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公开(公告)号:US20080139607A1
公开(公告)日:2008-06-12
申请号:US11930232
申请日:2007-10-31
申请人: Fredrik Almqvist , Erik Chorell , Pralay Das , Hans Emtenas , Ola Fjellstrom , Mickael Mogemark , Magnus Polla , Veronica Aberg
发明人: Fredrik Almqvist , Erik Chorell , Pralay Das , Hans Emtenas , Ola Fjellstrom , Mickael Mogemark , Magnus Polla , Veronica Aberg
IPC分类号: A61K31/4365 , C07D471/04 , C07D211/76 , A61K31/4412 , A61P9/10 , A61P9/00 , A61P11/00 , A61P35/00
CPC分类号: C07D513/04 , C07D213/64
摘要: The present invention relates to new compounds of formula (I), (II), or (III) wherein R1, R2, R3, R4, R5 and W are as defined herein, and methods of using the compounds to inhibit PAI-1 and to treat PAI-1 related disorders.
摘要翻译: 本发明涉及新的式(I),(II)或(III)化合物,其中R 1,R 2,R 3, R 4,R 5和W如本文所定义,以及使用该化合物抑制PAI-1并治疗PAI-1相关疾病的方法。
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公开(公告)号:US08598195B2
公开(公告)日:2013-12-03
申请号:US12990415
申请日:2009-04-30
申请人: Fredrik Almqvist , Magnus Sellstedt , Pralay Das
发明人: Fredrik Almqvist , Magnus Sellstedt , Pralay Das
IPC分类号: C07D417/14 , A61K31/4365 , A61K31/437
CPC分类号: C07D471/04 , C07D513/14
摘要: The present invention relates to new compounds of the formula (I), (II), or (III) wherein R1, R2, R3, R4, R5 and W are as defined herein, and pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially Aβ amyloid disease, such as observed in Alzheimer's disease, infectious diseases, PAI-I related disease, and in the manufacture of medicaments for such treatment.
摘要翻译: 本发明涉及式(I),(II)或(III)的新化合物,其中R 1,R 2,R 3,R 4,R 5和W如本文所定义,以及含有它们的药物组合物及其在 治疗淀粉样蛋白病,尤其是阿尔茨海默氏病,阿尔茨海默病,感染性疾病,PAI-1相关疾病以及制造用于治疗的药物等。
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公开(公告)号:US20110160241A1
公开(公告)日:2011-06-30
申请号:US12990415
申请日:2009-04-30
申请人: Fredrik Almqvist , Magnus Sellstedt , Pralay Das
发明人: Fredrik Almqvist , Magnus Sellstedt , Pralay Das
IPC分类号: A61K31/4365 , C07D495/14 , A61P9/00 , A61P9/10 , A61P11/00 , A61P3/10 , A61P3/04 , A61P25/28 , A61P35/00
CPC分类号: C07D471/04 , C07D513/14
摘要: The present invention relates to new compounds of the formula (I), (II), or (III) wherein R1, R2, R3, R4, R5 and W are as defined herein, and pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially Aβ amyloid disease, such as observed in Alzheimer's disease, infectious diseases, PAI-I related disease, and in the manufacture of medicaments for such treatment.
摘要翻译: 本发明涉及式(I),(II)或(III)的新化合物,其中R 1,R 2,R 3,R 4,R 5和W如本文所定义,以及含有它们的药物组合物及其在 治疗淀粉样疾病,特别是A&bgr; 淀粉样变性疾病,例如在阿尔茨海默病中观察到的,感染性疾病,PAI-1相关疾病以及用于制备用于治疗的药物。
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公开(公告)号:US07411066B2
公开(公告)日:2008-08-12
申请号:US11581518
申请日:2006-10-16
申请人: Scott J. Hultgren , Jerome S. Pinkner , Fredrik Almqvist , Nils Pemberton , Veronica Aberg , Andreas Larsson
发明人: Scott J. Hultgren , Jerome S. Pinkner , Fredrik Almqvist , Nils Pemberton , Veronica Aberg , Andreas Larsson
IPC分类号: C07D279/00 , C07F9/00
CPC分类号: C07D513/04
摘要: Novel amino methylated 2-pyridinones, precursors, intermediates, and derivatives; the methods for the preparation of the same; uses of the same for inhibiting pili formation in bacteria; and pharmaceutical compositions comprising these compounds are described in this application. The present compounds may be employed to inhibit biofilm formation and thereby inhibit adherence of bacteria to a host cell.
