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31. 发明公开

EP1307191A2 USE OF INDOLE DERIVATIVES FOR THE MANUFACTURE OF A MEDICAMENT FOR REDUCING INTRACULAR PRESSURE 审中-公开
标题翻译：吲哚衍生物用于制备所述药物用于INTRAOCULARDRUCKS的耻辱USE
公开(公告)号：EP1307191A2
公开(公告)日：2003-05-07
申请号：EP01959427.4
申请日：2001-07-27
申请人： Inspire Pharmaceuticals, Inc. , University Complutense de Madrid
发明人： PINTOR, Jesus, J. , PERAL, Maria, A. , PETERSON, Ward, M. , PLOURDE, Robert, Jr. , BROWN, Edward, G. , YERXA, Benjamin, R.
IPC分类号： A61K31/404 , A61P27/06
CPC分类号： A61K45/06 , A61K31/404 , A61K31/4045 , A61K31/55 , A61K2300/00
摘要： The present invention provides a method of reducing intraocular pressure by administering pharmaceutical compositions comprising indole derivatives. The pharmaceutical compositions useful in this invention comprise indole derivatives and melatonin analogs of Formulae (I) (II) (III) (IV). A preferred embodiment is a method of lowering intraocular pressure using 5-(methoxycarbonylamino)-N-acetyltryptamine (5-MCA-NAT), also known as GR 135531, which has a prolonged duration of action and greater efficacy in lowering intraocular pressure compared to melatonin. The present invention further provides a method of treating disorders associated with ocular hypertension, and a method of treating various forms of glaucoma; the method comprises administering an effective dose of a pharmaceutical composition comprising an indole derivative with or without agents commonly used to treat such disorders.

32. 发明公开

EP1087777A2 THERAPEUTIC DINUCLEOTIDE AND DERIVATIVES 有权
标题翻译：治疗性双核苷酸及其衍生物
公开(公告)号：EP1087777A2
公开(公告)日：2001-04-04
申请号：EP99924313.2
申请日：1999-05-19
申请人： Inspire Pharmaceuticals, Inc. , The University of North Carolina at Chapel Hill
发明人： YERXA, Benjamin, R. , PENDERGAST, William , RIDEOUT, Janet, L. , PICHER, Maryse , BOUCHER, Richard, C. , STUTTS, Monroe, Jackson
IPC分类号： A61K31/70 , C07H21/00
CPC分类号： A61K31/7048 , A61K31/70 , C07H19/207 , C07H21/00
摘要： The present invention relates to P1-(cytidine 5'-)-P4-(uridine 5'-)tetraphosphates and its salts, esters and amides, and formulations thereof which are highly stable and selective agonists of the P2Y¿2? and/or P2Y4 purinergic receptor. The compounds of the invention are useful in the treatment of chronic obstructive pulmonary diseases such as chronic bronchitis, primary ciliary dyskinesia, cystic fibrosis, as well as prevention of pneumonia due to immobility, and the induction of sputum and its expectoration. 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. They are also useful in the treatment of dry eye disease and retinal detachment.

33. 发明公开

EP1003474A1 METHOD OF TREATING DRY EYE DISEASE WITH PURINERGIC RECEPTOR AGONISTS 失效
标题翻译：方法为“干眼”杂志附嘌呤受体激动剂治疗
公开(公告)号：EP1003474A1
公开(公告)日：2000-05-31
申请号：EP98907434.9
申请日：1998-02-06
申请人： Inspire Pharmaceuticals, Inc.
发明人： YERXA, Benjamin, R. , JACOBUS, Karla, M. , PENDERGAST, William , RIDEOUT, Janet, L.
IPC分类号： A61K9/00
CPC分类号： C07H19/10 , A61K9/0048 , A61K31/7084 , A61K45/06 , C07H19/20 , C07H21/00 , Y10S514/912 , Y10S514/915
摘要： A method and preparation for the stimulation of tear secretion in a subject in need of such treatment is disclosed. The method comprises administering to the ocular surfaces of the subject a purinergic receptor agonist such as uridine 5'-triphosphate [UTP], dinucleotides, cytidine 5'-triphosphate [CTP], adenosine 5'-triphosphate [ATP], or their therapeutically useful analogs and derivatives, in an amount effective to stimulate tear fluid secretion and enhance drainage of the lacrimal system. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include: topical administration via a liquid, gel, cream, or as part of a contact lens or selective release membrane; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, intra-operative instillation or suppository form.

