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    COMPOSITIONS COMPRISING FLAVOPIRIDOL AND THEIR USE FOR HIV THERAPY
    91.
    发明申请
    COMPOSITIONS COMPRISING FLAVOPIRIDOL AND THEIR USE FOR HIV THERAPY 审中-公开
    包含氟维拉多的组合物及其用于艾滋病毒治疗的用途

    公开(公告)号：WO01060367A1

    公开(公告)日：2001-08-23

    申请号：PCT/US2001/004898

    申请日：2001-02-15

    IPC: A61K31/453 ,  A61K45/06 ,  A61P31/18 ,  A61K31/445

    CPC classification number: A61K45/06 ,  A61K31/453 ,  A61K2300/00

    Abstract: Disclosed is the unexpected discovery that flavopiridol binds tightly to the transcription elongation factor, P-TEFb and dramatically inhibits its activity. As P-TEFb is required for HIV propagation and replication, this invention provides new methods, compositions and kits for the effective treatment of HIV infections and AIDS using flavopiridol, both alone and in combination with other therapies.

    Abstract translation: 披露了意想不到的发现，flavopiridol与转录延伸因子P-TEFb紧密结合并显着抑制其活性。 由于P-TEFb是HIV繁殖和复制所必需的，本发明提供了用于单独使用和与其它疗法组合的有效治疗HIV感染和AIDS的新方法，组合物和试剂盒。

    THE USE OF 4-H-1-BENZOPYRAN-4-ONE DERIVATIVES AS INHIBITORS OF SMOOTH MUSCLE CELL PROLIFERATION
    92.
    发明申请
    THE USE OF 4-H-1-BENZOPYRAN-4-ONE DERIVATIVES AS INHIBITORS OF SMOOTH MUSCLE CELL PROLIFERATION 审中-公开
    4-H-1-BENZOPYRAN-4-ONE衍生物作为平滑肌细胞增殖抑制剂的应用

    公开(公告)号：WO00044362A2

    公开(公告)日：2000-08-03

    申请号：PCT/US2000/001104

    申请日：2000-01-18

    IPC: C07D405/04 ,  A61K31/00 ,  A61K31/445 ,  A61K31/453 ,  A61P9/00 ,  A61P9/10 ,  A61P21/00 ,  A61P35/00 ,  A61P43/00

    CPC classification number: A61K31/453

    Abstract: Smooth muscle cells (SMC) proliferation is a critical component of neointimal formation in many animal models of vascular injury, and in many human lesions as well. Cell cycle inhibition by gene transfer techniques can block SMC proliferation and lesion formation in many animal models, although these methods are not yet applicable to the treatment of human disease. Flavopiridol is a recently identified, potent, orally available cyclin-dependent kinase inhibitor. Given the role of smooth muscle cell (SMC) proliferation in vascular disease, we tested the effects of flavopiridol, a recently identified cyclin-dependent kinase inhibitor, on SMC growth in vitro and in vivo. Flavopiridol (75 nmol/L) potently blocked SMC proliferation, an effect that was associated with downregulation of cyclin-dependent kinase activity and cell cycle-related gene expression. We examined the effects of flavopiridol on SMC proliferation in vivo in the rat carotid injury model. Flavopiridol (5 mg/kg) decreased neointimal size by 35% and 39% at 7 and 14 days, respectively, after balloon injury. Flavopiridol may be a potential therapeutic tool in the treatement of SMC-rich vascular lesions. 4-H-1-benzopyran-4-one derivatives inhibit smooth muscle cell proliferation at low dosage levels.

    Abstract translation: 平滑肌细胞（SMC）增殖是血管损伤的许多动物模型以及许多人类病变中新内膜形成的关键组成部分。 通过基因转移技术的细胞周期抑制可以阻断许多动物模型中的SMC增殖和病变形成，尽管这些方法尚不适用于人类疾病的治疗。 黄酮类药物是最近确定的，有效的，口服的细胞周期蛋白依赖性激酶抑制剂。 鉴于血管疾病中平滑肌细胞（SMC）增殖的作用，我们测试了最近鉴定的细胞周期蛋白依赖性激酶抑制剂的flavopiridol对体外和体内SMC生长的影响。 Flavopolidol（75 nmol / L）有效阻断了SMC增殖，这与细胞周期蛋白依赖性激酶活性和细胞周期相关基因表达下调有关。 我们在大鼠颈动脉损伤模型中检查了flavopiridol对体内SMC增殖的影响。 球囊损伤后，分别在5天和4天时，黄曲霉毒素（5mg / kg）的新内膜大小分别降低了35％和39％。 黄素类药物可能是治疗富含SMC的血管病变的潜在治疗手段。 4-H-1-苯并吡喃-4-酮衍生物在低剂量水平下抑制平滑肌细胞增殖。

