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1. 发明专利

JP2012136544A Process for producing docetaxel, and medicine 有权
标题翻译：生产DOCETAXEL和药物的方法
公开(公告)号：JP2012136544A
公开(公告)日：2012-07-19
申请号：JP2012045438
申请日：2012-03-01
申请人： Indena Spa , インデナエッセピア
发明人： GABETTA BRUNO , GAMBINI ANDREA , BOMBARDELLI EZIO , FONTANA GABRIELE
IPC分类号： C07D305/14 , A61K31/337 , A61P35/00
CPC分类号： C07D413/12 , C07D305/14
摘要： PROBLEM TO BE SOLVED: To provide docetaxel having high purity.SOLUTION: The process comprises: producing 10-deacetyl-7,10-bis-trichloroacetylbaccatin III (VI) having small content of 7- or 10-mono-trichloroacetyl, so as to be 10-deacetyl-N-debenzoyl-paclitaxel (I); and reacting the 10-deacetyl-N-debenzoyl-paclitaxel (I) with di-tert-butyl dicarbonate to obtain the docetaxel having high purity.
摘要翻译：要解决的问题：提供高纯度的多西紫杉醇。解决方案：该方法包括：制备具有少量含量为7-或10-单 - 三氯乙酰基的10-脱乙酰-7,10-双 - 三氯乙酰基浆果赤霉素Ⅲ（Ⅵ），以制备10-脱乙酰基-N-脱苯甲酰基 - 紫杉醇（I）; 并使10-脱乙酰基-N-脱苯甲酰基 - 紫杉醇（I）与二碳酸二叔丁酯反应，得到高纯度的多西紫杉醇。版权所有（C）2012，JPO＆INPIT

2. 发明专利

JP2003002838A Soybean extract, preparation method therefor and pharmaceutical composition 审中-公开
标题翻译：大豆提取物，其制备方法和药物组合物
公开(公告)号：JP2003002838A
公开(公告)日：2003-01-08
申请号：JP2002120590
申请日：2002-04-23
申请人： Indena Spa , インデナエッセピア
发明人： BOMBARDELLI EZIO , GABETTA BRUNO
IPC分类号： A61K31/704 , A61K20060101 , A61K9/64 , A61K31/7048 , A61K36/00 , A61K36/48 , A61K131/00 , A61P20060101 , A61P5/00 , A61P13/08 , A61P15/00 , A61P15/12 , A61P25/32 , A61P31/00 , A61P35/00 , A61P35/02 , B01D11/02 , C07D311/04 , C07G11/00 , C07H15/00 , C07H17/07 , C07J1/00 , C07K1/14 , A61K35/78
CPC分类号： A61K36/48 , Y10S514/811 , Y10S514/899
摘要： PROBLEM TO BE SOLVED: To obtain a new soybean extract containing soybean saponin in a predetermined proportion to isoflavone glucoside, a preparation method therefor and a pharmaceutical composition containing the extract.
SOLUTION: The soybean extract contains isoflavone glucoside of at least 13 wt.% and a group B soybean saponin of 0.6-1.5 pts.wt. with respect to isoflavone glucoside of 1 pt.wt. The preparation method for producing the extract and the pharmaceutical preparation containing the extract for treating cancers, or the like, are also provided.
COPYRIGHT: (C)2003,JPO
摘要翻译：要解决的问题：为了获得含有大豆皂甙的新的大豆皂甙，其规定比例为异黄酮糖苷，其制备方法和含有提取物的药物组合物。解决方案：大豆提取物含有至少13重量％的异黄酮糖苷和0.6-1.5重量份的B组大豆皂角苷。相对于1重量％的异黄酮糖苷还提供了用于制备提取物的制备方法和含有用于治疗癌症的提取物的药物制剂等。

