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1. 发明专利

JPH10204025A GEMINAL CARBOXYLIC ACID USEFUL FOR THERAPY OF BONE DISBOLISM AND PHARMACEUTICAL PREPARATION CONTAINING THE ESTER 失效
公开(公告)号：JPH10204025A
公开(公告)日：1998-08-04
申请号：JP5710497
申请日：1997-02-26
申请人： DOMPE SPA
发明人： ALLEGRETTI MARCELLO , MANTOVANINI MARCO , CASELLI GIANFRANCO , FIORENTINO SIMONETTA , CLAVENNA GAETANO , GANDOLFI CARMELO A
IPC分类号： C07D295/08 , A61K31/19 , A61K31/215 , A61K31/38 , A61K31/381 , A61K31/385 , A61K31/40 , A61K31/42 , A61K31/44 , A61K31/4406 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61P19/10 , A61P43/00 , C07C57/13 , C07C69/708 , C07C69/712 , C07C69/734 , C07C323/51 , C07C335/32 , C07D207/16 , C07D211/22 , C07D211/34 , C07D211/42 , C07D211/46 , C07D213/30 , C07D213/32 , C07D213/55 , C07D213/65 , C07D213/68 , C07D233/42 , C07D239/10 , C07D239/26 , C07D261/08 , C07D295/14 , C07D295/15 , C07D307/46 , C07D309/06 , C07D309/12 , C07D333/24 , C07D333/26 , C07D333/32 , C07D333/34 , C07D335/02 , C07D339/06 , C07D401/12
摘要： PROBLEM TO BE SOLVED: To obtain the new compound capable of maintaining the normal activity of osteoclasts even in the hyperreactive syndromes of the osteoclasts and capable of being used for the treatments of osteoporosis, bone dispolism, malignant hyderpcalcemia, and Paget's disease. SOLUTION: A compound of formula I Ra , Rb are each H, an alkali metal cation, etc.; ϕ is a group of the formula: (Y)q -(CH2 )r (Y is CH2 , O, S); B is 2-propyl, a heterocyclic group of formula II (Z is HC, etc.; X is a single bond, CH2 , O, etc.), etc.; R is β-pyridyl, a group of formula III (when R is H and R is H, a 1-7C alkyl, etc., R is H, a 1-4C alkyl, etc., and can form a five or six-membered heterocyclic ring or a five to seven-membered saturated nitrogen-containing heterocyclic ring), etc.; (m) is 0, 1, 2, 3; (n) is 0.1 to 6; (q) is 0,1; (r) is an integer of 0, 1-3}, e.g. 5-BOC-amino-2-[2-(ethoxy)-ethoxy]-2- carboxy-pentanoic acid lithium salt. The compound of formula I is obtained by a substitution method at the methine group C-H of a malonic acid ester of formula IV (R'a , R'b are each a 1-4C alkyl, etc.).

2. 发明申请

WO2007060215A3 (R)-ARYLALKYLAMINO DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：（R） - 十二烷基胺衍生物和含有它们的药物组合物
公开(公告)号：WO2007060215A3
公开(公告)日：2007-10-04
申请号：PCT/EP2006068867
申请日：2006-11-24
申请人： DOMPE SPA , ALLEGRETTI MARCELLO , MORICONI ALESSIO , ARAMINI ANDREA , CESTA MARIA CANDIDA , BECCARI ANDREA , BERTINI RICCARDO
发明人： ALLEGRETTI MARCELLO , MORICONI ALESSIO , ARAMINI ANDREA , CESTA MARIA CANDIDA , BECCARI ANDREA , BERTINI RICCARDO
IPC分类号： C07C309/65 , A61K31/165 , A61K31/18 , A61P9/10 , C07C233/76 , C07C311/03 , C07C311/21 , C07D213/70 , C07D213/76 , C07D277/42 , C07D295/10 , C07D295/14 , C07D307/52 , C07D307/68 , C07D333/34
CPC分类号： C07C311/21 , C07C233/76 , C07C309/65 , C07C311/03 , C07D213/70 , C07D213/76 , C07D277/42 , C07D295/108 , C07D295/15 , C07D307/52 , C07D307/68 , C07D333/34
摘要： The present invention relates to selected (R)-arylalkylamino derivatives of formula (I), in which R, R1 and Ar are as defined in the claims. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
摘要翻译：本发明涉及式（I）的选择的（R） - 芳基烷基氨基衍生物，其中R，R 1和Ar如权利要求中所定义。这些化合物显示出对C5a诱导的人类PMN趋化性的惊人的有效抑制作用。本发明化合物绝对缺乏CXCL8抑制活性。所述化合物可用于治疗病理学，这取决于由补体的级分C5a诱导的嗜中性粒细胞和单核细胞的趋化活化。特别地，本发明的化合物可用于治疗败血症，牛皮癣，类风湿性关节炎，溃疡性结肠炎，急性呼吸窘迫综合征，特发性纤维化，肾小球性肾炎，以及预防和治疗由缺血和再灌注引起的损伤。