    PHARMACEUTICAL USES
    93.
    发明申请
    PHARMACEUTICAL USES 审中-公开
    药物用途

    公开(公告)号：WO00010545A2

    公开(公告)日：2000-03-02

    申请号：PCT/EP1999/006215

    申请日：1999-08-24

    IPC: A61K45/00 ,  A61K31/00 ,  A61K31/4468 ,  A61K31/453 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/517 ,  A61P3/02 ,  A61P21/00 ,  A61P29/00 ,  A61P43/00

    CPC classification number: A61K31/517 ,  A61K31/00 ,  A61K31/4468 ,  A61K31/452 ,  A61K31/453 ,  A61K31/4709 ,  A61K31/4725

    Abstract: The invention relates to the pharmaceutical use of specific substance P antagonists, in particular 1-acylpiperidine substance P antagonists, especially N-benzoyl-2-benzyl-4-(azanaphthoyl-amino)-piperidines, e.g. of formula (I), wherein X and Y are each independently of the other N and/or CH and the ring A is unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of lower alkyl, lower alkoxy, halogen, nitro and trifluoromethyl; and pharmaceutically acceptable salts thereof for treatment of chronic fatigue syndrome (CFS) in the absence of serotonin agonist/selective serotonin reuptake inhibitory therapy, or for the treatment of fibromyalgia or associated functional symptoms.

    Abstract translation: 本发明涉及特定物质P拮抗剂，特别是1-酰基哌啶物质P拮抗剂，特别是N-苯甲酰基-2-苄基-4-（氮杂萘甲酰基 - 氨基） - 哌啶的药物用途，例如， 的式（I）化合物，其中X和Y各自独立地是其它的N和/或CH，并且环A是未取代的或被选自下列的取代基单取代或多取代：低级烷基，低级烷氧基，卤素， 硝基和三氟甲基; 及其药学上可接受的盐在不存在5-羟色胺激动剂/选择性5-羟色胺再摄取抑制疗法的情况下用于治疗慢性疲劳综合征（CFS），或用于治疗纤维肌痛或相关功能症状。

    METHOD FOR TREATING TUMORS HAVING HIGH LDL REQUIREMENTS EMPLOYING MTP INHIBITORS
    96.
    发明申请
    METHOD FOR TREATING TUMORS HAVING HIGH LDL REQUIREMENTS EMPLOYING MTP INHIBITORS 审中-公开
    用于治疗具有使用MTP抑制剂的高LDL要求的肿瘤的方法

    公开(公告)号：WO1998003174A1

    公开(公告)日：1998-01-29

    申请号：PCT/US1997012158

    申请日：1997-07-14

    Applicant: BRISTOL-MYERS SQUIBB COMPANY

    Inventor： BRISTOL-MYERS SQUIBB COMPANY ,  FIRESTONE, Raymond, A.

    IPC: A61K31/445

    CPC classification number: A61K45/06 ,  A61K31/00 ,  A61K31/4468 ,  A61K31/453 ,  A61K31/4535 ,  A61K31/454

    Abstract: A method is provided for treating hematologic tumors and solid tumors, including certain types of leukemias and metastatic tumors, having high LDL requirements employing a delipidating agent such as an MTP inhibitor to substantially reduce LDL blood levels. In addition, a method is provided for treating tumors of the above types having high LDL requirements, especially hematologic tumors such as certain leukemias, employing a delipidating compound to substantially remove native LDL, and then administering a cytotoxic agent carried in reconstituted LDL.

    Abstract translation: 提供了一种用于治疗血液肿瘤和实体瘤的方法，包括某些类型的白血病和转移性肿瘤，具有高LDL需求，使用脱脂剂如MTP抑制剂以显着降低LDL血液水平。 此外，提供了一种用于治疗具有高LDL要求的上述类型的肿瘤的方法，特别是血液学肿瘤例如某些白血病，使用去脂化合物基本上除去天然的LDL，然后给予重组的LDL中携带的细胞毒性剂。

    THERAPEUTIC AGENT FOR CARDIAC FAILURE
    97.
    发明申请
    THERAPEUTIC AGENT FOR CARDIAC FAILURE 审中-公开
    治疗失败的治疗剂

    公开(公告)号：WO1997023209A1

    公开(公告)日：1997-07-03

    申请号：PCT/JP1996003761

    申请日：1996-12-24

    Applicant: NISSAN CHEMICAL INDUSTRIES, LTD. ,  TANIKAWA, Keizo ,  OHRAI, Kazuhiko ,  SATO, Masayuki ,  YAMASHITA, Toru

    Inventor： NISSAN CHEMICAL INDUSTRIES, LTD.

