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1. 发明授权

US06200558B1 Biopolymer-bound nitric oxide-releasing compositions, pharmaceutical compositions incorporating same and methods of treating biological disorders using same 失效
标题翻译：生物聚合物结合的一氧化氮释放组合物，包含其的药物组合物和使用其治疗生物学障碍的方法
公开(公告)号：US06200558B1
公开(公告)日：2001-03-13
申请号：US08837812
申请日：1997-04-22
申请人： Joseph E. Saavedra , Larry K. Keefer , Peter P. Roller , Miki Akamatsu
发明人： Joseph E. Saavedra , Larry K. Keefer , Peter P. Roller , Miki Akamatsu
IPC分类号： A61K4748
CPC分类号： A61K31/655 , A61K31/785 , A61K47/56 , A61K47/58 , A61K47/59 , A61K47/64
摘要： A polymeric composition capable of releasing nitric oxide under physiological conditions which includes a biopolymer, such as a peptide, polypeptide, protein, oligonucleotide or nucleic acid, to which is bound a nitric oxide-releasing N2O2− functional group; pharmaceutical compositions comprising the polymeric composition; and methods of treating biological disorders in which dosage with nitric oxide is therapeutic.
摘要翻译：能够在生理条件下释放一氧化氮的聚合物组合物，其包括结合一氧化氮释放N2O2-官能团的生物聚合物，例如肽，多肽，蛋白质，寡核苷酸或核酸; 包含聚合物组合物的药物组合物; 以及治疗用一氧化氮剂量治疗的生物学障碍的方法。

2. 发明授权

US5632981A Biopolymer-bound nitric oxide-releasing compositions, pharmaceutical compositions incorporating same and methods of treating biological disorders using same 失效
标题翻译：生物聚合物结合的一氧化氮释放组合物，包含其的药物组合物和使用其治疗生物学障碍的方法
公开(公告)号：US5632981A
公开(公告)日：1997-05-27
申请号：US344157
申请日：1994-11-22
申请人： Joseph E. Saavedra , Larry K. Keefer , Peter P. Roller , Miki Akamatsu
发明人： Joseph E. Saavedra , Larry K. Keefer , Peter P. Roller , Miki Akamatsu
IPC分类号： A61K45/00 , A61K31/401 , A61K31/655 , A61K31/70 , A61K31/785 , A61K31/787 , A61K35/12 , A61K38/00 , A61K38/22 , A61K39/395 , A61K47/48 , A61P1/00 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/08 , A61P15/06 , A61P15/10 , A61P25/00 , A61P35/00 , A61P35/04 , A61P37/00 , A61P43/00 , C07C291/08 , C07D207/50 , C07H21/02 , C07H21/04 , C07K1/107 , C07K5/062 , C07K5/097 , C08F8/30
CPC分类号： A61K31/785 , A61K31/655 , A61K47/48169 , A61K47/48192 , A61K47/48246 , C08F8/30
摘要： A polymeric composition capable of releasing nitric oxide under physiological conditions which includes a biopolymer, such as a peptide, polypeptide, protein, oligonucleotide or nucleic acid, to which is bound a nitric oxide-releasing N.sub.2 O.sub.2.sup.- functional group; pharmaceutical compositions comprising the polymeric composition; and methods of treating biological disorders in which dosage with nitric oxide is therapeutic.
摘要翻译：能够在生理条件下释放一氧化氮的聚合物组合物，其包括结合一氧化氮释放N2O2-官能团的生物聚合物，例如肽，多肽，蛋白质，寡核苷酸或核酸; 包含聚合物组合物的药物组合物; 以及治疗用一氧化氮剂量治疗的生物学障碍的方法。

3. 发明授权

US06379660B1 Nitric oxide-releasing 1-[(2-carboxylato)pyrrolidin-1-yl] diazen-1-ium-1,2-diolates and composition comprising same 有权
标题翻译：一氧化氮释放1 - [（2-羧基）吡咯烷-1-基]二氮烯-1- ium -1,2-二醇酯及其组合物
公开(公告)号：US06379660B1
公开(公告)日：2002-04-30
申请号：US09666668
申请日：2000-09-20
申请人： Joseph E. Saavedra , Larry K. Keefer , Peter P. Roller , Miki Akamatsu
发明人： Joseph E. Saavedra , Larry K. Keefer , Peter P. Roller , Miki Akamatsu
IPC分类号： A61K3174
CPC分类号： A61K31/655 , A61K31/785 , A61K47/56 , A61K47/58 , A61K47/59 , A61K47/64
摘要： A polymeric composition capable of releasing nitric oxide under physiological conditions which includes a biopolymer, such as a peptide, polypeptide, protein, oligonucleotide or nucleic acid, to which is bound a nitric oxide-releasing N2O2− functional group; pharmaceutical compositions comprising the polymeric composition; and methods of treating biological disorders in which dosage with nitric oxide is therapeutic.
摘要翻译：能够在生理条件下释放一氧化氮的聚合物组合物，其包括结合一氧化氮释放N2O2-官能团的生物聚合物，例如肽，多肽，蛋白质，寡核苷酸或核酸; 包含聚合物组合物的药物组合物; 以及治疗用一氧化氮剂量治疗的生物学障碍的方法。

