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    • 31. 发明申请
    • Isomers and 42-epimers of rapamycin ester analogs, methods of making and using the same
    • 雷帕霉素酯类似物的异构体和42-差向异构体,制备和使用它们的方法
    • US20070203169A1
    • 2007-08-30
    • US11364313
    • 2006-02-28
    • Jonathon Zhao
    • Jonathon Zhao
    • A61K31/4745C07D491/14
    • C07D498/18
    • Isomers and 42-epimers of rapamycin ester analogs and pharmaceutically acceptable salts or prodrugs thereof, are immunomodulatory agents and are useful in the treatment of restenosis and immune and autoimmune diseases. Also disclosed are cancer-, fungal growth-, restenosis-, post-transplant tissue rejection- and immune- and autoimmune disease-inhibiting compositions and a method of inhibiting cancer, fungal growth, restenosis, post-transplant tissue rejection, and immune and autoimmune disease in a mammal. One particular preferred application of such isomers and 42-epimers of rapamycin ester analogs is in medicated devices and local vascular delivery wherein the stability and lipid solubility and subsequently diffusion through tissue and cell membranes are essential to the success of rapamycin containing combination devices.
    • 雷帕霉素酯类似物和其药学上可接受的盐或前药的异构体和42-差向异构体是免疫调节剂,可用于治疗再狭窄和免疫和自身免疫性疾病。 还公开了癌症,真菌生长,再狭窄,移植后组织排斥和免疫和自身免疫疾病抑制组合物以及抑制癌症,真菌生长,再狭窄,移植后组织排斥和免疫和自身免疫的方法 哺乳动物的疾病 雷帕霉素酯类似物的这种异构体和42-差向异构体的一个特别优选的应用是在药物装置和局部血管输送中,其中稳定性和脂质溶解度以及随后通过组织和细胞膜的扩散对于含雷帕霉素的组合装置的成功是必需的。
    • 37. 发明申请
    • Camptothecin derivatives and improved synthetic methods
    • 喜树碱衍生物和改进的合成方法
    • US20070099948A1
    • 2007-05-03
    • US11588021
    • 2006-10-26
    • Brian Shull
    • Brian Shull
    • A61K31/4745C07D491/14
    • C07D491/22
    • The present invention relates to compositions and methods for preparing pharmaceutical compositions. In some embodiments, the invention includes compounds and methods of resolving chiral compounds. In some embodiments, the invention includes chiral and crystalline compositions and hydrates. In some embodiments, the invention contemplates compositions comprising camptothecin derivatives and synthetic intermediates thereof. In some embodiments, the invention includes methods of protecting, inserting, modifying, separating isomers, and removing chemical groups.
    • 本发明涉及制备药物组合物的组合物和方法。 在一些实施方案中,本发明包括拆分手性化合物的化合物和方法。 在一些实施方案中,本发明包括手性和结晶组合物和水合物。 在一些实施方案中,本发明涉及包含喜树碱衍生物及其合成中间体的组合物。 在一些实施方案中,本发明包括保护,插入,修饰,分离异构体和除去化学基团的方法。
    • 40. 发明申请
    • Phosphorus-containing compounds & uses thereof
    • 含磷化合物及其用途
    • US20060264456A1
    • 2006-11-23
    • US11494418
    • 2006-07-27
    • Chester MetcalfLeonard RozamusYihan WangDavid Berstein
    • Chester MetcalfLeonard RozamusYihan WangDavid Berstein
    • A61K31/4745C07D491/14
    • A61K45/06A61K31/675C07F9/6561
    • This invention concerns a new family of phosphorus-containing compounds containing a moiety JQA- in which: A is absent or is —O—, —S— or —NR2—; Q is absent or (if A is —O—, —S— or —NR2—) Q may be —V—, —OV—, —SV—, or —NR2V—, where V is an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, such that J is linked to the cyclohexyl ring directly, through A or through VA, OVA, SVA or NR2VA; K is O or S; each occurrence of Y is independently —O—, —S—, —NR2—, or a bond linking a R5 moiety to P; each occurrence of R2 and R5 is independently an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, or H; and each occurrence of R6 is independently —PK(YR5)(YR5), —SO2(YR5) or —(O)(YR5); so long as any R2, or R5 moiety linked directly to P is not H; wherein two R2, R5 and/or R6 moieties may be chemically linked to one another to form a ring; each occurrence of G is independently —O—, —S—, —NR2— or (M)x; each occurrence of M is independently a substituted or unsubstituted methylene moiety, and any M-M′ moiety may be saturated or unsaturated; each occurrence of x is independently an integer from 1-6; and the other variables are as defined herein.
    • 本发明涉及含有部分JQA-的新的含磷化合物族,其中:A不存在或为-O - , - S-或-NR 2 - 。 Q不存在或(如果A是-O-,-S-或-NR 2 - )Q可以是-V-,-OV-,-SV-或-NR 2 V-,其中V是脂族,杂脂族,芳基或杂芳基部分,使得J通过A或通过VA,OVA,SVA或NR 2 O直接与环己基环连接 > VA; K为O或S; 每次出现的Y独立地是-O - , - S - , - NR 2 - 或 - 连接R 5部分与P的键; 每个出现的R 2和R 5独立地是脂族,杂脂族,芳基或杂芳基部分,或H; 且每次出现的R 6独立地为-PK(YR 5),(YR 5), - SO 2 - (YR 5)或 - (O)(YR 5); 只要与P直接连接的任何R“或R 5”部分不是H; 其中两个R 2,R 5和/或R 6 O 6部分可以彼此化学连接以形成环; 每次出现的G独立地是-O - , - S - , - NR 2 - 或(M)x。 每次出现的M独立地是取代或未取代的亚甲基部分,任何M-M'部分可以是饱和或不饱和的; 每次出现的x独立为1-6的整数; 其他变量如本文所定义。