3. 发明专利

JP2010209099A Method for producing ferutinine from ferula genus plant 有权
标题翻译：从产地植物生产弗氏真菌的方法
公开(公告)号：JP2010209099A
公开(公告)日：2010-09-24
申请号：JP2010106573
申请日：2010-05-06
申请人： Indena Spa , インデナエッセピア
发明人： BOMBARDELLI EZIO , FONTANA GABRIELE , CRISTONI ALDO , MERCALLI ENRICO
IPC分类号： C07C67/31 , A61K8/37 , A61K8/97 , A61K31/235 , A61K36/23 , A61P17/00 , A61Q19/08 , C07C67/08 , C07C67/30 , C07C69/84
CPC分类号： C07C67/08 , A61K8/375 , A61K8/97 , A61Q19/08 , C07C67/30 , C07C67/31 , C07C2602/30 , C07C69/86 , C07C69/84
摘要： PROBLEM TO BE SOLVED: To provide a method for producing ferutinine (Ia) usable in the cosmetic and dermatological field. SOLUTION: Ferutinine (Ia) usable in the cosmetic and dermatological field is produced from Ferula spp extracts by carrying out basic hydrolysis of the extracts and treatment with p-pivaloyloxybenzoic acid. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供可用于化妆品和皮肤病学领域中的制备氟尿嘧啶（Ia）的方法。解决方案：可用于化妆品和皮肤病学领域的Ferutinine（Ia）通过进行提取物的碱性水解并用对新戊酰氧基苯甲酸处理从Ferula spp提取物产生。版权所有（C）2010，JPO＆INPIT

4. 发明专利

JP2004131509A Chalcone complex having antiproliferation activity against tumors of uterine, ovarian and mammary 审中-公开
公开(公告)号：JP2004131509A
公开(公告)日：2004-04-30
申请号：JP2003434456
申请日：2003-12-26
申请人： Indena Spa , インデナ・ソチエタ・ペル・アチオニ
发明人： BOMBARDELLI EZIO , MANCUSO SALVATORE , DELLE MONACHE FRANCO
IPC分类号： A61K31/66 , A61K31/12 , A61K31/121 , A61K31/215 , A61K31/23 , A61K47/24 , A61P35/00 , A61P43/00 , C07C49/248 , C07C49/82 , C07C69/017 , C07C69/157 , C07C69/16 , C07C69/24 , C07C69/28 , C07C69/52 , C07C69/533 , C07F9/10
CPC分类号： A61K31/12 , C07C69/017
摘要： PROBLEM TO BE SOLVED: To provide a chalcone complex having antitumor activity.
SOLUTION: It is the complex of a natural or synthetic phosphatide with a compound selected from the group consisting of isocordoin, cordoin, 4-hydroxyderricin, 2-hydroxyderricin, 3-hydroxyderricin, 2',4'-dihydroxychalcone and 4,2',4'-trihydroxychalcone. The complex has actions such as significantly inhibiting proliferation of mammary cancer.
COPYRIGHT: (C)2004,JPO

5. 发明专利

JP2002187848A POLYPHENOL FRACTION FROM TEA, USE THEREOF AND PREPARATION CONTAINING THE SAME 审中-公开
公开(公告)号：JP2002187848A
公开(公告)日：2002-07-05
申请号：JP2001306197
申请日：2001-10-02
申请人： INDENA SPA
发明人： BOMBARDELLI EZIO , MORAZZONI PAOLO , MUSTICH GIUSEPPE
IPC分类号： C07D311/62 , A23F3/16 , A23L1/30 , A61K8/33 , A61K8/49 , A61K8/96 , A61K8/97 , A61K9/08 , A61K9/10 , A61K9/20 , A61K9/48 , A61K31/353 , A61K36/00 , A61K36/18 , A61K36/82 , A61K127/00 , A61P9/00 , A61P9/10 , A61P19/02 , A61P35/00 , A61P39/02 , A61P39/06 , A61Q19/00 , B01D11/04 , A61K35/78 , A61K7/00
摘要： PROBLEM TO BE SOLVED: To provide a novel polyphenol fraction of tea (Camellia sinensis). SOLUTION: The objective polyphenol fraction of tea is obtained via the process for extracting the polyphenol fraction of Camellia sinensis including

6. 发明专利

JP2011079853A Formulation useful in treatment of male and female impotence 审中-公开
标题翻译：配方用于治疗男性和女性的不便
公开(公告)号：JP2011079853A
公开(公告)日：2011-04-21
申请号：JP2010269123
申请日：2010-12-02
申请人： Indena Spa , インデナ・ソチエタ・ペル・アチオニ
发明人： BOMBARDELLI EZIO , MORAZZONI PAOLO , RIVA ANTONELLA , SEGHIZZI ROBERTO
IPC分类号： A61K31/352 , A61K36/00 , A61J3/06 , A61J3/07 , A61K31/11 , A61K31/198 , A61K31/704 , A61K31/7048 , A61K36/10 , A61K36/18 , A61K36/185 , A61K36/29 , A61K36/296 , A61K36/54 , A61P15/00 , A61P15/08 , A61P15/10
CPC分类号： A61K31/198 , A61K31/11 , A61K31/192 , A61K31/70 , A61K36/185 , A61K36/296 , A61K36/54 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide a composition which is useful in treatment of male and female sexual dysfunction.
SOLUTION: A pharmaceutical composition includes extracts of Tribulus terrestris, Epimedium koreanum and Cinnamon cassia in weight ratio of 1.5-3.5:1-2:0.1-0.4 respectively, and optionally arginine or a physiologically equivalent ester, a salt or a precursor of the same.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供可用于治疗男性和女性性功能障碍的组合物。解决方案：药物组合物分别包括枸杞提取物，韩文淫羊藿和肉桂肉桂重量比分别为1.5-3.5：1-2：0.1-0.4，以及任选的精氨酸或生理学上等同的酯，盐或前体一样的。版权所有（C）2011，JPO＆INPIT

