公开(公告)号：US07108871B2

公开(公告)日：2006-09-19

申请号：US10608213

申请日：2003-06-30

申请人： Ezio Bombardelli ,  Bruno Gabetta

发明人： Ezio Bombardelli ,  Bruno Gabetta

IPC分类号： A01N65/00

CPC分类号： A61K36/48 ,  Y10S514/811 ,  Y10S514/899

摘要： A soya extract having a content of glucoside isoflavones of at least 13% by weight and a content of 0.6 to 1.5 parts by weight of group 3 soya saponins per 1 part by weight of glucoside isoflavones. Also, pharmaceutical compositions containing this extract and methods of administering the extract to treat conditions such as pre- or post-menopausal symptoms, cancer, such as breast or prostate cancer, or alcoholism. The extracts are made by a process which includes the steps of treating ripe whole soya beans or oil-free soya flour with an aliphatic alcohol to obtain a first extract; concentrating the first extract to form a concentrated first extract; purifying the concentrated first extract by treatment with at least one aliphatic hydrocarbon; and extracting active components from the purified concentrated first extract with a water-immiscible aliphatic alcohol to obtain a second extract. Preferably, the final extract is concentrated dried to form the desired soya extract.

摘要翻译： 含有每1重量份葡萄糖苷异黄酮的至少13重量％的葡萄糖苷异黄酮含量和0.6〜1.5重量份的3组大豆皂苷的含量的大豆提取物。 此外，含有该提取物的药物组合物和施用提取物以治疗诸如绝经前或绝经后症状的癌症，癌症例如乳腺癌或前列腺癌或酒精中毒的方法。 提取物通过包括用脂肪醇处理成熟的大豆或无油大豆粉以获得第一提取物的步骤的方法制备; 浓缩第一提取物以形成浓缩的第一提取物; 通过用至少一种脂族烃处理纯化浓缩的第一提取物; 并用水不混溶的脂族醇从纯化的浓缩的第一提取物提取活性成分，得到第二提取物。 优选将最终的提取物浓缩干燥以形成所需的大豆提取物。

公开(公告)号：US5843910A

公开(公告)日：1998-12-01

申请号：US817626

申请日：1997-03-21

申请人： Ezio Bombardelli ,  Bruno Gabetta

发明人： Ezio Bombardelli ,  Bruno Gabetta

IPC分类号： A61K31/00 ,  A61K31/12 ,  A61K31/135 ,  A61K31/165 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P17/00 ,  A61P25/04 ,  A61P29/00 ,  A61P35/00 ,  C07C67/08 ,  C07C69/40 ,  C07C69/42 ,  C07C69/44 ,  C07C233/32 ,  C07C323/22 ,  C07C323/41 ,  C07C323/60 ,  C07H15/248 ,  A61K31/16 ,  C07C321/00 ,  C07H15/00

CPC分类号： C07C323/41 ,  C07C323/60 ,  C07H15/248

摘要： The present invention relates to novel colchicine derivatives of formula (1), where Y is a --CH.sub.2 --CH--NH--R.sub.3 group or a --CH--CH.sub.2 OR.sub.3 group and the other variables are as defined in claim 1, having antiproliferative, antitumoral and anti-inflammatory activities. The novel compounds have a cytotoxicity on human tumoral cell lines comparable with colchicine, but, in comparison with the latter, they are less toxic and more selective, particularly on cells resistant to the usual medicaments. Some compounds have a marked activity on TNF and interleukine 2, and therefore are very potent anti-inflammatory agents. They can be included in pharmaceutical formulations useful for the parenteral, oral and topical administrations.

摘要翻译： PCT No.PCT / EP95 / 03823 Sec。 371日期1997年3月21日 102（e）1997年3月21日PCT PCT 1995年9月27日PCT公布。 出版物WO96 / 11184 日期：1996年04月18日本发明涉及式（1）的秋水仙碱衍生物，其中Y为-CH2-CH-NH-R3基或-CH-CH2OR3基，其他变量如权利要求1所定义， 具有抗增殖，抗肿瘤和抗炎活性。 新型化合物对与秋水仙素相当的人肿瘤细胞株具有细胞毒性，但与后者相比，它们毒性小，选择性更强，特别是耐常规药物的细胞。 一些化合物对TNF和白介素2具有明显的活性，因此是非常有效的抗炎药。 它们可以包括在用于肠胃外，口服和局部给药的药物制剂中。

