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1.发明授权Buforin I as a specific inhibitor and therapeutic agent for botulinum toxin B and tetanus neurotoxins 失效Buforin I作为特异性抑制剂和肉毒杆菌毒素B和破伤风神经毒素的治疗剂公开(公告)号：US06713444B1
公开(公告)日：2004-03-30
申请号：US09570023
申请日：2000-05-12
IPC分类号： A61K3800
CPC分类号： C07K14/8146 , A61K38/00
摘要： The compounds of the invention are generally described by the formula: X1X2B3X4B5X*6X7X8 B9X10B11X12B13X14 B15X16B17X*18X*19B20 X21X22X23Q24F25Z*26X27 X28B29X30B31B32X33X34 B35B36X37Z38Z39 (1) and the salts, esters, amides, and acyl forms thereof. Up to 15 amino acids may be truncated from the N-terminus and up to 6 amino acids may be truncated from the C-terminus. Each position represented by a letter indicates a single amino acid residue wherein B is a basic or polar/large amino acid or a modified form thereof; X is a small or hydrophobic amino acid or a modified form thereof; X* is a small or polar/large amino acid or a modified form thereof; Z is a polar/large or hydrophobic amino acid or a modified form thereof; Z* is Proline or a polar/large or hydrophobic amino acid or a modified form thereof. These compounds may be used to inhibit the protease activity of Botulinum B and tetanus toxins.
摘要翻译： 本发明的化合物通常用下式描述：及其盐，酯，酰胺及其酰基形式。 可以从N末端截断至多15个氨基酸，并且可以从C末端截断至多6个氨基酸。 由字母表示的每个位置表示单个氨基酸残基，其中B是碱性或极性/大氨基酸或其修饰形式; X是小或疏水性氨基酸或其修饰形式; X *是小或极/大氨基酸或其修饰形式; Z是极性/大或疏水性氨基酸或其修饰形式; Z *是脯氨酸或极性/大或疏水性氨基酸或其修饰形式。 这些化合物可用于抑制肉毒杆菌B和破伤风毒素的蛋白酶活性。
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2.发明授权Previns as specific inhibitors and therapeutic agents for Botulinum toxin B and Tetanus neurotoxins 失效前列腺素作为肉毒杆菌毒素B和破伤丹神经毒素的特异性抑制剂和治疗剂公开(公告)号：US06573244B1
公开(公告)日：2003-06-03
申请号：US09570022
申请日：2000-05-12
IPC分类号： A61K3800
CPC分类号： C07K7/06 , A61K38/00 , C07K7/08 , C07K7/22 , C07K14/8146
摘要： The compounds of the invention are generally described by the formula: B1Z*2B3Z*4X*5Q6F7X8X9X10X11 (1), B1X2X3X4X5Q6F7X8X9X10X11 (2), or B1X2B3X4Z5Q6F7Z*8X9X10X11 (3) and the salts, esters, amides, and acyl forms thereof. Each position represented by a letter indicates a single amino acid residue: B is a basic or polar/large amino acid or a modified form thereof; X is a small or hydrophobic amino acid or a modified form thereof; X* is a small or polar/large amino acid or a modified form thereof; Z is a polar/large or hydrophobic amino acid or a modified form thereof; Z* is Proline or a polar/large or hydrophobic amino acid or a modified form thereof. As described below, one or more of the peptide linkages between the amino acid residues may be replaced by a peptide linkage mimic. These compounds may be used as molecular building blocks to create compounds that are optimized for inhibiting the protease activity of Botulinum B and tetanus toxins.
