公开(公告)号：US5958897A

公开(公告)日：1999-09-28

申请号：US4784

申请日：1998-01-09

申请人： Karla Jacobus ,  Janet Rideout ,  Ben Yerxa ,  William Pendergast ,  Suhaib Siddiqi ,  David Drutz

发明人： Karla Jacobus ,  Janet Rideout ,  Ben Yerxa ,  William Pendergast ,  Suhaib Siddiqi ,  David Drutz

IPC分类号： C07H19/067 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61P11/02 ,  A61P43/00 ,  C07H19/10 ,  C07H19/167 ,  C07H19/20 ,  A61K31/70

CPC分类号： A61K31/7048 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  C07H19/10 ,  C07H19/20

摘要： A method of promoting drainage of congested mucous secretions in the sinuses of a subject in need of such treatment is disclosed. The method comprises administering to the sinuses of the subject a uridine phosphate such as uridine 5'-triphosphate (UTP) or P.sup.1,P.sup.4 -di(uridine-5') tetraphosphate (U.sub.2 P.sub.4), an analog of UTP, or any other analog, in an amount effective to promote drainage of congested fluid in the sinuses by hydrating mucous secretions or by stimulating ciliary beat frequency in the sinuses. 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 form (liquid or pill), aerosol inhalation, powder form, topical, injected, intra-operative instillation or suppository form.

摘要翻译： 公开了一种促进需要这种治疗的受试者的窦内的拥挤的粘液分泌物的引流的方法。 该方法包括对受试者的鼻窦施用尿苷磷酸酯，例如尿苷5'-三磷酸（UTP）或P1，P4-二（尿苷-5'）四磷酸（U2P4），UTP的类似物或任何其它类似物， 通过保湿粘液分泌物或通过刺激窦内的睫状肌痉挛频率，有效促进窦内充血液引流。 还公开了药物制剂及其制备方法。 给药方法包括任何液体悬浮液（包括滴鼻剂或喷雾剂），口服形式（液体或药丸），气雾剂吸入剂，粉末形式，局部用药，注射剂，术中滴注或栓剂形式。

公开(公告)号：US5789391A

公开(公告)日：1998-08-04

申请号：US675620

申请日：1996-07-03

申请人： Karla Jacobus ,  Janet Rideout ,  Ben Yerxa ,  William Pendergast ,  Suhaib Siddiqi ,  David Drutz

发明人： Karla Jacobus ,  Janet Rideout ,  Ben Yerxa ,  William Pendergast ,  Suhaib Siddiqi ,  David Drutz

IPC分类号： C07H19/067 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61P11/02 ,  A61P43/00 ,  C07H19/10 ,  C07H19/167 ,  C07H19/20 ,  A61K31/70

CPC分类号： A61K31/7048 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  C07H19/10 ,  C07H19/20

摘要： A method of promoting drainage of congested mucous secretions in the sinuses of a subject in need of such treatment is disclosed. The method comprises administering to the sinuses of the subject a uridine phosphate such as uridine 5'-triphosphate (UTP) or P.sup.1,P.sup.4 -di(uridine-5') tetraphosphate (U.sub.2 P.sub.4), an analog of UTP, or any other analog, in an amount effective to promote drainage of congested fluid in the sinuses by hydrating mucous secretions or by stimulating ciliary beat frequency in the sinuses. 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 form (liquid or pill), aerosol inhalation, powder form, topical, injected, intra-operative instillation or suppository form.

公开(公告)号：US20050197316A1

公开(公告)日：2005-09-08

申请号：US11114957

申请日：2005-04-25

申请人： Benjamin Yerxa ,  Karla Jacobus ,  William Pendergast ,  Janet Rideout

发明人： Benjamin Yerxa ,  Karla Jacobus ,  William Pendergast ,  Janet Rideout

IPC分类号： A61K9/06 ,  A61K9/00 ,  A61K9/08 ,  A61K9/10 ,  A61K9/12 ,  A61K9/127 ,  A61K9/14 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/7084 ,  A61K45/06 ,  A61K47/02 ,  A61K47/14 ,  A61K47/26 ,  A61K47/32 ,  A61K47/34 ,  A61K47/36 ,  A61P27/02 ,  A61P27/04 ,  C07H19/10 ,  C07H19/20 ,  C07H21/00

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 enhancing drainage of lacrimal system 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.

