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    Method of treating lung diseases with uridine 5′-diphosphate and analogs thereof
    1.
    发明授权
    Method of treating lung diseases with uridine 5′-diphosphate and analogs thereof 有权
    用尿苷5'-二磷酸治疗肺部疾病的方法及其类似物

    公开(公告)号：US06451288B1

    公开(公告)日：2002-09-17

    申请号：US09645161

    申请日：2000-08-24

    申请人： Richard C. Boucher, Jr. ,  Sammy Ray Shaver ,  William Pendergast ,  Benjamin Yerxa ,  Janet L. Rideout ,  Robert Dougherty ,  Dallas Croom

    发明人： Richard C. Boucher, Jr. ,  Sammy Ray Shaver ,  William Pendergast ,  Benjamin Yerxa ,  Janet L. Rideout ,  Robert Dougherty ,  Dallas Croom

    IPC分类号： A61K912

    CPC分类号： A61K31/7068 ,  A61K9/0073 ,  A61K31/7072 ,  A61K45/06 ,  C07H19/10 ,  Y10S514/826 ,  Y10S514/851 ,  A61K2300/00

    摘要： Compounds of Formula I: wherein: X1, and X2 are each independently either O− or S−; X3 and X4 are each independently either —H or —OH, with the proviso that X3 and X4 are not simultaneously —H; R1 is selected from the group consisting of O, imido, methylene and dihalomethylene; R2 is selected from the group consisting of H, halo, alkyl, substituted alkyl, alkoxyl, nitro and azido; R3 is selected from the group consisting of H, alkyl, acyl, aryl, and arylalkyl; and R4 is selected from the group consisting of —OR′, —SR′, —NR′, and —NR′R″, wherein R′ and R″ are independently selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, alkoxyl, and aryloxyl, with the proviso that R′ is absent when R4 is double bonded from an oxygen or sulfur atom to the carbon at the 4-position of the pyrimidine ring, are used in methods of hydrating lung mucus secretions and treating lung disorders such as cystic fibrosis, ventilator-associated pneumonia, chronic bronchitis, chronic obstructive pulmonary disorder and primary ciliary dyskinesia. Pharmaceutical compositions containing compounds of Formula I, and novel compounds of Formula I are also described.

    摘要翻译： 式I化合物：其中：X 1和X 2各自独立地为O-或S-; X 3和X 4各自独立地为-H或-OH，条件是X 3和X 4不同时为-H; R 1为选自 由O，亚氨基，亚甲基和二卤代亚甲基组成的组; R 2选自H，卤素，烷基，取代的烷基，烷氧基，硝基和叠氮基; R 3选自H，烷基，酰基， 芳基和芳基烷基; 和R 4选自-OR'，-SR'，-NR'和-NR'R“，其中R'和R”独立地选自H，烷基，取代的烷基， 芳基，取代的芳基，芳基烷基，烷氧基和芳氧基，条件是当R4与氧或硫原子双键连接到嘧啶环的4位上的碳时，R'不存在，用于水合 肺粘液分泌物和治疗肺部疾病如囊性纤维化，呼吸机相关肺炎，慢性支气管炎，慢性阻塞性肺病和原发性纤毛运动障碍。 还描述了含有式I化合物和式I的新化合物的药物组合物。

    Uridine 5'-diphosphate and analogs useful for treating lung diseases
    2.
    发明授权
    Uridine 5'-diphosphate and analogs useful for treating lung diseases 有权
    尿苷5'-二磷酸和类似物可用于治疗肺部疾病

    公开(公告)号：US6143279A

    公开(公告)日：2000-11-07

    申请号：US143297

    申请日：1998-08-28

    申请人： Richard C. Boucher, Jr. ,  Sammy Ray Shaver ,  William Pendergast ,  Benjamin Yerxa ,  Janet L. Rideout ,  Robert Dougherty ,  Dallas Croom

    发明人： Richard C. Boucher, Jr. ,  Sammy Ray Shaver ,  William Pendergast ,  Benjamin Yerxa ,  Janet L. Rideout ,  Robert Dougherty ,  Dallas Croom

    IPC分类号： A61K9/00 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61K45/06 ,  A61P11/00 ,  C07H19/10 ,  A61K9/12

