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1.发明申请SHORT CHAIN PEPTIDOMIMETICS BASED ORALLY ACTIVE GLP 1 AGONIST AND GLUCAGON RECEPTOR ANTAGONIST 审中-公开短链基团基于ORAGY活性GLP 1激动剂和GLUCAGON受体拮抗剂公开(公告)号：US20120264685A1
公开(公告)日：2012-10-18
申请号：US13502826
申请日：2010-10-18
申请人： Rajesh Bahekar , Mukul R. Jain , Pankaj R. Patel
发明人： Rajesh Bahekar , Mukul R. Jain , Pankaj R. Patel
CPC分类号： C07K14/605 , A61K38/00
摘要： The present invention provides novel short chain peptidomimetics, which act as GLP-1 receptors agonist and glucagon receptor antagonist. These dual acting peptidomimetics exhibit increased stability to proteolytic cleavage, especially against DPP-IV (Dipeptidyl peptidase-IV) enzyme, GIT enzymes such as pepsin and acidic stomach pH and also against liver microsomes (in vitro). Due to increased metabolic stability, other than parenteral route of administration, these short chain peptidomimetics can be delivered by oral routes of administration, for the treatment or prevention of diabetes and related metabolic disorders, such as obesity, hyperlipidemia and eating disorders.
摘要翻译： 本发明提供新的短链肽模拟物，其作为GLP-1受体激动剂和胰高血糖素受体拮抗剂。 这些双重作用的肽模拟物表现出增加的蛋白水解切割的稳定性，特别是对DPP-IV（二肽基肽酶-IV）酶，GIT酶如胃蛋白酶和酸性胃pH以及针对肝微粒体（体外）的稳定性。 由于代谢稳定性增加，除了肠胃外给药途径之外，这些短链肽模拟物可以通过口服给药途径递送，用于治疗或预防糖尿病和相关的代谢紊乱，例如肥胖，高脂血症和进食障碍。
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公开(公告)号：US08383581B2
公开(公告)日：2013-02-26
申请号：US13259706
申请日：2010-04-26
申请人： Rajesh Bahekar , Mukul R. Jain , Pankaj R. Patel
发明人： Rajesh Bahekar , Mukul R. Jain , Pankaj R. Patel
IPC分类号： A61K38/29
CPC分类号： C07K14/635 , A61K38/00
摘要： The present invention provides novel short-chain peptides, which primarily act as parathyroid hormone (PTH/PTH-1) receptor agonist. These short-chain peptides exhibit increased stability to proteolytic cleavage. Most of short-chain peptides were found to be stable in rat plasma up to 24 hours (in vitro), showed increased stability against GIT enzymes such as pepsin and acidic stomach pH and also against liver microsomes (in vitro). Due to increased metabolic stability, other than parenteral route of administration, some of the short-chain peptides can also be delivered by oral routes of administration, for the treatment/prevention of hypoparathyroidism and diseases characterized by bone mass reduction, such as osteoporosis, postmenopausal osteoporosis and for stimulating bone repair. A-Z1-Z2-Z3-Z4-Z5-Z6-Z7-Z8-Z9-Z10-Z11-Z12-Z13-Z14-Z15-B
摘要翻译： 本发明提供了主要作为甲状旁腺激素（PTH / PTH-1）受体激动剂的新型短链肽。 这些短链肽表现出增加的蛋白水解切割的稳定性。 发现大多数短链肽在大鼠血浆中稳定至多24小时（体外），显示出对GIT酶如胃蛋白酶和酸性胃pH以及针对肝微粒体（体外）的稳定性增加。 由于代谢稳定性增加，除了肠胃外给药途径外，一些短链肽也可以通过口服给药途径递送，用于治疗/预防甲状旁腺功能减退症和以骨量减少为特征的疾病，如骨质疏松症，绝经后 骨质疏松症和刺激骨修复。 A-Z1-Z2-Z3-Z4-Z5-Z6-Z7-Z8-Z9-Z10-Z11-Z12-Z13-Z14-Z15-B
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公开(公告)号：US20120108496A1
公开(公告)日：2012-05-03
申请号：US13259706
申请日：2010-04-26
申请人： Rajesh Bahekar , Mukul R. Jain , Pankaí R. Patel
发明人： Rajesh Bahekar , Mukul R. Jain , Pankaí R. Patel
CPC分类号： C07K14/635 , A61K38/00
摘要： The present invention provides novel short-chain peptides, which primarily act as parathyroid hormone (PTH/PTH-1) receptor agonist. These short-chain peptides exhibit increased stability to proteolytic cleavage. Most of short-chain peptides were found to be stable in rat plasma up to 24 hours (in vitro), showed increased stability against GIT enzymes such as pepsin and acidic stomach pH and also against liver microsomes (in vitro). Due to increased metabolic stability, other than parenteral route of administration, some of the short-chain peptides can also be delivered by oral routes of administration, for the treatment/prevention of hypoparathyroidism and diseases characterized by bone mass reduction, such as osteoporosis, postmenopausal osteoporosis and for stimulating bone repair. A-Z1—Z2—Z3—Z4—Z5—Z6—Z7—Z8—Z9—Z10—Z11—Z12—Z13—Z14—Z15—B
摘要翻译： 本发明提供了主要作为甲状旁腺激素（PTH / PTH-1）受体激动剂的新型短链肽。 这些短链肽表现出增加的蛋白水解切割的稳定性。 发现大多数短链肽在大鼠血浆中稳定至多24小时（体外），显示出对GIT酶如胃蛋白酶和酸性胃pH以及针对肝微粒体（体外）的稳定性增加。 由于代谢稳定性增加，除了肠胃外给药途径之外，一些短链肽也可以通过口服给药途径递送，用于治疗/预防甲状旁腺功能减退症和以骨量减少为特征的疾病，如骨质疏松症，绝经后 骨质疏松症和刺激骨修复。 A-Z1-Z2-Z3-Z4-Z5-Z6-Z7-Z8-Z9-Z10-Z11-Z12-Z13-Z14-Z15-B
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