摘要翻译： 本发明的化合物通常用下式描述：或其盐，酯，酰胺及其酰基形式。 由字母表示的每个位置表示单个氨基酸残基：B是碱性或极性/大氨基酸或其修饰形式; X是小或疏水性氨基酸或其修饰形式; X *是小或极/大氨基酸或其修饰形式; Z是极性/大或疏水性氨基酸或其修饰形式; Z *是脯氨酸或极性/大或疏水性氨基酸或其修饰形式。 如下所述，氨基酸残基之间的一个或多个肽键可以被肽键模拟物代替。这些化合物可以用作分子结构单元以产生针对抑制肉毒杆菌B和破伤风的蛋白酶活性而优化的化合物 毒素
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3.发明授权Previns as specific inhibitors and therapeutic agents for botulinum toxin B and tetanus neurotoxins 失效前列腺素作为肉毒杆菌毒素B和破伤风神经毒素的特异性抑制剂和治疗剂公开(公告)号：US07235521B1
公开(公告)日：2007-06-26
申请号：US09979101
申请日：2000-05-15
IPC分类号： A61K38/00
CPC分类号： C12Q1/37 , G01N2333/95 , G01N2500/00
摘要： The compounds of the invention are generally described by the formula (1): B1Z*2B3Z*4X*5Q6F7X8X9X10X11, (2): B1X2X3X4X5Q6F7X8X9X10X11, or (3): B1X2B3X4Z5Q6F7Z8X9X10X11 and the salts, esters, amides, and acyl forms thereof. Each position represented by a letter indicates a single amino acid residue: B is a basic or polar/large amino acid or a modified form thereof; X is a small or hydrophobic amino acid or a modified form thereof; X* is a small or polar/large amino acid or a modified form thereof; Z is a polar/large or hydrophobic amino acid or a modified form thereof; Z* is Proline or a polar/large or hydrophobic amino acid or a modified form thereof. As described below, one or more of the peptide linkages between the amino acid residues may be replaced by a peptide linkage mimic. These compounds may be used as molecular building blocks to create compounds that are optimized for inhibiting the protease activity of Botulinum B and tetanus toxins.
摘要翻译： 本发明的化合物通常由式（1）描述：B 1 Z * 2 B 3 Z * 4 < 5×6×6×6××××××××××××××××××××××××××××××××××××××××××< （2）：B 1 X 2 X 3 X 2 X 2 X 3 5 5 5 或（3）：B 1 X 2 B 3 3 5 X 5 5 5 它们的盐，酯，酰胺和酰基形式。 由字母表示的每个位置表示单个氨基酸残基：B是碱性或极性/大氨基酸或其修饰形式; X是小或疏水性氨基酸或其修饰形式; X *是小或极/大氨基酸或其修饰形式; Z是极性/大或疏水性氨基酸或其修饰形式; Z *是脯氨酸或极性/大或疏水性氨基酸或其修饰形式。 如下所述，氨基酸残基之间的一个或多个肽键可以被肽键模拟物代替。 这些化合物可用作分子结构单元以产生针对抑制肉毒杆菌B和破伤风毒素的蛋白酶活性而优化的化合物。
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4.发明授权公开(公告)号：US07375079B2
公开(公告)日：2008-05-20
申请号：US11268757
申请日：2005-11-04
IPC分类号： A61K38/00
CPC分类号： C07K7/06 , A61K38/00 , C07K7/08 , C07K7/22 , C07K14/8146
摘要： The compounds of the invention are generally described by the formula: B1Z*2B3Z*4X*5Q6F7X8X9X10X11, (1) B1X2X3X4X5Q6F7X8X9X10X11, or (2) B1Z2B3X4Z5Q6F7Z8X9X10X11 (3) and the salts, esters, amides, and acyl forms thereof. Each position represented by a letter indicates a single amino acid residue: B is a basic of polar/large amino acid or a modified form thereof; X is a small or hydrophobic amino acid or a modified form thereof; X* is a small or polar/large amino acid or a modified form thereof; Z is a polar/large or hydrophobic amino acid or a modified form thereof; Z* is Proline or a polar/large of hydrophobic amino acid or a modified form thereof. As described below, one or more of the peptide linkages between the amino acid residues may be replaced by a peptide linkage mimic. These compounds may be used as molecular building blocks to create compounds that are optimized for inhibiting the protease activity of Botulinum b and tetanus toxins.
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