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1. 发明申请

US20060160765A1 Inhibitors of nucleoside phosphorylases and nucleosidases 有权
标题翻译：核苷磷酸酶和核苷酸的抑制剂
公开(公告)号：US20060160765A1
公开(公告)日：2006-07-20
申请号：US10524995
申请日：2003-08-21
申请人： Gary Evans , Richard Hubert , Dirk Lenz , Vern Schramm , Peter Tyler , Olga Zubkova
发明人： Gary Evans , Richard Hubert , Dirk Lenz , Vern Schramm , Peter Tyler , Olga Zubkova
IPC分类号： A61K31/7076 , A61K31/519 , C07H19/16 , A61K31/655 , C07D487/02
CPC分类号： C07D473/30 , C07D473/34 , C07H19/23
摘要： The present invention relates to compounds of the general formula (I) which are inhibitors of purine muclioside phosphorylases (PNP), purine phosphoribosyltransferases (PPRT), 5′-methylthioadenosine phosphorylases (MTAP), 5′-methylthioadenosine mucliosidases (MTAN) and/or nucleoside hydrolases (NH). The invention also relates to the use of these compounds in the treatment of diseases and infections including cancer, bacterial infections, protozoal infections, and T-cell mediated disease and to pharmaceutical compositions containing the compounds.
摘要翻译：本发明涉及作为嘌呤粘蛋白磷酸化酶（PNP），嘌呤磷酸核糖基转移酶（PPRT），5'-甲硫基腺苷磷酸化酶（MTAP），5'-甲硫基腺苷粘蛋白酶（MTAN）和/或核苷水解酶（NH）。本发明还涉及这些化合物在治疗包括癌症，细菌感染，原生动物感染和T细胞介导的疾病的疾病和感染中的用途以及含有该化合物的药物组合物。

2. 发明申请

US20070269448A1 Transition State Analog Inhibitors Of Ricin A-Chain 失效
标题翻译：蓖麻毒素A链过渡态模拟抑制剂
公开(公告)号：US20070269448A1
公开(公告)日：2007-11-22
申请号：US10570673
申请日：2004-09-09
申请人： Vern Schramm , Richard Furneaux , Peter Tyler , Gary Evans
发明人： Vern Schramm , Richard Furneaux , Peter Tyler , Gary Evans
IPC分类号： A61K39/395 , A61K31/7076 , A61P35/00 , C07H19/16
CPC分类号： C12N15/11 , C12N2310/13 , C12N2310/323 , C12N2310/333 , C12N2310/53
摘要： Improved transition state analog inhibitors of ricin toxin-A are provided. Methods of using those inhibitors to inhibit ricin toxin-A and to prevent the toxic effects of rich toxin-A in a mammal are also provided.
摘要翻译：提供了改进的蓖麻毒素-A的过渡态类似物抑制剂。还提供了使用这些抑制剂来抑制蓖麻毒素-A并且防止浓毒素-A在哺乳动物中的毒性作用的方法。

3. 发明申请

US20070197561A1 Inhibitors of nucleoside metabolism 有权
标题翻译：核苷代谢抑制剂
公开(公告)号：US20070197561A1
公开(公告)日：2007-08-23
申请号：US11728730
申请日：2007-03-26
申请人： Richard Furneaux , Peter Tyler , Vern Schramm
发明人： Richard Furneaux , Peter Tyler , Vern Schramm
IPC分类号： A61K31/519 , C07D487/02
CPC分类号： C07D487/04 , C07H19/04
摘要： The present invention provides compounds having the formula: wherein A is CH or N; B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H, halogen or SCH3; R is an optionally substituted alkyl, aralkyl or aryl group; and X and Y are independently selected from H, OH or halogen except that when one of X and Y is hydroxy or halogen, the other is hydrogen; and Z is OH or, when X is hydroxy, Z is selected from hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof; and compounds having the formula: wherein A, X, Y, Z and R are defined for compounds of formula (I) where first shown above; E is chosen from CO2H or a corresponding salt form, CO2R, CN, CONH2, CONHR or CONR2; and G is chosen from NH2, NHCOR, NHCONHR or NHCSNHR; or a tautomer thereof, or a pharmaceutically acceptable salt thereof, or an ester thereof, or a prodrug thereof. The present invention also provides the use of the above compounds as pharmaceuticals, pharmaceutical compositions containing the compounds and processes for preparing the compounds.
摘要翻译：本发明提供具有下式的化合物：其中A是CH或N; B选自OH，NH 2，NHR，H或卤素; D选自OH，NH 2，NHR，H，卤素或SCH 3; R是任选取代的烷基，芳烷基或芳基; X和Y独立地选自H，OH或卤素，除了当X和Y中的一个是羟基或卤素时，另一个是氢; Z为OH或当X为羟基时，Z选自氢，卤素，羟基，SQ或OQ，Q为任选取代的烷基，芳烷基或芳基; 或其互变异构体; 或其药学上可接受的盐; 或其酯; 或其前药; 和具有下式的化合物：其中A，X，Y，Z和R定义为其中首先显示的式（I）化合物; E选自CO 2 H或相应的盐形式，CO 2 R，CN，CONH 2，CONHR或CONR 2 并且G选自NH 2，NHCOR，NHCONHR或NHCSNHR; 或其互变异构体，或其药学上可接受的盐或其酯，或其前药。本发明还提供了上述化合物作为药物，含有该化合物的药物组合物和制备该化合物的方法的用途。

