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1. 发明申请

WO2012000499A1 NEW POLYMORPHIC FORM OF A CALCIMIMETIC COMPOUND 审中-公开
标题翻译：一种计算化合物的新型多晶型
公开(公告)号：WO2012000499A1
公开(公告)日：2012-01-05
申请号：PCT/DK2011/000071
申请日：2011-06-24
申请人： LEO PHARMA A/S , EBDRUP, Søren , NIELSEN, Kim Troensegaard , GREVE, Tanja Maria
发明人： EBDRUP, Søren , NIELSEN, Kim Troensegaard , GREVE, Tanja Maria
IPC分类号： C07C213/10 , C07C217/74 , A61K31/196 , A61P3/14 , A61P5/18
CPC分类号： C07C217/74 , A61K31/196 , C07C213/10 , C07C2601/08
摘要： The present invention relates to the crystalline, polymorphic Form X of the calcimimetic compound {4-[(1 R , 3 S )-3-(( R )-1 -Naphthalen-1 -yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid, to methods of preparation thereof, to methods of characterization thereof by single crystal X-Ray crystallography (XRC), X-Ray Powder diffractometry, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, Solid State NMR spectroscopy and Differential Scanning Calorimetry (DSC), and to its use. The invention also relates to the preparation of Form X by crystallization from a saturated solution of {4-[(1 R ,3 S )-3-(( R )-1 -Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid in a C 1 -C 6 alkyl alcohol, or alternatively by precipitation from a neutralized saponification reaction mixture following the alkaline hydrolysis of a C 1 -C 6 alkyl ester of {4-[(1 R ,3 S )-3-(( R )-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid.
摘要翻译：本发明涉及拟钙化合物{4 - [（1R，3S）-3 - （（R）-1-萘-1-基 - 乙基氨基） - 环戊基] - 苯氧基} - 乙酸的晶体多晶型X 酸，其制备方法，通过单晶X射线晶体学（XRC），X射线粉末衍射，衰减全反射傅立叶变换红外（ATR-FTIR）光谱，固体NMR光谱和差示扫描的表征方法量热法（DSC）及其用途。本发明还涉及通过从饱和的{4 - [（1R，3S）-3 - （（R）-1-萘-1-基 - 乙基氨基） - 环戊基] - 苯氧基} - 乙酸在C1-C6烷基醇中反应，或者通过碱解水解{4 - [（1R，3S）-3 - （（R） - 1-萘基-1-基 - 乙基氨基） - 环戊基] - 苯氧基} - 乙酸。

2. 发明申请

WO2012000498A1 NEW POLYMORPHIC FORM OF A CALCIMIMETIC COMPOUND 审中-公开
标题翻译：一种计算化合物的新型多晶型
公开(公告)号：WO2012000498A1
公开(公告)日：2012-01-05
申请号：PCT/DK2011/000070
申请日：2011-06-24
申请人： LEO PHARMA A/S , EBDRUP, Søren , NIELSEN, Kim Troensegaard , GREVE, Tanja Maria
发明人： EBDRUP, Søren , NIELSEN, Kim Troensegaard , GREVE, Tanja Maria
IPC分类号： C07C213/10 , C07C217/74 , A61K31/196 , A61P3/14 , A61P5/18
CPC分类号： C07C217/74 , A61K31/196 , A61K31/592 , A61K31/593 , C07C213/10 , C07C2601/08
摘要： The present invention relates to the crystalline, polymorphic Form C of the calcimimetic compound {4-[(1 R ,3 S )-3-(( R )-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid, to methods of preparation thereof, to methods of characterization thereof by single crystal X-Ray crystallography (XRC), X-Ray Powder diffractometry, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, Solid State NMR spectroscopy and Differential Scanning Calorimetry (DSC), and to its use. The invention also relates to the preparation of Form C by crystallization from a saturated solution of {4- [(1 R ,3 S )-3-(( R )-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid in the presence of crystallization seeds of Form C, or alternatively by conversion of an amorphous starting material into the different crystalline polymorphic Form X by crystallization of {4-[(1 R, 3 S )-3-(( R )-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}- acetic acid, followed by a solid solution transformation thereof into the desired polymorphic Form C.
摘要翻译：本发明涉及拟钙化合物{4 - [（1R，3S）-3 - （（R）-1-萘基-1-乙基氨基） - 环戊基] - 苯氧基} - 乙酸的结晶多晶型C 酸，其制备方法，通过单晶X射线晶体学（XRC），X射线粉末衍射，衰减全反射傅立叶变换红外（ATR-FTIR）光谱，固态NMR光谱和差示扫描的表征方法量热法（DSC）及其用途。本发明还涉及通过从饱和的{4 - [（1R，3S）-3 - （（R）-1-萘基-1-基 - 乙基氨基） - 环戊基] - 苯氧基} - 乙酸在形式C的结晶晶种存在下，或者通过{4 - [（1R，3S）-3 - （（R）-1）的结晶将无定形原料转化成不同结晶多晶型X 萘-1-基 - 乙基氨基） - 环戊基] - 苯氧基} - 乙酸，然后将其固溶转化为所需的多晶型C.

