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11. 发明申请

US20060287242A1 Human glucagon-like-peptide-1 modulators and their use in treatment of diabetes and related conditions 有权
标题翻译：人胰高血糖素样肽-1调节剂及其在治疗糖尿病和相关病症中的应用
公开(公告)号：US20060287242A1
公开(公告)日：2006-12-21
申请号：US11170968
申请日：2005-06-30
申请人： William Ewing , Claudio Mapelli , Richard Sulsky , Tasir Haque , Ving Lee , Douglas Riexinger , Rogelio Martinez , Yeheng Zhu
发明人： William Ewing , Claudio Mapelli , Richard Sulsky , Tasir Haque , Ving Lee , Douglas Riexinger , Rogelio Martinez , Yeheng Zhu
IPC分类号： A61K38/10 , C07K7/08
CPC分类号： C07K7/06 , A61K38/00 , C07K14/605
摘要： The present invention provides novel human glucagon-like peptide-1 (GLP-1)-receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The peptides of this invention show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.
摘要翻译：本发明提供了具有与天然GLP-1肽相似或优于天然GLP-1肽的生物活性的新型人胰高血糖素样肽-1（GLP-1） - 受体调节剂，因此可用于治疗或预防与GLP活性相关的疾病或病症。此外，本发明提供新颖的化学修饰的肽，其不仅刺激II型糖尿病患者的胰岛素分泌，而且产生其它有益的促胰岛素反应。这些合成肽GLP-1受体调节剂表现出增加的蛋白水解切割的稳定性，使其成为口服或肠胃外给药的理想治疗候选物。本发明的肽在糖尿病的功效模型中显示出所需的药代动力学性质和期望的效力。

12. 发明授权

US07238671B2 Human glucagon-like-peptide-1 mimics and their use in the treatment of diabetes and related conditions 有权
标题翻译：人胰高血糖素样肽-1模拟物及其在治疗糖尿病和相关病症中的应用
公开(公告)号：US07238671B2
公开(公告)日：2007-07-03
申请号：US10419399
申请日：2003-04-21
申请人： Sesha Iyer Natarajan , Claudio Mapelli , Margarita M. Bastos , Michael Bernatowicz , Ving Lee , William R. Ewing
发明人： Sesha Iyer Natarajan , Claudio Mapelli , Margarita M. Bastos , Michael Bernatowicz , Ving Lee , William R. Ewing
IPC分类号： A61K38/08 , C07K7/04 , A61K38/00 , A61K38/02 , A61K38/16 , C07K2/00 , C07K7/08 , C07K1/00 , C07K1/14 , C07K1/107
CPC分类号： C07K14/605 , A61K38/00
摘要： The present invention provides novel human glucagon-like peptide-1 (GLP-1) peptide mimics that mimic the biological activity of the native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 mimics exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration.
摘要翻译：本发明提供了模拟天然GLP-1肽的生物学活性的新型人胰高血糖素样肽-1（GLP-1）肽模拟物，因此可用于治疗或预防与GLP活性相关的疾病或病症。此外，本发明提供新颖的化学修饰的肽，其不仅刺激II型糖尿病患者的胰岛素分泌，而且产生其它有益的促胰岛素反应。这些合成肽GLP-1模拟物表现出增加的蛋白水解切割的稳定性，使其成为口服或肠胃外给药的理想治疗候选物。

