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1. 发明申请

US20050009778A1 Method for treating retinal degeneration with purinergic receptor agonists 审中-公开
标题翻译：用嘌呤能受体激动剂治疗视网膜变性的方法
公开(公告)号：US20050009778A1
公开(公告)日：2005-01-13
申请号：US10916086
申请日：2004-08-10
申请人： Ward Peterson
发明人： Ward Peterson
IPC分类号： A61K9/02 , A61K9/06 , A61K9/08 , A61K9/10 , A61K9/12 , A61K9/127 , A61K9/14 , A61K9/70 , A61K9/72 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/7084 , A61K45/00 , A61P25/02 , A61P27/02 , A61P27/06 , A61P29/00 , A61P43/00 , C07H19/10 , C07H19/20 , C07H19/207
CPC分类号： C07H19/10 , C07H19/20 , C07H19/207
摘要： The present invention provides a method of preventing or treating retinal degeneration arising from pathophysiological or physical conditions. The method comprises administering to a patient a pharmaceutical composition comprising a purinergic P2Y receptor ligand, in an amount effective to elevate its extracellular concentration to activate retinal glial and neuronal cell surface P2Y receptors and mount a neuroprotective response. Methods of administering including intravitreal bolus and sustained administrations, transscleral delivery, topical, and systemic administrations. The pharmaceutical composition useful in this invention comprises a P2Y purinergic receptor agonist, which include uridine 5′-di- and triphosphate (UDP, UTP) and their analogs, adenosine 5′-diphosphate (ADP) and its analogs, cytidine 5′-di- and triphosphate (CDP, CTP) and their analogs, and dinucleoside polyphosphate compounds.
摘要翻译：本发明提供了预防或治疗由病理生理或身体状况引起的视网膜变性的方法。该方法包括向患者施用包含嘌呤能P2Y受体配体的药物组合物，其量可有效地提高其细胞外浓度以激活视网膜神经胶质细胞和神经元细胞表面P2Y受体并且起到神经保护作用。施用方法包括玻璃体内推注和持续施用，经巩膜递送，局部和全身施用。可用于本发明的药物组合物包含P2Y嘌呤能受体激动剂，其包括尿苷5'-二磷酸和三磷酸（UDP，UTP）及其类似物腺苷5'-二磷酸（ADP）及其类似物胞苷5'-二 - 和三磷酸（CDP，CTP）及其类似物，以及二核苷多磷酸盐化合物。

2. 发明申请

US20070244068A1 Degradation-resistant mononucleoside phosphate compounds 失效
标题翻译：降解抗性单核苷磷酸化合物
公开(公告)号：US20070244068A1
公开(公告)日：2007-10-18
申请号：US11285221
申请日：2005-11-21
申请人： James Douglass , Benjamin Yerxa , Sammy Shaver , Ward Peterson , Edward Brown , Christopher Crean , Jose Boyer
发明人： James Douglass , Benjamin Yerxa , Sammy Shaver , Ward Peterson , Edward Brown , Christopher Crean , Jose Boyer
IPC分类号： A61K31/7052 , A61P1/00 , A61P11/00 , A61P27/02 , A61P29/00 , A61P37/08 , A61P7/02 , C07H19/052 , C07H19/06
CPC分类号： C07H19/10 , C07H19/20
摘要： The present invention relates to mononucleoside phosphate compounds that have the benefits of a dinucleotide pharmaceutical. These mononucleoside phosphates can be made from a mononucleotide that has been modified by attaching a degradation-resistant substituent on the terminal phosphate of a polyphosphate mononucleotide. By attaching this degradation-resistant substituent, the stability from degradation matches or exceeds those of certain dinucleotides. The mononucleoside phosphate compounds of the present invention are useful in preventing and treating epithelial tissue diseases or diseases or disorders associated with platelet aggregation.
摘要翻译：本发明涉及具有二核苷酸药物益处的单核苷磷酸化合物。这些单核苷酸磷酸酯可以由已经通过在聚磷酸酯单核苷酸的末端磷酸酯上连接降解抗性取代基而被修饰的单核苷酸制成。通过连接该降解抗性的取代基，降解的稳定性与某些二核苷酸的匹配或超过某些二核苷酸。本发明的单核苷磷酸化合物可用于预防和治疗与血小板聚集有关的上皮组织疾病或疾病或病症。

3. 发明申请

US20050085439A1 Pharmaceutical formulation comprising dinucleoside polyphosphates and salts thereof 有权
标题翻译：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。

4. 发明申请

US20070197454A1 P1-(2'-DEOXYCYTIDINE 5'-)P4-(URIDINE 5'-)TETRAPHOSPHATE, TETRA-(ALKALI METAL) SALT, FOR TREATING DISORDERS 有权
标题翻译： P1-（2'-DEOXYCYTIDINE 5' - ）P4-（URIDINE 5' - ）TETRAPHOSPHATE，TETRA-（ALKALI METAL）SALT，用于治疗疾病
公开(公告)号：US20070197454A1
公开(公告)日：2007-08-23
申请号：US11690385
申请日：2007-03-23
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： A61K31/7072
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 present invention also provides a method of treating cystic fibrosis. The present invention further 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。本发明还提供治疗囊性纤维化的方法。本发明进一步提供了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。

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