公开(公告)号：US5407674A

公开(公告)日：1995-04-18

申请号：US88319

申请日：1993-07-07

申请人： Bruno Gabetta ,  Ezio Bombardelli

发明人： Bruno Gabetta ,  Ezio Bombardelli

IPC分类号： A61K31/335 ,  A61K31/337 ,  A61K36/00 ,  A61P35/00 ,  C07D305/14 ,  A61K35/78 ,  C07C69/76

CPC分类号： C07D305/14

摘要： The present invention relates to a new taxane having the structure (1), which is isolatable from root bark of plants of the Taxus genus. The compound (1) is endowed with antitumor activity higher than the one of taxol, the former being active, unlike the latter, also against adriamicine resistant cells and as antileukemic drug. ##STR1##

摘要翻译： 本发明涉及一种具有结构（1）的新型紫杉烷，其与紫杉属植物的根皮分离。 化合物（1）具有比紫杉醇更高的抗肿瘤活性，前者是活性的，不像后者，也是抗阿霉素抗性细胞和抗白血病药物。 1

公开(公告)号：US4764508A

公开(公告)日：1988-08-16

申请号：US882608

申请日：1986-07-07

申请人： Bruno Gabetta ,  Ezio Bombardelli ,  Giorgio Pifferi

发明人： Bruno Gabetta ,  Ezio Bombardelli ,  Giorgio Pifferi

IPC分类号： C07D311/22 ,  A61K31/35 ,  A61K31/357 ,  A61K31/685 ,  A61P1/16 ,  C07D319/00 ,  C07D407/04 ,  C07F9/10 ,  C07D311/00 ,  C07D311/32 ,  C07D319/20

CPC分类号： C07D407/04 ,  C07F9/106

摘要： The invention relates to novel compounds comprising lipophilic complexes of silybin, silidianin, and silicristin with phospholipids, and the preparation of these complexes by non-conventional methods. Absorption of the novel compounds in the gastrointestinal tract is appreciably greater, resulting in higher plasma levels than for the individual flavanolignans. The resulting improvement in the pharmacokinetic and pharmacological parameters is such that the substances can advantageously be used in the treatment of acute and chronic liver disease of toxic, metabolic or infective origin or of degenerative nature.

摘要翻译： 本发明涉及包含水飞蓟宾，硅藻土和硅藻土与磷脂的亲脂性复合物的新化合物，以及通过非常规方法制备这些络合物。 新型化合物在胃肠道中的吸收明显更大，导致比单独的黄烷醇胺类药物更高的血浆水平。 所得到的药代动力学和药理学参数的改善使得该物质可有利地用于治疗有毒，代谢或感染起源或退行性质的急性和慢性肝脏疾病。

公开(公告)号：US06333419B1

公开(公告)日：2001-12-25

申请号：US09724504

申请日：2000-11-28

申请人： Bruno Gabetta ,  Gianfranco Zini

发明人： Bruno Gabetta ,  Gianfranco Zini

IPC分类号： C07D30514

CPC分类号： C07D305/14

摘要： A method for separating paclitaxel from cephalomannin and other related compounds by obtaining a starting material that contains paclitaxel and cephalomannin; dissolving the starting material in any one of a number of particularly defined solvents such as butyl formate and butyl acetate to form a mixture; subjecting the mixture to column chromatography to obtain an eluted fraction of paclitaxel, an eluted fraction of cephalomannin and a residue; and separately drying the paclitaxel and cephalomannin fractions to obtain separate crystalline forms of paclitaxel and cephalomannin, respectively.

摘要翻译： 一种通过获得含有紫杉醇和头孢霉素的原料分离紫杉醇与头孢单宁等相关化合物的方法; 将原料溶解在许多特别限定的溶剂如丁酸甲酯和乙酸丁酯中的任何一种中以形成混合物; 使混合物进行柱色谱，得到紫杉醇的洗脱级分，头孢菌甘氨酸和残留物的洗脱级分; 并分别干燥紫杉醇和头孢麦仑单体，分别得到紫杉醇和头孢菌甘宁的单独结晶形式。

公开(公告)号：US08106231B2

公开(公告)日：2012-01-31

申请号：US12527887

申请日：2008-02-11

申请人： Daniele Ciceri ,  Bruno Gabetta ,  Nicola Vignola ,  Frieder Mitzel ,  Beat T. Weber

发明人： Daniele Ciceri ,  Bruno Gabetta ,  Nicola Vignola ,  Frieder Mitzel ,  Beat T. Weber

IPC分类号： C07C229/00

CPC分类号： C07C227/30 ,  C07C233/08 ,  C07C229/34

摘要： A process for the enantioselective preparation of (2R,3S)-3-phenylisoserine methyl ester acetate salt of formula (I) which is an useful building block for the synthesis of taxane derivatives. The process involves the resolution of racemic threo-phenylisoserine amide and its conversion into (I).

