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1. 发明申请

US20090023757A1 PROCESS FOR PREPARING BICYCLIC COMPOUNDS 审中-公开
标题翻译：制备双相化合物的方法
公开(公告)号：US20090023757A1
公开(公告)日：2009-01-22
申请号：US11910990
申请日：2006-04-06
申请人： Daniele Andreotti , Sergio Bacchi , Monica Delpogetto , Simone Guelfi , Alcide Perboni , Arianna Ribecai , Simone Spada , Paolo Stabile , Marsia Tampieri
发明人： Daniele Andreotti , Sergio Bacchi , Monica Delpogetto , Simone Guelfi , Alcide Perboni , Arianna Ribecai , Simone Spada , Paolo Stabile , Marsia Tampieri
IPC分类号： A61K31/519 , C07D471/04 , A61P1/00 , C07D207/14
CPC分类号： C07D471/04 , C07D207/22
摘要： The present invention relates to a novel process for preparing compounds of formula (IA), which are potent and specific antagonists of corticotropin-releasing factor (CRF) receptors, from intermediate compounds of formula (I), by a coupling reaction catalysed by copper.
摘要翻译：本发明涉及通过由铜催化的偶联反应制备式（I）的中间体化合物来制备作为促肾上腺皮质激素释放因子（CRF）受体的有效和特异性拮抗剂的式（IA）化合物的新方法。

2. 发明申请

US20080312444A1 Process for Preparing Bicyclic Compounds 审中-公开
标题翻译：双环化合物的制备方法
公开(公告)号：US20080312444A1
公开(公告)日：2008-12-18
申请号：US11910985
申请日：2006-04-06
申请人： Sergio Bacchi , Monica Delpogetto , Simone Guelfi , Alcide Perboni , Arianna Ribecai , Paolo Stabile , Marsia Tampieri
发明人： Sergio Bacchi , Monica Delpogetto , Simone Guelfi , Alcide Perboni , Arianna Ribecai , Paolo Stabile , Marsia Tampieri
IPC分类号： C07D471/04 , C07D207/22
CPC分类号： C07D471/04 , C07D207/22
摘要： The present invention relates to a novel process for preparing compounds of formula (IA), which are potent and specific antagonists of corticotropin-releasing factor (CRF) receptors, from intermediate compounds of formula (I), by a coupling reaction catalysed by copper.
摘要翻译：本发明涉及通过由铜催化的偶联反应制备式（I）的中间体化合物来制备作为促肾上腺皮质激素释放因子（CRF）受体的有效和特异性拮抗剂的式（IA）化合物的新方法。

