公开(公告)号：EP2018185B1

公开(公告)日：2016-08-31

申请号：EP07719268.0

申请日：2007-04-26

申请人： Universidade Federal de Minas Gerais ,  Max-Delbrück-Centrum für Molekulare Medizin (MDC)

发明人： SOUZA DOS SANTOS, Robson Augusto ,  SOUSA SANTOS, Sergio Henrique ,  ALVAREZ LEITE, Jaqueline Isaura ,  MATOS DE MOURA, Marina ,  SIQUEIRA HAIBARA, Andrea ,  RODRIQUES FERNANDEZ, Luciana ,  BADER, Michael ,  ALENINA, Natalia ,  SINISTERRA, Rubens Dario

IPC分类号： A61K45/00 ,  A61K38/08 ,  A61K31/415 ,  A61P3/00 ,  G01N33/50

CPC分类号： A61K31/415 ,  A61K38/085 ,  G01N33/68 ,  G01N33/6893 ,  G01N2333/726 ,  G01N2500/00

公开(公告)号：EP2018185A1

公开(公告)日：2009-01-28

申请号：EP07719268.0

申请日：2007-04-26

申请人： Universidade Federal De Minas Gerais ,  Max-Delbrück-Centrum für Molekulare Medizin (MDC)

发明人： SOUZA DOS SANTOS, Robson Augusto ,  SOUSA SANTOS, Sergio Henrique ,  ALVAREZ LEITE, Jaqueline Isaura ,  MATOS DE MOURA, Marina ,  SIQUEIRA HAIBARA, Andrea ,  RODRIQUES FERNANDEZ, Luciana ,  BADER, Michael ,  ALENINA, Natalia ,  SINISTERRA, Rubens Dario

IPC分类号： A61K45/00 ,  A61K38/08 ,  A61K31/415 ,  A61P3/00 ,  G01N33/50

CPC分类号： A61K31/415 ,  A61K38/085 ,  G01N33/68 ,  G01N33/6893 ,  G01N2333/726 ,  G01N2500/00

摘要： The present invention is characterized by the use of Mas-G- protein-coupled receptor agonists for the control, prevention and treatment of the body levels of triglycerides, cholesterol and glucose, as well as of hyper- tension and possible increase in body weight, which are characteristic of the clinical manifestation of the metabolic syndrome and its complications. Another characteristic of the invention is the use of Mas-G-protein- coupled receptor agonists, including the Angiotensin-(1-7) peptide and its analogs, agonists, either peptidic or non-peptidic, as modulators of the mani- festations of insulin resistance and glucose intolerance and in the prevention and treatment of the related alterations. The invention claims the use of MAS-G-protein-coupled receptor agonists, formulated with pharmaceutically and pharmacologically acceptable excipients or carriers, and Mas-G-protein-coupled receptor agonists, includ- ing the Angiotensin-(1-7) peptide and its analogs, agonists, either peptidic or non-peptidic, as modulators of the metabolic syndrome, the diseases that compose it and its complications.

公开(公告)号：EP2264048B1

公开(公告)日：2016-07-13

申请号：EP09841273.7

申请日：2009-02-13

申请人： Universidade Federal De Minas Gerais - UFMG

发明人： SOUZA DOS SANTOS, Robson Augusto ,  FERREIRA, Anderson José ,  SINISTERRA, Ruben Dario ,  FRAGA DA SILVA, Rodrigo Araújo ,  LAUTNER, Roberto Queiroga

IPC分类号： C07K7/14

CPC分类号： A61K38/085 ,  C07K7/14

摘要： "PEPTIDE DES-[ASP 1 ]-[ALA 1 ] ANGIOTENSIN-(1-7) AGONIST AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF DISEASES" The present invention is related to the peptide Des-[Asp 1 ]-[Ala 1 ]-Angiotensin-(1-7) (Ala 1 -Arg 2 -Val 3 -Tyr 4 -Ile 5 -His 6 -Pro 7 ) and/or its related compounds as vasodilating and cardioprotective agents to be used in mammals. This invention also comprises the production of compositions containing Des-[Asp 1 ]-[Ala 1 ]-Angiotensin-(1-7) and/or its related compounds and its use in methods for treating and preventing diseases.

