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1.发明授权Alpha amino acid derivatives-inhibitors of leukocyte adhesion mediated by VLA-4 有权α氨基酸衍生物 - 由VLA-4介导的白细胞粘附抑制剂公开(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。
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2.发明授权3-(heteroaryl) alanine derivatives-inhibitors of leukocyte adhesion mediated by VLA-4 失效3-（杂芳基）丙氨酸衍生物 - 由VLA-4介导的白细胞粘附抑制剂公开(公告)号：US07365073B2
公开(公告)日：2008-04-29
申请号：US10898576
申请日：2004-07-23
申请人： Andrei W. Konradi , Michael A. Pleiss , Eugene D. Thorsett , Darren B. Dressen , Francine S. Farouz , Christopher Semko , Ying-Zi Xu , Frank Stappenbeck
发明人： Andrei W. Konradi , Michael A. Pleiss , Eugene D. Thorsett , Darren B. Dressen , Francine S. Farouz , Christopher Semko , Ying-Zi Xu , Frank Stappenbeck
IPC分类号： A61K31/497 , C07D401/12 , C07D403/12
CPC分类号： C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/14 , C07D417/14
摘要： Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit 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并抑制由VLA-4介导的白细胞粘附的某些3-（杂芳基）丙氨酸衍生物。 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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3.发明授权公开(公告)号：US07576101B2
公开(公告)日：2009-08-18
申请号：US10763539
申请日：2004-01-26
申请人： Stephen J. Karlik , Michael A. Pleiss , Andrei W. Konradi , Francine S. Farouz , Christopher M. Semko , Darren B. Dressen , Elizabeth Messersmith , Stephen Freedman , Ted Yednock
发明人： Stephen J. Karlik , Michael A. Pleiss , Andrei W. Konradi , Francine S. Farouz , Christopher M. Semko , Darren B. Dressen , Elizabeth Messersmith , Stephen Freedman , Ted Yednock
IPC分类号： A61K31/445 , A61K31/63
CPC分类号： A61K45/06 , A61K31/10 , A61K31/16 , A61K31/185 , A61K31/195 , A61K31/21 , A61K31/496 , C07D417/14 , A61K2300/00
摘要： The application provides for methods and compositions for inhibiting demyelination, promoting remyelination and/or treating paralysis in a subject in need thereof. Preferably, such compositions include immunoglobulins (e.g., antibodies, antibody fragments, and recombinantly produced antibodies or fragments), polypeptides (e.g., soluble forms of the ligand proteins for integrins) and small molecules, which when administered in an effective amount inhibits demyelination and/or promotes remyelination in a patient. The compositions and methods described herein can also utilize other anti-inflammatory agents used to palliate conditions and diseases associated with demyelination.
摘要翻译： 本申请提供了在有需要的受试者中抑制脱髓鞘，促进髓鞘再生和/或治疗麻痹的方法和组合物。 优选地，这样的组合物包括免疫球蛋白（例如，抗体，抗体片段和重组产生的抗体或片段），多肽（例如，用于整联蛋白的配体蛋白的可溶形式）和小分子，其以有效量施用时抑制脱髓鞘和/ 或促进患者的髓鞘再生。 本文所述的组合物和方法还可以利用用于缓解与脱髓鞘相关的病症和疾病的其它抗炎剂。
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公开(公告)号：US20090143357A1
公开(公告)日：2009-06-04
申请号：US11908416
申请日：2006-03-29
申请人： Frank Diaz , Francine S. Farouz , Ryan Coatsworth Holcomb , Edward A. Kesicki , Hua Chee Ooi , Alexander Rudolph , Frank Stappenbeck , Eugene D. Thorsett , John Joseph Gaudino , Kimba Lee Fischer , Adam Wade Cook
发明人： Frank Diaz , Francine S. Farouz , Ryan Coatsworth Holcomb , Edward A. Kesicki , Hua Chee Ooi , Alexander Rudolph , Frank Stappenbeck , Eugene D. Thorsett , John Joseph Gaudino , Kimba Lee Fischer , Adam Wade Cook
IPC分类号： A61K31/553 , C07D267/10 , C07D413/02 , A61K31/5377 , C07D241/02 , A61K31/496 , C07D417/02 , A61K31/541 , A61P35/00
CPC分类号： C07D413/12 , C07D403/12 , C07D417/12
摘要： Substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division, also are disclosed.
