公开(公告)号：US06492421B1

公开(公告)日：2002-12-10

申请号：US09126095

申请日：1998-07-30

申请人： Eugene D. Thorsett ,  Christopher M. Semko ,  Dimitrios Sarantakis ,  Michael A. Pleiss ,  Louis John Lombardo ,  Anthony Kreft ,  Andrei W. Konradi ,  Francine S. Grant ,  Darren B. Dressen ,  Michael S. Dappen ,  Reinhardt Bernhard Baudy ,  Susan Ashwell

发明人： Eugene D. Thorsett ,  Christopher M. Semko ,  Dimitrios Sarantakis ,  Michael A. Pleiss ,  Louis John Lombardo ,  Anthony Kreft ,  Andrei W. Konradi ,  Francine S. Grant ,  Darren B. Dressen ,  Michael S. Dappen ,  Reinhardt Bernhard Baudy ,  Susan Ashwell

IPC分类号： A61K3119

CPC分类号： C07K5/06165 ,  C07K5/0823

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。

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。

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.

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。

公开(公告)号：US06436904B1

公开(公告)日：2002-08-20

申请号：US09489589

申请日：2000-01-21

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： A61K3805

CPC分类号： C07D207/48 ,  A61K38/00 ,  C07D401/12 ,  C07D403/04 ,  C07K5/06026 ,  C07K5/06078

摘要： Disclosed are compounds which bind VAL-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VAL-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：US07320960B2

公开(公告)日：2008-01-22

申请号：US10316205

申请日：2002-12-11

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： C07K5/06

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。

公开(公告)号：US06525026B2

公开(公告)日：2003-02-25

申请号：US09987900

申请日：2001-11-16

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： C07K506

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.

公开(公告)号：US06583139B1

公开(公告)日：2003-06-24

申请号：US09688820

申请日：2000-10-17

申请人： Eugene D. Thorsett ,  Christopher M. Semko ,  Michael A. Pleiss ,  Anthony Kreft ,  Andrei W. Konradi ,  Francine S. Grant ,  Reinhardt Bernhard Baudy ,  Dimitrios Sarantakis

发明人： Eugene D. Thorsett ,  Christopher M. Semko ,  Michael A. Pleiss ,  Anthony Kreft ,  Andrei W. Konradi ,  Francine S. Grant ,  Reinhardt Bernhard Baudy ,  Dimitrios Sarantakis

IPC分类号： A61K3154

CPC分类号： C07K14/001 ,  A61K31/401 ,  A61K31/4172 ,  A61K38/00 ,  C07K14/195

摘要： Disclosed as 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：US07973044B2

公开(公告)日：2011-07-05

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： A01N43/54 ,  C07D239/42

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：US07745454B2

公开(公告)日：2010-06-29

申请号：US10936070

申请日：2004-09-07

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. Farouz ,  Christopher M. 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. Farouz ,  Christopher M. Semko ,  Ying-Zi Xu

IPC分类号： A61K31/505 ,  A61K31/515 ,  C07D239/22 ,  C07D239/42 ,  A61P19/02 ,  A61P11/06 ,  A61P37/08

CPC分类号： C07D401/12 ,  C07D239/48 ,  C07D239/52 ,  C07D417/12

摘要： Disclosed are certain alpha amino acid 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的某些α氨基酸化合物。 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。