3. 发明公开

EP2317996A1 ELTOPRAZINE FOR SUPPRESSION OF L-DOPA INDUCED DYSKINESIAS 审中-公开
标题翻译： ELTROPRAZIN为了降低左旋多巴引起的运动障碍
公开(公告)号：EP2317996A1
公开(公告)日：2011-05-11
申请号：EP09769229.7
申请日：2009-06-23
申请人： Björklund, Anders , Carta, Manolo , Lassen, Jørgen Buus
发明人： Björklund, Anders , Carta, Manolo , Lassen, Jørgen Buus
IPC分类号： A61K31/198 , A61K31/496 , A61P25/14 , A61P25/16
CPC分类号： A61K31/496 , A61K31/198 , A61K2300/00
摘要： This invention relates to the use of the drug Eltoprazine for combating dyskinesias arising from chronic Levodopa (L-DOPA) therapy in patients suffering from Parkinson's disease.

4. 发明公开

EP2311835A1 Novel chromen-2-one derivatives and their use as monoamine neurotransmitter re-uptake inhibitors 审中-公开
标题翻译： Neue Chromen-2-On-Derivate und ihre Verwendung als Monoamin-Neurotransmitter-Wiederaufnahmeinhibitoren
公开(公告)号：EP2311835A1
公开(公告)日：2011-04-20
申请号：EP11150949.3
申请日：2007-02-13
申请人： NeuroSearch AS
发明人： Peters, Dan , Redrobe, John, Paul , Nielsen, Elsebet, Østergaard
IPC分类号： C07D451/06 , A61K31/135 , A61K31/46
CPC分类号： C07D451/06
摘要： This invention relates to novel chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors.
In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
摘要翻译：本发明涉及可用作单胺神经递质再摄取抑制剂的新型色烯-2-酮衍生物。在其它方面，本发明涉及这些化合物在治疗方法中的用途以及包含本发明化合物的药物组合物。

5. 发明授权

EP2081907B1 ARYL PIPERAZINE DERIVATIVES USEFUL FOR THE TREATMENT OF NEUROPSYCHIATRY DISORDERS 有权
标题翻译：精神疾病SUITABLE ARYLPIPERAZINDERIVATE NEURO的治疗
公开(公告)号：EP2081907B1
公开(公告)日：2011-01-26
申请号：EP07821255.2
申请日：2007-10-12
申请人： Universita Degli Studi di Siena
发明人： CAMPIANI, Giuseppe , BUTINI, Stefania , FATTORUSSO, Caterina , FRANCESCHINI, Silvia , THALE, Zia Irene , NIELSEN, Karin Sandager , SCHEEL-KRÜGER, Jørgen , MADSEN, Lars Siim
IPC分类号： C07D215/48 , A61K31/4709 , A61P25/18
CPC分类号： C07D215/48
摘要： This invention provides novel aryl piperazine derivatives represented by Formula (I) having medical utility, in particular as modulators of dopamine and serotonin receptors, preferably the D3, 5HT1A and 5-HT2A receptor subtypes, and in particular useful for the treatment of neuropsychiatric disorders, incl. schizophrenia.

6. 发明授权

EP2121677B1 NOVEL CHROMEN-2-ONE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS 有权
公开(公告)号：EP2121677B1
公开(公告)日：2010-11-03
申请号：EP07857757.4
申请日：2007-12-18
申请人： NeuroSearch A/S
发明人： PETERS, Dan , REDROBE, John, Paul , OLSEN, Gunnar, M. , NIELSEN, Elsebet Østergaard
IPC分类号： C07D451/06 , A61K31/46 , A61P25/00
CPC分类号： C07D451/06
摘要： This invention relates to novel chromen-2-one derivatives of Formula (I) useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

