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31. 发明授权

US07101855B2 Pyroglutamic acid derivatives and related compounds which inhibit leukocyte adhesion mediated by VLA-4 失效
公开(公告)号：US07101855B2
公开(公告)日：2006-09-05
申请号：US10139382
申请日：2002-05-07
申请人： Darren B. Dressen , Anthony Kreft , Dennis Kubrak , Charles William Mann , Michael A. Pleiss , Gary Paul Stack , Eugene D. Thorsett
发明人： Darren B. Dressen , Anthony Kreft , Dennis Kubrak , Charles William Mann , Michael A. Pleiss , Gary Paul Stack , Eugene D. Thorsett
IPC分类号： C07K5/06
CPC分类号： C07K5/06173 , A61K38/00 , C07K5/06139
摘要： Disclosed are pyroglutamic acid derivatives and related 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.

32. 发明授权

US07030114B1 Compounds which inhibit leukocyte adhesion mediated by VLA-4 失效
公开(公告)号：US07030114B1
公开(公告)日：2006-04-18
申请号：US09126096
申请日：1998-07-30
申请人： Eugene D. Thorsett , Christopher M. Semko , Michael A. Pleiss , Andrei W. Konradi , Francine S. Grant , Darren B. Dressen , Reinhardt Bernhard Baudy
发明人： Eugene D. Thorsett , Christopher M. Semko , Michael A. Pleiss , Andrei W. Konradi , Francine S. Grant , Darren B. Dressen , Reinhardt Bernhard Baudy
IPC分类号： C07D207/16 , A61K31/40
CPC分类号： C07K5/06034 , C07K5/06078
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.

33. 发明授权

US06974829B2 Succinoyl aminopyrazoles and related compounds 失效
标题翻译：琥珀酰氨基吡唑及相关化合物
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。

34. 发明授权

US06911439B2 Heteroaryl, heterocyclic and aryl compounds which inhibit leukocyte adhesion mediated by VLA-4 失效
标题翻译：抑制由VLA-4介导的白细胞粘附的杂芳基，杂环和芳基化合物
公开(公告)号：US06911439B2
公开(公告)日：2005-06-28
申请号：US10218366
申请日：2002-08-15
申请人： Andrei W. Konradi , Michael A. Pleiss , Eugene D. Thorsett , Susan Ashwell , Gregory S. Welmaker , Anthony Kreft , Dimitrios Sarntakis , Darren B. Dressen , Francine S. Grant , Christopher Semko , Ying-Zi Xu
发明人： Andrei W. Konradi , Michael A. Pleiss , Eugene D. Thorsett , Susan Ashwell , Gregory S. Welmaker , Anthony Kreft , Dimitrios Sarntakis , Darren B. Dressen , Francine S. Grant , Christopher Semko , Ying-Zi Xu
IPC分类号： C07D239/42 , A61K31/33 , A61K31/38 , A61K31/381 , A61K31/41 , A61K31/415 , A61K31/425 , A61K31/427 , A61K31/433 , A61K31/435 , A61K31/44 , A61K31/4439 , A61K31/445 , A61K31/4468 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/50 , A61K31/505 , A61K31/506 , A61K31/53 , A61K31/535 , A61K31/54 , A61K38/00 , A61P1/00 , A61P3/10 , A61P7/00 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P25/00 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/18 , A61P35/00 , A61P35/04 , A61P37/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D20060101 , C07D211/58 , C07D213/74 , C07D213/76 , C07D231/38 , C07D233/66 , C07D233/88 , C07D237/02 , C07D239/02 , C07D239/46 , C07D239/48 , C07D239/52 , C07D241/20 , C07D249/06 , C07D251/18 , C07D251/48 , C07D251/50 , C07D251/52 , C07D251/54 , C07D257/06 , C07D285/10 , C07D295/22 , C07D333/36 , C07D333/48 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/12 , C07D521/00
CPC分类号： A61K31/425 , A61K31/41 , A61K31/427 , A61K31/433 , A61K31/44 , A61K31/4439 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/50 , A61K31/505 , A61K31/506 , A61K31/53 , A61K31/535 , A61K31/54 , C07D211/58 , C07D213/74 , C07D213/76 , C07D233/88 , C07D239/32 , C07D239/42 , C07D239/47 , C07D239/48 , C07D239/52 , C07D241/20 , C07D249/06 , C07D251/18 , C07D251/48 , C07D251/50 , C07D251/52 , C07D251/54 , C07D257/06 , C07D285/06 , C07D285/10 , C07D333/36 , C07D333/48 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D413/12 , C07D417/12 , Y02A50/463 , A61K2300/00
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。