摘要翻译： 公开了用于治疗与DNA复制中的DNA损伤或病变相关的疾病和病症的替代的尿素化合物。 还公开了制备化合物的方法及其作为治疗剂的用途，例如用于治疗癌症和其它由DNA复制，染色体分离或细胞分裂缺陷而特征的疾病。
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公开(公告)号：US20080318974A1
公开(公告)日：2008-12-25
申请号：US11659389
申请日：2005-08-18
IPC分类号： A61K31/497 , C07D401/12 , A61P35/00 , C07D401/04
CPC分类号： C07D241/20 , C07D401/04 , C07D403/04 , C07D413/04
摘要： Aryl- and heteroaryl-substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division also are disclosed.
摘要翻译： 公开了可用于治疗与DNA复制中的DNA损伤或病变相关的疾病和病症的芳基和杂芳基取代的脲化合物。 还公开了制备化合物的方法及其作为治疗剂的用途，例如用于治疗癌症和其它以DNA复制，染色体分离或细胞分裂缺陷为特征的疾病。
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公开(公告)号：US20130274215A1
公开(公告)日：2013-10-17
申请号：US13639644
申请日：2011-04-06
IPC分类号： A61K31/47 , A61K31/428 , A61K31/277 , A61K31/4709 , A61K31/551 , A61K31/502 , A61K31/706 , A61K31/194 , A61K31/4375 , A61K31/337 , A61K31/165 , A61K31/444 , A61K31/429 , A61K31/58 , A61K31/7048 , A61K31/4985
CPC分类号： A61K31/47 , A61K31/00 , A61K31/165 , A61K31/194 , A61K31/277 , A61K31/337 , A61K31/428 , A61K31/429 , A61K31/4375 , A61K31/444 , A61K31/4709 , A61K31/4985 , A61K31/502 , A61K31/551 , A61K31/58 , A61K31/7048 , A61K31/706
摘要： The present invention provides methods for the prevention, treatment and/or amelioration of fibrosis or fibrotic conditions. The present invention further provides small molecule inhibitors of Wnt- and TGF-p-mediated β-catenin signaling to prevent, treat and/or ameliorate fibrosis or fibrotic conditions. Kits comprising small molecule inhibitors of Wnt- and TGF-p-mediated β-catenin signaling and methods of identifying small molecule inhibitors of Wnt- and TGF-p-mediated β-catenin signaling are also provided.
摘要翻译： 本发明提供了预防，治疗和/或改善纤维化或纤维化病症的方法。 本发明进一步提供Wnt-和TGF-p介导的β-连环蛋白信号传导的小分子抑制剂以预防，治疗和/或改善纤维化或纤维化病症。 还提供了包含Wnt-和TGF-p介导的β-连环蛋白信号的小分子抑制剂的试剂盒以及鉴定Wnt-和TGF-β-介导的β-连环蛋白信号传导的小分子抑制剂的方法。
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公开(公告)号：US08093244B2
公开(公告)日：2012-01-10
申请号：US11908416
申请日：2006-03-29
申请人： Frank Diaz , Francine S. Farouz , Ryan Coatsworth Holcomb , Edward A. Kesicki , Kimba Lee Fischer , Adam Wade Cook
发明人： Frank Diaz , Francine S. Farouz , Ryan Coatsworth Holcomb , Edward A. Kesicki , Kimba Lee Fischer , Adam Wade Cook
IPC分类号： A61P35/00 , A61K31/497 , A61K31/5355 , A61K31/541 , C07D403/12 , C07D413/12 , C07D417/12
CPC分类号： C07D413/12 , C07D403/12 , C07D417/12
摘要： Substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division, also are disclosed.
