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1. 发明申请

US20030195258A1 Taxol enhancer compounds 失效
标题翻译：紫杉醇增强剂化合物
公开(公告)号：US20030195258A1
公开(公告)日：2003-10-16
申请号：US10345885
申请日：2003-01-15
申请人： Synta Pharmaceuticals Corp.
发明人： Keizo Koya , Lijun Sun , Shoujun Chen , Noriaki Tatsuta , Yaming Wu , Mitsunori Ono
IPC分类号： A61K031/16 , A61K031/165 , C07C327/28 , C07C243/24
CPC分类号： C07D307/68 , A45D2008/006 , A61K31/337 , A61K47/58 , C07C327/56 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D209/42 , C07D209/44 , C07D213/83 , C07D261/18 , C07D333/38 , C07D333/68
摘要： Disclosed is a compound represented by the Structural Formula (I): 1 Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >CnullZ groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or nullC(R7R8)null. R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently nullH, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R5-R6 are independently nullH, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently nullH, an aliphatic or substituted aliphatic group, or R7 is nullH and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C1-C6 substituted or unsubstituted alkylene group. Z is nullO or nullS. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject with cancer by administering to the subject a compound of Structural Formula (I) in combination with taxol or an analog of taxol.
摘要翻译：公开了由结构式（I）表示的化合物：Y是共价键，亚苯基或取代或未取代的直链烃基。此外，Y与它所键合的两个> C = Z基团一起是取代或未取代的芳族基团。优选地，Y是共价键或-C（R <下标> 7 R <下标> 8 ） - 。 R <下标> 1 和R <下标> 2 独立地是芳基或取代的芳基，R <下标3 和R <下标4 独立的-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 R <下标> 5 -R <下标> 6 独立地是-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 R <下标> 7 和R <下标> 8 各自独立地为-H，脂族或取代的脂族基团，或R <下标7 为-H，R < 8 是一个取代或未取代的芳基，或者，R“下标”，“高亮”和“低级”）是C1-C6取代或未取代的亚烷基。 Z = 0或= S。还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。还公开了通过向受试者施用结构式（I）的化合物与紫杉醇或紫杉醇的类似物组合治疗患有癌症的受试者的方法。

2. 发明申请

US20040229952A1 Synthesis of taxol enhancers 失效
标题翻译：紫杉醇增强剂的合成
公开(公告)号：US20040229952A1
公开(公告)日：2004-11-18
申请号：US10807919
申请日：2004-03-24
申请人： Synta Pharmaceuticals Corp.
发明人： Shoujun Chen , Lijun Sun , Zhi-Qiang Xia , Keizo Koya , Mitsunori Ono
IPC分类号： A61K031/195
CPC分类号： C07D213/77 , C07C327/56 , C07C2601/14 , C07D209/42 , C07D209/44 , C07D213/83 , C07D261/18 , C07D307/54 , C07D333/38 , Y02P20/55
摘要： Disclosed is a method of preparing a thiohydrazide product compound from a hydrazide starting compound. The hydrazide starting compound is represented by Structural Formula (I): 1 The thiohydrazide product compound is represented by Structural Formula (II): 2 In Structural Formulas (I)-(II), R1 and R2 are independently an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R2 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. When R2 is an aryl group or a substituted aryl group, then R5 is a hydrazine protecting group; and when R2 is an aliphatic or substituted aliphatic group, then R5 is nullH or a hydrazine protecting group. R10 is nullH or a substituted or unsubstituted alkyl group. The method comprising the step of reacting the starting compound with a thionylating reagent.
摘要翻译：公开了从酰肼起始化合物制备硫代酰肼产物化合物的方法。酰肼起始化合物由结构式（I）表示：硫代酰肼产物化合物由结构式（II）表示：在结构式（I） - （II）中，R 1和R 2独立地为脂族基团，取代的脂族基团，芳基或取代的芳基，或者R 1和R 2与它们所键合的碳原子和氮原子一起形成任选地与芳环稠合的非芳族杂环。当R 2为芳基或取代芳基时，R 5为肼保护基; 当R 2为脂肪族或取代的脂族基团时，R 5为-H或肼保护基。 R 10为-H或取代或未取代的烷基。该方法包括使起始化合物与亚硫酰化试剂反应的步骤。

3. 发明申请

US20040152897A1 Synthesis of indolizines 审中-公开
标题翻译：中和衍生物的合成
公开(公告)号：US20040152897A1
公开(公告)日：2004-08-05
申请号：US10660358
申请日：2003-09-11
申请人： Synta Pharmaceuticals Corp.
发明人： Lijun Sun , Keizo Koya , Zhi-Qiang Xia , Teresa Przewloka , Shijie Zhang , Mitsunori Ono
IPC分类号： C07D487/02
CPC分类号： C07D471/04
摘要： Disclosed are methods of preparing substituted indolizines represented by the following formula: 1 comprising reacting a substrate represented by the following formula: 2 with either the cyclization reagent of the following formula: 3 or, a reagent prepared by reacting the compound represented the formula below with an alkylating agent: 4 The variables in the above formulas are defined herein.
摘要翻译：公开了制备由下式表示的取代的中氮茚的方法：包括使由下式表示的底物与下式的环化试剂反应：或通过使下式表示的化合物与烷基化剂反应制备的试剂：上述公式中的变量在此定义。

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