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    • 1. 发明申请
    • 1-Glyoxlylamide indolizines for treating cancer
    • 1-乙氧基酰胺中氮茚类药物用于治疗癌症
    • US20030153759A1
    • 2003-08-14
    • US10244088
    • 2002-09-13
    • SBR Pharmaceuticals Corp.
    • Keizo KoyaLijun SunMitsunori OnoWeiwen YingHao Li
    • C07D455/02A61K031/506A61K031/4745
    • C07D471/04
    • Disclosed is a compound represented by Structural Formula (I): 1 Ring A is substituted or unsubstituted and optionally fused to an aryl group. Z1 and Z2 are independently nullO, nullS, nullNnullOR12 or nullNR12 R1 and R2 are independently nullH, an aliphatic group, a substituted aliphatic group, an unsubstituted non-aromatic heterocylic group, a substituted non-aromatic heterocylic group, an aryl group or a substituted aryl group, provided that R1 and R2 are not both nullH. Alternatively, nullNR1R2, taken together, is a substituted or unsubstituted non-aromatic nitrogen-containing heterocyclic group or a substituted or unsubstituted nitrogen-containing heteroaryl group. R3 is a substituted or unsubstituted aryl group or a substituted or unsubstituted aliphatic group. X is a covalent bond, nullC(R4R5)null, nullN(R4)null, nullOnull, nullSnull, nullS(O)null, nullS(O)2null, nullC(nullO)null, nullC(nullO)nullN(R4)-, or nullN(R4)nullC(nullO)null. R4 and R5 are independently nullH or a substituted or unsubstituted aliphatic group. R12 is nullH or a substituted or unsubstituted alkyl group.
    • 公开了由结构式(I)表示的化合物:环A是取代或未取代的且任选地与芳基稠合。 Z 1和Z 2独立地为= O,= S,= N-OR 12或= NR 12 R 1和R 2独立地为-H,脂族基团,取代的脂族基团,未取代的非芳族杂环基团,取代的非芳族杂环基团 ,芳基或取代的芳基,条件是R1和R2不同时为-H。 或者,-NR 1 R 2一起是取代或未取代的非芳族含氮杂环基或取代或未取代的含氮杂芳基。 R3是取代或未取代的芳基或取代或未取代的脂族基团。 X是共价键,-C(R4R5) - , - N(R4) - , - O - , - S - , - S(O) - , - S(O) ,-C(= O)-N(R 4) - 或-N(R 4)-C(= O) - 。 R 4和R 5独立地为-H或取代或未取代的脂族基团。 R 12是-H或取代或未取代的烷基。
    • 7. 发明申请
    • TAXOL ENHANCER COMPOUNDS
    • TAXOL增强剂化合物
    • WO2003006428A1
    • 2003-01-23
    • PCT/US2002/021714
    • 2002-07-10
    • SBR PHARMACEUTICALS CORP.KOYA, KeizoSUN, LijunCHEN, ShoujunTATSUTA, NoriakiWU, YamingONO, MitsunoriXIA, Zhi-Qiang
    • KOYA, KeizoSUN, LijunCHEN, ShoujunTATSUTA, NoriakiWU, YamingONO, MitsunoriXIA, Zhi-Qiang
    • C07C327/56
    • C07D307/68A45D2008/006A61K31/337A61K31/505A61K31/53A61K31/5377A61K47/58C07C327/56C07C2601/02C07C2601/04C07C2601/08C07C2601/14C07D209/42C07D209/44C07D213/83C07D261/18C07D333/38C07D333/68
    • One embodiment of the present invention is a compound represented by Structural Formula (I) wherein Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or -C(R 7 R 8 )-. R 1 is an aliphatic group, a substituted aliphatic group, a non-aromatic hetereocyclic group, or a substituted non-aromatic hetereocyclic group, R 2 -R 4 are independently -H, an aliphatic group, a substituted aliphatic group, a non-aromatic hetereocyclic group, a substituted non-aromatic hetereocyclic group, an aryl group or a substituted aryl group, or R 1 and R 3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R 2 and R 4 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. R 5 -R 6 are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R 7 and R 8 are each independently -H, an aliphatic or substituted aliphatic group, or R 7 is -H and R 8 is a substituted or unsubstituted aryl group, or, R 7 and R 8 , taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is =0 or =S. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent.
