专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2005073187A1 IMPROVED PROCESS FOR THE PREPARATION OF AMORPHOUS ATORVASTATIN CALCIUM 审中-公开
标题翻译：用于制备不定形ATORVASTATIN钙的改进方法
公开(公告)号：WO2005073187A1
公开(公告)日：2005-08-11
申请号：PCT/CA2004/002161
申请日：2004-12-20
申请人： APOTEX PHARMACHEM INC. , CHE, Daqing , KINSMAN, Aaron, C. , GUNTOORI, Bhaskar, Reddy , MURTHY, Keshava, K.S. , ZHAO, Yajun , HORNE, Stephen, E.
发明人： CHE, Daqing , KINSMAN, Aaron, C. , GUNTOORI, Bhaskar, Reddy , MURTHY, Keshava, K.S. , ZHAO, Yajun , HORNE, Stephen, E.
IPC分类号： C07D207/34
CPC分类号： C07D207/34
摘要： A process for the preparation of amorphous atorvastatin calcium which comprises: (a) hydrolysis of the atorvastatin lactone of formula II to form atorvastatin sodium salt solution; (b) addition of the atorvastatin sodium salt solution to an aqueous calcium chloride or calcium acetate solution; (c) isolation of the product; and (d) drying to afford amorphous atorvastatin calcium salt.
摘要翻译：一种制备无定形阿托伐他汀钙的方法，其包括：（a）水解式II的阿托伐他汀内酯以形成阿托伐他汀钠盐溶液; （b）将阿托伐他汀钠盐溶液加入到氯化钙水溶液或乙酸钙溶液中; （c）产品的隔离; 和（d）干燥以得到无定形的阿托伐他汀钙盐。

2. 发明申请

WO2005087723A1 AN IMPROVED PREPARATION OF ATORVASTATIN 审中-公开
标题翻译：改进ATORVASTATIN的制备
公开(公告)号：WO2005087723A1
公开(公告)日：2005-09-22
申请号：PCT/CA2005/000368
申请日：2005-03-11
申请人： APOTEX PHARMACHEM INC. , GUNTOORI, Bhaskar, Reddy , CHE, Daqing , WANG, Fan , ZHAO, Yajun , MURTHY, Keshava, K.S. , HORNE, Stephen, E.
发明人： GUNTOORI, Bhaskar, Reddy , CHE, Daqing , WANG, Fan , ZHAO, Yajun , MURTHY, Keshava, K.S. , HORNE, Stephen, E.
IPC分类号： C07D207/416
CPC分类号： C07D207/416 , C07D207/34
摘要： A process for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-l-heptanoic acid, tert-butylester comprising: (a) reduction of 5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4[(phenylamino)carbonyl]-1H-pyrrol-l-yl]-3-oxo-l-pentanoic acid, (R)-2-hydroxy1,2,2-triphenylethyl ester; (b) hydrolysis of (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-l-pentanoic acid, (R)-2hydroxy-1,2,2-triphenylethyl ester using an alkali base in a solvent to form the acid; (c) alkylation of the acid forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3phenyl-4-[(phenylamino)carbonyl]-1 H-pyrrol-1-yl]-5-hydroxy-3-oxo- l -heptanoic acid, tert-butylester.
摘要翻译：制备（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 [（苯基氨基）羰基] -1H-吡咯-1-基] -5- 包括：（a）还原5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 [（苯基氨基）羰基）-2-羟基-3-氧代-1-庚酸 ] -1H-吡咯-1-基] -3-氧代-1-戊酸，（R）-2-羟基-1,2,2-三苯乙基酯; （b）（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 [（苯基氨基）羰基] -1H-吡咯-1-基] -3 - 羟基-1-戊酸，（R）-2-羟基-1,2,2-三苯乙基酯，使用碱在溶剂中形成酸; （c）酸形成（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基吡啶-3-基] -5-羟基-3-氧代-1-庚酸叔丁酯。

