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91. 发明申请

US20050107443A1 Pyridoxine and pyridoxal analogues: new uses 失效
标题翻译：吡哆醇和吡哆醛类似物：新用途
公开(公告)号：US20050107443A1
公开(公告)日：2005-05-19
申请号：US11016737
申请日：2004-12-21
申请人： Wasimul Haque
发明人： Wasimul Haque
IPC分类号： C07D213/40 , C07D213/48 , C07D213/66 , C07D401/06 , C07D401/12 , A61K31/4439 , A61K31/44 , A61K31/4415
CPC分类号： C07D401/06 , C07D213/40 , C07D213/48 , C07D213/66 , C07D401/12
摘要： The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions containing a therapeutically effective amount of at least one of these analogues. In accordance with the present invention, the pyridoxal and pyridoxine analogues can be used in the treatment or prevention of of heparin induced thrombocytopenia (HIT), stroke, and ischemia, and in the treatment of symptoms thereof. The the pyridoxal and pyridoxine analogues can be used in neuroprotection.
摘要翻译：本发明提供了吡哆醛和吡哆醛类似物，含有吡哆醛和吡哆醛类似物的药物组合物，以及施用含有治疗有效量的至少一种这些类似物的药物组合物的方法。根据本发明，吡哆醛和吡哆醛类似物可用于治疗或预防肝素诱导的血小板减少症（HIT），中风和局部缺血以及治疗其症状。吡哆醛和吡哆醛类似物可用于神经保护。

92. 发明授权

US06867215B2 Cardioprotective phosphonates and malonates 失效
标题翻译：心脏保护膦酸盐和丙二酸盐
公开(公告)号：US06867215B2
公开(公告)日：2005-03-15
申请号：US10377507
申请日：2003-02-28
申请人： Wasimul Haque
发明人： Wasimul Haque
IPC分类号： C07D491/056 , A61K31/436 , A61K31/44 , A61K31/662 , A61K31/675 , A61K31/683 , A61K38/28 , A61K45/00 , A61P3/00 , A61P3/04 , A61P3/10 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P13/02 , A61P43/00 , C07D213/65 , C07D213/66 , C07F9/58 , C07F9/6561 , A61K31/435 , C07F9/30 , C07F9/34
CPC分类号： C07D213/66 , C07D213/65 , C07F9/58 , C07F9/6561
摘要： The present invention provides for pyridoxine phosphonate analogues such as, for example, ((2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridyl)alkylphosphonates, and (2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridyl)azaalkylphosphonates) and to pyridoxine malonate analogues, such as, for example, ((2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridylmethyl)malonates), pharmaceutical compositions, and methods for treatment of cardiovascular and related diseases, and diabetes mellitus and related diseases.
摘要翻译：本发明提供了吡哆酮膦酸酯类似物，例如（（2-甲基-3-羟基-4-羟甲基-5-吡啶基）烷基膦酸酯）和（2-甲基-3-羟基-4-羟甲基-5- 吡啶基）氮杂烷基磷酸酯）和吡哆酮丙二酸酯类似物，例如（（2-甲基-3-羟基-4-羟甲基-5-吡啶基甲基）丙二酸酯），药物组合物和治疗心血管及相关疾病的方法，和糖尿病及相关疾病。

