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1. 发明公开

EP1444199A1 RACEMIC TAMSULOSIN FREE BASE AND METHODS OF MAKING THE SAME 有权
标题翻译：坦索罗辛的外消旋体游离碱及其制造方法
公开(公告)号：EP1444199A1
公开(公告)日：2004-08-11
申请号：EP02768175.8
申请日：2002-10-17
申请人： Synthon B.V.
发明人： HOORN, Hans, Jan , PETERS, Theodorus, Hendricus, Antonius , PIS, Jaroslav
IPC分类号： C07C303/44 , C07C217/54 , C07C311/39
CPC分类号： C07C217/20 , C07B2200/07 , C07B2200/13 , C07C303/44 , C07C311/37
摘要： Racemic tamsulosin free base is obtained in solid form. The solid form can be formed by precipitating racemic tamsulosin free base from a solvent that comprises at least one of water or a lower alcohol. The crystalline free base exhibits polymorphism and two unique forms are identified. Novel intermediates are disclosed useful in the production of tamsulosin free base: a sulfonic acid salt of 2-(o-ethoxyphenoxy)ethylamine and (3-aminosulfonyl-4-methoxy)phenylacetone.

2. 发明公开

EP1313474A2 PAROXETINE COMPOSITIONS AND PROCESSES FOR MAKING THE SAME 审中-公开
标题翻译：帕罗西汀组合物和方法及其
公开(公告)号：EP1313474A2
公开(公告)日：2003-05-28
申请号：EP01976929.8
申请日：2001-08-28
申请人： Synthon B.V.
发明人： VAN DALEN, Frans , PLATTEEUW, Johannes, Jan , PETERS, Theodorus, Hendricus, Antonius , LEMMENS, Jacobus, Maria , PICHA, Frantisek
IPC分类号： A61K31/4525 , A61K9/20
CPC分类号： A61K9/0095 , A61K9/0007 , A61K9/0056 , A61K9/2009 , A61K9/2013 , A61K9/2054 , A61K9/5078 , A61K31/4525
摘要： Paroxetine salt compositions having improved stability are formed by controlling the pH to 6.5 or less. The compositions can be made with the air of water without significant coloration problems. The paroxetine salt include paroxetine hydrochloride salts but preferably use paroxetine sulfonate salts such as paroxetine methane sulfonate.

3. 发明授权

EP1444199B1 RACEMIC TAMSULOSIN FREE BASE AND METHODS OF MAKING THE SAME 有权
标题翻译：坦索罗辛的外消旋体游离碱及其制造方法
公开(公告)号：EP1444199B1
公开(公告)日：2008-12-17
申请号：EP02768175.8
申请日：2002-10-17
申请人： Synthon B.V.
发明人： HOORN, Hans, Jan , PETERS, Theodorus, Hendricus, Antonius , PIS, Jaroslav
IPC分类号： C07C303/44 , C07C217/54 , C07C311/39
CPC分类号： C07C217/20 , C07B2200/07 , C07B2200/13 , C07C303/44 , C07C311/37
摘要： Racemic tamsulosin free base is obtained in solid form. The solid form can be formed by precipitating racemic tamsulosin free base from a solvent that comprises at least one of water or a lower alcohol. The crystalline free base exhibits polymorphism and two unique forms are identified. Novel intermediates are disclosed useful in the production of tamsulosin free base: a sulfonic acid salt of 2-(o-ethoxyphenoxy)ethylamine and (3-aminosulfonyl-4-methoxy)phenylacetone.

4. 发明公开

EP1444198A1 PROCESS FOR RESOLUTION OF TAMSULOSIN 审中-公开
标题翻译：解决过程用于生产坦索罗辛
公开(公告)号：EP1444198A1
公开(公告)日：2004-08-11
申请号：EP02768172.5
申请日：2002-10-15
申请人： Synthon B.V.
发明人： HOORN, Hans, Jan , PETERS, Theodorus, Hendricus, Antonius , PIS, Jaroslav , SCIGEL, Radim
IPC分类号： C07C303/44 , C07C311/39
CPC分类号： C07C217/20 , C07B2200/07 , C07B2200/13 , C07C303/44 , C07C311/37
摘要： Optically impure tamsulosin including racemic tamsulosin can be resolved into optically pure (R)- or (S)-tamsulosin by the use of diastereomeric sulfonate salts of tamsulosin in a fractional crystallization technique.

5. 发明公开

EP1440067A1 N-FORMYL DERIVATIVES OF PAROXETINE 有权
标题翻译：帕罗西汀N-甲酰基衍生物
公开(公告)号：EP1440067A1
公开(公告)日：2004-07-28
申请号：EP02768169.1
申请日：2002-10-15
申请人： Synthon B.V.
发明人： HOORN, Hans, Jan , PETERS, Theodorus, Hendricus, Antonius , PICHA, Frantisek
IPC分类号： C07D405/12 , A61P39/00
CPC分类号： C07D405/12 , C07D211/22
摘要： The invention relates to a compound or composition comprising N-formyl paroxetine of formula (1) and 0 to 99.97% of a paroxetine compound, based on the combined weight of said N-formyl paroxetine and said paroxetine compound, to a pharmaceutical composition, for treating a selective serotonin reuptake inhibitor-treatable disease or condition, comprising an effective amount of a paroxetine agent and at least one pharmaceutically acceptable excipient, wherein said paroxetine agent comprises of an N-formyl paroxetine compound of formula (1) and optionally a paroxetine compound, and to a process for producing a paroxetine compound which comprises treating an N-formyl paroxetine compound of formula (1) with a de-formylation agent, to a compound having the formula (2), to a process for determining the stability or purity of a paroxetine substance or composition, which comprises assaying a paroxetine substance or composition for the presence of an N-formyl paroxetine compound of formula (1), and to a process assaying the quality of paroxetine, which comprises forming a production lot of paroxetine pharmaceutical solid dosage forms wherein each dosage form comprises paroxetine or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable exipient; removing a sample of said paroxetine pharmaceutical solid dosage forms from said production lot; assaying said sample for the presence and/or amount of N-formyl paroxetine; and selling or releasing said production lot if said sample passes said assay with respect to the presence or amount of N-formyl paroxetine.