    CPC分类号： A61K31/7068 ,  A61K31/7072 ,  A61K45/06 ,  A61K9/0073 ,  C07H19/10 ,  Y10S514/826 ,  Y10S514/851

    摘要： Compounds of Formula I: ##STR1## wherein: X.sub.1, and X.sub.2 are each independently either O.sup.- or S.sup.- ;X.sub.3 and X.sub.4 are each independently either --H or --OH, with the proviso that X.sub.3 and X.sub.4 are not simultaneously --H;R.sub.1 is selected from the group consisting of O, imido, methylene and dihalomethylene;R.sub.2 is selected from the group consisting of H, halo, alkyl, substituted alkyl, alkoxyl, nitro and azido;R.sub.3 is selected from the group consisting of H, alkyl, acyl, aryl, and arylalkyl; andR.sub.4 is selected from the group consisting of --OR', --SR', --NR', and --NR'R", wherein R' and R" are independently selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, alkoxyl, and aryloxyl, with the proviso that R' is absent when R.sub.4 is double bonded from an oxygen or sulfur atom to the carbon at the 4-position of the pyrimidine ring, are used in methods of hydrating lung mucus secretions and treating lung disorders such as cystic fibrosis, ventilator-associated pneumonia, chronic bronchitis, chronic obstructive pulmonary disorder and primary ciliary dyskinesia. Pharmaceutical compositions containing compounds of Formula I, and novel compounds of Formula I are also described.

    摘要翻译： 式I化合物：其中：X 1和X 2各自独立地为O-或S-; X 3和X 4各自独立地是-H或-OH，条件是X 3和X 4不同时为-H; R1选自O，亚氨基，亚甲基和二卤代亚甲基; R2选自H，卤素，烷基，取代的烷基，烷氧基，硝基和叠氮基; R3选自H，烷基，酰基，芳基和芳基烷基; 并且R 4选自-OR'，-SR'，-NR'和-NR'R“，其中R'和R”独立地选自H，烷基，取代的烷基 ，芳基，取代的芳基，芳基烷基，烷氧基和芳氧基，条件是当R4与氧或硫原子双键连接到嘧啶环的4-位上的碳时，R'不存在，用于 水分肺粘液分泌物和治疗肺部疾病如囊性纤维化，呼吸机相关肺炎，慢性支气管炎，慢性阻塞性肺病和原发性纤毛运动障碍。 还描述了含有式I化合物和式I的新化合物的药物组合物。

    Method of treating lung diseases with uridine 5'-diphosphate and analogs thereof
    3.
    发明授权
    Method of treating lung diseases with uridine 5'-diphosphate and analogs thereof 有权
    用尿苷5'-二磷酸治疗肺部疾病的方法及其类似物

    公开(公告)号：US6022527A

    公开(公告)日：2000-02-08

    申请号：US352390

    申请日：1999-07-13

    申请人： Richard C. Boucher, Jr. ,  Sammy Ray Shaver ,  William Pendergast ,  Benjamin Yerxa ,  Janet L. Rideout ,  Robert Dougherty ,  Dallas Croom

    发明人： Richard C. Boucher, Jr. ,  Sammy Ray Shaver ,  William Pendergast ,  Benjamin Yerxa ,  Janet L. Rideout ,  Robert Dougherty ,  Dallas Croom

    IPC分类号： A61K9/00 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61K45/06 ,  A61P11/00 ,  C07H19/10 ,  A61K9/12

    CPC分类号： A61K31/7068 ,  A61K31/7072 ,  A61K45/06 ,  A61K9/0073 ,  C07H19/10 ,  Y10S514/826 ,  Y10S514/851

    摘要： Compounds of Formula I: ##STR1## wherein: X.sub.1, and X.sub.2 are each independently either O.sup.- or S.sup.- ;X.sub.3 and X.sub.4 are each independently either --H or --OH, with the proviso that X.sub.3 and X.sub.4 are not simultaneously --H;R.sub.1 is selected from the group consisting of O, imido, methylene and dihalomethylene;R.sub.2 is selected from the group consisting of H, halo, alkyl, substituted alkyl, alkoxyl, nitro and azido;R.sub.3 is selected from the group consisting of H, alkyl, acyl, aryl, and arylalkyl; andR.sub.4 is selected from the group consisting of --OR', --SR', --NR', and --NR'R", wherein R' and R" are independently selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, alkoxyl, and aryloxyl, with the proviso that R' is absent when R.sub.4 is double bonded from an oxygen or sulfur atom to the carbon at the 4-position of the pyrimidine ring, are used in methods of hydrating lung mucus secretions and treating lung disorders such as cystic fibrosis, ventilator-associated pneumonia, chronic bronchitis, chronic obstructive pulmonary disorder and primary ciliary dyskinesia. Pharmaceutical compositions containing compounds of Formula I, and novel compounds of Formula I are also described.