3. 发明申请

US20070232808A1 PROCESS FOR PREPARING HETEROCYCLIC DERIVATIVES 审中-公开
标题翻译：制备杂环衍生物的方法
公开(公告)号：US20070232808A1
公开(公告)日：2007-10-04
申请号：US11693757
申请日：2007-03-30
申请人： Sergio Bacchi
发明人： Sergio Bacchi
IPC分类号： C07D417/02 , C07D403/04
CPC分类号： C07D403/04 , C07D401/04 , C07D413/04 , C07D417/04
摘要： The present invention relates to a novel process, useful for preparing key intermediates of formula (I) in the synthesis of various compounds, among them compounds which are potent and specific antagonists of D3 receptors, in which X may be Nitrogen or Sulfur; Het means aryl or heteroaryl; each of which may be substituted by 1 to 4 groups J selected from: halogen, C1-C6 alkyl C1-C6 alkoxy, halo C1-C6 alkyl C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, —C(O)R1, nitro, hydroxy, —NR2R3, cyano or a group Z; R1 is a C1-C4 alkyl —OR3 or —NR3R4; R2 is hydrogen or C1-C6 alkyl; R3 is hydrogen or C1-C6 alkyl; R is H, C1-C6 alkyl aryl, benzyl; each of which may be substituted by 1 to 4 groups J; according to the following Scheme 1: in which step a means a reaction in basic conditions of compounds (IIA) with 3-thiosemicarbazide derivatives, followed by a treatment with an inorganic base and n-propane phosphonic cyclic anhydride and final pH adjustment with inorganic acids to give compounds of formula (II).
摘要翻译：本发明涉及用于制备各种化合物的合成中的式（I）的关键中间体的新方法，其中X是可以是氮或硫的D3受体的有效和特异性拮抗剂的化合物; Het表示芳基或杂芳基; 它们各自可以被1至4个选自以下的基团取代：卤素，C 1 -C 6烷基C 1 -C 6烷氧基，卤代C 1 -C 6烷基C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，-C（ O）R 1，硝基，羟基，-NR 2 R 3，氰基或基团Z; R 1是C 1 -C 4烷基-OR 3或-NR 3 R 4; R 2是氢或C 1 -C 6烷基; R 3是氢或C 1 -C 6烷基; R为H，C 1 -C 6烷基芳基，苄基; 其中每个可以被1至4个基团J取代; 根据以下方案1：其中步骤a表示化合物（IIA）与3-硫代氨基脲衍生物在碱性条件下的反应，然后用无机碱和正丙烷膦酸环状酸酐处理，并用无机酸进行最终pH调节得到式（II）的化合物。

4. 发明授权

US07838680B2 Process for preparing heterocyclic derivatives 有权
标题翻译：制备杂环衍生物的方法
公开(公告)号：US07838680B2
公开(公告)日：2010-11-23
申请号：US12608184
申请日：2009-10-29
申请人： Sergio Bacchi
发明人： Sergio Bacchi
IPC分类号： C07D417/02
CPC分类号： C07D403/04 , C07D401/04 , C07D413/04 , C07D417/04
摘要： The present invention relates to a novel process, useful for preparing key intermediates of formula (I) in the synthesis of various compounds, among them compounds which are potent and specific antagonists of D3 receptors, in which X may be Nitrogen or Sulfur; Het means aryl or heteroaryl; each of which may be substituted by 1 to 4 groups J selected from: halogen, C1-C6 alkyl C1-C6 alkoxy, halo C1-C6 alkyl C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, —C(O)R1, nitro, hydroxy, —NR2R3, cyano or a group Z; R1 is a C1-C4 alkyl —OR3 or —NR3R4; R2 is hydrogen or C1-C6 alkyl; R3 is hydrogen or C1-C6 alkyl; R is H, C1-C6 alkyl aryl, benzyl; each of which may be substituted by 1 to 4 groups J; according to the following Scheme 1: in which step a means a reaction in basic conditions of compounds (IIA) with 3-thiosemicarbazide derivatives, followed by a treatment with an inorganic base and n-propane phosphonic cyclic anhydride and final pH adjustment with inorganic acids to give compounds of formula (II).
摘要翻译：本发明涉及用于制备各种化合物的合成中的式（I）的关键中间体的新方法，其中X是可以是氮或硫的D3受体的有效和特异性拮抗剂的化合物; Het表示芳基或杂芳基; 它们各自可以被1至4个选自以下的基团取代：卤素，C 1 -C 6烷基C 1 -C 6烷氧基，卤代C 1 -C 6烷基C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，-C（ O）R 1，硝基，羟基，-NR 2 R 3，氰基或基团Z; R1是C1-C4烷基-OR3或-NR3R4; R2是氢或C1-C6烷基; R3是氢或C1-C6烷基; R为H，C 1 -C 6烷基芳基，苄基; 其中每个可以被1至4个基团J取代; 根据以下方案1：其中步骤a表示化合物（IIA）与3-硫代氨基脲衍生物在碱性条件下的反应，然后用无机碱和正丙烷膦酸环状酸酐处理，并用无机酸进行最终pH调节得到式（II）的化合物。

