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公开(公告)号：US20060014832A1
公开(公告)日：2006-01-19
申请号：US10532836
申请日：2004-04-03
IPC分类号： C07C229/52 , A61K31/24
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，其可被C 1-3烷氧基，氟，氯，溴，碘，硝基，氨基，羟基，氧代，巯基或氘代替。 标记有*（星形）的C原子可以（S）构型或其混合物以（R）构型存在。 本发明的特征在于上述化合物是纯度大于97wt％的游离碱。 本发明还涉及生产高纯度通式（I）化合物的方法及其在制备药物中的用途。
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2.发明授权公开(公告)号：US07670621B2
公开(公告)日：2010-03-02
申请号：US10533683
申请日：2004-04-03
IPC分类号： A61K9/14
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 C1-4alkyl, C3-10cycloalkyl, or phenyl, each of which can be substituted by C1-3alkoxy, 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.
摘要翻译： 本发明涉及一种用于透皮给药式（I）化合物的装置，其中A表示氢或氘，R表示选自C 1-4烷基，C 3-10环烷基或苯基中的基团，其各自可被C1- 3-烷氧基，氟，氯，溴，碘，硝基，氨基，羟基，氧代，巯基或氘，由*（星号）标记的C原子以R构型提供。 本发明的特征在于将通式（I）的化合物提供在聚合物基质中，并通过人皮肤以每天0.5至20mg的剂量释放。 本发明还涉及所述式（I）化合物在制备透皮药物中的用途。
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公开(公告)号：US20090012159A1
公开(公告)日：2009-01-08
申请号：US12141489
申请日：2008-06-18
IPC分类号： A61K31/24 , C07C229/38
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，其可被C 1-3烷氧基取代，氟，氯 ，溴，碘，硝基，氨基，羟基，氧代，巯基或氘。 标记有*（星形）的C原子可以（S）构型或其混合物以（R）构型存在。 本发明的特征在于上述化合物是纯度大于97wt％的游离碱。 本发明还涉及生产高纯度通式（I）化合物的方法及其在制备药物中的用途。
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4.发明申请公开(公告)号：US20060029673A1
公开(公告)日：2006-02-09
申请号：US10533683
申请日：2004-04-03
IPC分类号： A61K9/14
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 C1-4alkyl, C3-10cycloalkyl, 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.
摘要翻译： 本发明涉及一种用于透皮给药式（I）化合物的装置，其中A表示氢或氘，R表示选自C 1-4 - 烷基，C 3-10中的基团 可以被C 1-3烷氧基，氟，氯，溴，碘，硝基，氨基，羟基，氧代，巯基或氘代替的苯基， 以*（星号）标记的C原子被提供在R配置中。 本发明的特征在于将通式（I）的化合物提供在聚合物基质中，并通过人皮肤以每天0.5至20mg的剂量释放。 本发明还涉及所述式（I）化合物在制备透皮药物中的用途。
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公开(公告)号：US07989654B2
公开(公告)日：2011-08-02
申请号：US12141489
申请日：2008-06-18
IPC分类号： C07C69/017
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 characterized 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，其可被C 1-3烷氧基取代，氟，氯 ，溴，碘，硝基，氨基，羟基，氧代，巯基或氘。 标记有*（星形）的C原子可以（S）构型或其混合物以（R）构型存在。 本发明的特征在于上述化合物是纯度大于97wt％的游离碱。 本发明还涉及生产高纯度通式（I）化合物的方法及其在制备药物中的用途。
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公开(公告)号：US07919117B2
公开(公告)日：2011-04-05
申请号：US12417405
申请日：2009-04-02
IPC分类号： A61K9/14
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 C1-4alkyl, C3-10cycloalkyl, or phenyl, each of which can be substituted by C1-3alkoxy, 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.