93. 发明授权

US06780997B2 Cardioprotective phosphonates and malonates 失效
标题翻译：心脏保护膦酸盐和丙二酸盐
公开(公告)号：US06780997B2
公开(公告)日：2004-08-24
申请号：US10282328
申请日：2002-10-28
申请人： Wasimul Haque
发明人： Wasimul Haque
IPC分类号： C07D21330
CPC分类号： C07D213/66 , C07D213/65 , C07F9/58 , C07F9/6561
摘要： Pharmaceutical compositions including an effective amount of the compound of formula IV in which R1 is hydrogen or alkyl; R2 is —CHO, —CH2OH, —CH3 or —CO2R5 in which R5 is hydrogen, alkyl, or aryl; or R2 is —CH2O-alkyl- in which alkyl is covalently bonded to the oxygen at the 3-position instead of R1; R3 and R3′ are independently hydrogen or halo; or R3 and R3′ taken together constitute a second covalent bond between the carbons to which they are substituent; and R4 is hydrogen; or a pharmaceutically acceptable acid addition salt thereof, are taught. Also taught are methods of using the compositions, including for the treatment of myocardial infarctions, ischemia, congestive heart failure, arrhythmia, blood clots, hypertrophy, diabetes, insulin resistance, diabetes related damage, and obesity.
摘要翻译：药物组合物，包括有效量的式IV化合物，其中R 1是氢或烷基; R 2是-CHO，-CH 2 OH，-CH 3或-CO 2 R 5，其中R 5是氢，烷基或芳基; 或R 2是-CH 2 O-烷基 - 其中烷基在3-位上与氧共价结合而不是R 1; R 3和R 3'独立地是氢或卤素; 或R 3和R 3'组合在它们所取代的碳之间构成第二共价键; 和R 4是氢;或其药学上可接受的酸加成盐。还教导了使用组合物的方法，包括用于治疗心肌梗塞，缺血，充血性心力衰竭，心律失常，血凝块，肥大，糖尿病，胰岛素抵抗，糖尿病相关损伤和肥胖。

94. 发明授权

US06730686B1 Methods for inhibiting oxidative modification of proteins 有权
标题翻译：抑制蛋白质氧化修饰的方法
公开(公告)号：US06730686B1
公开(公告)日：2004-05-04
申请号：US09414877
申请日：1999-10-08
申请人： John W. Baynes , Joelle Onorato , Suzanne Thorpe , Raja Khalifah , Billy G. Hudson
发明人： John W. Baynes , Joelle Onorato , Suzanne Thorpe , Raja Khalifah , Billy G. Hudson
IPC分类号： A61K3144
CPC分类号： G01N33/6842 , A61K31/00 , A61K31/04 , A61K31/137 , A61K31/435 , A61K31/44 , A61K31/4415 , A61K31/506 , A61K31/675 , A61K38/05 , A61K38/06 , A61K38/07 , C07C215/50 , C07D213/66 , C07K5/06034 , C07K5/06052 , C07K5/0812 , G01N33/68 , G01N33/6812 , G01N2400/02 , G01N2500/04
摘要： The instant invention provides compositions and methods for modeling post-Amadori AGE formation and the identification and characterization of effective inhibitors of post-Amadori AGE formation, and such identified inhibitor compositions. The instant invention also teaches new methods to treat or prevent oxidative modification of proteins, including low density lipoproteins, to treat or prevent lipid peroxidation, and to treat or prevent atherosclerosis, comprising administering an amount effective of one of the compounds of the invention to treat or prevent the disorder.
摘要翻译：本发明提供了用于模拟阿马多前AGE形成的组合物和方法以及后Amadori AGE形成的有效抑制剂的鉴定和表征，以及这些鉴定的抑制剂组合物。本发明还教导了治疗或预防蛋白质（包括低密度脂蛋白）的氧化修饰以治疗或预防脂质过氧化以及治疗或预防动脉粥样硬化的新方法，包括给予本发明化合物之一的有效量来治疗或预防紊乱。

95. 发明授权

US06667315B2 Cardioprotective phosphonates and malonates 失效
公开(公告)号：US06667315B2
公开(公告)日：2003-12-23
申请号：US10282326
申请日：2002-10-28
申请人： Wasimul Haque
发明人： Wasimul Haque
IPC分类号： A61K314415
CPC分类号： C07D213/66 , C07D213/65 , C07F9/58 , C07F9/6561
摘要： The present invention provides for pyridoxine phosphonate analogues such as, for example, ((2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridyl)alkylphosphonates, and (2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridyl)azaalkylphosphonates) and to pyridoxine malonate analogues, such as, for example, ((2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridylmethyl)malonates), pharmaceutical compositions, and methods for treatment of cardiovascular and related diseases, and diabetes mellitus and related diseases.

