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1. 发明申请

WO2004098589A1 4- BROMO - 5 - (2- CHLORO - BENZOYLAMINO) - 1H - PYRAZOLE - 3 - CARBOXYLIC ACID AMIDE DERIVATIVES AND RELATED COMPOUNDS AS BRADYKININ B1 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译： 4-溴 - 5-（2-氯代苯甲酰氨基） - 1H-吡唑-3-羧酸酰胺衍生物及相关化合物作为治疗炎症性疾病的BRADYKININ B1受体拮抗剂
公开(公告)号：WO2004098589A1
公开(公告)日：2004-11-18
申请号：PCT/US2004/013219
申请日：2004-04-30
申请人： ELAN PHARMACEUTICALS, INC. , TUNG, Jay, S. , GAROFALO, Albert, W. , PLEISS, Michael, A. , WU, Jing , WONE, David, W., G. , GUINN, Ashley, C. , DRESSEN, Darren, B. , NEITZ, R., Jeffrey , MARUGG, Jennifer , NEITZEL, Martin
发明人： TUNG, Jay, S. , GAROFALO, Albert, W. , PLEISS, Michael, A. , WU, Jing , WONE, David, W., G. , GUINN, Ashley, C. , DRESSEN, Darren, B. , NEITZ, R., Jeffrey , MARUGG, Jennifer , NEITZEL, Martin
IPC分类号： A61K31/415
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 B 1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B 1 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B1受体拮抗剂的式I和II化合物，可用于治疗由缓激肽B1受体介导的哺乳动物中疾病或与疾病相关的不良症状。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。

2. 发明申请

WO2004098590A1 4-BROMO-5- (2-CHLORO-BENZOYLAMINO)-1H-PYRAZOLE-3-CARBOXYLIC ACID (1-(AMINOCARBONYL) ETH-1-YL) AMIDE DERIVATIVES AND RELATED COMPOUNDS AS BRADYKININ B1 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译： 4-溴-5-（2-氯苯甲酰氨基）-1H-吡唑-3-羧酸（1-（氨基羰基）ETH-1-YL）酰胺衍生物及相关化合物作为治疗炎症性疾病的BRADYKININ B1受体拮抗剂
公开(公告)号：WO2004098590A1
公开(公告)日：2004-11-18
申请号：PCT/US2004/013400
申请日：2004-04-30
申请人： ELAN PHARMACEUTICALS, INC. , TUNG, Jay, S. , GAROFALO, Albert, W. , PLEISS, Michael, A. , WU, Jing , WONE, David, W., G. , GUINN, Ashley, C. , DRESSEN, Darren, B. , MARUGG, Jennifer , NEITZEL, Martin
发明人： TUNG, Jay, S. , GAROFALO, Albert, W. , PLEISS, Michael, A. , WU, Jing , WONE, David, W., G. , GUINN, Ashley, C. , DRESSEN, Darren, B. , MARUGG, Jennifer , NEITZEL, Martin
IPC分类号： A61K31/415
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 formulae (I) and (II) that are bradykinin B 1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B 1 receptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action. Wherein Z is selected from O, S and NH; Q of formula (III) and the other substituents are as defined in claim 1.
摘要翻译：公开了缓激肽B1受体拮抗剂的式（I）和（II）化合物，并且可用于治疗由缓激肽B1受体介导的哺乳动物中疾病或与疾病相关的不良症状。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。其中Z选自O，S和NH; 式（III）的Q和其它取代基如权利要求1中所定义。

