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1. 发明专利

JP2012097119A RNAi INHIBITION OF CTGF FOR TREATMENT OF OCULAR DISORDER 审中-公开
标题翻译：用于治疗眼部疾病的CTGF的RNAi抑制
公开(公告)号：JP2012097119A
公开(公告)日：2012-05-24
申请号：JP2012029499
申请日：2012-02-14
申请人： Alcon Inc , アルコン,インコーポレイテッド
发明人： SHEPARD ALLAN R , PANG IOK-HOU
IPC分类号： A61K31/7105 , A61K48/00 , A61P27/02 , A61P27/06 , C12N15/113
CPC分类号： C12N15/1136 , A61K31/713 , C12N15/111 , C12N2310/14 , C12N2320/32
摘要： PROBLEM TO BE SOLVED: To provide RNA interference for inhibition of connective tissue growth factor mRNA expression in ocular disorders involving CTGF expression.SOLUTION: Ocular disorders involving aberrant CTGF expression include glaucoma, macular degeneration, diabetic retinopathy, choroidal neovascularization, proliferative vitreoretinopathy and wound healing. Such disorders are treated by administering interfering RNAs. There is provided a method of attenuating expression of connective tissue growth factor mRNA in an eye of a subject. The method comprises administering to the eye of the subject a composition comprising an effective amount of interfering RNA such as adouble-stranded (ds) siRNA or single-stranded (ss) siRNA having a lentgh of 19 to 49 nucleotides and a pharmaceutically acceptable carrier.
摘要翻译：要解决的问题：提供RNA干扰，用于抑制涉及CTGF表达的眼部疾病中的结缔组织生长因子mRNA表达。涉及异常CTGF表达的眼部疾病包括青光眼，黄斑变性，糖尿病性视网膜病变，脉络膜新生血管形成，增生性玻璃体视网膜病变和伤口愈合。通过施用干扰RNA来治疗这些病症。提供了减弱受试者眼睛中结缔组织生长因子mRNA表达的方法。该方法包括向受试者的眼睛施用包含有效量的干扰RNA的组合物，所述干扰RNA例如具有19至49个核苷酸的寡核苷酸的双链（ds）siRNA或单链（ss）siRNA和药学上可接受的载体。版权所有（C）2012，JPO＆INPIT

2. 发明申请

WO2006084217A2 RNAI-MEDIATED INHIBITION OF OCULAR HYPERTENSION TARGETS 审中-公开
标题翻译： RNAI介导的OCULAR HYPERTENSION目标的抑制作用
公开(公告)号：WO2006084217A2
公开(公告)日：2006-08-10
申请号：PCT/US2006004018
申请日：2006-02-01
申请人： ALCON INC , SHEPARD ALLAN R , CHATTERTON JON E , CLARK ABBOT F
发明人： SHEPARD ALLAN R , CHATTERTON JON E , CLARK ABBOT F
IPC分类号： A61K31/713 , C12N15/113
CPC分类号： C12N15/1137 , C12N15/1138 , C12N2310/111 , C12N2310/14 , C12N2310/53 , C12Y301/01007 , C12Y306/03009 , C12Y402/01001
摘要： RNA interference is provided for inhibition of ocular hypertension target mRNA expression for lowering elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Ocular hypertension targets include carbonic anhydrase II, IV, and XII; 1- and 2 adrenergic receptors; acetylcholinesterase; Na+/K+-ATPase; and Na-K-2Cl cotransporter. Ocular hypertension is treated by administering interfering RNAs of the present invention.
摘要翻译：提供RNA干扰用于抑制眼高血压靶mRNA表达，以降低开角型青光眼或高眼压患者眼内压升高。眼睛高血压指标包括碳酸酐酶II，IV和XII; 1-和2肾上腺素能受体; 乙酰胆碱酯酶; 的Na + / K + -ATP酶; 和Na-K-2Cl共转运蛋白。通过施用本发明的干扰RNA来治疗眼高血压。