3. 发明申请

WO2006092037A1 PROCESS FOR PRODUCING ATORVASTATIN HEMICALCIUM 审中-公开
标题翻译：生产ATORVASTATIN HEMICALCIUM的方法
公开(公告)号：WO2006092037A1
公开(公告)日：2006-09-08
申请号：PCT/CA2006/000190
申请日：2006-02-14
申请人： APOTEX PHARMACHEM INC. , MURTHY, K.S. Keshava , ZHAO, Yajun , CHE, Daqing , GUNTOORI, Bhaskar Reddy , DUNCAN, Sammy Chris , HORNE, Stephen, E.
发明人： MURTHY, K.S. Keshava , ZHAO, Yajun , CHE, Daqing , GUNTOORI, Bhaskar Reddy , DUNCAN, Sammy Chris , HORNE, Stephen, E.
IPC分类号： C07D207/34 , C07D405/06
CPC分类号： C07D207/34 , C07D405/06 , Y02P20/55
摘要： A process is provided for preparing pharmaceutical grade atorvastatin hemicalcium salt comprising: (a) deesterifying, (Formula I), wherein R is an ester protecting group to (Formula II), (b) extracting R(R*,R*)-3 into an organic solvent or mixture of solvents, (c) adding a base of formula NR 1 R 2 R 3 wherein R 1 , R 2 and R 3 are independently selected from H, substituted or non-substituted C1 to C7 alkyl, C6 to C9 aryl, C8 to C10 aralkyl or aminoalkyl to form atorvastatin base salt, (d) isolating by precipitation of the above atorvastatin base salt and purifying when necessary, (e) converting atorvastatin base salt to atorvastatin hemicalcium salt by treatment with a calcium salt solution, and (f) isolating the atorvastatin hemicalcium salt.
摘要翻译：提供了制备药物级阿托伐他汀半钙盐的方法，其包括：（a）脱酯化（式I），其中R是（式II）的酯保护基，（b）提取R（R *，R *） - 加入有机溶剂或溶剂混合物中，（c）加入式NR 1 R 2 R 3 R 3的碱，其中R 1 R 2，R 3和R 3独立地选自H，取代或未取代的C 1 -C 7烷基，C 6至C 9芳基，C 8至C 10芳烷基或氨基烷基以形成阿托伐他汀碱盐，（d）通过沉淀上述阿托伐他汀碱盐进行分离并在必要时进行纯化，（e）通过用钙盐溶液处理将阿托伐他汀碱盐转化成阿托伐他汀半钙盐，和（f）分离阿托伐他汀半钙盐。

4. 发明申请

WO2007140608A1 A NOVEL PROCESS FOR THE PREPARATION OF ESOMEPRAZOLE AND SALTS THEREOF 审中-公开
标题翻译：用于制备异喹诺酮和其盐的新方法
公开(公告)号：WO2007140608A1
公开(公告)日：2007-12-13
申请号：PCT/CA2007/001005
申请日：2007-06-08
申请人： APOTEX PHARMACHEM INC. , WANG, Fan , MONTEMAYOR, Laura, Kaye , CHE, Daqing , HORNE, Stephen, E.
发明人： WANG, Fan , MONTEMAYOR, Laura, Kaye , CHE, Daqing , HORNE, Stephen, E.
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , Y02P20/55
摘要： A novel process for the preparation of omeprazole and its enantiomers, such as esomeprazole, as well as the preparation of related 2-(2-pyridinylmethyl-sulphinyl)-1H-benzimidazoles, including pantoprazole, lansoprazole and rabeprazole, as recemates or single enantiomers, and their alkali or alkaline salts has been developed. The novel process involves the surprising discovery that protection of the free-base benzimidazole sulfoxide (e.g. omeprazole or esomeprazole), by reaction with an alkyl, aryl or aralkyl chloroformate following oxidation of the corresponding sulfide, eliminates the need for its direct isolation. Subsequent removal of the protecting group with a solution of alkali or alkaline earth alkoxide in a C1-C4 alcohol directly provides the corresponding salt. By eliminating the need to handle the free-base benzimidazole sulfoxide, this advantageous procedure provides increased chemical yields over processes described in the art.
摘要翻译：一种用于制备奥美拉唑及其对映异构体的新方法，例如艾美拉唑，以及相关的2-（2-吡啶基甲基 - 亚磺酰基）-1H-苯并咪唑（包括泮托拉唑，兰索拉唑和雷贝拉唑）作为受体或单一对映异构体的制备，并开发了它们的碱金属盐或碱金属盐。该新方法涉及令人惊奇的发现：在相应的硫化物氧化后，通过与烷基，芳基或氯甲酸烷基酯反应来保护游离碱性苯并咪唑亚砜（例如奥美拉唑或埃索美拉唑）消除了对其直接分离的需要。随后用碱金属或碱土金属醇溶液在C1-C4醇中除去保护基团直接提供相应的盐。通过消除处理游离碱性苯并咪唑亚砜的需要，与本领域中描述的方法相比，该有利的方法提供了增加的化学产率。

