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公开(公告)号：US07385025B2
公开(公告)日：2008-06-10
申请号：US11188552
申请日：2005-07-25
CPC分类号： A61K38/04 , A61K38/105 , A61K38/34 , C07K14/68 , A61K2300/00
摘要： Metallopeptides with a sequence of a biologically active alpha-melanocyte stimulating hormone (α-MSH), gamma-melanocyte stimulating hormone (γ-MSH), or bombesin sequence of length n residues, wherein a residue including a nitrogen atom and sulfur atom each available for complexation to a metal ion is inserted at any position from between the two and three position to the C-terminus side of the n position, or alternatively is substituted for the residue at any position from the three position to the n position, with a metal ion complexed thereto, with any proline (Pro) residue which is either of the two residues on the immediately adjacent N-terminus side of the inserted or substituent residue comprising a nitrogen atom and sulfur atom available for complexation to a metal ion is substituted with a homolog.
摘要翻译： 具有生物活性α-黑素细胞刺激激素（α-MSH），γ-黑素细胞刺激激素（γ-MSH）或长度为n个残基的铃蟾肽序列的序列的金属肽，其中包含氮原子和硫原子的残基各自可用 用于与金属离子的络合被插入到位于n位置的两个和三个位置到C末端侧的任何位置处，或者替代地在从三个位置到n个位置的任何位置处的残基代替， 金属离子与其中包含可与金属离子络合的氮原子和硫原子的插入或取代残基的直接相邻的N末端侧的两个残基中的任一种的脯氨酸（Pro）残基替换为 同系物
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公开(公告)号：US20080255033A1
公开(公告)日：2008-10-16
申请号：US12136233
申请日：2008-06-10
IPC分类号： A61K38/04
CPC分类号： A61K38/04 , A61K38/105 , A61K38/34 , C07K14/68 , A61K2300/00
摘要： Metallopeptides with a sequence of a biologically active gamma-melanocyte stimulating hormone sequence of length n residues, wherein a residue including a nitrogen atom and sulfur atom each available for complexation to a metal ion is inserted at any position from between the two and three position to the C-terminus side of the n position, or alternatively is substituted for the residue at any position from the three position to the n position, with a metal ion complexed thereto, with any proline (Pro) residue which is either of the two residues on the immediately adjacent N-terminus side of the inserted or substituent residue comprising a nitrogen atom and sulfur atom available for complexation to a metal ion is substituted with a homolog.
摘要翻译： 具有长度为n个残基的生物活性γ-黑素细胞刺激激素序列序列的金属肽，其中包含可用于与金属离子络合的氮原子和硫原子的残基被插入到两个和三个位置之间的任何位置， 或者在n位置的任何位置用n位置的任何位置取代残基，其中与其配合的金属离子与任何两个残基中的任一种的脯氨酸（Pro）残基 在包含可与金属离子络合的氮原子和硫原子的插入或取代残基的紧邻N末端侧被同系物取代。
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公开(公告)号：US07351690B2
公开(公告)日：2008-04-01
申请号：US10769695
申请日：2004-01-30
IPC分类号： A61K38/16
CPC分类号： C07K5/1008 , C07K1/047 , C07K5/1016 , C07K5/1024 , G01N33/6803
摘要： The invention provides methods for identification and determination of target-specific sites in peptides and proteins, including a method for determining the primary sequence of a secondary structure within a known parent polypeptide that binds to the target of interest. In one embodiment of the invention, a residue or mimetic containing a nitrogen atom and a sulfur atom available for binding to a metal ion is serially substituted for single residues in or inserted between adjacent residues in a known primary sequence of a peptide or protein. The resulting sequence is complexed with a metal ion thereby forming a metallopeptide. The resulting metallopeptides are then used in binding or functional assays related to the target of interest, and the metallopeptide(s) which result in significant or substantially decreased or changed binding or functionality are determined to identify the primary sequence involved in such binding or functionality.
摘要翻译： 本发明提供用于鉴定和确定肽和蛋白质中靶特异性位点的方法，包括确定结合目的靶标的已知亲本多肽内的二级结构的一级序列的方法。 在本发明的一个实施方案中，含有可与金属离子结合的氮原子和硫原子的残基或模拟物连续取代肽或蛋白质的已知一级序列中相邻残基之间或插入其中的单个残基。 所得到的序列与金属离子络合，从而形成金属肽。 然后将所得金属肽用于与感兴趣靶标相关的结合或功能测定，并确定导致显着或显着降低或改变的结合或功能的金属肽，以鉴定涉及这种结合或功能的一级序列。
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公开(公告)号：US20050282739A1
公开(公告)日：2005-12-22
申请号：US11188552
申请日：2005-07-25
申请人： Shubh Sharma , Yi-Qun Shi , Ramesh Rajpurohit , Hui-Zhi Cai , Margarita Bastos
发明人： Shubh Sharma , Yi-Qun Shi , Ramesh Rajpurohit , Hui-Zhi Cai , Margarita Bastos
CPC分类号： A61K38/04 , A61K38/105 , A61K38/34 , C07K14/68 , A61K2300/00
摘要： Metallopeptides with a sequence of a biologically active alpha-melanocyte stimulating hormone (α-MSH), gamma-melanocyte stimulating hormone (γ-MSH), or bombesin sequence of length n residues, wherein a residue including a nitrogen atom and sulfur atom each available for complexation to a metal ion is inserted at any position from between the two and three position to the C-terminus side of the n position, or alternatively is substituted for the residue at any position from the three position to the n position, with a metal ion complexed thereto, with any proline (Pro) residue which is either of the two residues on the immediately adjacent N-terminus side of the inserted or substituent residue comprising a nitrogen atom and sulfur atom available for complexation to a metal ion is substituted with a homolog.
