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41. 发明授权

US06911439B2 Heteroaryl, heterocyclic and aryl compounds which inhibit leukocyte adhesion mediated by VLA-4 失效
标题翻译：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：US06911439B2
公开(公告)日：2005-06-28
申请号：US10218366
申请日：2002-08-15
申请人： Andrei W. Konradi , Michael A. Pleiss , Eugene D. Thorsett , Susan Ashwell , Gregory S. Welmaker , Anthony Kreft , Dimitrios Sarntakis , 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 Sarntakis , Darren B. Dressen , Francine S. Grant , Christopher Semko , Ying-Zi Xu
IPC分类号： C07D239/42 , A61K31/33 , A61K31/38 , A61K31/381 , A61K31/41 , A61K31/415 , A61K31/425 , A61K31/427 , A61K31/433 , A61K31/435 , A61K31/44 , A61K31/4439 , A61K31/445 , A61K31/4468 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/50 , A61K31/505 , A61K31/506 , A61K31/53 , A61K31/535 , A61K31/54 , A61K38/00 , A61P1/00 , A61P3/10 , A61P7/00 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P25/00 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/18 , A61P35/00 , A61P35/04 , A61P37/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D20060101 , C07D211/58 , C07D213/74 , C07D213/76 , C07D231/38 , C07D233/66 , C07D233/88 , C07D237/02 , C07D239/02 , C07D239/46 , C07D239/48 , C07D239/52 , C07D241/20 , C07D249/06 , C07D251/18 , C07D251/48 , C07D251/50 , C07D251/52 , C07D251/54 , C07D257/06 , C07D285/10 , C07D295/22 , C07D333/36 , C07D333/48 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/12 , C07D521/00
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。

42. 发明授权

US06900179B2 Carbamyloxy compounds which inhibit leukocyte adhesion mediated by VLA-4 失效
标题翻译：抑制由VLA-4介导的白细胞粘附的氨基甲酰氧基化合物
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。

43. 发明授权

US06492372B1 Heteroaryl, heterocyclic and aryl compounds which inhibit leukocyte adhesion mediated by VLA-4 有权
标题翻译：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：US06492372B1
公开(公告)日：2002-12-10
申请号：US09489377
申请日：2000-01-21
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： A61K3133
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。

44. 发明授权

US06465513B1 Multicyclic compounds which inhibit leukocyte adhesion mediated by VLA-4 有权
标题翻译：抑制由VLA-4介导的白细胞粘附的多环化合物
公开(公告)号：US06465513B1
公开(公告)日：2002-10-15
申请号：US09489157
申请日：2000-01-21
申请人： Francine S. Grant , Bradley S. Johnson , Michael A. Pleiss , Eugene D. Thorsett
发明人： Francine S. Grant , Bradley S. Johnson , Michael A. Pleiss , Eugene D. Thorsett
IPC分类号： A01N3700
CPC分类号： C07C233/84 , C07C233/63 , C07C233/85 , C07C233/87 , C07C237/22 , C07C255/60 , C07C271/22 , C07C271/34 , C07C271/42 , C07C271/44 , C07C275/16 , C07C275/18 , C07C275/20 , C07C275/24 , C07C2601/14 , C07C2603/74 , C07D213/55 , C07D213/64 , C07D213/80 , C07D213/89 , C07D239/52 , C07D239/54 , C07D261/08 , C07D277/48 , C07D295/15 , C07D295/205 , C07D453/02
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。

45. 发明授权

US06410781B1 &agr;-aminoacetic acid derivatives-&agr;4&bgr;7 receptor antagonists 失效
标题翻译： α-氨基乙酸衍生物-α4β7受体拮抗剂
公开(公告)号：US06410781B1
公开(公告)日：2002-06-25
申请号：US09514773
申请日：2000-02-28
申请人： Andrei W. Konradi , Michael A. Pleiss , Eugene D. Thorsett
发明人： Andrei W. Konradi , Michael A. Pleiss , Eugene D. Thorsett
IPC分类号： C07C27144
CPC分类号： C07D295/205 , C07C271/44 , C07C2601/14 , C07D213/56 , C07D263/24
摘要： Disclosed are compounds which bind &agr;4&bgr;7 integrin. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by &agr;4&bgr;7 integrin. 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α4β7整联蛋白的化合物。这些化合物中的某些也抑制白细胞粘附，特别是由α4β7整联蛋白介导的白细胞粘附。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。

46. 发明授权

US08716296B2 Inhibitors of protein kinases 失效
标题翻译：蛋白激酶抑制剂
公开(公告)号：US08716296B2
公开(公告)日：2014-05-06
申请号：US12226286
申请日：2008-10-13
申请人： Hans Allgeier , Martin Augustin , Anke Müller , Lutz Zeitlmann , Andreas Marquardt , Michael A. Pleiss , Ulrich Heiser , André Johannes Niestroj
发明人： Hans Allgeier , Martin Augustin , Anke Müller , Lutz Zeitlmann , Andreas Marquardt , Michael A. Pleiss , Ulrich Heiser , André Johannes Niestroj
IPC分类号： A01N43/54 , C07D401/00
CPC分类号： C07D403/12 , C07D239/42 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D487/04
摘要： Compounds of general formula (I): are useful as inhibitors of cyclin dependent kinases such as CDK9.
摘要翻译：通式（I）的化合物：可用作细胞周期依赖性激酶如CDK9的抑制剂。

