公开(公告)号：US08030328B2

公开(公告)日：2011-10-04

申请号：US11438659

申请日：2006-05-22

Applicant: Frank Stappenbeck ,  Andrei Konradi ,  Jacek Jagodzinski ,  Christopher M. Semko ,  Ying-zi Xu ,  Jenifer L. Smith ,  Kassandra Rossiter

Inventor： Frank Stappenbeck ,  Andrei Konradi ,  Jacek Jagodzinski ,  Christopher M. Semko ,  Ying-zi Xu ,  Jenifer L. Smith ,  Kassandra Rossiter

IPC: A61K31/4166 ,  A61K31/437 ,  C07D235/26 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein the variables A, n, R5, R21-R24 and Q are defined herein. These compounds bind VLA-4. Certain of these compound 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.

Abstract translation: 公开了下式的化合物及其药学上可接受的盐，其中变量A，n，R5，R21-R24和Q在本文中定义。 这些化合物结合VLA-4。 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：US20070142416A1

公开(公告)日：2007-06-21

申请号：US11529815

申请日：2006-09-28

Applicant: Christopher Semko ,  Ying-zi Xu ,  Frank Stappenbeck ,  Jenifer Smith ,  Kassandra Rossiter ,  Juri Fukuda ,  Andrei Konradi

Inventor： Christopher Semko ,  Ying-zi Xu ,  Frank Stappenbeck ,  Jenifer Smith ,  Kassandra Rossiter ,  Juri Fukuda ,  Andrei Konradi

IPC: A61K31/505 ,  C07D403/02 ,  C07D239/50

CPC classification number: C07D403/02 ,  C07D239/50 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

Abstract: 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, 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.

Abstract translation: 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，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：US20070037804A1

公开(公告)日：2007-02-15

申请号：US11438659

申请日：2006-05-22

Applicant: Frank Stappenbeck ,  Andrei Konradi ,  Jacek Jagodzinski ,  Christopher Semko ,  Ying-zi Xu ,  Jenifer Smith ,  Kassandra Rossiter

Inventor： Frank Stappenbeck ,  Andrei Konradi ,  Jacek Jagodzinski ,  Christopher Semko ,  Ying-zi Xu ,  Jenifer Smith ,  Kassandra Rossiter

IPC: A61K31/5377 ,  A61K31/496 ,  A61K31/4745 ,  A61K31/427 ,  A61K31/4184 ,  A61K31/423 ,  C07D471/02

CPC classification number: C07D471/04

Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein the variables A, n, R5, R21—R24 and Q are defined herein. These compounds bind VLA-4. Certain of these compound 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.

Abstract translation: 公开了下式的化合物及其药学上可接受的盐，其中变量A，n，R 5，R 21和R 24和 Q在本文中定义。 这些化合物结合VLA-4。 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：US20070129390A1

公开(公告)日：2007-06-07

申请号：US11541205

申请日：2006-09-28

Applicant: Christopher Semko ,  Ying-zi Xu ,  Frank Stappenbeck ,  Jenifer Smith ,  Kassandra Rossiter ,  Juri Fukuda ,  Andrei Konradi

Inventor： Christopher Semko ,  Ying-zi Xu ,  Frank Stappenbeck ,  Jenifer Smith ,  Kassandra Rossiter ,  Juri Fukuda ,  Andrei Konradi

IPC: A61K31/505 ,  A61K31/4439 ,  A61K31/44 ,  C07D403/02 ,  C07D401/02

CPC classification number: C07D417/12 ,  C07D239/50 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14

Abstract: 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.

Abstract translation: 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：US20070032475A1

公开(公告)日：2007-02-08

申请号：US11398711

申请日：2006-04-06

Applicant: Xiaocong Ye ,  Albert Garofalo ,  Rose Lawler ,  Juri Fukuda ,  Andrei Konradi ,  Ryan Holcomb ,  Kassandra Rossiter ,  David Wone ,  Jing Wu

Inventor： Xiaocong Ye ,  Albert Garofalo ,  Rose Lawler ,  Juri Fukuda ,  Andrei Konradi ,  Ryan Holcomb ,  Kassandra Rossiter ,  David Wone ,  Jing Wu

IPC: A61K31/5513 ,  A61K31/55 ,  A61K31/4709 ,  A61K31/4545 ,  A61K31/454 ,  C07D217/22 ,  C07D211/68

CPC classification number: C07D277/12 ,  C07D209/46 ,  C07D333/40 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/10 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10

Abstract: Disclosed are compounds that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor.

Abstract translation: 公开了缓激肽B 1受体拮抗剂的化合物，并且可用于治疗由缓激肽B 1受体介导的哺乳动物中疾病或与疾病状况相关的不良症状。