3. 发明申请

WO2005090295A3 2-PHENYLPROPIONIC ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译： 2-苯基丙酸衍生物和含有它们的药物组合物
公开(公告)号：WO2005090295A3
公开(公告)日：2005-10-27
申请号：PCT/EP2005051302
申请日：2005-03-21
申请人： DOMPE SPA , ALLEGRETTI MARCELLO , BERTINI RICCARDO , CESTA MARIA CANDIDA , MOSCA MARCO , COLOTTA FRANCESCO
发明人： ALLEGRETTI MARCELLO , BERTINI RICCARDO , CESTA MARIA CANDIDA , MOSCA MARCO , COLOTTA FRANCESCO
IPC分类号： C07C309/65 , C07D277/46 , C07D295/13 , A61K31/255 , A61P11/00 , C07D295/12
CPC分类号： C07C309/65 , C07C2601/08 , C07D295/13
摘要： (R)-2-[4-(Trifluoromethanesulphonyloxy)phenyl]propionamide derivatives of_ formula (I), where the variables are as defined in the claims, and pharmaceutical compositions containing such compounds are useful in inhibiting. the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of interieukin-8 (IL-8) with CXCRI and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclooxygenase inhibition. activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.
摘要翻译：（I）的（R）-2- [4-（三氟甲磺酰氧基）苯基]丙酰胺衍生物，其中变量如权利要求中所定义，并且含有这些化合物的药物组合物可用于抑制。由白细胞介素-8（IL-8）与CXCRI和CXCR2膜受体的相互作用诱导的嗜中性粒细胞（PMN白细胞）的趋化活化。所述化合物用于预防和治疗由所述活化引起的病理学。值得注意的是，这些代谢物没有环加氧酶抑制作用。活性，并且特别可用于治疗嗜中性粒细胞依赖性病理学如牛皮癣，溃疡性结肠炎，黑素瘤，慢性阻塞性肺病（COPD），大疱性类天疱疮，类风湿性关节炎，特发性纤维化，肾小球性肾炎，以及预防和治疗由缺血和再灌注。