47. 发明授权

US08263063B2 Multimeric VLA-4 antagonists comprising polymer moieties 失效
标题翻译：包含聚合物部分的多聚VLA-4拮抗剂
公开(公告)号：US08263063B2
公开(公告)日：2012-09-11
申请号：US12877496
申请日：2010-09-08
申请人： Andrei W. Konradi , Michael A. Pleiss , Christopher M. Semko , Theodore Yednock , Jenifer L. Smith
发明人： Andrei W. Konradi , Michael A. Pleiss , Christopher M. Semko , Theodore Yednock , Jenifer L. Smith
IPC分类号： A61K31/74
CPC分类号： A61K45/06 , A61K31/785 , A61K47/60 , A61Q5/00
摘要： Disclosed are conjugates exhibiting VLA-4 antagonistic properties. Certain of these conjugates also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. The conjugates of this invention are characterized as containing more than one VLA-4 inhibiting compound covalently attached to a bio-compatible polymer, such as polyethylene glycol. Conjugates of the invention are defined by formula I, wherein A, B, and q are described in the specification. Such conjugates 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 conjugates can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
摘要翻译：公开了表现出VLA-4拮抗性质的缀合物。这些缀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。本发明的缀合物的特征在于含有多于一种共价连接到生物相容性聚合物如聚乙二醇的VLA-4抑制化合物。本发明的缀合物由式I定义，其中A，B和q在说明书中描述。这样的缀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，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）中的炎性疾病。也可以将缀合物用于治疗炎性脑疾病如多发性硬化症。

48. 发明申请

US20120076831A1 COMPOSITIONS AND METHODS FOR INDUCTION OF ANTIGEN-SPECIFIC TOLERANCE 审中-公开
标题翻译：用于诱导抗原特异性耐受性的组合物和方法
公开(公告)号：US20120076831A1
公开(公告)日：2012-03-29
申请号：US13144918
申请日：2010-01-20
申请人： Stephen Miller , Russell L. Bromley , Michael A. Pleiss , Daniel Getts , Aaron Martin
发明人： Stephen Miller , Russell L. Bromley , Michael A. Pleiss , Daniel Getts , Aaron Martin
IPC分类号： A61K39/00 , A61P37/02 , A61P29/00 , A61P11/06 , A61P25/00 , A61P3/10 , A61K9/14 , A61P37/08 , B82Y5/00
CPC分类号： A61K39/0008 , A61K9/127 , A61K47/58 , A61K47/593 , A61K47/595 , A61K47/6911 , A61K47/6915 , A61K47/6921 , A61K2039/55555 , A61K2039/6093
摘要： The present invention utilizes carrier particles to present antigen peptides and proteins to the immune system in such a way as to induce antigen specific tolerance. The carrier particle is designed in order to trigger an immune tolerance effect. The invention is useful for treatment of immune related disorders such as autoimmune disease, transplant rejection and allergic reactions.
摘要翻译：本发明利用载体颗粒以抗原特异性耐受性的方式将抗原肽和蛋白质提供给免疫系统。设计载体颗粒以引发免疫耐受效应。本发明可用于治疗免疫相关疾病，例如自身免疫性疾病，移植排斥反应和过敏反应。

49. 发明申请

US20110306602A1 4, 6-DISUBSTITUTED AMINOPYRIMIDINE DERIVATIVES AS INHIBITORS OF PROTEIN KINASES 失效
标题翻译：作为蛋白激酶抑制剂的4,6-取代的氨基嘧啶衍生物
公开(公告)号：US20110306602A1
公开(公告)日：2011-12-15
申请号：US12451039
申请日：2008-04-24
申请人： Philipp Wabnitz , Heike Schauerte , Hans Allgeier , Lutz Zeitlmann , Anke Mueller , Martin Augustin , Michael A. Pleiss , Gabriele Stumm , Axel Choidas , Bert Klebl , Gerhard Mueller , Wilfried Schwab , Joelle Le , Jackie Macritchie , Don Simpson
发明人： Philipp Wabnitz , Heike Schauerte , Hans Allgeier , Lutz Zeitlmann , Anke Mueller , Martin Augustin , Michael A. Pleiss , Gabriele Stumm , Axel Choidas , Bert Klebl , Gerhard Mueller , Wilfried Schwab , Joelle Le , Jackie Macritchie , Don Simpson
IPC分类号： A61K31/55 , C07D405/12 , C07D409/12 , C07D401/12 , C07D413/12 , C07D403/12 , C07D417/12 , C07D401/10 , C07D413/10 , C07D403/10 , A61K31/505 , A61K31/5377 , A61K31/541 , A61K31/506 , A61P29/00 , A61P37/00 , A61P35/00 , A61P31/00 , A61P9/00 , A61P25/28 , C07D239/42
CPC分类号： C07D239/42 , C07D239/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to inhibitors of general Formula (I) of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to compounds for preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases.
摘要翻译：本发明涉及细胞周期蛋白依赖性激酶的通式（I）的抑制剂及其治疗应用。此外，本发明涉及用于预防和/或治疗任何类型的疼痛，炎症性疾病，免疫疾病，增殖性疾病，感染性疾病，心血管疾病和神经变性疾病的化合物。

50. 发明授权

US07968547B2 Heteroaryl, heterocyclic and aryl compounds which inhibit leukocyte adhesion mediated by VLA-4 失效
标题翻译：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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