13. 发明申请

US20100210552A1 HUMAN GLUCAGON-LIKE PEPTIDE-1 MIMICS AND THEIR USE IN THE TREATMENT OF DIABETES AND RELATED CONDITIONS 审中-公开
标题翻译：人类GLUCAGON-LIKE PEPTIDE-1 MIMICS及其在治疗糖尿病及相关病症中的应用
公开(公告)号：US20100210552A1
公开(公告)日：2010-08-19
申请号：US12771096
申请日：2010-04-30
申请人： Sesha Iyer Natarajan , Claudio Mapelli , Margarita M. Bastos , Michael Bernatowicz , Ving Lee , William R. Ewing
发明人： Sesha Iyer Natarajan , Claudio Mapelli , Margarita M. Bastos , Michael Bernatowicz , Ving Lee , William R. Ewing
IPC分类号： A61K38/16 , C07K14/00 , C07K7/00 , A61K38/04 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/12
CPC分类号： A61K45/06 , A61K38/00 , C07K14/605
摘要： The present invention provides novel human glucagon-like peptide-1 (GLP-1) peptide mimics that mimic the biological activity of the native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 mimics exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration.
摘要翻译：本发明提供了模拟天然GLP-1肽的生物学活性的新型人胰高血糖素样肽-1（GLP-1）肽模拟物，因此可用于治疗或预防与GLP活性相关的疾病或病症。此外，本发明提供新颖的化学修饰的肽，其不仅刺激II型糖尿病患者的胰岛素分泌，而且产生其它有益的促胰岛素反应。这些合成肽GLP-1模拟物表现出增加的蛋白水解切割的稳定性，使其成为口服或肠胃外给药的理想治疗候选物。

14. 发明授权

US07238670B2 Human glucagon-like-peptide-1 mimics and their use in the treatment of diabetes and related conditions 有权
公开(公告)号：US07238670B2
公开(公告)日：2007-07-03
申请号：US10273975
申请日：2002-10-18
申请人： Sesha Iyer Natarajan , Claudio Mapelli , Margarita M. Bastos , Michael Bernatowicz , Ving Lee , William R. Ewing
发明人： Sesha Iyer Natarajan , Claudio Mapelli , Margarita M. Bastos , Michael Bernatowicz , Ving Lee , William R. Ewing
IPC分类号： A61K38/08 , C07K7/04 , A61K38/00 , A61K38/02 , A61K38/16 , C07K2/00 , C07K7/08 , C07K1/00 , C07K1/14 , C07K1/107
CPC分类号： A61K45/06 , A61K38/00 , C07K14/605
摘要： The present invention provides novel human glucagon-like peptide-1 (GLP-1) peptide mimics that mimic the biological activity of the native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 mimics exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration.

15. 发明申请

US20070149763A1 Beta secretase exosite binding peptides and methods for identifying beta secretase modulators 审中-公开
标题翻译： β分泌酶外切位点结合肽和用于鉴定β分泌酶调节剂的方法
公开(公告)号：US20070149763A1
公开(公告)日：2007-06-28
申请号：US11649035
申请日：2007-01-03
申请人： Michael Kornacker , Robert Copeland , Joseph Hendrick , Zhihong Lai , Claudio Mapelli , Mark Witmer , Jovita Marcinkeviciene , William Metzler , Ving Lee , Douglas Riexinger , Jody Muckelbauer , Chiehying Chang , Daniel Camac , Paul Morin
发明人： Michael Kornacker , Robert Copeland , Joseph Hendrick , Zhihong Lai , Claudio Mapelli , Mark Witmer , Jovita Marcinkeviciene , William Metzler , Ving Lee , Douglas Riexinger , Jody Muckelbauer , Chiehying Chang , Daniel Camac , Paul Morin
IPC分类号： C07K7/08 , C07K7/06
CPC分类号： C07K5/1016 , C07K7/06
摘要： The present invention provides the crystal structure of BACE-1 complexed with both an active site inhibitor and an exosite peptide containing the core sequence YPYFI. The crystal structure shows the exosite peptide bound to the BACE-1 exosite and identifies a novel peptide binding site on the surface of the BACE-1. The invention also provides the residues that make up the exosite binding site within 6.0 Å of any exosite peptide atom which are: E316, K317, F318, P319, F322, G325, E326, Q327, L328, V329, C330, W331, Q332, A333, T335, D372, V373, A374, S376, D378, D379, C380, Y381.
摘要翻译：本发明提供了与活性位点抑制剂和含有核心序列YPYFI的外部位点肽复合的BACE-1的晶体结构。晶体结构显示了与BACE-1外切位点结合的外显肽，并鉴定了BACE-1表面上的新肽结合位点。本发明还提供了构成外部位点结合位点的任何外部位点肽原子的残基：E316，K317，F318，P319，F322，G325，E326，Q327，L328，V329，C330，W331，Q332， A333，T335，D372，V373，A374，S376，D378，D379，C380，Y381。

