公开(公告)号：US5856482A

公开(公告)日：1999-01-05

申请号：US957976

申请日：1997-10-21

申请人： Vincenzo Cannata ,  Tiziano Ferrario ,  Barbara Galbiati

发明人： Vincenzo Cannata ,  Tiziano Ferrario ,  Barbara Galbiati

IPC分类号： C07D405/12 ,  C07D405/14

CPC分类号： C07D405/12

摘要： The process for the production of the form I of the terazosin monohydrochloride anhydrous consists of treating at the boiling temperature terazosin monohydrochloride dihydrate with a mixture of methanol and a solvent selected from C.sub.2 -C.sub.6 straight or branched alcohols, the esters of the C.sub. -C.sub.8 carboxylic aliphatic acids with C.sub.1 -C.sub.8 straight or branched alcohols, C.sub.3 to C.sub.8 aliphatic ketones, C.sub.4 to C.sub.8 straight, branched or cyclic aliphatic ethers, aliphatic amides and the aliphatic nitriles.

摘要翻译： 制备特拉唑嗪单盐酸盐的形式I的方法包括在沸腾温度下用特拉唑斯单盐酸盐二水合物与甲醇和选自C 2 -C 6直链或支链醇的溶剂的混合物处理，C-C8羧酸酯 具有C1-C8直链或支链醇的脂族酸，C3至C8脂族酮，C4至C8直链，支链或环状脂族醚，脂族酰胺和脂族腈。

公开(公告)号：US5760220A

公开(公告)日：1998-06-02

申请号：US657490

申请日：1996-06-04

申请人： Pierre Giguere ,  Silvio Iera ,  Michel Bernatchez ,  Giuseppe Barreca ,  Graziano Castaldi ,  Vincenzo Cannata

发明人： Pierre Giguere ,  Silvio Iera ,  Michel Bernatchez ,  Giuseppe Barreca ,  Graziano Castaldi ,  Vincenzo Cannata

IPC分类号： C07D471/04 ,  C07D257/04 ,  C07D487/04

CPC分类号： C07D471/04 ,  Y02P20/55

摘要： A process is described for preparing a compound of the formula I: ##STR1## or a salt thereof; wherein X is a protecting group and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen, C.sub.1-6 alkyl or C.sub.1-6 perfluoroalkyl, R.sub.5 is hydrogen or when n is 1 R.sub.5 taken together with R.sub.3 comprises a double bond; m is 1, 2 or 3; n is 0 or 1, and p is 0, 1 or 2.

摘要翻译： 描述了制备式I化合物或其盐的方法： 其中X是保护基，R 1，R 2，R 3和R 4各自独立地是氢，C 1-6烷基或C 1-6全氟烷基，R 5是氢或当n是1时，R 5与R 3一起包括双键; m为1,2或3; n为0或1，p为0,1或2。

公开(公告)号：US5550287A

公开(公告)日：1996-08-27

申请号：US397955

申请日：1995-03-03

申请人： Vincenzo Cannata ,  Valeriano Merli ,  Claudio Dal Santo

发明人： Vincenzo Cannata ,  Valeriano Merli ,  Claudio Dal Santo

IPC分类号： A61K49/04 ,  B01D15/08 ,  C07C231/12 ,  C07C231/22 ,  C07C231/24 ,  C07C233/05 ,  C07C237/46

CPC分类号： C07C231/12 ,  C07C231/24 ,  C07C237/46

摘要： A process for the preparation and purification of L-5-(2-hydroxypropionylamino)-2,4,6-triiodoisophthalic acid bis-(1,3-dihydroxypropylamide) by using ion-exchange resins is described.