3. 发明申请

WO2004099155A2 SELECTED SUBSTITUTED PYRAZOLE DERIVATIVES AND RELATED COMPOUNDS AS BRADYKININ B1 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：选择性取代的吡唑衍生物及相关化合物作为BRADYKININ B1受体拮抗剂
公开(公告)号：WO2004099155A2
公开(公告)日：2004-11-18
申请号：PCT/US2004/013655
申请日：2004-04-30
申请人： ELAN PHARMACEUTICALS, INC. , GAROFALO, Albert, W. , TUNG, Jay, S. , PLEISS, Michael, A. , WU, Jing , WONE, David, W., G. , GUINN, Ashley, C. , DRESSEN, Darren, B. , MARUGG, Jennifer , NEITZEL, Martin
发明人： GAROFALO, Albert, W. , TUNG, Jay, S. , PLEISS, Michael, A. , WU, Jing , WONE, David, W., G. , GUINN, Ashley, C. , DRESSEN, Darren, B. , MARUGG, Jennifer , NEITZEL, Martin
IPC分类号： C07D231/00
CPC分类号： C07D401/12 , C07D231/16 , C07D231/40 , C07D403/12 , C07D417/12
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B1受体拮抗剂的化合物，可用于治疗由缓激肽B1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。

4. 发明申请

WO2003064396A1 HYDROXYALKANOYL AMINOPYRAZOLES AND RELATED COMPOUNDS 审中-公开
标题翻译：羟基烷基亚氨基和其相关化合物
公开(公告)号：WO2003064396A1
公开(公告)日：2003-08-07
申请号：PCT/US2003/003143
申请日：2003-01-31
申请人： ELAN PHARMACEUTICALS, INC. , TUNG, Jay, S. , GUINN, Ashley, C. , THORSETT, Gene , PLEISS, Mike, A.
发明人： TUNG, Jay, S. , GUINN, Ashley, C. , THORSETT, Gene , PLEISS, Mike, A.
IPC分类号： C07D231/40
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 product thereof. The invention is further directed to a method for inhibiting ß-amyloid peptide release and/or synthesis, a method for inhibiting γ-secretase activity and a method for treating neurological disorders associated with ß-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：本发明涉及一类化合物（I），其包括羟基烷酰基氨基吡唑，羟基链烷酰基氨基噻二唑，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，羟基链烷酰氨基乙内酰脲，羟基链烷酰苯胺和羟基烷酰基衍生物的特权结构。本发明还涉及包含药学上可接受的盐形式的化合物或其产物的药物形式。本发明进一步涉及抑制β-淀粉样蛋白肽释放和/或合成的方法，抑制γ-分泌酶活性的方法和用于治疗与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。

5. 发明申请

WO2007047305A1 METHODS OF TREATING AMYLOIDOSIS USING CYCLOPROPYL DERIVATIVE ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译：用环丙基衍生物天冬氨酸蛋白酶抑制剂治疗淀粉样病变的方法
公开(公告)号：WO2007047305A1
公开(公告)日：2007-04-26
申请号：PCT/US2006/039719
申请日：2006-10-11
申请人： ELAN PHARMACEUTICALS, INC. , NEITZ, R., Jeffrey , TISDALE, Eric , JAGODZINSKA, Barabara , TRUONG, Anh , TUNG, Jay, S.
发明人： NEITZ, R., Jeffrey , TISDALE, Eric , JAGODZINSKA, Barabara , TRUONG, Anh , TUNG, Jay, S.
IPC分类号： C07C237/24 , C07D231/12 , C07C233/36 , C07C323/26 , C07D261/08 , C07D249/04 , C07C233/78 , C07D295/18 , A61K31/165 , A61K31/415 , A61K31/42 , A61K31/41 , A61P25/28
CPC分类号： C07D249/04 , C07C233/36 , C07C233/78 , C07C237/24 , C07C323/26 , C07C2601/02 , C07C2602/18 , C07D207/06 , C07D231/12 , C07D261/08 , C07D295/108 , C07D295/182
摘要： The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
摘要翻译：本发明涉及治疗与淀粉样变性有关的疾病，病症和病症的新型化合物和方法。淀粉样变性是指与A-β蛋白异常沉积有关的疾病，病症和病症的集合。