摘要翻译： 具有生物活性α-黑素细胞刺激激素（α-MSH），γ-黑素细胞刺激激素（γ-MSH）或长度为n个残基的铃蟾肽序列的序列的金属肽，其中包含氮原子和硫原子的残基各自可用 用于与金属离子的络合被插入到位于n位置的两个和三个位置到C末端侧的任何位置处，或者替代地在从三个位置到n个位置的任何位置处的残基代替， 金属离子与其中包含可与金属离子络合的氮原子和硫原子的插入或取代残基的直接相邻的N末端侧的两个残基中的任一种的脯氨酸（Pro）残基取代， 同系物
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公开(公告)号：US07964181B2
公开(公告)日：2011-06-21
申请号：US11694181
申请日：2007-03-30
申请人： Shubh D. Sharma , Margarita Bastos , Wei Yang , Hui-Zhi Cai
发明人： Shubh D. Sharma , Margarita Bastos , Wei Yang , Hui-Zhi Cai
IPC分类号： A61K31/785 , A61K47/16 , A61K38/02 , A01N43/34
CPC分类号： C07K14/58 , C07D403/04 , C07K7/16
摘要： Ring-constrained amino acid surrogates of formula I: where R1, R2, R3, R4, R5, R6a, R6b, R7, and y are as defined in the specification, methods for synthesizing ring-constrained amino acid surrogates of formula I, methods of use of ring-constrained amino acid surrogates of formula I, including use in linear or cyclic compounds which include a plurality of amino acid residues and one or more ring-constrained amino acid surrogates of formula I and linear or cyclic compounds which include a plurality of amino acid residues and one or more ring-constrained amino acid surrogates of formula I.
摘要翻译： 式I的环受限氨基酸替代物：其中R1，R2，R3，R4，R5，R6a，R6b，R7和y如本说明书中所定义，用于合成式I的环受限氨基酸替代物的方法，方法 包括用于包括多个氨基酸残基和一个或多个式I的环受约束的氨基酸替代物的直链或环状化合物的线形或环状化合物，其包括多个 的氨基酸残基和一个或多个式I的环受限氨基酸替代物。
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公开(公告)号：US07622440B2
公开(公告)日：2009-11-24
申请号：US11694260
申请日：2007-03-30
申请人： Shubh D. Sharma , Margarita Bastos , Wei Yang , Hui-Zhi Cai
发明人： Shubh D. Sharma , Margarita Bastos , Wei Yang , Hui-Zhi Cai
CPC分类号： C07K14/58
摘要： Cyclic constructs with an N-terminus and a C-terminus which bind to a natriuretic peptide receptor and include a plurality of amino acid residues, at least one amino acid surrogate of formula I: where R, R′, Q, Y, W, Z, J, x and n are as defined in the specification, and optionally at least one prosthetic group, pharmaceutical compositions including such cyclic constructs, and methods of treating congestive heart failure or other conditions, syndromes or diseases for which induction of anti-hypertensive, cardiovascular, renal or endocrine effects are desired.
摘要翻译： 具有结合利尿钠肽受体并包含多个氨基酸残基的N末端和C末端的至少一个式I的氨基酸替代物的环状构建体：其中R，R'，Q，Y，W， Z，J，x和n如说明书中所定义，以及任选的至少一个假体基团，包括这种环状构建体的药物组合物，以及治疗充血性心力衰竭或其它病症的方法，综合征或疾病，其诱导抗高血压 ，心血管，肾脏或内分泌效应。
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公开(公告)号：US07795221B2
公开(公告)日：2010-09-14
申请号：US11694358
申请日：2007-03-30
申请人： Shubh D. Sharma , Margarita Bastos , Wei Yang , Hui-Zhi Cai
发明人： Shubh D. Sharma , Margarita Bastos , Wei Yang , Hui-Zhi Cai
IPC分类号： A61K38/10
CPC分类号： C07D241/08 , A61K38/00 , A61K47/60 , C07K14/58
摘要： Linear constructs with an N-terminus and a C-terminus which bind to a natriuretic peptide receptor and include a plurality of amino acid residues and at least one amino acid surrogate of formula I: where R, R′, Q, Y, W, Z, J, x and n are as defined in the specification, and optionally at least one prosthetic group covalently bound to a reactive group of at least one of the amino acid residues or surrogates, pharmaceutical compositions including such linear constructs, and methods of treating congestive heart failure or other conditions, syndromes or diseases for which induction of anti-hypertensive, cardiovascular, renal or endocrine effects are desired.
