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1. 发明申请

WO2006053429A1 PROCESS FOR THE MANUFACTURE OF 3-HYDROXY-N-ALKYL-1-CYCLOALKYL-6-ALKYL-4-OXO-1,4-DIHYDROPYRIDINE-2-CARBOXAMIDE AND ITS RELATED ANALOGUES 审中-公开
标题翻译： 3-羟基-N-烷基-1-环烷基-6-烷基-4-氧代-1,4-二氢吡啶-2-羧酸酰胺及其相关模拟物的制备方法
公开(公告)号：WO2006053429A1
公开(公告)日：2006-05-26
申请号：PCT/CA2005/001746
申请日：2005-11-17
申请人： APOTEX INC. , TAM, Tim, Fat , LEUNG-TOUNG, Regis , ZHAO, Yanqing , LI, Wanren , WANG, Yingsheng , AGOSTINO, Sandra, Vittoria , SHAH, Birenkumar, Hasmukhbhai
发明人： TAM, Tim, Fat , LEUNG-TOUNG, Regis , ZHAO, Yanqing , LI, Wanren , WANG, Yingsheng , AGOSTINO, Sandra, Vittoria , SHAH, Birenkumar, Hasmukhbhai
IPC分类号： C07D211/86 , C07D413/06 , C07D401/06
CPC分类号： C07D213/81 , Y02P20/55
摘要： The present invention relates to a novel process for the preparation of 1-alkyl or 1-cycloalkyl derivatives of 3-hydroxy-4-oxo-1,4-dihydropyridine-2-carboxamide of formula (I). The process includes reacting an amine R 2 NH 2 with a compound of formula (II) in a solution of metal hydroxide in water to give a compound of formula (III). Subsequent reaction of the compound of formula (III) with an acid chloride formation reagent in an inert solvent gives compounds of formula (I). The acid chloride formation reagent is selected from oxalyl chloride and dimethylformamide, dimethyichloromethylene-ammonium chloride and thionyl chloride and dimethylformamide. If desired, a compound of formula (I) where R 5 is hydrogen may be formed when an intermediate substituent is used wherein R 5 is an alcohol protective group removable by catalytic hydrogenation.
摘要翻译：本发明涉及制备式（I）的3-羟基-4-氧代-1,4-二氢吡啶-2-甲酰胺的1-烷基或1-环烷基衍生物的新方法。该方法包括使胺R 2 H 2 NH 2与式（II）化合物在金属氢氧化物在水中的溶液中反应，得到式（III）化合物。式（III）化合物与酰氯形成试剂在惰性溶剂中的随后反应得到式（I）化合物。酰氯形成试剂选自草酰氯和二甲基甲酰胺，二甲基亚甲基氯化铵和亚硫酰氯和二甲基甲酰胺。如果需要，其中R 5为氢的式（I）化合物可以在使用其中R 5为可通过催化氢化除去的醇保护基团的中间取代基时形成。

