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1. 发明申请

WO2010083597A1 METHODS OF MAKING LUBIPROSTONE AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备LUBIPROSTONE及其中间体的方法
公开(公告)号：WO2010083597A1
公开(公告)日：2010-07-29
申请号：PCT/CA2010/000083
申请日：2010-01-22
申请人： APOTEX PHARMACHEM INC. , KOTHAKONDA, Kiran, Kumar , WANG, Fan , GUNTOORI, Bhaskar, Reddy , NGUYEN, Minh, T.N. , CECCARELLI, Alfredo, Paul , ZHAO, Yajun , KOTIPALLI, Uma , DUNCAN, Sammy, Chris , MILNEE, Kaarina, K. , KELLS, Kevin, W. , MONTEMAYOR, Laura, Kaye
发明人： KOTHAKONDA, Kiran, Kumar , WANG, Fan , GUNTOORI, Bhaskar, Reddy , NGUYEN, Minh, T.N. , CECCARELLI, Alfredo, Paul , ZHAO, Yajun , KOTIPALLI, Uma , DUNCAN, Sammy, Chris , MILNEE, Kaarina, K. , KELLS, Kevin, W. , MONTEMAYOR, Laura, Kaye
IPC分类号： C07C69/734 , C07C59/66 , C07C69/738 , C07D307/935 , C07D311/94 , C07F7/18
CPC分类号： C07F7/1892 , C07C69/734 , C07C69/738 , C07C405/00 , C07C2601/08 , C07D307/935
摘要： There is provided processes for preparing Lubiprostone and intermediates thereof. Also provided are compounds, including intermediates for preparing Lubiprostone as well as compositions comprising Lubiprostone and other compounds, including intermediates for preparing Lubiprostone and other compounds. (I)
摘要翻译：提供了用于制备柳普罗石及其中间体的方法。还提供了化合物，包括用于制备兰比罗石的中间体以及包含卢比石和其它化合物的组合物，包括用于制备兰普罗石和其他化合物的中间体。（一世）

2. 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。

3. 发明申请

WO2013026149A1 DIMETHYL-(3,3-DIFLUORO-2,2-DIHYDROXYHEPTYL)PHOSPHONATE AND PROCESSES FOR ITS PREPARATION 审中-公开
标题翻译：二甲基 - （3,3,3-二氟-2,2-二羟基乙基）膦酸酯及其制备方法
公开(公告)号：WO2013026149A1
公开(公告)日：2013-02-28
申请号：PCT/CA2012/000793
申请日：2012-08-24
申请人： APOTEX PHARMACHEM INC. , ZHAO, Yajun , DATTA, Probal, Kanti , DUNCAN, Sammy, Chris , KOTIPALLI, Uma , KONDAMREDDY, Murali , NAGIREDDY, Nalini
发明人： ZHAO, Yajun , DATTA, Probal, Kanti , DUNCAN, Sammy, Chris , KOTIPALLI, Uma , KONDAMREDDY, Murali , NAGIREDDY, Nalini
IPC分类号： C07F9/40 , C07D311/94
CPC分类号： C07F9/4006 , C07D311/94
摘要： A compound dimethyl-(3,3-difluoro-2,2-dihydroxyheptyl)phosphonate (I), a crystalline form of this compound, processes for its preparation, and use of this compound in the preparation of prostaglandin derivatives such as Lubiprostone.
摘要翻译：该化合物的结晶形式的复合二甲基 - （3,3-二氟-2,2-二羟基庚基）膦酸酯（I）用于其制备，以及该化合物在制备前列腺素衍生物例如Lubiprostone中的用途。

