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18 条记录 (耗时 0.031 秒)

    Compositions and Methods Employing Aminopterin
    1.
    发明申请
    Compositions and Methods Employing Aminopterin 审中-公开
    使用氨蝶呤的组合物和方法

    公开(公告)号：US20100009998A1

    公开(公告)日：2010-01-14

    申请号：US12564912

    申请日：2009-09-22

    申请人： Barton Kamen ,  Peter Cole ,  Angela Smith ,  John A. Zebala

    发明人： Barton Kamen ,  Peter Cole ,  Angela Smith ,  John A. Zebala

    IPC分类号： A61K31/4985 ,  A61P35/00

    CPC分类号： A61K31/519

    摘要： The present invention relates to pharmaceutical compositions containing the antifolate aminopterin, processes for making the compositions, and methods of using them to treat disorders in adult and pediatric patients. Pharmaceutical compositions substantially free of impurities are provided comprising a therapeutically effective amount of aminopterin, or a pharmaceutically acceptable salt thereof. Relative to the teachings of the prior art, the disclosed methods and compositions provide unexpected improvements that include a greater interpatient oral bioavailability in pediatric patients, a smaller interpatient coefficient of variation of oral bioavailability, a smaller mean intrapatient coefficient of variation of oral bioavailability, a greater therapeutic index, a smaller coefficient of variation of toxicity, efficacy in combination therapy, and efficacy of certain polyglutamated metabolites.

    摘要翻译： 本发明涉及含有抗叶酸氨蝶呤的药物组合物，用于制备组合物的方法，以及使用它们治疗成人和儿科患者的疾病的方法。 提供了基本上不含杂质的药物组合物，其包含治疗有效量的氨基喋呤或其药学上可接受的盐。 相对于现有技术的教导，所公开的方法和组合物提供意想不到的改进，其包括在儿科患者中具有更大的患者口服生物利用度，口服生物利用度的较小的间质变异系数，口服生物利用度的较小的平均脑室内变异系数 更大的治疗指数，较小的毒性变异系数，联合治疗的疗效以及某些聚谷氨酸代谢物的功效。

    Pharmaceutical composition comprising racemic aminopterin
    2.
    发明授权
    Pharmaceutical composition comprising racemic aminopterin 有权
    包含外消旋氨喋呤的药物组合物

    公开(公告)号：US08349837B2

    公开(公告)日：2013-01-08

    申请号：US12692593

    申请日：2010-01-23

    申请人： John A. Zebala ,  Dean Y. Maeda ,  Joel R. Morgan ,  Stuart J. Kahn

    发明人： John A. Zebala ,  Dean Y. Maeda ,  Joel R. Morgan ,  Stuart J. Kahn

    IPC分类号： A61K31/495 ,  A01N43/58 ,  A01N43/60 ,  C07D475/00

    CPC分类号： A61K31/519

    摘要： There is disclosed a pharmaceutical composition comprising racemic aminopterin or pharmaceutically acceptable salts thereof. There is further disclosed a method to treat a disorder in a patient comprising administering a therapeutically effective amount of racemic aminopterin or pharmaceutically acceptable salts of racemic aminopterin. More particularly, there is disclosed a method for treating disorders modulated by at least dihydrofolate reductase activity, such as cancers and inflammatory disorders, wherein the method comprises administering to a patient in need thereof a therapeutically effective amount of racemic aminopterin or a pharmaceutically acceptable salt thereof.

    摘要翻译： 公开了包含外消旋氨基蝶呤或其药学上可接受的盐的药物组合物。 进一步公开了一种治疗患者疾病的方法，包括给予治疗有效量的外消旋氨基蝶呤或外消旋氨基蝶呤的药学上可接受的盐。 更具体地，公开了一种治疗由至少二氢叶酸还原酶活性调节的疾病如癌症和炎性疾病的方法，其中所述方法包括向有需要的患者施用治疗有效量的外消旋氨基蝶呤或其药学上可接受的盐 。

    PHOTOCLEAVABLE SENSE-ANTISENSE COMPLEX
    3.
    发明申请
    PHOTOCLEAVABLE SENSE-ANTISENSE COMPLEX 有权
    可拍摄的感觉反应复合物

    公开(公告)号：US20100105120A1

    公开(公告)日：2010-04-29

    申请号：US12489434

    申请日：2009-06-23

    申请人： John A. Zebala

    发明人： John A. Zebala

    IPC分类号： C12N13/00 ,  C07H21/04

    CPC分类号： C12N13/00 ,  C12N15/111 ,  C12N2310/14 ,  C12N2310/318 ,  C12N2310/3181 ,  C12N2310/3233 ,  C12N2310/344 ,  C12N2320/51

    摘要： There is disclosed a photocleavable sense-antisense nucleobase polymer complex capable of modulating gene expression comprising an unnatural antisense nucleobase polymer that targets an mRNA, and a photocleavable sense nucleobase polymer noncovalently bound to the antisense nucleobase polymer, wherein the photocleavable sense nucleobase polymer comprises a plurality of nucleobase polymers connected by a photocleavable linkage. There is also disclosed a method for controlling the time and spatial position of gene expression comprising selecting a target mRNA, introducing the photocleavable sense-antisense nucleobase polymer complex into a cell, and selectively irradiating the cell with light.

