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81. 发明授权

US07145036B2 Formoterol tartrate polymorph 有权
公开(公告)号：US07145036B2
公开(公告)日：2006-12-05
申请号：US11052268
申请日：2005-02-07
申请人： Gerald J. Tanoury , Chris H. Senanayake , Donald W. Kessler
发明人： Gerald J. Tanoury , Chris H. Senanayake , Donald W. Kessler
IPC分类号： C07C233/03 , C07C231/20 , A61K31/16
CPC分类号： A61K31/205 , C07B2200/13 , C07C231/24 , C07C233/25 , C07C233/43
摘要： A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.

82. 发明授权

US07105699B2 Treatment of CNS disorders with trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine and its formamide 有权
公开(公告)号：US07105699B2
公开(公告)日：2006-09-12
申请号：US11220891
申请日：2005-09-07
申请人： Thomas P. Jerussi , Qun Kevin Fang , Mark G. Currie
发明人： Thomas P. Jerussi , Qun Kevin Fang , Mark G. Currie
IPC分类号： C07C211/45 , C07C233/15 , A61K31/135 , A61K31/03 , A61K31/165
CPC分类号： C07C211/42 , C07B2200/07 , C07C2602/10 , C07C2602/28
摘要： Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful.

83. 发明授权

US07087623B2 Thiazole and other heterocyclic ligands for mammalian dopamine, muscarinic and serotonin receptors and transporters, and methods of use thereof 有权
公开(公告)号：US07087623B2
公开(公告)日：2006-08-08
申请号：US10786612
申请日：2004-02-25
申请人： Gregory D. Cuny , James R. Hauske , Michele L. R. Heffernan , Joanne M. Holland , Paul E. Persons , Heike Radeke
发明人： Gregory D. Cuny , James R. Hauske , Michele L. R. Heffernan , Joanne M. Holland , Paul E. Persons , Heike Radeke
IPC分类号： A61K31/445 , C07D401/00
CPC分类号： C07D271/07 , C07D277/42 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14
摘要： One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various mammalian cellular receptors, including G-protein coupled receptors. A third aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for mammalian dopamine, muscarinic or serotonin receptors or transporters. Another aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for mammalian dopamine, muscarinic or serotonin receptors. The compounds of the present invention will also find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, Tourette's syndrome, psychiatric disorders, stroke, senile dementia, peptic ulcers, pulmonary obstruction disorders, and asthma.

84. 发明授权

US07071234B2 Methods of treating or preventing erectile dysfunction 失效
标题翻译：治疗或预防勃起功能障碍的方法
公开(公告)号：US07071234B2
公开(公告)日：2006-07-04
申请号：US10395298
申请日：2003-03-25
申请人： Thomas P Jerussi , Chrisantha H. Senanayake , Qun K. Fang
发明人： Thomas P Jerussi , Chrisantha H. Senanayake , Qun K. Fang
IPC分类号： A61K31/136 , A61K31/44
CPC分类号： A61K45/06 , A61K31/11 , A61K31/135 , A61K31/137 , A61K2300/00
摘要： Methods are disclosed for the treatment and prevention of disorders and conditions including, but are not limited to, erectile dysfunction, affective disorders, weight gain, cerebral functional disorders, pain, obsessive-compulsive disorder, substance abuse, chronic disorders, anxiety, eating disorders, migraines, and incontinence. The methods comprise the administration of a dopamine reuptake inhibitor and optionally an additional pharmacologically active compound. Pharmaceutical compositions and dosage forms are also disclosed that comprise a dopamine reuptake inhibitor and optionally an additional pharmacologically active compound. Preferred dopamine reuptake inhibitors are racemic or optically pure sibutramine metabolites and pharmaceutically acceptable salts, solvates, and clathrates thereof. Preferred additional pharmacologically active compounds include drugs that affect the central nervous system, such as 5-HT3 antagonists.
摘要翻译：公开了用于治疗和预防疾病和病症的方法，包括但不限于勃起功能障碍，情感障碍，体重增加，脑功能障碍，疼痛，强迫症，药物滥用，慢性障碍，焦虑，进食障碍，偏头痛和失禁。所述方法包括施用多巴胺再摄取抑制剂和任选的另外的药理活性化合物。还公开了包含多巴胺再摄取抑制剂和任选的另外的药理学活性化合物的药物组合物和剂型。优选的多巴胺再摄取抑制剂是外消旋或光学纯的西布曲明代谢物及其药学上可接受的盐，溶剂化物和包合物。优选的额外的药理活性化合物包括影响中枢神经系统的药物，例如5-HT 3拮抗剂。