    摘要翻译： 式I化合物：其中：X 1和X 2各自独立地为O-或S-; X 3和X 4各自独立地是-H或-OH，条件是X 3和X 4不同时为-H; R1选自O，亚氨基，亚甲基和二卤代亚甲基; R2选自H，卤素，烷基，取代的烷基，烷氧基，硝基和叠氮基; R3选自H，烷基，酰基，芳基和芳基烷基; 并且R 4选自-OR'，-SR'，-NR'和-NR'R“，其中R'和R”独立地选自H，烷基，取代的烷基 ，芳基，取代的芳基，芳基烷基，烷氧基和芳氧基，条件是当R4与氧或硫原子双键连接到嘧啶环的4-位上的碳时，R'不存在，用于 水分肺粘液分泌物和治疗肺部疾病如囊性纤维化，呼吸机相关肺炎，慢性支气管炎，慢性阻塞性肺病和原发性纤毛运动障碍。 还描述了含有式I化合物和式I的新化合物的药物组合物。

    Method of treating dry eye disease with purinergic receptor agonists
    5.
    发明申请
    Method of treating dry eye disease with purinergic receptor agonists 有权
    用嘌呤能受体激动剂治疗干眼病的方法

    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。

    Pharmaceutical formulation comprising dinucleoside polyphosphates and salts thereof
    6.
    发明申请
    Pharmaceutical formulation comprising dinucleoside polyphosphates and salts thereof 有权
    包含二核苷多磷酸盐及其盐的药物制剂

    公开(公告)号：US20050085439A1

    公开(公告)日：2005-04-21

    申请号：US10962016

    申请日：2004-10-07

    申请人： Benjamin Yerxa ,  Ward Peterson ,  Janet Rideout ,  William Pendergast

    发明人： Benjamin Yerxa ,  Ward Peterson ,  Janet Rideout ,  William Pendergast

    IPC分类号： A61K31/7084 ,  C07H19/04 ,  C07H19/10 ,  C07H19/20 ,  C07H21/00 ,  A61K31/7072

    CPC分类号： C07H19/10 ,  A61K31/7072 ,  A61K31/7084 ,  C07H19/04 ,  C07H19/20 ,  C07H21/00 ,  Y10S514/851

    摘要： The present invention provides a method of treating edematous retinal disorders. The method comprises administration of a pharmaceutical formulation comprising a hydrolysis-resistant P2Y receptor agonist to stimulate the removal of pathological extraneous fluid from the subretinal and retinal spaces and thereby reduce the accumulation of said fluid associated with retinal detachment and retinal edema. The P2Y receptor agonist can be administered with therapeutic and adjuvant agents commonly used to treat edematous retinal disorders. The pharmaceutical formulation useful in this invention comprises a P2Y receptor agonist with enhanced resistance to extracellular hydrolysis, such as dinucleoside polyphosphate compounds, or hydrolysis-resistant mononucleoside triphosphate salts. The present invention also provides P1-(2′-deoxycytidine 5′-)P4-(uridine 5′-)tetraphosphate, tetra-(alkali metal) salts such as tetrasodium, tetralithium, tetrapotassium, and mixed (tetra-alkali metal) salts. The present further provides a pharmaceutical formulation comprising a P1-(2′-deoxycytidine 5′-)P4-(uridine 5′-)tetraphosphate, tetra-(alkali metal) salt, in a pharmaceutically acceptable carrier.

    摘要翻译： 本发明提供治疗水肿性视网膜病变的方法。 该方法包括施用包含水解抗性P2Y受体激动剂的药物制剂，以刺激从视网膜下和视网膜空间中除去病理性外来流体，从而减少与视网膜脱离和视网膜水肿相关的所述流体的积聚。 P2Y受体激动剂可以与通常用于治疗水肿性视网膜疾病的治疗剂和辅助剂一起施用。 可用于本发明的药物制剂包含具有增强的细胞外水解抗性的P2Y受体激动剂，例如二核苷多磷酸酯化合物或耐水解的单核苷三磷酸盐。 本发明还提供了P 1 - （2'-脱氧胞苷5' - ）P 4 - （尿苷5'-）四磷酸盐，四（碱金属盐）盐 作为四钠，四锂，四钾和混合（四碱金属）盐。 本发明还提供一种药物制剂，其包含P 1 - （2'-脱氧胞苷5' - ）P 4 - （尿苷5' - ）四磷酸酯，四 - （碱 金属）盐，在药学上可接受的载体中。

