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Compositions and Methods for treating ocular inflammation with less risk of increased intraocular pressure. Use

机译:用于治疗眼内炎症的组合物和方法,其眼内压升高的风险较小。采用

摘要

Claim 1: Use of a Dissociated glucocorticoid receptor agonist (u00f4digrau00f6) or an ester or a pharmaceutically acceptable Salt thereof for preparing medicine to Treat or manage a condition or Disorder, inflammatory Eye Disease.Where the digra has the formula (1) where a and q are selected irrespective of the group consisting of aryl and heteroaryl groups substituted and unsubstituted cycloalkyl groups, and heterocicloalquilo substituted and unsubstituted and substituted groups and heterocicloalquenilo, cicloalquenilo Cicloalquinilo groups and not replaced, heterocicloalquinilo substituted and unsubstituted,And Heterocyclic groups substituted and unsubstituted; R1 and R2 are independently selected from the group consisting of hydrogen, linear or branched alkyl groups C1 - 15 not replaced, linear or branched alkyl groups substituted cycloalkyl groups C1 - C3 - 15, 15 were not replaced, and groups Cycloalkyl substituted C3 - 15; R3 is selected from the group consisting of hydrogen,Linear or branched alkyl groups C1 - 15 not replaced, linear or branched alkyl groups substituted cycloalkyl groups 15 - C1, C3 and heterocicloalquilo unsubstituted cycloalkyl groups 15, 15 and heterocicloalquilo C3 -, substituted aryl and heteroaryl groups, groups, groups heterociclilicos B includes a divalent Hydrocarbon amino carbonyl,,,Heterohidrocarburo or Group; and it is a Hydroxy or amino Group; and D is absent or includes a carbonyl Group, - NH -, or ID ', where r' is a linear or branched alkyl group, substituted or non substituted C1 - 15; and where R1 and R2 together can form a cycloalkyl Group C3 - 15 Replacement Gone or not replaced; where digra, a prodrug thereof,Or a pharmaceutically acceptable Salt thereof of the Ester is present in an effective amount to Treat or control the inflammatory Eye Disease, condition or Disorder; wherein the composition provides a Lower risk of increased IOP that a composition that Presid A glucocorticoidAnd where the risk is lower for a Lower Production miocilina a meshwork of a Subject that receives such a composition for the Treatment or control.Claim 2: the use of claim 1, wherein Said disease or condition, disorder selected from the group consisting of panuveu00edtis anterior uveitis, posterior uveitis, keratitis, conjunctivitis, Vernal keratoconjunctivitis, atopic keratoconjunctivitis, Corneal ulcer, edema of cor Neal, sterile corneal infiltrates, scleritis, episcleritis, blepharitis,And post-operative ocular inflammation (post Surgical) for procedures such as Fotorefractiva Keratectomy, Cataract removal surgery, implantation of intraocular lenses, laser assisted in situ keratomileusis (u00f4lasiku00f6), Conductive Keratoplasty, queratotomu00ed Radial, Dry Eye, Macular Degeneration, Diabetic Retinopathy, macular edema,Wet age-related Macular Degeneration, Dry Age related Macular Degeneration, glaucoma. Claim 2: the use of Claim 5, wherein the digra has the formula (6).Claim 7: Use of claim 6, wherein Said composition further comprises an anti-inflammatory Agent selected from the group consisting of NSAIDs, agonists of PPAR, combinations thereof, and mixtures thereof.
机译:1。解离的糖皮质激素受体激动剂( u00f4digra u00f6)或其酯或药学上可接受的盐在制备用于治疗或控制炎症性眼病或病症的药物中的用途,其中digra具有式(1)其中a和q不考虑由芳基和杂芳基取代和未取代的环烷基,杂环烷基取代和未取代和取代的基团和未取代的杂环基喹啉基,杂环基喹啉基和取代基,杂环基喹啉基取代和未取代以及杂环基取代和未取代R 1和R 2独立地选自氢,未被取代的直链或支链烷基C1-15,未被取代的直链或支链烷基取代的环烷基C1至C3-15、15,和被环烷基取代的C3-15基团。 ; R3选自氢,未取代的直链或支链烷基C1-15,经取代的直链或支链烷基,环烷基15-C1,C3和未取代的杂环氯基环烷基15、15和杂环氯基C3-,取代的芳基和杂芳基B包括杂价芳基,杂芳基,杂杂芳基或杂芳基;并且是羟基或氨基; D不存在或包括羰基,-NH-或ID′,其中r′为直链或支链烷基,取代或未取代的C1-15;其中R1和R2一起可以形成环烷基C3-15取代或不被取代;如果存在digra,其前药或其药学上可接受的酯盐,其有效量可治疗或控制炎症性眼部疾病,病症或疾病; 2.权利要求2的用途,其中所述组合物提供比葡糖皮质激素类化合物高的IOP的较低风险,并且其中低产率的miocilina的风险较低,接受该组合物的受试者的网眼接受所述组合物的治疗或控制。 1,其中所述疾病或病状,病症选自:足膜前葡萄膜炎,后葡萄膜炎,角膜炎,结膜炎,春季角膜结膜炎,特应性角膜结膜炎,角膜溃疡,皮质神经水肿,无菌角膜浸润,巩膜炎,巩膜炎睑缘炎,以及术后眼部炎症(手术后),例如Fotorefractiva角膜切除术,白内障摘除手术,人工晶状体植入,激光辅助原位角膜磨镶术(Kuatomyus),传导性角膜成形术,que骨切开术,干眼Rad ,黄斑变性,糖尿病性视网膜病变,黄斑水肿,湿性老年性黄斑变性,干龄特德黄斑变性,青光眼。权利要求2:权利要求5的用途,其中二头草具有式(6)。7,权利要求6的用途,其中所述组合物还包含选自NSAID,PPAR激动剂,组合的抗炎剂它们及其混合物。

著录项

  • 公开/公告号AR076342A1

    专利类型

  • 公开/公告日2011-06-01

    原文格式PDF

  • 申请/专利权人 BAUSCH & LOMB INCORPORATED;

    申请/专利号AR2010P101303

  • 发明设计人

    申请日2010-04-20

  • 分类号A61K31/4709;A61P27/02;

  • 国家 AR

  • 入库时间 2022-08-21 18:07:27

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