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1.发明申请PYRIMIDINYL SULFONAMIDE COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 有权VLA-4介导的抑制白蛋白粘合的吡咯烷酮磺酰胺化合物公开(公告)号：US20100016345A1
公开(公告)日：2010-01-21
申请号：US12505383
申请日：2009-07-17
IPC分类号： A61K31/506 , A61P11/06 , A61P19/02
CPC分类号： C07D239/50
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 human or animal subject such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, Crohn's 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。 此类化合物可用于治疗人或动物受试者如哮喘，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，克罗恩病，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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2.发明授权Pyrimidinyl sulfonamide 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嘧啶基磺酰胺化合物公开(公告)号：US07579466B2
公开(公告)日：2009-08-25
申请号：US11679042
申请日：2007-02-26
IPC分类号： C07D239/50 , C07D403/12 , A61K31/506 , A61P19/02
CPC分类号： C07D239/50
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 human or animal subject such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, Crohn's 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。 此类化合物可用于治疗人或动物受试者如哮喘，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，克罗恩病，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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3.发明申请HETEROARYL, HETEROCYCLIC AND ARYL COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 失效由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。
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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。
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5.发明授权Heteroaryl, heterocyclic and aryl 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杂芳基，杂环和芳基化合物公开(公告)号：US07968547B2
公开(公告)日：2011-06-28
申请号：US12637719
申请日：2009-12-14
申请人： Andrei W. Konradi , Michael A. Pleiss , Eugene D. Thorsett , Darren B. Dressen , Francine S. Grant , Christopher Semko , Ying-Zi Xu , Susan Ashwell , Gregory S. Welmaker , Anthony Kreft , Dimitrios Sarantakis
发明人： Andrei W. Konradi , Michael A. Pleiss , Eugene D. Thorsett , Darren B. Dressen , Francine S. Grant , Christopher Semko , Ying-Zi Xu , Susan Ashwell , Gregory S. Welmaker , Anthony Kreft , Dimitrios Sarantakis
IPC分类号： C07D241/02 , A61K31/497
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。
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6.发明申请公开(公告)号：US20100160343A1
公开(公告)日：2010-06-24
申请号：US12637719
申请日：2009-12-14
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： A61K31/4965 , C07D241/20 , A61P19/02
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.
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7.发明授权3-(heteroaryl) alanine derivatives-inhibitors of leukocyte adhesion mediated by VLA-4 失效3-（杂芳基）丙氨酸衍生物 - 由VLA-4介导的白细胞粘附抑制剂公开(公告)号：US07365073B2
公开(公告)日：2008-04-29
申请号：US10898576
申请日：2004-07-23
申请人： Andrei W. Konradi , Michael A. Pleiss , Eugene D. Thorsett , Darren B. Dressen , Francine S. Farouz , Christopher Semko , Ying-Zi Xu , Frank Stappenbeck
发明人： Andrei W. Konradi , Michael A. Pleiss , Eugene D. Thorsett , Darren B. Dressen , Francine S. Farouz , Christopher Semko , Ying-Zi Xu , Frank Stappenbeck
IPC分类号： A61K31/497 , C07D401/12 , C07D403/12
CPC分类号： C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/14 , C07D417/14
摘要： Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit 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并抑制由VLA-4介导的白细胞粘附的某些3-（杂芳基）丙氨酸衍生物。 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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公开(公告)号：US07291645B2
公开(公告)日：2007-11-06
申请号：US10735499
申请日：2003-12-12
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： A01N47/10 , A61K31/27 , A07C261/00 , A07C269/00 , A07C271/00
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。
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公开(公告)号：US07015216B2
公开(公告)日：2006-03-21
申请号：US09910431
申请日：2001-07-19
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： C07D213/02 , C07D213/30 , C07D403/06 , A61K31/44 , A61P19/02
CPC分类号： C07D213/81 , C07D251/46 , C07D401/12 , C07D409/12 , C07D413/12
摘要： Disclosed are a series of heteroaryl-β-alanine derivatives, compositions containing them, processes for their preparation and their use in medicine.
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10.发明授权Heteroaryl, heterocyclic and aryl 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杂芳基，杂环和芳基化合物公开(公告)号：US07378529B2
公开(公告)日：2008-05-27
申请号：US11033079
申请日：2005-01-10
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： C07D285/10 , C07D271/00 , A01N43/64 , 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。
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