    Di(uridine 5'-)tetraphosphate and salts thereof
    7.
    发明申请
    Di(uridine 5'-)tetraphosphate and salts thereof 有权
    二（尿苷5' - ）四磷酸及其盐

    公开(公告)号：US20050148540A1

    公开(公告)日：2005-07-07

    申请号：US11055170

    申请日：2005-02-09

    申请人： Benjamin Yerxa ,  Edward Brown

    发明人： Benjamin Yerxa ,  Edward Brown

    IPC分类号： C07H21/00 ,  A61K31/7072

    CPC分类号： A61K31/7048 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  C07H19/10 ,  C07H19/20 ,  C07H21/00 ,  Y10S514/851

    摘要： The present invention are directed to P1,P4-di(uridine 5′-)tetraphosphate, tetra-alkali metal salts such as tetrasodium, tetralithium, tetrapotassium, and mixed tetra-alkali metal cations thereof. The tetra alkali metal salts of P1,P4-di(uridine 5′-)tetraphosphate are water-soluble, nontoxic, and easy to handle during manufacture. These tetra-monovalent alkali metal salts are more resistant to hydrolysis than the mono-, di-, or tri-acid salts, therefore, they provide an improved stability and a longer shelf life for storage. The present invention also provides methods for the synthesis of P1,P4-di(uridine 5′-)tetraphosphate, and its pharmaceutically acceptably acceptable salts thereof, and demonstrates the applicability to the production of large quantities. The methods substantially reduce the time required to synthesize diuridine tetraphosphate, for example, to three days or less.

    摘要翻译： 本发明涉及P 1，P 4 - 二（尿苷5'-）四磷酸盐，四碱金属盐如四钠，四锂，四钾，并混合 其四碱金属阳离子。 P 1，4 -di（尿苷5'-）四磷酸的四碱金属盐是水溶性的，无毒的，并且在制造过程中易于处理。 这些四价一价碱金属盐比单 - ，二 - 或三 - 酸盐更耐水解，因此，它们提供了改进的稳定性和更长的储存期限。 本发明还提供了合成P 1，P 4 - 二（尿苷5' - ）四磷酸及其药学上可接受的盐的方法，并且证明了 适用于大批量生产。 所述方法基本上减少了合成二脯氨酸四磷酸酯所需的时间，例如为3天或更短。

    Compositions for the treatment of glaucoma or ocular hypertension
    9.
    发明申请
    Compositions for the treatment of glaucoma or ocular hypertension 审中-公开
    用于治疗青光眼或高眼压症的组合物

    公开(公告)号：US20050130931A1

    公开(公告)日：2005-06-16

    申请号：US11049201

    申请日：2005-02-01

    申请人： Jose Boyer ,  Benjamin Yerxa ,  Robert Plourde ,  Edward Brown ,  James Douglass

    发明人： Jose Boyer ,  Benjamin Yerxa ,  Robert Plourde ,  Edward Brown ,  James Douglass

    IPC分类号： A61K31/7068 ,  A61K31/7072 ,  A61K31/7084 ,  C07H19/04 ,  C07H19/10 ,  C07H19/20 ,  C07H19/207 ,  C07H21/00 ,  A61K31/675

    CPC分类号： A61K31/7084 ,  A61K31/7068 ,  A61K31/7072 ,  C07H19/04 ,  C07H19/10 ,  C07H19/20 ,  C07H19/207 ,  C07H21/00

    摘要： The present invention is directed to a method of reducing intraocular pressure. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a nucleoside 5′-pyrophosphate pyranoside or analogue, which is defined by general Formula I. The method of the present invention is useful in the treatment or prevention of ocular hypertension, such as found in glaucoma, including primary and secondary glaucoma. The method can be used alone to reduce intraocular pressure. The method can also be used in conjunction with another therapeutic agent or adjunctive therapy commonly used to treat glaucoma to enhance the therapeutic effect of reducing the intraocular pressure. The present invention also provides a novel composition comprising a nucleoside 5′-pyrophosphate pyranoside or analogue.

    摘要翻译： 本发明涉及降低眼内压的方法。 该方法包括向受试者施用包含有效量的由通式I定义的核苷5'-焦磷酸吡喃糖苷或类似物的药物组合物。本发明的方法可用于治疗或预防高眼压症， 例如在青光眼中发现，包括原发性和继发性青光眼。 该方法可单独使用以降低眼内压。 该方法还可以与通常用于治疗青光眼的另一种治疗剂或辅助治疗联合使用，以增强降低眼内压的治疗效果。 本发明还提供了包含核苷5'-焦磷酸吡喃糖苷或类似物的新型组合物。