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1. 发明授权

EP2406242B1 PROCESS FOR THE PREPARATION OF RAMELTEON 有权
标题翻译：用于生产拉米替隆
公开(公告)号：EP2406242B1
公开(公告)日：2013-06-05
申请号：EP09787661.9
申请日：2009-03-10
申请人： Industriale Chimica S.R.L.
发明人： LENNA, Roberto , GHIDOLI, Cristina , PANZA, Luigi
IPC分类号： C07D307/77 , C07F7/18
CPC分类号： C07D307/77 , C07F7/1856

2. 发明公开

EP2597101A1 Process for the preparation of drospirenone 审中-公开
标题翻译：制备屈螺酮的方法
公开(公告)号：EP2597101A1
公开(公告)日：2013-05-29
申请号：EP11190133.6
申请日：2011-11-22
申请人： Industriale Chimica S.R.L.
发明人： Lenna, Roberto , Vanossi, Andrea
IPC分类号： C07J75/00
CPC分类号： C07J53/008
摘要： It is described a process for the preparation of Drospirenone, a synthetic steroid with progestogenic anti-mineralocorticoid and antiandrogenic activity having the formula 1 shown below, useful in the preparation of contraceptive pharmaceutical compositions, starting from 17α-(3-hydroxypropyl)-6β,7β;15β,16β-dimethylene-5β-androstan-3β,5,17β-triol.
摘要翻译：描述了制备屈螺酮的方法，所述屈螺酮是一种具有下述式1的孕激素抗盐皮质激素和抗雄激素活性的合成类固醇，可用于制备避孕药物组合物，起始于17α-（3-羟丙基）-6β， 7β;15β，16β - 二亚甲基 - 5β雄烷-3β，5,17β三醇。

3. 发明授权

EP1571153B1 A process for the preparation of drospirenone 有权
标题翻译：阿屈螺酮的制备方法
公开(公告)号：EP1571153B1
公开(公告)日：2010-11-03
申请号：EP05101511.3
申请日：2005-02-28
申请人： INDUSTRIALE CHIMICA S.r.l.
发明人： Costantino, Francesca , Lenna, Roberto , Piuri, Silvia
IPC分类号： C07J53/00 , C07J71/00
CPC分类号： C07J53/008

4. 发明公开

EP1828222A1 PROCESS FOR THE PREPARATION OF DROSPIRENONE 有权
标题翻译：用于生产屈螺酮
公开(公告)号：EP1828222A1
公开(公告)日：2007-09-05
申请号：EP05819134.7
申请日：2005-11-14
申请人： INDUSTRIALE CHIMICA S.r.l.
发明人： COSTANTINO, Francesca , LENNA, Roberto , PIURI, Silvia
IPC分类号： C07J53/00 , A61K31/585 , A61P15/18
CPC分类号： C07J53/008
摘要： A process is described for the preparation of drospirenone, a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic activity, useful for preparing pharmaceutical compositions with contraceptive action; comprising the oxidation of 17α-(3-hydroxypropyl)-6β, 7β, 15β, 16β-dimethylene-5β-androstane- 3β , 5, 17β -triol.

5. 发明授权

EP0915874B1 PROCESS OF PREPARATION OF VALACYCLOVIR AND RELEVANT INTERMEDIATES 失效
标题翻译：用于生产之间的伐昔洛韦和相关连结
公开(公告)号：EP0915874B1
公开(公告)日：2003-12-10
申请号：EP97937496.4
申请日：1997-07-17
申请人： INDUSTRIALE CHIMICA S.r.l.
发明人： MONTORO, Maurizio , PIROVANO, Silvio
IPC分类号： C07D473/00 , A61K31/52
CPC分类号： C07D473/18
摘要： Process of preparation of valacyclovir (I), wherein derivative (IV) of acyclovir (I), in which the OH group of acyclovir at the omega position has been replaced by a good leaving group Z, is reacted with an alkaline salt of L-valine (V), to give intermediate (VI), which is successively hydrolyzed in an acid medium to give the corresponding salified valacyclovir (I-A), which may be optionally transformed into valacyclovir (I).

6. 发明公开

EP0700926A1 Process for the preparation of gestodene 失效
标题翻译： Verfahren zur Herstellung von Gestoden
公开(公告)号：EP0700926A1
公开(公告)日：1996-03-13
申请号：EP95112768.7
申请日：1995-08-14
申请人： INDUSTRIALE CHIMICA S.r.l.
发明人： Prendin, Rino , Pirovano, Silvio
IPC分类号： C07J1/00 , C07J21/00
CPC分类号： C07J21/006 , C07J1/007 , C07J1/0096
摘要： Process for preparing Gestodene from (-)estra-1,3,5(10),8-tetraen-3-methoxy-18-methyl-17β-hydroxy, comprising the following steps:

a) hydrogenation of the double bond in 8(Li in liquid NH₃ in presence of aniline);
b) hydrogenation of a double bond of the aromatic ring (Li in liquid NH₃ in presence of ter.butanol);
c) hydrolysis of the methoxyl in 3 with introduction of a ketonic group and transposition of the double bond from 5-10 to 4-5;
d) conversion of the ketonic group in 3 to acetalic group and transposition of the double bond from 4-5 to 5-6 (or 5-10);
e) oxydation of the hydroxyl in 17 to a ketonic group;
f) formation of a double bond in 15-16 by oxidation with Pd(II) acetate after transformation to sililenolether;
g) ethynylation in position 17 with Li acetilide;
h) hydrolysis of the acetalic group of position 3.
摘要翻译：由（ - ）雌-1,3,5（10），8-四烯-3-甲氧基-18-甲基-17β-羟基制备孕二烯的方法，包括以下步骤：a）在8 （Li在苯胺存在下为液态NH 3）; b）芳环的双键氢化（在叔丁醇存在下，Li在液体NH 3中）; c）引入酮基时，3位甲氧基的水解，双键的转置从5-10到4-5; d）将酮基转化为3至缩醛基团并将双键转置从4-5至5-6（或5-10）; e）17中的羟基氧化成酮基; f）在转化成硅烯醇后，通过用Pd（II）乙酸酯氧化形成15-16中的双键; g）使用Li-乙酰苯胺在位置17的乙炔化; h）位置3的缩醛基团的水解。

