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    Pyrimidine compounds
    4.
    发明授权
    Pyrimidine compounds 失效
    嘧啶化合物

    公开(公告)号：US07465725B2

    公开(公告)日：2008-12-16

    申请号：US11193001

    申请日：2005-07-29

    申请人： Mitsunori Ono ,  Lijun Sun ,  Teresa Przewloka ,  Shijie Zhang ,  Elena Kostik ,  Weiwen Ying ,  Yumiko Wada ,  Keizo Koya

    发明人： Mitsunori Ono ,  Lijun Sun ,  Teresa Przewloka ,  Shijie Zhang ,  Elena Kostik ,  Weiwen Ying ,  Yumiko Wada ,  Keizo Koya

    IPC分类号： A61K31/506 ,  A61P17/06 ,  A61P19/02 ,  A61P25/28 ,  C07D401/04 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04 ,  C07D239/24

    CPC分类号： C07D239/48 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/541 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

    摘要： This invention features pyrimidine compounds of formula (I): R1 is 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： 本发明具有式（I）的嘧啶化合物：R1是芳基或杂芳基; R 2和R 4各自独立地是Rc，卤素，硝基，氰基，异硫脲，SRc或ORc; 或R 2和R 4一起是羰基; R3是Rc，烯基，炔基，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或C（O）NRcRd; 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，CH2，C（O），C-N-Rc，C-N-ORc，C-N-SRc，O，S，S（O），S（O 2）或NRc; Z是N或CH; U和V之一是N，另一个是CRc; 并且W是O，S，S（O），S（O 2），NR c或NC（O）R c; 其中R a和R b各自独立地为H，烷基，芳基，杂芳基; R c和R d各自独立地为H，烷基，芳基，杂芳基，环基，杂环基或烷基羰基。

    Bis(thio-hydrazide amide) salts for treatment of cancers
    5.
    发明授权
    Bis(thio-hydrazide amide) salts for treatment of cancers 有权
    用于治疗癌症的双（硫代酰肼）酰胺盐

    公开(公告)号：US08048925B2

    公开(公告)日：2011-11-01

    申请号：US12871587

    申请日：2010-08-30

    申请人： Keizo Koya ,  Lijun Sun ,  Elena Kostik ,  Farid Vaghefi ,  Shoujun Chen ,  Noriaki Tatsuta ,  Guiqing Liang ,  Takayo Inoue ,  Zhi-Qiang Xia

    发明人： Keizo Koya ,  Lijun Sun ,  Elena Kostik ,  Farid Vaghefi ,  Shoujun Chen ,  Noriaki Tatsuta ,  Guiqing Liang ,  Takayo Inoue ,  Zhi-Qiang Xia

    IPC分类号： A61K31/16

    CPC分类号： C07D305/14 ,  C07C327/56 ,  C07C2601/02

    摘要： Disclosed are bis(thio-hydrazide amide) disalts, which are represented by Structural Formula (I): Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group. R1-R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 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. Z is —O or —S. M+ is a pharmaceutically acceptable monovalent cation and M2+ is a pharmaceutically acceptable divalent cation.Also, disclosed are pharmaceutical compositions comprising a bis(thio-hydrazide amide) disalt described above. Further disclosed are methods of treating a subject with cancer. The methods comprise the step of administering an effective amount of a bis(thio-hydrazide amide) disalt described above.

    摘要翻译： 公开了由结构式（I）表示的双（硫代 - 酰肼酰胺）二醛：Y是共价键或取代或未取代的直链烃基。 R 1 -R 4独立地为-H，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 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。 Z是-O或-S。 M +是药学上可接受的一价阳离子，M2 +是药学上可接受的二价阳离子。 还公开了包含上述双（硫代 - 酰肼酰胺）二盐的药物组合物。 进一步公开的是用癌症治疗受试者的方法。 所述方法包括施用有效量的上述双（硫代 - 酰肼酰胺）二盐的步骤。

    BIS(THIO-HYDRAZIDE AMIDE) SALTS FOR TREATMENT OF CANCERS
    6.
    发明申请
    BIS(THIO-HYDRAZIDE AMIDE) SALTS FOR TREATMENT OF CANCERS 有权
    BIS（THIO-HYDRAZIDE AMIDE）用于治疗癌症的药物

    公开(公告)号：US20090281172A1

    公开(公告)日：2009-11-12

    申请号：US12503661

    申请日：2009-07-15

    申请人： Keizo Koya ,  Lijun Sun ,  Elena Kostik ,  Farid Vaghefi ,  Shoujun Chen ,  Noriaki Tatsuta ,  Guiqing Liang ,  Takayo Inoue ,  Zhi-Qiang Xia

    发明人： Keizo Koya ,  Lijun Sun ,  Elena Kostik ,  Farid Vaghefi ,  Shoujun Chen ,  Noriaki Tatsuta ,  Guiqing Liang ,  Takayo Inoue ,  Zhi-Qiang Xia

    IPC分类号： A61K31/166 ,  A61P35/00 ,  C07C327/48 ,  A61K31/337

    CPC分类号： C07D305/14 ,  C07C327/56 ,  C07C2601/02

    摘要： Disclosed are bis(thio-hydrazide amide) disalts, which are represented by Structural Formula (I): Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group. R1-R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 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. Z is —O or —S. M+ is a pharmaceutically acceptable monovalent cation and M2+ is a pharmaceutically acceptable divalent cation.Also, disclosed are pharmaceutical compositions comprising a bis(thio-hydrazide amide) disalt described above. Further disclosed are methods of treating a subject with cancer. The methods comprise the step of administering an effective amount of a bis(thio-hydrazide amide) disalt described above.

