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1. 发明申请

US20100160341A1 HETEROARYL, HETEROCYCLIC AND ARYL COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 失效
标题翻译：由VLA-4介导的抑制白云石粘合剂的杂环，杂环和芳基化合物
公开(公告)号：US20100160341A1
公开(公告)日：2010-06-24
申请号：US12645154
申请日：2009-12-22
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： A61K31/496 , A61K31/505 , A61K31/506 , A61P1/00 , A61K31/41
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。

2. 发明授权

US07166580B2 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化合物
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。

3. 发明授权

US07053220B2 Hydroxyalkanoyl aminopyrazoles and related compounds 失效
标题翻译：羟基烷酰基氨基吡唑及其相关化合物
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。

4. 发明授权

US06949570B2 Compounds which inhibit leukocyte adhesion mediated by VLA-4 失效
公开(公告)号：US06949570B2
公开(公告)日：2005-09-27
申请号：US10139370
申请日：2002-05-07
申请人： Susan Ashwell , Reinhardt Bernhard Baudy , Michael A. Pleiss , Dimitrios Sarantakis , Eugene D. Thorsett
发明人： Susan Ashwell , Reinhardt Bernhard Baudy , Michael A. Pleiss , Dimitrios Sarantakis , Eugene D. Thorsett
IPC分类号： A61K38/00 , C07D207/48 , C07D401/12 , C07D403/04 , C07K5/06 , C07K5/065 , A61K31/445 , A61K31/40 , C07D207/46 , C07D257/00 , C07D401/00
CPC分类号： C07D207/48 , A61K38/00 , C07D401/12 , C07D403/04 , C07K5/06026 , 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.

5. 发明授权

US06689781B2 Phenylalanine derivatives as alpha 4 integrin inhibitors 失效
标题翻译：苯丙氨酸衍生物作为α4整联蛋白抑制剂
公开(公告)号：US06689781B2
公开(公告)日：2004-02-10
申请号：US09910685
申请日：2001-07-20
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： C07D23942
CPC分类号： C07D239/42
摘要： Disclosed are a series of phenylalanine derivatives, to compositions containing them, to processes for their preparation, and to their use in medicine.
摘要翻译：公开了一系列苯丙氨酸衍生物，含有它们的组合物，其制备方法及其在医药中的应用。

6. 发明授权

US06545160B2 &agr;aminocetic acid derivatives- &agr;4&bgr;7 receptor antagonists 失效
标题翻译： α-氨基酸衍生物-α4β7受体拮抗剂
公开(公告)号：US06545160B2
公开(公告)日：2003-04-08
申请号：US10147884
申请日：2002-05-20
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： C07D26306
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。

7. 发明授权

US06518424B1 Substituted pyrimidine compositions and methods of use 失效
标题翻译：取代的嘧啶组合物和使用方法
公开(公告)号：US06518424B1
公开(公告)日：2003-02-11
申请号：US09438103
申请日：1999-11-10
申请人： Varghese John , Russell E. Rydel , Michael S. Dappen , Eugene D. Thorsett
发明人： Varghese John , Russell E. Rydel , Michael S. Dappen , Eugene D. Thorsett
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。

8. 发明授权

US06506782B1 Heterocyclic compounds, pharmaceutical compositions comprising same, and methods for inhibiting &bgr;-amyloid peptide release and/or its synthesis by use of such compounds 失效
标题翻译：杂环化合物，包含其的药物组合物，以及通过使用这些化合物抑制β-淀粉样蛋白肽释放和/或其合成的方法
公开(公告)号：US06506782B1
公开(公告)日：2003-01-14
申请号：US09032019
申请日：1998-02-27
申请人： Eugene D. Thorsett , Warren J. Porter , Jeffrey S. Nissen , Lee H. Latimer , James E. Audia , James Droste
发明人： Eugene D. Thorsett , Warren J. Porter , Jeffrey S. Nissen , Lee H. Latimer , James E. Audia , James Droste
IPC分类号： A61K314245
CPC分类号： A61K31/4245
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.
摘要翻译：公开了抑制β-淀粉样蛋白肽释放和/或其合成的化合物，因此具有治疗阿尔茨海默病的效用。还公开了包含抑制β-淀粉样蛋白肽释放和/或其合成的化合物的药物组合物以及用这种药物组合物预防性和治疗性地治疗阿尔茨海默病的方法。

9. 发明授权

US06495693B2 N-(aryl/heteroaryl) amino acid derivatives, pharmaceutical compositions comprising same, and methods for inhibiting &bgr;-amyloid peptide release and/or its synthesis by use of such compounds 失效
标题翻译： N-（芳基/杂芳基）氨基酸衍生物，包含其的药物组合物，以及通过使用这些化合物抑制β-淀粉样蛋白肽释放和/或其合成的方法
公开(公告)号：US06495693B2
公开(公告)日：2002-12-17
申请号：US09280966
申请日：1999-03-30
申请人： James E. Audia , Beverly K. Folmer , Varghese John , Lee H. Latimer , Jeffrey S. Nissen , Warren J. Porter , Eugene D. Thorsett , Jing Wu
发明人： James E. Audia , Beverly K. Folmer , Varghese John , Lee H. Latimer , Jeffrey S. Nissen , Warren J. Porter , Eugene D. Thorsett , Jing Wu
IPC分类号： C07D27782
CPC分类号： C07D215/38 , A61K31/00 , A61K31/198 , A61K31/223 , C07C237/08 , C07C237/10 , C07C237/12 , C07C271/22 , C07D209/20 , C07D233/64 , C07D277/62 , C07D277/82
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.
摘要翻译：公开了抑制β-淀粉样蛋白肽释放和/或其合成的化合物，因此具有治疗阿尔茨海默病的效用。还公开了包含抑制β-淀粉样蛋白肽释放和/或其合成的化合物的药物组合物以及用这种药物组合物预防性和治疗性地治疗阿尔茨海默病的方法。

10. 发明授权

US06489300B1 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：US06489300B1
公开(公告)日：2002-12-03
申请号：US09126958
申请日：1998-07-31
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： C07K5078
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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