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1. 发明申请

WO2010062506A2 DECAHYDRO-1H-INDENOQUINOLINONE AND DECAHYDRO-3H-CYCLOPENTAPHENANTHRIDINONE CYP17 INHIBITORS 审中-公开
标题翻译：十氢化萘-1-茚并喹啉酮和十氢化-3H-环戊二烯并嘧啶CYP17抑制剂
公开(公告)号：WO2010062506A2
公开(公告)日：2010-06-03
申请号：PCT/US2009/061550
申请日：2009-10-21
申请人： LEAD THERAPEUTICS, INC. , CHU, Daniel , MYERS, Peter, L. , WANG, Bing
发明人： CHU, Daniel , MYERS, Peter, L. , WANG, Bing
IPC分类号： C07D215/04 , C07D215/02 , C07D311/04 , C07D311/02 , A61K31/57 , A61P35/00
CPC分类号： A61K31/352 , A61K31/473 , A61K31/497 , A61K31/506 , C07J73/003 , C07J73/005 , C07J75/005
摘要： Provided herein are inhibitors of CYP17 enzyme. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions.
摘要翻译：本文提供了CYP17酶的抑制剂。本文还描述了包含本文所述的至少一种化合物和本文所述的化合物或药物组合物用于治疗雄激素依赖性疾病，病症和病症的药物组合物。

2. 发明申请

WO2010065174A1 NOVEL SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译：新型半合成糖苷作为抗菌剂
公开(公告)号：WO2010065174A1
公开(公告)日：2010-06-10
申请号：PCT/US2009/055633
申请日：2009-09-01
申请人： LEAD THERAPEUTICS, INC. , CHU, Daniel , YE, Tao , WANG, Bing
发明人： CHU, Daniel , YE, Tao , WANG, Bing
IPC分类号： C07K19/00 , C07K9/00
CPC分类号： C07K9/008 , A61K38/00 , A61K45/06
摘要： Semi-synthetic glycopeptides having antibacterial activity are described, in particular, the semi¬ synthetic glycopeptides described herein are made by chemical modification of a glycopeptide (Compound A, Compound B, Compound H or Compound C) or monosaccharide made by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide; conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety on these scaffolds with certain acyl groups; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. Key reaction is the treatment of properly protected intermediate compound with isocyanate. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.
摘要翻译：具体描述具有抗菌活性的半合成糖肽，特别是本文所述的半合成糖肽通过化学修饰糖肽（化合物A，化合物B，化合物H或化合物C）或通过水解二糖部分在酸性介质中母体糖肽的氨基酸-4得到氨基酸-4单糖; 单糖转化为氨基糖衍生物; 在这些支架上的氨基酸4氨基取代的糖部分上的氨基取代基被某些酰基酰化; 并将这些支架的大环上的酸部分转化为某些取代的酰胺。关键反应是用异氰酸酯处理适当保护的中间体化合物。还提供了合成化合物的方法，含有该化合物的药物组合物，以及该化合物用于治疗和/或预防疾病，特别是细菌感染的方法。

3. 发明申请

WO2010048340A2 NOVEL SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译：新型半合成糖苷作为抗菌剂
公开(公告)号：WO2010048340A2
公开(公告)日：2010-04-29
申请号：PCT/US2009/061555
申请日：2009-10-21
申请人： LEAD THERAPEUTICS, INC. , CHU, Daniel , YE, Tao , WANG, Bing
发明人： CHU, Daniel , YE, Tao , WANG, Bing
IPC分类号： A01N37/18 , A01N43/16 , A61K38/14 , A61K38/00 , A01P1/00
CPC分类号： C07K9/006
摘要： Semi-synthetic glycopeptides having antibacterial activity are described, in particular, the semi-synthetic glycopeptides described herein are made by chemical modification of the a glycopeptide (Compound A, Compound B, Compound H or Compound C) or the monosaccharide made by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide; conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety on these scaffolds with certain acyl groups; conversion of the amide group in amino acid-3 on these scaffolds to various acylamide, acylsulfonamide, acylsulfonylurea derivatives; aminomethylation with substituent containing sulfonamide or acylsulfonamide group on amino acid -7 through Mannich reaction; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.
摘要翻译：具体描述了具有抗菌活性的半合成糖肽，特别是本文所述的半合成糖肽通过化学修饰糖肽（化合物A，化合物B，化合物H或化合物C）或通过水解二糖而制备的单糖在酸性介质中母体糖肽的氨基酸-4部分得到氨基酸-4单糖; 单糖转化为氨基糖衍生物; 在这些支架上的氨基酸4氨基取代的糖部分上的氨基取代基被某些酰基酰化; 这些支架上氨基酸-3中的酰胺基转化为各种酰基酰胺，酰基磺酰胺，酰基磺酰脲衍生物; 通过曼尼希反应在氨基酸-7上氨基甲基化与含有磺酰胺或酰基磺酰胺基团的取代基; 并将这些支架的大环上的酸部分转化为某些取代的酰胺。还提供了合成化合物的方法，含有该化合物的药物组合物，以及该化合物用于治疗和/或预防疾病，特别是细菌感染的方法。

