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公开(公告)号：US08076453B2
公开(公告)日：2011-12-13
申请号：US11916136
申请日：2006-05-31
IPC分类号： C07K7/00
摘要： The present invention provides for novel kinin B1 receptors peptide agonists of formula (I) having very good to excellent affinities and selectivity for the B1 receptor, in vitro and in vivo increased resistance to enzymatic degradation, superior pharmacokinetic properties to those of naturally occurring agents, capacity to significantly enhance delivery of chemotherapeutic substances across the blood brain barrier and within peripheral tissues for the treatment of tumors, capacity to protect and restore kidney, heart, brain and other organ functions, when given alone or in combination with other therapies in the treatment of hypertension, diabetes and other cardiovascular diseases particularly, but not limited to, atherosclerosis and arteriosclerosis. Formula (I): aay-aax-aa0-aa1-aa2-aa3-aa4-aa5-Ser6-Pro7-D-Phe8-X.
摘要翻译： 本发明提供式（I）的新型激肽B1受体肽激动剂对于B1受体具有非常好的至极好的亲和力和选择性，体外和体内增加了对酶降解的抗性，与天然存在的药物的药代动力学性质优异， 当治疗单独或与治疗中的其他疗法组合时，能够显着增强穿过血脑屏障和外周组织的化疗物质的递送以治疗肿瘤的能力，保护和恢复肾，心脏，脑和其他器官功能的能力 高血压，糖尿病和其他心血管疾病，特别但不限于动脉粥样硬化和动脉硬化。 式（I）：aay-aax-aa0-aa1-aa2-aa3-aa4-aa5-Ser6-Pro7-D-Phe8-X。
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公开(公告)号：US20090054347A1
公开(公告)日：2009-02-26
申请号：US11916136
申请日：2006-05-31
摘要： The present invention provides for novel kinin B1 receptors peptide agonists of formula (I) having very good to excellent affinities and selectivity for the B1 receptor, in vitro and in vivo increased resistance to enzymatic degradation, superior pharmacokinetic properties to those of naturally occurring agents, capacity to significantly enhance delivery of chemotherapeutic substances across the blood brain barrier and within peripheral tissues for the treatment of tumors, capacity to protect and restore kidney, heart, brain and other organ functions, when given alone or in combination with other therapies in the treatment of hypertension, diabetes and other cardiovascular diseases particularly, but not limited to, atherosclerosis and arteriosclerosis. Formula (I): aay-aax-aa0-aa1-aa2-aa3-aa4-aa5-Ser6-Pro7-D-Phe8-X.
摘要翻译： 本发明提供式（I）的新型激肽B1受体肽激动剂对于B1受体具有非常好的至极好的亲和力和选择性，体外和体内增加了对酶降解的抗性，与天然存在的药物的药代动力学性质优异， 当治疗单独或与治疗中的其他疗法组合时，能够显着增强穿过血脑屏障和外周组织的化疗物质的递送以治疗肿瘤的能力，保护和恢复肾，心脏，脑和其他器官功能的能力 高血压，糖尿病和其他心血管疾病，特别但不限于动脉粥样硬化和动脉硬化。 式（I）：aay-aax-aa0-aa1-aa2-aa3-aa4-aa5-Ser6-Pro7-D-Phe8-X。
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公开(公告)号：US20150141324A1
公开(公告)日：2015-05-21
申请号：US14371134
申请日：2012-08-31
申请人： Robert Day , Witold A. Neugebauer , Yves Dory
发明人： Robert Day , Witold A. Neugebauer , Yves Dory
CPC分类号： C07K7/06 , A61K38/00 , A61K38/08 , A61K45/06 , A61K47/542 , A61K47/60 , Y02A50/469 , Y02A50/475
摘要： It is provided furin inhibitors and their uses for treating pathogen infection. Particularly, it is provided a method or use for the treatment of a pathogen infection, in a subject, comprising administering to the subject a therapeutically effective amount of the furin inhibitors or the composition disclosed, thereby preventing or treating pathogen infection, in the subject.
摘要翻译： 提供弗林蛋白酶抑制剂及其用于治疗病原体感染的用途。 特别地，提供了在受试者中治疗病原体感染的方法或用途，其包括向受试者施用治疗有效量的所述弗林蛋白酶抑制剂或所公开的组合物，从而预防或治疗受试者的病原体感染。
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公开(公告)号：US09809621B2
公开(公告)日：2017-11-07
申请号：US14342041
申请日：2012-08-30
申请人： Robert Day , Witold A. Neugebauer , Yves Dory
发明人： Robert Day , Witold A. Neugebauer , Yves Dory
CPC分类号： C07K7/06 , A61K38/00 , A61K38/08 , A61K45/06 , A61K47/542 , A61K47/60 , Y02A50/469 , Y02A50/475
摘要： It is provided PACE4 inhibitors and their uses for treating infection, cancer. Particularly, it is provided a method or use for the treatment of a cancer in a subject, comprising administering to the subject a therapeutically effective amount of the PACE4 inhibitors or the composition disclosed.
