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1. 发明申请

WO2006111570A2 NEW BIOLOGICALLY ACTIVE FORMULATION 审中-公开
标题翻译：新生物活性配方
公开(公告)号：WO2006111570A2
公开(公告)日：2006-10-26
申请号：PCT/EP2006/061724
申请日：2006-04-21
申请人： ENDURA S.P.A. , PICCOLO, Oreste , BORZATTA, Valerio , DELOGU, Giovanna , CAPPARELLA, Elisa , DE CANDIA, Cristina , GOBBI, Carlotta , DI BLASI, Giovanna
发明人： PICCOLO, Oreste , BORZATTA, Valerio , DELOGU, Giovanna , CAPPARELLA, Elisa , DE CANDIA, Cristina , GOBBI, Carlotta , DI BLASI, Giovanna
IPC分类号： A01N25/10 , A01N57/16 , A01N47/40 , A01N47/18 , A01N47/02 , A01N43/78 , A01N43/54 , A01N43/50 , A01P7/04 , A01N43/30
CPC分类号： A01N25/10
摘要： The present invention provides a formulation characterised by the simultaneous presence in cyclodextrin based supramolecular complexes, of two components, one of which possesses insecticidal, acaricidal, fungicidal, snailcidal or vermicidal activity and the other possesses an activity synergistic with the first, enhancing its effectiveness. The biologically active substance is chosen from the following classes of chemical products: carbamates, organophosphates, thioureas, pentatomic or hexatomic heterocycles in which 1 , 2 or 3 nitrogen atoms are present. The synergistic substance can be chosen from components containing at least one aromatic or non aromatic carbocyclic ring, such as piperonyl butoxide, sesamol, verbutin or MGK 264. For the same dose, the activity of the present formulations is greater than that of the mixture of the two active components alone or separately complexed with cyclodextrin. The process for preparing said formulation and its use for the activities herein indicated are further aspects of the present invention.
摘要翻译：本发明提供一种制剂，其特征在于同时存在两种组分的两种组分的基于环糊精的超分子复合物，其中一种具有杀虫，杀螨，杀真菌，杀虫或杀虫活性，另一种具有与第一种协同作用的活性，提高其有效性。生物活性物质选自以下类别的化学产品：其中存在1,2或3个氮原子的氨基甲酸酯，有机磷酸酯，硫脲，五原子或六原子杂环。协同物质可以选自含有至少一个芳族或非芳族碳环的组分，例如胡椒基丁醚，芝麻酚，鸟嘌呤或MGK 264.对于相同的剂量，本发明制剂的活性大于两种活性组分单独或分别与环糊精复合。制备所述制剂的方法及其用于本文所述活性的用途是本发明的另外的方面。

2. 发明申请

WO2005039287A2 INSECTICIDE FORMULATION 审中-公开
标题翻译：杀虫剂配方
公开(公告)号：WO2005039287A2
公开(公告)日：2005-05-06
申请号：PCT/EP2004/052665
申请日：2004-10-26
申请人： ENDURA S.P.A. , PICCOLO, Oreste , DELOGU, Giovanna , BORZATTA, Valerio
发明人： PICCOLO, Oreste , DELOGU, Giovanna , BORZATTA, Valerio
IPC分类号： A01N
CPC分类号： A01N53/00 , A01N25/08 , A01N37/38 , A01N43/90 , C08B37/0015 , A01N43/30 , A01N43/653 , A01N2300/00
摘要： The present invention provides a new insecticide formulation based on cyclodextrin characterised in that the active substance (insecticide and/or insect growth regulator), and a compound synergistic with the active substance, are complexed simultaneously with cyclodextrin. The formulation presents as a solid or as a solid/oil composition, and is soluble or completely emulsifiable in water or in aqueous mixtures of water miscible solvents. The activity of the present formulations was found to be greater than that of a mixture of the two active components each complexed separately with cyclodextrin, for the same dose. The preparation process of said formulation and its use as an insecticide in agriculture, for veterinary use or to eliminate household insects, are further aspects of the present invention.
摘要翻译：本发明提供了基于环糊精的新型杀虫剂制剂，其特征在于活性物质（杀虫剂和/或昆虫生长调节剂）和与活性物质协同作用的化合物与环糊精同时络合。该制剂以固体或固体/油组合物形式存在，并且可溶于或完全可乳化于水或可与水混溶的溶剂的含水混合物中。发现本制剂的活性大于两种活性组分的混合物的活性，所述两种活性组分分别与环糊精分别与相同剂量复合。所述制剂的制备方法及其在农业，兽用或消除家庭昆虫中作为杀虫剂的用途是本发明的进一步方面。

