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1.发明授权A 1-(1H-1,2,4-TRIAZOL-1-YL)BUTAN-2-OL DERIVATIVE FOR PHARMACEUTICAL USE, AND THE USE OF A 1-(1H-1,2,4-TRIAZOL-1-YL)BUTAN-2-OL DERIVATE WITH SUBSTANTIALLY UNDEFINED CRYSTAL SHAPE FOR PREPARING SAID 1-(1H-1,2,4-TRIAZOL-1-YL)BUTAN-2-OL DERIVATIVE 有权1-（1H-1,2,4-三唑-1-基）药物用途丁-2-醇衍生物和1-（1H-1,2,4-三唑-1-基）USE丁-2- 具有未定义晶型用于制备醇衍生物SAID 1-（1H-1,2,4- TRIAHOL -1-基）丁-2-醇衍生物
公开(公告)号：EP2470529B1
公开(公告)日：2014-11-19
申请号：EP10737869.7
申请日：2010-07-23
申请人： Medichem, S.A.
IPC分类号： C07D403/06 , A61K31/506 , A61P31/10
CPC分类号： C07D403/06 , Y10T428/2982
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2.发明授权
公开(公告)号：EP1426356B1
公开(公告)日：2008-04-16
申请号：EP01969812.5
申请日：2001-09-14
申请人： Medichem S.A.
发明人： BOSCH I LLADO, Jordi , CAMPS GARCIA, Pelayo , CONTRERAS LASCORZ, Juan , ONRUBIA MIGUEL, Ma Carmen
IPC分类号： C07C233/11 , C07C231/02 , C07D241/04
CPC分类号： C07C237/22 , C07D241/04
摘要： The invention relates to intermediate compounds that are used for the preparation of mirtazapine and the production methods thereof. The inventive method is used to produce (+/-)-3-phenyl-1-methylpiperazine which is an important intermediate for the production of mirtazapine. Said method consists in subjecting novel compounds having general formula (I), wherein Z is a leaving group that can undergo nucleophilic displacement, to a cyclization reaction in the presence of a reducing agent. The invention also relates to a method of producing novel compounds having formula (I).
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3.发明公开A 1-(1H-1,2,4-TRIAZOL-1-YL)BUTAN-2-OL DERIVATIVE FOR PHARMACEUTICAL USE, AND THE USE OF A 1-(1H-1,2,4-TRIAZOL-1-YL)BUTAN-2-OL DERIVATE WITH SUBSTANTIALLY UNDEFINED CRYSTAL SHAPE FOR PREPARING SAID 1-(1H-1,2,4-TRIAZOL-1-YL)BUTAN-2-OL DERIVATIVE 有权1-（1H-1,2,4-三唑-1-基）药物用途丁-2-醇衍生物和1-（1H-1,2,4-三唑-1-基）USE丁-2- 具有未定义晶型用于制备醇衍生物SAID 1-（1H-1,2,4- TRIAHOL -1-基）丁-2-醇衍生物
公开(公告)号：EP2470529A1
公开(公告)日：2012-07-04
申请号：EP10737869.7
申请日：2010-07-23
申请人： Medichem, S.A.
IPC分类号： C07D403/06 , A61K31/506 , A61P31/10
CPC分类号： C07D403/06 , Y10T428/2982
摘要： The present invention relates to voriconazole, processes of preparing voriconazole, and pharmaceutical compositions and therapeutic uses thereof. In particular, it relates to a voriconazole product prepared from voriconazole with substantially undefined crystal shape and / or crystal habit and to the provision of voriconazole according to the present invention with modified specific surface area and / or Sauter diameter and / or as appropriate sphericity factor.
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公开(公告)号：EP4003957A1
公开(公告)日：2022-06-01
申请号：EP20746194.8
申请日：2020-07-24
申请人： Medichem, S.A.
IPC分类号： C07D213/74
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5.发明公开
公开(公告)号：EP1426356A1
公开(公告)日：2004-06-09
申请号：EP01969812.5
申请日：2001-09-14
申请人： Medichem S.A.
发明人： BOSCH I LLADO, Jordi , CAMPS GARCIA, Pelayo , CONTRERAS LASCORZ, Juan , ONRUBIA MIGUEL, Ma Carmen
IPC分类号： C07C233/11 , C07C231/02 , C07D241/04
CPC分类号： C07C237/22 , C07D241/04
摘要： Intermediate compounds for the preparation of mirtazapine and obtention methods thereof. A method is described for obtaining (±)-3-phenyl-1-methylpiperazine, an important intermediate for obtaining mirtazapine, which is based on imposing a cyclation reaction, in the presence of a reducing agent, on new compounds of general formula (I)
in which Z is a leaving group capable of undergoing a nucleophylic displacement. A method is also described for obtaining the new compounds of formula (I).摘要翻译： 用于它们的米尔塔扎平和获得方法的方法制备的中间体化合物。 描述了一种方法，用于获得（+/-） - 3-苯基-1-甲基哌嗪，以重要中间体用于获得米氮平，所有这是基于强加环化反应，在还原剂的存在下，对通式的新化合物 （I）
其中Z是能够进行亲核置换的离去基团。 因此一种方法是描述用于获得式（I）的新化合物。
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