4. 发明申请

US20070015772A1 Nucleoside metabolism inhibitors 审中-公开
标题翻译：核苷代谢抑制剂
公开(公告)号：US20070015772A1
公开(公告)日：2007-01-18
申请号：US11486954
申请日：2006-07-13
申请人： Richard Furneaux , Peter Tyler , Vern Schramm
发明人： Richard Furneaux , Peter Tyler , Vern Schramm
IPC分类号： C07D487/02 , A61K31/519
CPC分类号： C07H19/14
摘要： The present invention provides a compound of formula (I), wherein: A is selected from N, CH and CR, where R is selected from halogen, optionally substituted alkyl, aralkyl and aryl, OH, NH2, NHR1, NR1R2 and SR3, where R1, R2 and R3 are each optionally substituted alkyl, aralkyl or aryl groups; B is selected from OH, NH2, NHR4, H and halogen, where R4 is an optionally substituted alkyl, aralkyl or aryl group; D is selected from OH, NH2, NHR5, H, halogen and SCH3, where R5 is an optionally substituted alkyl, aralkyl or aryl group; X and Y are independently selected from H, OH and halogen, with the proviso that when one of X and Y is hydroxy or halogen, the other is hydrogen; Z is OH, or, when X is hydroxy, Z is selected from hydrogen, halogen, hydroxy, SQ and OQ, where Q is an optionally substituted alkyl, aralkyl or aryl group; and W is OH or H, with the proviso that when W is OH, then A is CR where R is as defined above; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof. The invention also provides a pharmaceutical composition comprising a compound of formula (I), as well as methods of treatment using a compound of formula (I). The invention further provides methods of preparing compounds of formula (I).
摘要翻译：本发明提供式（I）化合物，其中：A选自N，CH和CR，其中R选自卤素，任选取代的烷基，芳烷基和芳基，OH，NH 2，，NHR 1，NR 1，R 2和SR 3，其中R 1， R 2和R 3各自为任选取代的烷基，芳烷基或芳基; B选自OH，NH 2，NHR 4，H和卤素，其中R 4是任选取代的烷基，芳烷基或芳基 ; D选自OH，NH 2，NHR 5，H，卤素和SCH 3，其中R 5，是任选取代的烷基，芳烷基或芳基; X和Y独立地选自H，OH和卤素，条件是当X和Y中的一个是羟基或卤素时，另一个是氢; Z是OH，或当X是羟基时，Z选自氢，卤素，羟基，SQ和OQ，其中Q是任选取代的烷基，芳烷基或芳基; 并且W是OH或H，条件是当W是OH时，则A是CR，其中R如上定义; 或其互变异构体; 或其药学上可接受的盐; 或其酯; 或其前药。本发明还提供了包含式（I）化合物的药物组合物，以及使用式（I）化合物的治疗方法。本发明还提供制备式（I）化合物的方法。

