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    Methods of treating cancer using a heat shock factor activity inhibitor
    1.
    发明申请
    Methods of treating cancer using a heat shock factor activity inhibitor 失效
    使用热休克因子活性抑制剂治疗癌症的方法

    公开(公告)号：US20030149077A1

    公开(公告)日：2003-08-07

    申请号：US10339063

    申请日：2003-01-09

    发明人： Shin-Ichi Yokota ,  Kozo Yamamoto ,  Souichi Morikawa ,  Yoshihide Fuse ,  Mikio Kitahara

    IPC分类号： A61K031/4525 ,  A61K031/4025 ,  C07D47/02

    CPC分类号： C07D405/06

    摘要： A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor. The novel compound benzo-1,3-dioxole provides an inhibitor of HSF activity or an inhibitor of inducing the production of a protein regulated by HSF, which inhibits the activity of a heat shock factor, a transcriptional regulatory factor, thereby in turn inhibiting transcription of a structural gene having a heat shock element sequence in the gene region for transcriptional regulation into RNA, and thus inhibiting translation of the gene into a protein, and resulting in inhibition of inducing production of RNA or protein encoded by the gene. It also provides a drug for treating or preventing cancer through thermotherapy and a drug for treating or preventing stress diseases such as depression.

    摘要翻译： 通过控制由热休克因子诱导的蛋白质的表达来提供疾病治疗。 新型化合物苯并-1,3-二氧杂环戊烷提供HSF活性的抑制剂或诱导产生由HSF调节的蛋白质的抑制剂，其抑制热休克因子（转录调节因子）的活性，从而进而抑制转录 在基因区域中具有用于转录调节成RNA的热休克元件序列的结构基因，从而抑制基因翻译成蛋白质，并导致抑制由该基因编码的RNA或蛋白质的产生。 它还提供通过热疗治疗或预防癌症的药物和用于治疗或预防压力疾病如抑郁症的药物。

    Halogen substituted tetracyclic tetrahydrofuran derivatives
    3.
    发明申请
    Halogen substituted tetracyclic tetrahydrofuran derivatives 失效
    卤素取代四环四氢呋喃衍生物

    公开(公告)号：US20030134852A1

    公开(公告)日：2003-07-17

    申请号：US10292270

    申请日：2002-11-12

    发明人： Jose Ignacio Andres-Gil ,  Francisco Javier Fernandez-Gadea ,  Pilar Gil-Lopetegui ,  Adolfo Diaz-Martinez

    IPC分类号： A61K031/5377 ,  A61K031/496 ,  A61K031/4525 ,  A61K031/4035 ,  A61K031/4025 ,  C07D413/02 ,  C07D45/02 ,  C07D47/02

    CPC分类号： C07D405/06 ,  C07D307/93 ,  C07D493/04

    摘要： This invention concerns the compounds of formula (I), 1 the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero, 1, 2, 3, 4, 5 or 6; X is CH2 or O; R1 and R2 each independently are hydrogen, C1-6alkyl, C1-6alkylcarbonyl, halomethylcarbonyl or C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3 and R4 are both halogen; or R3 is halogen and R4 is hydrogen; or R3 is hydrogen and R4 is halogen; and aryl is phenyl or phenyl substituted with 1, 2 or 3 substituents selected from halo, hydroxy, C1-6alkyl and halomethyl. The compounds of formula (I) may be used as therapeutic agents.

    摘要翻译： 本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中n为0,1,2,3,4,5或6; X是CH 2或O; R 1和R 2各自独立地为氢，C 1-6烷基，C 1-6烷基羰基，卤代甲基羰基或被羟基，C 1-6烷氧基，羧基，C 1-6烷基羰基氧基，C 1-6烷氧基羰基或芳基取代的C 1-6烷基。 或者R 1和R 2与它们所连接的氮原子一起可以形成吗啉基环或任选取代的杂环; R3和R4都是卤素; 或R3是卤素，R4是氢; 或R3是氢，R4是卤素; 并且芳基是苯基或被1,2或3个选自卤素，羟基，C 1-6烷基和卤代甲基的取代基取代的苯基。 式（I）化合物可用作治疗剂。

    Paroxetine compositions
    5.
    发明申请
    Paroxetine compositions 审中-公开
    帕罗西汀组合物

    公开(公告)号：US20010049442A1

    公开(公告)日：2001-12-06

    申请号：US09922072

    申请日：2001-08-03

    申请人： SmithKline Beecham p.l.c.

