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公开(公告)号：US06787315B2
公开(公告)日：2004-09-07
申请号：US10209692
申请日：2002-07-31
IPC分类号： C12Q168
CPC分类号： G01N33/6842 , C12Q1/6811 , G01N33/566 , G01N33/6848 , G01N2500/02
摘要： Methods of identifying ligand binding sites in a target molecule such as a polynucleotide or polypeptide, as well as methods for determining whether a particular site in a target molecule is at or near the ligand binding site, are provided. Ligand binding affinities corresponding to both the target molecule and a modified version thereof are compared, preferably using mass spectral analysis. The modified molecules, or test molecules, incorporate a modification capable of modulating ligand binding affinity when located at or near the ligand binding sites. Binding site information is derived from the known position of the modification.
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公开(公告)号：US08207173B2
公开(公告)日：2012-06-26
申请号：US12620307
申请日：2009-11-17
IPC分类号： A61P31/14 , A61K31/415 , C07D491/00
CPC分类号： C07D401/04 , C04B35/632 , C07B2200/11 , C07D235/30 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D473/00 , C07D487/04 , C07D491/04 , C07D491/14
摘要： Provided are compounds of the formula: wherein RN1 is a substituent of formula G1-NX1X2, wherein G1 is an optionally further substituted alkylene, which optionally forms, together with RN2, a cyclic group, and each of X1 and X2 is independently H or an N-substituent, or X1 and X2 together form a heterocyclic ring, or X1 together with G1 forms a cyclic group and X2 is H or an N-substituent; and each of Z1, Z2, Z3 and Z4 is H or a substituent, or two of Z1, Z2, Z3 and Z4 together form an optionally substituted ring, and further wherein at least one of Z1, Z2, Z3 and Z4 is other than H, and salts thereof, pharmaceutical compositions and methods of using the compounds. The compounds have antiviral activity.
摘要翻译： 提供下式的化合物：其中RN1是式G1-NX1X2的取代基，其中G1是任选进一步取代的亚烷基，其任选地与RN2一起形成环状基团，并且X 1和X 2各自独立地为H或 X取代基或X1和X2一起形成杂环，或者X1与G1一起形成环状基团，X 2是H或N-取代基; Z1，Z2，Z3和Z4各自为H或取代基，Z1，Z2，Z3和Z4中的两个一起形成任选取代的环，其中Z1，Z2，Z3和Z4中的至少一个不是 H及其盐，药物组合物和使用该化合物的方法。 该化合物具有抗病毒活性。
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公开(公告)号：US20100130513A1
公开(公告)日：2010-05-27
申请号：US12620307
申请日：2009-11-17
IPC分类号： A61K31/4188 , C07D491/048 , C07D491/147 , A61K31/519 , C12N7/00
CPC分类号： C07D401/04 , C04B35/632 , C07B2200/11 , C07D235/30 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D473/00 , C07D487/04 , C07D491/04 , C07D491/14
摘要： Provided are compounds of the formula: wherein RN1 is a substituent of formula G1-NX1X2, wherein G1 is an optionally further substituted alkylene, which optionally forms, together with RN2, a cyclic group, and each of X1 and X2 is independently H or an N-substituent, or X1 and X2 together form a heterocyclic ring, or X1 together with G1 forms a cyclic group and X2 is H or an N-substituent; and each of Z1, Z2, Z3 and Z4 is H or a substituent, or two of Z1, Z2, Z3 and Z4 together form an optionally substituted ring, and further wherein at least one of Z1, Z2, Z3 and Z4 is other than H, and salts thereof, pharmaceutical compositions and methods of using the compounds. The compounds have antiviral activity.
摘要翻译： 提供下式的化合物：其中RN1是式G1-NX1X2的取代基，其中G1是任选进一步取代的亚烷基，其任选地与RN2一起形成环状基团，并且X 1和X 2各自独立地为H或 X取代基或X1和X2一起形成杂环，或者X1与G1一起形成环状基团，X 2是H或N-取代基; Z1，Z2，Z3和Z4各自为H或取代基，Z1，Z2，Z3和Z4中的两个一起形成任选取代的环，其中Z1，Z2，Z3和Z4中的至少一个不是 H及其盐，药物组合物和使用该化合物的方法。 该化合物具有抗病毒活性。
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公开(公告)号：US07642265B2
公开(公告)日：2010-01-05
申请号：US10946757
申请日：2004-09-22
IPC分类号： A61P31/12 , A61K31/4188 , C07D491/12
CPC分类号： C07D401/04 , C04B35/632 , C07B2200/11 , C07D235/30 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D473/00 , C07D487/04 , C07D491/04 , C07D491/14
摘要： Provided are compounds of the formula: wherein RN1 is a substituent of formula G1—NX1X2, wherein G1 is an optionally further substituted alkylene, which optionally forms, together with RN2, a cyclic group, and each of X1 and X2 is independently H or an N-substituent, or X1 and X2 together form a heterocyclic ring, or X1 together with G1 forms a cyclic group and X2 is H or an N-substituent; and each of Z1, Z2, Z3 and Z4 is H or a substituent, or two of Z1, Z2, Z3 and Z4 together form an optionally substituted ring, and further wherein at least one of Z1, Z2, Z3 and Z4 is other than H, and salts thereof, pharmaceutical compositions and methods of using the compounds. The compounds have antiviral activity.