4. 发明申请

WO2010017055A2 DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) 审中-公开
标题翻译：聚（ADP-RIBOSE）聚合酶（PARP）的二氢吲哚哒嗪酮抑制剂
公开(公告)号：WO2010017055A2
公开(公告)日：2010-02-11
申请号：PCT/US2009/051879
申请日：2009-07-27
申请人： LEAD THERAPEUTICS, INC. , WANG, Bing , CHU, Daniel
发明人： WANG, Bing , CHU, Daniel
IPC分类号： C07D487/14 , C07D487/12 , A61K31/495 , A61K31/50 , A61P3/10 , A61P29/00 , A61P9/02
CPC分类号： A61K31/5025 , A61K31/282 , A61K31/4745 , A61K31/495 , A61K31/5377 , A61K33/24 , A61N5/10 , A61N2005/1098 , C07D471/06
摘要： A compound having the structure set forth in Formula (I) and Formula (II) wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
摘要翻译：具有式（I）和式（II）所示结构的化合物，其中取代基Y，Z，A，B，R 1，R 2，R 3，R 4和R 5如本文所定义。本文提供了聚（ADP-核糖）聚合酶活性的抑制剂。本文还描述了包含本文所述的至少一种化合物和本文所述的化合物或药物组合物用于治疗通过抑制PARP活性而改善的疾病，病症和病症的药物组合物。

5. 发明申请

WO2009099736A2 BENZOXAZOLE CARBOXAMIDE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) 审中-公开
标题翻译：聚（ADP-RIBOSE）聚合酶（PARP）的苯并噻唑羧酰胺抑制剂
公开(公告)号：WO2009099736A2
公开(公告)日：2009-08-13
申请号：PCT/US2009/031163
申请日：2009-01-15
申请人： LEAD THERAPEUTICS, INC. , CHU, Daniel , WANG, Bing
发明人： CHU, Daniel , WANG, Bing
IPC分类号： C07D498/04
CPC分类号： C07D263/57 , C07D413/04 , C07D413/10 , C07D455/02 , C07D487/04 , C07D487/08
摘要： A compound having the structure set forth in Formula (I) or Formula (II): Formula (I) Formula (II) wherein the variables Y, R 1 , R 2 , R 3 , and R 4 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
摘要翻译：具有式（I）或式（II）所示结构的化合物：其中变量Y，R1，R2，R3和R4如本文所定义的式（I）式（II）。本文提供了聚（ADP-核糖）聚合酶活性的抑制剂。本文还描述了包含本文所述的至少一种化合物和本文所述的化合物或药物组合物用于治疗通过抑制PARP活性而改善的疾病，病症和病症的药物组合物。