6. 发明申请

WO2006071775A2 NOVEL COMPOUNDS USEFUL FOR BRADYKININ B1 RECEPTOR ANTAGONISM 审中-公开
标题翻译：新型化合物对BRADYKININ B1受体拮抗剂有用
公开(公告)号：WO2006071775A2
公开(公告)日：2006-07-06
申请号：PCT/US2005/046785
申请日：2005-12-21
申请人： ELAN PHARMACEUTICALS, INC. , TUNG, Jay, S. , DRESSEN, Darren, D. , NETIZ, R., Jeffrey , PLEISS, Michael, A.
发明人： TUNG, Jay, S. , DRESSEN, Darren, D. , NETIZ, R., Jeffrey , PLEISS, Michael, A.
CPC分类号： C07D249/18 , A61K31/00 , A61K31/397 , A61K31/445 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/55 , A61K31/5513 , C07D243/14 , C07D243/24 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14
摘要： Disclosed are compounds that are bradykinin B 1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B 1 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。某些化合物表现出更高的效力，并且还预期表现出增加的作用持续时间。

7. 发明申请

WO2007047306A1 METHODS OF TREATING AMYLOIDOSIS USING ARYL-CYCLOPROPYL DERIVATIVE ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译：使用ARYL-CYROPROPYL衍生性ASPARTYL蛋白酶抑制剂治疗淀粉样变性的方法
公开(公告)号：WO2007047306A1
公开(公告)日：2007-04-26
申请号：PCT/US2006/039725
申请日：2006-10-11
申请人： ELAN PHARMACEUTICALS, INC. , HOM, Roy , TOTH, Gergely , PROBST, Gary , BOWERS, Simeon , TRUONG, Anh , TUNG, Jay, S. , NEITZ, R. Jeffrey
发明人： HOM, Roy , TOTH, Gergely , PROBST, Gary , BOWERS, Simeon , TRUONG, Anh , TUNG, Jay, S. , NEITZ, R. Jeffrey
IPC分类号： C07D213/56 , C07D231/12 , C07D405/10 , C07D249/04 , C07C321/26 , C07C233/36 , C07D317/30 , C07D263/32 , C07D277/30 , C07D491/08 , C07D295/14 , C07D403/10 , C07D409/04 , C07D321/06 , C07D209/52
CPC分类号： C07C233/36 , C07C323/31 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/18 , C07C2602/42 , C07D209/52 , C07D213/56 , C07D231/12 , C07D249/04 , C07D261/08 , C07D263/32 , C07D277/28 , C07D277/30 , C07D295/135 , C07D295/155 , C07D307/06 , C07D307/14 , C07D309/04 , C07D309/06 , C07D317/30 , C07D319/12 , C07D321/06 , C07D403/10 , C07D405/10 , C07D409/04 , C07D491/08 , C07D498/18
摘要： The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
摘要翻译：本发明涉及治疗与淀粉样变性相关的疾病，病症和病症的新化合物和方法。淀粉样变性是指与A-β蛋白异常沉积相关的疾病，病症和病症的集合。

8. 发明申请

WO2006010094A1 OXIME DERIVATIVE HYDROXYETHYLAMINE ASPARTYL-PROTEASE INHIBITORS 审中-公开
标题翻译： OXIME衍生的羟基乙酰胺ASPARTYL-PROTEASE抑制剂
公开(公告)号：WO2006010094A1
公开(公告)日：2006-01-26
申请号：PCT/US2005/024468
申请日：2005-07-11
申请人： ELAN PHARMACEUTICALS, INC. , SEALY, Jennifer , HOM, Roy , JOHN, Varghese , PROBST, Gary , TUNG, Jay, S.
发明人： SEALY, Jennifer , HOM, Roy , JOHN, Varghese , PROBST, Gary , TUNG, Jay, S.
IPC分类号： C07C251/32 , C07C233/40 , C07C235/34 , C07D213/40 , C07D311/68 , C07D409/12 , C07D413/12 , C07C233/78
CPC分类号： C07D239/74 , C07C233/36 , C07C237/18 , C07C251/44 , C07C251/54 , C07C251/58 , C07C251/84 , C07C255/31 , C07C255/61 , C07C2601/14 , C07D207/335 , C07D213/40 , C07D213/53 , C07D231/12 , C07D231/56 , C07D239/18 , C07D239/26 , C07D261/20 , C07D307/52 , C07D317/72 , C07D333/22 , C07D403/10 , C07D405/10 , C07D409/04 , C07D409/10
摘要： The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
摘要翻译：本发明涉及治疗与淀粉样变性相关的疾病，病症和病症的新化合物和方法。淀粉样变性是指与A-β蛋白异常沉积相关的疾病，病症和病症的集合。