5. 发明申请

US20050026936A1 Inhibitors of nucleoside metabolism 有权
标题翻译：核苷代谢抑制剂
公开(公告)号：US20050026936A1
公开(公告)日：2005-02-03
申请号：US10932841
申请日：2004-09-02
申请人： Richard Furneaux , Peter Tyler , Vern Schramm
发明人： Richard Furneaux , Peter Tyler , Vern Schramm
IPC分类号： C07D487/04 , A01N43/04 , A01N61/00 , A61K31/519 , A61P33/06 , A61P37/06 , A61P43/00 , C07D207/34 , C07D403/04 , C07D487/02 , C07H19/00 , C07H19/04 , C07H21/00
CPC分类号： C07D487/04 , C07H19/04
摘要： The present invention provides compounds having the formula: wherein A is CH or N; B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H, halogen or SCH3; R is an optionally substituted alkyl, aralkyl or aryl group; and X and Y are independently selected from H, OH or halogen except that when one of X and Y is hydroxy or halogen, the other is hydrogen; and Z is OH or, when X is hydroxy, Z is selected from hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof; and compounds having the formula: wherein A, X, Y, Z and R are defined for compounds of formula (I) where first shown above; E is chosen from CO2H or a corresponding salt form, CO2R, CN, CONH2, CONHR or CONR2; and G is chosen from NH2, NHCOR, NHCONHR or NHCSNHR; or a tautomer thereof, or a pharmaceutically acceptable salt thereof, or an ester thereof, or a prodrug thereof. The present invention also provides the use of the above compounds as pharmaceuticals, pharmaceutical compositions containing the compounds and processes for preparing the compounds.
摘要翻译：本发明提供具有下式的化合物：其中A是CH或N; B选自OH，NH2，NHR，H或卤素; D选自OH，NH 2，NHR，H，卤素或SCH 3; R是任选取代的烷基，芳烷基或芳基; X和Y独立地选自H，OH或卤素，除了当X和Y中的一个是羟基或卤素时，另一个是氢; Z为OH或当X为羟基时，Z选自氢，卤素，羟基，SQ或OQ，Q为任选取代的烷基，芳烷基或芳基; 或其互变异构体; 或其药学上可接受的盐; 或其酯; 或其前药; 和具有下式的化合物：其中A，X，Y，Z和R定义为其中首先显示的式（I）化合物; E选自CO 2 H或相应的盐形式，CO 2 R，CN，CONH 2，CONHR或CONR 2; G选自NH2，NHCOR，NHCONHR或NHCSNHR; 或其互变异构体，或其药学上可接受的盐或其酯，或其前药。本发明还提供了上述化合物作为药物，含有该化合物的药物组合物和制备该化合物的方法的用途。

6. 发明申请

US20070161667A1 Process for preparing inhibitors of nucleoside metabolism 有权
标题翻译：制备核苷代谢抑制剂的方法
公开(公告)号：US20070161667A1
公开(公告)日：2007-07-12
申请号：US11716100
申请日：2007-03-09
申请人： Richard Furneaux , Peter Tyler , Vern Schramm
发明人： Richard Furneaux , Peter Tyler , Vern Schramm
IPC分类号： A61K31/519 , C07D487/02
CPC分类号： C07D207/416 , C07D487/04 , C07H19/14 , Y02P20/55
摘要： A process of preparing a compound of the formula (I) wherein B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H halogen or SCH3; R is an optionally substituted alkyl, aralkyl or aryl group; and Z is selected from OH, hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof, which comprises reacting a compound of the formula (II) with an anion produced by abstraction of the bromine or iodine atom from a compound of formula (XIX),
摘要翻译：制备式（I）化合物的方法，其中B选自OH，NH 2，NHR，H或卤素; D选自OH，NH 2，NHR，H卤素或SCH 3; R是任选取代的烷基，芳烷基或芳基; Z选自OH，氢，卤素，羟基，SQ或OQ，Q是任选取代的烷基，芳烷基或芳基; 或其互变异构体; 或其药学上可接受的盐; 或其酯; 或其前药，其包括使式（II）的化合物与通过从式（XIX）的化合物中提取溴或碘原子产生的阴离子反应，

7. 发明申请

US20060089498A1 Process for preparing inhibitors of nucleoside metabolism 有权
标题翻译：制备核苷代谢抑制剂的方法
公开(公告)号：US20060089498A1
公开(公告)日：2006-04-27
申请号：US11297954
申请日：2005-12-08
申请人： Richard Furneaux , Peter Tyler , Vern Schramm
发明人： Richard Furneaux , Peter Tyler , Vern Schramm
IPC分类号： C07D487/02
CPC分类号： C07D207/416 , C07D487/04 , C07H19/14 , Y02P20/55
摘要： A process of preparing a compound of the formula (I) wherein B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H halogen or SCH3; R is an optionally substituted alkyl, aralkyl or aryl group; and Z is selected from OH, hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof, which comprises reacting a compound of the formula (II) with an anion produced by abstraction of the bromine or iodine atom from a compound of formula (XIX), to form a compound of formula (XX) The compound of formula (XX) is N- and O-deprotected to obtain the compound of formula (I).
摘要翻译：制备式（I）化合物的方法，其中B选自OH，NH 2，NHR，H或卤素; D选自OH，NH 2，NHR，H卤素或SCH 3; R是任选取代的烷基，芳烷基或芳基; Z选自OH，氢，卤素，羟基，SQ或OQ，Q是任选取代的烷基，芳烷基或芳基; 或其互变异构体; 或其药学上可接受的盐; 或其酯; 其包括使式（II）的化合物与通过从式（XIX）的化合物中提取溴或碘原子产生的阴离子反应形成式（XX）的化合物。式（XX）是N-和O-去保护的，得到式（I）化合物。

