Method of promoting cervical and vaginal secretions
    21.
    发明授权
    Method of promoting cervical and vaginal secretions 有权
    促进子宫颈和阴道分泌物的方法

    公开(公告)号:US07432252B1

    公开(公告)日:2008-10-07

    申请号:US09531851

    申请日:2000-03-20

    IPC分类号: A61K31/70

    CPC分类号: C07H21/00

    摘要: The present invention provides a method of stimulating cervical and vaginal secretions in a mammal by treatment with P2Y2 and/or P2Y4 purinergic receptor agonists. Treatment of vaginal dryness associated with menopause, chemotherapy, and various disease states as well as the treatment of vulvar pain is discussed. Suitable agonists such as UTP, CTP, ATP, dinucleotides and analogs thereof are disclosed.

    摘要翻译: 本发明提供了通过用P2Y2和/或P2Y4N4嘌呤能受体激动剂治疗来刺激哺乳动物的宫颈和阴道分泌物的方法。 讨论了与绝经,化疗和各种疾病状态相关的阴道干燥的治疗以及外阴疼痛的治疗。 公开了合适的激动剂,例如UTP,CTP,ATP,二核苷酸及其类似物。

    Certain dinucleotides and their use as modulators of mucociliary clearance and ciliary beat frequency
    25.
    发明授权
    Certain dinucleotides and their use as modulators of mucociliary clearance and ciliary beat frequency 失效
    某些二核苷酸及其作为粘膜纤毛清除和睫状肌拍频的调节剂

    公开(公告)号:US06348589B1

    公开(公告)日:2002-02-19

    申请号:US09101395

    申请日:1998-07-10

    IPC分类号: C07H2100

    摘要: The present invention relates to certain novel dinucleotides and formulations thereof which are highly selective agonists of the P2Y2 and/or P2Y4 purinergic receptor. They are useful in the treatment of chronic obstructive pulmonary diseases such as chronic bronchitis, PCD, cystic fibrosis, as well as prevention of pneumonia due to immobility. Furthermore, because of their general ability to clear retained mucus secretions and stimulate ciliary beat frequency, the compounds of the present invention are also useful in the treatment of sinusitis, otitis media and nasolacrimal duct obstruction. They are also useful for treatment of dry eye disease and retinal detachment.

    摘要翻译: 本发明涉及作为P2Y2和/或P2Y4嘌呤能受体的高选择性激动剂的某些新型二核苷酸及其制剂。 它们可用于治疗慢性阻塞性肺疾病如慢性支气管炎,PCD,囊性纤维化,以及由于不动而预防肺炎。 此外,由于它们具有清除保留的粘液分泌物并刺激睫状肌搏动频率的一般能力,本发明的化合物也可用于治疗鼻窦炎,中耳炎和鼻泪管阻塞。 它们也可用于治疗干眼病和视网膜脱离。

    Dinucleotides and their use as modulators of mucociliary clearance and
ciliary beat frequency
    26.
    发明授权
    Dinucleotides and their use as modulators of mucociliary clearance and ciliary beat frequency 失效
    二核苷酸及其作为粘膜纤毛清除和睫状肌拍频的调节剂

    公开(公告)号:US5837861A

    公开(公告)日:1998-11-17

    申请号:US798508

    申请日:1997-02-10

    摘要: The present invention encompasses structures of the formula ##STR1## wherein: X is oxygen, methylene, or difluoromethylene; n=0 or 1; m=0 or 1; n+m=0, 1 or 2; and B and B' are each independently a purine residue or a pyrimidine residue linked through the 9- or 1-position, respectively, provided that compounds disclosed in Table I are excluded. In the instance where B and B' are uracil, attached at the N-1 position to the ribosyl moiety, then the total of m+n may equal 3 or 4 when X is oxygen. The compounds of the present invention are highly selective agonists of the P2Y.sub.2 purinergic receptor, thus, they are useful in the treatment of chronic obstructive pulmonary diseases such as chronic bronchitis, PCD, cystic fibrosis, as well as prevention of pneumonia due to immobility. Furthermore, because of their general ability to clear retained mucus secretions and stimulate ciliary beat frequency, the compounds of the present invention are also useful in the treatment of sinusitis and otitis media.

    摘要翻译: 本发明包括下式的结构:其中:X是氧,亚甲基或二氟亚甲基; n = 0或1; m = 0或1; n + m = 0,1或2; 并且B和B'各自独立地是嘌呤残基或连接在9-位或1-位上的嘧啶残基,条件是排除表I中公开的化合物。 在B和B'是尿嘧啶的情况下,在N-1位置连接到核糖基部分,则当X是氧时,m + n的总和可以等于3或4。 本发明的化合物是P2Y2嘌呤能受体的高选择性激动剂,因此它们可用于治疗慢性阻塞性肺疾病如慢性支气管炎,PCD,囊性纤维化,以及由于不动而预防肺炎。 此外,由于它们具有清除保留的粘液分泌物和刺激睫状肌搏动频率的一般能力,本发明的化合物也可用于治疗鼻窦炎和中耳炎。

    METHOD OF REDUCING CONTACT LENS INTOLERANCE WITH NON-DRYING ANTIHISTAMINES
    28.
    发明申请
    METHOD OF REDUCING CONTACT LENS INTOLERANCE WITH NON-DRYING ANTIHISTAMINES 审中-公开
    使用非干性抗生素降低接触镜片不透明度的方法

    公开(公告)号:US20130344139A1

    公开(公告)日:2013-12-26

    申请号:US14013794

    申请日:2013-08-29

    IPC分类号: A61K31/55

    CPC分类号: A61K31/55 Y10S514/912

    摘要: A method and preparation for reducing dry eye symptoms and promoting tear secretion in a subject in need of such treatment is disclosed. The method is useful in treating dry eye diseases. The method is also useful in reducing contact lens intolerance in the eyes. The method comprises administering to the eyes of a subject in need thereof a non-drying antihistamine compound, such as epinastine hydrochloride, in an amount effective to reduce dry eye symptoms and stimulate tear fluid secretion. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the compound include topical administration via a liquid, gel, cream, or as part of a contact lens or a continuous or selective release device; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form, injectable, intra-operative instillation or suppository form.

    摘要翻译: 公开了减少需要这种治疗的受试者的干眼症状和促进泪液分泌的方法和制剂。 该方法可用于治疗干眼病。 该方法也可用于减少眼睛中的隐形眼镜不耐受。 该方法包括以有效减少干眼症状并刺激泪液分泌的量向有需要的受试者的眼睛施用非干燥的抗组胺药化合物,例如盐酸依诺斯汀。 还公开了药物制剂及其制备方法。 施用化合物的方法包括通过液体,凝胶,霜剂或作为隐形眼镜或连续或选择性释放装置的一部分的局部给药; 或通过鼻滴或喷雾进行全身给药,通过喷雾器或其他装置吸入,口服形式,可注射的,术中滴注或栓剂形式。