2. 发明申请

WO2005049609A1 CYCLOALKYL DERIVATIVES OF 3-HYDROXY-4-PYRIDINONES 审中-公开
标题翻译： 3-羟基-4-吡啶酮的环烷基衍生物
公开(公告)号：WO2005049609A1
公开(公告)日：2005-06-02
申请号：PCT/CA2004/001986
申请日：2004-11-18
申请人： APOTEX INC. , TAM, Tim, Fat , SPINO, Michael , LI, Wanren , WANG, Yingsheng , ZHAO, Yanqing , SHAH, Birenkumar Hasmukhbhai
发明人： TAM, Tim, Fat , SPINO, Michael , LI, Wanren , WANG, Yingsheng , ZHAO, Yanqing , SHAH, Birenkumar Hasmukhbhai
IPC分类号： C07D413/06
CPC分类号： C07D213/81
摘要： The present invention provides an cycloalkyl derivative of 3-hydroxy-4-pyridinone which is useful for the chelation of metal ions such as iron. Its preparation and use is described. In particular, the invention concerns the removal of iron in chemical and biological systems including chelating agents having the formula (I); wherein R 1 is X with the proviso that R 2 is Y; or R 1 is T with the proviso that R 2 is W; or R 1 is X with the proviso that R 2 R 5 N when taken together form a heterocyclic ring selected from piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl, wherein the group piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl is either unsubstituted or substituted with one to three C 1 to C 6 alkyl groups. X is C 3 -C 6 cycloalkyl; Y is selected from the group consisting of C 1 to C 6 cycloalkyl; C 1 to C 6 alkyl, and C 1 to C 6 alkyl monosubstituted with a C 3 -C 6 cycloalkyl; T is C 1 to C 6 alkyl; W is C 3 -C 6 cycloalkyl; R 3 is selected from the group consisting of hydrogen and C 1 to C 6 alkyl; R 4 is selected from the group consisting of hydrogen and C 1 to C 6 alkyl; R 5 is selected from the group consisting of hydrogen and C 1 to C 6 alkyl; and its pharmaceutically acceptable salt thereof. Pharmaceutical compositions of such compounds are useful in the removal of excess body iron from patients with iron overload diseases.
摘要翻译：本发明提供3-羟基-4-吡啶酮的环烷基衍生物，其可用于螯合金属离子如铁。描述其准备和使用。特别地，本发明涉及在化学和生物系统中去除铁，包括具有式（I）的螯合剂; 其中R 1为X，条件是R 2为Y;且其中R 1为T，条件是R 2为W; 或R 1为X，条件是R 2 R 5一起形成选自哌啶基，吗啉基，吡咯烷基或哌嗪基的杂环，其中哌啶基，吗啉基，吡咯烷基或哌嗪基是未取代的或被一至三个C 1至C 6烷基取代。 X是C 3 -C 6环烷基; Y选自C1-C6环烷基; C 1 -C 6烷基和被C 3 -C 6环烷基单取代的C 1至C 6烷基; T是C1-C6烷基; W是C3-C6环烷基; R 3选自氢和C 1至C 6烷基; R 4选自氢和C 1至C 6烷基; R 5选自氢和C 1至C 6烷基; 及其药学上可接受的盐。这些化合物的药物组合物可用于从具有铁超负荷疾病的患者中去除过量的身体铁。

3. 发明申请

WO2012129680A1 PRODRUGS OF D-GAMMA-GLUTAMYL-D-TRYPTOPHAN AND D-GAMMA- GLUTAMYL-L-TRYPTOPHAN 审中-公开
标题翻译： D-葡萄糖 - 谷氨酰-D-三磷酸和D-γ-氨基 - 谷氨酰-L-三磷酸的产物
公开(公告)号：WO2012129680A1
公开(公告)日：2012-10-04
申请号：PCT/CA2012/000327
申请日：2012-03-30
申请人： APOTEX TECHNOLOGIES INC. , TAM, Tim, Fat , LEUNG-TOUNG, Regis , WANG, Yingsheng , ZHAO, Yanqing , XIN, Tao , LI, Wanren , WODZINSKA, Jolanta, Maria , RABADIA, Vrajlal, S. , SHAH, Birenkumar , FEENEY, Christopher, John
发明人： TAM, Tim, Fat , LEUNG-TOUNG, Regis , WANG, Yingsheng , ZHAO, Yanqing , XIN, Tao , LI, Wanren , WODZINSKA, Jolanta, Maria , RABADIA, Vrajlal, S. , SHAH, Birenkumar , FEENEY, Christopher, John
IPC分类号： C07D209/20 , A61K31/404 , A61K38/03 , C07K5/037
CPC分类号： C07K5/0215 , A61K31/404
摘要： The present invention provides pro-drugs of D-gamma-glutamyl-[D/L] -tryptophan, said pro-drugs are compounds of Formula I or pharmaceutically acceptable salts thereof, wherein G is C 1 -C 8 alkyl or benzyl, T is C 1 -C 8 alkyl or benzyl, and * is a chiral carbon in a (R) or (S) configuration, provided that when * is in the (R) configuration, at least one of G and T is C 5 -C 8 alkyl; and use of compounds of Formula I in a pharmaceutical composition.
摘要翻译：本发明提供了D-γ-谷氨酰基 - [D / L] - 色氨酸的前药，所述前药是式I化合物或其药学上可接受的盐，其中G为C1-C8烷基或苄基，T为C1 -C8烷基或苄基，和*是（R）或（S）构型的手性碳，条件是当*是（R）构型时，G和T中的至少一个是C 5 -C 8烷基; 以及在药物组合物中使用式I化合物。

