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1. 发明申请

WO0142272A9 EPLERENONE CRYSTALLINE FORM EXHIBITING ENHANCED DISSOLUTION RATE 审中-公开
标题翻译： EPLERENONE CRYSTALLINE FORM展现增强溶解速度
公开(公告)号：WO0142272A9
公开(公告)日：2002-12-12
申请号：PCT/US0032416
申请日：2000-12-04
申请人： PHARMACIA CORP , BARTON KATHLEEN , BORCHARDT THOMAS B , CARLOS MARLON V , DESAI SUBHASH , FERRO LEONARD J , GAUD HENRY T , GANSER SCOTT , LITTLE CLAY R , MUDIPALLI PARTHA S , PIETZ MARK A , PILIPAUSKAS DANIEL R , SING YUEN-LUNG L , STAHL GLENN L , WIECZOREK JOSEPH J , YAN CHRIS Y
发明人： BARTON KATHLEEN , BORCHARDT THOMAS B , CARLOS MARLON V , DESAI SUBHASH , FERRO LEONARD J , GAUD HENRY T , GANSER SCOTT , LITTLE CLAY R , MUDIPALLI PARTHA S , PIETZ MARK A , PILIPAUSKAS DANIEL R , SING YUEN-LUNG L , STAHL GLENN L , WIECZOREK JOSEPH J , YAN CHRIS Y
IPC分类号： A61K31/58 , A61P1/16 , A61P9/04 , A61P9/12 , A61P43/00 , C07J71/00 , C07J75/00 , C07J1/00
CPC分类号： C07J71/0015
摘要： A novel crystalline form (Form H) of the aldosterone receptor antagonist drug eplerenone is provided having a relatively rapid dissolution rate in aqueous media. Also provided are novel solvated crystalline forms of eplerenone that, when desolvated, can yield Form H eplerenone. Also provided is amorphous eplerenone. Pharmaceutical compositions are provided comprising Form H eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form H eplerenone and for preparing compositions comprising Form H eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form H eplerenone.
摘要翻译：提供醛固酮受体拮抗剂药物依普利酮的新型结晶形式（形式H），其在水性介质中具有相对快速的溶解速率。还提供了eplerenone的新型溶剂化结晶形式，当脱溶时，可以产生H形式。还提供了非依依普利酮。提供了药物组合物，其包含H形式H eplerenone，任选地伴随有一种或多种其他固体形式的依普利酮，总单位剂量为约10至约1000mg的依普利酮，并且还包含一种或多种药学上可接受的赋形剂。提供了制备H形式H eplerenone和制备包含H型肝素的组合物的方法。还提供了用于预防和/或治疗醛固酮介导的病症或病症的方法，其包括向受试者施用治疗有效量的依普利酮，其中至少一部分所述的依普利酮是H型肾上腺素。

2. 发明申请

WO2006081335A3 PROCESS FOR PREPARING SUBSTITUTED 1- [3- ( PYRAZOLYL) PHENYL] -3-PHENYL UREAS 审中-公开
标题翻译：制备取代的1- [3-（吡咯烷基）苯基] -3-苯基脲的方法
公开(公告)号：WO2006081335A3
公开(公告)日：2007-05-24
申请号：PCT/US2006002721
申请日：2006-01-25
申请人： ARENA PHARM INC , GHARBAOUI TAWFIK , AVERBUJ CLAUDIA , CARLOS MARLON V , LALLY EDWARD A , SENGUPTA DIPANJAN , FRITCH JOHN R
发明人： GHARBAOUI TAWFIK , AVERBUJ CLAUDIA , CARLOS MARLON V , LALLY EDWARD A , SENGUPTA DIPANJAN , FRITCH JOHN R
IPC分类号： C07D231/16
CPC分类号： C07D231/16
摘要： The present invention is directed to processes for the preparation of substituted phenylpyrazole ureas of Formula (I) that are useful as 5-HT 2A serotonin receptor modulators for the treatment of disease.
摘要翻译：本发明涉及制备式（I）的取代苯基吡唑脲的方法，其可用作治疗疾病的5-HT 2A 2 5-羟色胺受体调节剂。

