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    • 23. 发明授权
    • Pyrimidine compounds
    • 嘧啶化合物
    • US07470685B2
    • 2008-12-30
    • US11041537
    • 2005-01-21
    • Lijun SunMitsunori OnoElena KostikYumiko Wada
    • Lijun SunMitsunori OnoElena KostikYumiko Wada
    • A61K31/506A61P3/10A61P17/06A61P19/02A61P25/28C07D239/24C07D401/04C07D405/04C07D413/04C07D417/04
    • C07D239/48A61K31/506A61K31/53A61K31/5377A61K31/541C07D401/12C07D401/14C07D403/12
    • This invention features pyrimidine compounds of formula (I): R1 is in which one of Ra and Rb is H or alkyl, and the other is aryl or heteroaryl optionally substituted with Rd and Rem; each of R2 and R4 is H; R3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is NRc; Y is 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 Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; Rd is halogen, CN, alkyl, alkyloxy, alkylcarbonyl, alkyloxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, hydroxyalkyl, alkylamino, or alkylaminocarbonyl; Re is halogen, CN, hydroxyl, alkyl, aryl, heteroaryl, alkoxyl, aryloxyl, or heteroaryloxyl; and m is 0, 1, 2, 3, or 4. The pyrimidine compounds can be used to treat an IL-12 overproduction-related disorder (e.g., rheumatoid arthritis, sepsis, Crohn's disease, multiple sclerosis, psoriasis, or insulin-dependent diabetes mellitus).
    • 本发明的特征在于式(I)的嘧啶化合物:其中R 1和R b中的一个是H或烷基,另一个是任选被Rd和Rem取代的芳基或杂芳基; R2和R4各自为H; R3是H,烷基,芳基,杂芳基,环基,杂环基或烷基羰基; R5是H或烷基; n是0,1,2,3,4,5或6; X是NRc; 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 c是H,烷基,芳基,杂芳基,环基,杂环基或烷基羰基; Rd是卤素,CN,烷基,烷氧基,烷基羰基,烷氧基羰基,芳氧基羰基,杂芳氧基羰基,羟基烷基,烷基氨基或烷基氨基羰基; Re是卤素,CN,羟基,烷基,芳基,杂芳基,烷氧基,芳氧基或杂芳氧基; 嘧啶化合物可用于治疗IL-12过度生产相关疾病(例如类风湿性关节炎,败血症,克罗恩病,多发性硬化,牛皮癣或胰岛素依赖型 糖尿病)。
    • 24. 发明授权
    • Synthesis of taxol enhancers
    • 紫杉醇增强剂的合成
    • US07435843B2
    • 2008-10-14
    • US11440429
    • 2006-05-24
    • Shoujun ChenLijun SunZhi-Qiang XiaKeizo KoyaMitsunori Ono
    • Shoujun ChenLijun SunZhi-Qiang XiaKeizo KoyaMitsunori Ono
    • C07C327/56
    • 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 > 2 独立地是脂族基团,取代的脂族基团,芳基或取代的芳基,或R 1和R 2与 与它们键合的碳原子和氮原子形成任选地与芳环稠合的非芳族杂环。 当R 2是芳基或取代的芳基时,R 5是肼保护基; 当R 2是脂族或取代的脂族基团时,R 5是-H或肼保护基。 R 10是-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。
    • 26. 发明申请
    • Synthesis of taxol enhancers
    • 紫杉醇增强剂的合成
    • US20060281811A1
    • 2006-12-14
    • US11440429
    • 2006-05-24
    • Shoujun ChenLijun SunZhi-Qiang XiaKeizo KoyaMitsunori Ono
    • Shoujun ChenLijun SunZhi-Qiang XiaKeizo KoyaMitsunori Ono
    • A61K31/235A61K31/195
    • 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 > 2 独立地是脂族基团,取代的脂族基团,芳基或取代的芳基,或R 1和R 2与 与它们键合的碳原子和氮原子形成任选地与芳环稠合的非芳族杂环。 当R 2是芳基或取代的芳基时,R 5是肼保护基; 当R 2是脂族或取代的脂族基团时,R 5是-H或肼保护基。 R 10是-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。