AMELIORATION OF VITRECTOMY-INDUCED CATARACTS
    65.
    发明申请
    AMELIORATION OF VITRECTOMY-INDUCED CATARACTS 审中-公开
    诱导诱导的CATARACTS的调节

    公开(公告)号:WO2006127592A2

    公开(公告)日:2006-11-30

    申请号:PCT/US2006/019721

    申请日:2006-05-22

    摘要: Methods to prevent, inhibit, or slow the development of vitrectomy-induced cataracts are disclosed. The methods comprise administering to the eye of a subject a composition comprising an ophthalmologically acceptable carrier or diluent and at least one hydroxylamine compound in a therapeutically sufficient amount to prevent, inhibit, or slow the development of a vitrectomy- induced cataract in the subject to which the composition is administered.

    摘要翻译: 公开了预防,抑制或减缓玻璃体切割术诱导的白内障发展的方法。 所述方法包括向受试者施用包含眼科学上可接受的载体或稀释剂和至少一种治疗上足够量的羟胺化合物的组合物以防止,抑制或减缓受试者中玻璃体切割术诱发的白内障发展, 给予组合物。

    5-HT2B RECEPTOR ANTAGONISTS
    66.
    发明申请
    5-HT2B RECEPTOR ANTAGONISTS 审中-公开
    5-HT2B受体拮抗剂

    公开(公告)号:WO2005097113A3

    公开(公告)日:2006-10-12

    申请号:PCT/GB2005001378

    申请日:2005-04-08

    摘要: The use of a compound of formula: (Ia); or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment of increased visceral sensitivity or visceral pain, wherein: one of R 1 and R 4 is selected from the group consisting of H, and optionally substituted C1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyl-C 1-4 alkyl, and phenyl-C 1-4 alkyl; and the other of R 1 and R 4 is an optionally substituted C 9-14 aryl group; R 2 and R 3 are either: (i) independently selected from H, R, R', SO 2 R, C(=O)R, (CH 2 ) n NR 5 R 6 , where n is from 1 to 4 and R 5 and R 6 are independently selected from H and R, where R is optionally substituted C 1-4 alkyl, and R' is optionally substituted phenyl-C 1-4 alkyl, or (ii) together with the nitrogen atom to which they are attached, form an optionally substituted C 5-7 heterocyclic group. The use of 2-aminopyrimidines, 2-aninoimidazoles,. 2-aminothiazoles and 2-aminotriazoles is also claimed.

    摘要翻译: 使用式(Ia)化合物: 或其药学上可接受的盐在制备用于治疗增加的内脏敏感性或内脏疼痛的药物中的用途,其中:R 1和R 4之一选自 由H和任选取代的C 1-6 - 烷基,C 3-7环烷基,C 3-7环烷基-C 1-4烷基和苯基-C 1-4烷基; R 1和R 4中的另一个是任选取代的C 9-14芳基; R 2和R 3是:(i)独立地选自H,R,R',SO 2 R,C(= O )R,(CH 2)2 NR 6,其中n为1至4,R H和R 6独立地选自H和R,其中R是任选取代的C 1-4烷基,R'任选被取代 苯基-C 1-4烷基,或(ii)与它们所连接的氮原子一起形成任选取代的C 5〜5-7杂环基。 使用2-氨基嘧啶,2-苯并咪唑, 还要求2-氨基噻唑和2-氨基三唑。

    TREATMENT OR PREVENTION OF PRURITUS
    67.
    发明申请
    TREATMENT OR PREVENTION OF PRURITUS 审中-公开
    治疗或预防PRURITUS

    公开(公告)号:WO2006102899A2

    公开(公告)日:2006-10-05

    申请号:PCT/DK2006/000180

    申请日:2006-03-30

    CPC分类号: A61K31/421 A61K31/426

    摘要: The invention provides methods and medicaments for the treatment of pruritus in general or pruritus caused by or associated with dermatological diseases including the treatment of the underlying disease by topically administering to skin or by systemically administering to a subject Oxaprozin or a closely related compound or a salt thereof.

    摘要翻译: 本发明提供用于治疗一般的瘙痒症或由皮肤病引起的或与皮肤病相关的瘙痒的方法和药物,所述方法和药物包括通过局部施用于皮肤或通过全身施用受试者奥沙普秦或密切相关的化合物或盐 它们。

    角結膜障害治療剤
    68.
    发明申请
    角結膜障害治療剤 审中-公开
    KERATOCONJUNCTIVA病症治疗药物

    公开(公告)号:WO2006030753A1

    公开(公告)日:2006-03-23

    申请号:PCT/JP2005/016788

    申请日:2005-09-13

    摘要:  本発明は、E-4-[4-(5-メチル-2-フェニル-4-オキサゾリルメトキシ)ベンジルオキシイミノ]-4-フェニル酪酸、Z-2-[4-(5-メチル-2-フェニル-4-オキサゾリルメトキシ)ベンジルオキシイミノ]-2-(4-フェノキシフェニル)酢酸、2-[2-プロピル-3-[3-[2-エチル-4-(4-フルオロフェニル)-5-ヒドロキシフェノキシ]プロポキシ]フェノキシ]安息香酸、2(S)-メトキシ-3-[4-[3-(4-フェノキシフェノキシ)プロポキシ]フェニル]プロピオン酸またはそれらの塩の新たな医薬用途を探索することを課題とする。上記カルボン酸化合物またはそれらの塩はいずれも、角膜障害モデルにおいて優れた改善効果を発揮し、ドライアイ、角膜潰瘍、角膜炎、結膜炎、点状表層角膜症、角膜上皮欠損、結膜上皮欠損、乾性角結膜炎、上輪部角結膜炎、糸状角膜炎などの角結膜障害の治療剤として有用である。