4. 发明授权

US07439226B2 Serine protease inhibitors 失效
标题翻译：丝氨酸蛋白酶抑制剂
公开(公告)号：US07439226B2
公开(公告)日：2008-10-21
申请号：US10957266
申请日：2004-09-30
申请人： Peter P. Roller , Peng Li
发明人： Peter P. Roller , Peng Li
IPC分类号： A61K38/00
CPC分类号： C07K7/64 , A61K38/00
摘要： The present disclosure concerns peptides and peptidomimetics having inhibitory activity against serine proteases. The disclosed peptides and peptidomimetics are particularly useful as selective inhibitors of matriptase and MTSP1. Pharmaceutical compositions comprising serine protease inhibitors and methods for administering the compositions also are disclosed.
摘要翻译：本公开涉及对丝氨酸蛋白酶具有抑制活性的肽和肽模拟物。公开的肽和肽模拟物特别可用作matriptase和MTSP1的选择性抑制剂。公开了包含丝氨酸蛋白酶抑制剂的药物组合物和用于施用组合物的方法。

5. 发明授权

US06951915B2 Redox-stable, non-phosphorylated cyclic peptide inhibitors of SH2 domain binding to target protein, conjugates thereof, compositions and methods of synthesis and use 有权
标题翻译：与靶蛋白结合的SH2结构域的氧化还原稳定的非磷酸化环肽抑制剂，其结合物，组合物和合成和使用方法
公开(公告)号：US06951915B2
公开(公告)日：2005-10-04
申请号：US09998350
申请日：2001-11-30
申请人： Peter P. Roller , Ya-Qiu Long , Feng-Di T. Lung , C. Richter King , Dajun Yang
发明人： Peter P. Roller , Ya-Qiu Long , Feng-Di T. Lung , C. Richter King , Dajun Yang
IPC分类号： A61K38/00 , C07K7/06 , C07K7/56 , C07K7/00 , A61K31/00 , C07K7/50
CPC分类号： C07K7/06 , A61K38/00 , C07K7/56
摘要： A compound of formula: in which L is sulfur, sulfoxide, oxygen or methylene, and a compound of formula: in which (i) aa1 is Adi and aa4 is Glu or (ii) each of aa1 and aa4 is Adi, L is sulfur, sulfoxide, oxygen or methylene, which compounds (and their conjugates) bind to an SH2 domain in a protein comprising an SH2 domain, are non-phosphorylated, are redox-stable in vivo, are characterized by an IC50 in vivo of less than about 4.0 μM with respect to the SH2 domain in Grb2, and, upon binding to the SH2 domain of Grb2, have a turn conformation. A conjugate comprising a compound as described above and a carrier agent, a composition comprising (i) a compound or a conjugate as described above and (ii) a carrier, a method of inhibiting binding of an SH2 domain in a protein comprising an SH2 domain to a target protein in an animal, wherein the SH2 domain is contacted with a target protein-binding inhibiting effective amount of a compound or a conjugate as described above, and a method of synthesizing such conjugates.
摘要翻译：下式的化合物：其中L是硫，亚砜，氧或亚甲基，以及下式的化合物：其中（i）aa 1是Adi和aa 4是 Glu或（ii）aa 1和a 4中的每一个为Adi，L为硫，亚砜，氧或亚甲基，该化合物（及其共轭物）与SH2结合包含SH2结构域的未被磷酸化，在体内氧化还原稳定的蛋白质的结构域的特征在于体内相对于Grb2中的SH2结构域的小于约4.0μM的IC 50 并且在与Grb2的SH2结构域结合时具有转向构象。包含如上所述的化合物和载体的缀合物，包含（i）如上所述的化合物或缀合物和（ii）载体的组合物，抑制包含SH2结构域的蛋白质中SH2结构域结合的方法涉及一种动物中的靶蛋白，其中SH2结构域与靶蛋白结合抑制有效量的上述化合物或结合物接触，以及合成这种缀合物的方法。

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