    发明人： Victor Witold Jacewicz ,  Neal Ward

    IPC分类号： A61K031/4525 ,  C07D47/02

    CPC分类号： A61K31/4525 ,  A61K9/1688

    摘要： Paroxetine hydrochloride is obtained in a free-flowing and easily soluble form (suitable for preparing solid formulations or aqueous solutions, suitable for parenteral use) by spray-drying solutions of paroxetine hydrochloride hemihydrate or other anhydrate/hydrate/solvate/amorphous forms.

    摘要翻译： 通过喷雾干燥的盐酸帕罗西汀半水合物或其他无水物/水合物/溶剂合物/无定形形式的溶液，以自由流动且容易溶解的形式（适于制备适于肠胃外使用的固体制剂或水溶液）获得盐酸帕罗西汀。

    Compositions and methods for chemotherapy having reduced nephrotoxicity
    8.
    发明申请
    Compositions and methods for chemotherapy having reduced nephrotoxicity 审中-公开
    化疗的组合物和方法具有降低的肾毒性

    公开(公告)号：US20020183333A1

    公开(公告)日：2002-12-05

    申请号：US10103520

    申请日：2002-03-19

    发明人： Sudhir V. Shah ,  Radhakrishna Baliga

    IPC分类号： A61K031/497 ,  A61K031/4525 ,  A61K031/325 ,  A61K031/10

    CPC分类号： A61K31/10 ,  A61K31/325 ,  A61K31/4525 ,  A61K31/497

    摘要： Compositions and methods for chemotherapy are disclosed. The compositions and methods disclose herein are effective inhibitors of chemotherapy-induced nephrotoxicity, yet unexpectedly do not inhibit the antineoplastic activity of the chemotherapeutic compound. The chemotherapeutic compositions and methods of the invention comprise an inhibitor of catalytic iron. In a preferred embodiment, the inhibitor is a cytochrome P450 inhibitor and the chemotherapeutic compound is cisplatin.

    摘要翻译： 公开了化疗的组合物和方法。 本文公开的组合物和方法是化学疗法诱导的肾毒性的有效抑制剂，但意外地不抑制化疗化合物的抗肿瘤活性。 本发明的化学治疗组合物和方法包括催化铁的抑制剂。 在优选的实施方案中，抑制剂是细胞色素P450抑制剂，化疗化合物是顺铂。

    Regimen and kit for amelioration of premature ejaculation
    9.
    发明申请
    Regimen and kit for amelioration of premature ejaculation 审中-公开
    用于改善早泄的方案和试剂盒

    公开(公告)号：US20020035131A1

    公开(公告)日：2002-03-21

    申请号：US09970293

    申请日：2001-10-03

    申请人： Pentech Pharmaceuticals, Inc.

    发明人： Ragab El-Rashidy ,  Chris McMahon

    IPC分类号： A61K031/4525

    CPC分类号： A61K31/4525

    摘要： Male patients suffering from premature ejaculation dysfunction are treated by an oral therapy regimen of administration of paroxetine substantially within several hours before sexual intercourse. The beneficial effect of the paroxetine treatment can be optimized and maintained by a combination oral therapy regimen in which the patient converts to continual maintenance paroxetine administration after an initial loading period of daily doses of paroxetine taken over of relatively short duration.

    摘要翻译： 患有早泄功能障碍的男性患者在性交前几小时内通过口服治疗方案治疗帕罗西汀。 帕罗西汀治疗的有益效果可以通过组合口服治疗方案进行优化和维持，其中患者在持续维持帕罗西汀的日剂量帕罗西汀的持续时间相对较短的初期加载期后转化为持续维持帕罗西汀。