摘要翻译： 本发明涉及一种用于透皮给药式（I）化合物的装置，其中A表示氢或氘，R表示选自C 1-4烷基，C 3-10环烷基或苯基中的基团，其各自可被C1- 3-烷氧基，氟，氯，溴，碘，硝基，氨基，羟基，氧代，巯基或氘，由*（星号）标记的C原子以R构型提供。 本发明的特征在于将通式（I）的化合物提供在聚合物基质中，并通过人皮肤以每天0.5至20mg的剂量释放。 本发明还涉及所述式（I）化合物在制备透皮药物中的用途。
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公开(公告)号：US09186335B2
公开(公告)日：2015-11-17
申请号：US10523908
申请日：2003-07-29
IPC分类号： A61K9/50 , A61K9/70 , A61K31/381
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.
摘要翻译： 本发明涉及一种含有含有rotigotine的粘合剂层的透皮治疗系统（TTS），其特征在于粘合剂层含有可热熔接触的粘合剂。 本发明还涉及使用罗替戈汀来制造热熔融方法中的TTS的粘合剂层，以及这种TTS的制造方法。
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公开(公告)号：US20050260254A1
公开(公告)日：2005-11-24
申请号：US10523908
申请日：2003-07-29
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) 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.
摘要翻译： 本发明涉及一种含有含有rotigotine的粘合剂层的透皮治疗系统（TTS），其特征在于粘合剂层含有可热熔接触的粘合剂。 本发明还涉及使用罗替戈汀来制造热熔融方法中的TTS的粘合剂层，以及这种TTS的制造方法。
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公开(公告)号：US08211462B2
公开(公告)日：2012-07-03
申请号：US10630633
申请日：2003-07-29
CPC分类号： A61K9/7069 , A61K31/381
摘要： This patent application relates to a transdermal therapeutic system (TTS) that comprises a Rotigotine-containing cement layer, characterized in that the cement layer contains a hot-meltable adhesive in which Rotigotine as the active substance is dispersed and partly or completely dissolved.The patent application further relates to the use of Rotigotine in the production of the cement layer of a TTS by a hot-melt method.
摘要翻译： 本专利申请涉及一种包含含罗替多汀的水泥层的透皮治疗系统（TTS），其特征在于，所述水泥层含有热可熔性粘合剂，其中作为活性物质的罗替戈汀被分散并部分或完全溶解。 该专利申请还涉及使用罗替戈汀通过热熔法生产TTS的水泥层。
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公开(公告)号：US09539206B2
公开(公告)日：2017-01-10
申请号：US14238619
申请日：2012-07-09
CPC分类号： A61K9/0056 , A61K9/006 , A61K9/2095 , A61K9/7007 , A61K47/38
摘要： Method for producing and monitoring oral active ingredient films with a base to which a solution containing at least one active ingredient is applied, the method comprising the steps: • metering and mixing the base formulation, • coating the base formulation onto a substrate, so that a strip results • if necessary, drying the base formulation strip coated on the substrate • printing a colorant solution containing at least one active ingredient onto the upper side of the base formulation strip according to the flexographic printing method, • drying the base formulation strip coated on the substrate together with the printed active ingredient solution, • penetrating the base formulation strip coated on the substrate together with the printed active ingredient solution from the upper and/or lower side by means of radiation from a radiation source, • measuring the transmission of the penetrating radiation by means of at least one reception unit on the opposite side of the base formulation strip coated on the substrate together with the printed active ingredient solution.
摘要翻译： 用于制备和监测含有至少一种活性成分的溶液的基质的口服活性成分膜的方法，所述方法包括以下步骤：·计量和混合所述基础制剂，·将所述基础制剂涂布在基材上，使得 条带结果•如果需要，干燥涂覆在基材上的基础制剂条带•根据柔性版印刷方法将含有至少一种活性成分的着色剂溶液印刷到基底制剂条的上侧上;•将涂布的基础制剂条 与印刷的活性成分溶液一起在基底上;·通过来自辐射源的辐射，从上和/或下侧将印刷的活性成分溶液与印刷的活性成分溶液一起穿透基底制剂条;·测量 穿透辐射借助于在该相对侧的至少一个接收单元 e制剂条带与印刷的活性成分溶液一起涂覆在基材上。
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