摘要翻译： 公开了一种用于增强需要这种治疗的受试者中泪液系统排泄的方法和制备方法。 该方法包括向受试者的眼表面施用嘌呤能受体激动剂如尿苷5'-三磷酸（UTP），二核苷酸，胞苷5'-三磷酸（CTP），腺苷5'-三磷酸（ATP）或其治疗上有用的 类似物和衍生物，其量有效地刺激泪液分泌并增强泪液系统的引流。 还公开了药物制剂及其制备方法。 施用该方法的方法将包括：通过液体，凝胶，霜剂或作为隐形眼镜或选择性释放膜的一部分局部给药; 或通过鼻滴或喷雾进行全身给药，通过喷雾器或其它装置吸入，口服形式（液体或丸剂），可注射的，术中滴注或栓剂形式。

公开(公告)号：US5981506A

公开(公告)日：1999-11-09

申请号：US4785

申请日：1998-01-09

申请人： Karla Jacobus ,  Janet Rideout ,  Ben Yerxa ,  William Pendergast ,  Suhaib Siddiqi ,  David Drutz

发明人： Karla Jacobus ,  Janet Rideout ,  Ben Yerxa ,  William Pendergast ,  Suhaib Siddiqi ,  David Drutz

IPC分类号： C07H19/067 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61P11/02 ,  A61P43/00 ,  C07H19/10 ,  C07H19/167 ,  C07H19/20 ,  A61K31/70

CPC分类号： A61K31/7048 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  C07H19/10 ,  C07H19/20

摘要： A method of promoting drainage of congested mucous secretions in the sinuses of a subject in need of such treatment is disclosed. The method comprises administering to the sinuses of the subject a uridine phosphate such as uridine 5'-triphosphate (UTP) or P.sup.1,P.sup.4 -di(uridine-5') tetraphosphate (U.sub.2 P.sub.4), an analog of UTP, or any other analog, in an amount effective to promote drainage of congested fluid in the sinuses by hydrating mucous secretions or by stimulating ciliary beat frequency in the sinuses. 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 form (liquid or pill), aerosol inhalation, powder form, topical, injected, intra-operative instillation or suppository form.

摘要翻译： 公开了一种促进需要这种治疗的受试者的窦内的拥挤的粘液分泌物的引流的方法。 该方法包括对受试者的鼻窦施用尿苷磷酸酯，例如尿苷5'-三磷酸（UTP）或P1，P4-二（尿苷-5'）四磷酸（U2P4），UTP的类似物或任何其它类似物， 通过保湿粘液分泌物或通过刺激窦内的睫状肌痉挛频率，有效促进窦内充血液引流。 还公开了药物制剂及其制备方法。 给药方法包括任何液体悬浮液（包括滴鼻剂或喷雾剂），口服形式（液体或药丸），气雾剂吸入剂，粉末形式，局部用药，注射剂，术中滴注或栓剂形式。

公开(公告)号：US20080009463A1

公开(公告)日：2008-01-10

申请号：US11821091

申请日：2007-06-20

申请人： Benjamin Yerxa ,  Karla Jacobus ,  William Pendergast ,  Janet Rideout

发明人： Benjamin Yerxa ,  Karla Jacobus ,  William Pendergast ,  Janet Rideout

IPC分类号： A61K31/7084 ,  A61P27/02

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.

摘要翻译： 公开了用于刺激需要这种治疗的受试者的泪液分泌的方法和制剂。 该方法包括向受试者的眼表面施用嘌呤能受体激动剂如尿苷5'-三磷酸（UTP），二核苷酸，胞苷5'-三磷酸（CTP），腺苷5'-三磷酸（ATP）或其治疗上有用的 类似物和衍生物，其量有效地刺激泪液分泌并增强泪液系统的引流。 还公开了药物制剂及其制备方法。 施用该方法的方法将包括：通过液体，凝胶，霜剂或作为隐形眼镜或选择性释放膜的一部分局部给药; 或通过鼻滴或喷雾进行全身给药，通过喷雾器或其它装置吸入，口服形式（液体或丸剂），可注射的，术中滴注或栓剂形式。

公开(公告)号：US5972904A

公开(公告)日：1999-10-26

申请号：US4786

申请日：1998-01-09

申请人： Karla Jacobus ,  Janet Rideout ,  Ben Yerxa ,  William Pendergast ,  Suhaib Siddiqi ,  David Drutz

发明人： Karla Jacobus ,  Janet Rideout ,  Ben Yerxa ,  William Pendergast ,  Suhaib Siddiqi ,  David Drutz

