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1. 发明申请

WO2007078990A2 MODIFIED LYSINE-MIMETIC COMPOUNDS 审中-公开
标题翻译：改性赖氨酸 - 化合物
公开(公告)号：WO2007078990A2
公开(公告)日：2007-07-12
申请号：PCT/US2006048790
申请日：2006-12-21
申请人： ZEALAND PHARMA AS , WYETH CORP , LARSEN BJARNE DUE , PETERSEN JORGEN SOBERG , HAUGAN KETIL JORGEN , BUTERA JOHN A , HENNAN JAMES K , KERNS EDWARD H , PIATNITSKI EVGUENI LVOVICH
发明人： LARSEN BJARNE DUE , PETERSEN JORGEN SOBERG , HAUGAN KETIL JORGEN , BUTERA JOHN A , HENNAN JAMES K , KERNS EDWARD H , PIATNITSKI EVGUENI LVOVICH
IPC分类号： C07C233/81 , A61K31/4015 , A61K31/4166 , A61P9/00 , C07D207/16 , C07D207/50 , C07D233/02
CPC分类号： C07D207/16 , C07C233/31 , C07C233/61 , C07C233/83 , C07C237/20 , C07C237/24 , C07C237/30 , C07D233/02 , C07D403/04 , C07D403/06 , C07D405/04 , C07D407/12 , C07D413/04 , C07K5/06026
摘要： Lysine mimetic compounds having useful pharmacological activity such as antiarrhythmic activity and desirable bioavailability properties are disclosed.
摘要翻译：公开了具有有用的药理学活性如抗心律不齐活性和所需生物利用度性质的赖氨酸模拟物质。

2. 发明申请

WO02077017A3 MEDICAL USES OF INTERCELLULAR COMMUNICATION FACILITATING COMPOUNDS 审中-公开
标题翻译：细胞间通讯促进化合物的医学用途
公开(公告)号：WO02077017A3
公开(公告)日：2003-10-09
申请号：PCT/US0205773
申请日：2002-02-22
申请人： ZEALAND PHARMA AS , LARSEN BJARNE DUE , PETERSEN JORGEN SOBERG , MEIER EDDIE , KJOLBYE ANNE LOUISE , JORGENSEN NIKLAS RYE , NIELSEN MORTEN SCHAK , HOLSTEIN-RATHLOU NIELS-HENRIK , MARTINS JAMES B
发明人： LARSEN BJARNE DUE , PETERSEN JORGEN SOBERG , MEIER EDDIE , KJOLBYE ANNE LOUISE , JORGENSEN NIKLAS RYE , NIELSEN MORTEN SCHAK , HOLSTEIN-RATHLOU NIELS-HENRIK , MARTINS JAMES B
IPC分类号： A61K38/00 , A61K31/00 , A61K31/05 , A61K31/198 , A61K31/485 , A61K31/53 , A61K38/04 , A61K38/08 , A61K38/11 , A61K38/12 , A61P1/00 , A61P1/02 , A61P1/04 , A61P1/14 , A61P3/00 , A61P3/10 , A61P7/00 , A61P7/02 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/04 , A61P13/10 , A61P13/12 , A61P15/04 , A61P15/08 , A61P15/10 , A61P17/00 , A61P17/02 , A61P19/00 , A61P19/02 , A61P19/04 , A61P19/10 , A61P25/00 , A61P25/04 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/00 , A61P27/02 , A61P27/12 , A61P27/16 , A61P29/00 , A61P35/00 , A61P37/06 , A61P43/00 , C07K20060101 , C07K5/00 , C07K5/023 , C07K5/06 , C07K5/062 , C07K5/072 , C07K5/08 , C07K5/083 , C07K5/087 , C07K5/10 , C07K5/103 , C07K5/107 , C07K5/12 , C07K7/00 , C07K7/06 , C07K7/54 , C07K7/64 , A61K31/195 , A61K31/4353 , C07C237/22
CPC分类号： C07K7/06 , A61K31/00 , A61K38/00 , C07K5/06026 , C07K5/06104 , C07K5/0806 , C07K5/0812 , C07K5/1008 , C07K5/1016 , C07K7/64
摘要： Disclosed are novel peptides including antiarrhythmic peptides that have improved stability. Further disclosed are compositions that include such peptides and methods of using the compositions particularly as medicaments.
摘要翻译：公开了包括具有改善的稳定性的抗心律失常肽的新型肽。进一步公开的是包括这些肽的组合物以及将组合物特别用作药物的方法。

