Compositions and methods for modulating guanylyl cyclase signaling receptor (gc-c) activity and for treating meniere's disease
    2.
    发明申请
    Compositions and methods for modulating guanylyl cyclase signaling receptor (gc-c) activity and for treating meniere's disease 审中-公开
    调节鸟苷酸环化酶信号受体(gc-c)活性和治疗梅尼埃病的组合物和方法

    公开(公告)号:US20040152868A1

    公开(公告)日:2004-08-05

    申请号:US10473841

    申请日:2004-03-29

    IPC分类号: C07K007/64 A61K038/12

    CPC分类号: C12N9/88

    摘要: Disclosed are compositions and methods for modulating guanylyl cyclase signaling receptor (GC-C). Further disclosed are highly useful in vitro and in vivo screens for detecting compounds that modulate the GC-C receptor. The invention has a wide spectrum of useful applications including providing therapeutic compounds that can be employed to prevent and/or treat inner ear disorders and particularly Mnullninullre's disease.

    摘要翻译: 公开了调节鸟苷酸环化酶信号受体(GC-C)的组合物和方法。 进一步公开的是用于检测调节GC-C受体的化合物的体外和体内筛选。 本发明具有广泛的有用应用,包括提供可用于预防和/或治疗内耳障碍,特别是梅内尔病的治疗化合物。

    Pharmaceutical composition for prevention and remedy of osteoporosis
    3.
    发明申请
    Pharmaceutical composition for prevention and remedy of osteoporosis 审中-公开
    用于预防和治疗骨质疏松症的药物组合物

    公开(公告)号:US20040102365A1

    公开(公告)日:2004-05-27

    申请号:US10467802

    申请日:2003-08-12

    发明人: Kazuo Nagai

    IPC分类号: C07K007/64 A61K038/12

    CPC分类号: A61K38/15

    摘要: The present invention relates to a pharmaceutical composition for prevention and remedy of osteoporosis containing destruxin derivative as an active principle and cyclodepsipeptide of this invention, originated mold, is greatly efficacious on the activity inhibition ability for the osteoclast without regard to existence of the parathyroid hormone.

    摘要翻译: 本发明涉及用于预防和治疗含有destruxin衍生物作为活性成分的骨质疏松症的药物组合物和本发明的起始模具的环缩缩肽,对于破骨细胞的活性抑制能力而言,不考虑甲状旁腺激素的存在是非常有效的。

    Echinocandin derivatives, pharmaceutical compositions containing same and use thereof as drugs
    4.
    发明申请
    Echinocandin derivatives, pharmaceutical compositions containing same and use thereof as drugs 审中-公开
    棘白菌素衍生物,含有它们的药物组合物和作为药物的用途

    公开(公告)号:US20040082757A1

    公开(公告)日:2004-04-29

    申请号:US10468142

    申请日:2003-08-25

    IPC分类号: C07K007/64

    CPC分类号: C07K7/56 A61K38/00

    摘要: This invention relates to new polypeptide compound represented by the following formula (I), wherein R1, R2, R3, R4, R5, R6, and R7 are described in the specification, or a salt thereof which have antimicrobial activities (especially, antifungal activities), inhibitory activity on null-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for the prophylactic and/or therapeutic treatment of infectious diseases including Pneumocystis carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal. 1

    摘要翻译: 本发明涉及由下式(I)表示的新的多肽化合物,其中R 1,R 2,R 3,R 4,R 5,R 6和R 6, 7>在说明书中描述,或其盐具有抗微生物活性(特别是抗真菌活性),对β-1,3-葡聚糖合酶的抑制活性,其制备方法,其包含其的药物组合物,和 涉及在人或动物中预防和/或治疗治疗感染性疾病的方法,包括卡氏肺囊虫感染(例如肺孢子虫肺炎)。

    Synthesis of cyclosporin analogs
    8.
    发明申请
    Synthesis of cyclosporin analogs 有权
    环孢菌素类似物的合成

    公开(公告)号:US20030212249A1

    公开(公告)日:2003-11-13

    申请号:US10274437

    申请日:2002-10-17

    申请人: Isotechnika, Inc.

    IPC分类号: C07K007/64

    摘要: The invention is directed to isomeric mixtures of cyclosporine analogues that are structurally similar to cyclosporine A. The mixtures possess enhanced efficacy and reduced toxicity over the individual isomers and over naturally occurring and other presently known cyclosporines and cyclosporine derivatives. Embodiments of the present invention are directed toward cis and trans-isomers of cyclosporin A analogs referred to as ISATX247, and derivatives thereof. ISATX247 isomers and alkylated, arylated, and deuterated derivatives are synthesized by stereoselective pathways where the particular conditions of a reaction determine the degree of stereoselectivity. Stereoselective pathways may utilize a Wittig reaction, or an organometallic reagent comprising inorganic elements such as boron, silicon, titanium, and lithium. The ratio of isomers in a mixture may range from about 10 to 90 percent by weight of the (E)-isomer to about 90 to 10 percent by weight of the (Z)-isomer, based on the total weight of the mixture.

    摘要翻译: 本发明涉及结构类似于环孢霉素A的环孢菌素类似物的异构体混合物。该混合物具有比单个异构体和天然存在的和其它目前已知的环孢菌素和环孢菌素衍生物更强的功效和降低的毒性。 本发明的实施方案涉及称为ISATX247的环孢菌素A类似物的顺式和反式异构体及其衍生物。 ISATX247异构体和烷基化,芳基化和氘代衍生物通过立体选择性途径合成,其中反应的特定条件决定了立体选择性的程度。 立体选择性途径可以利用维蒂希反应或包含无机元素如硼,硅,钛和锂的有机金属试剂。 基于混合物的总重量,混合物中异构体的比例可以为(E) - 异构体的约10至90重量%至(Z) - 异构体的约90至10重量%。