7. 发明专利

JP2010265274A Semi-synthetic method for production of n-debenzoylpaclitaxel 审中-公开
标题翻译：用于生产N-取代苯并噻唑的半合成方法
公开(公告)号：JP2010265274A
公开(公告)日：2010-11-25
申请号：JP2010137314
申请日：2010-06-16
申请人： Indena Spa , インデナ・ソチエタ・ペル・アチオニ
发明人： BOMBARDELLI EZIO , FONTANA GABRIELE
IPC分类号： C07D305/14 , C07B51/00 , C07B61/00 , C07C313/24 , C07D263/04 , C07D263/06 , C07D413/12
CPC分类号： C07D413/12 , C07D263/06 , C07D305/14 , Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide a new method for producing N-debenzoylpaclitaxel which is a precursor of paclitaxel having antitumor activity. SOLUTION: The method includes condensation of a carboxylic acid expressed by formula (II) (in the formula, R1 is aryl or heteroaryl), its salt or its activated derivative with a 7-protected baccatin, and solvolysis of the obtained condensed compound with an acid catalyst to remove a part of the protective groups and open the oxazoline ring. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供一种新的具有抗肿瘤活性的紫杉醇前体的N-脱苯甲酰紫杉醇的制备方法。解决方案：该方法包括由式（II）表示的羧酸（在式中，R1是芳基或杂芳基），其盐或其活化衍生物与7-保护的浆果赤霉素的缩合，以及所得缩合的与酸催化剂混合以除去一部分保护基团并打开恶唑啉环。版权所有（C）2011，JPO＆INPIT

8. 发明专利

JP2007137898A 10-DEACETYLBACCATINE III AND 10-DEACETYL 14β-HYDROXYBACCATINE III DERIVATIVE, PROCESS FOR PRODUCING THE SAME AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME 审中-公开
标题翻译： 10-脱乙酰胆碱酯酶III和10-脱乙酰基-β-羟基卡必汀III衍生物，其制备方法和含有其的药物组合物
公开(公告)号：JP2007137898A
公开(公告)日：2007-06-07
申请号：JP2007049738
申请日：2007-02-28
申请人： Indena Spa , インデナ・ソチエタ・ペル・アチオニ
发明人： BOMBARDELLI EZIO , DE BELLIS PAOLO , GABETTA BRUNO
IPC分类号： C07D305/14 , A61K31/335 , A61K31/337 , A61P35/00 , C07D263/04 , C07D263/06 , C07D493/10 , C07F7/18
CPC分类号： C07D263/04 , C07D305/14 , C07D493/10 , C07F7/1856
摘要： PROBLEM TO BE SOLVED: To provide new derivatives of 10-deacetylbaccatine III and 10-deacetyl 14β-hydroxybaccatine III having cytotoxicity and antitumor activity.
SOLUTION: The derivatives are prepared starting from the so-called syntons or from other taxanes of natural origin by the selective oxidation of the hydroxyl in position 10 to keto functional group and, if necessary, subsequent esterification in position 13 with variously substituted isoserine chains. The products of the invention can be administered, when suitably formulated, by injection or oral administration.
COPYRIGHT: (C)2007,JPO&INPIT
摘要翻译：要解决的问题：提供具有细胞毒性和抗肿瘤活性的10-脱乙酰基巴豆苷III和10-脱乙酰基14β-羟基浆果甘油三酯的新衍生物。解决方案：通过选择性氧化10位羟基至酮官能团，如果需要，随后在不同取代的位置13进行酯化，衍生物从所谓的合成物或天然来源的其他紫杉烷开始制备异丝氨酸链。当适当配制时，本发明的产品可以通过注射或口服施用。版权所有（C）2007，JPO＆INPIT

