公开(公告)号：US07417152B2

公开(公告)日：2008-08-26

申请号：US10555519

申请日：2004-04-30

申请人： Jay S. Tung ,  Albert W. Garofalo ,  Michael A. Pleiss ,  Jing Wu ,  David W. G. Wone ,  Ashley C. Guinn ,  Darren B. Dressen ,  R. Jeffrey Neitz ,  Jennifer Marugg ,  Martin Neitzel

发明人： Jay S. Tung ,  Albert W. Garofalo ,  Michael A. Pleiss ,  Jing Wu ,  David W. G. Wone ,  Ashley C. Guinn ,  Darren B. Dressen ,  R. Jeffrey Neitz ,  Jennifer Marugg ,  Martin Neitzel

IPC分类号： C07D231/12 ,  C07D233/04

CPC分类号： C07D401/14 ,  C07D231/16 ,  C07D231/40 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D453/02 ,  C07D471/04 ,  C07D471/08 ,  C07D487/08

摘要： Disclosed are compounds of formula I and II that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action.

摘要翻译： 公开了作为缓激肽B 1受体拮抗剂的式I和II化合物，并且可用于治疗由缓激肽B 1介导的哺乳动物中疾病或与疾病相关的不良症状， SUB>受体。 某些化合物表现出增加的效力，并且还预期表现出增加的作用持续时间。

公开(公告)号：US07432379B2

公开(公告)日：2008-10-07

申请号：US10837231

申请日：2004-04-30

申请人： Jay S. Tung ,  Albert W. Garofalo ,  Michael A. Pleiss ,  Jing Wu ,  David W. G. Wone ,  Ashley C. Guinn ,  Darren B. Dressen ,  R. Jeffrey Neitz ,  Jennifer Marugg ,  Martin Neitzel

发明人： Jay S. Tung ,  Albert W. Garofalo ,  Michael A. Pleiss ,  Jing Wu ,  David W. G. Wone ,  Ashley C. Guinn ,  Darren B. Dressen ,  R. Jeffrey Neitz ,  Jennifer Marugg ,  Martin Neitzel

IPC分类号： C07D401/12

CPC分类号： C07D401/14 ,  C07D231/16 ,  C07D231/40 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D453/02 ,  C07D471/04 ,  C07D471/08 ,  C07D487/08

摘要： Disclosed are compounds that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action.

摘要翻译： 公开了缓激肽B 1受体拮抗剂的化合物，并且可用于治疗由缓激肽B 1受体介导的哺乳动物中疾病或与疾病状况相关的不良症状。 某些化合物表现出增加的效力，并且还预期表现出增加的作用持续时间。

公开(公告)号：US07053220B2

公开(公告)日：2006-05-30

申请号：US10355700

申请日：2003-01-31

申请人： Jay S. Tung ,  Ashley C. Guinn ,  Eugene D. Thorsett ,  Michael A. Pleiss

发明人： Jay S. Tung ,  Ashley C. Guinn ,  Eugene D. Thorsett ,  Michael A. Pleiss

IPC分类号： C07D285/135

CPC分类号： C07D233/80 ,  C07D233/74

摘要： This invention is directed to a class of compounds (Formula I) including hydroxyalkanoyl amino pyrazoles, hydroxyalkanoyl amino thiadiazoles, hydroxyalkanoyl amino acid esters, hydroxyalkanoyl amino acid amides, hydroxyalkanoyl amino alcohols, hydroxyalkanoyl amino ketoes, hydroxyalkanoyl amino hydantoins, hydroxyalkanoyl anilines, and hydroxyalkanoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting β-amyloid peptide release and/or synthesis, a method for inhibiting γ-secretase activity and a method for treating neurological disorders associated with β-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.

摘要翻译： 本发明涉及一类包括羟基烷酰基氨基吡唑，羟基烷酰基氨基噻二唑，羟基烷酰基氨基酸酯，羟基烷酰基氨基酸酰胺，羟基烷酰基氨基醇，羟基链烷酰基氨基酮，羟基链烷酰基氨基乙内酰脲，羟基烷酰基苯胺和羟基烷酰基衍生物 的特权结构。 本发明还涉及药物组合物，其包含药学上可接受的盐形式的这种化合物或其前体药物。 本发明进一步涉及一种抑制β-淀粉样蛋白肽释放和/或合成的方法，一种抑制γ-分泌酶活性的方法和一种治疗与β-淀粉样蛋白肽生产相关的神经障碍的方法。 该方法包括向宿主施用包含有效量的式I化合物的药物制剂。式I化合物可用于预防和治疗阿尔茨海默氏病。

公开(公告)号：US06974829B2

公开(公告)日：2005-12-13

申请号：US10434528

申请日：2003-05-07

申请人： Jay S. Tung ,  Ashley C. Guinn ,  Eugene D. Thorsett ,  Michael A. Pleiss

发明人： Jay S. Tung ,  Ashley C. Guinn ,  Eugene D. Thorsett ,  Michael A. Pleiss

IPC分类号： C07D231/40 ,  C07D233/80 ,  C07D285/12 ,  C07D285/135 ,  A61K31/41 ,  A61P25/00 ,  C07P285/08

CPC分类号： C07D285/135 ,  C07D231/40 ,  C07D233/80

摘要： This invention is directed to a class of compounds (Formula I) including succinoyl amino pyrazoles, succinoyl amino thiadiazoles, succinoyl amino acid esters, succinoyl amino acid amides, succinoyl amino alcohols, succinoyl amino ketones, succinoyl amino hydantoins, succinoyl anilines, and succinoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting β-amyloid peptide release and/or synthesis, a method for inhibiting γ-secretase activity and a method for treating neurological disorders associated with β-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.

摘要翻译： 本发明涉及一类包括琥珀酰基氨基吡唑，琥珀酰基氨基噻二唑，琥珀酰氨基酸酯，琥珀酰氨基酰胺，琥珀酰氨基醇，琥珀酰氨基酮，琥珀酰基氨基乙内酰脲，琥珀酰基苯胺和琥珀酰基衍生物的化合物（式I） 的特权结构。 本发明还涉及药物组合物，其包含药学上可接受的盐形式的这种化合物或其前体药物。 本发明进一步涉及一种抑制β-淀粉样蛋白肽释放和/或合成的方法，一种抑制γ-分泌酶活性的方法和一种治疗与β-淀粉样蛋白肽生产相关的神经障碍的方法。 该方法包括向宿主施用包含有效量的式I化合物的药物制剂。式I化合物可用于预防和治疗阿尔茨海默氏病。