4. 发明申请

WO2012129671A1 PRODRUGS OF D-ISOGLUTAMYL-[D/L]-TRYPTOPHAN 审中-公开
标题翻译： D-葡聚糖 - [D / L] -TRYPTOPHAN的产品
公开(公告)号：WO2012129671A1
公开(公告)日：2012-10-04
申请号：PCT/CA2012/000304
申请日：2012-03-30
申请人： APOTEX TECHNOLOGIES INC. , TAM, Tim, Fat , LEUNG-TOUNG, Regis , WANG, Yingsheng , ZHAO, Yanqing , XIN, Tao , LI, Wanren , WODZINSKA, Jolanta, Maria , RABADIA, Vrajlal, S. , FEENEY, Christopher, John
发明人： TAM, Tim, Fat , LEUNG-TOUNG, Regis , WANG, Yingsheng , ZHAO, Yanqing , XIN, Tao , LI, Wanren , WODZINSKA, Jolanta, Maria , RABADIA, Vrajlal, S. , FEENEY, Christopher, John
IPC分类号： C07D209/20 , A61K38/05 , A61K9/72 , C07K5/037
CPC分类号： C07D209/20 , C07K5/0215
摘要： Provided are carboxylic ester derivatives of formula (I), methods of preparing them, and methods for using them. These compounds are prodrugs of D-isoglutamyl-[D/L]-tryptophan. The in vitro bioconversion of some of the prodrugs to the parent drug D-isoglutamyl-D-tryptophan (or thymodepressin ) was tested in human hepatocytes and in human blood. In vivo pharmacokinetic studies following oral administration of some of the prodrugs to rats are also reported.
摘要翻译：提供式（I）的羧酸酯衍生物，其制备方法和使用它们的方法。这些化合物是D-异谷氨酰基 - [D / L] - 色氨酸的前药。在人肝细胞和人血液中测试了一些前药到母体药物D-异谷氨酰-D-色氨酸（或胸腺嘧啶抑制素）的体外生物转化。还报道了口服给予大鼠一些前药后的体内药代动力学研究。

5. 发明申请

WO2008074128A1 PHARMACEUTICALLY ACCEPTABLE SALTS OF THYMODEPRESSIN AND PROCESSES FOR THEIR MANUFACTURE 审中-公开
标题翻译： THYMODEPRININ的药物可接受的盐及其制造方法
公开(公告)号：WO2008074128A1
公开(公告)日：2008-06-26
申请号：PCT/CA2007/002235
申请日：2007-12-13
申请人： APOTEX TECHNOLOGIES INC. , TAM, Tim, Fat , N'ZEMBA, Blaise , LEUNG-TOUNG, Regis , WANG, Yingsheng , ZHAO, Yanqing , YU, Lily
发明人： TAM, Tim, Fat , N'ZEMBA, Blaise , LEUNG-TOUNG, Regis , WANG, Yingsheng , ZHAO, Yanqing , YU, Lily
IPC分类号： C07K5/037 , A61K38/05 , A61P17/06 , C07K1/107 , C07K1/30 , C07K5/02 , C07K5/06
CPC分类号： C07D209/20 , A61K38/05 , C07K5/0215
摘要： The present invention relates to pharmaceutically acceptable crystalline and amorphous salts of D-isoglutamyl-D-tryptophan as well as processes for their manufacture, pharmaceutical compositions comprising them, and their uses in the preparation of pharmaceutical compositions for the treatment of various conditions and/or diseases. In particular, the present invention relates to D-isoglutamyl-D-tryptophan potassium salt (1:1), D-isoglutamyl-D-tryptophan lithium salt (1:1), D-isoglutamyl-D-tryptophan calcium salt (2:1), D-isoglutamyl-D-tryptophan magnesium salt (2:1), and D-isoglutamyl-D- tryptophan organic ammonium salts (1:1).
摘要翻译：本发明涉及D-异谷氨酰-D-色氨酸的药学上可接受的结晶和无定形盐以及其制备方法，包含它们的药物组合物及其在制备药物组合物中用于治疗各种病症和/或疾病。特别地，本发明涉及D-异谷氨酰-D-色氨酸钾盐（1：1），D-异谷氨酰基-D-色氨酸锂盐（1:1），D-异谷氨酰-D-色氨酸钙盐（2： 1），D-异谷氨酰-D-色氨酸镁盐（2:1）和D-异谷氨酰基-D-色氨酸有机铵盐（1:1）。

