公开(公告)号：US20070027131A1

公开(公告)日：2007-02-01

申请号：US11527901

申请日：2006-09-26

Applicant: Andrei Konradi ,  Christopher Semko ,  Ying-zi Xu ,  Frank Stappenbeck ,  Brian Stupi ,  Jenifer Smith ,  Michael Pleiss ,  Eugene Thorsett

Inventor： Andrei Konradi ,  Christopher Semko ,  Ying-zi Xu ,  Frank Stappenbeck ,  Brian Stupi ,  Jenifer Smith ,  Michael Pleiss ,  Eugene Thorsett

IPC: A61K31/506 ,  C07D403/02

CPC classification number: C07D401/12 ,  C07D239/50 ,  C07D403/12

Abstract: 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.

Abstract translation: 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：US20050119290A1

公开(公告)日：2005-06-02

申请号：US10494790

申请日：2003-05-27

Applicant: Andrei Konradi ,  Christopher Semko ,  Ying-Zi Xu ,  Frank Stappenbeck ,  Brian Stupi ,  Jenifer Smith ,  Michael Pleiss ,  Eugene Thorsett

Inventor： Andrei Konradi ,  Christopher Semko ,  Ying-Zi Xu ,  Frank Stappenbeck ,  Brian Stupi ,  Jenifer Smith ,  Michael Pleiss ,  Eugene Thorsett

IPC: C07D239/69 ,  A61K31/505 ,  A61K31/506 ,  A61P19/02 ,  A61P29/00 ,  A61P43/00 ,  C07D239/50 ,  C07D401/12 ,  C07D403/12 ,  C07D43/02

CPC classification number: C07D401/12 ,  C07D239/50 ,  C07D403/12

Abstract: 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.

Abstract translation: 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：US08889860B2

公开(公告)日：2014-11-18

申请号：US13615284

申请日：2012-09-13

Applicant: Brian Stupi ,  Hong Li ,  Weidong Wu ,  Megan N. Hersh ,  David Hertzog ,  Sidney E. Morris ,  Michael L. Metzker

Inventor： Brian Stupi ,  Hong Li ,  Weidong Wu ,  Megan N. Hersh ,  David Hertzog ,  Sidney E. Morris ,  Michael L. Metzker

IPC: C07D487/00 ,  C07D239/02 ,  C07H19/173 ,  C07H19/20 ,  C07H19/14 ,  C12Q1/68 ,  C07H19/073 ,  C07H19/10

CPC classification number: C12Q1/6869 ,  B01L3/5027 ,  B01L2300/0654 ,  B01L2300/168 ,  C07H19/073 ,  C07H19/10 ,  C07H19/14 ,  C07H19/173 ,  C07H19/20 ,  C12Q1/6874 ,  C12Q1/6883 ,  C12Q2525/117 ,  C12Q2600/156 ,  C12Q2600/16

Abstract: The present invention relates generally to 3′-OH unblocked, labeled and unlabeled nucleotides and nucleosides with 5-methoxy-substituted nitrobenzyl-based photocleavable terminating groups for use in methods and systems related to DNA and RNA sequencing and analysis. These compounds, which may be represented by the following formulas: wherein the variables are defined herein, may be used as reversible terminators as they exhibit fast nucleotide incorporation kinetics, single-base termination, high nucleotide selectivity, and rapid terminating group cleavage that results in a naturally occurring nucleotide.

Abstract translation: 本发明一般涉及用于与DNA和RNA测序和分析相关的方法和系统中的5'-甲氧基取代的基于硝基苄基的可光切割终止基团的3'-OH未封闭，标记和未标记的核苷酸和核苷。 可以由下式表示的这些化合物：其中变量在本文中定义，可用作可逆终止子，因为它们表现出快速的核苷酸掺入动力学，单碱基终止，高核苷酸选择性和快速终止基团切割 天然存在的核苷酸。

公开(公告)号：US20130122489A1

公开(公告)日：2013-05-16

申请号：US13615284

申请日：2012-09-13

Applicant: Brian STUPI ,  Hong Li ,  Weidong Wu ,  Megan N. Hersh ,  David Hertzog ,  Sidney E. Morris ,  Michael L. Metzker

Inventor： Brian STUPI ,  Hong Li ,  Weidong Wu ,  Megan N. Hersh ,  David Hertzog ,  Sidney E. Morris ,  Michael L. Metzker

IPC: C12Q1/68 ,  C07H19/10 ,  C07H19/14

CPC classification number: C12Q1/6869 ,  B01L3/5027 ,  B01L2300/0654 ,  B01L2300/168 ,  C07H19/073 ,  C07H19/10 ,  C07H19/14 ,  C07H19/173 ,  C07H19/20 ,  C12Q1/6874 ,  C12Q1/6883 ,  C12Q2525/117 ,  C12Q2600/156 ,  C12Q2600/16

Abstract: The present invention relates generally to 3′-OH unblocked nucleotides and nucleosides labeled and unlabeled with 5-methoxy-substituted nitrobenzyl-based photocleavable terminating groups for use in methods and systems related to DNA and RNA sequencing and analysis. These compounds may be used as reversible terminators as they exhibit fast nucleotide incorporation kinetics, single-base termination, high nucleotide selectivity, and rapid terminating group cleavage that results in a naturally occurring nucleotide.

Abstract translation: 本发明一般涉及用于与DNA和RNA测序和分析相关的方法和系统中使用的5-甲氧基取代的硝基苄基基可光切割终止基团的3'-OH未封闭核苷酸和核苷标记和未标记的核苷。 这些化合物可以用作可逆终止子，因为它们表现出快速的核苷酸掺入动力学，单碱基终止，高核苷酸选择性以及导致天然存在的核苷酸的快速终止基团切割。

公开(公告)号：US20050130999A1

公开(公告)日：2005-06-16

申请号：US10494788

申请日：2003-05-27

Applicant: Andrei Konradi ,  Christopher Semko ,  Ying-zi Xu ,  Frank Stappenbeck ,  Brian Stupi ,  Jenifer Smith ,  Michael Pleiss ,  Eugene Thorsett

Inventor： Andrei Konradi ,  Christopher Semko ,  Ying-zi Xu ,  Frank Stappenbeck ,  Brian Stupi ,  Jenifer Smith ,  Michael Pleiss ,  Eugene Thorsett

IPC: A61K31/505 ,  A61P19/02 ,  A61P29/00 ,  A61P43/00 ,  C07D239/48 ,  C07D239/50

CPC classification number: C07D239/50

Abstract: 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.

Abstract translation: 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。