34. 发明公开

EP0941099A1 METHOD OF TREATING BRONCHITIS WITH URIDINE TRIPHOSPHATES AND RELATED COMPOUNDS 失效
标题翻译：了治疗支气管炎三磷酸尿苷和ANVERWANDTEVERBINDUNGEN
公开(公告)号：EP0941099A1
公开(公告)日：1999-09-15
申请号：EP97912761.0
申请日：1997-10-21
申请人： Inspire Pharmaceuticals, Inc.
发明人： SHAFFER, Christy, L. , BOUCHER, Richard, C. , RIDEOUT, Janet, L. , JACOBUS, Karla, M.
IPC分类号： A61K , C07H19 , A61K9 , A61K31 , A61P11 , C07D473
CPC分类号： A61K31/7076 , A61K31/7072
摘要： A method of promoting clearance of retained mucous secretions in the bronchi, bronchioles and small terminal airways of a subject in need of such treatment is disclosed. The method comprises administering to the bronchi of the subject a uridine phosphate such as uridine 5'Îtriphosphate (UTP), or P1,P4-di(uridine-5Î) tetraphosphate (U2P4), an analog of UTP, or any other analog, in an amount effective to promote mucociliary clearance and/or cough clearance of retained fluid in the bronchi, bronchioles and small terminal airways. Methods of administering the same would include; aerosol inhalation, any liquid suspension (including nasal drops or spray), oral form (liquid or pill), injected, intra-operative instillation or suppository form.

35. 发明公开

EP0897301A1 METHOD OF TREATING OTITIS MEDIA WITH URIDINE TRIPHOSPHATES AND RELATED COMPOUNDS 失效
标题翻译：方法中耳炎由URIDINTRIPHOSPHATEN和相关基金的处理
公开(公告)号：EP0897301A1
公开(公告)日：1999-02-24
申请号：EP97905953.0
申请日：1997-02-14
申请人： Inspire Pharmaceuticals, Inc.
发明人： DRUTZ, David, J. , RIDEOUT, Janet, L. , JACOBUS, Karla, M.
IPC分类号： C07H19 , A61K31 , A61P27 , B65B43
CPC分类号： A61K31/7076 , A61K31/7072
摘要： A method of promoting drainage of congested middle ear fluid in a subject in need of such treatment is disclosed. The method comprises administering to the middle ear of the subject a uridine triphosphate such as uridine 5'-triphosphate (UTP), an analog of UTP, or any other analog, in an amount effective to promote drainage of congested middle ear fluid by hydrating mucous secretions in the middle ear or by stimulating ciliary beat frequency in the middle ear or eustachian tube. The method is useful for treating patients afflicted with otitis media and other middle ear diseases, otitis externa, and inner ear diseases including Ménière's Disease. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include any liquid suspension (including nasal drops or spray), oral, inhaled by nebulization, topical, injected or suppository form.

36. 发明公开

EP2512239A4 BRIDGED BICYCLIC RHO KINASE INHIBITOR COMPOUNDS, COMPOSITION AND USE 审中-公开
标题翻译：桥双环Rho激酶抑制剂化合物，组合物及其使用
公开(公告)号：EP2512239A4
公开(公告)日：2014-11-26
申请号：EP10838164
申请日：2010-12-10
申请人： INSPIRE PHARMACEUTICALS INC
发明人： LAMPE JOHN W , WATSON PAUL S , SLADE DAVID J
IPC分类号： C07D451/04 , A61K31/416 , A61K31/439 , A61K31/4709 , A61K31/55 , A61P11/06 , A61P11/14 , A61P27/02 , A61P27/06 , C07D401/12 , C07D403/12 , C07D413/12 , C07D453/06 , C07D471/08 , C07D487/08
CPC分类号： C07D451/04 , A61K31/46 , A61K31/4725 , C07D401/12 , C07D403/12 , C07D413/12 , C07D453/06 , C07D471/08 , C07D487/08

37. 发明公开

EP2597953A4 METHOD FOR TREATING OPHTHALMIC DISEASES USING KINASE INHIBITOR COMPOUNDS IN PRODRUG FORMS 审中-公开
标题翻译： VERFAHREN ZUR BEHANDLUNG VON AUGENKRANKHEITEN UNTER VERWENDUNG VON KINASEHEMMERVERBINDUNGEN IN PRODRUG-FORMEN
公开(公告)号：EP2597953A4
公开(公告)日：2013-12-25
申请号：EP11813019
申请日：2011-07-25
申请人： INSPIRE PHARMACEUTICALS INC
发明人： LAMPE JOHN W , SHAVER SAMMY R , WATSON PAUL S
IPC分类号： A01N43/34
CPC分类号： C07D401/12 , A61K9/0048 , C07D401/14 , C07D403/12
摘要： This invention is directed to prodrugs of rho kinase (ROCK) inhibitors. These prodrugs are in general the ester or the amide derivatives of the parent compounds. These prodrugs are often weak inhibitors of ROCK, but their parent compounds have good activities. Upon instillation into the eyes, the ester or the amide group of these prodrugs is rapidly hydrolyzed into alcohol, amine, or acid, and the prodrugs are converted into the active base compounds. The prodrugs of ROCK inhibitors provide several advantages such as delivery of higher concentrations of the active species into the target site and reduction of ocular discomfort. The invention is also directed to a method of treating ophthalmic diseases such as glaucoma, allergic conjunctivitis, macular edema, macular degeneration, and blepharitis, by administering an effective amount of a ROCK prodrug compound of Formula I to the eyes of the patient in need of.
摘要翻译：本发明涉及rho激酶（ROCK）抑制剂的前体药物。这些前体药物通常是母体化合物的酯或酰胺衍生物。这些前体药物通常是ROCK的弱抑制剂，但它们的母体化合物具有良好的活性。在滴入眼中后，这些前体药物的酯或酰胺基团迅速水解成醇，胺或酸，并且前药转化为活性碱化合物。 ROCK抑制剂的前体药物提供了几个优点，例如将更高浓度的活性物质递送到靶部位并减少眼部不适。本发明还涉及通过给需要治疗的患者的眼睛施用有效量的式I的ROCK前药化合物来治疗眼科疾病例如青光眼，变应性结膜炎，黄斑水肿，黄斑变性和睑缘炎的方法。

