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91. 发明申请

US20140051768A1 METHOD OF TREATING DISEASES THAT RESPOND TO THERAPY BY DOPAMINE OR DOPAMINE AGONISTS 有权
标题翻译：治疗多巴胺或多巴胺激素治疗疾病的方法
公开(公告)号：US20140051768A1
公开(公告)日：2014-02-20
申请号：US14063821
申请日：2013-10-25
申请人： UCB Pharma GmbH
发明人： Dieter Scheller , Klaus Hansen
IPC分类号： C07C219/26
CPC分类号： C07C219/26 , A61K31/135
摘要： The invention relates to a medicament containing (S)-2-N-propylamino-5-hydroxytetralin, the salts or prodrugs thereof. As a D3 agonist, (S)-2-N-propylamino-5-hydroxytetralin is suitable particularly for the treatment of dopa-sensitive movement disorders.
摘要翻译：本发明涉及含有（S）-2-N-丙基氨基-5-羟基四氢萘酮的药物，其盐或前药。作为D3激动剂，（S）-2-N-丙基氨基-5-羟基四氢萘酮特别适用于治疗多巴敏感性运动障碍。

92. 发明授权

US08609641B2 (S)-2-N-propylamino-5-hydroxytetralin as a D3-agonist 有权
标题翻译：（S）-2-N-丙基氨基-5-羟基四氢化萘作为D3-激动剂
公开(公告)号：US08609641B2
公开(公告)日：2013-12-17
申请号：US10587637
申请日：2004-12-13
申请人： Dieter Scheller , Klaus Hansen
发明人： Dieter Scheller , Klaus Hansen
IPC分类号： A61K31/66 , A61K31/27 , A61K31/255 , A61K31/185 , A61K31/135
CPC分类号： C07C219/26 , A61K31/135
摘要： The invention relates to a medicament containing (S)-2-N-propylamino-5-hydroxytetralin, the salts or prodrugs thereof. As a D3 agonist, (S)-2-N-propylamino-5-hydroxytetralin is suitable particularly for the treatment of dopa-sensitive movement disorders.
摘要翻译：本发明涉及含有（S）-2-N-丙基氨基-5-羟基四氢萘酮的药物，其盐或前药。作为D3激动剂，（S）-2-N-丙基氨基-5-羟基色烯特别适用于治疗多巴敏感性运动障碍。

93. 发明授权

US08545872B2 Device for the transdermal administration of a rotigotine base 有权
标题翻译：用于透皮给药罗替戈汀碱的装置
公开(公告)号：US08545872B2
公开(公告)日：2013-10-01
申请号：US13020414
申请日：2011-02-03
申请人： Armin Breitenbach
发明人： Armin Breitenbach
IPC分类号： A61K31/381 , A61K9/70
CPC分类号： A61K9/7069 , A61K31/381
摘要： The invention relates to a polymer matrix suitable for the transdermal administration of rotigotine [(−)-5, 6, 7, 8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-1-naphtol], containing a matrix for the transdermal administration of rotigotine [(−)-5, 6, 7, 8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-1 naphtol], containing a matrix polymer which is supersaturated with a rotigotine base. Said polymer matrix is characterised in that the part of the rotigotine which is not dissolved in the matrix polymer is dispersed in the matrix polymer as amorphous particles having a maximum mean diameter of 30 μm, and the matrix is free of solubilisers, crystallisation inhibitors and dispersants. The invention also relates to a flat device for the transdermal administration of rotigotine, containing the above-mentioned, preferably silicon-based polymer matrix which is supersaturated with rotigotine, and a rear layer which is impermeable to the active ingredient.
摘要翻译：本发明涉及适用于透皮给药罗替戈汀[（ - ） - 5,6,7,8-四氢-6- [丙基[2-（2-噻吩基）乙基]氨基] -1-萘酚]的聚合物基质，，其含有用于透皮给药罗替戈汀[（ - ）] -5,6,7,8-四氢-6- [丙基[2-（2-噻吩基）乙基]氨基] -1萘酚]的基质，其含有基质聚合物其用罗替戈汀碱过饱和。所述聚合物基质的特征在于，不溶于基体聚合物的罗替戈汀的部分以最大平均直径为30μm的无定形颗粒分散在基质聚合物中，并且基质不含增溶剂，结晶抑制剂和分散剂。本发明还涉及一种用于透皮给药罗替戈汀的扁平装置，其包含上述优选的硅基聚合物基质，该基质用罗替戈汀过饱和，并且对于活性成分是不可渗透的后层。