6. 发明公开

EP1280775A1 TOSYLATE SALTS OF 4-(p-FLUOROPHENYL)-PIPERIDINE-3-CARBINOLS 审中-公开
标题翻译：苯氧基苯酚4-（对氟苯基） - 哌啶-3-羰基苯酚
公开(公告)号：EP1280775A1
公开(公告)日：2003-02-05
申请号：EP00927978.7
申请日：2000-05-12
申请人： Synthon B.V.
发明人： PETERS, Theodorus, Hendricus, Antonius , LEMMENS, Jacobus, Maria , SLANINA, Pavel
IPC分类号： C07D211/22
CPC分类号： C07D211/22
摘要： A process for purifying a compound of formula (1) from a des-fluoroimpurity of formula (7) wherein R in both compounds (1) and (7) represents a hydrogen atom, a lower alkyl group, an aryl group, an aralkyl group, an alkoxycarbonyl group or an aryloxycarbonyl group, which comprises the step of reacting a compound of formula (1) with toluene sulfonic acid.

7. 发明公开

EP1124802A1 PROCESS FOR PRODUCING 4-ARYLPIPERIDINE-3-CARBINOLS AND RELATED COMPOUNDS 审中-公开
标题翻译：用于生产4-芳基哌啶-3-甲醇（衍生物）及相关化合物
公开(公告)号：EP1124802A1
公开(公告)日：2001-08-22
申请号：EP99951035.7
申请日：1999-11-01
申请人： Synthon B.V.
发明人： PETERS, Theodorus, Hendricus, Antonius , BENNEKER, Franciscus, Bernardus, Gemma , HOORN, Hans, Jan , PICHA, Frantisek
IPC分类号： C07D211/76 , C07D211/22
CPC分类号： C07D211/76 , C07D211/22
摘要： Aryl-2-piperidones of formula (7) can be reduced to form aryl-piperidine carbinols of formula (1), which are useful in forming a variety of pharmaceutical compounds including paroxetine, in good yield and purity. Related compounds and synthesis schemes are also set forth. In said formulas, X represents a hydrogen atom, a halogen atom, a lower alkyl group, an aralkyl group, an alkoxy group, a dialkylamino group or an alkylthio group; R represents a hydrogen atom, a lower alkyl group, an aryl group, an aralkyl group, an alkoxycarbonyl group, aralkoxycarbonyl group or an aryloxycarbonyl group; and R1 represents a hydrogen atom, a lower alkyl group, an aryl group or an aralkyl group.

8. 发明公开

EP1711503A1 SYNTHESIS OF OLANZAPINE AND INTERMEDIATES THEREOF 审中-公开
标题翻译：奥氮平及中间体合成方法
公开(公告)号：EP1711503A1
公开(公告)日：2006-10-18
申请号：EP05707056.7
申请日：2005-01-26
申请人： Synthon B.V.
发明人： KELTJENS, Rolf , PETERS, Theodorus, Hendricus, Antonius
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Olanzapine and salts thereof are made by a process that utilizes an N-formyl olanzapine intermediate of formula (4) or a salt thereof.

9. 发明授权

EP1286965B1 PIPERIDINE COMPOUNDS AND PROCESS FOR PROVIDING SUCH 无效
标题翻译：哌啶和方法及其
公开(公告)号：EP1286965B1
公开(公告)日：2004-01-14
申请号：EP00927979.5
申请日：2000-05-12
申请人： Synthon B.V.
发明人： PETERS, Theodorus, Hendricus, Antonius , LEMMENS, Jacobus, Maria , SLANINA, Pavel
IPC分类号： C07D211/22 , C07D405/12
CPC分类号： C07D211/22 , C07D405/12
摘要： Process for providing a compound of formula (6), a hydrate, solvate, and/or salt thereof, for example a pharmaceutically acceptable acid addition salt, comprising the step of reacting a compound of formula (1), with a tosyl moiety, providing compound.

10. 发明公开

EP1163241A1 ZOLPIDEM SALTS 有权
标题翻译：唑吡坦的盐类
公开(公告)号：EP1163241A1
公开(公告)日：2001-12-19
申请号：EP00913159.0
申请日：2000-03-13
申请人： Synthon B.V.
发明人： ETTEMA, Gerrit, Jan, Bouke , LEMMENS, Jacobus, Maria , PETERS, Theodorus, Hendricus, Antonius , PICHA, Frantisek
IPC分类号： C07D471/04 , A61K31/437 , A61P25/20
CPC分类号： C07D471/04
摘要： The invention relates to a zolpidem salt, excluding the salt zolpidem tartrate exhibiting a melting endotherm corresponding to zolpidem free base upon heating from about 20 °C to about 250 °C at a rate of 5 °C/minute.

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