7. 发明公开

EP2235006A1 N-ARYL-N-PIPERIDIN-4-YL-PROPIONAMIDE DERIVATIVES AND THEIR USE AS OPIOID RECEPTOR LIGANDS 审中-公开
标题翻译： N-芳基-N-哌啶-4-炔丙酰胺衍生物及其作为阿片受体配体的用途
公开(公告)号：EP2235006A1
公开(公告)日：2010-10-06
申请号：EP08861973.9
申请日：2008-12-18
申请人： NeuroSearch A/S
发明人： PETERS, Dan , MUNRO, Gordon , NIELSEN, Elsebet, Østergaard
IPC分类号： C07D405/06 , A61K31/4468 , A61P25/00
CPC分类号： C07D405/06
摘要： This invention relates to novel /\/-aryl-/\/-piperidin-4-yl-propionamide derivatives useful as opioid receptor ligands. In other aspects the invention relates to the use of these compounds in a method for therapy, such as for the treatment of pain, and to pharmaceutical compositions comprising the compounds of the invention.
摘要翻译：本发明涉及用作阿片受体配体的新的N-芳基-N-哌啶-4-基丙酰胺衍生物。在其它方面，本发明涉及这些化合物在用于治疗的方法例如用于治疗疼痛的用途中的用途，以及涉及包含本发明化合物的药物组合物。

8. 发明公开

EP2231610A1 NOVEL 2-DIMETHYLAMINO-3-AMIDO-6-AMINO-PYRIDINE DERIVATIVES USEFUL AS POTASSIUM CHANNEL ACTIVATORS 审中-公开
标题翻译： NEW 2-二甲基氨基-3-氨基-6-氨基 - 吡啶衍生物可用作钾通道活化剂
公开(公告)号：EP2231610A1
公开(公告)日：2010-09-29
申请号：EP08859320.7
申请日：2008-12-10
申请人： NeuroSearch A/S
发明人： BROWN, William, Dalby , JESSEN, Carsten , STRØBÆK, Dorte
IPC分类号： C07D213/75 , A61K31/44 , A61P29/00
CPC分类号： C07D213/75
摘要： This invention relates to novel 2-dimethylamino-3-amido-6-amino-pyhdine derivatives having medical utility, to use of the 2-dimethylamino-3-amido-6-amino- pyridine derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the 2-dimethylamino-3-amido-6-amino- pyridine derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to activation of Kv7 channels.

9. 发明公开

EP2201005A1 NOVEL PHENOXAZIN-3-ONE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS 审中-公开
标题翻译： NEW吩恶嗪-3-酮衍生物及其作为单胺神经递质再摄取抑制剂
公开(公告)号：EP2201005A1
公开(公告)日：2010-06-30
申请号：EP08803804.7
申请日：2008-09-08
申请人： NeuroSearch A/S
发明人： PETERS, Dan , REDROBE, John, Paul , NIELSEN, Elsebet, Østergaard
IPC分类号： C07D413/12 , A61K31/535 , A61P25/00
CPC分类号： C07D413/12
摘要： This invention relates to novel phenoxazin-3-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

10. 发明公开

EP2152272A2 NOVEL 2,3-DIAMINO-QUINAZOLINONE DERIVATIVES AND THEIR MEDICAL USE 审中-公开
标题翻译：新的2,3-二氨基喹唑啉酮衍生物及其医药用途
公开(公告)号：EP2152272A2
公开(公告)日：2010-02-17
申请号：EP08759923.9
申请日：2008-05-22
申请人： NeuroSearch A/S
发明人： JESSEN, Carsten , BROWN, William, Dalby , DEMNITZ, Joachim , STRØBÆK, Dorte , KORSGAARD, Mads, Gersdorff , CHRISTOPHERSEN, Palle
IPC分类号： A61K31/498 , C07D239/95 , C07D403/04 , C07D405/12 , A61P25/06 , A61P25/08 , A61P25/18 , A61P25/24 , A61P13/00
CPC分类号： C07D239/95 , C07D403/04 , C07D405/12
摘要： This invention relates to novel 2,3-diamino-quinazolinone derivatives having medical utility, to use of the 2,3-diamino-quinazolinone derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the 2,3- diamino-quinazolinone derivatives of the invention, and to methods of treating a disord disease or a condition of a subject, which disorder, disease or condition is responsiv to activation of KV7 channels. A 2,3-diamino-quinazolinone derivative of Formula (I) a stereoisomer or a mixture of its stereoisomers, or a pharmaceutically-acceptable addition salt thereof, or an N-oxide thereof.

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