6. 发明申请

WO2009085562A1 NOVEL SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译：新型半合成糖苷作为抗菌剂
公开(公告)号：WO2009085562A1
公开(公告)日：2009-07-09
申请号：PCT/US2008/085716
申请日：2008-12-05
申请人： LEAD THERAPEUTICS, INC. , CHU, Daniel , YE, Tao
发明人： CHU, Daniel , YE, Tao
IPC分类号： C07C235/00
CPC分类号： C07K9/008
摘要： Semi-synthetic glycopeptides having antibacterial activity are described, in particular, the semi-synthetic glycopeptides described herein are made by chemical modification of a glycopeptide (Compound A, Compound B, Compound H or Compound C) or monosaccharide made by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide; conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety on these scaffolds with certain acyl groups; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. Key reaction is the treatment of properly protected intermediate compound with isocyanate or carrying a Hofmann degradation of the primary amide of the 3rd amino acid asparagines with phenyl-bis-trifluoroacetate to give the primary amine. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.
摘要翻译：具体描述了具有抗菌活性的半合成糖肽，特别是本文所述的半合成糖肽通过化学修饰糖肽（化合物A，化合物B，化合物H或化合物C）或通过水解二糖部分在酸性介质中母体糖肽的氨基酸-4得到氨基酸-4单糖; 单糖转化为氨基糖衍生物; 在这些支架上的氨基酸4氨基取代的糖部分上的氨基取代基被某些酰基酰化; 并将这些支架的大环上的酸部分转化为某些取代的酰胺。关键反应是用异氰酸酯处理适当保护的中间体化合物或者用苯基二 - 三氟乙酸盐对第三氨基酸天门冬酰胺的伯酰胺进行霍夫曼降解，得到伯胺。还提供了合成化合物的方法，含有该化合物的药物组合物，以及该化合物用于治疗和/或预防疾病，特别是细菌感染的方法。

7. 发明申请

WO2008140973A1 SEMI-SYNTHETIC GLYCOPEPTIDES WITH ANTIBACTERIAL ACTIVITY 审中-公开
标题翻译：具有抗菌活性的半合成糖蛋白
公开(公告)号：WO2008140973A1
公开(公告)日：2008-11-20
申请号：PCT/US2008/062483
申请日：2008-05-02
申请人： LEAD THERAPEUTICS, INC. , CHU, Daniel
发明人： CHU, Daniel
IPC分类号： C07C235/00 , C07K9/00 , A61K38/00
CPC分类号： C07K9/008 , A61K38/00
摘要： Semi- synthetic glycopeptides having antibacterial activity are described, in particular, the semi-synthetic glycopeptides described hereins are made by subjecting the a glycopeptide (Compound A, Compound B, COMPOUND H or Compound C) in acidic medium to hydrolyze the disaccharide moiety of the amino acid-4 of the parent glycopeptide to give the amino acid-4 monosaccharide; temporary protection of the amino grouρ(s); conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety on these scaffolds with certain acyl groups; conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides and removal of the tempory aimo protection grouρ(s). Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.
摘要翻译：具体描述了具有抗菌活性的半合成糖肽，特别是本文所述的半合成糖肽是通过在酸性介质中使糖肽（化合物A，化合物B，化合物H或化合物C）使糖肽（化合物A，化合物B，化合物C或化合物C）母体糖肽的氨基酸-4，得到氨基酸-4单糖; 临时保护氨基酸; 单糖转化为氨基糖衍生物; 在这些支架上的氨基酸4氨基取代的糖部分上的氨基取代基被某些酰基酰化; 将这些支架的大环上的酸部分转化为某些取代的酰胺，并除去温度目标保护组合物。还提供了合成化合物的方法，含有该化合物的药物组合物，以及该化合物用于治疗和/或预防疾病，特别是细菌感染的方法。

8. 发明申请

WO2009029375A1 NOVEL INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) 审中-公开
标题翻译：聚（ADP-RIBOSE）聚合酶（PARP）的新型抑制剂
公开(公告)号：WO2009029375A1
公开(公告)日：2009-03-05
申请号：PCT/US2008/071622
申请日：2008-07-30
申请人： LEAD THERAPEUTICS, INC. , CHU, Daniel
发明人： CHU, Daniel
IPC分类号： A61K31/501 , A61K31/16 , C07D403/10 , C07D401/10
CPC分类号： C07D401/10 , C07D401/04 , C07D403/04 , C07D403/10 , C07D451/02
摘要： A compound having the structure set forth in Formula (I): wherein the variables Y, R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein. Compounds described herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of such compounds and pharmaceutical compositions to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
摘要翻译：具有式（I）所示结构的化合物：其中变量Y，R1，R2，R3，R4和R5如本文所定义。本文描述的化合物是聚（ADP-核糖）聚合酶活性的抑制剂。本文还描述了包含本文所述的至少一种化合物和这些化合物和药物组合物用于治疗通过抑制PARP活性而改善的疾病，病症和病症的药物组合物。