3. 发明申请

WO2006111553A1 INNOVATIVE FORMULATION 审中-公开
标题翻译：创新公式
公开(公告)号：WO2006111553A1
公开(公告)日：2006-10-26
申请号：PCT/EP2006/061688
申请日：2006-04-20
申请人： ENDURA S.P.A. , BORZATTA, Valerio , PICCOLO, Oreste , CAPPARELLA, Elisa
发明人： BORZATTA, Valerio , PICCOLO, Oreste , CAPPARELLA, Elisa
IPC分类号： A01N25/28 , A01N53/00 , A01N53/06 , A01N43/30 , A01N57/16 , A01N51/00 , A01N47/40 , A01N43/58 , A01N43/54 , A01N31/14 , A01P7/00 , A01P3/00
CPC分类号： A01N43/30 , A01N25/28 , A01N53/00 , A01N2300/00
摘要： The present invention relates to a new formulation characterised by the presence of two components, one of which (A) possesses insecticidal, acaricidal, fungicidal, snailcidal or vermicidal activity and the other (B) exhibits synergistic activity with the first by enhancing its effectiveness, and in which the average release time of component (A) is 1 to 12 hours later than the average release time of component (B). The formulation is obtained by: a) separate microencapsulation of both components (A) and (B) within a multilayer system of specific polymers in which component (A) is in a more interior portion of the capsule than component (B), being separated from component (B) by a polymer layer of suitable thickness (Figure 1); b) microencapsulation of both components within a single layer system (Figure 2), combined with an immediate-release emulsion/microemulsion containing an additional amount of component (B).
摘要翻译：本发明涉及一种新的制剂，其特征在于两种成分的存在，其中一种成分（A）具有杀虫，杀螨，杀真菌，杀虫或杀虫活性，另一种（B）通过提高其有效性与第一种成分具有协同作用，其中组分（A）的平均释放时间比组分（B）的平均释放时间晚1至12小时。该制剂通过以下方法获得：a）在特定聚合物的多层体系内单独的组分（A）和（B）的微胶囊化，其中组分（A）在组分（B）的更多内部部分中，分离从组分（B）通过合适厚度的聚合物层（图1）; b）单层系统（图2）中两种组分的微囊化，与含有额外量的组分（B）的立即释放乳液/微乳液组合。

4. 发明申请

WO2004092106A2 PROCESS FOR PREPARING ALKOXY- AND ARYLOXY-PHENOLS 审中-公开
标题翻译：制备烷基和芳基苯酚的方法
公开(公告)号：WO2004092106A2
公开(公告)日：2004-10-28
申请号：PCT/EP2004/050470
申请日：2004-04-07
申请人： ENDURA S.P.A. , BORZATTA, Valerio , PICCOLO, Oreste , CAPPARELLA, Elisa , POLUZZI, Elisa
发明人： BORZATTA, Valerio , PICCOLO, Oreste , CAPPARELLA, Elisa , POLUZZI, Elisa
IPC分类号： C07C43/00
CPC分类号： C07D317/64 , C07C41/26 , C07C67/42 , C07D319/18 , C07C69/017 , C07C43/295 , C07C43/23
摘要： Process for preparing alkoxy- and aryloxy-phenols, comprising oxidizing the ketone of formula (I) with peracids to give the corresponding ester of formula (II) which is then hydrolysed to give the corresponding aryloxy- or alkoxy-phenol.
摘要翻译：制备烷氧基 - 和芳氧基 - 苯酚的方法，包括用过酸氧化式（I）酮，得到相应的式（II）酯，然后将其水解，得到相应的芳氧基 - 或烷氧基 - 苯酚。

5. 发明申请

WO2003010129A1 PROCESS FOR THE PREPARATION OF (R)- OR (S)-AMINOCARNITINE INNER SALT, THE SALTS AND DERIVATIVES THEREOF 审中-公开
标题翻译：制备（R） - 或（S） - 胺盐酸盐，其盐及其衍生物的方法
公开(公告)号：WO2003010129A1
公开(公告)日：2003-02-06
申请号：PCT/IT2002/000468
申请日：2002-07-17
申请人： SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A. , PICCOLO, Oreste , CASTAGNANI, Roberto , DE WITT SCALFARO, Paolo
发明人： PICCOLO, Oreste , CASTAGNANI, Roberto , DE WITT SCALFARO, Paolo
IPC分类号： C07C227/16
CPC分类号： C07C227/16 , C07C231/02 , C07C273/1827 , C07C229/26 , C07C233/47
摘要： A process for the production of (R)- or (S)-aminocarnitine starting respectively from (R)- or (S)-nitryloxycarnitine, through the formation and hydrogenation of the azidocarnitine intermediate with the same absolute configuration is described. (R)-aminocarnitine inner salt is obtained after purification, which is then converted into non-deliquescent salts. A further subject of the present invention is a process for the preparation of derivatives of (R)- and (S)-aminocarnitine, in particular acylated or ureic derivatives, having known pharmacological properties, starting from (R)- and (S)-aminocarnitine salts, releasing the aminic function in situ.
摘要翻译：描述了通过形成和氢化具有相同绝对构型的叠氮基卡那霉素中间体，分别从（R） - 或（S） - 硝基氧肉碱生产（R） - 或（S） - 氨卡尼汀的方法。（R） - 氨基卡那肽内盐，然后转化成非潮解性盐。本发明的另一个主题是制备（R） - 和（S） - 氨基卡尼汀衍生物的方法，特别是具有已知药理学性质的酰化或脲类衍生物，（R） - 和（S） - 氨卡尼汀盐，原位释放氨基功能。