16. 发明授权

US5424395A Antimicrobial peptides active against plant pathogens 失效
标题翻译：抗植物病原体的抗菌肽
公开(公告)号：US5424395A
公开(公告)日：1995-06-13
申请号：US937236
申请日：1992-08-28
申请人： Newell F. Bascomb , Claudio Mapelli , Michael D. Swerdloff , Jon I. Williams , Nicholas P. Everett
发明人： Newell F. Bascomb , Claudio Mapelli , Michael D. Swerdloff , Jon I. Williams , Nicholas P. Everett
IPC分类号： G01N33/15 , A01N37/20 , A01N63/00 , A01N63/02 , A61K38/00 , A61P31/04 , C07H21/04 , C07K14/46 , C12N15/05 , C12N15/09 , C12N15/12 , C12N15/82 , C12P21/02 , C12R1/19 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： A01N63/02 , C07K14/46 , C12N15/8281 , C12N15/8282
摘要： The present invention relates to a number of peptides which have antimicrobial activity and which are useful in retarding plant pathogens. In addition, compounds in accordance with the present invention may have improved resistance to degradation by plant proteases, and/or sufficiently low phytotoxicity to render them likely candidates for use in conjunction with plants. The present invention also relates to oligonucleotides which are capable of expressing the aforementioned peptides. Also provided hereby is a process of retarding the growth of plant pathogens using the compounds of the present invention as well as a screening method and screening reagent useful in determining the proteolytic degradation resistance of a known compound.
摘要翻译：本发明涉及许多具有抗微生物活性并可用于延缓植物病原体的肽。此外，根据本发明的化合物可具有改善的抗植物蛋白酶降解性和/或足够低的植物毒性，使其成为可能与植物结合使用的候选物。本发明还涉及能够表达上述肽的寡核苷酸。此处也提供了使用本发明化合物延缓植物病原体生长的方法以及可用于测定已知化合物的蛋白水解降解抗性的筛选方法和筛选试剂。