9. 发明申请

WO2011140009A1 METHODS OF USING SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译：使用半合成糖尿病作为抗菌药物的方法
公开(公告)号：WO2011140009A1
公开(公告)日：2011-11-10
申请号：PCT/US2011/034885
申请日：2011-05-03
申请人： BIOMARIN PHARMACEUTICAL INC. , CHU, Daniel , WANG, Bing
发明人： CHU, Daniel , WANG, Bing
IPC分类号： A61K31/7048 , A61K38/14 , C07K9/00 , A61P31/04
CPC分类号： C07K9/008 , A61K31/7048 , A61K38/00
摘要： Methods of using semi-synthetic glycopeptides of formula I-XIV having antibacterial activity are described.
摘要翻译：描述了使用具有抗菌活性的式I-XIV的半合成糖肽的方法。

10. 发明申请

WO2012054698A1 CRYSTALLINE (8S,9R)-5-FLUORO-8-(4-FLUOROPHENYL)-9-(1-METHYL-1H-1,2,4-TRIAZOL-5-YL)-8,9-DIHYDRO-2H-PYRIDO[4,3,2-DE]PHTHALAZIN-3(7H)-ONE TOSYLATE SALT 审中-公开
标题翻译：（8S，9R）-5-氟-9-（4-氟代戊基）-9-（1-甲基-1H-1,2,4-三唑-5-基）-8,9-二氢-2H-吡喃 [4,3,2-DE]苯乙烯-3（7H） - 苯甲酸盐
公开(公告)号：WO2012054698A1
公开(公告)日：2012-04-26
申请号：PCT/US2011/057039
申请日：2011-10-20
申请人： BIOMARIN PHARMACEUTICAL INC. , WANG, Bing , CHU, Daniel , LIU, Yongbo , PENG, Shichun
发明人： WANG, Bing , CHU, Daniel , LIU, Yongbo , PENG, Shichun
IPC分类号： C07D471/06 , A61K31/5025 , A61P35/00
CPC分类号： C07D471/06
摘要： Provided herein are (8 S , 9 R )-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-lH-1,2,4-triazol-5- yl)-8,9-dihydro-2 H -pyrido[4,3,2- de ]phthalazin-3(7 H )-one tosylate salt forms, including crystalline forms, and methods of their preparation. Pharmaceutical compositions comprising a (8 S ,9 R )-5-fiuoro-8-(4-fluorophenyl)-9-(1-methyl-1 H -1,2,4-triazol-5-yl)-8,9-dihydro-2 H - pyrido[4,3,2- de ]phthalazin-3(7 H )-one tosylate salt are also provided, as are methods of using (8 S ,9 R )-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1 H -1,2,4-triazol-5-yl)-8,9-dihydro-2 H - pyrido[4,3,2- de ]phthalazin-3(7 H )-one tosylate salt to treat a disease or condition, such as a cancer.
摘要翻译：本文提供的是（8S，9R）-5-氟-8-（4-氟苯基）-9-（1-甲基-1H-1,2,4-三唑-5-基）-8,9-二氢-2H- - 吡啶并[4,3,2-de]酞嗪-3（7H） - 酮甲磺酸盐形式，包括晶型，及其制备方法。包含（8S，9R）-5-氟-8-（4-氟苯基）-9-（1-甲基-1H-1,2,4-三唑-5-基）-8,9-二氢 - 还提供了使用（8S，9R）-5-氟-8-（4-氟苯基）-9（2H） - 吡啶并[4,3,2- - （1-甲基-1H-1,2,4-三唑-5-基）-8,9-二氢-2H-吡啶并[4,3,2- [de] 2,3-二氮杂萘-3（7H） - 酮甲苯磺酸盐，治疗疾病或病症，如癌症。

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