4. 发明申请

WO2004078102A3 STERILIZATION OF BECLOMETHASONE DRUG PARTICLES FOR PULMONARY DELIVERY 审中-公开
标题翻译：用于脉冲递送的贝伐珠酮药物颗粒的灭菌
公开(公告)号：WO2004078102A3
公开(公告)日：2004-11-18
申请号：PCT/EP2004050235
申请日：2004-03-02
申请人： DOMPE SPA , GENTILE MARCO , DRAGANI MARIA CONCETTA , DELL UOMO MARCO
发明人： GENTILE MARCO , DRAGANI MARIA CONCETTA , DELL UOMO MARCO
IPC分类号： A61K9/00 , A61K31/56 , A61K31/57 , A61K31/573 , A61L2/00 , A61L2/04 , A61L2/07 , C07J5/00 , C07J7/00 , C07J51/00 , C07J75/00
CPC分类号： C07J7/00 , A61K9/0078 , A61K31/56 , A61K31/57 , A61K31/573 , A61L2/0005 , A61L2/0011 , A61L2/0023 , A61L2/04 , A61L2/07 , C07J5/0015 , C07J5/0061 , C07J51/00 , C07J75/00
摘要： A process for the sterilization of water insoluble solid medicinal substances is described.The process provides the sterilization of beclomethasone, which is suitable for pulmonary administration. In particular, the process is used in industrial plants for the production of formulations of sterile beclomethasone for inhalation delivery, so as to avoid any modifications in particle size distribution and in the impurities profile of the drug. The process is carried out by heating a mixture of micronized beclomethasone and purified water only, preferably at a temperature of about 120° C for 20 minutes. The process is particularly efficient and economic for the steam sterilization of beclomethasone dipropionate in formulations for pulmonary delivery.
摘要翻译：描述了对水不溶性固体药物灭菌的方法。该方法提供了适用于肺部给药的倍氯米松的灭菌方法。特别地，该方法用于生产用于吸入输送的无菌倍氯米松配方的工业装置中，以避免药物的粒度分布和杂质分布的任何修改。该方法通过仅加热微粉化的倍氯米松和纯化水的混合物，优选在约120℃的温度下加热20分钟来进行。该方法对于用于肺部输送的制剂中的丙酸倍氯米松的蒸汽灭菌是特别有效和经济的。

5. 发明申请

WO02068107A8 APPARATUS AND METHOD FOR MICRON AND SUBMICRON PARTICLE FORMATION 审中-公开
标题翻译：微米和亚微米颗粒形成的装置和方法
公开(公告)号：WO02068107A8
公开(公告)日：2003-10-16
申请号：PCT/GB0200840
申请日：2002-02-26
申请人： DOMPE SPA , DEL RE GIOVANNI , PUTRIGNANO MATTEO , DI GIACOMO GABRIELE , DI PALMA CESARE , PIESOLD ALEXANDER JAMES
发明人： DEL RE GIOVANNI , PUTRIGNANO MATTEO , DI GIACOMO GABRIELE , DI PALMA CESARE
IPC分类号： C12M1/00 , A61L2/07 , B01D9/02 , B01J2/04 , B01J3/00 , B01J7/00 , B05B7/08 , C12N9/00
CPC分类号： B05B7/08 , B01J2/04
摘要： An apparatus is described for micron and submicron particles formation of a substance using the GAS process, comprising a particles formation vessel (22) and means for introducing a solution of the substance and a supercritical fluid into the particles formation vessel (22), wherein said means comprise a nozzle (27) having a central orifice (39) serving to carry a flow of solution, and a plurality of separate outer orifices (41) serving to carry a flow of pure supercritical fluid or a flow of supercritical fluid mixed with a modifier, such that the solvent is extracted from the solution by the supercritical fluid and precipitation of micron and submicron particles occurs. Also a process is described, carried out with such an apparatus.
摘要翻译：描述了使用GAS方法形成物质的微米和亚微米颗粒的装置，其包括颗粒形成容器（22）和用于将物质和超临界流体的溶液引入到颗粒形成容器（22）中的装置，其中所述装置包括具有用于承载溶液流的中心孔口（39）的喷嘴（27）和用于承载纯超临界流体流或混合有超临界流体的超临界流体流的多个分开的外部孔口（41）使得通过超临界流体从溶液中提取溶剂并发生微米和亚微米颗粒的沉淀。还描述了使用这种装置进行的过程。

