Chemical inhibitors of soluble adenylyl cyclase (sAC)

    公开(公告)号:US09649295B2

    公开(公告)日:2017-05-16

    申请号:US10586929

    申请日:2005-01-20

    Abstract: The present invention relates to a method of treating a disorder mediated by soluble adenylyl cyclase in a subject. The method involves administering to a subject an effective amount of a compound disclosed herein that modulates soluble adenylyl cyclase, under conditions effective to treat the disorder mediated by soluble adenylyl cyclase. The present invention also relates to a method of treating a disorder mediated by soluble adenylyl cyclase in a subject, where the disorder is selected from the group consisting of: learning or memory disorders, malaria, fungal infection, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, and peripheral neuropathy. The method involves modulating soluble adenylyl cyclase in the subject. Another aspect of the present invention relates to a method of modulating soluble adenylyl cyclase. The method involves contacting eukaryotic cells with a compound that modulates soluble adenylyl cyclase, under conditions effective to modulate soluble adenylyl cyclase.

    Adenylyl cyclases as novel targets for the treatment of infection by eukaryotic pathogens
    2.
    发明授权
    Adenylyl cyclases as novel targets for the treatment of infection by eukaryotic pathogens 有权
    腺苷酸环化酶作为治疗真核病原体感染的新靶点

    公开(公告)号:US09095578B2

    公开(公告)日:2015-08-04

    申请号:US12523019

    申请日:2008-01-11

    Abstract: The present invention relates to a method of preventing or treating a disease caused by infection by a eukaryotic pathogen, wherein the method comprises administering an effective amount of a modulator of a eukaryotic pathogen's adenylyl cyclase. The invention also provides pharmaceutical compositions useful for preventing or treating a disease, with the compositions containing a therapeutically effective amount of a modulator of a eukaryotic pathogen's adenylyl cyclase. The invention also provides screening methods for identifying selective modulators of a eukaryotic pathogen's adenylyl cyclase that do not substantially modulate an adenylyl cyclase of the subject. The invention also provides methods for culturing eukaryotic pathogens and methods for inducing the pathogenic state in vitro.

    Abstract translation: 本发明涉及一种预防或治疗由真核病原体感染引起的疾病的方法,其中所述方法包括施用有效量的真核病原体腺苷酸环化酶的调节剂。 本发明还提供了可用于预防或治疗疾病的药物组合物,其中组合物含有治疗有效量的真核病原体腺苷酸环化酶的调节剂。 本发明还提供了用于鉴定真核生物病原体腺苷酸环化酶的选择性调节剂的筛选方法,所述选择性调节剂基本上不调节受试者的腺苷酸环化酶。 本发明还提供培养真核病原体的方法和用于诱导体外致病状态的方法。

    ADENYLYL CYCLASES AS NOVEL TARGETS FOR ANTIBACTRIAL INTERVENTIONS
    3.
    发明申请
    ADENYLYL CYCLASES AS NOVEL TARGETS FOR ANTIBACTRIAL INTERVENTIONS 有权
    作为抗菌干预的新目标的ADENYLYL CYCLASES

    公开(公告)号:US20100168203A1

    公开(公告)日:2010-07-01

    申请号:US12523011

    申请日:2008-01-11

    CPC classification number: A61K31/415 G01N2333/988 G01N2500/00

    Abstract: The present invention relates to a method of preventing or treating a disease caused by bacterial infection by administering an effective amount of a modulator of bacterial adenylyl cyclase. The invention also provides pharmaceutical compositions useful for preventing or treating a disease, with the compositions containing a therapeutically effective amount of a modulator of bacterial adenylyl cyclase. The invention also provides screening methods for identifying selective modulators of bacterial adenylyl cyclase that do not substantially modulate adenylyl cyclase of the subject. The invention also provides methods for culturing bacterial pathogens and methods for inducing the pathogenic state in vitro.

    Abstract translation: 本发明涉及通过施用有效量的细菌腺苷酸环化酶调节剂来预防或治疗由细菌感染引起的疾病的方法。 本发明还提供了可用于预防或治疗疾病的药物组合物,其中组合物含有治疗有效量的细菌腺苷酸环化酶调节剂。 本发明还提供了用于鉴定细菌腺苷酸环化酶的选择性调节剂的筛选方法,所述选择性调节剂基本上不调节受试者的腺苷酸环化酶。 本发明还提供培养细菌病原体的方法和在体外诱导致病状态的方法。

    Ligand for the c-kit receptor and methods of use thereof
    4.
    发明申请
    Ligand for the c-kit receptor and methods of use thereof 审中-公开
    c-kit受体的配体及其使用方法

    公开(公告)号:US20050276784A1

    公开(公告)日:2005-12-15

    申请号:US10988476

    申请日:2004-11-12

    Abstract: A pharmaceutical composition which comprises the c-kit ligand (KL) purified by applicants or produced by applicants' recombinant methods in combination with other hematopoietic factors and a pharmaceutically acceptable carrier is provided as well as methods of treating patients which comprise administering to the patient the pharmaceutical composition of this invention. This invention provides combination therapies using c-kit ligand (KL) and a purified c-kit ligand (KL) polypeptide, or a soluble fragment thereof and other hematopoietic factors. It also provides methods and compositions for ex-vivo use of KL alone or in combination therapy. A mutated KL antagonist is also described. Such an antagonist may also be a small molecule. Antisense nucleic acids to KL as therapeutics are also described. Lastly, compositions and methods are described that take advantage of the role of KL in germ cells, mast cells and melanocytes.