3. 发明申请

WO2006083945A3 RNAI-MEDIATED INHIBITION OF OCULAR TARGETS 审中-公开
标题翻译： RNAi介导的眼球抑制作用
公开(公告)号：WO2006083945A3
公开(公告)日：2007-08-23
申请号：PCT/US2006003515
申请日：2006-02-01
申请人： ALCON INC , SHEPARD ALLAN R , CHATTERTON JON E , CLARK ABBOT F , WAX MARTIN B
发明人： SHEPARD ALLAN R , CHATTERTON JON E , CLARK ABBOT F , WAX MARTIN B
IPC分类号： A61K31/713 , C12N15/113
CPC分类号： C12N15/1137 , C12N15/1138 , C12N2310/111 , C12N2310/14 , C12N2310/53 , C12Y301/01007 , C12Y306/03009 , C12Y402/01001
摘要： RNA interference is provided for inhibition of ocular hypertension target mRNA expression for lowering elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Ocular hypertension targets include carbonic anhydrase II, IV, and XII; ß1- and ß2 adrenergic receptors; acetylcholinesterase; Na + /K + -ATPase; and Na-K-2Cl cotransporter. Ocular hypertension is treated by administering interfering RNAs of the present invention.
摘要翻译：提供RNA干扰抑制高眼压症目标mRNA表达以降低患有开角型青光眼或高眼压症患者的眼内压升高。眼高血压目标包括碳酸酐酶II，IV和XII; β1-和β2肾上腺素能受体; 乙酰胆碱酯酶; 娜^{+ / K ^{+ -ATP酶; 和Na-K-2Cl协同转运蛋白。通过施用本发明的干扰RNA来治疗眼高压。}}

4. 发明申请

WO2007070866A3 CONTROL OF INTRAOCULAR PRESSURE USING ALK5 MODULATION AGENTS 审中-公开
标题翻译：使用ALK5调节剂控制内压
公开(公告)号：WO2007070866A3
公开(公告)日：2008-01-03
申请号：PCT/US2006062151
申请日：2006-12-15
申请人： ALCON INC , FLEENOR DEBRA L , PANG IOK-HOU , SHEPARD ALLAN R , HELLBERG MARK R , CLARK ABBOT F , KLIMKO PETER G
发明人： FLEENOR DEBRA L , PANG IOK-HOU , SHEPARD ALLAN R , HELLBERG MARK R , CLARK ABBOT F , KLIMKO PETER G
IPC分类号： A61K31/357 , A61K31/381 , A61K31/4192 , A61K31/4196 , A61K31/44 , A61K31/47 , A61K31/519 , A61K31/5375 , A61P27/06 , G01N3/50
CPC分类号： G01N33/5008 , A61K31/357 , A61K31/381 , A61K31/4192 , A61K31/4196 , A61K31/44 , A61K31/4439 , A61K31/444 , A61K31/47 , A61K31/4709 , A61K31/4745 , A61K31/506 , A61K31/519 , A61K31/5375 , A61K31/5377 , A61K45/06 , G01N33/5023 , G01N33/5044 , A61K2300/00
摘要： An ophthalmic pharmaceutical composition useful in the treatment of glaucoma and control of intraocular pressure comprising an effective amount of a selective modulator of ALK5 receptor activity is disclosed. Also disclosed is a method of treating glaucoma and controlling intraocular pressure comprising applying a therapeutically effective amount of a pharmaceutical composition comprising a selective modulator of ALK5 receptor activity to an affected eye of a patient.
摘要翻译：公开了一种可用于治疗青光眼和控制眼内压的眼用药物组合物，其包含有效量的ALK5受体活性的选择性调节剂。还公开了一种治疗青光眼并控制眼内压的方法，其包括将治疗有效量的包含ALK5受体活性的选择性调节剂的药物组合物施用于患者的受影响的眼睛。

5. 发明申请

WO2006083945A8 RNAI-MEDIATED INHIBITION OF OCULAR TARGETS 审中-公开
标题翻译： RNAI介导的OCARAR目标的抑制作用
公开(公告)号：WO2006083945A8
公开(公告)日：2007-10-11
申请号：PCT/US2006003515
申请日：2006-02-01
申请人： ALCON INC , SHEPARD ALLAN R , CHATTERTON JON E , CLARK ABBOT F , WAX MARTIN B
发明人： SHEPARD ALLAN R , CHATTERTON JON E , CLARK ABBOT F , WAX MARTIN B
IPC分类号： A61K31/713 , C12N15/113
CPC分类号： C12N15/1137 , C12N15/1138 , C12N2310/111 , C12N2310/14 , C12N2310/53 , C12Y301/01007 , C12Y306/03009 , C12Y402/01001
摘要： RNA interference is provided for inhibition of ocular hypertension target mRNA expression for lowering elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Ocular hypertension targets include carbonic anhydrase II, IV, and XII; ß1- and ß2 adrenergic receptors; acetylcholinesterase; Na + /K + -ATPase; and Na-K-2Cl cotransporter. Ocular hypertension is treated by administering interfering RNAs of the present invention.
摘要翻译：提供RNA干扰用于抑制眼高血压靶mRNA表达，以降低开角型青光眼或高眼压患者眼内压升高。眼睛高血压指标包括碳酸酐酶II，IV和XII; β1-和β2肾上腺素能受体; 乙酰胆碱酯酶; 娜^{+ / K ^{+ -ATP酶; 和Na-K-2Cl共转运蛋白。通过施用本发明的干扰RNA来治疗眼高血压。}}