6. 发明申请

WO02068107A3 APPARATUS AND METHOD FOR MICRON AND SUBMICRON PARTICLE FORMATION 审中-公开
标题翻译：微米和亚微米颗粒形成的装置和方法
公开(公告)号：WO02068107A3
公开(公告)日：2002-12-05
申请号：PCT/GB0200840
申请日：2002-02-26
申请人： DOMPE SPA , DEL RE GIOVANNI , PUTRIGNANO MATTEO , DI GIACOMO GABRIELE , DI PALMA CESARE , PIESOLD ALEXANDER JAMES
发明人： DEL RE GIOVANNI , PUTRIGNANO MATTEO , DI GIACOMO GABRIELE , DI PALMA CESARE
IPC分类号： C12M1/00 , A61L2/07 , B01D9/02 , B01J2/04 , B01J3/00 , B01J7/00 , B05B7/08 , C12N9/00
CPC分类号： B05B7/08 , B01J2/04
摘要： An apparatus is described for micron and submicron particles formation of a substance using the GAS process, comprising a particles formation vessel (22) and means for introducing a solution of the substance and a supercritical fluid into the particles formation vessel (22), wherein said means comprise a nozzle (27) having a central orifice (39) serving to carry a flow of solution, and a plurality of separate outer orifices (41) serving to carry a flow of pure supercritical fluid or a flow of supercritical fluid mixed with a modifier, such that the solvent is extracted from the solution by the supercritical fluid and precipitation of micron and submicron particles occurs. Also a process is described, carried out with such an apparatus.
摘要翻译：描述了使用GAS方法形成物质的微米和亚微米颗粒的装置，其包括颗粒形成容器（22）和用于将物质和超临界流体的溶液引入到颗粒形成容器（22）中的装置，其中所述装置包括具有用于承载溶液流的中心孔口（39）的喷嘴（27）和用于承载纯超临界流体流或混合有超临界流体的超临界流体流的多个分开的外部孔口（41）使得通过超临界流体从溶液中提取溶剂并发生微米和亚微米颗粒的沉淀。还描述了使用这种装置进行的过程。

7. 发明申请

WO0168899A3 MOLECULAR WEIGHT MARKERS FOR WESTERN BLOT 审中-公开
标题翻译：西班牙分子重量标记
公开(公告)号：WO0168899A3
公开(公告)日：2002-02-21
申请号：PCT/EP0102890
申请日：2001-03-15
申请人： DOMPE SPA , RUGGIERO PAOLO , MAURIZI GIOVANNI , CIABINI ANNIBALE , CIOCCIO VITO DI
发明人： RUGGIERO PAOLO , MAURIZI GIOVANNI , CIABINI ANNIBALE , DI CIOCCIO VITO
IPC分类号： G01N33/50 , C12Q1/28 , G01N27/447 , G01N33/535 , G01N33/58 , G01N33/68
CPC分类号： C12Q1/28 , G01N33/581 , G01N33/6803
摘要： The present information discloses molecular weight markers for Western blot, comprising standard molecular weight markers for SDS-PAGE conjugated with an enzyme having peroxidase activity, e.g. cytochrome C or horseradish peroxidase.
摘要翻译：本信息公开了用于蛋白质印迹的分子量标记，其包含与具有过氧化物酶活性的酶缀合的SDS-PAGE的标准分子量标记。细胞色素C或辣根过氧化物酶。

8. 发明申请

WO0125236A3 A STEREOSELECTIVE PROCESS FOR THE PREPARATION OF ENDO-3-AMINOAZABICYCLOALKANES 审中-公开
标题翻译：制备内-3-氨基亚硫酰氯的立体选择性方法
公开(公告)号：WO0125236A3
公开(公告)日：2002-01-17
申请号：PCT/IB0001360
申请日：2000-09-26
申请人： DOMPE SPA , ALLEGRETTI MARCELLO , CURTI ROBERTO , CESTA MARIA CANDIDA , NICOLINI LUCA
发明人： ALLEGRETTI MARCELLO , CURTI ROBERTO , CESTA MARIA CANDIDA , NICOLINI LUCA
IPC分类号： C07D451/04
CPC分类号： C07D451/04
摘要： A one-step stereoselective process for the preparation of endo-3-aminoazabicycloalkanes from azabicycloalkanones by means of reductive amination is described.
摘要翻译：描述了通过还原胺化从氮杂双环烷酮制备内-3-氨基氮杂双环烷烃的一步立体选择性方法。

