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1.发明授权
公开(公告)号：EP1530461B1
公开(公告)日：2007-10-03
申请号：EP04725614.4
申请日：2004-04-03
申请人： SCHWARZ PHARMA AG
IPC分类号： A61K9/70 , A61K31/403 , C07C219/26
CPC分类号： A61K9/7053 , A61K31/403
摘要： The invention relates to a device for transdermally administering a compound of formula (I), wherein A represents hydrogen or deuterium, R represents a group selected among C1-6 alkyl, C3-10 cycloalkyl, or phenyl, each of which can be substituted by C1-3 alkoxy, fluoride, chlorine, bromine, iodine, nitro, amino, hydroxy, oxo, mercapto, or deuterium, the C atom marked by * (asterisk) being provided in the R configuration. The invention is characterized in that the compound of general formula (I) is provided in a polymer matrix and is released at a dose of 0.5 to 20 mg per day through human skin. The invention further relates to the use of said compounds of formula (I) for producing transdermal medicaments.
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2.发明授权PHARMAZEUTISCHE FORMULIERUNGEN ENTHALTEND HOCHREINE BASEN VON 3,3-DIPHENYLPROPYLAMINMONOESTERN 有权化合物制剂中烯雌酚烯雌酮3,3-二苯基丙氨基甲酸酯
公开(公告)号：EP1613584B1
公开(公告)日：2007-11-21
申请号：EP04725610.2
申请日：2004-04-03
申请人： SCHWARZ PHARMA AG
IPC分类号： C07C217/62 , A61K31/135 , C07C213/10 , A61P13/00
CPC分类号： C07C219/28 , A61K9/7053 , A61K31/135
摘要： The invention relates to a compound of general formula (I) wherein A represents deuterium or hydrogen, R represents a group selected from C1-6 alkyl, C3-10 cycloalkyl or phenyl, which can be substituted by C1-3 alkoxy, fluorine, chlorine, bromine, iodine, nitro, amino, hydroxyl, oxo, mercapto or deuterium. The C atom marked with a * (star) can be present in an (R) configuration, in an (S)-configuration or a mixture thereof. The invention is characterised in that the above-mentioned compounds are free bases with a degree of purity of more than 97 wt %. The invention also relates to a method for the production of highly pure compounds of general formula (I) and to the use thereof in the production of medicaments.
摘要翻译： 本发明涉及通式（I）的化合物，其中A表示氘或氢，R表示选自C 1-6烷基，C 3-10环烷基或苯基的基团，其可以被C 1-3烷氧基，氟，氯 ，溴，碘，硝基，氨基，羟基，氧代，巯基或氘。 标有*（星号）的C原子可以以（R）构型，（S）构型或其混合物存在。 本发明的特征在于上述化合物是纯度大于97重量％的游离碱。 本发明还涉及通式（I）的高纯化合物的生产方法及其在药物生产中的用途。
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公开(公告)号：EP1492517B1
公开(公告)日：2006-05-03
申请号：EP03750403.2
申请日：2003-07-29
申请人： SCHWARZ PHARMA AG
IPC分类号： A61K9/70 , A61K31/381
CPC分类号： A61K9/7069 , A61K31/381
摘要： The invention relates to a transdermal therapeutic system (TTS) containing a rotigotine-containing adhesive layer, which is characterized by the fact that the adhesive layer contains a hot-meltable contact adhesive. The invention also relates to the use of rotigotine for producing the adhesive layer of a TTS in a hot melt method.
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4.发明公开
公开(公告)号：EP1530461A1
公开(公告)日：2005-05-18
申请号：EP04725614.4
申请日：2004-04-03
申请人： SCHWARZ PHARMA AG
IPC分类号： A61K9/70 , A61K31/403 , C07C219/26
CPC分类号： A61K9/7053 , A61K31/403
摘要： The invention relates to a device for transdermally administering a compound of formula (I), wherein A represents hydrogen or deuterium, R represents a group selected among C1-6 alkyl, C3-10 cycloalkyl, or phenyl, each of which can be substituted by C1-3 alkoxy, fluoride, chlorine, bromine, iodine, nitro, amino, hydroxy, oxo, mercapto, or deuterium, the C atom marked by * (asterisk) being provided in the R configuration. The invention is characterized in that the compound of general formula (I) is provided in a polymer matrix and is released at a dose of 0.5 to 20 mg per day through human skin. The invention further relates to the use of said compounds of formula (I) for producing transdermal medicaments.
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公开(公告)号：EP1490052B1
公开(公告)日：2007-05-30
申请号：EP03789421.9
申请日：2003-12-24
申请人： SCHWARZ PHARMA AG
发明人： BREITENBACH, Armin
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]-1naphtol], 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 ñm, 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.
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公开(公告)号：EP1613584A1
公开(公告)日：2006-01-11
申请号：EP04725610.2
申请日：2004-04-03
申请人： SCHWARZ PHARMA AG
IPC分类号： C07C217/62 , A61K31/135 , C07C213/10 , A61P13/00
CPC分类号： C07C219/28 , A61K9/7053 , A61K31/135
摘要： The invention relates to a compound of general formula (I) wherein A represents deuterium or hydrogen, R represents a group selected from C1-6 alkyl, C3-10 cycloalkyl or phenyl, which can be substituted by C1-3 alkoxy, fluorine, chlorine, bromine, iodine, nitro, amino, hydroxyl, oxo, mercapto or deuterium. The C atom marked with a * (star) can be present in an (R) configuration, in an (S)-configuration or a mixture thereof. The invention is characterised in that the above-mentioned compounds are free bases with a degree of purity of more than 97 wt %. The invention also relates to a method for the production of highly pure compounds of general formula (I) and to the use thereof in the production of medicaments.
摘要翻译： 本发明涉及通式（I）的化合物，其中A表示氘或氢，R表示选自C 1-6烷基，C 3-10环烷基或苯基的基团，其可以被C 1-3烷氧基，氟，氯 ，溴，碘，硝基，氨基，羟基，氧代，巯基或氘。 标有*（星号）的C原子可以以（R）构型，（S）构型或其混合物存在。 本发明的特征在于上述化合物是纯度大于97重量％的游离碱。 本发明还涉及通式（I）的高纯化合物的生产方法及其在药物生产中的用途。
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公开(公告)号：EP1492517A2
公开(公告)日：2005-01-05
申请号：EP03750403.2
申请日：2003-07-29
申请人： SCHWARZ PHARMA AG
IPC分类号： A61K31/00
CPC分类号： A61K9/7069 , A61K31/381
摘要： The invention relates to a transdermal therapeutic system (TTS) which contains a rotigotine-containing adhesive layer and is characterized by the fact that the adhesive layer contains a hot-meltable contact adhesive. The invention also relates to the use of rotigotine for producing the adhesive layer of a TTS in a hot melt method, and a method for producing such a TTS.
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公开(公告)号：EP1490052A1
公开(公告)日：2004-12-29
申请号：EP03789421.9
申请日：2003-12-24
申请人： SCHWARZ PHARMA AG
发明人： BREITENBACH, Armin
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]-1naphtol], 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.
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