4. 发明申请

WO2006089401A1 AN IMPROVED PROCESS FOR THE PREPARATION OF ATORVASTATIN AND INTERMEDIATES 审中-公开
标题翻译：改进ATORVASTATIN和中间体的制备方法
公开(公告)号：WO2006089401A1
公开(公告)日：2006-08-31
申请号：PCT/CA2006/000243
申请日：2006-02-21
申请人： APOTEX PHARMACHEM INC. , WANG, Fan , CHE, Daqing , GUNTOORI, Bhaskar Reddy , ZHAO, Yajun , KINSMAN, Aaron, C. , FAUGHT, Jody , CHOW, Alan
发明人： WANG, Fan , CHE, Daqing , GUNTOORI, Bhaskar Reddy , ZHAO, Yajun , KINSMAN, Aaron, C. , FAUGHT, Jody , CHOW, Alan
IPC分类号： C07D207/34
CPC分类号： C07D207/34
摘要： A process is provided for preparing (R)-5-[2-(4-fluorophenyl)-5-(l- methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-lH-pyrrol-l-yl]-5-hydroxy-3-oxo- 1-heptanoic acid, R-substituted ester 9 comprising: (a) reacting 5-(4-fluorophenyl)-2-(l -methylethyl)-l -(3-oxopropyl)-N,4- diphenyl-lH-pyrrole-3-carboxamide, 1, with the enolate form of (S)-2- hydroxy- 1 ,2,2-triphenylethyl acetate substituent in a chelating co- solvent; (b) hydrolysis of (R,S)-5-[2-(4-fluorophenyl)-5-(l -methylethyl)-3-phenyl- 4-[(phenylamino)carbonyl]- 1 H-pyrrol- 1 -yl]-3-hydroxy- 1 -pentanoic acid, (S)-2 -hydroxy- 1 ,2,2-triphenylethyl ester (2a and 2b) using a base, preferably an alkali metal base, preferably in a solvent to form the (R,S)-5-[2-(4-fluorophenyl)-5-(l -methylethyl)-3-phenyl-4- [(phenylamino)carbonyl]- 1 H-pyrrol- 1 -yl]-3 -hydroxy- 1 -pentanoic acid, 7; (c) treating the carboxylic acid 7 with a chiral base to form a salt and purifying the salt to obtain enantiomerically enriched (R)-7 chiral base salt; (d) alkylation of the (R)-7 chiral base salt or the free acid derived from (R)-7, forming (R)-5-[2-(4-fluorophenyl)-5-(l-methylethyl)-3-phenyl- 4-[(phenylamino)carbonyl]-lH-pyrrol-l-yl]-5-hydroxy-3-oxo-l- heptanoic acid, R-substituted ester 9, wherein the R substituent is a Cl to C6 alkyl, C6 to C9 aryl or C7 to Cl0 aralkyl. Subsequently, R-substituted ester 9 may be converted into atorvastatin calcium 6 based on procedures known in the art.
摘要翻译：提供了制备（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-羟基-3-氧代-1-庚酸，R-取代的酯9，其包含：（a）使5-（4-氟苯基）-2-（1-甲基乙基）-1-（3-氧代丙基）-N ，4-二苯基-1H-吡咯-3-甲酰胺，1，在螯合助溶剂中具有（S）-2-羟基-1,2-二苯基乙基乙酸酯取代基的烯醇化物形式; （b）（R，S）-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] -3-羟基-1-戊酸，（S）-2-羟基-1,2-二苯基乙酯（2a和2b），使用碱，优选碱金属碱，优选在溶剂中形成（R，S）-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] 羟基-1-戊酸，7; （c）用手性碱处理羧酸7以形成盐并纯化该盐以获得对映体富集的（R）-7手性碱盐; （d）（R）-7手性碱盐或衍生自（R）-7的游离酸的烷基化，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] -5-羟基-3-氧代-1-庚酸R-取代的酯9，其中R取代基是C1至C6 烷基，C 6至C 9芳基或C 7至C 10芳烷基。随后，基于本领域已知的方法，R取代的酯9可以转化成阿托伐他汀钙6。

5. 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。

6. 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。

7. 发明申请

WO2008089557A1 ATORVASTATIN CALCIUM PROPYLENE GLYCOL SOLVATES 审中-公开
标题翻译： ATORVASTATIN钙丙二醇溶液
公开(公告)号：WO2008089557A1
公开(公告)日：2008-07-31
申请号：PCT/CA2008/000131
申请日：2008-01-24
申请人： APOTEX PHARMACHEM INC. , MURTHY, Keshava, K., S. , ZHAO, Yajun , REY, Allan, W. , DAQING, Che , STRADIOTTO, David, A. , KOTIPALLI, Uma
发明人： MURTHY, Keshava, K., S. , ZHAO, Yajun , REY, Allan, W. , DAQING, Che , STRADIOTTO, David, A. , KOTIPALLI, Uma
IPC分类号： C07D207/34 , A61P3/06 , A61K31/40
CPC分类号： C07D207/34
摘要： The present application relates to atorvastatin calcium propylene glycol solvates and processes of preparing the same. The atorvastatin calcium propylene glycol solvates are crystalline and show high chemical and solid state stability, low hygroscopicity, and good flow properties.The solvates can be efficiently prepared from various forms of atorvastatin and either (R), (S), or mixtures of (R) and (S) propylene glycol, and may be easily filtered and dried on an industrial scale.
摘要翻译：本申请涉及阿托伐他汀钙丙二醇溶剂合物及其制备方法。阿托伐他汀钙丙二醇溶剂合物是结晶的，显示出高的化学和固态稳定性，低吸湿性和良好的流动性。溶剂化物可以有效地由各种形式的阿托伐他汀和（R），（S）或（ R）和（S）丙二醇，并且可以容易地以工业规模过滤和干燥。