摘要翻译： 描述了使用离子交换树脂制备和纯化L-5-（2-羟基丙酰基氨基）-2,4,6-三碘代邻苯二甲酸双 - （1,3-二羟丙基酰胺）的方法。

公开(公告)号：US5107013A

公开(公告)日：1992-04-21

申请号：US634742

申请日：1990-12-27

申请人： Vincenzo Cannata ,  Claudio Calzolari ,  Giancarlo Tamerlani

发明人： Vincenzo Cannata ,  Claudio Calzolari ,  Giancarlo Tamerlani

IPC分类号： C07C45/46 ,  C07C45/65 ,  C07C51/377 ,  C07C69/734 ,  C07C231/12 ,  C07C255/37

CPC分类号： C07C255/37 ,  C07C231/12 ,  C07C45/46 ,  C07C45/65 ,  C07C51/377 ,  C07C69/734

摘要： Naphthalenes of formula ##STR1## wherein X represents COCH.sub.3, COC.sub.2 H.sub.5, CH(CH.sub.3)COOH, CH(CH.sub.3)COOR, CH(CH.sub.3)CN and CH(CH.sub.3)CONHR.sub.1, R represents alkyl and R.sub.1 represents hydrogen, alkyl or hydroxyalkyl, are debrominated by means of acceptors of bromine, like alkylarenes and alkoxyarenes, in the presence of Lewis acids.

公开(公告)号：US5097058A

公开(公告)日：1992-03-17

申请号：US512909

申请日：1990-04-25

申请人： Vincenzo Cannata ,  Giancarlo Tamerlani ,  Graziano Zagnoni

发明人： Vincenzo Cannata ,  Giancarlo Tamerlani ,  Graziano Zagnoni

IPC分类号： C07D301/02 ,  C07B61/00 ,  C07C45/00 ,  C07C45/58 ,  C07C47/277 ,  C07C67/00 ,  C07C239/00 ,  C07C249/08 ,  C07C251/36 ,  C07C251/40 ,  C07C253/00 ,  C07C255/37 ,  C07C255/53 ,  C07D303/48

CPC分类号： C07C255/00 ,  C07C45/58 ,  C07C47/277 ,  C07D303/48

摘要： New process for the synthesis of the .alpha.-(1-m.ethylethyl)-3,4-dimethoxyacetonitrile of formula (I): ##STR1## which is known as an intermediate in the synthesis of the drug internationally known as verapamil. The process starts from the isobutyryl-3,4-dimethoxybenzene of formula (II): ##STR2## which, by means of the Darzens condensation, gives an epoxyester which, by alkaline hydrolysis and subsequent decarboxylation, gives the .alpha.-(1-methylethyl)-3,4-dimethoxybenzeneacetaldehyde. This product is reacted with hydroxylamine to obtain the corresponding oxime that, by dehydration, gives the nitrile of formula I.

公开(公告)号：US5057624A

公开(公告)日：1991-10-15

申请号：US502038

申请日：1990-03-30

申请人： Vincenzo Cannata ,  Giancarlo Tamerlani ,  Graziano Zagnoni

发明人： Vincenzo Cannata ,  Giancarlo Tamerlani ,  Graziano Zagnoni

IPC分类号： C07C213/04 ,  C07C213/00 ,  C07C213/02 ,  C07C217/60

CPC分类号： C07C213/02 ,  C07C217/60

摘要： New process for the synthesis of the N-methyl-3,4-dimetoxyphenylethylamine of formula ##STR1## intermediate in the synthesis of the drug internationally known as verapamil. The process starts from the 3,4-dimethoxybenzaldehyde which, by means of a Darzens condensation, gives an epoxyester that, by alkaline hydrolysis and subsequent decarboxylation, gives the 3,4-dimethoxyphenylacetaldehyde. This aldehyde gives the amine of formula I by reaction with monomethylamine followed by reduction with sodium borohydride.

公开(公告)号：US20120203000A1

公开(公告)日：2012-08-09

申请号：US13448356

申请日：2012-04-16

申请人： Giuseppe Claudio Viscomi ,  Manuela Campana ,  Dario Braga ,  Donatella Confortini ,  Vincenzo Cannata ,  Paolo Righi ,  Goffredo Rosini

发明人： Giuseppe Claudio Viscomi ,  Manuela Campana ,  Dario Braga ,  Donatella Confortini ,  Vincenzo Cannata ,  Paolo Righi ,  Goffredo Rosini

IPC分类号： C07D491/22

CPC分类号： C07D498/22 ,  C07B2200/13 ,  C07D491/22

摘要： Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin α and rifaximin β, and a poorly crystalline form named rifaximin γ, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.

