael A. Pleiss , Cynthia Y. Robinson , Dimitrios Sarantakis , Eugene D. Thorsett
发明人： Michael S. Dappen , Darren B. Dressen , Francine S. Grant , Michael A. Pleiss , Cynthia Y. Robinson , Dimitrios Sarantakis , Eugene D. Thorsett
IPC分类号： C07K5/06
CPC分类号： C07K5/06069 , A61K38/00 , C07K5/06026 , C07K5/06121
摘要： Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
摘要翻译： 公开了结合VLA-4的化合物。 这些化合物中的某些也抑制白细胞粘附，特别是由VLA-4介导的白细胞粘附。 这样的化合物可用于治疗哺乳动物患者，例如人类例如哮喘，阿尔茨海默氏病，动脉粥样硬化，艾滋病痴呆，糖尿病，炎性肠病，类风湿性关节炎，组织移植，肿瘤转移和心肌缺血等炎性疾病。 化合物也可以用于治疗炎性脑疾病如多发性硬化症。
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8.发明授权Dipeptide and related compounds which inhibit leukocyte adhesion mediated by VLA-4 失效抑制由VLA-4介导的白细胞粘附的二肽和相关化合物公开(公告)号：US06423688B1
公开(公告)日：2002-07-23
申请号：US09126329
申请日：1998-07-31
申请人： Eugene D. Thorsett , Christopher M. Semko , Michael A. Pleiss , Louis John Lombardo , Francine S. Grant , Darren B. Dressen , Michael S. Dappen
发明人： Eugene D. Thorsett , Christopher M. Semko , Michael A. Pleiss , Louis John Lombardo , Francine S. Grant , Darren B. Dressen , Michael S. Dappen
IPC分类号： C07K5078
CPC分类号： C07K5/06026 , A61K38/00 , C07K5/06104 , C07K5/06139 , C07K5/06165
摘要： Disclosed are compounds which bind VLA-4. Certain of these compounds aslo inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
摘要翻译： 公开了结合VLA-4的化合物。 这些化合物中的某些化合物抑制白细胞粘附，特别是由VLA-4介导的白细胞粘附。 这样的化合物可用于治疗哺乳动物患者，例如人类例如哮喘，阿尔茨海默氏病，动脉粥样硬化，艾滋病痴呆，糖尿病，炎性肠病，类风湿性关节炎，组织移植，肿瘤转移和心肌缺血等炎性疾病。 化合物也可以用于治疗炎性脑疾病如多发性硬化症。
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9.发明授权Sulfonylquinoxalone derivatives and related compounds as bradykinin antagonists 失效磺酰喹诺酮衍生物和相关化合物作为缓激肽拮抗剂公开(公告)号：US07183281B2
公开(公告)日：2007-02-27
申请号：US10429917
申请日：2003-05-02
申请人： Francine S. Grant , Sarah Bartulis , Louis Brogley , Michael S. Dappen , Ramesh Kasar , Mohammed A. Khan , Martin Neitzel , Michael A. Pleiss , Eugene D. Thorsett , John Tucker , Michael Ye , Jon E. Hawkinson
发明人： Francine S. Grant , Sarah Bartulis , Louis Brogley , Michael S. Dappen , Ramesh Kasar , Mohammed A. Khan , Martin Neitzel , Michael A. Pleiss , Eugene D. Thorsett , John Tucker , Michael Ye , Jon E. Hawkinson
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D413/00
CPC分类号： C07D401/14 , C07D241/44 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Disclosed are sulfonylquinoxalone derivatives of the general formula: These compounds are useful as bradykinin antagonists.
摘要翻译： 公开了以下通式的磺酰基喹诺酮衍生物：这些化合物可用作缓激肽拮抗剂。
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公开(公告)号：US07056937B2
公开(公告)日：2006-06-06
申请号：US10429203
申请日：2003-05-02
申请人： Francine S. Grant , Sarah Bartulis , Louis Brogley , Michael S. Dappen , Ramesh Kasar , Ryan Holcomb , Michael A. Pleiss , Eugene D. Thorsett , Michael Ye , Jon E. Hawkinson
发明人： Francine S. Grant , Sarah Bartulis , Louis Brogley , Michael S. Dappen , Ramesh Kasar , Ryan Holcomb , Michael A. Pleiss , Eugene D. Thorsett , Michael Ye , Jon E. Hawkinson
IPC分类号： A01N43/40 , A61K31/44 , C07D239/00 , C07D239/70 , C07D47/00
CPC分类号： C07D401/14 , C07D241/44 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Disclosed are 1-sulfonylquioxalone acetamides and derivatives thereof. The compounds are exemplified by compounds of the formula: Such compounds, derivatives and related compounds are useful as bradykinin antagonists.
摘要翻译： 公开了1-磺酰基二氧杂环己烷乙酰胺及其衍生物。 化合物的实例是下式的化合物：这样的化合物，衍生物和相关化合物可用作缓激肽拮抗剂。
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