96. 发明申请

US20030195236A1 Pyridoxal analogues and methods of treatment 失效
标题翻译：吡哆醛类似物和治疗方法
公开(公告)号：US20030195236A1
公开(公告)日：2003-10-16
申请号：US10453414
申请日：2003-06-03
申请人： Medicure Inc. , The University of Manitoba
发明人： Wasimul Haque
IPC分类号： A61K031/4415 , C07D213/78
CPC分类号： C07D213/66 , A61K31/44 , A61K45/06 , C07D491/04 , A61K2300/00
摘要： Pyridoxal analogues can be useful for treating B6 deficiency and related diseases; cardiovascular and related diseases; melanoma and related diseases; and symptoms thereof. One such analogue is a compound of the formula: 1 or a pharmaceutically acceptable acid addition salt thereof, in which R1 is alkyl, alkenyl, in which alkyl or alkenyl can be interrupted by nitrogen, oxygen, or sulfur, and can be substituted at the terminal carbon by hydroxy, alkoxy, alkanoyloxy, alkanoyloxyaryl, alkoxyalkanoyl, alkoxycarbonyl, or dialkylcarbamoyloxy; alkoxy; dialkylamino; alkanoyloxy; alkanoyloxyaryl; alkoxyalkanoyl; alkoxycarbonyl; dialkylcarbamoyloxy; or aryl, aryloxy, arylthio, or aralkyl, in which aryl can be substituted by alkyl, alkoxy, amino, hydroxy, halo, nito, or alkanoyloxy. These analogues can be administered, either alone or concurrently with known medications, to treat the above-described diseases.
摘要翻译：吡哆醛类似物可用于治疗B＆lt; 6＆lt; 6＆gt;缺陷和相关疾病; 心血管疾病及相关疾病; 黑素瘤及相关疾病; 及其症状。一种这样的类似物是下式的化合物或其药学上可接受的酸加成盐，其中R 1是烷基或链烯基，其中烷基或烯基可被氮，氧或硫中断并且可以在末端被羟基，烷氧基，烷酰氧基，烷酰氧基芳基，烷氧基烷酰基，烷氧基羰基或二烷基氨基甲酰氧基取代; 烷氧基二烷基氨基; 烷酰氧基; 烷酰氧基芳基烷氧基烷酰基烷氧基羰基二烷基氨基甲酰氧基或芳基，芳氧基，芳硫基或芳烷基，其中芳基可以被烷基，烷氧基，氨基，羟基，卤素，硝基或烷酰氧基取代。这些类似物可以单独使用或与已知药物同时施用以治疗上述疾病。

97. 发明申请

US20030181422A1 Cardioprotective phosphonates and malonates 失效
公开(公告)号：US20030181422A1
公开(公告)日：2003-09-25
申请号：US10377507
申请日：2003-02-28
申请人： Medicure International Inc.
发明人： Wasimul Haque
IPC分类号： A61K031/675
CPC分类号： C07D213/66 , C07D213/65 , C07F9/58 , C07F9/6561
摘要： The present invention provides for pyridoxine phosphonate analogues such as, for example, ((2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridyl)alkylphosphonates, and (2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridyl)azaalkylphosphonates) and to pyridoxine malonate analogues, such as, for example, ((2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridylmethyl)malonates), pharmaceutical compositions, and methods for treatment of cardiovascular and related diseases, and diabetes mellitus and related diseases.