摘要翻译： 结晶多形态的利福昔明（INN）抗生素名为利福昔明α和利福昔明，并且结晶形式名为利福昔明γ，可用于生产含有利福昔明用于口服和局部使用的药物制剂，并通过结晶进行 将生的利福昔明热溶解在乙醇中，并通过在确定的温度下加入水并在一定的时间内引起产物的结晶，然后在受控条件下进行干燥，直到达到沉淀的含水量 最终产品是本发明的目的。

公开(公告)号：US08173801B2

公开(公告)日：2012-05-08

申请号：US13041346

申请日：2011-03-04

申请人： Giuseppe Claudio Viscomi ,  Manuela Campana ,  Dario Braga ,  Donatella Confortini ,  Vincenzo Cannata ,  Paolo Righi ,  Goffredo Rosini

发明人： Giuseppe Claudio Viscomi ,  Manuela Campana ,  Dario Braga ,  Donatella Confortini ,  Vincenzo Cannata ,  Paolo Righi ,  Goffredo Rosini

IPC分类号： C07D498/22

CPC分类号： C07D498/22

摘要： Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin α and rifaximin β, and a poorly crystalline form named rifaximin γ, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.

摘要翻译： 结晶多形态的利福昔明（INN）抗生素名为利福昔明α和利福昔明，并且结晶形式名为利福昔明γ，可用于生产含有利福昔明用于口服和局部使用的药物制剂，并通过结晶进行 将生的利福昔明热溶解在乙醇中，并通过在确定的温度下加入水并在一定的时间内引起产物的结晶，然后在受控条件下进行干燥，直到达到沉淀的含水量 最终产品是本发明的目的。

公开(公告)号：US08158644B2

公开(公告)日：2012-04-17

申请号：US13041347

申请日：2011-03-04

申请人： Giuseppe Claudio Viscomi ,  Manuela Campana ,  Dario Braga ,  Donatella Confortini ,  Vincenzo Cannata ,  Paolo Righi ,  Goffredo Rosini

发明人： Giuseppe Claudio Viscomi ,  Manuela Campana ,  Dario Braga ,  Donatella Confortini ,  Vincenzo Cannata ,  Paolo Righi ,  Goffredo Rosini

IPC分类号： A61K31/395

CPC分类号： C07D498/22 ,  A61K31/437 ,  C07B2200/13

摘要： Crystalline polymorphous forms of rifaximin (INN), referred to as rifaximin α and rifaximin β, and a poorly crystalline form referred to as rifaximin γ, useful in the production of medicaments containing rifaximin for oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a fixed temperature and for a fixed period of time, followed by a drying under controlled conditions until reaching a precise water content in the end product, are the object of the invention.

摘要翻译： 称为利福昔明（rifaximin）α和利福昔明（rifaximin）的结晶多晶形式，以及称为利福昔明γ的结晶不良形式，可用于生产含有利福昔明用于口服和局部使用并通过结晶获得的药物 通过将生的利福昔明热溶解在乙醇中并通过在固定温度下加入水而使产物结晶并持续一段时间进行，然后在受控条件下干燥直到达到精确的含水量 在最终产品中，是本发明的目的。

公开(公告)号：US20110152516A1

公开(公告)日：2011-06-23

申请号：US13041347

申请日：2011-03-04

申请人： Giuseppe Claudio Viscomi ,  Manuela Campana ,  Dario Braga ,  Donatella Confortini ,  Vincenzo Cannata ,  Paolo Righi ,  Goffredo Rosini

发明人： Giuseppe Claudio Viscomi ,  Manuela Campana ,  Dario Braga ,  Donatella Confortini ,  Vincenzo Cannata ,  Paolo Righi ,  Goffredo Rosini

IPC分类号： C07D498/22

CPC分类号： C07D498/22 ,  A61K31/437 ,  C07B2200/13

摘要： Crystalline polymorphous forms of rifaximin (INN), referred to as rifaximin α and rifaximin β, and a poorly crystalline form referred to as rifaximin γ, useful in the production of medicaments containing rifaximin for oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a fixed temperature and for a fixed period of time, followed by a drying under controlled conditions until reaching a precise water content in the end product, are the object of the invention.

摘要翻译： 称为利福昔明（rifaximin）α和利福昔明（rifaximin）的结晶多晶形式，以及称为利福昔明γ的结晶不良形式，可用于生产含有利福昔明用于口服和局部使用并通过结晶获得的药物 通过将生的利福昔明热溶解在乙醇中并通过在固定温度下加入水而使产物结晶并持续一段时间进行，然后在受控条件下干燥直到达到精确的含水量 在最终产品中，是本发明的目的。