5. 发明申请

WO2007098573A1 A PROCESS FOR THE PREPARATION OF PHENYLCARBAMATES 审中-公开
标题翻译：一种制备苯甲酸酯的方法
公开(公告)号：WO2007098573A1
公开(公告)日：2007-09-07
申请号：PCT/CA2007/000253
申请日：2007-02-28
申请人： APOTEX PHARMACHEM INC. , WANG, Zhi-Xian , HORNE, Stephen, E. , MURTHY, K.S., Keshava
发明人： WANG, Zhi-Xian , HORNE, Stephen, E. , MURTHY, K.S., Keshava
IPC分类号： C07C269/04 , C07C271/42
CPC分类号： C07C269/04 , C07C271/44
摘要： A process for the preparation of aminoalkyl phenyl carbamate compounds of Formula I, wherein R 1 and R 2 independently are hydrogen or a C 1-6 alkyl; R 3 and R 4 are the same or different and each is a C 1-6 alkyl; or R 3 and R 4 together with the nitrogen to which they are attached form a cyclic three to eight membered ring, with or without a heteroatom like nitrogen or oxygen; R 5 and R 6 independently are hydrogen, linear, branched or cyclic C 1-6 alkyl; or R 5 and R 6 together with the nitrogen to which they are attached form a cyclic three to eight membered ring, with or without a heteroatom like nitrogen or oxygen; the carbon centre designated "*" can be racemic or enantiomerically enriched in the (R)- or (S)- configuration; and pharmaceutically acceptable acid addition salts thereof.
摘要翻译：制备式I的氨基烷基苯基氨基甲酸酯化合物的方法，其中R 1和R 2独立地是氢或C 1-6烷基，烷基; R 3和R 4相同或不同，各自为C 1-6烷基; 或R 3和R 4与它们所连接的氮一起形成具有或不具有杂原子如氮或氧的环状三元至八元环; R 5和R 6独立地是氢，直链，支链或环状C 1-6烷基; 或R 5和R 6与它们所连接的氮一起形成具有或不具有杂原子如氮或氧的环状三元至八元环; 指定为“*”的碳中心可以是（R） - 或（S） - 构型的外消旋或对映异构体富集; 及其药学上可接受的酸加成盐。

6. 发明申请

WO2006094395A1 PREPARATION OF ACID ADDITION SALTS OF AMINE BASES BY SOLID PHASE-GAS PHASE REACTIONS 审中-公开
标题翻译：通过固相气相反应制备胺基酸的添加剂
公开(公告)号：WO2006094395A1
公开(公告)日：2006-09-14
申请号：PCT/CA2006/000337
申请日：2006-03-10
申请人： APOTEX PHARMACHEM INC. , REY, Allan W. , DERDOUR, Lofti , MURTHY, K. S. Keshava , DATTA, Probal Kanti , EHLERT, Martin , HORNE, Stephen, E.
发明人： REY, Allan W. , DERDOUR, Lofti , MURTHY, K. S. Keshava , DATTA, Probal Kanti , EHLERT, Martin , HORNE, Stephen, E.
IPC分类号： C07D405/14 , C07D401/14 , C07D307/52 , C07D211/22 , A61K31/4458 , A61K31/341
CPC分类号： C07D405/12 , C07D211/28 , C07D307/52 , C07D401/14
摘要： A process for the preparation of an acid addition salt of an organic base comprising exposing the organic base in solid form to a gaseous acid, with the proviso that ziprasidone, its acid addition salts and intermediates thereof are excluded.
摘要翻译：一种制备有机碱的酸加成盐的方法，包括将固体形式的有机碱暴露于气态酸，条件是排除了齐拉西酮，其酸加成盐和中间体。