    摘要翻译： 公开了由结构式（I）表示的双（硫代 - 酰肼酰胺）二醛：Y是共价键或取代或未取代的直链烃基。 R 1 -R 4独立地为-H，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 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。 Z是-O或-S。 M +是药学上可接受的一价阳离子，M2 +是药学上可接受的二价阳离子。 还公开了包含上述双（硫代 - 酰肼酰胺）二盐的药物组合物。 进一步公开的是用癌症治疗受试者的方法。 所述方法包括施用有效量的上述双（硫代 - 酰肼酰胺）二盐的步骤。

    Bis(thio-hydrazide amide) salts for treatment of cancers
    8.
    发明授权
    Bis(thio-hydrazide amide) salts for treatment of cancers 有权
    用于治疗癌症的双（硫代酰肼）酰胺盐

    公开(公告)号：US07795313B2

    公开(公告)日：2010-09-14

    申请号：US12503661

    申请日：2009-07-15

    申请人： Keizo Koya ,  Lijun Sun ,  Elena Kostik ,  Farid Vaghefi ,  Shoujun Chen ,  Noriaki Tatsuta ,  Guiqing Liang ,  Takayo Inoue ,  Zhi-Qiang Xia

    发明人： Keizo Koya ,  Lijun Sun ,  Elena Kostik ,  Farid Vaghefi ,  Shoujun Chen ,  Noriaki Tatsuta ,  Guiqing Liang ,  Takayo Inoue ,  Zhi-Qiang Xia

    IPC分类号： A61K31/16

    CPC分类号： C07D305/14 ,  C07C327/56 ,  C07C2601/02

    摘要： Disclosed are bis(thio-hydrazide amide) disalts, which are represented by Structural Formula (I): Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group. R1-R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 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. Z is —O or —S. M+ is a pharmaceutically acceptable monovalent cation and M2+ is a pharmaceutically acceptable divalent cation. Also, disclosed are pharmaceutical compositions comprising a bis(thio-hydrazide amide) disalt described above. Further disclosed are methods of treating a subject with cancer. The methods comprise the step of administering an effective amount of a bis(thio-hydrazide amide) disalt described above.

    摘要翻译： 公开了由结构式（I）表示的双（硫代 - 酰肼酰胺）二醛：Y是共价键或取代或未取代的直链烃基。 R 1 -R 4独立地为-H，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 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。 Z是-O或-S。 M +是药学上可接受的一价阳离子，M2 +是药学上可接受的二价阳离子。 还公开了包含上述双（硫代 - 酰肼酰胺）二盐的药物组合物。 进一步公开的是用癌症治疗受试者的方法。 所述方法包括施用有效量的上述双（硫代 - 酰肼酰胺）二盐的步骤。

    BIS (thio-hydrazide amide) salts for treatment of cancers
    9.
    发明授权
    BIS (thio-hydrazide amide) salts for treatment of cancers 失效
    用于治疗癌症的BIS（硫代酰肼）酰胺盐

    公开(公告)号：US07579503B2

    公开(公告)日：2009-08-25

    申请号：US12148312

    申请日：2008-04-18

    申请人： Keizo Koya ,  Lijun Sun ,  Elena Kostik ,  Farid Vaghefi ,  Shoujun Chen ,  Noriaki Tatsuta ,  Guiqing Liang ,  Takayo Inoue ,  Zhi-Qiang Xia

    发明人： Keizo Koya ,  Lijun Sun ,  Elena Kostik ,  Farid Vaghefi ,  Shoujun Chen ,  Noriaki Tatsuta ,  Guiqing Liang ,  Takayo Inoue ,  Zhi-Qiang Xia

    IPC分类号： C07C327/38 ,  A61K31/16

    CPC分类号： C07D305/14 ,  C07C327/56 ,  C07C2601/02

    摘要： Disclosed are bis(thio-hydrazide amide) disalts, which are represented by Structural Formula (I): Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group. R1-R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 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. Z is —O or —S. M+ is a pharmaceutically acceptable monovalent cation and M2+ is a pharmaceutically acceptable divalent cation.Also, disclosed are pharmaceutical compositions comprising a bis(thio-hydrazide amide) disalt described above. Further disclosed are methods of treating a subject with cancer. The methods comprise the step of administering an effective amount of a bis(thio-hydrazide amide) disalt described above.

    摘要翻译： 公开了由结构式（I）表示的双（硫代 - 酰肼酰胺）二醛：Y是共价键或取代或未取代的直链烃基。 R 1 -R 4独立地为-H，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 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。 Z是-O或-S。 M +是药学上可接受的一价阳离子，M2 +是药学上可接受的二价阳离子。 还公开了包含上述双（硫代 - 酰肼酰胺）二盐的药物组合物。 进一步公开的是用癌症治疗受试者的方法。 所述方法包括施用有效量的上述双（硫代 - 酰肼酰胺）二盐的步骤。