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5.发明授权Multi-LEU peptides and analogues thereof as selective PACE4 inhibitors and effective antiproliferative agents 有权多LEU肽及其类似物作为选择性PACE4抑制剂和有效的抗增殖剂公开(公告)号：US08658591B2
公开(公告)日：2014-02-25
申请号：US13003628
申请日：2009-07-06
申请人： Robert Day , Martin Fugère , Witold A. Neugebauer
发明人： Robert Day , Martin Fugère , Witold A. Neugebauer
CPC分类号： C07K7/06 , A61K38/00 , C07K5/1019 , C07K14/811 , C12Q1/37 , G01N2333/96438 , G01N2500/04
摘要： Disclosed herein are PACE4 inhibitors, compositions comprising PACE4 inhibitors and their uses thereof for lowering PACE4 activity, reducing cell proliferation, reducing tumor growth, reducing metastasis formation, preventing and/or treating cancer. Also provided are methods for lowering PACE4 activity, reducing the proliferation of a cell, reducing tumor growth and/or treating and preventing cancer. Methods for screening PACE4 inhibitors and cell proliferation inhibitors are further provided.
摘要翻译： 本文公开了PACE4抑制剂，包含PACE4抑制剂的组合物及其用于降低PACE4活性，降低细胞增殖，降低肿瘤生长，减少转移形成，预防和/或治疗癌症的用途。 还提供降低PACE4活性，减少细胞增殖，降低肿瘤生长和/或治疗和预防癌症的方法。 还提供了筛选PACE4抑制剂和细胞增殖抑制剂的方法。
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公开(公告)号：US20140206622A1
公开(公告)日：2014-07-24
申请号：US14342041
申请日：2012-08-30
申请人： Robert Day , Witold A. Neugebauer , Yves Dory
发明人： Robert Day , Witold A. Neugebauer , Yves Dory
CPC分类号： C07K7/06 , A61K38/00 , A61K38/08 , A61K45/06 , A61K47/542 , A61K47/60 , Y02A50/469 , Y02A50/475
摘要： It is provided PACE4 inhibitors and their uses for treating infection, cancer. Particularly, it is provided a method or use for the treatment of a cancer in a subject, comprising administering to the subject a therapeutically effective amount of the PACE4 inhibitors or the composition disclosed.
摘要翻译： 提供PACE4抑制剂及其用于治疗感染，癌症的用途。 特别地，提供了用于治疗受试者中的癌症的方法或用途，其包括向受试者施用治疗有效量的PACE4抑制剂或所公开的组合物。
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公开(公告)号：US07041785B1
公开(公告)日：2006-05-09
申请号：US09242751
申请日：1997-08-14
申请人： Domenico Recoli , Gerard E. Plante , Fernand Gobeil , Witold A. Neugebauer , Adriana Zucollo , Orlando L. Catanzaro
发明人： Domenico Recoli , Gerard E. Plante , Fernand Gobeil , Witold A. Neugebauer , Adriana Zucollo , Orlando L. Catanzaro
CPC分类号： A61K38/04
摘要： The present invention relates to novel antagonists to a B1-bradykinin (B1-BK) receptor which have a good affinity and selectivity therefor, some of which being at least partially resistant to enzymatic degradation. The synthesis of the B1 receptors is induced during inflammation. Symptoms associated with inflammation (elevated hydrostatic pressure and plasma leakage or extravasation) have been observed in diabetic animal models (streptozotocin-induced diabetes (STZ)) as well as in spontaneously hypertensive rats (SHR). The present inventors confirm the presence of B1-BK receptors in these two models. B1-BK antagonists abolished the vasocontraction induced by B1-BK in SHR and STZ, and reduced the glycemia of diabetic animals to normal levels. The present B1-antagonists are useful for treating any condition wherein B1-receptor is expressed, particularly during inflammation, and more particularly wherein B1-receptor expression results in diabetic vasculopathy, other diabetic symptoms associated with an insulitis and a post-capillary resistance building as a consequence of the presence of a B1-receptor.
摘要翻译： 本发明涉及对其具有良好亲和性和选择性的B 1 - 半激动素（B 1 -BK）受体的新型拮抗剂，其中一些至少部分地 耐酶降解。 在炎症期间诱导B 1受体的合成。 在糖尿病动物模型（链脲霉素诱发的糖尿病（STZ））以及自发性高血压大鼠（SHR）中观察到与炎症相关的症状（升高的静水压力和血浆渗漏或外渗）。 本发明人证实在这两种模型中存在B 1 -KK受体。 B 1 BK拮抗剂消除了SHR和STZ中B 1 -BK引起的血管收缩，并将糖尿病动物的血糖降低至正常水平。 本发明的B 1 - 拮抗剂可用于治疗其中B 1 - 受体表达的任何情况，特别是在炎症期间，更具体地，其中B 1
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