摘要翻译: 新型氨基甲基化2-吡啶酮,前体,中间体和衍生物; 其制备方法; 用于抑制细菌中的细菌形成; 并且包含这些化合物的药物组合物在本申请中描述。 本发明化合物可用于抑制生物膜形成,从而抑制细菌对宿主细胞的粘附。
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公开(公告)号:US07915417B2
公开(公告)日:2011-03-29
申请号:US12189443
申请日:2008-08-11
申请人: Scott J. Hultgren , Jerome S. Pinkner , Fredrik Almqvist , Nils Pemberton , Veronica Aberg , Andreas Larsson
发明人: Scott J. Hultgren , Jerome S. Pinkner , Fredrik Almqvist , Nils Pemberton , Veronica Aberg , Andreas Larsson
IPC分类号: C07D279/00 , C07F9/00
CPC分类号: C07D513/04
摘要: Novel amino methylated 2-pyridinones, precursors, intermediates, and derivatives; the methods for the preparation of the same; uses of the same for inhibiting pili formation in bacteria; and pharmaceutical compositions comprising these compounds are described in this application. The present compounds may be employed to inhibit biofilm formation and thereby inhibit adherence of bacteria to a host cell.
摘要翻译: 新型氨基甲基化2-吡啶酮,前体,中间体和衍生物; 其制备方法; 用于抑制细菌中的细菌形成; 并且包含这些化合物的药物组合物在本申请中描述。 本发明化合物可用于抑制生物膜形成,从而抑制细菌对宿主细胞的粘附。
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公开(公告)号:US20080311644A1
公开(公告)日:2008-12-18
申请号:US12189443
申请日:2008-08-11
申请人: Scott J. Hultgren , Jerome S. Pinkner , Fredrik Almqvist , Nils Pemberton , Veronica Aberg , Andreas Larsson
发明人: Scott J. Hultgren , Jerome S. Pinkner , Fredrik Almqvist , Nils Pemberton , Veronica Aberg , Andreas Larsson
IPC分类号: C12N1/20 , C07D513/04 , C07D413/14
CPC分类号: C07D513/04
摘要: Novel amino methylated 2-pyridinones, precursors, intermediates, and derivatives; the methods for the preparation of the same; uses of the same for inhibiting pili formation in bacteria; and pharmaceutical compositions comprising these compounds are described in this application. The present compounds may be employed to inhibit biofilm formation and thereby inhibit adherence of bacteria to a host cell.
摘要翻译: 新型氨基甲基化2-吡啶酮,前体,中间体和衍生物; 其制备方法; 用于抑制细菌中的细菌形成; 并且包含这些化合物的药物组合物在本申请中描述。 本发明化合物可用于抑制生物膜形成,从而抑制细菌对宿主细胞的粘附。
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公开(公告)号:US20070082887A1
公开(公告)日:2007-04-12
申请号:US11581518
申请日:2006-10-16
申请人: Scott Hultgren , Jerome Pinkner , Fredrik Almqvist , Nils Pemberton , Veronica Aberg , Andreas Larsson
发明人: Scott Hultgren , Jerome Pinkner , Fredrik Almqvist , Nils Pemberton , Veronica Aberg , Andreas Larsson
IPC分类号: A61K31/55 , A61K31/4745 , C07D455/02
CPC分类号: C07D513/04
摘要: Novel amino methylated 2-pyridinones, precursors, intermediates, and derivatives; the methods for the preparation of the same; uses of the same for inhibiting pili formation in bacteria; and pharmaceutical compositions comprising these compounds are described in this application. The present compounds may be employed to inhibit biofilm formation and thereby inhibit adherence of bacteria to a host cell.
摘要翻译: 新型氨基甲基化2-吡啶酮,前体,中间体和衍生物; 其制备方法; 用于抑制细菌中的细菌形成; 并且包含这些化合物的药物组合物在本申请中描述。 本发明化合物可用于抑制生物膜形成,从而抑制细菌对宿主细胞的粘附。
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公开(公告)号:US20110203995A1
公开(公告)日:2011-08-25
申请号:US12931829
申请日:2011-02-11
申请人: Jonas Persson , Kjell Öberg , Fredrik Almqvist , Knut Irgum
发明人: Jonas Persson , Kjell Öberg , Fredrik Almqvist , Knut Irgum
CPC分类号: B01J19/28 , B01D15/02 , B01D15/1892 , B01F7/00033 , B01F7/00041 , B01F7/006 , B01F7/007 , B01F7/1625 , B01F7/163 , B01F7/1635 , B01F11/0088 , B01F13/0818 , B01J4/007 , B01J8/025 , B01J8/10 , B01J19/1843 , B01J47/00 , B01J47/10 , B01J47/11 , B01J2208/00433 , B01J2208/00442 , B01J2208/00814 , B01J2208/028 , B01J2219/00139 , B01J2219/00141 , Y10T137/0318
摘要: A device is provided for performing chemical transformation in a fluid, with a flow distributor having at least one fluid medium inlet, at least one fluid medium outlet, and at least one confinement wherein the chemical transformation is performed; and a means for rotating, rocking, wagging, or oscillating the device. At least one confinement may be equipped with a provision for providing heat, cooling, sound, light or other types of radiation, such provision being contacted to an external source through an actuator shaft. The flow distributor may be provided with sectors connected with the centrally located fluid medium inlet and a designated peripheral fluid medium outlet. The means for rotating, rocking, wagging, or oscillating the device may be an element producing magnetic fields or a shaft mechanically connected to an external actuating device.