17. 发明授权

US5516642A Polypeptides derived from major histocompatibility complex Class I antigen 失效
标题翻译：多肽衍生自主要组织相容性复合体I类抗原
公开(公告)号：US5516642A
公开(公告)日：1996-05-14
申请号：US976872
申请日：1992-11-16
申请人： Claudio Mapelli , Chester A. Meyers
发明人： Claudio Mapelli , Chester A. Meyers
IPC分类号： A61K38/00 , C07K14/74 , C07K7/08 , C07K14/00 , G01N33/534
CPC分类号： C07K14/70539 , A61K38/00
摘要： Disclosed herein are polypeptides of the formulaR.sup.1 --AA--A.sup.1 --A.sup.2 --A.sup.3 --A.sup.4 --A.sup.5 --A.sup.6 --A.sup.7 --A.sup.8 --A.sup.9 --A.sup.10 --A.sup.11 --A.sup.12 --A.sup.13 --R.sup.2 that are useful in treatment of diabetes mellitus, wherein:AA is a single bond or a polypeptide chain of 1 to 12 natural amino acid residues;A.sup.1 is seryl, A.sup.2 is phenylalanyl, A.sup.3 is arginyl, A.sup.4 is valyl, A.sup.5 is aspartyl, A.sup.6 is leucyl, A.sup.7 is arginyl, A.sup.8 is threonyl, A.sup.9 is leucyl, A.sup.10 is leucyl, A.sup.11 is arginyl, and A.sup.12 is tyrosyl, wherein one of A.sup.1 through A.sup.12 may be replaced with a natural amino acid residue, and wherein when A.sup.12 is phenylalanyl, tyrosyl or tryptophyl, its aromatic ring may be substituted with 1 or 2 iodo atoms;A.sup.13 is a natural amino acid residue other than tyrosyl, the D-form of a natural amino acid residue, --N(R.sup.4)--CH(R.sup.3)--C(O)--, or --N(R.sup.4)--CH(R.sup.3)--CH.sub.2 --;R.sup.1 is hydrogen, lower alkyl, R.sup.5 --C(O)--, aryl, aryl(lower alkyl), cycloalkyl, cycloalkyl(lower alkyl), aryl(lower alkoxy), cycloalkyl(lower alkoxy), or arylsulfenyl, wherein the aryl or cycloalkyl may be substituted with 1 to 5 substituents selected from 1 to 5 halo, 1 to 3 nitro, 1 to 5 lower alkyl, and 1 to 5 lower alkoxy groups;R.sup.2 is hydrogen, lower alkyl, aryl, aryl(lower alkyl), cycloalkyl, cycloalkyl(lower alkyl), hydroxyl, lower alkoxy, aryloxy, aryl(lower alkoxy), cycloalkyloxy, cycloalkyl(lower alkoxy), N.sub.3, --NR.sup.6 R.sup.7, or --N(R.sup.8)--NR.sup.6 R.sup.7 ;R.sup.3 is hydrogen, --R.sup.9 --R.sup.10, or --NR.sup.6 R.sup.7, and R.sup.4 is hydrogen or alkyl, or R.sup.3 and R.sup.4 together are alkylene;and the remaining symbols are as defined in the specification.
摘要翻译：本文公开了可用于治疗糖尿病的式R1-AA-A1-A2-A3-A4-A5-A6-A7-A8-A9-A10-A11-A12-A13-R2的多肽，其中：AA 是1至12个天然氨基酸残基的单键或多肽链; A1为丝氨酰基，A2为苯丙氨酰基，A3为缬氨酰基，A4为缬氨酰基，A5为天冬氨酰基，A6为亮氨酰，A7为芳基，A8为苏氨酰基，A9为亮氨酰，A10为亮氨酰，A12为酪氨酰， A1至A12之一可以被天然氨基酸残基替代，并且其中当A12是苯丙氨酰，酪氨酰或色氨酸时，其芳环可以被1或2个碘原子取代; A13是除酪氨酰之外的天然氨基酸残基，天然氨基酸残基的D型，-N（R 4）-CH（R 3）-C（O） - 或-N（R 4）-CH（R 3） -CH 2 - ; R1是氢，低级烷基，R5-C（O） - ，芳基，芳基（低级烷基），环烷基，环烷基（低级烷基），芳基（低级烷氧基），环烷基（低级烷氧基）或芳硫基，环烷基可以被1至5个选自1至5个卤素，1至3个硝基，1至5个低级烷基和1至5个低级烷氧基的取代基取代; R2是氢，低级烷基，芳基，芳基（低级烷基），环烷基，环烷基（低级烷基），羟基，低级烷氧基，芳氧基，芳基（低级烷氧基），环烷氧基，环烷基（低级烷氧基），N3，-NR6R7或 -N（R 8）-NR 6 R 7; R3是氢，-R9-R10或-NR6R7，R4是氢或烷基，或R3和R4一起是亚烷基; 其余符号如说明书中所定义。

18. 发明授权

US5519115A Reverse antimicrobial peptides 失效
标题翻译：反向抗菌肽
公开(公告)号：US5519115A
公开(公告)日：1996-05-21
申请号：US164151
申请日：1993-12-09
申请人： Claudio Mapelli , Michael D. Swerdloff , Jon I. Williams , Nicholas P. Everett
发明人： Claudio Mapelli , Michael D. Swerdloff , Jon I. Williams , Nicholas P. Everett
IPC分类号： A61K38/00 , A01N63/02 , A61P31/04 , A61P31/10 , C07K7/00 , C07K7/06 , C07K7/08 , C07K14/00 , C07K14/46 , C07K19/00 , C12N15/82 , C07K5/00 , C07K17/00
CPC分类号： C07K7/06 , A01N63/02 , C07K14/46 , C07K7/08 , C12N15/8281 , C12N15/8282 , A61K38/00 , C07K2319/00 , C07K2319/036 , C07K2319/55
摘要： The present invention relates to several types of antimicrobial peptides including reverse antimicrobial peptides, antimicrobial oligopeptides and other antimicrobial compositions, such as cecropin P1. The present invention also relates to the use of these antimicrobial peptides to provide organisms, and, in particular, plants, with protection from microbial pathogens. Finally, the present invention relates to a screening method which may be useful for determining the phytotoxity of an antimicrobial peptide.
摘要翻译：本发明涉及几种类型的抗微生物肽，包括反向抗微生物肽，抗微生物寡肽和其它抗微生物组合物，如天蚕素P1。本发明还涉及这些抗微生物肽在生物体，特别是植物中提供保护免受微生物病原体的用途。最后，本发明涉及可用于测定抗微生物肽的植物毒性的筛选方法。