7. 发明申请

WO2006047893A1 PROCESS FOR THE PREPARATION OF ZIPRASIDONE (5-[2-[4-(1,2-BENZISOTHIAZOL-3-Y1)-1-PIPERAZINY1]ETHY1]-6-CHLORO-1,3-DIHYDRO-2H-INDOL-2-ONE) 审中-公开
标题翻译：制备ZIPRASIDONE（5- [2- [4-（1,2-苄基联苯-3-基）-1-哌嗪-1-基]乙基] -6-氯-1,3-二氢-2H-吲哚-2-酮的方法，一）
公开(公告)号：WO2006047893A1
公开(公告)日：2006-05-11
申请号：PCT/CA2005/001721
申请日：2005-11-04
申请人： APOTEX PHARMACHEM INC. , ZETINA-ROCHA, Carlos , REY, Allan, W. , HORNE, Stephen, E. , BUCK, Matthew, A.
发明人： ZETINA-ROCHA, Carlos , REY, Allan, W. , HORNE, Stephen, E. , BUCK, Matthew, A.
IPC分类号： C07D417/04
CPC分类号： C07D417/14
摘要： The present invention provides a new and useful process for preparing 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3dihydro-2H-indol-2-one (ziprasidone) and methods for its purification. The process comprises the steps of: (i) mixing 6-chloro-5-(2-chloroethyl)-1,3-dihydro-2H-indol-2-one with either a free base or salt form of 3-(1-piperazinyl)-1,2benzoisothiazole, in the presence of an alkaline compound and a high-boiling polar organic solvent or mixture of high boiling polar organic solvents, (ii) heating the mixture and stirring for a sufficient amount of time to obtain ziprasidone formation, (iii) cooling the mixture, adding it to water and filtering off the product, (iv) adding water to the product and stirring the suspension, and (v) isolating crude ziprasidone.
摘要翻译：本发明提供了一种制备5- [2- [4-（1,2-苯并异噻唑-3-基）-1-哌嗪基]乙基] -6-氯-1,3-二氢-2H-吲哚的新的有用的方法 -2-二（齐拉西酮）及其纯化方法。该方法包括以下步骤：（i）将6-氯-5-（2-氯乙基）-1,3-二氢-2H-吲哚-2-酮与游离碱或盐形式的3-（1- 哌嗪基）-1,2-苯并异噻唑，在碱性化合物和高沸点极性有机溶剂或高沸点极性有机溶剂的混合物的存在下，（ii）加热混合物并搅拌足够的时间以获得齐拉西酮形成，（iii）冷却混合物，将其加入水中并过滤掉产物，（iv）向产物中加入水并搅拌悬浮液，和（v）分离粗制齐拉西酮。

8. 发明申请

WO2006094396A1 PREPARATION OF ACID ADDITION SALTS OF ZIPRASIDONE AND INTERMEDIATES THEREOF BY SOLID PHASE-GAS PHASE REACTIONS 审中-公开
标题翻译：通过固体相气相反应制备拉伐沙星及其中间体的酸添加剂
公开(公告)号：WO2006094396A1
公开(公告)日：2006-09-14
申请号：PCT/CA2006/000338
申请日：2006-03-10
申请人： APOTEX PHARMACHEM INC. , REY, Allan W. , DERDOUR, Lofti , MURTHY, K.S. Keshava , DATTA, Probal Kanti , EHLERT, Martin , HORNE, Stephen, E.
发明人： REY, Allan W. , DERDOUR, Lofti , MURTHY, K.S. Keshava , DATTA, Probal Kanti , EHLERT, Martin , HORNE, Stephen, E.
IPC分类号： C07D417/14
CPC分类号： C07D417/14
摘要： A process for the preparation of an acid addition salt of ziprasidone base and intermediates thereof comprising exposing the ziprasidone base in solid form to a gaseous acid in a substantially dry environment. The process is solvent free and the gaseous acid is mixed with one or more inert gases. The process produces ziprasidone hydrochloride in high yield and purity and is reliable, consistent and suitable for large scale manufacturing. The process can also be used to prepare ziprasidone hydrobromide and ziprasidone acetate.
摘要翻译：用于制备齐拉西酮碱的酸加成盐的方法及其中间体，其包括将固体形式的齐拉西酮碱在基本干燥的环境中暴露于气态酸。该方法是无溶剂的，气态酸与一种或多种惰性气体混合。该方法以高产率和纯度生产齐拉昔酮盐酸盐，可靠，一致，适合大规模生产。该方法也可用于制备齐拉西酮氢溴酸盐和齐拉西酮醋酸酯。