3. 发明申请

WO2007007060A2 N- OR C- TERMINALLY MODIFIED SMALL PEPTIDES 审中-公开
标题翻译： N-或C-末端修饰的小肽
公开(公告)号：WO2007007060A2
公开(公告)日：2007-01-18
申请号：PCT/GB2006002527
申请日：2006-07-07
申请人： ZEALAND PHARMA AS , KIDDLE SIMON JOHN , LARSEN BJARNE DUE , KERNS EDWARD H
发明人： LARSEN BJARNE DUE , KERNS EDWARD H
IPC分类号： C07K5/06 , A61K38/00
CPC分类号： C07K5/06113 , A61K38/00 , C07K5/06026 , C07K5/06078 , C07K5/06139 , C07K5/06191
摘要： N- or C-terminally modified small peptides having antiarrhythmic properties are disclosed, and in particular to small peptides that possess improved pharmacokinetic properties such as have a reduced tendency to inhibit the activity of isozyme 3A4 of cytochrome P 450 oxidase. The invention further relates to uses of said compounds in the preparation of a medicament, and to pharmaceutical compositions comprising said compounds.
摘要翻译：公开了具有抗心律失常特性的N-或C-末端修饰的小肽，特别是具有改善的药代动力学性质的小肽，例如抑制细胞色素P 450氧化酶的同工酶3A4的活性的降低趋势。本发明还涉及所述化合物在制备药物中的用途，以及包含所述化合物的药物组合物。

4. 发明申请

WO0198324A8 PEPTIDE CONJUGATES MODIFIED N- AND/OR C-TERMINALLY BY SHORT CHARGED PEPTIDE CHAINS 审中-公开
标题翻译：通过短荷载链修饰N-和/或C-末端的肽结合
公开(公告)号：WO0198324A8
公开(公告)日：2002-03-21
申请号：PCT/US0119113
申请日：2001-06-15
申请人： ZEALAND PHARMACEUTICALS AS , LARSEN BJARNE DUE , PETERSEN JORGEN SOBERG , KAPUSTA DANIEL R , HARLOW KENNETH WILLIAM
发明人： LARSEN BJARNE DUE , PETERSEN JORGEN SOBERG , KAPUSTA DANIEL R , HARLOW KENNETH WILLIAM
IPC分类号： C12N15/09 , A61K38/00 , A61K38/04 , A61K38/16 , A61K38/33 , A61K47/48 , A61P1/18 , A61P3/12 , A61P3/14 , A61P7/10 , A61P9/04 , A61P9/12 , C07K1/00 , C07K7/04 , C07K7/06 , C07K7/08 , C07K14/00 , C07K14/575 , C07K14/665 , C07K16/18 , C07K16/44 , C07K17/00 , C07K19/00 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N15/12 , C12P21/02 , C12P21/08
CPC分类号： C07K7/08 , A61K38/00 , A61K47/646 , C07K7/06
摘要： Disclosed are a variety of peptide conjugates represented by the following general formula (I): R1-Z-X-Z'-R2, wherein X represents a hexapeptide of the formula (II): A -A -A -A -A -A wherein A represents Arg, Lys, or His, A represents Tyr, Trp, or Phe, A represents Tyr, Asn, Trp or Phe, A represents Lys, Arg or His, A represents Phe, Tyr, Trp, Leu, Val or Ile, and A represents Arg, Lys, or His and wherein each amino acid residue in said hexapeptide may be in the L or D form; Z represents a charged peptide chain of from 4 to 20 amino acid residues having the D or L configuration or is missing; and Z' represents a charged peptide chain of from 4 to 20 amino acid residues having the D or L configuration or is missing, providing that not both of Z and Z' are missing; R1 represents H or an acyl group; R2 represents NR3R4 where each of R3 and R4 independently represents hydrogen, C(1-6)alkoxy, aryloxy, or a lower alkyl as defined herein; or R2 represents OH; the peptide conjugates of formula (I) being optionally further linked to a transport moiety; and salts, hydrates and solvates thereof, and C-terminally amidated or esterified derivatives thereof with suitable organic or inorganic acids, including methods or making and using such conjugates. Also provided are antibodies that specifically bind the peptide conjugates. The present invention has a wide spectrum of important applications including use in the treatment of disorders impacted by nociceptin and related opioid-like peptides.
摘要翻译：公开了由以下通式（I）表示的各种肽缀合物：R1-ZX-Z'-R2，其中X表示式（II）的六肽：A 1 -A 2 -A 3→-A 4 -A 5 -A -A 6其中A 1表示Arg，Lys或His，A 2表示Tyr，Trp或Phe，A 3表示Tyr，Asn ，Trp或Phe，A 4表示Lys，Arg或His，A 5表示Phe，Tyr，Trp，Leu，Val或Ile，A 6表示Arg，Lys或His，其中各氨基酸所述六肽中的残基可以是L或D形式; Z表示具有D或L构型或缺失的4至20个氨基酸残基的带电荷的肽链; 并且Z'表示具有D或L构型或缺失的4至20个氨基酸残基的带电荷的肽链，假定不存在Z和Z'两者; R1表示H或酰基; R 2表示NR 3 R 4，其中R 3和R 4各自独立地表示氢，C（1-6）烷氧基，芳氧基或如本文所定义的低级烷基; 或R 2表示OH; 式（I）的肽缀合物任选进一步连接至转运部分; 和其盐，水合物和溶剂化物，以及C末端酰胺化或酯化的衍生物与合适的有机或无机酸，包括方法或制备和使用这些共轭物。还提供了特异性结合肽缀合物的抗体。本发明具有广泛的重要应用，包括用于治疗受伤害感受肽和相关类阿片样肽类影响的障碍。