    摘要翻译: E-4- [4-(5-甲基-2-苯基-4-恶唑基甲氧基)苄氧基亚氨基] -4-苯基丁酸Z-2- [4-(5-甲基-2-苯基-4- 恶唑基甲氧基)苄氧基亚氨基] -2-(4-苯氧基苯基)乙酸,2- [2-丙基-3- [3- [2-乙基-4-(4-氟苯基)-5-羟基苯氧基]丙氧基]苯氧基]苯甲酸, 2(S) - 甲氧基-3- [4- [3-(4-苯氧基苯氧基)丙氧基]苯基]丙酸,或其中任何一种的盐。 这些羧酸化合物及其盐对角膜障碍模型产生优异的缓解作用,可作为角膜结膜病,如干眼症,角膜溃疡,角膜炎,结膜炎,浅表性点状角膜病,上皮下角膜缺损,上皮下结膜缺陷 ,角结膜炎,角膜结膜炎,角膜结膜炎和丝状角膜炎。

    USE OF C-KIT INHIBITORS FOR TREATING INFLAMMATORY MUSCLE DISORDERS INCLUDING MYOSITIS AND MUSCULAR DYSTROPHY
    69.
    发明申请
    USE OF C-KIT INHIBITORS FOR TREATING INFLAMMATORY MUSCLE DISORDERS INCLUDING MYOSITIS AND MUSCULAR DYSTROPHY 审中-公开
    用于治疗炎症性肌肉疾病(包括神经肌肉和肌瘤)的C-CIT抑制剂的使用

    公开(公告)号:WO2005102325A1

    公开(公告)日:2005-11-03

    申请号:PCT/IB2005/001367

    申请日:2005-04-19

    IPC分类号: A61K31/426

    摘要: The present invention relates to a method for treating inflammatory muscle disorders including myositis and muscular dystrophy comprising administering a compound capable of depleting mast cells or a compound inhibiting mast cell degranulation, to a human in need of such treatment. Such compounds can be chosen from c-kit inhibitors and more particularly non-toxic, selective and potent c-kit inhibitors. Preferably, said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.

    摘要翻译: 本发明涉及一种治疗包括肌炎和肌营养不良的炎性肌肉疾病的方法,包括向需要这种治疗的人施用能够消耗肥大细胞的化合物或抑制肥大细胞脱粒的化合物。 这些化合物可以选自c-kit抑制剂,更特别是无毒,选择性和有效的c-kit抑制剂。 优选地,所述抑制剂不能促进IL-3存在下培养的IL-3依赖性细胞的死亡。

    BIOAVAILABLE SOLID DOSAGE FORMS OF METAXALONE
    70.
    发明申请
    BIOAVAILABLE SOLID DOSAGE FORMS OF METAXALONE 审中-公开
    可生物量的固体剂型

    公开(公告)号:WO2005087204A1

    公开(公告)日:2005-09-22

    申请号:PCT/US2005/007480

    申请日:2005-03-08

    申请人: SPIREAS, Spiridon

    发明人: SPIREAS, Spiridon

    IPC分类号: A61K9/20

    摘要: Pharmaceutical compositions comprising metaxalone which demonstrate improved dissolution and bioavailability characteristics compared to the commercially available product, and methods of producing them are provided. In a preferred embodiment, a dosage form comprising metaxalone and at least one inactive powder excipient is bioequivalent to its commercially available counterpart (Skelaxin ® 400-mg tablets) after oral administration to fasting or non-fasting human subjects, while at the same time displaying faster drug dissolution rates than the Skelaxin ® tablets as demonstrated from three different dissolution tests. In another preferred embodiment, a dosage form comprising metaxalone, at least one inactive powder excipient and a nonvolatile liquid is significantly more bioavailable than the commercially available Skelaxin ® 400-mg tablets after oral administration to fasting human subjects.

    摘要翻译: 提供了包含与市售产品相比显示出改善的溶解度和生物利用度特性的美他沙酮的药物组合物及其生产方法。 在优选的实施方案中,包含美他沙酮和至少一种无活性粉末赋形剂的剂型在口服给予禁食或禁食的人受试者之后与其市售对应物(Skelaxin 400mg片剂)是生物等效的,而在 同时显示比三种不同溶出度试验证明的药物溶出速度快于Skelaxin片剂。 在另一个优选的实施方案中,包含美他沙酮,至少一种无活性粉末赋形剂和非挥发性液体的剂型在口服给予禁食的人受试者后,比商购的400mg片剂显着更具生物利用度。