    Abstract translation: 提供了包含由申请人纯化或由申请人的重组方法与其他造血因子组合产生的c- 试剂盒配体(KL)和药学上可接受的载体的药物组合物,以及治疗方法 包括向患者施用本发明的药物组合物的患者。 本发明提供了使用c-kit配体(KL)和纯化的c- 试剂盒配体(KL)多肽或其可溶性片段和其他造血因子的组合疗法。 它还提供单独使用KL或联合治疗的离体使用KL方法和组合物。 还描述了突变的KL拮抗剂。 这样的拮抗剂也可以是小分子。 还描述了作为治疗剂的KL的反义核酸。 最后,描述了利用KL在生殖细胞,肥大细胞和黑素细胞中的作用的组合物和方法。

    Isolation, purification and cloning of retinol dehydratase
    6.
    发明授权
    Isolation, purification and cloning of retinol dehydratase 失效
    视黄醇脱水酶的分离,纯化和克隆

    公开(公告)号:US5928931A

    公开(公告)日:1999-07-27

    申请号:US852481

    申请日:1997-05-07

    CPC classification number: C12N9/88 A61K38/00

    Abstract: The present invention relates to retinol dehydratase, the enzyme which synthesizes the retro-retinoid anhydroretinol in the Spodoptera frugiperda insect cell line Sf-21, as well as the DNA molecule encoding that enzyme. The DNA molecule can be incorporated in a DNA expression system and a host for recombinant production of anhydroretinol dehydratase. The isolated retinol dehydratase protein or polypeptide of the present invention can be combined with a pharmaceutically-acceptable carrier or used alone for administration to mammals, particularly humans, for preventing cell growth and/or uncontrolled cell growth in cells which are growth dependent on retinol and/or 14 hydroxy-4, 14-retro-retinol.

    Abstract translation: 本发明涉及视黄醇脱水酶,该酶是在草地夜蛾(Fododoptera frugiperda)昆虫细胞系Sf-21中合成后视黄醇脱水解蛋白的酶,以及编码该酶的DNA分子。 DNA分子可以并入DNA表达系统和用于重组生产脱氢赖氨醇脱水酶的宿主。 本发明的分离的视黄醇脱水酶蛋白或多肽可以与药学上可接受的载体组合,或者单独使用用于哺乳动物,特别是人,用于预防细胞生长和/或不依赖视黄醇生长的细胞中的不受控制的细胞生长,以及 /或14羟基-4,14-复古视黄醇。

    METHOD FOR DIAGNOSING MELANOCYTIC PROLIFERATIONS
    9.
    发明申请
    METHOD FOR DIAGNOSING MELANOCYTIC PROLIFERATIONS 有权
    用于诊断肌肉增生的方法

    公开(公告)号:US20130065246A1

    公开(公告)日:2013-03-14

    申请号:US13642475

    申请日:2011-04-06

    Abstract: The invention provides a method for diagnosing a melanocytic proliferation in a subject comprising staining a sample of lesional melanocytes with an antibody against soluble adenylyl cyclase (sAC) and interpreting the sAC staining pattern, which is associated with a diagnosis of a melanocytic proliferation. The sAC staining pattern, which is complex, is discriminatory and distinctive according to the nature of the melanocytic proliferation. The sAC staining pattern comprises one or more of dot-like Golgi staining, broad granular Golgi staining, diffuse cytoplasmic staining, nucleolar staining, incomplete granular nuclear staining, and pan-nuclear staining. The method of the invention is particularly useful in confirming or disaffirming a diagnosis reached through conventional histologic examination of a sample. Additionally, the invention provides a kit for use in interpreting melanocytic proliferations.

    Abstract translation: 本发明提供了一种用于诊断受试者中黑素细胞增殖的方法,包括用针对可溶性腺苷酸环化酶(sAC)的抗体染色病变黑素细胞样品,并解释与诊断黑素细胞增殖相关的sAC染色模式。 根据黑素细胞增殖的性质,复杂的sAC染色模式具有歧视性和独特性。 sAC染色模式包括点状高尔基体染色,宽粒状高尔基体染色,弥漫性细胞质染色,核仁染色,不完全粒状核染色和泛核染色中的一种或多种。 本发明的方法特别可用于确认或不肯定通过常规的样品组织学检查达成的诊断。 另外,本发明提供了用于解释黑素细胞增殖的试剂盒。

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