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公开(公告)号：US08114844B2
公开(公告)日：2012-02-14
申请号：US12244880
申请日：2008-10-03
申请人： Shubh D. Sharma , Margarita Bastos , Wei Yang
发明人： Shubh D. Sharma , Margarita Bastos , Wei Yang
IPC分类号： A61K38/12 , A61K38/08 , C07D403/00
CPC分类号： C07D403/12 , C07D403/14 , C07D487/04 , C07K7/16 , C07K14/58
摘要： Linear and cyclic peptidomimetics which bind to one or more melanocortin receptors are provided, which peptidomimetics include at least one ring-constrained amino acid surrogate of formula I: where R1, R2, R3, R4, R5, R6, R7, R8, and y are as defined in the specification, together with methods for synthesizing ring-constrained amino acid surrogates of formula I and peptidomimetics incorporating the same, and methods of use of peptidomimetics in the treatment of various diseases, syndromes and conditions.
摘要翻译： 提供了结合一种或多种黑皮质素受体的线性和环肽模拟物，其中肽模拟物包括至少一个式I的环受限氨基酸替代物：其中R1，R2，R3，R4，R5，R6，R7，R8和y 以及用于合成式I的环受限制的氨基酸替代物的方法和包含其的肽模拟物的方法，以及使用肽模拟物治疗各种疾病，综合征和病症的方法。
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公开(公告)号：US08580746B2
公开(公告)日：2013-11-12
申请号：US12572284
申请日：2009-10-02
申请人： Shubh D. Sharma , Margarita Bastos , Wei Yang
发明人： Shubh D. Sharma , Margarita Bastos , Wei Yang
摘要： Cyclic constructs 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 a cyclic linkage including one or two amide bonds, 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： 结合利尿钠肽受体并包含多个氨基酸残基的至少一种氨基酸替代物，其中R，R'，Q，Y，W，Z，J，x和n如上所定义， 在本说明书中，包括一个或两个酰胺键的环状连接，包括这种环状构建体的药物组合物，治疗充血性心力衰竭或其它病症的方法，综合征或诱导抗高血压，心血管，肾脏或内分泌效应的疾病 是理想的。
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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：US20100035821A1
公开(公告)日：2010-02-11
申请号：US12572284
申请日：2009-10-02
申请人： Shubh D. Sharma , Margarita Bastos , Wei Yang
发明人： Shubh D. Sharma , Margarita Bastos , Wei Yang
摘要： Cyclic constructs 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 a cyclic linkage including one or two amide bonds, 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： 结合利尿钠肽受体并包含多个氨基酸残基的至少一种氨基酸替代物，其中R，R'，Q，Y，W，Z，J，x和n如上所定义， 在本说明书中，包括一个或两个酰胺键的环状连接，包括这种环状构建体的药物组合物，治疗充血性心力衰竭或其它病症的方法，综合征或诱导抗高血压，心血管，肾脏或内分泌效应的疾病 是理想的。
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公开(公告)号：US20090069224A1
公开(公告)日：2009-03-12
申请号：US12244880
申请日：2008-10-03
申请人： Shubh D. Sharma , Margarita Bastos , Wei Yang
发明人： Shubh D. Sharma , Margarita Bastos , Wei Yang
CPC分类号： C07D403/12 , C07D403/14 , C07D487/04 , C07K7/16 , C07K14/58
摘要： Linear and cyclic peptidomimetics which bind to one or more melanocortin receptors are provided, which peptidomimetics include at least one ring-constrained amino acid surrogate of formula I: where R1, R2, R3, R4, R5, R6, R7, R8, and y are as defined in the specification, together with methods for synthesizing ring-constrained amino acid surrogates of formula I and peptidomimetics incorporating the same, and methods of use of peptidomimetics in the treatment of various diseases, syndromes and conditions.
摘要翻译： 提供了结合一种或多种黑皮质素受体的线性和环肽模拟物，其中肽模拟物包括至少一个式I的环受限氨基酸替代物：其中R1，R2，R3，R4，R5，R6，R7，R8和y 以及用于合成式I的环受限制的氨基酸替代物的方法和包含其的肽模拟物的方法，以及使用肽模拟物治疗各种疾病，综合征和病症的方法。
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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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