9. 发明申请

WO2005111032A1 NEW AMORPHOUS ZIPRASIDONE HYDROCHLORIDE (5-[2-[4-(1,2-BENZISOTHIAZOL-3-YL)-1-PIPERAZINYL]ETHYL]-6-CHLORO-1,3-DIHYDRO-2H-INDL-2-ONE HYDROCHLORIDE) AND PROCESS TO PRODUCE THE SAME 审中-公开
标题翻译：新的非对羟基萘啶酮氢氯化物（5- [2- [4-（1,2-苄基联苯-3-基）-1-哌嗪基]乙基] -6-氯-1,3-二氢-2H-吲哚-2-酮氢氯酸盐）及其生产方法
公开(公告)号：WO2005111032A1
公开(公告)日：2005-11-24
申请号：PCT/CA2004/000981
申请日：2004-07-07
申请人： APOTEX PHARMACHEM INC. , REY, Allan, W. , ZETINA-ROCHA, Carlos , BUCK, Matthew, A. , DERDOUR, Lotfi , HORNE, Stephen, E. , MURTHY, Keshava, K. S.
发明人： REY, Allan, W. , ZETINA-ROCHA, Carlos , BUCK, Matthew, A. , DERDOUR, Lotfi , HORNE, Stephen, E. , MURTHY, Keshava, K. S.
IPC分类号： C07D417/12
CPC分类号： C07D417/12
摘要： The present invention relates to a new and useful amorphous form of ziprasidone hydrochloride (5-[2-[4-(1,2-benzisothiazol-3-yl)-1piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one hydrochloride) and preparations thereof.
摘要翻译：本发明涉及一种新的和有用的无定形齐拉昔酮盐酸盐（5- [2- [4-（1,2-苯并异噻唑-3-基）-1-哌嗪基]乙基] -6-氯-1,3-二氢 -2H-吲哚-2-酮盐酸盐）及其制剂。

10. 发明申请

WO2003101967A1 PREPARATION OF CHIRAL 1,2,3,4-TETRAHYDRO-6,7-DIALKOXY-3-ISOQUINOLINECARBOXYLIC ACID AND DERIVATIVES BY REACTING LEVODOPA WITH FORMALDEHYDE OR FORMALDEHYDE PRECURSORS 审中-公开
标题翻译：通过用甲醛或甲醛前体反应LEVODOPA来制备化合物1,2,3,4-四氢-6,7-二甲氧基-3-异喹啉羧酸和衍生物
公开(公告)号：WO2003101967A1
公开(公告)日：2003-12-11
申请号：PCT/CA2003/000747
申请日：2003-05-23
申请人： BRANTFORD CHEMICALS INC. , WANG, Zhi-Xian , HORNE, Stephen, E.
发明人： WANG, Zhi-Xian , HORNE, Stephen, E.
IPC分类号： C07D217/26
CPC分类号： C07D217/26 , Y02P20/55
摘要： A process for preparation of (S)-1,2,3,4-tetrahydro-6,7-dialkoxy-3-isoquinolinecarboxylic acid compounds and their derivatives of the formula (1) the process compring: (i) reacting Levodopa of formula (2) with formaldehyde or formaldehyde precursors to obtain (S)-1,2,3,4-tetrahydro-6,7-dihydroxy-3-isoquinolinecarboxylic acid of formula (3); (ii) protecting the amino group of formula (3); (iii) alkylating the phenol groups of formula (4) to form compound of formula (5); and (iv) esterifying the carcoxylic acid of formula (5) and optionally removing N-protecting group wherein R 1 is hydrogen, lower alkyl, C2-C12 acyl, or R 1 O together are methylenedioxy; R 2 is hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, aryl, substituted aryl, aralkyl or substituted aralkyl group; R 3 is hydrogen, C2-C12 acyl group, benzyl, alkoxylcarbonyl group, or aralkoxyl carbonyl group; wherein P is the protecting group selected from alkoxycarbonyl, acyl, alkyl, aryl, siryl, sulfenyl and sulfonyl.
摘要翻译：制备（S）-1,2,3,4-四氢-6,7-二烷氧基-3-异喹啉羧酸化合物及其式（1）的衍生物的方法，该方法包括：（i）使式（IV）的左旋多巴（2）与甲醛或甲醛前体反应，得到式（3）的（S）-1,2,3,4-四氢-6,7-二羟基-3-异喹啉羧酸; （ii）保护式（3）的氨基; （iii）将式（4）的酚基烷基化以形成式（5）的化合物; 和（iv）酯化式（5）的羧甲酸和任选除去其中R 1是氢的低级烷基，C 2 -C 12酰基或者R 1 O的N-保护基是亚甲二氧基; R2是氢，烷基，取代的烷基，烯基，取代的烯基，芳基，取代的芳基，芳烷基或取代的芳烷基; R3是氢，C2-C12酰基，苄基，烷氧基羰基或芳烷氧基羰基; 其中P是选自烷氧基羰基，酰基，烷基，芳基，西尔基，亚磺酰基和磺酰基的保护基。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式