摘要翻译： 具有与利尿钠肽受体结合的N末端和C末端并且包括多个氨基酸残基和至少一个式I的氨基酸替代物的线性构建体：其中R，R'，Q，Y，W， Z，J，x和n如说明书中所定义，以及任选地至少一个与至少一个氨基酸残基或替代物的反应性基团共价结合的假基团，包括这种线型构建体的药物组合物，以及治疗方法 充血性心力衰竭或其它需要诱导抗高血压，心血管，肾或内分泌作用的综合征或疾病。
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公开(公告)号：US20100075895A1
公开(公告)日：2010-03-25
申请号：US12622055
申请日：2009-11-19
申请人： Shubh D. Sharma , Margarita Bastos , Wei Yang , Hui-Zhi Cai
发明人： Shubh D. Sharma , Margarita Bastos , Wei Yang , Hui-Zhi Cai
CPC分类号： C07K14/58
摘要： Cyclic constructs with an N-terminus and a C-terminus which bind to a natriuretic peptide receptor and include a plurality of amino acid residues, at least one amino acid surrogate of formula I: where R, R′, Q, Y, W, Z, J, x and n are as defined in the specification, and optionally at least one prosthetic group, pharmaceutical compositions including such cyclic constructs, and methods of treating congestive heart failure or other conditions, syndromes or diseases for which induction of anti-hypertensive, cardiovascular, renal or endocrine effects are desired.
摘要翻译： 具有结合利尿钠肽受体并包含多个氨基酸残基的N末端和C末端的至少一个式I的氨基酸替代物的环状构建体：其中R，R'，Q，Y，W， Z，J，x和n如说明书中所定义，以及任选的至少一个假体基团，包括这种环状构建体的药物组合物，以及治疗充血性心力衰竭或其它病症的方法，综合征或疾病，其诱导抗高血压 ，心血管，肾脏或内分泌效应。
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公开(公告)号：US08580747B2
公开(公告)日：2013-11-12
申请号：US12622055
申请日：2009-11-19
申请人： Shubh D. Sharma , Margarita Bastos , Wei Yang , Hui-Zhi Cai
发明人： Shubh D. Sharma , Margarita Bastos , Wei Yang , Hui-Zhi Cai
CPC分类号： C07K14/58
摘要： Cyclic constructs with an N-terminus and a C-terminus which bind to a natriuretic peptide receptor and include a plurality of amino acid residues, at least one amino acid surrogate of formula I: where R, R′, Q, Y, W, Z, J, x and n are as defined in the specification, and optionally at least one prosthetic group, pharmaceutical compositions including such cyclic constructs, and methods of treating congestive heart failure or other conditions, syndromes or diseases for which induction of anti-hypertensive, cardiovascular, renal or endocrine effects are desired.
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公开(公告)号：US20070232546A1
公开(公告)日：2007-10-04
申请号：US11694358
申请日：2007-03-30
申请人： Shubh D. Sharma , Margarita Bastos , Wei Yang , Hui-Zhi Cai
发明人： Shubh D. Sharma , Margarita Bastos , Wei Yang , Hui-Zhi Cai
CPC分类号： C07D241/08 , A61K38/00 , A61K47/60 , C07K14/58
摘要： Linear constructs with an N-terminus and a C-terminus which bind to a natriuretic peptide receptor and include a plurality of amino acid residues and at least one amino acid surrogate of formula I: where R, R′, Q, Y, W, Z, J, x and n are as defined in the specification, and optionally at least one prosthetic group covalently bound to a reactive group of at least one of the amino acid residues or surrogates, pharmaceutical compositions including such linear constructs, and methods of treating congestive heart failure or other conditions, syndromes or diseases for which induction of anti-hypertensive, cardiovascular, renal or endocrine effects are desired.
摘要翻译： 具有与利尿钠肽受体结合的N末端和C末端并且包括多个氨基酸残基和至少一个式I的氨基酸替代物的线性构建体：其中R，R'，Q，Y，W， Z，J，x和n如说明书中所定义，以及任选地至少一个与至少一个氨基酸残基或替代物的反应性基团共价结合的假基团，包括这种线型构建体的药物组合物，以及治疗方法 充血性心力衰竭或其它需要诱导抗高血压，心血管，肾或内分泌作用的综合征或疾病。
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