35. 发明授权

US06900179B2 Carbamyloxy compounds which inhibit leukocyte adhesion mediated by VLA-4 失效
标题翻译：抑制由VLA-4介导的白细胞粘附的氨基甲酰氧基化合物
公开(公告)号：US06900179B2
公开(公告)日：2005-05-31
申请号：US09987619
申请日：2001-11-15
申请人： Eugene D. Thorsett , Christopher M. Semko , Dimitrios Sarantakis , Michael A. Pleiss , Anthony Kreft , Andrei W. Konradi , Francine S. Grant , Darren B. Dressen , Susan Ashwell , Reinhardt Bernhard Baudy , Louis John Lombardo
发明人： Eugene D. Thorsett , Christopher M. Semko , Dimitrios Sarantakis , Michael A. Pleiss , Anthony Kreft , Andrei W. Konradi , Francine S. Grant , Darren B. Dressen , Susan Ashwell , Reinhardt Bernhard Baudy , Louis John Lombardo
IPC分类号： A61K31/397 , A61K31/4015 , A61K31/404 , A61K31/495 , A61K31/54 , A61K38/00 , C07K5/02 , C07K5/06 , C07K5/078
CPC分类号： A61K31/397 , A61K31/4015 , A61K31/404 , A61K31/495 , A61K31/54 , A61K38/00 , C07K5/0215 , C07K5/06026 , C07K5/06139 , C07K5/06165 , C07K5/06191
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，例如哮喘，阿尔茨海默病，动脉粥样硬化，AIDS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）中的炎性疾病。化合物也可以用于治疗炎性脑疾病如多发性硬化症。

36. 发明授权

US06667305B1 Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting &bgr;-amyloid peptide release and/or its synthesis by use of such compounds 失效
公开(公告)号：US06667305B1
公开(公告)日：2003-12-23
申请号：US10336745
申请日：2003-01-06
申请人： Jing Wu , Jay S. Tung , Eugene D. Thorsett , Michael A. Pleiss , Jeffrey S. Nissen , R. Jeffrey Neitz , Lee H. Latimer , Varghese John , Stephen Freedman , Thomas C. Britton , James A. Audia , Jon K. Reel , Thomas E. Mabry , Bruce A. Dressman , Cynthia L. Cwi , James J. Droste , Steven S. Henry , Stacey L. McDaniel , William Leonard Scott , Russell D. Stucky , Warren J. Porter
发明人： Jing Wu , Jay S. Tung , Eugene D. Thorsett , Michael A. Pleiss , Jeffrey S. Nissen , R. Jeffrey Neitz , Lee H. Latimer , Varghese John , Stephen Freedman , Thomas C. Britton , James A. Audia , Jon K. Reel , Thomas E. Mabry , Bruce A. Dressman , Cynthia L. Cwi , James J. Droste , Steven S. Henry , Stacey L. McDaniel , William Leonard Scott , Russell D. Stucky , Warren J. Porter
IPC分类号： A61P2528
CPC分类号： C07D471/04 , A61K31/40 , A61K31/4015 , A61K31/445 , A61K31/5513 , A61K38/05 , C07C237/22 , C07C2603/32 , C07D223/18 , C07D307/33 , C07D311/76 , C07D471/06 , C07D471/08
摘要： Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

37. 发明授权

US06579867B2 Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting &bgr;-amyloid peptide release and/or its synthesis by use of such compounds 失效
公开(公告)号：US06579867B2
公开(公告)日：2003-06-17
申请号：US09915379
申请日：2001-07-27
申请人： Jing Wu , Jay S. Tung , Eugene D. Thorsett , Michael A. Pleiss , Jeffrey S. Nissen , Jeffrey Neitz , Lee H. Latimer , Varghese John , Stephen Freedman , Thomas C. Britton , James A. Audia , Jon K. Reel , Thomas E. Mabry , Bruce A. Dressman , James J. Droste , Steven S. Henry , Stacey L. McDaniel , Russell D. Stucky , Warren J. Porter
发明人： Jing Wu , Jay S. Tung , Eugene D. Thorsett , Michael A. Pleiss , Jeffrey S. Nissen , Jeffrey Neitz , Lee H. Latimer , Varghese John , Stephen Freedman , Thomas C. Britton , James A. Audia , Jon K. Reel , Thomas E. Mabry , Bruce A. Dressman , James J. Droste , Steven S. Henry , Stacey L. McDaniel , Russell D. Stucky , Warren J. Porter
IPC分类号： A61K3155
CPC分类号： C07D471/04 , A61K31/40 , A61K31/4015 , A61K31/445 , A61K31/5513 , A61K38/05 , C07C237/22 , C07C2603/32 , C07D223/18 , C07D307/33 , C07D311/76 , C07D471/06 , C07D471/08
摘要： Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