公开(公告)号：EP2957569A1

公开(公告)日：2015-12-23

申请号：EP13837467.3

申请日：2013-09-13

申请人： Universidade Federal De Minas Gerais - UFMG

发明人： SOUZA DOS SANTOS, Robson Augusto ,  FERNANDES VILAS BÔAS, Suéllen Kathiane ,  FÉLIX BRAGA, Janaina ,  JEAN GEORGES FREZARD, Frederic ,  DARIO SINISTERRA, Ruben ,  CALDEIRA SILVA, Neiva ,  QUEIROGA LAUTNER, Roberto ,  ARAÚJO FRAGA DA SILVA, Rodrigo

IPC分类号： C07K7/14 ,  A61K38/08 ,  A61P9/08

CPC分类号： C07K7/06 ,  A61K9/0019 ,  A61K9/0095 ,  A61K38/00 ,  C07K7/14 ,  C12N5/0653 ,  C12N5/0657 ,  C12N5/0693 ,  C12N2501/32

摘要： The present invention relates to the peptide (arg0) n-angiotensin-(1-7) [(arg0) n-Ang-(1-7)], where n is 1 to 10 (Xaa-Asp-Arg-Val-Tyr-Ile-His-Pro; SEQ ID NO:1 where Xaa represents 1 to 10 L-Arg residues), which is produced by inserting at least one arginine amino acid at the amino terminal position of Ang-(1-7), as well as pharmaceutical compositions containing this peptide and the use thereof for the treatment or prevention of diseases or disorders that are due or associated with reduced nitric oxide production. Non-limiting examples of these diseases or disorders are cardiopulmonary and liver diseases, vascular disorders, metabolic disorders, neural disorders, genito-urinary tract disorders, skeletal muscle disorders, kidney disorders, skin disorders, alopecia or tumors. The peptide is able to cause, for example, dilation of aortic and mesenteric vessels, reduction of mean arterial blood pressure, decrease of body weight gain, blockade of the development of visceral adiposity, reduced serum and liver cholesterol levels, the normalization of glucose intolerance and insulin resistance, and an anti-proliferative effect. The peptides of the invention, such as (arg0) n-Ang-(1-7), optionally can be associated with a carrier system or controlled drug release system.

摘要翻译： 本发明涉及所述肽（为arg0）N血管紧张素 - （1-7）[（为arg0）正的Ang-（1-7）]，其中n为1至10（的Xaa - 天冬氨酸 - 精氨酸 - 缬氨酸 - 酪氨酸 -Ile-His的-PRO; SEQ ID NO：1其中Xaa darstellt 1〜10 L-精氨酸残基），所有这一切是通过在昂的）的氨基末端位置（1-7插入至少一个氨基酸精氨酸产生，如 孔含有该肽和其用于治疗疾病或病症没有治疗或预防中使用的药物组合物是因或具有减少的一氧化氮的产生相关联。 非限制性疾病或病症论文的例子心肺及肝脏疾病，血管疾病，代谢性疾病，神经性疾病，生殖泌尿道疾病，骨骼肌疾病，肾脏疾病，皮肤疾病，脱发或肿瘤。 该肽能够使得，例如，主动脉和肠系膜血管的扩张，减少平均动脉血压的，体重增加的减少，内脏肥胖的发展的封锁，减少的血清和肝脏胆固醇水平，葡萄糖耐受不良的正常化 和胰岛素抵抗，和抗增殖作用。 发明，：如（为arg0）的肽正的Ang-（1-7），可以任选地与载体系统或控制药物释放系统相关联。