9. 发明专利

JP2010270145A Taxane derivative functionalized at the 14-position, and method for production thereof 审中-公开
标题翻译：在14位置实施的TAXANE衍生功能及其生产方法
公开(公告)号：JP2010270145A
公开(公告)日：2010-12-02
申请号：JP2010172650
申请日：2010-07-30
申请人： Indena Spa , インデナ・ソチエタ・ペル・アチオニ
发明人： FONTANA GABRIELE , BOMBARDELLI EZIO , BATTAGLIA ARTURO , BALDELLI ELENORA , GUERRINI ANDREA , GELMI MARIA LUISA , CARENZI GIACOMO , POCAR DONATO
IPC分类号： C07D305/14 , A61K31/337 , A61K31/422 , A61P35/00 , C07D413/12
CPC分类号： C07D305/14 , Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide a novel 13-ketobaccatin III, a taxane derivative and a method for production thereof.
SOLUTION: The method for production of the taxane derivative includes functionalizing the 14-position of a 13-ketobaccatin derivative, and further converting into a compound of formula III (wherein X is -N
3 , -NH
2 , -NH-R
3 , =CH-R
8 , or -O-R
3 when R
6 is different from phenyl; R
2 is hydrogen or acyl; R
3 is 1-4C alkoxycarbonyl, or taken together with R
4 to form carbonyl, thiocarbonyl, SO or SO
2 ; R
4 is hydrogen or taken together with R
3 or R
8 to form the groups specified in the respective definitions of R
3 and R
8 ; R
5 is hydrogen or an alcohol-protecting group; R
6 is aryl, substituted aryl, heteroaryl, with the proviso that it is different from phenyl when X is OR
3 ; R
8 is hydrogen, 1-4C alkyl, 1-4C alkoxycarbonyl, or taken together with R
4 to form carbonyl; and R
9 is acyl or hydroxyaminoacyl).
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供一种新型的13-酮糊豆素III，一种紫杉烷衍生物及其生产方法。解决方案：制备紫杉烷衍生物的方法包括使13-酮缩糊蛋白衍生物的14位官能化，并进一步转化为式III化合物（其中X为-N 3 SB 3，，-NH-R SB 3，= CH-R SB 8或-SOR 3，当R 苯乙烯不同于苯基; R SB 2是氢或酰基; R SB 3是1-4C烷氧基羰基，或与R SB一起使用， 4 以形成羰基，硫代羰基，SO或SO 2 SB; R SB 4是氢或与R 3或R 3一起， SB> 8 以形成在R SB 3和R SB 8的各自定义中指定的基团; R SB 5是氢或醇保护基; R 6是芳基，取代的芳基，杂芳基，条件是当X是OR时，它不同于苯基; R 8 < / SB>是氢，1-4C烷基，1-4C烷氧基羰基，或与R SB 4一起形成羰基; R SB 9是酰基或羟基氨基酰基）。版权所有（C）2011，JPO＆INPIT

10. 发明专利

JPH11322737A ANTITUMOR COMPOUND AND ITS PREPARATION 失效
公开(公告)号：JPH11322737A
公开(公告)日：1999-11-24
申请号：JP10293599
申请日：1999-04-09
申请人： UNIV NEW YORK , INDENA SPA
发明人： OJIMA IWAO , BOMBARDELLI EZIO
IPC分类号： A61K31/00 , A61K31/335 , A61K31/337 , A61P35/00 , C07D205/08 , C07D305/14 , C07F7/18
摘要： PROBLEM TO BE SOLVED: To obtain a new antitumor compound having strong antitumor activity against human breast cancer cell, non-small cell lung cancer cell, ovarian cancer cell and colon carcinoma cell. SOLUTION: This compound is shown by formula I (R is an alkyl, an alkenyl or the like; R is an alkyl, a cycloalkyl or the like; R , R and R are each H, an acyl or the like; R is a 1-20C acyl; R is H or a hydroxyl protecting group) such as (-)(1R,2S)-2-phenyl-1-cyclohexyltriisopropylsilyloxyacetate. The compound of formula I is obtained by subjecting a baccatin of formula II (G1 , G2 and G4 are each an acyl, an alkyl or the like) and a β-lactam of formula III (G is methoxymethyl, methoxyethyl or the like) in the presence of a base (e.g. sodium hexamethyldisilazide or the like) preferably at a temp. of -50 to 25 deg.C in an inert gas atmosphere to deprotect a hydroxyl protecting group. The ratio of the β-lactam to the baccatin is preferably 1:1.

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