38. 发明授权

US06492372B1 Heteroaryl, heterocyclic and aryl compounds which inhibit leukocyte adhesion mediated by VLA-4 有权
标题翻译：抑制由VLA-4介导的白细胞粘附的杂芳基，杂环和芳基化合物
公开(公告)号：US06492372B1
公开(公告)日：2002-12-10
申请号：US09489377
申请日：2000-01-21
申请人： Andrei W. Konradi , Michael A. Pleiss , Eugene D. Thorsett , Susan Ashwell , Gregory S. Welmaker , Anthony Kreft , Dimitrios Sarantakis , Darren B. Dressen , Francine S. Grant , Christopher Semko , Ying-Zi Xu
发明人： Andrei W. Konradi , Michael A. Pleiss , Eugene D. Thorsett , Susan Ashwell , Gregory S. Welmaker , Anthony Kreft , Dimitrios Sarantakis , Darren B. Dressen , Francine S. Grant , Christopher Semko , Ying-Zi Xu
IPC分类号： A61K3133
CPC分类号： A61K31/425 , A61K31/41 , A61K31/427 , A61K31/433 , A61K31/44 , A61K31/4439 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/50 , A61K31/505 , A61K31/506 , A61K31/53 , A61K31/535 , A61K31/54 , C07D211/58 , C07D213/74 , C07D213/76 , C07D233/88 , C07D239/32 , C07D239/42 , C07D239/47 , C07D239/48 , C07D239/52 , C07D241/20 , C07D249/06 , C07D251/18 , C07D251/48 , C07D251/50 , C07D251/52 , C07D251/54 , C07D257/06 , C07D285/06 , C07D285/10 , C07D333/36 , C07D333/48 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D413/12 , C07D417/12 , Y02A50/463 , A61K2300/00
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。

39. 发明授权

US06465513B1 Multicyclic compounds which inhibit leukocyte adhesion mediated by VLA-4 有权
标题翻译：抑制由VLA-4介导的白细胞粘附的多环化合物
公开(公告)号：US06465513B1
公开(公告)日：2002-10-15
申请号：US09489157
申请日：2000-01-21
申请人： Francine S. Grant , Bradley S. Johnson , Michael A. Pleiss , Eugene D. Thorsett
发明人： Francine S. Grant , Bradley S. Johnson , Michael A. Pleiss , Eugene D. Thorsett
IPC分类号： A01N3700
CPC分类号： C07C233/84 , C07C233/63 , C07C233/85 , C07C233/87 , C07C237/22 , C07C255/60 , C07C271/22 , C07C271/34 , C07C271/42 , C07C271/44 , C07C275/16 , C07C275/18 , C07C275/20 , C07C275/24 , C07C2601/14 , C07C2603/74 , C07D213/55 , C07D213/64 , C07D213/80 , C07D213/89 , C07D239/52 , C07D239/54 , C07D261/08 , C07D277/48 , C07D295/15 , C07D295/205 , C07D453/02
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。

40. 发明授权

US06410781B1 &agr;-aminoacetic acid derivatives-&agr;4&bgr;7 receptor antagonists 失效
标题翻译： α-氨基乙酸衍生物-α4β7受体拮抗剂
公开(公告)号：US06410781B1
公开(公告)日：2002-06-25
申请号：US09514773
申请日：2000-02-28
申请人： Andrei W. Konradi , Michael A. Pleiss , Eugene D. Thorsett
发明人： Andrei W. Konradi , Michael A. Pleiss , Eugene D. Thorsett
IPC分类号： C07C27144
CPC分类号： C07D295/205 , C07C271/44 , C07C2601/14 , C07D213/56 , C07D263/24
摘要： Disclosed are compounds which bind &agr;4&bgr;7 integrin. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by &agr;4&bgr;7 integrin. 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α4β7整联蛋白的化合物。这些化合物中的某些也抑制白细胞粘附，特别是由α4β7整联蛋白介导的白细胞粘附。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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