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1. 发明申请

WO2008079028A1 AZETIDINE ANALOGUES OF NUCLEOSIDASE AND PHOSPHORYLASE INHIBITORS 审中-公开
标题翻译：核苷酸酶和磷酸酶抑制剂的AZETIDINE ANALOGUES
公开(公告)号：WO2008079028A1
公开(公告)日：2008-07-03
申请号：PCT/NZ2007/000387
申请日：2007-12-21
申请人： INDUSTRIAL RESEARCH LIMITED , ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY , EVANS, Gary Brian , FURNEAUX, Richard Hubert , GREATREX, Ben William , SCHRAMM, Vern L. , TYLER, Peter Charles
发明人： EVANS, Gary Brian , FURNEAUX, Richard Hubert , GREATREX, Ben William , SCHRAMM, Vern L. , TYLER, Peter Charles
IPC分类号： C07D403/14 , C07D401/02 , C07D401/04 , C07D401/06 , C07D405/14
CPC分类号： C07D471/04
摘要： Azetidine analogues of nucleosidase and nucleoside phosphorylase inhibitors having the general formula (I), the use of these compounds as pharmaceuticals, pharmaceutical compositions containing the compounds, methods of treating certain diseases using the compounds, processes for preparing the compounds, and intermediates useful in the preparation of the compounds wherein W and X are each independently selected from hydrogen, CH 2 OH, CH 2 OQ and CH 2 SQ; Y and Z are each independently selected from hydrogen, halogen, CH 2 OH, CH 2 OQ, CH 2 SQ, SQ, OQ and Q; Q is an alkyl, aralkyl or aryl group each of which may be optionally substituted with one or more substituents selected from hydroxy, halogen, methoxy, amino, or carboxy; R 1 is a radical of the formula (II) or R 1 is a radical of the formula (III) A is selected from N, CH and CR 2 , where R 2 is selected from halogen, alkyl, aralkyl, aryl, OH, NH 2 , NHR 3 , NR 3 R 4 and SR 5 , where R 3 , R 4 and R 5 are each alkyl, aralkyl or aryl groups optionally substituted with hydroxy or halogen, and where R 2 is optionally substituted with hydroxy or halogen when R 2 is alkyl, aralkyl or aryl; B is selected from hydroxy, NH 2 , NHR 6 , SH, hydrogen and halogen, where R 6 is an alkyl, aralkyl or aryl group optionally substituted with hydroxy or halogen; D is selected from hydroxy, NH 2 , NHR 7 , hydrogen, halogen and SCH 3 , where R 7 is an alkyl, aralkyl or aryl group optionally substituted with hydroxy or halogen; E is selected from N and CH; G is a C 1-4 saturated or unsaturated alkyl group optionally substituted with hydroxy or halogen, or G is absent; or a tautomer thereof, or a pharmaceutically acceptable salt thereof, or an ester thereof, or a prodrug thereof.
摘要翻译：具有通式（I）的核苷酸的氮杂环丁烷类似物和具有通式（I）的核苷磷酸化酶抑制剂，这些化合物作为药物的用途，含有该化合物的药物组合物，使用该化合物治疗某些疾病的方法，制备该化合物的方法和用于其中W和X各自独立地选自氢，CH 2 OH，CH 2 OQ和CH 2 SQ的化合物的制备; Y和Z各自独立地选自氢，卤素，CH 2 OH，CH 2 OQ，CH 2 SQ，SQ，OQ和Q ; Q是烷基，芳烷基或芳基，其各自可以任选被一个或多个选自羟基，卤素，甲氧基，氨基或羧基的取代基取代; R 1是式（II）的基团或R 1是式（III）的基团，A选自N，CH和CR 2 其中R 2选自卤素，烷基，芳烷基，芳基，OH，NH 2，NHR 3，NR 3，其中R 3，R 4，R 4和R 4独立地为氢，任何被羟基或卤素任选取代的烷基，芳烷基或芳基，其中R 2任选地被羟基或卤素取代时，R 2，是烷基，芳烷基或芳基; B选自羟基，NH 2，NHR 6，SH，氢和卤素，其中R 6是烷基，芳烷基或芳基任选被羟基或卤素取代; D选自羟基，NH 2，NHR 7，氢，卤素和SCH 3，其中R 7，是任选被羟基或卤素取代的烷基，芳烷基或芳基; E选自N和CH; G是任选被羟基或卤素取代的C 1-4 - 饱和或不饱和烷基，或G不存在; 或其互变异构体，或其药学上可接受的盐或其酯，或其前药。