9. 发明申请

WO9938967A3 RECOMBINANT PROTEINS DERIVED FROM HGF AND MSP 审中-公开
标题翻译： HGF和MSP衍生的重组蛋白
公开(公告)号：WO9938967A3
公开(公告)日：1999-09-16
申请号：PCT/EP9900478
申请日：1999-01-27
申请人： DOMPE SPA , MEDICO ENZO , MICHIELI PAOLO , COLLESI CHIARA , CASELLI GIANFRANCO , COMOGLIO PAOLO
发明人： MEDICO ENZO , MICHIELI PAOLO , COLLESI CHIARA , CASELLI GIANFRANCO , COMOGLIO PAOLO
IPC分类号： C12N15/09 , A61K38/00 , A61P39/02 , C07K14/47 , C07K14/475 , C07K19/00 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N15/12 , C12P21/02 , A61K38/18
CPC分类号： C07K14/4753 , A61K38/00 , C07K2319/02 , C12N2799/026
摘要： Recombinant proteins deriving from recombination of structural domains deriving from the alpha subunits of HGF and/or MSP growth factors. The recombinant proteins of the present invention have biological activity, and protect cells from death (apoptosis) induced by chemotherapeutic drugs. These molecules can conveniently be used to prevent or to treat the toxic side effects of chemotherapeutic agents used in cancer therapy.
摘要翻译：衍生自HGF和/或MSP生长因子的α亚基的结构域的重组的重组蛋白质。本发明的重组蛋白质具有生物活性，保护细胞免受化疗药物诱导的死亡（凋亡）。这些分子可以方便地用于预防或治疗癌症治疗中使用的化学治疗剂的毒副作用。

10. 发明申请

WO03035673A9 SUPERCRITICAL FLUIDS PROCESSING: PREPARATION OF PROTEIN MICROPARTICLES AND THEIR STABILISATION 审中-公开
标题翻译：超临界流体处理：蛋白质微粒的制备及其稳定化
公开(公告)号：WO03035673A9
公开(公告)日：2003-11-13
申请号：PCT/EP0211761
申请日：2002-10-21
申请人： DOMPE SPA , GENTILE MARCO , DI PALMA CESARE , CESTA MARIA CANDIDA
发明人： GENTILE MARCO , DI PALMA CESARE , CESTA MARIA CANDIDA
IPC分类号： C12N9/96 , C07K1/30 , C07K1/32
CPC分类号： C07K1/30 , Y02P20/544
摘要： A process for the co-precipitation of a substance with a stabiliser therefor, by a gas anti solvent process comprising introducing into a particle formation vessel a supercritical fluid pure or mixed with a modifier; and a solution comprising said substance and said stabiliser dissolved in a solvent; so as said solvent is extracted from the solution by said supercritical fluid and co-precipitation of the substance and stabiliser occurs. The process may be carried out using an apparatus comprising a particle formation vessel (22) and a nozzle (27) having a central orifice (39) serving to introduce a solution of the substance and a plurality of outer orifices (41) serving to carry a flow of supercritical fluid into the particle formation vessel (22), such that the solvent is extracted from the solution by the supercritical fluid and precipitation of micron sized particles of the substance/stabilizer occurs. The substance is preferably a protein of pharmaceutical interest, which is highly stabilized for storage by this process.
摘要翻译：一种通过气体反溶剂方法使物质与稳定剂共沉淀的方法，该方法包括向颗粒形成容器中引入纯净的或与改性剂混合的超临界流体; 以及包含溶解在溶剂中的所述物质和所述稳定剂的溶液; 从而通过所述超临界流体从溶液中提取所述溶剂并且发生物质和稳定剂的共沉淀。该过程可以使用包括颗粒形成容器（22）和喷嘴（27）的装置来实施，所述喷嘴具有用于引入所述物质的溶液的中心孔口（39）和用于承载所述物质的多个外部孔口（41）超临界流体流入颗粒形成容器（22）中，使得通过超临界流体从溶液中提取溶剂并且发生物质/稳定剂的微米尺寸颗粒的沉淀。该物质优选是药物感兴趣的蛋白质，其通过该过程高度稳定以用于储存。

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