19. 发明申请

US20070287670A1 HUMAN GLUCAGON-LIKE PEPTIDE-1 MIMICS AND THEIR USE IN THE TREATMENT OF DIABETES AND RELATED CONDITIONS 审中-公开
标题翻译：人类GLUCAGON-LIKE PEPTIDE-1 MIMICS及其在治疗糖尿病及相关病症中的应用
公开(公告)号：US20070287670A1
公开(公告)日：2007-12-13
申请号：US11740031
申请日：2007-04-25
申请人： Sesha Natarajan , Claudio Mapelli , Margarita Bastos , Michael Bernatowicz , Ving Lee , William Ewing
发明人： Sesha Natarajan , Claudio Mapelli , Margarita Bastos , Michael Bernatowicz , Ving Lee , William Ewing
IPC分类号： A61K38/10 , A61K38/05 , A61K38/06 , A61P3/00 , C07K7/00 , C07K7/08 , C07K7/06 , A61P3/10 , A61K38/07 , A61K38/08
CPC分类号： A61K45/06 , A61K38/00 , C07K14/605
摘要： The present invention provides novel human glucagon-like peptide-1 (GLP-1) peptide mimics that mimic the biological activity of the native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 mimics exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration.
摘要翻译：本发明提供了模拟天然GLP-1肽的生物学活性的新型人胰高血糖素样肽-1（GLP-1）肽模拟物，因此可用于治疗或预防与GLP活性相关的疾病或病症。此外，本发明提供新颖的化学修饰的肽，其不仅刺激II型糖尿病患者的胰岛素分泌，而且产生其它有益的促胰岛素反应。这些合成肽GLP-1模拟物表现出增加的蛋白水解切割的稳定性，使其成为口服或肠胃外给药的理想治疗候选物。

20. 发明申请

US20120309028A1 IMMUNOASSAY STANDARDS AND MEASUREMENT OF CLINICAL BIOMARKERS USING INTRA-ASSAY CALIBRATION STANDARDS 审中-公开
标题翻译：临床生物标志物的免疫标准和测量使用内标测定标准
公开(公告)号：US20120309028A1
公开(公告)日：2012-12-06
申请号：US13577463
申请日：2011-02-09
申请人： Paul Rhyne , Claudio Mapelli , Oi Tak Allen Wong , Flora Berisha , Robert John Neely
发明人： Paul Rhyne , Claudio Mapelli , Oi Tak Allen Wong , Flora Berisha , Robert John Neely
IPC分类号： C07K19/00 , G01N33/566
CPC分类号： G01N33/6896 , C07K14/4711 , C07K16/28 , G01N33/531 , G01N33/54393 , G01N2333/4709 , G01N2496/00
摘要： The present invention provides novel compositions and methods for creating quantitative standards to calibrate analytes. These compositions and methods enable the creation of standards and calibrators for analyzing analytes and measuring clinical biomarkers. Also provided are kits comprising the novel compositions for use in assays, for example sandwich immunoassays.
摘要翻译：本发明提供用于产生校准分析物的定量标准的新型组合物和方法。这些组合物和方法能够创建用于分析分析物和测量临床生物标志物的标准品和校准品。还提供了包含用于测定的新型组合物的试剂盒，例如夹心免疫测定。

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