2. 发明申请

WO2007069924A1 DEAZAPURINE ANALOGS OF 4'-AZA-L-NUCLEOSIDES 审中-公开
标题翻译： 4'-氨基-L-核苷酸的DEAZAPURINE ANALOGS
公开(公告)号：WO2007069924A1
公开(公告)日：2007-06-21
申请号：PCT/NZ2006/000332
申请日：2006-12-15
申请人： INDUSTRIAL RESEARCH LIMITED , ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY , ISIS INNOVATION LIMITED , FURNEAUX, Richard Hubert , TYLER, Peter Charles , MEE, Simon Peter Harold , EVANS, Gary Brian , SCHRAMM, Vern L. , FLEET, George
发明人： FURNEAUX, Richard Hubert , TYLER, Peter Charles , MEE, Simon Peter Harold , EVANS, Gary Brian , SCHRAMM, Vern L. , FLEET, George
IPC分类号： C07D207/04 , A61P35/00 , C07D487/04 , A61K31/4025 , A61P37/02 , C07H5/04 , A61P31/04 , C07D255/02 , A61P33/02 , C07D473/34
CPC分类号： C07D487/04 , C07H5/04
摘要： The invention relates to compounds of the formula (I), which are L-enantiomeric forms of nucleoside analogues, and to pharmaceutical compositions containing the compounds, methods of treating certain diseases, including cancer, bacterial infection, parasitic infection, and T-cell mediated diseases, using the compounds, processes for preparing the compounds, and intermediates useful in the preparation of the compounds.
摘要翻译：本发明涉及式（I）化合物，其为核苷类似物的L-对映体形式，以及含有该化合物的药物组合物，治疗某些疾病的方法，包括癌症，细菌感染，寄生虫感染和T细胞介导使用化合物的疾病，制备化合物的方法和可用于制备化合物的中间体。

3. 发明申请

WO2008030119A1 ACYCLIC AMINE INHIBITORS OF NUCLEOSIDE PHOSPHORYLASES AND HYDROLASES 审中-公开
标题翻译：核苷酸磷酸盐和水解物的酰胺类抑制剂
公开(公告)号：WO2008030119A1
公开(公告)日：2008-03-13
申请号：PCT/NZ2007/000261
申请日：2007-09-07
申请人： INDUSTRIAL RESEARCH LIMITED , ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY , CLINCH, Keith , EVANS, Gary Brian , FURNEAUX, Richard Hubert , KELLY, Peter Michael , SCHRAMM, Vern L. , TYLER, Peter Charles , WOOLHOUSE, Anthony David
发明人： CLINCH, Keith , EVANS, Gary Brian , FURNEAUX, Richard Hubert , KELLY, Peter Michael , SCHRAMM, Vern L. , TYLER, Peter Charles , WOOLHOUSE, Anthony David
IPC分类号： C07D487/04 , A61P31/04 , A61P37/06 , A61K31/519 , A61P33/02 , A61P17/06 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention relates to compounds of the general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNPs) and/or nucleoside hydrolases (NHs). 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核苷磷酸化酶（PNP）和/或核苷水解酶（NHs）的抑制剂的通式（I）的化合物。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。

4. 发明申请

WO2007097648A1 METHODS OF TREATING DISEASES USING INHIBITORS OF NUCLEOSIDE PHOSPHORYLASES AND NUCLEOSIDASES 审中-公开
标题翻译：使用核苷酸磷酸酶和核苷酸抑制剂治疗疾病的方法
公开(公告)号：WO2007097648A1
公开(公告)日：2007-08-30
申请号：PCT/NZ2007/000038
申请日：2007-02-23
申请人： INDUSTRIAL RESEARCH LIMITED , ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY , FURNEAUX, Richard Hubert , TYLER, Peter Charles , EVANS, Gary Brian , SCHRAMM, Vern L.
发明人： FURNEAUX, Richard Hubert , TYLER, Peter Charles , EVANS, Gary Brian , SCHRAMM, Vern L.
IPC分类号： A61K31/519 , A61K31/7042 , A61P35/00
CPC分类号： A61K31/519 , A61K31/7042
摘要： The invention relates to treating a disease or condition in which it is desirable to inhibit 5'-methylthioadenosine phosphorylase (MTAP) and/or 5'-methylthioadenosine nucleosidase (MTAN). The invention particularly relates to the co-administration of 5'-methylthioadenosine (MTA), or a prodrug of MTA, with one or more MTAP/MTAN inhibitors. Included among the diseases treatable are prostate cancer and head and neck cancer.
摘要翻译：本发明涉及治疗期望抑制5'-甲硫基腺苷磷酸化酶（MTAP）和/或5'-甲基硫代腺苷核苷酸酶（MTAN）的疾病或病症。本发明特别涉及5-methylthioadenosine（MTA）或MTA前药与一种或多种MTAP / MTAN抑制剂的共同给药。可治疗的疾病包括前列腺癌和头颈癌。