3. 发明申请

WO2006081335A2 PROCESSES FOR PREPARING SUBSTITUTED PHENYLPYRAZOLE UREAS 审中-公开
标题翻译：制备取代的苯基脲的方法
公开(公告)号：WO2006081335A2
公开(公告)日：2006-08-03
申请号：PCT/US2006/002721
申请日：2006-01-25
申请人： ARENA PHARMACEUTICALS, INC. , GHARBAOUI, Tawfik , AVERBUJ, Claudia , CARLOS, Marlon V. , LALLY, Edward A. , SENGUPTA, Dipanjan , FRITCH, John R.
发明人： GHARBAOUI, Tawfik , AVERBUJ, Claudia , CARLOS, Marlon V. , LALLY, Edward A. , SENGUPTA, Dipanjan , FRITCH, John R.
IPC分类号： C07D231/16
CPC分类号： C07D231/16
摘要： The present invention is directed to processes for the preparation of substituted phenylpyrazole ureas of Formula (I) that are useful as 5-HT2A serotonin receptor modulators for the treatment of disease.
摘要翻译：本发明涉及用于制备用作治疗疾病的5-HT2A 5-羟色胺受体调节剂的式（I）的取代的苯基吡唑脲的方法。

4. 发明申请

WO2006032970A2 PROCESS FOR PREPARING 7a-ALKOXYCARBONYL SUBSTITUTED STEROIDS 审中-公开
标题翻译：制备7a-烷氧基羰基取代的类固醇的方法
公开(公告)号：WO2006032970A2
公开(公告)日：2006-03-30
申请号：PCT/IB2005002757
申请日：2005-08-25
申请人： PHARMACIA CORP , ABBAS S ZAHEER , BAUER MICHAEL , CARLOS MARLON V , DAVID PAUL , FRANCZYK THADDEUS , KIM CHUNG C , LAWSON JON P , MAISTO KEITH D , MCKENZIE DAVID , POZZO MARK , WIECZOREK JOSEPH
发明人： ABBAS S ZAHEER , BAUER MICHAEL , CARLOS MARLON V , DAVID PAUL , FRANCZYK THADDEUS , KIM CHUNG C , LAWSON JON P , MAISTO KEITH D , MCKENZIE DAVID , POZZO MARK , WIECZOREK JOSEPH
IPC分类号： C07J53/00 , C07J21/00
CPC分类号： C07J21/001 , C07J53/002 , Y02P20/582
摘要： Processes are described for the conversion of a steroid substrate having a 4,7-carbonyl bridge to a structure comprising a 7a-alkoxycarbonyl substituent by reaction of the substrate with an alkoxy group source, preferably in the presence of a base. Several optional process modifications are described. The reaction may be conducted at a temperature greater than about 70°C, with substantially shorter residence times than are required at lower temperatures. A saponification target may be incorporated into the reaction medium to consume free hydroxide compounds. The product 7a-alkoxycarbonyl compound may be recovered by crystallization, residual steroid values may be recovered from the crystallization mother liquor by extraction, and the extract may be processed to produce a repulp solution wherein the steroids may be re-equilibrated to produce additional 7a-alkoxycarbonyl substituted steroid product. Alternatively, the repulp solution may be recycled to a primary reactor wherein 4,7-carbonyl bridge substrate is converted to 7a-alkoxycarbonyl product. The process is particularly useful in the preparation of eplerenone, wherein a diketone intermediate comprising a 4,7-carbonyl bridge is reacted with an alkali metal methoxide to yield an 11a-hydroxy-7a-methoxycarbonyl compound (hydroxyester), the 11a-hydroxy group is converted to a leaving group which is then abstracted to produce a ?-9,11 enester, and the enester is epoxidized to eplerenone. Also disclosed is an epoxidation reaction conducted at relatively low hydrogen peroxide to enester substrate ratio.
摘要翻译：描述了通过底物与烷氧基源优选在碱存在下反应将具有4,7-羰基桥的类固醇底物转化为包含7α-烷氧基羰基取代基的结构的方法。描述了几个可选的过程修改。该反应可以在大于约70℃的温度下进行，其停留时间明显短于在较低温度下所需的停留时间。可以将皂化目标结合到反应介质中以消耗游离的氢氧化物化合物。产物7a-烷氧基羰基化合物可以通过结晶回收，可以通过萃取从结晶母液中回收剩余的类固醇值，并且可以对提取物进行处理以产生再溶解溶液，其中类固醇可以被再平衡以产生另外的7a- 烷氧羰基取代的甾体产物。或者，再浆化溶液可循环至其中4,7-羰基桥基质被转化为7α-烷氧基羰基产物的主反应器。该方法在制备依普利农中特别有用，其中使包含4,7-羰基桥的二酮中间体与碱金属甲醇盐反应，得到11a-羟基-7a-甲氧基羰基化合物（羟基酯），11a-羟基转化为离去基团，然后将其抽出以产生α-9,11烯烃，并将烯烃环氧化成依普利农。还公开了在相对较低的过氧化氢与烯烃底物比例下进行的环氧化反应。