7. 发明授权

EP2892909B1 PROCESS FOR THE PREPARATION OF 11-METHYLENE-18-METHYLESTR-4-EN-3,17-DIONE, USEFUL AS AN INTERMEDIATE IN THE SYNTHESIS OF COMPOUNDS WITH PHARMACOLOGICAL ACTIVITY. 有权
标题翻译：用于生产-11-亚甲基-18-甲基雌-4- EN -3,17- DION，USED中间体分子与营销动作合成
公开(公告)号：EP2892909B1
公开(公告)日：2016-08-24
申请号：EP13777150.7
申请日：2013-09-03
申请人： Industriale Chimica S.R.L.
发明人： LENNA, Roberto , MARIANI, Edoardo , VANOSSI, Andrea
IPC分类号： C07J21/00 , C07J1/00
CPC分类号： C07J21/006 , C07J1/0059 , C07J1/007

8. 发明公开

EP3009443A1 PROCESS FOR THE PREPARATION OF 7ALFA-(METHOXYCARBONYL)-3-OXO-17ALFA-PREGN-4,9(11)-DIEN-21,17-CARBOLACTONE, A USEFUL INTERMEDIATE FOR THE SYNTHESIS OF MOLECULES WITH PHARMACOLOGICAL ACTIVITY 有权
标题翻译：用于生产7ALFA-（甲氧羰基）-3-氧代17α-乙烯孕甾-4,9（11）二烯21,17羧内酯，有用的中间体分子与药理作用合成
公开(公告)号：EP3009443A1
公开(公告)日：2016-04-20
申请号：EP15190131.1
申请日：2015-10-16
申请人： INDUSTRIALE CHIMICA S.r.l.
发明人： LENNA, Roberto , DI BRISCO, Riccardo , BARBIERI, Francesco
IPC分类号： C07J21/00
CPC分类号： C07J21/003
摘要： An improved process for the preparation of intermediate (V) through the elimination of a molecule of water from intermediate (IV) is described.

Intermediate (V) is a key molecule for the synthesis of eplerenone, a synthetic steroid with pharmacological activity used in the treatment of chronic pathological conditions, including hypertension.
摘要翻译：用于通过水分子的从中间体（IV）中描述了消除制备中间体（V）的改进方法。中间体（V）为依普利酮的合成，合成的类固醇具有在慢性病理条件，包括用来治疗高血压药理学活性中的关键分子。

9. 发明公开

EP2892909A1 PROCESS FOR PREPARING 11 -METHYLENE-18-METHYL-ESTR-4-EN-3, 17- DIONE, USEFUL AS INTERMEDIATE COMPOUND FOR THE SYNTHESIS OF MOLECULES HAVING A PHARMACOLOGICAL ACTIVITY 有权
标题翻译：用于生产-11-亚甲基-18-甲基雌-4- EN -3,17- DION，USED中间体分子与营销动作合成
公开(公告)号：EP2892909A1
公开(公告)日：2015-07-15
申请号：EP13777150.7
申请日：2013-09-03
申请人： Industriale Chimica S.R.L.
发明人： LENNA, Roberto , MARIANI, Edoardo , VANOSSI, Andrea
IPC分类号： C07J21/00 , C07J1/00
CPC分类号： C07J21/006 , C07J1/0059 , C07J1/007
摘要： There is described a process for the industrial synthesis of 11-methylene-18- methyl-estr-4-en-3, 17-dione, a compound having the structure formula (I) depicted below: (Formula I) (I) useful as intermediate compound in the synthesis of the progestin compounds Desogestrel and Etonogestrel.

10. 发明公开

EP2890705A1 PROCESS FOR THE PREPARATION OF ABIRATERONE OR ABIRATERONE ACETATE 有权
标题翻译： VERFAHREN ZUR HERSTELLUNG VON ABIRATERON ODER ABIRATERONACETAT
公开(公告)号：EP2890705A1
公开(公告)日：2015-07-08
申请号：EP14755340.8
申请日：2014-07-23
申请人： Industriale Chimica S.R.L.
发明人： LENNA, Roberto , DI BRISCO, Riccardo
IPC分类号： C07J31/00 , C07J43/00
CPC分类号： C07J43/003 , C07J31/006
摘要： The present invention relates to a novel process for the synthesis of abiraterone and in particular abiraterone acetate, a compound of formula (I) reported below: having pharmacological activity suitable for slowing down the progression of advanced stage prostate cancer. The process is characaterised by the fact that the intermediate triflation step is carried out on prasterone (DHEA) or its 3-acetate using Ar-N(OTf)
2 as the triflation reagent, but where Ar is not phenyl, and by the fact that the base used in this step is an alkali metal alcoholate.
摘要翻译：本发明涉及一种用于合成阿维酮酮，特别是乙酸阿比酮酮，下文所述的式（I）化合物的新方法：具有适于减缓晚期前列腺癌进展的药理学活性。该方法的特征在于，使用Ar-N（OTf）2作为三氟化试剂，但是Ar不是苯基，并且通过以下事实，中间三价相通步骤在prasterone（DHEA）或其3-乙酸酯上进行，该步骤中使用的碱是碱金属醇化物。

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