公开(公告)号：EP2264048A2

公开(公告)日：2010-12-22

申请号：EP09841273.7

申请日：2009-02-13

申请人： Universidade Federal De Minas Gerais - UFMG

发明人： SOUZA DOS SANTOS, Robson Augusto ,  FERREIRA, Anderson José ,  SINISTERRA, Ruben Dario

IPC分类号： C07K7/14

CPC分类号： A61K38/085 ,  C07K7/14

摘要： "PEPTIDE DES-[ASP 1 ]-[ALA 1 ] ANGIOTENSIN-(1-7) AGONIST AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF DISEASES"
The present invention is related to the peptide Des-[Asp 1 ]-[Ala 1 ]-Angiotensin-(1-7) (Ala 1 -Arg 2 -Val 3 -Tyr 4 -Ile 5 -His 6 -Pro 7 ) and/or its related compounds as vasodilating and cardioprotective agents to be used in mammals. This invention also comprises the production of compositions containing Des-[Asp 1 ]-[Ala 1 ]-Angiotensin-(1-7) and/or its related compounds and its use in methods for treating and preventing diseases.

摘要翻译： “肽DES [ASP 1] - [ALA 1]血管紧张素 - （1-7）激动剂和药物组合物疾病治疗的” 本发明涉及肽Des- [ASP 1] - [丙氨酸1] - 血管紧张素 - （1-7）（丙氨酸1 -Arg 2 -Val 3 -Tyr 4 -Ile 5 -His 6 -Pro 7）和/或其相关化合物作为血管舒张和心脏保护剂在哺乳动物中使用。 本发明因此包括生产含沙漠[ASP 1]组合物的 - [丙氨酸1] - 血管紧张素 - （1-7）和/或其相关化合物及其在方法中使用的用于治疗和预防疾病。

公开(公告)号：EP1904087A2

公开(公告)日：2008-04-02

申请号：EP06741348.4

申请日：2006-06-28

申请人： Universidade Federal de Minas Gerais

发明人： SOUZA DOS SANTOS, Robson Augusto ,  VELOSO BRANT PINHEIRO, Sérgio ,  DE FARIA E SILVA, Raphael ,  SILVA LULA, Ivana ,  BARROS DE SOUSA, Frederico ,  FRÉZARD, Frédéric Jean Georges ,  DOS REIS, Adelina Martha ,  DE FRANCA, Luiz Renato ,  FERREIRA, Anderson, José ,  SINISTERRA, Rubén Dario ,  CAMPAGNOLE-SANTOS, Maria José ,  DE OLIVEIRA SAMPAIO, Walkyria Neyde ,  DE CASTRO LEAL, Marcelo ,  KAPPES BECKER, Lenice

IPC分类号： A61K38/08 ,  A61P43/00

CPC分类号： A61K38/085

摘要： The present invention is characterized by the use of Mas G- protein-coupled receptor agonists and antagonists as apoptotic activity modulators for study, prevention and treatment of diseases. It is further characterized by the use of Mas G-protein-coupled receptor agonist and antagonists for modulation of the apoptotic activity involving alterations in the activity of the protein kinase B/Akt. Another characteristic of the invention is the use of Mas G-protein-coupled receptor agonists and antagonists, including the Ang- (1-7) peptide and its analogues, agonists and antagonists, either peptidic or non-peptidic, as modulators of apoptotic activity for study, prevention and treatment of degenerative diseases of organs and systems, as an auxiliary measure for organs transplantation, treatment with embryonic, non- embryonic stem cells, re-implantation of organs and tissues and other treatments that need temporary or chronic reduction of the apoptotic activity, not limitative. The invention further claims the use of Mas G-protein-coupled receptor agonists and antagonists, including the Angiotensin-(1-7) peptide and its analogues, agonists and antagonists, either peptidic or non-peptidic, formulated with pharmaceutically and pharmacologically acceptable excipients or carriers, as modulators of the apoptotic activity.