Heterocyclic compounds
    91.
    发明授权

    公开(公告)号:US07122665B2

    公开(公告)日:2006-10-17

    申请号:US10686505

    申请日:2003-10-14

    摘要: This invention features a compound of formula (I): R1 is aryl or heteroaryl; each of R2 and R4, independently, is H, halogen, CN, alkyl, ORa, or NRaRb; R3 is H, halogen, CN, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyclyl, heterocyclyl, ORa, OC(O)Ra, OC(O)NRaRb, NRaRb, NRaC(O)Rb, NRaS(O)Rb, NRaS(O)2Rb, NRaC(O)NRbRc, NRaC(S)NRbRc, NRaC(NRb)NRcRd, NRaC(O)ORb, S(O)NRaRb, S(O)2NRaRb, S(O)Ra, S(O)2Ra, C(O)Ra, C(O)ORa, or C(O)NRaRb; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; A is O, S, S(O), S(O)2, or NRe; B is N or CRf; X is O, S, S(O), S(O)2, NRe, or C(O); Y is a covalent bond, C(O), C═NRa, O, S, S(O), S(O)2, or NRe; Z is N or CH; each of U and V, independently, is N or CR; and W is O, S, or NRe; in which each of Ra, Rb, Rc, and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl; Re is H, alkyl, aryl, acyl, or sufonyl; and Rf is H, alkyl, aryl, acyl, sulfonyl, alkoxyl, amino, ester, amide, CN, or halogen. The compound is useful for treating an interleukin-12 overproduction-related disorder.

    Pyrimidine compounds
    92.
    发明授权
    Pyrimidine compounds 有权
    嘧啶化合物

    公开(公告)号:US06693097B2

    公开(公告)日:2004-02-17

    申请号:US10000742

    申请日:2001-11-30

    IPC分类号: C07D41704

    摘要: 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.

    摘要翻译: 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。

    Synthesis of taxol enhancers
    94.
    发明申请
    Synthesis of taxol enhancers 失效
    紫杉醇增强剂的合成

    公开(公告)号:US20090005594A1

    公开(公告)日:2009-01-01

    申请号:US12231217

    申请日:2008-08-29

    IPC分类号: C07C327/00

    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): 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.

    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。

    Synthesis of taxol enhancers
    95.
    发明授权
    Synthesis of taxol enhancers 失效
    紫杉醇增强剂的合成

    公开(公告)号:US07652168B2

    公开(公告)日:2010-01-26

    申请号:US12231217

    申请日:2008-08-29

    IPC分类号: C07C327/56

    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): 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.

    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。