38. 发明公开

EP2627336A1 METHOD FOR TREATING CYSTIC FIBROSIS WITH INHALED DENUFOSOL 审中-公开
标题翻译：方法囊性纤维化治疗吸入地纽福索
公开(公告)号：EP2627336A1
公开(公告)日：2013-08-21
申请号：EP11833157.8
申请日：2011-10-06
申请人： Inspire Pharmaceuticals, Inc.
发明人： KRISHNAMOORTHY, Ramesh , EVANS, Carole M. , BURKE, Brian J. , SCHABERG, Amy E. , COADY, Thomas G.
IPC分类号： A61K31/7072
CPC分类号： A61K9/0078 , A61K31/7072 , A61M11/001 , A61M15/00 , A61M16/14
摘要： The present invention is directed to a method for treating cystic fibrosis. The method comprises the steps of: identifying a patient suffering from cystic fibrosis, applying about 0.8-3 mL of a solution comprising about 18-65 mg/mL of denufosol into a medication reservoir of an nebulizer to achieve a target loading dose of denufosol of about 25-52 mg denufosol per dosing regimen, nebulizing the solution by passing through holes of an vibrating mesh device equipped with an oscillating membrane in the nebulizer, and delivering an inhaled respiratory dose of 20-33 mg to the lungs of the patient by inhalation within 3-9 minutes.

39. 发明公开

EP2595665A1 BIFUNCTIONAL RHO KINASE INHIBITOR COMPOUNDS, COMPOSITION AND USE 审中-公开
标题翻译：双功能Rho激酶抑制剂化合物，组合物及适当地使用该
公开(公告)号：EP2595665A1
公开(公告)日：2013-05-29
申请号：EP11810195.5
申请日：2011-07-15
申请人： Inspire Pharmaceuticals, Inc.
发明人： LAMPE, John W. , WATSON, Paul S. , VITTITOW, Jason L. , PETERSON, Ward M.
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： C07D401/12 , A61K31/454 , A61K31/4725 , A61K31/5575 , A61K47/55 , C07D401/14
摘要： This invention relates to synthetic bifunctional compounds comprising a first rho-associated kinase (ROCK) inhibiting compound and a second pharmaceutically active compound with complementary activity; the first and the second compounds are covalently linked by a biologically labile bond. This invention also relates to methods of making such compounds. The invention also relates to methods of using such bifunctional compounds in the prevention or treatment of diseases or conditions that are affected or can be assisted by altering the integrity or rearrangement of the cytoskeleton. Particularly, this invention relates to methods of treating ophthalmic diseases such as disorders in which intraocular pressure is elevated, for example primary open-angle glaucoma, using the bifunctional compounds.

40. 发明公开

EP2512239A1 BRIDGED BICYCLIC RHO KINASE INHIBITOR COMPOUNDS, COMPOSITION AND USE 审中-公开
标题翻译：桥双环Rho激酶抑制剂化合物，组合物及其使用
公开(公告)号：EP2512239A1
公开(公告)日：2012-10-24
申请号：EP10838164.1
申请日：2010-12-10
申请人： Inspire Pharmaceuticals, Inc.
发明人： LAMPE, John, W. , WATSON, Paul, S. , SLADE, David, J.
IPC分类号： A01N43/00 , A61K31/55
CPC分类号： C07D451/04 , A61K31/46 , A61K31/4725 , C07D401/12 , C07D403/12 , C07D413/12 , C07D453/06 , C07D471/08 , C07D487/08
摘要： The present invention is directed to synthetic bridged bicyclic compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. The method comprises administering to a subject a therapeutically effective amount of a Rho kinase inhibitory compound of Formula I, wherein said amount is effective to influence the actomyosin interactions, for example, by leading to cellular relaxation and alterations in cell-substratum adhesions. In one embodiment, the method treats increased intraocular pressure, such as primary open-angle glaucoma. In another embodiment, the method treats diseases or conditions of the lung associated with excessive cell proliferation, remodeling, inflammation, vasoconstriction, bronchoconstriction, airway hyperreactivity and edema.

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