5. 发明申请

WO2007069923A1 DEAZAPURINE ANALOGS OF 1'-AZA-L-NUCLEOSIDES 审中-公开
标题翻译： 1'-AZA-L-核苷酸的DEAZAPURINE ANALOGS
公开(公告)号：WO2007069923A1
公开(公告)日：2007-06-21
申请号：PCT/NZ2006/000331
申请日：2006-12-15
申请人： INDUSTRIAL RESEARCH LIMITED , ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY , FURNEAUX, Richard Hubert , TYLER, Peter Charles , EVANS, Gary Brian , SCHRAMM, Vern L. , CLINCH, Keith
发明人： FURNEAUX, Richard Hubert , TYLER, Peter Charles , EVANS, Gary Brian , SCHRAMM, Vern L. , CLINCH, Keith
IPC分类号： C07D207/04 , A61P35/00 , C07D487/04 , A61K31/4025 , A61P37/02 , C07H5/04 , A61P31/04 , C07D255/02 , A61P33/02 , C07D473/34
CPC分类号： C07D487/04
摘要： The invention relates to compounds of the formula (I), which are L-enantiomeric forms of nucleoside analogues, and to pharmaceutical compositions containing the compounds, methods of treating certain diseases, including cancer, bacterial infection, parasitic infection, and T-cell mediated diseases, using the compounds, processes for preparing the compounds, and intermediates useful in the preparation of the compounds.
摘要翻译：本发明涉及式（I）化合物，其为核苷类似物的L-对映体形式，以及含有该化合物的药物组合物，治疗某些疾病的方法，包括癌症，细菌感染，寄生虫感染和T细胞介导使用化合物的疾病，制备化合物的方法和可用于制备化合物的中间体。

6. 发明申请

WO2008030118A1 ACYCLIC AMINE INHIBITORS OF 5'-METHYLTHIOADENOSINE PHOSPHORYLASE AND NUCLEOSIDASE 审中-公开
标题翻译： 5'-亚甲基二氢卟吩酶和核苷酸的交联胺抑制剂
公开(公告)号：WO2008030118A1
公开(公告)日：2008-03-13
申请号：PCT/NZ2007/000260
申请日：2007-09-07
申请人： INDUSTRIAL RESEARCH LIMITED , ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY , CLINCH, Keith , EVANS, Gary Brian , FRÖHLICH, Richard , FURNEAUX, Richard Hubert , KELLY, Peter Michael , MASON, Jennifer Mary , SCHRAMM, Vern L. , TYLER, Peter Charles
发明人： CLINCH, Keith , EVANS, Gary Brian , FRÖHLICH, Richard , FURNEAUX, Richard Hubert , KELLY, Peter Michael , MASON, Jennifer Mary , SCHRAMM, Vern L. , TYLER, Peter Charles
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of the general formula (I) which are inhibitors of 5'-methylthioadenosine phosphorylase or 5'-methylthioadenosine nucleosidase. The invention also relates to the use of these compounds in the treatment of diseases or conditions in which it is desirable to inhibit 5'-methylthioadenosine phosphorylase or 5'-methylthioadenosine nucleosidase including cancer, and to pharmaceutical compositions containing the compounds.
摘要翻译：本发明涉及作为5'-甲硫基腺苷磷酸化酶或5'-甲硫基腺苷核苷酸酶抑制剂的通式（I）化合物。本发明还涉及这些化合物在治疗期望抑制5'-甲硫基腺苷磷酸化酶或包括癌症的5'-甲基硫代腺苷核苷酸酶的疾病或病症的用途，以及含有该化合物的药物组合物。

7. 发明申请

WO2007097643A1 ANALOGUES OF COFORMYCIN AND THEIR USE FOR TREATING PROTOZOAN PARASITE INFECTIONS 审中-公开
标题翻译：协和霉素及其用于治疗原生动物寄生虫感染的方法
公开(公告)号：WO2007097643A1
公开(公告)日：2007-08-30
申请号：PCT/NZ2007/000031
申请日：2007-02-22
申请人： INDUSTRIAL RESEARCH LIMITED , ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY , FURNEAUX, Richard Hubert , TYLER, Peter Charles , EVANS, Gary Brian , SCHRAMM, Vern L. , KIM, Kami , FRÖHLICH, Richard
发明人： FURNEAUX, Richard Hubert , TYLER, Peter Charles , EVANS, Gary Brian , SCHRAMM, Vern L. , KIM, Kami , FRÖHLICH, Richard
IPC分类号： C07H19/23 , A61K31/4188 , A61K31/55 , A61K31/7052 , A61P33/06 , C07H5/10 , C07H15/14
CPC分类号： C07H5/10 , C07H15/14 , C07H19/23
摘要： This invention relates to compounds that are analogues of coformycin, pharmaceutical compositions containing the compounds, and methods of using the compounds for treating protozoan parasite infections, especially malaria.
摘要翻译：本发明涉及共转霉素类似物的化合物，含有该化合物的药物组合物，以及使用该化合物治疗原生动物寄生虫感染特别是疟疾的方法。