94. 发明申请

US20130102794A1 Novel Process for the Preparation of Nitrogen Substituted Aminotetralins Derivatives 有权
标题翻译：制备氮取代的氨基四氢萘衍生物的新方法
公开(公告)号：US20130102794A1
公开(公告)日：2013-04-25
申请号：US13806378
申请日：2011-06-24
申请人： Celal Ates , Arnaud Schule , Magali Palacio , Paul Deutsch , David Vasselin , Nicolas Carly , Ganesh Phadtare , Swapnil Yerande , Jean-Pierre Delatinne , Maria Luisa Escudero Hernandez , Veronique Pinilla
发明人： Celal Ates , Arnaud Schule , Magali Palacio , Paul Deutsch , David Vasselin , Nicolas Carly , Ganesh Phadtare , Swapnil Yerande , Jean-Pierre Delatinne , Maria Luisa Escudero Hernandez , Veronique Pinilla
IPC分类号： C07C213/10 , C07C271/02 , C07C269/08 , C07C217/52 , C07D333/20
CPC分类号： C07C213/10 , C07B57/00 , C07B2200/07 , C07C51/353 , C07C51/412 , C07C213/00 , C07C213/08 , C07C217/52 , C07C217/54 , C07C269/08 , C07C271/02 , C07C271/24 , C07C2602/10 , C07D333/20 , C07C59/48 , C07C59/56 , C07C59/64 , C07C215/46
摘要： The present invention provides an alternative synthesis of N-substituted aminotetralines comprising resolution of N-substituted aminotetralins of formula (II), wherein R1, R2 and R3 are as defined for compound of formula (I).
摘要翻译：本发明提供了N-取代的氨基四氢化萘的替代合成方法，其包括拆分式（II）的N-取代的氨基四氢化萘，其中R 1，R 2和R 3如式（I）化合物所定义。

95. 发明授权

US08246979B2 Transdermal delivery system for the administration of rotigotine 有权
标题翻译：用于给予罗替戈汀的透皮递送系统
公开(公告)号：US08246979B2
公开(公告)日：2012-08-21
申请号：US10623864
申请日：2003-07-22
申请人： Dietrich Wilhelm Schacht , Mike Hannay , Hans-Michael Wolff
发明人： Dietrich Wilhelm Schacht , Mike Hannay , Hans-Michael Wolff
IPC分类号： A61F13/00 , A61F13/02 , A61K9/70 , A61L15/16
CPC分类号： A61K9/7061 , A61K9/7069 , A61K9/7076 , A61K31/38
摘要： An improved transdermal delivery system (TDS) comprises a self-adhesive matrix comprising a solid or semi-solid semi-permeable polymer which contains rotigotine in its free base form as a multitude of microreservoirs within the matrix. The self-adhesive matrix is highly permeable to the free base of rotigotine and is impermeable to the protonated form of rotigotine.
摘要翻译：改进的透皮递送系统（TDS）包括自粘性基质，其包含固体或半固体半透性聚合物，其在游离碱形式中含有作为基质内的多个微储层的罗替戈汀。自粘基质对罗替戈汀的游离碱是高度可渗透的，并且对于质子化形式的罗替戈汀是不可渗透的。

96. 发明授权

US08232414B2 Polymorphic form of rotigotine and process for production 有权
标题翻译：罗替戈汀的多晶型和生产工艺
公开(公告)号：US08232414B2
公开(公告)日：2012-07-31
申请号：US12324166
申请日：2008-11-26
申请人： Hans-Michael Wolff , Luc Quere , Jens Riedner
发明人： Hans-Michael Wolff , Luc Quere , Jens Riedner
IPC分类号： C07D333/20
CPC分类号： C07D333/20
摘要： The present invention relates to a novel polymorphic form of rotigotine characterized by at least one of the following powder X-ray diffraction peaks: 12.04, 13.68, 17.72 and 19.01±0.2 (° 2θ), measured with a Cu—Kα irradiation (1.54060 Å), and a process for production thereof, which is useful for the manufacture of a stable medicament for treating or alleviating symptoms of Parkinson's disease and other dopamine-related disorders.
摘要翻译：本发明涉及一种新型多晶型罗替戈汀，其特征在于以Cu-Kα辐射（1.54060）测量的以下粉末X射线衍射峰中的至少一种：12.04,13.68,17.72和19.01±0.2（°2） Å）及其生产方法，其可用于制备用于治疗或缓解帕金森病和其他多巴胺相关疾病症状的稳定药物。

97. 发明授权

US08053476B2 Method for treating peripheral neuropathic pain 失效
标题翻译：治疗周围神经性疼痛的方法
公开(公告)号：US08053476B2
公开(公告)日：2011-11-08
申请号：US11507110
申请日：2006-08-21
申请人： Norma Selve
发明人： Norma Selve
IPC分类号： A61K31/16 , A61K31/165 , C07C229/38
CPC分类号： A61K31/198 , A61K31/165 , A61K31/445 , A61K31/535
摘要： The present invention concerns the use of compounds of the Formula (I) for treating different types of acute and chronic pain, especially non neuropathic inflammatory pain in mammals. The pain to be treated may be e.g. chronic inflammatory pain, rheumatoid arthritis pain and/or secondary inflammatory osteoarthritic pain. The compounds show an antinociceptive profile and differ from classical analgesics like opioids and non-steroidal anti-inflammatory drugs (NSAIDs) and are useful as specific analgesics.
摘要翻译：本发明涉及式（I）化合物用于治疗哺乳动物中急性和慢性疼痛，特别是非神经性炎性疼痛的不同类型和症状。待治疗的疼痛可以是例如慢性炎性疼痛，类风湿性关节炎疼痛和/或继发性炎性骨关节炎疼痛。这些化合物显示抗感受伤害特征，并且与古典镇痛药（如阿片样物质和非甾体抗炎药物（NSAID））不同，可用作特定止痛剂。

