公开(公告)号：US07452912B2

公开(公告)日：2008-11-18

申请号：US10316189

申请日：2002-12-11

申请人： Francine S. Grant ,  Andrei W. Konradi ,  Michael A. Pleiss ,  Eugene D. Thorsett

发明人： Francine S. Grant ,  Andrei W. Konradi ,  Michael A. Pleiss ,  Eugene D. Thorsett

IPC分类号： A61P29/00 ,  A61P19/02 ,  A61K31/415 ,  C07D235/16 ,  C07D235/26

CPC分类号： C07D263/58 ,  C07D235/30 ,  C07D239/94 ,  C07D239/95 ,  C07D277/82

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。

公开(公告)号：US07049306B2

公开(公告)日：2006-05-23

申请号：US10251442

申请日：2002-09-20

申请人： Andrei W. Konradi ,  Michael A. Pleiss ,  Eugene D. Thorsett ,  Darren B. Dressen ,  Francine S. Grant ,  Christopher Semko ,  Ying-Zi Xu

发明人： Andrei W. Konradi ,  Michael A. Pleiss ,  Eugene D. Thorsett ,  Darren B. Dressen ,  Francine S. Grant ,  Christopher Semko ,  Ying-Zi Xu

IPC分类号： A61K31/313 ,  A61K31/4985 ,  C07D241/00 ,  C07D242/02

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.

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。

公开(公告)号：US07005433B2

公开(公告)日：2006-02-28

申请号：US10748089

申请日：2003-12-29

申请人： Andrei W. Konradi ,  Michael A. Pleiss ,  Eugene D. Thorsett ,  Darren B. Dressen ,  Francine S. Grant ,  Christopher Semko ,  Ying-Zi Xu

发明人： Andrei W. Konradi ,  Michael A. Pleiss ,  Eugene D. Thorsett ,  Darren B. Dressen ,  Francine S. Grant ,  Christopher Semko ,  Ying-Zi Xu

IPC分类号： C07D239/42 ,  C07D239/48 ,  A61K31/505

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.

公开(公告)号：US07335663B2

公开(公告)日：2008-02-26

申请号：US10494788

申请日：2003-05-27

申请人： Andrei W. Konradi ,  Christopher M. Semko ,  Ying-zi Xu ,  Frank Stappenbeck ,  Brian P. Stupi ,  Jenifer Smith ,  Michael A. Pleiss ,  Eugene D. Thorsett

发明人： Andrei W. Konradi ,  Christopher M. Semko ,  Ying-zi Xu ,  Frank Stappenbeck ,  Brian P. Stupi ,  Jenifer Smith ,  Michael A. Pleiss ,  Eugene D. Thorsett

IPC分类号： A01N43/54

CPC分类号： C07D239/50

摘要： Disclosed are compounds which bind α4 integrins, where the α4 integrin is preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by α4 integrins, where the α4 integrin is preferably 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α4+整联蛋白的化合物，其中α4+整联蛋白优选为VLA-4。 这些化合物中的某些还抑制白细胞粘附，特别是由α4H整联蛋白介导的白细胞粘附，其中α4整联蛋白优选为VLA-4。 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。

公开(公告)号：US07026328B2

公开(公告)日：2006-04-11

申请号：US10447308

申请日：2003-05-27

申请人： Andrei W. Konradi ,  Christopher M. Semko ,  Ying-zi Xu ,  Frank Stappenbeck ,  Brian P. Stupl ,  Jenifer L. Smith ,  Michael A. Pleiss ,  Eugene D. Thorsett

发明人： Andrei W. Konradi ,  Christopher M. Semko ,  Ying-zi Xu ,  Frank Stappenbeck ,  Brian P. Stupl ,  Jenifer L. Smith ,  Michael A. Pleiss ,  Eugene D. Thorsett

IPC分类号： C07D239/50 ,  A61K31/505

CPC分类号： C07D401/12 ,  C07D239/50 ,  C07D403/12

摘要： Disclosed are compounds which bind α4 integrins, preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by α4 integrins, preferably 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.