IPC分类号： C07H19/067 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61P11/02 ,  A61P43/00 ,  C07H19/10 ,  C07H19/167 ,  C07H19/20 ,  A61K31/70

CPC分类号： A61K31/7048 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  C07H19/10 ,  C07H19/20

摘要： A method of promoting drainage of congested mucous secretions in the sinuses of a subject in need of such treatment is disclosed. The method comprises administering to the sinuses of the subject a uridine phosphate such as uridine 5'-triphosphate (UTP) or P.sup.1,P.sup.4 -di(uridine-5') tetraphosphate (U.sub.2 P.sub.4), an analog of UTP, or any other analog, in an amount effective to promote drainage of congested fluid in the sinuses by hydrating mucous secretions or by stimulating ciliary beat frequency in the sinuses. 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 form (liquid or pill), aerosol inhalation, powder form, topical, injected, intra-operative instillation or suppository form.

公开(公告)号：US5962432A

公开(公告)日：1999-10-05

申请号：US675555

申请日：1996-07-03

申请人： Karol La Croix ,  Christy Shaffer ,  Karla Jacobus ,  Janet Rideout ,  David Drutz

发明人： Karol La Croix ,  Christy Shaffer ,  Karla Jacobus ,  Janet Rideout ,  David Drutz

IPC分类号： A61K9/00 ,  A61K9/08 ,  A61K31/70 ,  A61K47/02

CPC分类号： A61K9/0078 ,  A61K31/7072 ,  A61K47/02 ,  A61K9/08

摘要： A novel formulation of uridine 5'-triphosphate (UTP) for use in promoting increased mucociliary clearance of retained mucous secretions of the human airways, middle/inner ears, or sinuses is disclosed. The composition comprises UTP and aqueous solution having a therapeutic concentration between 5 and 35 mg/mL, which has controlled tonicity within the range of 250 to 1000 mOsM, pH-adjusted, having pH between 7.0 and 7.5; and sterile. The pH-adjusted formulation is capable of long-term storage in the refrigerated state, with a shelf life of up to 30 months if kept refrigerated at 5.degree. C. The formulation is delivered therapeutically either in a nebulized form using any of several commercially available nebulizers (e.g., jet, ultrasonic, etc.), or in liquid form.

摘要翻译： 公开了用于促进人气道，中耳/内耳或鼻窦的残留粘液分泌物的增加的粘膜纤毛清除的尿苷5'-三磷酸（UTP）的新制剂。 该组合物包含治疗浓度为5至35mg / mL的UTP和水溶液，其具有控制的张力度在250至1000mOsM的范围内，pH调节，pH在7.0至7.5之间; 无菌。 pH调节的制剂能够在冷藏状态下长期储存，如果在5℃下冷藏，保质期可长达30个月。使用几种商业上可得到的方法，以雾化形式递送该制剂 喷雾器（例如喷射，超声波等）或液体形式。

公开(公告)号：US06696425B2

公开(公告)日：2004-02-24

申请号：US10027520

申请日：2001-12-19

申请人： Benjamin R. Yerxa ,  Karla Jacobus ,  William Pendergast ,  Janet L. Rideout

发明人： Benjamin R. Yerxa ,  Karla Jacobus ,  William Pendergast ,  Janet L. Rideout

IPC分类号： A61K3170

CPC分类号： A61K45/06 ,  Y10S514/912

摘要： This invention is directed to a method of stimulating tear secretion and mucin production in eyes. The method comprises the step of administering to the eyes of a subject a composition comprising a compound of Formula I, II, III, or IV and its pharmaceutically acceptable salts, in an amount effective to stimulate tear fluid secretion. The method of the present invention may be used to increase tear production for any reason, including, but not limited to, treatment of dry eye disease and corneal injury. 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.

摘要翻译： 本发明涉及刺激眼睛中的泪液分泌和粘蛋白产生的方法。 该方法包括以有效刺激泪液分泌的量向受试者施用包含式I，II，III或IV化合物及其药学上可接受的盐的组合物的步骤的步骤。 本发明的方法可以用于由于任何原因增加泪液产生，包括但不限于干眼病和角膜损伤的治疗。 还公开了药物制剂及其制备方法。 施用该方法的方法将包括：通过液体，凝胶，霜剂或作为隐形眼镜或选择性释放膜的一部分局部给药; 或通过鼻滴或喷雾进行全身给药，通过喷雾器或其它装置吸入，口服形式（液体或丸剂），可注射的，术中滴注或栓剂形式。