98. 发明授权

US06610852B2 Post-Amadori inhibitors of advanced glycation reactions 有权
标题翻译：晚期糖化反应后阿马多利抑制剂
公开(公告)号：US06610852B2
公开(公告)日：2003-08-26
申请号：US10085787
申请日：2001-10-19
申请人： Raja Khalifah , Aaron Ashley Booth
发明人： Raja Khalifah , Aaron Ashley Booth
IPC分类号： C07D21304
CPC分类号： C07D213/66 , C07D213/65 , C07D401/14 , C07F9/58
摘要： The present invention provides novel compounds, pharmaceutical compositions, methods, and kits for inhibiting the conversion of Amadori compounds to post Amadori advanced glycation endproducts, and for treating and preventing chronic tissue damage and diabetic complication.
摘要翻译：本发明提供新的化合物，药物组合物，方法和试剂盒，用于抑制阿马多利化合物转化为阿马多立后期糖基化终产物，以及治疗和预防慢性组织损伤和糖尿病并发症。

99. 发明授权

US06555700B1 1,3-propane diol esters and ethers and methods for their use in drug delivery 失效
标题翻译： 1,3-丙二醇酯和醚及其用于药物递送的方法
公开(公告)号：US06555700B1
公开(公告)日：2003-04-29
申请号：US08945667
申请日：1998-01-28
申请人： David Frederick Horrobin , Mehar Manku , Austin McMordie , Philip Knowles , Peter Redden , Andrea Pitt , Paul Bradley , Paul Wakefield
发明人： David Frederick Horrobin , Mehar Manku , Austin McMordie , Philip Knowles , Peter Redden , Andrea Pitt , Paul Bradley , Paul Wakefield
IPC分类号： C07C5713
CPC分类号： C07D213/30 , C07C69/007 , C07C69/587 , C07C69/76 , C07D209/28 , C07D213/66 , C07D233/94 , C07D279/36 , C07D321/00 , C07D339/04 , C07D499/00 , C07F9/091 , C07F9/65522 , C07J1/0059 , C07J5/0053
摘要： The invention relates to compounds of formula: wherein R1 is selected from the group consisting of fatty acid acyl groups of 12 to 30 carbon atoms and fatty alcohol groups of 12 to 30 carbon atoms, and wherein R2 is selected from the group consisting of H, fatty acid acyl of 12 to 30 carbon atoms and fatty alcohol groups of 12 to 30 carbon atoms, the same as or different from R1, and the residue of a nutrient, drug, or other bioactive compound, and to the use of these compounds to deliver drugs and other bioactive compounds.
摘要翻译：本发明涉及下式的化合物：其中R1选自12至30个碳原子的脂肪酸酰基和12-30个碳原子的脂肪醇基团，其中R2选自H， 12至30个碳原子的脂肪酸酰基和12至30个碳原子的脂肪醇基团，与R1相同或不同，以及营养物，药物或其它生物活性化合物的残基，以及这些化合物的用途递送药物和其他生物活性化合物。

100. 发明授权

US06436969B1 Dialysis solutions and methods 有权
标题翻译：透析解决方案和方法
公开(公告)号：US06436969B1
公开(公告)日：2002-08-20
申请号：US09544416
申请日：2000-04-06
申请人： Raja Gabriel Khalifah , Billy G. Hudson
发明人： Raja Gabriel Khalifah , Billy G. Hudson
IPC分类号： A61K3144
CPC分类号： G01N33/6842 , A61K31/00 , A61K31/04 , A61K31/435 , A61K31/44 , A61K31/4415 , A61K31/506 , A61K31/675 , A61K38/05 , A61K38/06 , A61K38/07 , A61K45/06 , C07C215/50 , C07D213/66 , C07K5/06034 , C07K5/06052 , C07K5/0812 , G01N33/68 , G01N2400/02 , G01N2500/04
摘要： The present invention provides improved dialysis compositions and methods for dialysis comprising utilizing the disclosed AGE inhibitors, together with methods to reduce dialysis-related complications and disorders.
摘要翻译：本发明提供改进的透析组合物和透析方法，其包括利用所公开的AGE抑制剂以及减少透析相关并发症和病症的方法。

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