公开(公告)号：US07427628B2

公开(公告)日：2008-09-23

申请号：US11527901

申请日：2006-09-26

申请人： Andrei W. Konradi ,  Christopher M. Semko ,  Ying-zi Xu ,  Frank Stappenbeck ,  Brian P. Stupi ,  Jenifer Smith ,  Michael A. Pleiss ,  Eugene D. Thorsett

发明人： Andrei W. Konradi ,  Christopher M. Semko ,  Ying-zi Xu ,  Frank Stappenbeck ,  Brian P. Stupi ,  Jenifer Smith ,  Michael A. Pleiss ,  Eugene D. Thorsett

IPC分类号： A61K31/505 ,  A61P19/02 ,  A61P25/00 ,  C07D239/50

CPC分类号： C07D401/12 ,  C07D239/50 ,  C07D403/12

摘要： Disclosed are compounds which bind α4 integrins, preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by α4 integrins, preferably 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α4+整联蛋白，优选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α4A整联蛋白（优选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。

公开(公告)号：US07135477B2

公开(公告)日：2006-11-14

申请号：US10494790

申请日：2003-05-27

申请人： Andrei W. Konradi ,  Christopher M. Semko ,  Ying-zi Xu ,  Frank Stappenbeck ,  Brian P. Stupi ,  Jenifer Smith ,  Michael A. Pleiss ,  Eugene D. Thorsett

发明人： Andrei W. Konradi ,  Christopher M. Semko ,  Ying-zi Xu ,  Frank Stappenbeck ,  Brian P. Stupi ,  Jenifer Smith ,  Michael A. Pleiss ,  Eugene D. Thorsett

IPC分类号： A61K31/505 ,  A61P19/02 ,  C07D239/50

CPC分类号： C07D401/12 ,  C07D239/50 ,  C07D403/12

摘要： Disclosed are compounds which bind α4 integrins, preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by α4 integrins, preferably 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α4+整联蛋白，优选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α4A整联蛋白（优选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。

公开(公告)号：US07008949B2

公开(公告)日：2006-03-07

申请号：US10447208

申请日：2003-05-27

申请人： Andrei W. Konradi ,  Christopher M. Semko ,  Ying-zi Xu ,  Frank Stappenbeck ,  Brian P. Stupi ,  Jenifer L. Smith ,  Michael A. Pleiss ,  Eugene D. Thorsett

发明人： Andrei W. Konradi ,  Christopher M. Semko ,  Ying-zi Xu ,  Frank Stappenbeck ,  Brian P. Stupi ,  Jenifer L. Smith ,  Michael A. Pleiss ,  Eugene D. Thorsett

IPC分类号： C07D239/50 ,  A61K31/505

CPC分类号： C07D239/50

摘要： Disclosed are compounds which bind α4 integrins, where the α4 integrin is preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by α4 integrins, where the α4 integrin is preferably 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α4+整联蛋白的化合物，其中α4+整联蛋白优选为VLA-4。 这些化合物中的某些还抑制白细胞粘附，特别是由α4H整联蛋白介导的白细胞粘附，其中α4整联蛋白优选为VLA-4。 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。

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。

公开(公告)号：US06423688B1

公开(公告)日：2002-07-23

申请号：US09126329

申请日：1998-07-31

申请人： Eugene D. Thorsett ,  Christopher M. Semko ,  Michael A. Pleiss ,  Louis John Lombardo ,  Francine S. Grant ,  Darren B. Dressen ,  Michael S. Dappen

发明人： Eugene D. Thorsett ,  Christopher M. Semko ,  Michael A. Pleiss ,  Louis John Lombardo ,  Francine S. Grant ,  Darren B. Dressen ,  Michael S. Dappen

IPC分类号： C07K5078

CPC分类号： C07K5/06026 ,  A61K38/00 ,  C07K5/06104 ,  C07K5/06139 ,  C07K5/06165

摘要： Disclosed are compounds which bind VLA-4. Certain of these compounds aslo 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化合物抑制白细胞粘附，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。