摘要翻译： 提供下式的化合物：其中RN1是式G1-NX1X2的取代基，其中G1是任选进一步取代的亚烷基，其任选地与RN2一起形成环状基团，并且X 1和X 2各自独立地为H或 X取代基或X1和X2一起形成杂环，或者X1与G1一起形成环状基团，X 2是H或N-取代基; Z1，Z2，Z3和Z4各自为H或取代基，Z1，Z2，Z3和Z4中的两个一起形成任选取代的环，其中Z1，Z2，Z3和Z4中的至少一个不是 H及其盐，药物组合物和使用该化合物的方法。 该化合物具有抗病毒活性。
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公开(公告)号：US06933288B2
公开(公告)日：2005-08-23
申请号：US10067017
申请日：2002-02-04
IPC分类号： A61K31/506 , A61K31/519 , A61K38/00 , C07D405/04 , C07H19/06 , C07K5/02 , C07D407/04 , A61K31/7068
CPC分类号： C07D405/04 , A61K31/506 , A61K31/519 , A61K38/00 , C07H19/06 , C07K5/0202 , C07K5/021
摘要： This invention is directed to novel pyranosyl cytosine compounds depicted graphically as structure I. This invention is further directed to a unique methodology for their preparation using solid-phase methodology. These hexopyranosyl cytosine derived natural product analogs share their parent compounds broad-spectrum antimicrobial and anti-fungal profile and represent a vast, novel compound class of 50S rRNA directed inhibitors of protein translation.
摘要翻译： 本发明涉及以图形方式描绘为结构I的新型吡喃糖基胞嘧啶化合物。本发明进一步涉及使用固相方法制备其独特的方法。 这些六吡喃糖基胞嘧啶衍生的天然产物类似物共享其母体化合物广谱抗微生物和抗真菌分布，代表了广泛的新型化合物类型的50S rRNA定向的蛋白质翻译抑制剂。
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86.发明授权Antibacterial 4,6-substituted 6′, 6″ and 1 modified aminoglycoside analogs 失效抗菌4,6-取代的6'，6“和1个修饰的氨基糖苷类似物公开(公告)号：US08377896B2
公开(公告)日：2013-02-19
申请号：US13044226
申请日：2011-03-09
CPC分类号： C07H15/234
摘要： The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.
摘要翻译： 本发明涉及氨基糖苷类化合物的类似物以及它们作为抗微生物感染的预防或治疗剂的制备和用途。
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87.发明申请ANTIBACTERIAL 4,5-SUBSTITUTED AMINOGLYCOSIDE ANALOGS HAVING MULTIPLE SUBSTITUENTS 有权具有多种替代物的抗体4,5-取代的氨基酰胺类似物公开(公告)号：US20130005674A1
公开(公告)日：2013-01-03
申请号：US13344247
申请日：2012-01-05
申请人： Eric E. Swayze , Stephen Hanessian , Janek Szychowski , Susanta Sekhar Adhikari , Kandasamy Pachamuthu , Xiaojing Wang , Michael T. Migawa , Richard H. Griffey
发明人： Eric E. Swayze , Stephen Hanessian , Janek Szychowski , Susanta Sekhar Adhikari , Kandasamy Pachamuthu , Xiaojing Wang , Michael T. Migawa , Richard H. Griffey
IPC分类号： A61K31/7036 , A61P31/04
CPC分类号： C07H15/23 , C07H15/232
摘要： The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.
摘要翻译： 本发明涉及氨基糖苷类化合物的类似物以及它们作为抗微生物感染的预防或治疗剂的制备和用途。
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88.发明申请ANTIBACTERIAL 4,6-SUBSTITUTED 6', 6" AND 1 MODIFIED AMINOGLYCOSIDE ANALOGS 失效抗菌素4,6-取代6'，6“和1修饰的氨基酰胺类似物公开(公告)号：US20110245476A1
公开(公告)日：2011-10-06
申请号：US13044226
申请日：2011-03-09
IPC分类号： C07H15/234
CPC分类号： C07H15/234
摘要： The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.
摘要翻译： 本发明涉及氨基糖苷类化合物的类似物以及它们作为抗微生物感染的预防或治疗剂的制备和用途。
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89.发明授权Antibacterial 4,5-substituted aminoglycoside analogs having multiple substituents 有权具有多个取代基的抗菌的4,5-取代的氨基糖苷类似物公开(公告)号：US07893039B2
公开(公告)日：2011-02-22
申请号：US12130048
申请日：2008-05-30
申请人： Eric E. Swayze , Stephen Hanessian , Janek Szychowski , Susanta Sekhar Adhikari , Kandasamy Pachamuthu , Xiaojing Wang , Michael T. Migawa , Richard H. Griffey
发明人： Eric E. Swayze , Stephen Hanessian , Janek Szychowski , Susanta Sekhar Adhikari , Kandasamy Pachamuthu , Xiaojing Wang , Michael T. Migawa , Richard H. Griffey
IPC分类号： A01N43/04 , A61K31/715
CPC分类号： C07H15/23 , C07H15/232
摘要： The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.
摘要翻译： 本发明涉及氨基糖苷类化合物的类似物以及它们作为抗微生物感染的预防或治疗剂的制备和用途。
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公开(公告)号：US06730485B2
公开(公告)日：2004-05-04
申请号：US10210684
申请日：2002-07-31
IPC分类号： C12Q168
CPC分类号： G01N33/6842 , C12Q1/6811 , G01N33/566 , G01N33/6848 , G01N2500/02
摘要： Methods of identifying ligand binding sites in a target molecule such as a polynucleotide or polypeptide, as well as methods for determining whether a particular site in a target molecule is at or near the ligand binding site, are provided. Ligand binding affinities corresponding to both the target molecule and a modified version thereof are compared, preferably using mass spectral analysis. The modified molecules, or test molecules, incorporate a modification capable of modulating ligand binding affinity when located at or near the ligand binding sites. Binding site information is derived from the known position of the modification.
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