5. 发明申请

WO2006117565A3 GLUCAGON-LIKE-PEPTIDE-2 (GLP-2) ANALOGUES 审中-公开
标题翻译： GLUCAGON-LIKE-PEPTIDE-2（GLP-2）ANALOGUES
公开(公告)号：WO2006117565A3
公开(公告)日：2007-01-11
申请号：PCT/GB2006001633
申请日：2006-05-04
申请人： ZEALAND PHARMA AS , LARSEN BJARNE DUE , PETERSEN YVETTE MIATA , EBBEHOEJ KIRSTEN
发明人： LARSEN BJARNE DUE , PETERSEN YVETTE MIATA , EBBEHOEJ KIRSTEN
IPC分类号： C07K14/605 , A61K38/26
CPC分类号： C07K14/605 , A61K9/0019 , A61K35/54 , A61K35/74 , A61K38/00 , A61K38/26 , A61K48/00 , C12N7/00 , C12N2710/10043 , C12N2710/20043 , C12N2710/22043 , C12N2760/20243
摘要： GLP-2 analogues are disclosed which comprise one of more substitutions as compared to [hGly2]GLP-2 and which improved biological activity in vivo and/or improved chemical stability, e.g. as assessed in in vitro stability assays. More particularly, preferred GLP-2 analogues disclosed herein comprise substitutions at one or more of positions 8, 16, 24 and/or 28 of the wild-type GLP-2 sequence, optionally in combination with further substitutions at position 2 (as mentioned in the introduction) and one or more of positions 3, 5, 7, 10 and 11, and/or a deletion of one or more of amino acids 31 to 33 and/or the addition of a N-terminal or C-terminal stabilizing peptide sequence. The analogues are particularly useful for the prophylaxis or treatment of stomach and bowel-related disorders and for ameliorating side effects of chemotherapy.
摘要翻译：公开了GLP-2类似物，其包含与[hGly2] GLP-2相比更多的取代之一，并且其在体内和/或改善的化学稳定性，例如，如在体外稳定性测定中评估的。更具体地，本文公开的优选的GLP-2类似物包括在野生型GLP-2序列的8,16,24和/或28位的一个或多个位置上的取代，任选与第2位的进一步取代组合（如引入）和位置3,5,7,10和11中的一个或多个，和/或缺失一个或多个氨基酸31至33和/或添加N-末端或C-末端稳定肽序列。类似物对于预防或治疗胃和肠相关疾病以及改善化学疗法的副作用特别有用。