    IPC: A61K31/35

    CPC classification number: C07D311/68 ,  A61K31/353 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/453 ,  A61K31/55

    Abstract: A therapeutic agent for cardiac failure comprising as the active ingredient either a benzopyran derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, wherein R and R each independently represent hydrogen, halogeno, nitro, cyano, amino, C1-6 alkylcarbonylamino, etc.; R and R each independently represents hydrogen, C1-6 alkyl, or phenyl, or R and R are bonded together to form C3-6 cycloalkyl in cooperation with the carbon atom bonded thereto; R represents hydroxy, C1-6 alkoxy, or C1-6 alkylcarbonyloxy, or R is bonded to R to form a bond; R represents hydrogen, or R is bonded to R to form a bond; and R and R each independently represent hydrogen or C1-6 alkyl, or R and R are bonded together to form pyrrolidinyl, imidazolidinyl, pyrazolidinyl, piperidyl, piperazinyl, etc. in cooperation with the nitrogen atom bonded thereto, or R and R are bonded together to form, in cooperation with the nitrogen atom bonded thereto, pyrrole ring optionally substituted with R (where R has the same meaning as R ).

    Abstract translation: 一种用于心力衰竭的治疗剂，其包含作为活性成分的通式（I）表示的苯并吡喃衍生物或其药理学上可接受的盐，其中R 1和R 2各自独立地表示氢，卤素，硝基，氰基， 氨基，C 1-6烷基羰基氨基等; R 3和R 4各自独立地表示氢，C 1-6烷基或苯基，或者R 3和R 4与键合的碳原子一起形成C 3-6环烷基; R 5表示羟基，C 1-6烷氧基或C 1-6烷基羰基氧基，或R 5与R 6结合形成键; R 6表示氢，或R 6与R 5键合形成键; R 7和R 8各自独立地表示氢或C 1-6烷基，或者R 7和R 8结合在一起形成吡咯烷基，咪唑烷基，吡唑烷基，哌啶基，哌嗪基等，与 与其键合的氮原子或R 7和R 8键合在一起，以与其键合的氮原子一起形成任选被R 9取代的吡咯环（其中R 9具有相同的含义 作为R 1）。

    P27 TYROSINE PHOSPHORYLATION AS A MARKER OF CDK4 ACTIVITY AND METHODS OF USE THEREOF
    100.
    发明申请
    P27 TYROSINE PHOSPHORYLATION AS A MARKER OF CDK4 ACTIVITY AND METHODS OF USE THEREOF 审中-公开
    P27酪氨酸磷酸化作为CDK4活性的标志物及其使用方法

    公开(公告)号：WO2017147326A1

    公开(公告)日：2017-08-31

    申请号：PCT/US2017/019184

    申请日：2017-02-23

    Applicant: THE RESEARCH FOUNDATION FOR THE STATE UNIVERSITY OF NEW YORK

    Inventor： BLAIN, Stacy, W.

    IPC: A61K31/415 ,  A61K31/497 ,  A61K38/00 ,  G01N33/574 ,  G01N33/00 ,  A61K38/04

    CPC classification number: A61K31/52 ,  A61K31/09 ,  A61K31/404 ,  A61K31/4439 ,  A61K31/453 ,  A61K31/454 ,  A61K31/496 ,  A61K31/506 ,  A61K31/519 ,  A61K38/45 ,  G01N33/6893 ,  A61K2300/00

    Abstract: Compositions and methods for the treatment of malignancy are disclosed. Specifically, the disclosure provides a method for treating cancer comprises assessing tyrosine 88 (Y88) phosphorylation (pY88) levels in p27 in a biological sample comprising cancer cells from a subject, and stratifying pY88 phosphorylation levels as 0, 1, 2 or 3 as compared to pY88 phosphorylation levels observed in control tissues; where a level of 0 indicates no detectable sensitivity to cyclin-dependent kinase 4 (cd4k) inhibition; a level of 1, low or no detectable sensitivity; and a level of 2 or 3, indicates detectable sensitivity to cdk4 inhibition. Further provided is a kit for practicing the method.

    Abstract translation: 公开了用于治疗恶性肿瘤的组合物和方法。 具体而言，本公开提供了用于治疗癌症的方法，包括评估包含来自受试者的癌细胞的生物样品中p27中的酪氨酸88（Y88）磷酸化（pY88）水平，并将pY88磷酸化水平分层为0,1,2或3 到在对照组织中观察到的pY88磷酸化水平; 其中0的水平表示对细胞周期蛋白依赖性激酶4（cd4k）抑制没有可检测的敏感性; 1的水平，低或无可检测的灵敏度; 和2或3的水平，表明对cdk4抑制的可检测的敏感性。 还提供了一个实践该方法的工具包。

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