5. 发明申请

WO2005092913A1 IMPROVED PROCESS FOR THE PREPARATION OF 9,11 EPOXY STEROIDS 审中-公开
标题翻译：改进制备9,11环氧甾体的方法
公开(公告)号：WO2005092913A1
公开(公告)日：2005-10-06
申请号：PCT/US2005/009381
申请日：2005-03-22
申请人： PHARMACIA & UPJOHN COMPANY , WIECZOREK, Joseph, J. , MAISTO, Keith, D. , DAVID, Paul , CARLOS, Marlon, V. , KIM, Chung, C.
发明人： WIECZOREK, Joseph, J. , MAISTO, Keith, D. , DAVID, Paul , CARLOS, Marlon, V. , KIM, Chung, C.
IPC分类号： C07J71/00
CPC分类号： C07J21/00 , C07J71/00 , Y02P20/582
摘要： Processes are described for epoxidation reactions. In particular, the process comprises the conversion of a steroid substrate having an olefinic unsaturation in the steroid nucleus to a structure comprising a 9,11-epoxy substituent by reaction of the substrate with a peroxide compound in the presence of a peroxide activator. The epoxidation processes described are conducted at relatively low hydrogen peroxide to steroid substrate ratio. Several optional process modifications are described.
摘要翻译：描述了用于环氧化反应的方法。特别地，该方法包括通过在过氧化物活化剂存在下使底物与过氧化物反应，将类固醇核中具有烯属不饱和键的类固醇底物转化成包含9,11-环氧取代基的结构。所描述的环氧化方法在相对低的过氧化氢条件下进行至类固醇底物的比例。描述了几个可选的过程修改。

6. 发明申请

WO2001042272A3 EPLERENONE CRYSTALLINE FORM EXHIBITING ENHANCED DISSOLUTION RATE 审中-公开
公开(公告)号：WO2001042272A3
公开(公告)日：2001-06-14
申请号：PCT/US2000/032416
申请日：2000-12-04
申请人： PHARMACIA CORPORATION , BARTON, Kathleen , BORCHARDT, Thomas, B. , CARLOS, Marlon, V. , DESAI, Subhash , FERRO, Leonard, J. , GAUD, Henry, T. , GANSER, Scott , LITTLE, Clay, R. , MUDIPALLI, Partha, S. , PIETZ, Mark, A. , PILIPAUSKAS, Daniel, R. , SING, Yuen-Lung, L. , STAHL, Glenn, L. , WIECZOREK, Joseph, J. , YAN, Chris, Y.
发明人： BARTON, Kathleen , BORCHARDT, Thomas, B. , CARLOS, Marlon, V. , DESAI, Subhash , FERRO, Leonard, J. , GAUD, Henry, T. , GANSER, Scott , LITTLE, Clay, R. , MUDIPALLI, Partha, S. , PIETZ, Mark, A. , PILIPAUSKAS, Daniel, R. , SING, Yuen-Lung, L. , STAHL, Glenn, L. , WIECZOREK, Joseph, J. , YAN, Chris, Y.
IPC分类号： C07J1/00
摘要： A novel crystalline form (Form H) of the aldosterone receptor antagonist drug eplerenone is provided having a relatively rapid dissolution rate in aqueous media. Also provided are novel solvated crystalline forms of eplerenone that, when desolvated, can yield Form H eplerenone. Also provided is amorphous eplerenone. Pharmaceutical compositions are provided comprising Form H eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form H eplerenone and for preparing compositions comprising Form H eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form H eplerenone.