5. 发明申请

US20100048895A1 Process for Preparing Heterocyclic Derivatives 有权
标题翻译：制备杂环衍生物的方法
公开(公告)号：US20100048895A1
公开(公告)日：2010-02-25
申请号：US12608184
申请日：2009-10-29
申请人： Sergio Bacchi
发明人： Sergio Bacchi
IPC分类号： C07D403/04 , C07D263/30 , C07D277/04 , C07D401/04
CPC分类号： C07D403/04 , C07D401/04 , C07D413/04 , C07D417/04
摘要： The present invention relates to a novel process, useful for preparing key intermediates of formula (I) in the synthesis of various compounds, among them compounds which are potent and specific antagonists of D3 receptors, in which X may be Nitrogen or Sulfur; Het means aryl or heteroaryl; each of which may be substituted by 1 to 4 groups J selected from: halogen, C1-C6 alkyl C1-C6 alkoxy, halo C1-C6 alkyl C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, —C(O)R1, nitro, hydroxy, —NR2R3, cyano or a group Z; R1 is a C1-C4 alkyl —OR3 or —NR3R4; R2 is hydrogen or C1-C6 alkyl; R3 is hydrogen or C1-C6 alkyl; R is H, C1-C6 alkyl aryl, benzyl; each of which may be substituted by 1 to 4 groups J; according to the following Scheme 1: in which step a means a reaction in basic conditions of compounds (IIA) with 3-thiosemicarbazide derivatives, followed by a treatment with an inorganic base and n-propane phosphonic cyclic anhydride and final pH adjustement with inorganic acids to give compounds of formula (II).
摘要翻译：本发明涉及用于制备各种化合物的合成中的式（I）的关键中间体的新方法，其中X是可以是氮或硫的D3受体的有效和特异性拮抗剂的化合物; Het是指芳基或杂芳基; 它们各自可以被1至4个选自以下的基团取代：卤素，C 1 -C 6烷基C 1 -C 6烷氧基，卤代C 1 -C 6烷基C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，-C（ O）R 1，硝基，羟基，-NR 2 R 3，氰基或基团Z; R1是C1-C4烷基-OR3或-NR3R4; R2是氢或C1-C6烷基; R3是氢或C1-C6烷基; R为H，C 1 -C 6烷基芳基，苄基; 其中每个可以被1至4个基团J取代; 根据以下方案1：其中步骤a表示化合物（IIA）与3-硫代氨基脲衍生物在碱性条件下的反应，然后用无机碱和正丙烷膦酸环状酸酐处理，并用无机酸进行最终pH调节得到式（II）的化合物。

6. 发明申请

US20080058398A1 Compounds 审中-公开
标题翻译：化合物
公开(公告)号：US20080058398A1
公开(公告)日：2008-03-06
申请号：US11841015
申请日：2007-08-20
申请人： Clare Anderton , Sergio Bacchi , Stefania Beato , Franco Sartor
发明人： Clare Anderton , Sergio Bacchi , Stefania Beato , Franco Sartor
IPC分类号： A61K31/422 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36 , C07D413/14
CPC分类号： C07D413/14
摘要： The present invention relates to the tartrate salt of 1-[2-fluoro-4-(trifluoromethyl)phenyl]-3-(3-{[4-methyl-5-(4-methyl-1,3-oxazol-5-yl)-4H-1,2,4-triazol-3-yl]thio}propyl)-3-azabicyclo[3.1.0]hexane and solvates thereof, pharmaceutical formulations, processes for their preparation, and their use in medicine.
摘要翻译：本发明涉及1- [2-氟-4-（三氟甲基）苯基] -3-（3 - {[4-甲基-5-（4-甲基-1,3-恶唑-5-基）吡啶-4-基）-4H-1,2,4-三唑-3-基]硫基}丙基）-3-氮杂双环[3.1.0]己烷及其溶剂合物，药物制剂，其制备方法及其在医药中的应用。

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