8. 发明申请

WO2014040164A1 PROCESSES FOR THE PREPARATION OF 3-ALKYL INDOLES 审中-公开
标题翻译：制备3-烷基吲哚的方法
公开(公告)号：WO2014040164A1
公开(公告)日：2014-03-20
申请号：PCT/CA2013/000766
申请日：2013-09-12
申请人： APOTEX PHARMACHEM INC.
发明人： STEWART, Craig , BLAZECKA, Peter Garth , WEERATUNGA, Gamini , KOTIPALLI, Uma , DUNCAN, Sammy Chris , ZHAO, Yajun
IPC分类号： A61K31/4184 , C07D209/08 , C07D405/12
CPC分类号： C07D209/10 , A61K31/496 , C07D209/08 , C07D405/12
摘要： This invention provides processes for preparation of 3-alkyl indoles of Formula 1 : wherein A 1 , A 2 and A 3 are independently selected from the group consisting of: H, X, OR 1 , CN, CONR 2 2 and C0 2 R 3 ; R 1 is C 1 -C 6 alkyl; R 2 is H or C 1 -C 6 alkyl; R 3 is C 1 -C 6 alkyl; LG is a leaving group; X is a halogen; and n is 1, 2 or 3.
摘要翻译：本发明提供制备式1的3-烷基吲哚的方法：其中A1，A2和A3独立地选自：H，X，OR1，CN，CONR2 2和CO 2 R 3; R1是C1-C6烷基; R2是H或C1-C6烷基; R3是C1-C6烷基; LG是离职团体 X是卤素; n为1,2或3。

9. 发明申请

WO2013185211A1 POLYMORPHIC FORMS OF RIFAXIMIN 审中-公开
标题翻译： RIFAXIMIN的多形态
公开(公告)号：WO2013185211A1
公开(公告)日：2013-12-19
申请号：PCT/CA2013/000562
申请日：2013-06-13
申请人： APOTEX PHARMACHEM INC.
发明人： BLAZECKA, Peter Garth , MOHAMED, Nageib , MCPHAIL, Cameron L. , DUNCAN, Sammy Chris , EL-HAJ, Randa E. , ZHAO, Yajun
IPC分类号： C07D498/22
CPC分类号： C07D491/22 , C07D498/22
摘要： Provided for in the instant application are two additional forms of rifaximin, namely rifaximin polymorphic forms ΑΡΟ-III and APO-IV. Also provided are allegedly novel processes for preparing the previously disclosed rifaximin polymorphic forms APO-I and ΑΡΟ-II. Rifaximin is a non-aminoglycoside antibiotic that has previously been found to be useful for the treatment of traveller's diarrhea caused by Escherichia coli bacteria, as well as in the treatment of irritable bowel syndrome, diverticular disease, hepatic encephalopathy, pyogenic skin infections and as an antibacterial prophylactic prior to colon surgery.
摘要翻译：在本申请中提供了两种另外形式的利福昔明，即利福昔明多晶型αRhoOmicron-III和APO-IV。据称还提供了用于制备先前公开的利福昔明多晶形式APO-1和αRhoOmicron-II的新方法。利福昔明是一种非氨基糖甙类抗生素，以前被发现可用于治疗由大肠杆菌引起的旅行者腹泻，以及治疗肠易激综合征，憩室疾病，肝性脑病，化脓性皮肤感染和作为结肠手术前抗菌预防。

10. 发明申请

WO2003097599A1 PREPARATION OF 4-(4-FLUOROPHENYL)-N-SUBSTITUTEDNIPECOTINATE ESTERS 审中-公开
标题翻译： 4-（4-氟代戊基）-N-取代基氨基酸酯的制备
公开(公告)号：WO2003097599A1
公开(公告)日：2003-11-27
申请号：PCT/CA2003/000700
申请日：2003-05-14
申请人： BRANTFORD CHEMICALS INC. , REY, Allan, W. , MURTHY, Keshava, K., S. , RADATUS, Bruno , ZHAO, Yajun , NISH, Tania, E.
发明人： REY, Allan, W. , MURTHY, Keshava, K., S. , RADATUS, Bruno , ZHAO, Yajun , NISH, Tania, E.
IPC分类号： C07D211/60
CPC分类号： C07D405/12 , C07D211/60
摘要： A process for the industrial scale manufacture of 4-(4-fluorophenyl)-N-alkylnipecotinate esters by the addition of 4-fluorophenylmagnesium halide in tetrahydrofuran to 3,4-unsaturated-3-piperidine esters.
摘要翻译：通过在四氢呋喃中加入4-氟苯基卤化镁至3,4-不饱和-3-哌啶酯，工业规模生产4-（4-氟苯基）-N-烷基哌啶酸酯的方法。

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