7. 发明申请

WO2010062323A3 COMPOSITIONS OF A 5-HT2A SEROTONIN RECEPTOR MODULATOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译：用于治疗与相关疾病相关的5-HT2A蛋白受体调节剂的组合物
公开(公告)号：WO2010062323A3
公开(公告)日：2010-08-26
申请号：PCT/US2009005811
申请日：2009-10-27
申请人： ARENA PHARM INC , SILVEY GARY L , CARLOS MARLON V , MAFFUID PAUL , SHAN YUN
发明人： SILVEY GARY L , CARLOS MARLON V , MAFFUID PAUL , SHAN YUN
IPC分类号： A61K9/20 , A61K31/415
CPC分类号： A61K31/415 , A61K9/1635 , A61K9/2027 , A61K9/2054 , C07D231/16
摘要： The present invention relates to certain compositions of a 5-HT2A serotonin receptor modulator and methods for their preparation. The compositions disclosed herein are useful for increasing slow wave sleep, improving sleep consolidation, improving sleep maintenance and improving sleep quality, and for treating insomnia and related sleep disorders, dyssomnias, parasomnias and nonrestorative sleep and the like. The compositions disclosed herein are further useful for treating platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders and progressive multifocal leukoencephalopathy and the like.
摘要翻译：本发明涉及5-HT2A 5-羟色胺受体调节剂的某些组合物及其制备方法。本文公开的组合物可用于增加慢波睡眠，改善睡眠巩固，改善睡眠维持和改善睡眠质量，以及用于治疗失眠和相关的睡眠障碍，睡眠障碍，异睡眠和非恢复性睡眠等。本文公开的组合物还可用于治疗血小板聚集，冠状动脉疾病，心肌梗塞，短暂性脑缺血发作，心绞痛，中风，心房颤动，血栓形成，哮喘或其症状，其激动或症状，行为障碍，药物诱导的精神病，兴奋性精神病，Gilles de la Tourette综合征，躁狂症，有机或NOS精神病，精神病，精神病，急性精神分裂症，慢性精神分裂症，精神分裂症精神分裂症和相关疾病，糖尿病相关疾病和进行性多灶性脑白质病等。

8. 发明申请

WO2010062321A1 PROCESSES USEFUL FOR THE PREPARATION OF 1-[3-(4-BROMO-2-METHYL-2H-PYRAZOL-3-YL)-4-METHOXY-PHENYL]-3-(2,4-DIFLUORO-PHENYL)-UREA AND CRYSTALLINE FORMS RELATED THERETO 审中-公开
标题翻译：用于制备1- [3-（4-溴-2-甲基-2H-吡唑-3-基）-4-甲氧基苯基] -3-（2,4-二氟苯基） - 乙烯的方法和与其相关的晶体形式
公开(公告)号：WO2010062321A1
公开(公告)日：2010-06-03
申请号：PCT/US2009/005809
申请日：2009-10-27
申请人： ARENA PHARMACEUTICALS, INC. , CARLOS, Marlon V. , DONG, Weitong , MACIAS, Mark , SATO, Suzanne Michiko , SILVEY, Gary
发明人： CARLOS, Marlon V. , DONG, Weitong , MACIAS, Mark , SATO, Suzanne Michiko , SILVEY, Gary
IPC分类号： C07D231/16
CPC分类号： A61K31/415 , C07D231/12 , C07D231/16
摘要： The present invention is directed to processes and intermediates useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea (Compound I), crystalline forms and solvate forms thereof; and compositions comprising 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea, crystalline forms and solvate forms thereof prepared by processes as described herein.
摘要翻译：本发明涉及可用于制备1- [3-（4-溴-2-甲基-2H-吡唑-3-基）-4-甲氧基 - 苯基] -3-（2,4 - 二氟 - 苯基） - 脲（化合物I），其结晶形式和溶剂合物形式; 和包含1- [3-（4-溴-2-甲基-2H-吡唑-3-基）-4-甲氧基 - 苯基] -3-（2,4-二氟 - 苯基） - 脲的结晶的组合物，其通过如本文所述的方法制备的溶剂合物形式。