摘要翻译： 公开了用于治疗与DNA复制中的DNA损伤或病变相关的疾病和病症的替代的尿素化合物。 还公开了制备化合物的方法及其作为治疗剂的用途，例如用于治疗癌症和其它由DNA复制，染色体分离或细胞分裂缺陷而特征的疾病。
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公开(公告)号：US20120207744A1
公开(公告)日：2012-08-16
申请号：US13257291
申请日：2010-03-19
IPC分类号： A61K35/12 , C12N5/074 , C12N5/0735 , A61K38/43 , A61K31/713 , A61K38/02 , A61K39/395 , C12N5/071 , A61K31/7088
CPC分类号： C12N15/111 , C12N5/0696 , C12N15/113 , C12N2310/14 , C12N2310/3515 , C12N2320/30 , C12N2320/32 , C12N2501/602 , C12N2501/603 , C12N2501/604 , C12N2501/605 , C12N2510/00
摘要： The present invention provides compositions and methods of using the compositions to alter the developmental potency of a cell. The present invention provides in vivo and ex vivo cell reprogramming and programming methods suitable for autologous cell therapy and regenerative medicine.
摘要翻译： 本发明提供使用该组合物来改变细胞的发育潜能的组合物和方法。 本发明提供适于自体细胞治疗和再生医学的体内和体外细胞重编程和编程方法。
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9.发明申请COMPOSITIONS COMPRISING CYCLIC AMP ENHANCERS AND/OR EP LIGANDS, AND METHODS OF PREPARING AND USING THE SAME 审中-公开包含环状AMP增强剂和/或EP配体的组合物及其制备和使用方法公开(公告)号：US20120202288A1
公开(公告)日：2012-08-09
申请号：US13257290
申请日：2010-03-18
CPC分类号： A61K31/21 , A61K31/35 , A61K31/557 , A61K38/164 , A61K38/2271 , Y02A50/471 , A61K2300/00
摘要： Provided are improved pharmaceutical compositions that comprise ligands or agonists to prostaglandin EP receptors, and/or cyclic AMP enhancers, and suitable organic solvents that are substantially free of methyl acetate, the compositions being provided for storage and/or use in an endotoxin-free vessel, such as a tube or PE bag. The compositions are suitable for in vitro, ex vivo, and in vivo use, and in particular for ex vivo therapeutic use, such as in hematopoietic stem cell transplants. Also provided are methods of using the compositions in ex vivo therapeutic applications, and methods of preparing the compositions. Kits with instructions on use are also provided.
摘要翻译： 提供了包含前列腺素EP受体的配体或激动剂和/或环AMP增强剂的改进的药物组合物，以及基本上不含乙酸甲酯的合适的有机溶剂，所述组合物用于在不含内毒素的血管中储存和/或使用 ，如管或PE袋。 该组合物适用于体外，离体和体内使用，特别是用于离体治疗用途，例如在造血干细胞移植中。 还提供了在离体治疗应用中使用组合物的方法和制备组合物的方法。 还提供了使用说明的工具包。
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10.发明授权5-(5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-ylamino)pyrazine-2-carbonitrile, pharmaceutically acceptable salts thereof, or solvate of salts 有权5-（5-（2-（3-氨基丙氧基）-6-甲氧基苯基）-1H-吡唑-3-基氨基）吡嗪-2-甲腈，其药学上可接受的盐，或盐的溶剂合物公开(公告)号：US08314108B2
公开(公告)日：2012-11-20
申请号：US12634725
申请日：2009-12-10
IPC分类号： A61K31/4965
CPC分类号： C07D403/12 , A61K31/4965 , A61K45/06 , A61K2300/00
摘要： The present invention provides an aminopyrazole compound, more particularly, or a pharmaceutically acceptable salt thereof or a solvate of the salt, that inhibits Chk1 and is useful in the treatment of cancer.
摘要翻译： 本发明提供抑制Chk1的氨基吡唑化合物，更具体地，或其药学上可接受的盐或盐的溶剂合物，并且可用于治疗癌症。
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