85. 发明授权

US07030122B2 1,4-disubstituted piperazine ligands for neurotransmitter receptors 有权
标题翻译：用于神经递质受体的1,4-二取代哌嗪配体
公开(公告)号：US07030122B2
公开(公告)日：2006-04-18
申请号：US10401106
申请日：2003-03-27
申请人： James R. Hauske , Joanne M. Holland , Heike S. Radeke
发明人： James R. Hauske , Joanne M. Holland , Heike S. Radeke
IPC分类号： A61K31/497 , A61K31/4965 , C07D401/12 , C07D241/04
CPC分类号： C07D221/04 , A61K31/495 , C07D221/16 , C07D295/13 , C07D487/04
摘要： One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including serotonin receptors and dopamine receptors. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, Tourette's syndrome, psychiatric disorders, stroke, and senile dementia.
摘要翻译：本发明的一个方面涉及新的杂环化合物。本发明的第二方面涉及新型杂环化合物作为各种细胞受体（包括血清素受体和多巴胺受体）的配体的用途。本发明的化合物可用于治疗多种疾病，疾病，其包括但不限于成瘾，焦虑，抑郁，性功能障碍，高血压，偏头痛，阿尔茨海默病，肥胖，呕吐，精神病，止痛，精神分裂症，帕金森病，不宁腿综合征，睡眠障碍，注意缺陷多动障碍，肠易激综合征，早泄，月经性烦躁综合症，尿失禁，炎性疼痛，神经性疼痛，莱氏阴道炎，威尔逊病，图雷特综合征，精神障碍，中风和老年痴呆。

86. 发明授权

US07018995B2 Carbonate and carbamate modified forms of glucocorticoids 有权
公开(公告)号：US07018995B2
公开(公告)日：2006-03-28
申请号：US10369828
申请日：2003-02-20
申请人： Mark G. Currie , Steve Jones , Paul Grover , Chris H. Senanayake , Q. Kevin Fang
发明人： Mark G. Currie , Steve Jones , Paul Grover , Chris H. Senanayake , Q. Kevin Fang
IPC分类号： A61K31/573 , C07J5/00 , C07J71/00
CPC分类号： C07J71/0031 , A61K31/58 , C07J5/0076 , C07J5/0092 , C07J41/0033 , A61K2300/00
摘要： Carbonates and carbamates of the formula and related steroid carbonates and carbamates are disclosed. The compounds are useful for treating rhinitis and asthma, particularly by inhalation, and for treating inflammation, particularly by local or topical administration.

87. 发明授权

US06974838B2 Methods of treating or preventing pain using sibutramine metabolites 有权
标题翻译：使用西布曲明代谢物治疗或预防疼痛的方法
公开(公告)号：US06974838B2
公开(公告)日：2005-12-13
申请号：US10806415
申请日：2004-03-23
申请人： Chrisantha Hugh Senanayake , Qun Kevin Fang , Zhengxu Han , Dhileepkumar Krishnamurthy
发明人： Chrisantha Hugh Senanayake , Qun Kevin Fang , Zhengxu Han , Dhileepkumar Krishnamurthy
IPC分类号： A61B6/00 , A61B6/02 , A61K31/11 , A61K31/135 , A61K31/137 , A61K45/06 , A61K31/22
CPC分类号： A61K45/06 , A61K31/11 , A61K31/135 , Y02A50/401 , A61K2300/00
摘要： Methods of making and using racemic and optically pure metabolites of sibutramine, and pharmaceutically acceptable salts, solvates, and clathrates thereof, are disclosed. Pharmaceutical compositions and dosage forms are also disclosed which comprise a dopamine reuptake inhibitor, such as a racemic or optically pure sibutramine metabolite, and optionally an additional pharmacologically active compound.
摘要翻译：公开了制备和使用西布曲明的外消旋和光学纯的代谢物及其药学上可接受的盐，溶剂合物和笼形物的方法。还公开了药物组合物和剂型，其包含多巴胺再摄取抑制剂，例如外消旋或光学纯的西布曲明代谢物，以及任选的另外的药理活性化合物。