8. 发明申请

WO2003080620A1 INHIBITORS OF NUCLEOSIDE PHOSPHORYLASES AND NUCLEOSIDASES 审中-公开
标题翻译：核苷酸磷酸酶和核苷酸的抑制剂
公开(公告)号：WO2003080620A1
公开(公告)日：2003-10-02
申请号：PCT/NZ2003/000050
申请日：2003-03-25
申请人： INDUSTRIAL RESEARCH LIMITED , ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY , FURNEAUX, Richard Hubert , SCHRAMM, Vern L. , TYLER, Peter Charles , EVANS, Gary Brian
发明人： FURNEAUX, Richard Hubert , SCHRAMM, Vern L. , TYLER, Peter Charles , EVANS, Gary Brian
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07H19/052 , C07H19/14 , C07H19/16
摘要： The present invention relates to compounds of the general formula (I) which are inhibitors of 5'-methylthioadenosine phosphorylases and 5'-methylthioadenosine nucleosidases (MTAP and MTAN), the invention also relates to the use of these compounds in treatment of diseases and infections including cancer, bacterial infections and parasitic infections, and to pharmaceutical compositions containing the compounds.
摘要翻译：本发明涉及作为5'-甲硫基腺苷磷酸酶和5'-甲硫基腺苷核苷酸抑制剂（MTAP和MTAN）的通式（I）化合物，本发明还涉及这些化合物在治疗疾病和感染中的用途包括癌症，细菌感染和寄生虫感染，以及含有这些化合物的药物组合物。

9. 发明申请

WO2012150866A1 PHOSPHORIBOSYLTRANSFERASE INHIBITORS AND USES THEREOF 审中-公开
标题翻译：磷酸二酯酶抑制剂及其用途
公开(公告)号：WO2012150866A1
公开(公告)日：2012-11-08
申请号：PCT/NZ2012/000053
申请日：2012-04-16
申请人： INDUSTRIAL RESEARCH LIMITED , ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY , CLINCH, Keith , CRUMP, Douglas Ronald , EVANS, Gary Brian , HAZLETON, Keith Zachary , MASON, Jennifer Mary , SCHRAMM, Vern L. , TYLER, Peter Charles
发明人： CLINCH, Keith , CRUMP, Douglas Ronald , EVANS, Gary Brian , HAZLETON, Keith Zachary , MASON, Jennifer Mary , SCHRAMM, Vern L. , TYLER, Peter Charles
IPC分类号： C07F9/6561 , C07D487/04 , A61K31/675 , A61P33/06
CPC分类号： C07F9/6561 , A61K31/675 , C07D487/04 , Y02A50/409 , Y02A50/411 , Y02A50/414 , Y02A50/491
摘要： The invention relates to compounds of formula (I) that are inhibitors of hypoxanthine and/or guanine purine phosphoribosyltransferases and to pharmaceutical compositions containing the compounds, processes for preparing the compounds, and methods of treating diseases or conditions in which it is desirable to inhibit hypoxanthine and/or guanine purine phosphoribosyltransferases. Such diseases include malaria.
摘要翻译：本发明涉及作为次黄嘌呤和/或鸟嘌呤嘌呤磷酸核糖基转移酶的抑制剂的式（I）化合物和含有该化合物的药物组合物，制备该化合物的方法以及治疗其中希望抑制次黄嘌呤的疾病或病症的方法和/或鸟嘌呤嘌呤磷酸核糖基转移酶。这些疾病包括疟疾。

10. 发明申请

WO2004018496A1 INHIBITORS OF NUCLEOSIDE PHOSPHORYLASES AND NUCLEOSIDASES 审中-公开
标题翻译：核苷酸磷酸酶和核苷酸的抑制剂
公开(公告)号：WO2004018496A1
公开(公告)日：2004-03-04
申请号：PCT/NZ2003/000186
申请日：2003-08-21
申请人： ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY , INDUSTRIAL RESEARCH LIMITED , EVANS, Gary Brian , FURNEAUX, Richard Hurbert , LENZ, Dirk Henning , SCHRAMM, Vern L. , TYLER, Peter Charles , ZUBKOVA, Olga Vladimirovna
发明人： EVANS, Gary Brian , FURNEAUX, Richard Hurbert , LENZ, Dirk Henning , SCHRAMM, Vern L. , TYLER, Peter Charles , ZUBKOVA, Olga Vladimirovna
IPC分类号： C07H19/23
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。

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