98. 发明授权

US07982058B2 Chiral intermediate, process for producing the same and its use in the manufacture of tolterodine, fesoterodine, or the active metabolite thereof 有权
标题翻译：手性中间体，其制备方法及其在制备托特罗定，非索罗定或其活性代谢物中的用途
公开(公告)号：US07982058B2
公开(公告)日：2011-07-19
申请号：US12304323
申请日：2007-06-06
申请人： Claus Meese
发明人： Claus Meese
IPC分类号： C07D311/00
CPC分类号： C07D311/20 , A61K31/222 , C07C213/00 , C07C227/12 , C07C215/54 , C07C219/28
摘要： The compound of formula (I): is provided. It may be produced by subjecting a compound of formula (IV) to a reduction reaction wherein R represents hydrogen, straight or branched C1-C6 alkyl. This compound is a valuable intermediate which may be used in the synthesis of fesoterodine, tolterodine, its active metabolite, and related compounds.
摘要翻译：提供式（I）化合物。其可以通过使式（IV）的化合物进行还原反应来制备，其中R表示氢，直链或支链C 1 -C 6烷基。该化合物是一种有价值的中间体，可用于合成非索特罗定，托特罗定及其活性代谢物和相关化合物。

99. 发明申请

US20110165247A1 DEVICE FOR THE TRANSDERMAL ADMINISTRATION OF A ROTIGOTINE BASE 有权
标题翻译：转基因基因的转录管理设备
公开(公告)号：US20110165247A1
公开(公告)日：2011-07-07
申请号：US13020414
申请日：2011-02-03
申请人： Armin Breitenbach
发明人： Armin Breitenbach
IPC分类号： A61K31/381 , A61K9/10 , A61P25/24 , A61P25/16 , A61P25/14
CPC分类号： A61K9/7069 , A61K31/381
摘要： The invention relates to a polymer matrix suitable for the transdermal administration of rotigotine [(−)-5, 6, 7, 8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-1-naphtol], containing a matrix for the transdermal administration of rotigotine [(−)-5, 6, 7, 8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-1 naphtol], containing a matrix polymer which is supersaturated with a rotigotine base. Said polymer matrix is characterised in that the part of the rotigotine which is not dissolved in the matrix polymer is dispersed in the matrix polymer as amorphous particles having a maximum mean diameter of 30 ?m, and the matrix is free of solubilisers, crystallisation inhibitors and dispersants. The invention also relates to a flat device for the transdermal administration of rotigotine, containing the above-mentioned, preferably silicon-based polymer matrix which is supersaturated with rotigotine, and a rear layer which is impermeable to the active ingredient.
摘要翻译：本发明涉及适用于透皮给药罗替戈汀[（ - ） - 5,6,7,8-四氢-6- [丙基[2-（2-噻吩基）乙基]氨基] -1-萘酚]的聚合物基质，，其含有用于透皮给药罗替戈汀[（ - ）] -5,6,7,8-四氢-6- [丙基[2-（2-噻吩基）乙基]氨基] -1萘酚]的基质，其含有基质聚合物其用罗替戈汀碱过饱和。所述聚合物基质的特征在于，不溶于基质聚合物的罗替戈汀的部分以最大平均直径为30μm的无定形颗粒分散在基质聚合物中，并且基质不含增溶剂，结晶抑制剂和分散剂。本发明还涉及一种用于透皮给药罗替戈汀的扁平装置，其包含上述优选的硅基聚合物基质，该基质用罗替戈汀过饱和，并且对于活性成分是不可渗透的后层。

100. 发明申请

US20110130350A1 SYNTHESIS SCHEME FOR LACOSAMIDE 有权
标题翻译： LACOSAMIDE的合成方案
公开(公告)号：US20110130350A1
公开(公告)日：2011-06-02
申请号：US12961705
申请日：2010-12-07
申请人： Jens Riedner , Gavin Dunne
发明人： Jens Riedner , Gavin Dunne
IPC分类号： A61K38/05 , C07C231/14 , C07C231/24 , C07C231/10 , C07C227/16
CPC分类号： C07C231/02 , C07C273/1809 , C07C273/1854 , C07C275/10 , C07C275/16 , Y02P20/55 , C07C235/06
摘要： The present invention is concerned with an improved method of producing (R)-2-acetamido-N-benzyl-3-methoxypropionamide (lacosamide) comprising the 0-methylation of a compound of formula (I) to produce a compound of formula (II) in a single step reaction.
摘要翻译：本发明涉及一种制备（R）-2-乙酰氨基-N-苄基-3-甲氧基丙酰胺（lacosamide）的改进方法，其包括式（I）化合物的O-甲基化以产生式（II）化合物）在一步反应。

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