9. 发明申请

WO0142272A2 EPLERENONE CRYSTALLINE FORM EXHIBITING ENHANCED DISSOLUTION RATE 审中-公开
标题翻译：表现出增强溶出率的普罗酮结晶形式
公开(公告)号：WO0142272A2
公开(公告)日：2001-06-14
申请号：PCT/US0032416
申请日：2000-12-04
申请人： PHARMACIA CORP , BARTON KATHLEEN , BORCHARDT THOMAS B , CARLOS MARLON V , DESAI SUBHASH , FERRO LEONARD J , GAUD HENRY T , GANSER SCOTT , LITTLE CLAY R , MUDIPALLI PARTHA S , PIETZ MARK A , PILIPAUSKAS DANIEL R , SING YUEN LUNG L , STAHL GLENN L , WIECZOREK JOSEPH J , YAN CHRIS Y
发明人： BARTON KATHLEEN , BORCHARDT THOMAS B , CARLOS MARLON V , DESAI SUBHASH , FERRO LEONARD J , GAUD HENRY T , GANSER SCOTT , LITTLE CLAY R , MUDIPALLI PARTHA S , PIETZ MARK A , PILIPAUSKAS DANIEL R , SING YUEN-LUNG L , STAHL GLENN L , WIECZOREK JOSEPH J , YAN CHRIS Y
IPC分类号： A61K31/58 , A61P1/16 , A61P9/04 , A61P9/12 , A61P43/00 , C07J71/00 , C07J75/00 , C07J
CPC分类号： C07J71/0015
摘要： A novel crystalline form (Form H) of the aldosterone receptor antagonist drug eplerenone is provided having a relatively rapid dissolution rate in aqueous media. Also provided are novel solvated crystalline forms of eplerenone that, when desolvated, can yield Form H eplerenone. Also provided is amorphous eplerenone. Pharmaceutical compositions are provided comprising Form H eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form H eplerenone and for preparing compositions comprising Form H eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form H eplerenone.
摘要翻译：提供了在水性介质中具有相对快速的溶解速率的醛固酮受体拮抗剂药物依普利农的新晶型（晶型H）。还提供了依普利农的新型溶剂化晶体形式，当去溶剂化时，可以产生H型依普利农。还提供了无定形依匹乐酮。提供了包含H型依普利农的药物组合物，任选地伴随有一种或多种其他固态形式的依普利农，总单位剂量的依匹乐酮为约10至约1000mg，并且还包含一种或多种药学上可接受的赋形剂。提供了制备H型依普利农和用于制备包含H型依普利农的组合物的方法。还提供了用于预防和/或治疗醛固酮介导的病症或障碍的方法，其包括向受试者施用治疗有效量的依普利酮，其中存在至少一部分依匹乐酮是H型依普利农。

10. 发明申请

WO2009111004A1 PROCESSES FOR THE PREPARATION OF INTERMEDIATES RELATED TO THE 5-HT2C AGONIST (R)-8-CHLORO-1-METHYL-2,3,4,5-TETRAHYDRO-1H-3-BENZAZEPINE 审中-公开
标题翻译：制备与5-羟色胺-8-CH-1-甲基-2,3,4,5-四氢-1H-苯并恶唑相关的中间体的方法
公开(公告)号：WO2009111004A1
公开(公告)日：2009-09-11
申请号：PCT/US2009/001340
申请日：2009-03-03
申请人： ARENA PHARMACEUTICALS, INC. , CARLOS, Marlon V. , CASTRO, Ryan O. , GHARBAOUI, Tawfik , LU, Xiao-Xiong , MA, You-An , SAN MARTIN, Nicholas D.
发明人： CARLOS, Marlon V. , CASTRO, Ryan O. , GHARBAOUI, Tawfik , LU, Xiao-Xiong , MA, You-An , SAN MARTIN, Nicholas D.
IPC分类号： C07C17/16 , C07C215/08 , C07C209/68 , C07C211/29 , C07D223/16
CPC分类号： C07C209/74 , C07C17/16 , C07C17/38 , C07C213/08 , C07C25/02 , C07C211/29 , C07C215/08
摘要： The present invention provides processes and intermediates useful in the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1 H -3-benzazepine, a serotonin (5-HT) receptor agonist that is useful in the treatment or prophylaxis of, for example, central nervous system disorders, such as obesity.
摘要翻译：本发明提供了可用于制备8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并吖庚因的方法和中间体，5-羟色胺（5-HT）受体激动剂可用于治疗或预防例如中枢神经系统疾病，例如肥胖症。

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