    摘要翻译： 公开了能够调节基因表达的可光切割的有义 - 反义核碱基聚合物复合物，其包含靶向mRNA的非天然反义核碱基聚合物和非共价结合于反义核碱基聚合物的可光切割的有义核碱基聚合物，其中可光致裂解的感觉核碱基聚合物包含多个 的核碱基聚合物通过可光切割连接键连接。 还公开了一种用于控制基因表达的时间和空间位置的方法，包括选择靶mRNA，将可光切割的有义 - 反义核碱基聚合物复合物引入细胞，并用光选择性照射细胞。

    Stable solid dosage forms of aminopterin
    5.
    发明授权
    Stable solid dosage forms of aminopterin 有权
    稳定的氨基蝶呤固体剂型

    公开(公告)号：US09168256B2

    公开(公告)日：2015-10-27

    申请号：US11928257

    申请日：2007-10-30

    申请人： Absar Faruqui ,  John A. Zebala ,  Barton A. Kamen

    发明人： Absar Faruqui ,  John A. Zebala ,  Barton A. Kamen

    IPC分类号： A61K31/519

    CPC分类号： A61K31/519

    摘要： There is disclosed stable pharmaceutical compositions containing pharmaceutically acceptable salts of aminopterin surface deposited onto solid excipients. The stable pharmaceutical compositions are hermetically sealed from the atmosphere. The formation of degradation products of aminopterin is reduced or eliminated.

    摘要翻译： 公开了稳定的药物组合物，其含有沉积在固体赋形剂上的氨基蝶呤表面药学上可接受的盐。 将稳定的药物组合物与大气密封。 氨蝶呤的降解产物的形成被减少或消除。

    COMPOSITIONS AND METHODS FOR OVERCOMING RESISTANCE TO TRAMADOL
    6.
    发明申请
    COMPOSITIONS AND METHODS FOR OVERCOMING RESISTANCE TO TRAMADOL 审中-公开
    用于阻断TRAMADOL的组合物和方法

    公开(公告)号：US20130011444A1

    公开(公告)日：2013-01-10

    申请号：US13543883

    申请日：2012-07-08

    申请人： John A. Zebala

    发明人： John A. Zebala

    IPC分类号： A61K31/135 ,  A61K9/00 ,  A61P25/00 ,  A61P25/30 ,  A61P3/04 ,  A61P13/00 ,  C07C215/42 ,  A61P25/04

    摘要： There is disclosed a composition for oral administration of O-desmethyltramadol. There is further disclosed a method for treating disorders modulated by at least opiate receptor activity or monoamine activity, including acute and chronic pain, comprising administering a pharmaceutical formulation comprising O-desmethyltramadol. Compositions and methods are also provided that are effective for overcoming resistance to tramadol in patients.

    摘要翻译： 公开了口服O-去甲基曲马多的组合物。 还公开了一种治疗由至少阿片受体活性或单胺活性调节的疾病的方法，包括急性和慢性疼痛，包括给予包含O-去甲基曲马多的药物制剂。 还提供了有效克服患者中曲马多的抗性的组合物和方法。

    Facile process for the preparation of high-purity aminopterin
    8.
    发明授权
    Facile process for the preparation of high-purity aminopterin 有权
    制备高纯度氨基蝶呤的简便方法

    公开(公告)号：US07235660B1

    公开(公告)日：2007-06-26

    申请号：US11619102

    申请日：2007-01-02

    申请人： John A. Zebala

    发明人： John A. Zebala

    IPC分类号： C07D475/00 ,  C07D475/08

    CPC分类号： C07D475/08

    摘要： A process for the preparation of aminopterin with a purity greater than 90%, which comprises reacting folic acid, with a silazane in an organic solvent at a temperature from 60 to 180° C., the said solvent being a tertiary amine organic solvent, or, if a catalyst which is acid in nature is present, a basic organic solvent or acetonitrile, and further adding water such that there is about 2.8 to 7.0 mole water for each mole of folic acid.

    摘要翻译： 一种制备纯度大于90％的氨基蝶呤的方法，其包括使叶酸与有机溶剂中的硅氮烷在60至180℃的温度下反应，所述溶剂是叔胺有机溶剂，或 如果存在本质上是酸的催化剂，碱性有机溶剂或乙腈，并进一步加入水，使得每摩尔叶酸具有约2.8-7.0摩尔的水。