6. 发明申请

WO2011000104A1 FLUORINATED DERIVATIVES OF 3-HYDROXYPYRIDIN-4-ONES 审中-公开
标题翻译： 3-羟基吡啶-4-酮的氟化衍生物
公开(公告)号：WO2011000104A1
公开(公告)日：2011-01-06
申请号：PCT/CA2010/001027
申请日：2010-07-05
申请人： APOTEX TECHNOLOGIES INC. , TAM, Tim Fat , LEUNG-TOUNG, Regis , WANG, Yingsheng , ZHAO, Yanqing , XIN, Tao , SHAH, Birenkumar , N'ZEMBA, Blaise , WODZINSKA, Jolanta Maria , PREMYSLOVA, Marina
发明人： TAM, Tim Fat , LEUNG-TOUNG, Regis , WANG, Yingsheng , ZHAO, Yanqing , XIN, Tao , SHAH, Birenkumar , N'ZEMBA, Blaise , WODZINSKA, Jolanta Maria , PREMYSLOVA, Marina
IPC分类号： C07D213/69 , A61K31/4422 , A61P11/00 , A61P13/12 , A61P25/28 , A61P35/00
CPC分类号： C07D213/26 , A61K31/4412 , A61K31/4545 , A61K31/496 , C07D211/86 , C07D213/69 , C07D213/74 , C07D213/79 , C07D401/06
摘要： Provided are compounds of Formula I which are derivatives of 3-Hydroxypyridin-4-ones. The compounds may be used in treatment of a medical condition related to a toxic concentration of iron. The compounds may be used for preparation of a medicament for treatment of a medical condition related to a toxic concentration of iron. The medical condition related to a toxic concentration of iron may be selected from the group consisting of: cancer, pulmonary disease, progressive kidney disease and Frederich's Ataxia.
摘要翻译：提供作为3-羟基吡啶-4-酮衍生物的式I化合物。该化合物可用于治疗与毒素浓度相关的医学病症。所述化合物可用于制备用于治疗与毒性浓度铁相关的医学病症的药物。与毒性浓度相关的医学状况可以选自癌症，肺部疾病，进行性肾脏疾病和弗雷德里希共济失调。

7. 发明申请

WO2008098355A1 CRYSTALLINE FORMS OF THE MONO-SODIUM SALT OF D-ISOGLUTAMYL-D-TRYPTOPHAN 审中-公开
标题翻译： D-葡聚糖-D-三磷酸单钠盐的晶体形态
公开(公告)号：WO2008098355A1
公开(公告)日：2008-08-21
申请号：PCT/CA2008/000271
申请日：2008-02-11
申请人： APOTEX TECHNOLOGIES INC. , TAM, Tim, Fat , N'ZEMBA, Blaise , LEUNG-TOUNG, Regis , WANG, Yingsheng , ZHAO, Yanqing , YU, Lily
发明人： TAM, Tim, Fat , N'ZEMBA, Blaise , LEUNG-TOUNG, Regis , WANG, Yingsheng , ZHAO, Yanqing , YU, Lily
IPC分类号： C07K5/037 , A61K38/05 , A61P17/06 , A61P29/00 , A61P37/00 , C07K1/30 , C07K1/34 , C30B7/00 , C07D209/20 , C07K5/06
CPC分类号： C07D209/20 , A61K38/00 , C30B7/00
摘要： The present invention relates to crystalline forms of the mono-sodium salt of D- isoglutamyl-D-tryptophan, pharmaceutical compositions comprising them, their use in the treatment of various diseases and conditions, and processes for their preparation. In particular, the present invention relates the crystal modification 1 (polymorphic form F), the crystal modification 2 (polymorphic form I), and the crystal modification 3 (polymorphic form X) of the mono-sodium salt of D-isoglutamyl-D-tryptophan.
摘要翻译：本发明涉及D-异谷氨酰-D-色氨酸的单钠盐的结晶形式，包含它们的药物组合物，它们在各种疾病和病症的治疗中的用途及其制备方法。特别地，本发明涉及D-异谷氨酰基-D-多糖的单钠盐的晶体改性1（多晶型F），晶体改性2（多晶型I）和晶体改性3（多晶型X）色氨酸。