    • 本发明的一个实施方案是由结构式(I)表示的化合物,其中Y是取代或未取代的直链烃基的共价键。 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Y为共价键或-C(R 7 R 8) - 。 R1是脂肪族基团,取代脂肪族基团,非芳香族杂环基团或取代的非芳香族杂环基团,R2-R4独立地是-H,脂肪族基团,取代的脂肪族基团,非芳香族的杂环基团 ,取代的非芳香族杂环基团,芳基或取代的芳基,或者R 1和R 3与它们所键合的碳原子和氮原子一起,和/或R 2和R 4与碳和氮原子一起 形成与芳环稠合的非芳族杂环。 R5-R6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 7和R 8各自独立地为-H,脂族或取代的脂族基团,或者R 7为-H且R 8为取代或未取代的芳基,或者R 7和R 8一起为C 2 -C 6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。
    • 9. 发明申请
    • 1-GLYOXLYLAMIDE INDOLIZINES FOR TREATING CANCER
    • 1-GLYOXLYLAMIDE INDOLIZINES FOR TRANTING CANCER
    • WO2003022846A1
    • 2003-03-20
    • PCT/US2002/029154
    • 2002-09-13
    • SBR PHARMACEUTICALS CORP.KOYA, KeizoSUN, LijunONO, MitsunoriYING, WeiwenLI, Hao
    • KOYA, KeizoSUN, LijunONO, MitsunoriYING, WeiwenLI, Hao
    • C07D471/04
    • C07D471/04
    • Disclosed is a compound represented by Structural Fonnula (I): Ring A is substituted or unsubstituted and optionally fused to an aryl group. Z 1 and Z 2 are independently =0, =S, =N-OR 12 or =NR 12 ; R 1 and R 2 are independently -H, an aliphatic group, a substituted aliphatic group, an unsubstituted non-aromatic heterocylic group, a substituted non-aromatic heterocylic group, an aryl group or a substituted aryl group, provided that R 1 and R 2 are not both -H. Alternatively, -NR 1 R 2 , taken together, is a substituted or unsubstituted non-aromatic nitrogen-containing heterocyclic group or a substituted or unsubstituted nitrogen-containing heteroaryl group. R 3 is a substituted or unsubstituted aryl group or a substituted or unsubstituted aliphatic group. X is a covalent bond, -C(R 4 R 5 )-, -N(R 4 )-, -0-, -S-, -S(O)-, -S(0) 2 -, -C(=O)-, -C(=0)-N(R 4 )-, or N(R 4 )-C(=O)-. R 4 and R 5 are independently -H or a substituted or unsubstituted aliphatic group. R 12 is -H or a substituted or unsubstituted alkyl group.
    • 公开了由结构式(I)表示的化合物:环A是取代或未取代的,并任选地与芳基稠合。 Z> 1 <和Z> 2 <独立地= 0,= S,= N-OR> 12 <或= NR> 12 < R 1和R 2独立地是-H,脂族基团,取代的脂族基团,未取代的非芳族杂环基团,取代的非芳族杂环基团,芳基或取代的芳基,条件是 R&gt; 1&lt;和&lt; 2&gt;不同于-H。 或者,-NR> 1 2一起是取代或未取代的非芳族含氮杂环基或取代或未取代的含氮杂芳基。 R 3是取代或未取代的芳基或取代或未取代的脂族基。 X是共价键,-C(R 5)5 - , - (R 4) - , - O - , - S - , - S(O) - , - S(O) > - , - (= O) - , - (= O)-N(R 4) - 或N(R 4))C(= O) - 。 R 4和R 5独立地是-H或取代或未取代的脂族基团。 R 12为-H或取代或未取代的烷基。