6. 发明申请

WO2003074169A3 METALORGANIC CATALYSTS FOR CHEMO-, REGIO- AND STEREOSELECTIVE REACTIONS, AND CORRESPONDING PRECURSORS 审中-公开
公开(公告)号：WO2003074169A3
公开(公告)日：2003-09-12
申请号：PCT/EP2003/002160
申请日：2003-03-03
申请人： CHEMI S.P.A. , SANNICOLO, Francesco , PICCOLO, Oreste , BENINCORI, Tiziana , SADA, Mara , VERRAZZANI, Alessandra , TOLLIS, Simona , ULLUCCI, Elio , DE FERRA, Lorenzo , RIZZO, Simona
发明人： SANNICOLO, Francesco , PICCOLO, Oreste , BENINCORI, Tiziana , SADA, Mara , VERRAZZANI, Alessandra , TOLLIS, Simona , ULLUCCI, Elio , DE FERRA, Lorenzo , RIZZO, Simona
IPC分类号： B01J31/24
摘要： Metallic catalysts of the general formula (I) and their precursors, suitable for chemo- regio- and stereoselective reactions, derived from ortho- bis(1-phospholanyl)-heteroarenes. The new catalysts are characterized by the presence of two homomorphic phospholanic rings set in adjacent positions of an aromatic pentatomic heterocycle.

7. 发明申请

WO2011036303A1 NEW AMINOACID DERIVATIVES, THEIR PROCESS OF PREPARATION AND THEIR THERAPEUTICAL USES AS INHIBITORS OF ONCOGENIC SIGNALS BY THE MET FAMILY 审中-公开
标题翻译：新的氨基酸衍生物，它们的制备过程及其作为由MET家族的基因信号的抑制剂使用的治疗方法
公开(公告)号：WO2011036303A1
公开(公告)日：2011-03-31
申请号：PCT/EP2010/064332
申请日：2010-09-28
申请人： UNIVERSITE DE LA MEDITERRANEE AIX-MARSEILLE II , MAINA, Flavio , DONO, Rosanna , CAMBILLAU, Christian , PICCOLO, Oreste , PASSARELLA, Daniele , COLOMBO, Francesco , BOSCH, Joan , MAIGRET, Bernard , LEROUX, Vincent
发明人： MAINA, Flavio , DONO, Rosanna , CAMBILLAU, Christian , PICCOLO, Oreste , PASSARELLA, Daniele , COLOMBO, Francesco , BOSCH, Joan , MAIGRET, Bernard , LEROUX, Vincent
IPC分类号： C07D513/04 , A61K31/729 , A61P29/00 , A61P35/00
CPC分类号： C07D513/04
摘要： The present invention concerns novel aminoacids derivatives, in particular some aminoacid amides derivatives, their process of preparation and their use for inhibiting Met-triggered disorders, in particular cancer.
摘要翻译：本发明涉及新的氨基酸衍生物，特别是一些氨基酸酰胺衍生物，其制备方法及其用于抑制Met-触发性疾病，特别是癌症的用途。

8. 发明公开

EP1644311A2 ENANTIOSELECTIVE SYNTHESIS OF ENANTIOMERICALLY ENRICHED COMPOUNDS 审中-公开
标题翻译：对映体富集的连接对映选择性合成
公开(公告)号：EP1644311A2
公开(公告)日：2006-04-12
申请号：EP04763070.2
申请日：2004-07-01
申请人： CONSIGLIO NAZIONALE DELLE RICERCHE , Piccolo, Oreste
发明人： PICCOLO, Oreste , ULGHERI, Fausta , MARCHETTI, Mauro
IPC分类号： C07C67/303 , C07D311/74 , C07C215/54
CPC分类号： C07D311/20 , C07B2200/07 , C07C213/10 , C07C215/54
摘要： Method of preparing an enantiomerically enriched compound of formula (II) comprising enantioselective hydrogenation of a compound of general formula (I): where W, X and Z have the meanings indicated in the description, to give a compound of general formula (II): where W, Y, T and C* have the meanings indicated in the description, in the presence of a catalyst or its suitable precursor based on Rh, Ru or Ir, having an oxidation state of 0, +1 or +2, and containing at least one enantiomerically enriched chiral ligand.