88. 发明申请

US20050222211A1 S(-)rabeprazole compositions and methods 审中-公开
标题翻译： S（ - ）雷贝拉唑组合物和方法
公开(公告)号：US20050222211A1
公开(公告)日：2005-10-06
申请号：US11140675
申请日：2005-05-27
申请人： Patrick Koch , Paul Rubin , William Yelle
发明人： Patrick Koch , Paul Rubin , William Yelle
IPC分类号： A61K9/20 , A61K9/48 , A61K31/00 , A61K31/4439 , A61P1/04 , A61P17/06
CPC分类号： A61K31/4439 , A61K31/00
摘要： Methods and compositions are disclosed utilizing optically pure S(−)rabeprazole for the treatment of ulcers in humans while substantially reducing the concomitant liability of adverse effects associated with the racemic mixture of rabeprazole. The optically pure S(−) isomer is also useful for the treatment of gastroesophageal reflux. S(−)rabeprazole is an inhibitor of H+ release and is therefore useful in the treatment of other conditions related to gastric hypersecretion such as Zollinger-Ellison Syndrome.
摘要翻译：公开了使用光学纯的S（ - ）雷贝拉唑治疗人体溃疡的方法和组合物，同时显着减少与雷贝拉唑的外消旋混合物相关的副作用的伴随的责任。光学纯的S（ - ）异构体也可用于治疗胃食管反流。 S（ - ）雷贝拉唑是一种H +抑制剂，因此可用于治疗与胃分泌异常有关的其他病症，如Zollinger-Ellison综合征。

89. 发明授权

US06946477B2 3-Substituted piperidines comprising urea functionality, and methods of use thereof 有权
标题翻译： 3-取代的包含脲官能团的哌啶及其使用方法
公开(公告)号：US06946477B2
公开(公告)日：2005-09-20
申请号：US10289121
申请日：2002-11-05
申请人： Brian M. Aquila , Gregory D. Cuny , James R. Hauske , Liming Shao , Xinhe Wu
发明人： Brian M. Aquila , Gregory D. Cuny , James R. Hauske , Liming Shao , Xinhe Wu
IPC分类号： C07D211/26 , C07D211/60 , C07D401/04 , C07D401/06 , C07D211/20 , C07D277/04 , C07D277/18 , A51K31/445
CPC分类号： C07D401/04 , C07D211/26 , C07D211/60 , C07D401/06
摘要： One aspect of the present invention relates to novel heterocyclic compounds comprising urea functionality. A second aspect of the present invention relates to the use of the novel heterocyclic compounds comprising urea functionality as ligands for various cellular receptors, including opioid receptors, other G-protein-coupled receptors and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds comprising urea functionality as analgesics.
摘要翻译：本发明的一个方面涉及包含脲官能团的新型杂环化合物。本发明的第二方面涉及包含尿素官能团的新型杂环化合物在各种细胞受体（包括阿片受体，其他G蛋白偶联受体和离子通道）的配体中的用途。本发明的另一方面涉及包含尿素官能团的新型杂环化合物作为止痛剂的用途。

90. 发明申请

US20050197392A1 O-desmethylvenlafaxine and methods of preparing and using the same 审中-公开
标题翻译： O-去甲基文拉法新及其制备和使用方法
公开(公告)号：US20050197392A1
公开(公告)日：2005-09-08
申请号：US11091518
申请日：2005-03-29
申请人： Thomas Jerussi , Chrisantha Senanayake
发明人： Thomas Jerussi , Chrisantha Senanayake
IPC分类号： A61K9/20 , A61K9/48 , A61K31/135 , A61K31/137 , A61K47/12 , A61K47/26 , A61K47/38 , A61P3/04 , A61P15/10 , A61P23/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07C209/50 , C07C215/46 , C07C215/64 , C07C217/14 , C07C217/74 , C07C231/02 , C07C233/18 , C07C235/34 , C07C255/36 , C07C255/37 , C07D295/192 , A61K31/277
CPC分类号： C07D295/192 , A61K9/2054 , A61K9/2059 , A61K9/4866 , A61K31/135 , C07C215/64 , C07C217/74 , C07C233/18 , C07C255/36 , C07C255/37 , C07C2601/14
摘要： Methods of preparing, and compositions comprising, derivatives of venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders, obesity and weight gain, incontinence, dementia and related disorders.
摘要翻译：公开了制备方法和包含文拉法辛衍生物的组合物。还公开了治疗和预防疾病和病症的方法，包括但不限于情感障碍如抑郁，双相和躁狂症，注意力缺陷障碍，具有多动症的注意缺陷障碍，帕金森病，癫痫，脑功能障碍，肥胖症和体重增加，失禁，痴呆和相关疾病。

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