9. 发明申请

WO2005009344A2 ACYLATED AMINO ACID AMIDYL PYRAZOLES AND RELATED COMPOUNDS 审中-公开
标题翻译：酰胺化氨基亚氨基吡咯及相关化合物
公开(公告)号：WO2005009344A2
公开(公告)日：2005-02-03
申请号：PCT/US2004/018202
申请日：2004-06-04
申请人： ELAN PHARMACEUTICALS, INC. , TUNG, Jay, S. , GAROFALO, Albert , PLEISS, Mike, A.
发明人： TUNG, Jay, S. , GAROFALO, Albert , PLEISS, Mike, A.
IPC分类号： A61K
CPC分类号： C07D231/40 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12
摘要： This invention is directed to acylated amino acid amidyl pyrazoles and related compounds of Formula (I). The invention is also directed to a pharmaceutical formation comprising such compound or in a pharmaceutically acceptable salt form thereof. The invention is further directed to a method for inhibiting ß-amyloid peptide release and/or synthesis, a method for inhibiting γ-secretase activity, and a method for treating neurological disorders associated with ß-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：本发明涉及酰化氨基酸氨基吡唑和式（I）的相关化合物。本发明还涉及包含这种化合物或其药学上可接受的盐形式的药物组合物。本发明还涉及抑制β-淀粉样蛋白肽释放和/或合成的方法，抑制γ-分泌酶活性的方法，以及用于治疗与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）的化合物可用于预防和治疗阿尔茨海默氏病。

10. 发明申请

WO2006010095A2 OXIME DERIVATIVE SUBSTITUTED HYDROXYETHYLAMINE ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： OXIME衍生物取代的羟乙胺天冬氨酸蛋白酶抑制剂
公开(公告)号：WO2006010095A2
公开(公告)日：2006-01-26
申请号：PCT/US2005/024469
申请日：2005-07-11
申请人： ELAN PHARMACEUTICALS INC. , JOHN, Varghese , MAILLARD, Michel , JAGODZINSKA, Barbara , AQUINO, Jose , PROBST, Gary , TUNG, Jay, S.
发明人： JOHN, Varghese , MAILLARD, Michel , JAGODZINSKA, Barbara , AQUINO, Jose , PROBST, Gary , TUNG, Jay, S.
IPC分类号： C07C233/40 , C07C235/34 , C07D209/20 , C07D213/40 , C07D215/42 , C07D311/68 , C07D335/06 , C07D409/12 , C07D413/12 , C07D405/12 , C07D403/12 , C07D207/32 , C07D233/54
CPC分类号： C07D285/08 , C07C233/36 , C07C237/20 , C07C251/44 , C07C251/54 , C07C251/84 , C07C255/42 , C07C255/58 , C07C2601/04 , C07C2601/14 , C07D213/40 , C07D231/12 , C07D231/56 , C07D233/64 , C07D257/04 , C07D261/20 , C07D271/10 , C07D335/06 , C07D405/10
摘要： The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a colletion of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
摘要翻译：本发明涉及治疗与淀粉样变性有关的疾病，病症和病症的新型化合物和方法。淀粉样变性是指收集与A-β蛋白异常沉积相关的疾病，病症和病症。

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