6. 发明申请

WO2004035623A3 STABILIZED EXENDIN-4 COMPOUNDS 审中-公开
标题翻译：稳定的维生素-4化合物
公开(公告)号：WO2004035623A3
公开(公告)日：2004-06-03
申请号：PCT/DK0300651
申请日：2003-10-02
申请人： ZEALAND PHARMA AS , EBBEHOEJ KIRSTEN , JEPSEN TRINE , KNUDSEN CARSTEN BOYE , LARSEN BJARNE DUE , KNOTT DAVID
发明人： EBBEHOEJ KIRSTEN , JEPSEN TRINE , KNUDSEN CARSTEN BOYE , LARSEN BJARNE DUE , KNOTT DAVID
IPC分类号： A61K38/22 , C07K14/575
CPC分类号： C07K14/57563 , A61K38/00
摘要： The present invention disclosed compositions comprising a stabilized Exendin-4 (1-39) and related compounds. The invention describes stabilized Exendin-4 agonists that include at least one modified amino acid residue particularly at positions Gln 13, Met14, Trp25, or Asn28 of the Exendin-4 (1-39) molecule. Disclosed are preferred modifications of deaminated, hydrolyzed, oxidized, or isomerized reaction products of the specified amino acid residues corresponding to the same positions in the Exendin-4 molecule. The invention also relates to methods of making and using the stabilized Exendin compounds, such as for the treatment of diabetes.
摘要翻译：本发明公开了包含稳定的毒蜥外泌肽-4（1-39）和相关化合物的组合物。本发明描述了稳定的毒蜥外泌肽-4激动剂，其包括至少一个修饰的氨基酸残基，特别是在毒蜥外泌肽-4（1-39）分子的Gln 13，Met14，Trp25或Asn28的位置。公开了对应于毒蜥外泌肽-4分子中相同位置的特定氨基酸残基的脱氨基，水解的，氧化的或异构化的反应产物的优选修饰。本发明还涉及制备和使用稳定的毒蜥外泌肽化合物的方法，例如用于治疗糖尿病。

7. 发明申请

WO2009010733A3 PEPTIDE GAP JUNCTION MODULATORS 审中-公开
标题翻译：肽间隙连接调节剂
公开(公告)号：WO2009010733A3
公开(公告)日：2009-06-25
申请号：PCT/GB2008002405
申请日：2008-07-14
申请人： ZEALAND PHARMA AS , UNIV NEW YORK STATE RES FOUND , KIDDLE SIMON J , LARSEN BJARNE DUE , DELMAR MARIO , TAFFET STEVEN M , COOMBS WANDA , VERMA VANDANA
发明人： LARSEN BJARNE DUE , DELMAR MARIO , TAFFET STEVEN M , COOMBS WANDA , VERMA VANDANA
IPC分类号： C07K5/02 , A61K38/07 , A61K38/08 , A61K38/10 , A61K38/16 , C07K5/10 , C07K7/06 , C07K7/08 , C07K14/00
CPC分类号： C07K14/705 , A61K38/00 , C07K5/0817 , C07K5/1019
摘要： Disclosed are peptides that facilitate the intercellular communication mediated by gap junctions. The invention has a wide spectrum of useful applications including use in the treatment of diseases associated with impaired gap junction intracellular communication (GJIC).
摘要翻译：公开了促进由间隙连接介导的细胞间通讯的肽。本发明具有广泛的有用应用，包括用于治疗与间隙连接细胞间通讯障碍（GJIC）相关的疾病。

8. 发明申请

WO2005061437A3 ISOPEPTIDE GAP JUNCTION MODULATORS 审中-公开
标题翻译：异位间隙连接调节剂
公开(公告)号：WO2005061437A3
公开(公告)日：2005-08-25
申请号：PCT/GB2004005416
申请日：2004-12-23
申请人： ZEALAND PHARMA AS , LARSEN BJARNE DUE , KIDDLE SIMON
发明人： LARSEN BJARNE DUE
IPC分类号： C07C237/12 , C07K5/00 , A61K38/04 , A61P9/06
CPC分类号： C07C237/12 , A61K38/00
摘要： The invention relates to isopeptides capable of modulating intracellular gap junctional communication. The invention further relates to methods of using the isopeptides to maintain or enhance such communication. In one aspect, the isopeptides are antiarrhythmic isopeptides which target the same cells targeted by AAP, AAP10, HP5, and/or functional analogs thereof, i.e. the isopeptides are able to modulate the function of these cells by agonizing or antagonizing the function of AAP, AAP10, HP5, and/or functional analogs thereof.
摘要翻译：本发明涉及能够调节细胞间隙连接通讯的异肽。本发明还涉及使用异肽来维持或增强这种通讯的方法。一方面，异肽是靶向AAP，AAP10，HP5和/或其功能类似物的相同细胞的抗心律不齐的异肽，即异肽能够通过激动或拮抗AAP的功能来调节这些细胞的功能， AAP10，HP5和/或其功能类似物。

