公开(公告)号：US20090326266A1

公开(公告)日：2009-12-31

申请号：US12400080

申请日：2009-03-09

申请人： Katiuscia ARRIGHI ,  Vincenzo CANNATA ,  Francesco CORCELLA ,  Gaetano MARCHIORO ,  Andrea NICOLI ,  Maurizio PAIOCCHI ,  Marco VILLA

发明人： Katiuscia ARRIGHI ,  Vincenzo CANNATA ,  Francesco CORCELLA ,  Gaetano MARCHIORO ,  Andrea NICOLI ,  Maurizio PAIOCCHI ,  Marco VILLA

IPC分类号： C07C229/28

CPC分类号： C07C231/02 ,  C07C2601/14 ,  C07C233/08

摘要： A process for the preparation of 1,1-cyclohexanediacetic acid monoamide comprising the amination of 1,1-cyclohexanediacetic acid anhydride by reaction with aqueous NH3 at a temperature lower than 30° C. by using a NH3/anhydride molar ratio lower than 3, and the product precipitation through the acidification of the reaction mixture; a precipitation process of 1,1-cyclohexanediacetic acid monoamide; and a process for the synthesis of gabapentin comprising the above preparation of 1,1-cyclohexanediacetic acid monoamide, the Hofmann transposition of the same monoamide, the purification of a gabapentin salt and the crystallization from organic solvent.

摘要翻译： 一种制备1,1-环己烷二乙酸单酰胺的方法，该方法包括使用低于3的NH 3 /酐摩尔比，通过与NH 3水溶液在低于30℃的温度下反应来胺化1,1-环己烷二乙酸酐， 并通过反应混合物酸化产物沉淀; 1,1-环己烷二乙酸单酰胺的沉淀过程; 以及合成加巴喷丁的方法，其包括上述1,1-环己烷二乙酸单酰胺的制备，相同单酰胺的霍夫曼转位，加巴喷丁盐的纯化和有机溶剂的结晶。

公开(公告)号：US20110034719A1

公开(公告)日：2011-02-10

申请号：US12910550

申请日：2010-10-22

申请人： Aldo BELLI ,  Vincenzo CANNATA ,  Telly FONDUCA ,  Martin HEDBERG ,  Andreas WESTERMARK ,  Marco VILLA

发明人： Aldo BELLI ,  Vincenzo CANNATA ,  Telly FONDUCA ,  Martin HEDBERG ,  Andreas WESTERMARK ,  Marco VILLA

IPC分类号： C07C201/02

CPC分类号： C07C309/73 ,  A61K31/21 ,  C07C67/08 ,  C07C67/58 ,  C07C201/02 ,  C07C303/28 ,  C07C309/66 ,  C07C309/67 ,  C07C69/734 ,  C07C203/04

摘要： The present invention relates to a new process for the preparation of the (S)-naproxen 4-nitrooxybutyl ester and to new intermediates obtained and used therein. The invention further relates to the use of the new intermediates for the manufacturing of pharmaceutically active compounds such as (S)-naproxen 4-nitrooxybutyl ester. The invention also relates to the use of (S)-naproxen 4-nitrooxybutyl ester prepared according to the process of the present invention for the manufacturing of a medicament for the treatment of pain.

摘要翻译： 本发明涉及制备（S） - 萘普生4-硝基氧丁基酯的新方法及其中获得和使用的新中间体。 本发明还涉及新中间体用于制备药学活性化合物如（S） - 萘普生4-硝基氧基丁基酯的用途。 本发明还涉及根据本发明的方法制备的（S） - 萘普生4-硝基氧基丁基酯在制备用于治疗疼痛的药物中的用途。

公开(公告)号：US20090170934A1

公开(公告)日：2009-07-02

申请号：US12143100

申请日：2008-06-20

申请人： Johan ANDERSSON ,  Aldo BELLI ,  Vincenzo CANNATA ,  Martin HEDBERG ,  Andreas PALMGREN ,  Sigrid SCHULDEI ,  Marika STROM ,  Marco VILLA

发明人： Johan ANDERSSON ,  Aldo BELLI ,  Vincenzo CANNATA ,  Martin HEDBERG ,  Andreas PALMGREN ,  Sigrid SCHULDEI ,  Marika STROM ,  Marco VILLA