6. 发明专利

AU2004308938B2 CDK2 antagonists as short form c-Maf transcription factor antagonists for treatment of glaucoma 未知
公开(公告)号：AU2004308938B2
公开(公告)日：2011-06-23
申请号：AU2004308938
申请日：2004-12-21
申请人： ALCON INC
发明人： CLARK ABBOT F , NASREEN JACOBSON , SHEPARD ALLAN R
IPC分类号： A61K31/00 , A61K31/52
摘要： The short form version of c-Maf transcription factor is up-regulated in steroid-treated and transforming growth factor beta2-treated trabecular meshwork cells, and is present at elevated levels in glaucomatous versus normal trabecular meshwork cells and in glaucomatous versus normal optic nerve head tissue. Expression of short form c-Maf transcription factor under these conditions indicates a causal or effector role for the factor in primary open-angle and steroid-induced glaucoma pathogenesis. Antagonism of short form c-Maf transcription factor expression and/or activity in the trabecular meshwork or other ocular tissue is provided for inhibiting or alleviating glaucoma pathogenesis. Antagonists include cyclin-dependent kinase 2 inhibitors.

7. 发明专利

CA2595790A1 RNAI-MEDIATED INHIBITION OF OCULAR HYPERTENSION TARGETS 未知
公开(公告)号：CA2595790A1
公开(公告)日：2006-08-10
申请号：CA2595790
申请日：2006-02-01
申请人： ALCON INC
发明人： SHEPARD ALLAN R , CHATTERTON JON E , CLARK ABBOT F
IPC分类号： A61K31/713 , C12N15/113
摘要： RNA interference is provided for inhibition of ocular hypertension target mRNA expression for lowering elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Ocular hypertension targets include carbonic anhydrase II, IV, and XII; &bgr;1- and &bgr;2 adrenergic receptors; acetylcholinesterase; Na+/K+-ATPase; and Na—K-2Cl cotransporter. Ocular hypertension is treated by administering interfering RNAs of the present invention.

8. 发明专利

BRPI0619966A2 未知
公开(公告)号：BRPI0619966A2
公开(公告)日：2011-10-25
申请号：BRPI0619966
申请日：2006-12-15
申请人： ALCON INC
发明人： FLEENOR DEBRA L , PANG IOK-HOU , SHEPARD ALLAN R , HELLBERG MARK R , CLARK ABBOT F , KLIMKO PETER G
IPC分类号： A61K31/357 , A61K31/381 , A61K31/4192 , A61K31/4196 , A61K31/44 , A61K31/47 , A61K31/519 , A61K31/5375 , A61P27/06 , G01N3/50
摘要： An ophthalmic pharmaceutical composition useful in the treatment of glaucoma and control of intraocular pressure comprising an effective amount of a selective modulator of ALK5 receptor activity is disclosed. Also disclosed is a method of treating glaucoma and controlling intraocular pressure comprising applying a therapeutically effective amount of a pharmaceutical composition comprising a selective modulator of ALK5 receptor activity to an affected eye of a patient.

9. 发明专利

ZA200706084B RNAI-mediated inhibition of ocular hypertension targets 未知
公开(公告)号：ZA200706084B
公开(公告)日：2009-04-29
申请号：ZA200706084
申请日：2006-02-01
申请人： ALCON INC
发明人： SHEPARD ALLAN R , CHATTERTON JON E , CLARK ABBOT F
IPC分类号： A61K20090101 , C12N20090101

10. 发明专利

BRPI0510245A 未知
公开(公告)号：BRPI0510245A
公开(公告)日：2007-10-23
申请号：BRPI0510245
申请日：2005-04-25
申请人： ALCON INC
发明人： HELLBERG MARK R , FLEENOR DEBRA L , SHEPARD ALLAN R , PANG IOK-HOU
IPC分类号： A61K31/00 , A61K9/00 , A61K31/225 , A61K31/366 , A61K31/401 , A61P27/06
摘要： The use of HMG-CoA reductase inhibitors (e.g., statins) to treat glaucoma, control intraocular pressure, preserve the trabecular meshwork, protect against ocular neurodegeneration and/or protect against glaucomatous retinopathy is described. The preferred HMG-CoA reductase inhibitors, which are statins having an RI value of 0.2 to 0.7 (e.g., pravastatin), are administered via topical application to the affected eye(s) of the patient.

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