9. 发明申请

WO2004104004A3 TRIAZA-SPIRO COMPOUNDS AS NOCICEPTIN ANALOGUES AND USES THEREOF 审中-公开
标题翻译： TRIAZA-SPIRO化合物作为NOCICEPTIN类似物及其用途
公开(公告)号：WO2004104004A3
公开(公告)日：2005-03-03
申请号：PCT/DK2004000360
申请日：2004-05-21
申请人： ZEALAND PHARMA AS , HANSEN LARS BO LAURENBORG , LARSEN BJARNE DUE , THORKILDSEN CHRISTIAN , KNUDSEN CARSTEN BOYE
发明人： HANSEN LARS BO LAURENBORG , LARSEN BJARNE DUE , THORKILDSEN CHRISTIAN , KNUDSEN CARSTEN BOYE
IPC分类号： A61P7/10 , A61P25/00 , C07D471/10 , C07D519/00 , A61K31/4747
CPC分类号： C07D471/10
摘要： The present invention. relates to nociceptin analogues represented by the following formula I: and uses thereof to modulate biological functions. In one aspect, the invention provides modified triaza-spiroo compounds that include at least one specialized chemical group that is bound to the compounds. The invention has a wide range of applications including providing a. new class of therapeutically useful aquaretics.
摘要翻译：本发明。涉及由下式I表示的伤害感受肽类似物：及其用于调节生物功能的用途。一方面，本发明提供了修饰的三氮杂 - 螺环化合物，其包括与化合物结合的至少一个特殊的化学基团。本发明具有广泛的应用，包括提供a。新一类治疗有用的矫饰剂。

10. 发明申请

WO2009012224A2 PEPTIDE-BASED REGULATION OF GAP JUNCTIONS 审中-公开
标题翻译：基于肽基的GAP结构调节
公开(公告)号：WO2009012224A2
公开(公告)日：2009-01-22
申请号：PCT/US2008069980
申请日：2008-07-14
申请人： UNIV NEW YORK STATE RES FOUND , DELMAR MARIO , TAFFET STEVEN M , LARSEN BJARNE DUE
发明人： DELMAR MARIO , TAFFET STEVEN M , LARSEN BJARNE DUE
IPC分类号： A61K38/10
CPC分类号： A61K38/10
摘要： The present invention relates to proteins and polypeptides that (i) have the formula A - [Wm - A]n where each A is independently a peptide of formula XXXXRXPXXXX where each X is independently any amino acid, R is arginine, and P is proline; each W is independently a linker; m is 1 or 2; and n is any number from 1 through 5; (ii) consist essentially of the formula XnRXPXm where each X is independently any amino acid, R is arginine, P is proline, n is any number from zero to fifteen, m is any number from zero to fifteen, and the sum of n and m is any number from eight to fifteen; (iii) have the formula A - An where each A is independently a peptide of formula XXXXRXPXXXX where each X is independently any amino acid, R is arginine, and P is proline; and n is any number from 1 through 5; or (iv) consist essentially of the formula XnRXPXm where each X is independently any amino acid, R is arginine, P is proline, n is any number from zero to seven, m is any number from zero to seven, and the sum of n and m is any number from zero to seven. Methods using these proteins and polypeptides to: identify the location of an RXP -binding domain of Cx43CT, modulate a Cx43 gap junction channel, screen for compounds that modulate Cx43CT, and measure Cx43CT-binding affinity of a compound that binds to Cx43CT, are also disclosed.
摘要翻译：本发明涉及（i）具有式A - [Wm-A] n的蛋白质和多肽，其中每个A独立地是式XXXXRXPXXXX的肽，其中每个X独立地是任何氨基酸，R是精氨酸，P是脯氨酸 ; 每个W独立地是一个连接体; m为1或2; n是从1到5的任何数字; （ii）基本上由式XnRXPXm组成，其中每个X独立地是任何氨基酸，R是精氨酸，P是脯氨酸，n是从零到十五的任何数，m是从零到十五的任何数，以及n和 m是从8到15的任何数字; （iii）具有式A-An，其中每个A独立地是式XXXXRXPXXXX的肽，其中每个X独立地是任何氨基酸，R是精氨酸，P是脯氨酸; n是从1到5的任何数字; 或（iv）基本上由式XnRXPXm组成，其中每个X独立地是任何氨基酸，R是精氨酸，P是脯氨酸，n是从0到7的任何数字，m是从0到7的任何数字，并且n的总和 m是从零到七的任何数字。使用这些蛋白质和多肽的方法：鉴定Cx43CT的RXP结合结构域的位置，调节Cx43间隙连接通道，筛选调节Cx43CT的化合物和测量与Cx43CT结合的化合物的Cx43CT结合亲和力，也是披露。

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