Biopolymer marker indicative of disease state having a molecular weight of 2267 daltons
    111.
    发明申请
    Biopolymer marker indicative of disease state having a molecular weight of 2267 daltons 失效
    指示分子量为2267道尔顿的疾病状态的生物聚合物标记物

    公开(公告)号:US20020161183A1

    公开(公告)日:2002-10-31

    申请号:US09846348

    申请日:2001-04-30

    CPC classification number: G01N33/6893 G01N2800/042 Y10T436/24 Y10T436/25

    Abstract: The instant invention involves the use of a combination of preparatory steps in conjunction with mass spectroscopy and time-of-flight detection procedures to maximize the diversity of biopolymers which are verifiable within a particular sample. The cohort of biopolymers verified within such a sample is then viewed with reference to their ability to evidence at least one particular disease state; thereby enabling a diagnostician to gain the ability to characterize either the presence or absence of said at least one disease state relative to recognition of the presence and/or the absence of said biopolymer.

    Abstract translation: 本发明涉及使用组合的准备步骤与质谱法和飞行时间检测程序的组合,以使特定样品中可验证的生物聚合物的多样性最大化。 然后,在这样一个样本中验证的生物聚合物队列参照其证明至少一种特定疾病状态的能力; 从而使得诊断者能够获得表征所述至少一种疾病状态的存在或不存在与识别所述生物聚合物的存在和/或不存在的能力。

    Cyclosporins for the treatment of respiratory diseases
    117.
    发明申请
    Cyclosporins for the treatment of respiratory diseases 有权
    环孢菌素治疗呼吸系统疾病

    公开(公告)号:US20020142946A1

    公开(公告)日:2002-10-03

    申请号:US09800856

    申请日:2001-03-05

    CPC classification number: C07K7/645 A61K38/00

    Abstract: The present invention relates to novel semisynthetic cyclosporin analogs of Formula (I): 1 X is absent, nullC1-C6 alkyl-, or nullC3-C6 cycloalkyl- Y is selected from the group consisting of: (i) C(O)nullOnullR1, where R1 is hydrogen, C1-C6 alkyl, optionally substituted with halogen, heterocyclic, aryl, C1-C6 alkoxy, C1-C6 alkylthio, halogen-substituted C1-C6 alkoxy, or halogen-substituted C1-C6 alkylthio; (ii) C(O)nullSnullR1, where R1 is as previously defined; (iii) C(O)nullOCH2nullOC(O)R2, where R2 is C1-C6 alkyl, optionally substituted with halogen, C1-C6 alkoxy; C1-C6 alkylthio, heterocyclic or aryl; (iv) C(S)nullOnullR1, where R1 is as previously defined, and (v) C(S)nullSnullR1, where R1 is as previously defined; B is -nullAbu-, -Val-, -Thr- or -Nva-; and U is -(D)Ala-, -(D)Ser-, nullnullOnull(2-hydroxyethyl)(D)Sernull-, nullnullO-acyl(D)Sernull- or nullnullOnull(2-acyloxyethyl)(D)Sernull-.

    Abstract translation: 本发明涉及式(I)的新型半合成环孢菌素类似物:X不存在,-C 1 -C 6烷基 - 或-C 3 -C 6环烷基-Y选自:(i)C(O) - O-R 1,其中R 1是氢,任选被卤素,杂环,芳基,C 1 -C 6烷氧基,C 1 -C 6烷硫基,卤素取代的C 1 -C 6烷氧基或卤素取代的C 1 -C 6烷硫基取代的C 1 -C 6烷基; (ⅱ)C(O)-S-R 1,其中R 1如前所定义; (ⅲ)C(O)-OCH 2 -O(O)R 2,其中R 2为任选被卤素,C 1 -C 6烷氧基取代的C 1 -C 6烷基; C 1 -C 6烷硫基,杂环或芳基; (iv)C(S)-O-R 1,其中R 1如前所定义,和(ⅴ)C(S)-S-R 1,其中R 1如前所定义; B是-alphaAbu-,-Val-,-Thr-或-Nva-; 并且U是 - (D)Ala-, - (D)Ser-, - [O-(2-羟乙基)(D)Ser] - , - [O-酰基(D)Ser] - 或 - 2-酰氧基乙基)(D)Ser] - 。

    Deuterated cyclosporine analogs and their use as immunomodulating agents
    120.
    发明申请
    Deuterated cyclosporine analogs and their use as immunomodulating agents 审中-公开
    氘代环孢菌素类似物及其作为免疫调节剂的用途

    公开(公告)号:US20020132763A1

    公开(公告)日:2002-09-19

    申请号:US09985997

    申请日:2001-11-07

    Abstract: Cyclosporine derivatives are disclosed which possess enhanced efficacy and reduced toxicity over naturally occurring and other presently known cyclosporins and cyclosporine derivatives. The cyclosporine derivatives of the present invention are produced by chemical and isotopic substitution of the cyclosporine A (CsA) molecule by: (1) Chemical substitution and optionally deuterium substitution of amino acid 1; and (2) deuterium substitution at key sites of metabolism of the cyclosporine A molecule such as amino acids 1, 4, 9. Also disclosed are methods of producing the cyclosporine derivatives and method of producing immunosuppression with reduced toxicity with the disclosed cyclosporine derivatives.

    Abstract translation: 公开了与天然存在的和其他目前已知的环孢菌素和环孢菌素衍生物相比具有增强的功效和降低的毒性的环孢菌素衍生物。 本发明的环孢菌素衍生物通过以下方式通过环孢菌素A(CsA)分子的化学和同位素取代产生:(1)氨基酸1的化学取代和任选的氘取代; 和(2)在环孢菌素A分子的代谢关键位置的氘代替,例如氨基酸1,4,9。还公开了产生环孢菌素衍生物的方法和与所公开的环孢菌素衍生物一起产生具有降低的毒性的免疫抑制的方法。

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