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    • 22. 发明申请
    • Synthesis of taxol enhancers
    • 紫杉醇增强剂的合成
    • US20090005594A1
    • 2009-01-01
    • US12231217
    • 2008-08-29
    • Shoujun ChenLijun SunZhi-Qiang XiaKeizo KovaMitsunori Ono
    • Shoujun ChenLijun SunZhi-Qiang XiaKeizo KovaMitsunori Ono
    • C07C327/00
    • C07D213/77C07C327/56C07C2601/14C07D209/42C07D209/44C07D213/83C07D261/18C07D307/54C07D333/38Y02P20/55
    • 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): The thiohydrazide product compound is represented by Structural Formula (II): 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 —H or a hydrazine protecting group. R10 is —H or a substituted or unsubstituted alkyl group. The method comprising the step of reacting the starting compound with a thionylating reagent.
    • 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。
    • 25. 发明授权
    • Taxol enhancer compounds
    • 紫杉醇增强剂化合物
    • US06800660B2
    • 2004-10-05
    • US10193075
    • 2002-07-10
    • Keizo KoyaLijun SunShoujun ChenNoriaki TatsutaYaming WuMitsunori Ono
    • Keizo KoyaLijun SunShoujun ChenNoriaki TatsutaYaming WuMitsunori Ono
    • A61K3116
    • A61K47/48176A61K31/16A61K31/165A61K31/277A61K31/337A61K31/381A61K31/44A61K31/505A61K31/53A61K47/58C07C327/56C07C2601/02C07C2601/04C07C2601/08C07C2601/14C07D209/42C07D209/44C07D213/83C07D261/18C07D305/14C07D307/68C07D333/38C07D333/68C07D407/12
    • Disclosed is a compound represented by the Structural Formula (I): Y is a covalent bond, a phenylene group or 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(R7R8)—. R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ═O or ═S. 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.
    • 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(R7R8) - ,R1和R2独立地是芳基或取代的芳基,R3和R4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 5 -R 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 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是 -H和R8是取代或未取代的芳基,或者R 7和R 8一起是C 2 -C 6取代或未取代的亚烷基。Z = O或= S。还公开了药物组合物,其包含 本发明和药学上可接受的载体或稀释剂。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。
    • 27. 发明授权
    • Pyrimidine compounds
    • 嘧啶化合物
    • US06693097B2
    • 2004-02-17
    • US10000742
    • 2001-11-30
    • Mitsunori OnoShijie ZhangTeresa PrzewlokaK. KoyaElena KostikYuniko WadaLijun SunWeiwen Ying
    • Mitsunori OnoShijie ZhangTeresa PrzewlokaK. KoyaElena KostikYuniko WadaLijun SunWeiwen Ying
    • C07D41704
    • C07D239/48A61K31/506A61K31/53A61K31/5377A61K31/541C07D401/12C07D401/14C07D403/12
    • This invention features pyrimidine compounds of formula (I): aryl, or heteroaryl; each of R2 and R4, independently, is Rc, halogen, nitro, cyano, isothionitro, SRc, or ORc; or R2 and R4, taken together, is carbonyl; R3 is Rc, alkenyl, alkynyl, ORc, OC(O)Rc, SO2Rc, S(O)Rc, S(O2)NRcRd, SRc, NRcRd, NRcCORd, NRcC(O)ORd, NRcC(O)NRcRd, NRcSO2Rd, CORc, C(O)ORc, or C(O)NRcRd; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is O, S, S(O), S(O2), or NRc; Y is a covalent bond, CH2, C(O), C═N—Rc, C═N—ORc, C═N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and each of Rc and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.
    • 本发明的特征在于式(I)的嘧啶化合物:芳基或杂芳基; R 2和R 4各自独立地是R c,卤素,硝基,氰基,异硫代,SR c或OR c; 或R 2和R 4一起是羰基; R 3是R c,链烯基,炔基,OR c,OC(O)R c,SO 2 R c,S(O)R c,S(O 2)NR c NR c C(O)OR d,NR c C(O)NR c, R d,NR c,SO 2 R d,COR c,C(O)OR c或C(O)NR c R d; R5是H或烷基; n是0,1,2,3,4,5或6; X是O,S,S(O),S(O 2)或NR c; Y是共价键,CH 2,C(O),C = NR c,C = N-OR c,C = N-SR c,O,S,S(O) )或NR ; Z是N或CH; U和V之一是N,另一个是CR ; 并且W是O,S,S(O),S(O 2),NR c或NC(O)R c; 其中R 1和R 2各自独立地是H,烷基,芳基,杂芳基; R c和R d各自独立地是H,烷基,芳基,杂芳基,环基,杂环基或烷基羰基。