摘要翻译： 用于对映选择性制备式（I）的（2R，3S）-3-苯基异丝氨酸甲酯乙酸盐的方法，其是用于合成紫杉烷衍生物的有用的结构单元。 该方法涉及拆分外消旋的苏氨基苯基异丝氨酰胺及其转化为（I）。

公开(公告)号：US20090298926A1

公开(公告)日：2009-12-03

申请号：US11918283

申请日：2006-04-07

申请人： Bruno Gabetta ,  Andrea Gambini

发明人： Bruno Gabetta ,  Andrea Gambini

IPC分类号： A61K31/337 ,  C07D305/14

CPC分类号： C07D305/14 ,  Y02P20/55

摘要： A process for the preparation of 10-deacetyl-7,10-bis-trichloroacetylbaccatine III with HPLC purity higher than 99% and free from 2-debenzoyl-2-pentenoylbaccatine III by purification of 10-deacetyl-7,10-bis-trichloroacetylbaccatineIII followed by alkaline hydrolysis of the protecting groups in position 7 and 10.

摘要翻译： 一种通过纯化10-脱乙酰-7,10-双 - 三氯乙酰基巴卡星III制备HPLC-纯度高于99％且不含2-脱苯甲酰基-2-戊烯酰基胞嘧啶III的10-脱乙酰-7,10-双 - 三氯乙酰基浆果赤霉素III的方法 然后碱性水解7和10位的保护基。

公开(公告)号：US5200186A

公开(公告)日：1993-04-06

申请号：US562216

申请日：1990-08-03

申请人： Bruno Gabetta ,  Gianfranco Zini

发明人： Bruno Gabetta ,  Gianfranco Zini

IPC分类号： C07H1/08 ,  A61K36/18 ,  A61K36/45 ,  C07B63/02 ,  C07H17/065

CPC分类号： C07H17/065

摘要： A process for the preparation of extracts with high content in anthocyanosides consists in treating plants, parts of plants or crude extracts with bisulfite ions to give anthocyanoside-bisulfite adducts. Said adducts are then eluted on non ionogenic resins at pH 5-6 and the obtained solution is extracted with polar organic solvents immiscible in water. The obtained extracts have a constant and standardized composition in anthocyanosides.

公开(公告)号：US4925870A

公开(公告)日：1990-05-15

申请号：US356895

申请日：1989-05-25

申请人： Bruno Gabetta ,  Maria J. Magistretti ,  Philippe Dostert

发明人： Bruno Gabetta ,  Maria J. Magistretti ,  Philippe Dostert

IPC分类号： A61K31/35 ,  A61P1/04 ,  A61P3/06 ,  A61P9/14 ,  A61P43/00 ,  C07D493/18

CPC分类号： C07D493/18 ,  A61K31/35 ,  A61K36/77 ,  A61K9/4858 ,  A61K2236/00 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0056 ,  Y10S514/926 ,  Y10S514/927

摘要： There is described a process for preparing proanthocyanidine A2 by extraction from cortex or fruits of Aesculus hippocastanum and related species and its activity for stimulating healing processes, e.g. healing wounds and injuries of various origins, gastric and duodenal ulcers for modifying conditions of impaired capillary permeability and resistance and for obtaining an anti-lipid peroxidation effect.There are also described pharmaceutical formulations suitable for use by topical and systemic routes.

公开(公告)号：US08742080B2

公开(公告)日：2014-06-03

申请号：US12994485

申请日：2009-04-09

申请人： Stephen Beszant ,  Bruno Gabetta

发明人： Stephen Beszant ,  Bruno Gabetta

IPC分类号： C07H15/248

CPC分类号： C07H15/248 ,  C07C231/12 ,  C07C319/20 ,  C07C2603/34 ,  Y02P20/55 ,  C07C323/41 ,  C07C233/25

摘要： A process for the preparation of compounds having formula (I) is disclosed, wherein: —R1 is a methoxy or methylthio group; —R2 is a O-glycosyloxy residue. Compounds having formula (I) are prepared by reacting the corresponding precursor having R2═OH and the suitably protected 1-acetyl-glycose.

摘要翻译： 公开了制备具有式（I）的化合物的方法，其中：-R1是甲氧基或甲硫基; -R2是O-糖氧基残基。 具有式（I）的化合物通过使具有R2 = OH的相应前体和适当保护的1-乙酰 - 糖苷反应来制备。