8. 发明申请

US20070275988A1 Transition state structure and inhibitors of thymidine phosphorylases 审中-公开
标题翻译：过渡态结构和胸苷磷酸酶抑制剂
公开(公告)号：US20070275988A1
公开(公告)日：2007-11-29
申请号：US10570475
申请日：2004-09-03
申请人： Vern Schramm
发明人： Vern Schramm
IPC分类号： A61K31/513 , A61K31/427 , C07D417/02 , C07D403/02
CPC分类号： C07D277/56 , A61K31/427 , A61K31/506 , C07D401/06 , C07D403/06 , C07D417/04 , C07D417/06 , C07F9/6512 , C07F9/6536 , C07F9/65586 , C12Q1/48 , G01N2333/91142
摘要： The transition state structure of thymidine phosphorylase is provided, along with thymidine phosphorylase inhibitors that resemble the charge and geometry of the thymidine phosphorylase transition state. Also provided are methods of inhibiting a thymidine phosphorylase, methods of treating cancer, and methods of inhibiting angiogenesis which utilize the thymidine phosphorylase transition state inhibitors.
摘要翻译：提供了胸苷磷酸化酶的过渡态结构，以及胸苷磷酸化酶抑制剂，其类似于胸苷磷酸化酶转变状态的电荷和几何形状。还提供了抑制胸苷磷酸化酶的方法，治疗癌症的方法，以及利用胸苷磷酸化酶过渡状态抑制剂抑制血管发生的方法。

9. 发明申请

US20060084616A1 Inhibitors of ADP-ribosyl transferases, cyclases, and hydrolases, and uses thereof 失效
公开(公告)号：US20060084616A1
公开(公告)日：2006-04-20
申请号：US11294932
申请日：2005-12-05
申请人： Anthony Sauve , Vern Schramm
发明人： Anthony Sauve , Vern Schramm
IPC分类号： A61K31/7052 , C07H19/048 , A61K31/7072
CPC分类号： C07D405/04 , C07D307/20 , C07H19/04 , C07H19/10 , C07H19/20
摘要： The present invention provides compounds having the formula: wherein A is chosen from a nitrogen-, oxygen-, or sulfur-linked aryl, alkyl, cyclic, or heterocyclic group; both B and C are hydrogen, or either B or C is a halogen, amino, or thiol group and the other of B or C is hydrogen; and D is a primary alcohol, a hydrogen, or an oxygen, nitrogen, carbon, or sulfur linked to phosphate, a phosphoryl group, a pyrophosphoryl group, or adenosine monophosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted phosphodiester bridge, or to adenosine diphosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted pyrophosphodiester bridge. The present invention also provides pharmaceutical compositions containing the above compounds, methods of using the above compounds as pharmaceuticals, and processes for preparing the above compounds. Also provided are methods for inhibiting an ADP-ribosyl transferase, ADP-ribosyl cyclase, or ADP-ribosyl hydrolase enzyme, and methods for treating a disease or condition associated with an ADP-ribosyl transferase, ADP-ribosyl cyclase, or ADP-ribosyl hydrolase enzyme in a subject in need of treatment thereof.

10. 发明申请

US20060094670A1 Inhibitors of ADP-ribosyl transferases, cyclases, and hydrolases 审中-公开
公开(公告)号：US20060094670A1
公开(公告)日：2006-05-04
申请号：US11295120
申请日：2005-12-05
申请人： Anthony Sauve , Vern Schramm
发明人： Anthony Sauve , Vern Schramm
IPC分类号： A61K31/7056 , C07H19/048 , C07H19/056
CPC分类号： C07H19/052 , C07H19/048
摘要： The present invention provides compounds having the formula: wherein A is a nitrogen-, oxygen-, or sulfur-linked aryl, alkyl, cyclic, or heterocyclic group, the group being further substituted with an electron contributing moiety; B is hydrogen, or a halogen, amino, or thiol group; C is hydrogen, or a halogen, amino, or thiol group; and D is a primary alcohol, a hydrogen, or an oxygen, nitrogen, carbon, or sulfur linked to phosphate, a phosphoryl group, a pyrophosphoryl group, or adenosine monophosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted phosphodiester bridge, or to adenosine diphosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted pyrophosphodiester bridge. The present invention also provides pharmaceutical compositions containing the above compounds, methods of using the above compounds as pharmaceuticals, and processes for preparing the above compounds. Also provided are methods for inhibiting an ADP-ribosyl transferase, ADP-ribosyl cyclase, ADP-ribosyl hydrolase, or NAD-dependent deacetylase enzyme, and methods for treating a disease or condition associated with an ADP-ribosyl transferase, ADP-ribosyl cyclase, ADP-ribosyl hydrolase, or NAD-dependent deacetylase enzyme in a subject in need of treatment thereof.

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