9. 发明申请

WO2012098044A1 PROCESS FOR THE PREPARATION OF N,N-DIISOPROPYL-3-(2-HYDROXY-5-METHYLPHENYL)- 3-PHENYL PROPYLAMINE AND ITS SALTS STARTING FROM A NOVEL INTERMEDIATE 审中-公开
标题翻译：制备N，N-二异丙基-3-（2-羟基-5-甲基苯基）-3-苯基丙胺的方法及其从新型中间体开始的盐
公开(公告)号：WO2012098044A1
公开(公告)日：2012-07-26
申请号：PCT/EP2012/050436
申请日：2012-01-12
申请人： CAMBREX PROFARMACO MILANO S.R.L. , GIANOLLI, Edoardo , GIANNINI, Elios , BIGINI, Laura , PICCOLO, Oreste , HOLMBERG, Pär , LUNDHOLM, Tommy
发明人： GIANOLLI, Edoardo , GIANNINI, Elios , BIGINI, Laura , PICCOLO, Oreste , HOLMBERG, Pär , LUNDHOLM, Tommy
IPC分类号： C07C213/02 , C07C231/12 , C07C235/34 , C07C215/54
CPC分类号： C07C213/02 , C07C231/12 , C07C235/32 , C07C215/54 , C07C235/34
摘要： The invention concerns an improved process for the preparation of tolterodine (N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenyl propyl amine) and its salts, in particular for the preparation of the tartrate salt, and more particularly for the (+)-(R) enantiomer of tolterodine L-tartrate, starting from a novel intermediate, N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3- phenyl-2-propenamide, which can be used as pure Z or E isomer or as a mixture of Z and E isomers. When the target is the preparation of the enantiomer (R)-(+)-(N,N- diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropylamine) and diastereomeric crystallization of suitable compound is applied, the present invention covers also the use of racemisation of undesired (S)-(-)- (N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3 -phenyl propylamine) enantiomer and its recycle in the process.
摘要翻译：本发明涉及一种制备托特罗定（N，N-二异丙基-3-（2-羟基-5-甲基苯基）-3-苯基丙基胺）及其盐的改进方法，特别是制备酒石酸盐，更特别是对于来自新型中间体N，N-二异丙基-3-（2-羟基-5-甲基苯基）-3-苯基-2-丙烯酰胺的托特罗定L-酒石酸盐的（+） - （R）对映异构体，其可以用作纯Z或E异构体或作为Z和E异构体的混合物。当靶是制备对映异构体（R） - （+） - （N，N-二异丙基-3-（2-羟基-5-甲基苯基）-3-苯基丙胺）时，应用合适的化合物的非对映体结晶，本发明还涉及不期望的（S） - （ - ） - （N，N-二异丙基-3-（2-羟基-5-甲基苯基）-3-苯基丙胺）对映异构体的外消旋化及其在该方法中的再循环的用途。

10. 发明申请

WO2007128474A3 ENANTIOMERIC RESOLUTION OF A CARNITINAMIDE SALT BY PREFERENTIAL CRYSTALLIZATION 审中-公开
公开(公告)号：WO2007128474A3
公开(公告)日：2007-11-15
申请号：PCT/EP2007/003861
申请日：2007-05-02
申请人： UNIVERSITA' DEGLI STUDI DI MILANO , PICCOLO, Oreste , PALLAVICINI, Marco , VALOTI, Ermanno , BOLCHI, Cristiano , FUMAGALLI, Laura
发明人： PICCOLO, Oreste , PALLAVICINI, Marco , VALOTI, Ermanno , BOLCHI, Cristiano , FUMAGALLI, Laura
IPC分类号： C07C231/20 , C07C237/06
摘要： A process for the resolution of (D,L)-carnitinamide (D,L-I) chloride in its enantiomers (D-I) and (L-I), characterized in that a supersaturated solution or suspension of (D,L-I) in a suitable solvent or mixture of solvents, optionally added with a surfactant, is used. A series of alternate preferential crystallizations is carried out after adding minimum amount of seeds of one of the two enantiomers, (D-I) or (L-I), that is to be precipitated, and subsequently restoring the supersaturation conditions by adding an appropriate amount of (D,L-I) racemate.

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