IPC分类号： A61K31/24 ,  C07C229/42 ,  C07C203/00

CPC分类号： C07C303/28 ,  A61K31/216 ,  C07C67/08 ,  C07C201/02 ,  C07C203/04 ,  C07C227/16 ,  C07C227/20 ,  C07C229/42 ,  C07C309/66 ,  C07C69/738

摘要： The present invention relates to a new process for the preparation of NO-donating compounds using a sulfonated intermediate. The invention relates to new intermediates prepared therein suitable for large scale manufacturing of NO-donating compounds. The invention further relates to the use of the new intermediates for the manufacturing of pharmaceutically active NO-donating compounds. The invention further relates to a substantially crystalline form of NO-donating NSAIDs, especially 2-[2-(nitrooxy)ethoxy]ethyl {2-[(2,6-dichlorophenyl)amino]phenyl}acetate, the preparation thereof and to pharmaceutical formulations containing said crystalline form and to the use of said crystalline form in the preparation of a medicament.

摘要翻译： 本发明涉及使用磺化中间体制备供给NO的化合物的新方法。 本发明涉及其中制备的适用于大量制备供体化合物的新中间体。 本发明还涉及新的中间体用于制备药物活性的供体化合物的用途。 本发明进一步涉及一种基本上呈结晶形式的给予NO的NSAID，尤其是{2 - [（2,6-二氯苯基）氨基]苯基}乙酸酯的2- [2-（硝基氧基）乙氧基]乙酯，其制备方法和药物 含有所述结晶形式的制剂以及所述结晶形式在制备药物中的用途。

公开(公告)号：US20200299992A1

公开(公告)日：2020-09-24

申请号：US16649221

申请日：2018-09-11

申请人： Marco VILLA ,  Danilo FERREMI

发明人： Marco VILLA ,  Danilo FERREMI

IPC分类号： E05B3/04 ,  E05B1/00 ,  E05B17/00 ,  E05B15/04

摘要： A handle assembly for a door or window comprises a handle and a second element, installable on opposite sides of the door or window, and a pin element rotatable around a pin rotation axis and insertable into the handle or in the second element at variable depths. The handle assembly further comprises a friction reducing group positioned coaxially to the pin element and positionable between the handle and the door or window in the axial direction of the pin rotation axis. Clamping devices constrain the handle and/or the second element on the pin element at adjustable distances along the axial direction according to the thickness of the door or window, so that when the handle assembly is installed on the door or window, an axial clamping pressure of the handle and of the second element is maintained on the respective side of the door or window. An installation method of the handle assembly on the door or window is also provided.

公开(公告)号：US20110263851A1

公开(公告)日：2011-10-27

申请号：US13173599

申请日：2011-06-30

申请人： Nicola DIULGHEROFF ,  Moran PIRKES ,  Alessandro PONTIROLI ,  Marco VILLA

发明人： Nicola DIULGHEROFF ,  Moran PIRKES ,  Alessandro PONTIROLI ,  Marco VILLA

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： Provided are processes for preparing intermediates of pemetrexed.

摘要翻译： 提供了制备培美曲塞中间体的方法。

公开(公告)号：US20110196155A1

公开(公告)日：2011-08-11

申请号：US13070432

申请日：2011-03-23

申请人： Jonathan BUSOLLI ,  Nicola DIULGHEROFF ,  Csilla Nemethne Racz ,  Moran PIRKES ,  Alessandro PONTIROLI ,  Marco VILLA ,  Judith ARONHIME

发明人： Jonathan BUSOLLI ,  Nicola DIULGHEROFF ,  Csilla Nemethne Racz ,  Moran PIRKES ,  Alessandro PONTIROLI ,  Marco VILLA ,  Judith ARONHIME

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： Provided are crystalline forms of N-[4-[2-(2-amino-4,7-dihydro-4-oxo-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid, pemetrexed diacid, and processes for the preparation thereof.

摘要翻译： 提供的是N- [4- [2-（2-氨基-4,7-二氢-4-氧代-1H-吡咯并[2,3-d]嘧啶-5-基）乙基]苯甲酰基] -L- 谷氨酸，培美曲塞二酸及其制备方法。