8. 发明申请

WO2008064465A1 CRYSTALLINE D-ISOGLUTAMYL-D-TRYPTOPHAN AND THE MONO AMMONIUM SALT OF D-ISOGLUTAMYL- D-TRYPTOPHAN 审中-公开
标题翻译：结晶D-异山梨糖醇-D-胰蛋白胨和D-异山梨糖醇-D-胰蛋白胨的单铵盐
公开(公告)号：WO2008064465A1
公开(公告)日：2008-06-05
申请号：PCT/CA2007/002123
申请日：2007-11-26
申请人： APOTEX TECHNOLOGIES INC. , TAM, Tim, Fat , N'ZEMBA, Blaise , LEUNG-TOUNG, Regis , WANG, Yingsheng , ZHAO, Yanqing , YU, Lily
发明人： TAM, Tim, Fat , N'ZEMBA, Blaise , LEUNG-TOUNG, Regis , WANG, Yingsheng , ZHAO, Yanqing , YU, Lily
IPC分类号： C07K5/037 , A61K38/05 , A61P17/06 , C07K1/107 , C07K1/16 , C07K1/30 , C07K5/02 , C30B7/14 , C07K5/06
CPC分类号： C07K5/0215 , A61K38/00
摘要： A process for making pure crystalline D-isoglutamyl-D-tryptophan is provided which includes the step of deprotecting essentially pure N-tert-butoxycarbonyl-D- isoglutamyl-D-tryptophan or its diester to yield essentially pure D-isoglutamyl-D- tryptophan. A process is also provided for the preparation of pure mono ammonium salt of D-isoglutamyl-D-tryptophan from essentially pure N-tert-butoxycarbonyl-D- isoglutamyl-D-tryptophan. D-isoglutamyl-D-tryptophan, ammonium salt (1 :1) is a stable pharmaceutical solid.
摘要翻译：提供了制备纯的结晶D-异戊二酰基-D-色氨酸的方法，其包括将基本上纯的N-叔丁氧基羰基-D-异戊酰基-D-色氨酸或其二酯去保护基本上得到纯的D-异戊酰基-D-色氨酸。还提供了由基本上纯的N-叔丁氧基羰基-D-异戊酰基-D-色氨酸制备D-异戊酰基-D-色氨酸的纯单铵盐的方法。 D-异谷氨酰-D-色氨酸铵盐（1：1）是一种稳定的药物固体。

9. 发明申请

WO2008116301A1 FLUORINATED DERIVATIVES OF DEFERIPRONE 审中-公开
标题翻译： DEFERIPRONE的氟化衍生物
公开(公告)号：WO2008116301A1
公开(公告)日：2008-10-02
申请号：PCT/CA2008/000558
申请日：2008-03-27
申请人： APOTEX TECHNOLOGIES INC. , TAM, Tim, Fat , LEUNG-TOUNG, Regis , WANG, Yingsheng , ZHAO, Yanquing
发明人： TAM, Tim, Fat , LEUNG-TOUNG, Regis , WANG, Yingsheng , ZHAO, Yanquing
IPC分类号： C07D213/69 , A61K31/351 , A61K31/4412 , A61P25/16 , A61P25/28 , A61P39/04 , C07D309/40
CPC分类号： C07D309/40 , C07D213/69
摘要： The present invention relates to novel derivatives of deferiprone. In particular, the present invention relates to fluorinated derivatives of deferiprone or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, processes for the manufacture thereof and their use in the treatment of neurodegenerative diseases caused by the presence of free iron or iron accumulation in neural tissues and in diseases wherein excess iron must be removed or redistributed.
摘要翻译：本发明涉及去铁酮的新型衍生物。特别地，本发明涉及去铁酮的氟化衍生物或其药学上可接受的盐，包含其的药物组合物，其制备方法及其用于治疗由神经组织中游离铁或铁积聚引起的神经变性疾病的治疗以及必须除去或重新分配过量铁的疾病。

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