摘要翻译: 提供了一种用于在流体中进行化学转化的装置,流量分配器具有至少一个流体介质入口,至少一个流体介质出口和至少一个进行化学转化的限制; 以及用于旋转,摇摆,摇摆或摆动装置的装置。 至少一个限制可以配备有用于提供热,冷却,声音,光或其他类型的辐射的设备,这种设备通过致动器轴与外部源接触。 流量分配器可以设置有与中心定位的流体介质入口和指定的外围流体介质出口连接的区段。 用于旋转,摇摆,摆动或摆动装置的装置可以是产生磁场的元件或机械地连接到外部致动装置的轴。
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公开(公告)号:US20100119424A1
公开(公告)日:2010-05-13
申请号:US12451432
申请日:2008-05-14
申请人: Fredrik Almqvist , Basudeb Basu
发明人: Fredrik Almqvist , Basudeb Basu
CPC分类号: C07C67/343 , B01J23/44 , B01J31/08 , B01J31/165 , B01J37/06 , B01J2231/4211 , B01J2231/4261 , B01J2531/824 , C07C1/321 , C07C17/263 , C07C37/18 , C07C41/30 , C07C2523/44 , C07C2531/08 , C07C2603/24 , C07D213/61 , C07D401/04 , C07D413/04 , C07D491/147 , C07C15/14 , C07C25/18 , C07C69/618 , C07C69/65 , C07C43/205 , C07C39/15
摘要: The present invention relates to a method of producing a heterogeneous catalyst suitable for catalyzing Heck, Suzuki-Miyaura Sonogashira coupling and Buchwald-Hartwig reactions, comprising the steps of: a) providing a macroporous carrier, said macroporous carrier consisting of a core and a plurality of ion exchange groups covalently bonded to the surface of said core, where at least 90% of the ions bound to said carrier are formate ions; b) swelling said carrier in a polar solvent; c) providing a palladium (II) salt; d) suspending said carrier in an organic solvent thereby obtaining a suspension; e) adding said palladium salt to said suspension and allowing the resulting mixture to react at a temperature within the range of 0 70° C. until said carrier has turned black; f) washing said carrier in water; g) drying said carrier under vacuum.
摘要翻译: 本发明涉及适用于催化Heck,Suzuki-Miyaura Sonogashira偶联剂和Buchwald-Hartwig反应的多相催化剂的制备方法,包括以下步骤:a)提供大孔载体,所述大孔载体由核和多个 共价结合到所述芯的表面上的离子交换基团,其中与所述载体结合的至少90%的离子是甲酸根离子; b)在极性溶剂中溶胀载体; c)提供钯(II)盐; d)将所述载体悬浮在有机溶剂中,从而获得悬浮液; e)将所述钯盐加入到所述悬浮液中,并使所得混合物在0℃至70℃的温度下反应,直到所述载体变黑; f)在水中清洗载体; g)在真空下干燥所述载体。
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公开(公告)号:US06495539B1
公开(公告)日:2002-12-17
申请号:US09252792
申请日:1999-02-19
IPC分类号: C07D50100
CPC分类号: C07D499/00 , C07D277/12
摘要: Compounds of the formula and the salts, esters and amides thereof wherein Z is S, SO, SO2 or O; each of R1, R2 and R3 is independently H or substituted or unsubstituted alkyl (1-10C), substituted or unsubstituted alkenyl, substituted or unsubstituted acyl (2-11C), substituted or unsubstituted aryl (6-14C), substituted or unsubstituted arylcarbonyl (7-15C), substituted or unsubstituted arylalkyl (7-15C), substituted or unsubstituted pyridyl wherein substituents on any alkyl, alkenyl, or acyl moiety are selected from the group consisting of halo, and RO, wherein R is H or alkyl (1-6C), and substituents on any aryl or pyridyl moiety are selected from the group consisting of halo, and RO, where R is H or alkyl (1-6C), —CN and —CF3; with the proviso that R1 is not H and R1 and R3 are not identical and with the proviso that in formula (1), the B ring may contain one double bond that is located between positions 2 and 3, and in formula (2), the B ring may contain one double bond that can be located between positions 2 and 3 or positions 3 and 4 are useful as antibacterial agents.
摘要翻译: 式中的化合物及其盐,酯和酰胺,其中Z为S,SO,SO 2或O; R 1,R 2和R 3各自独立地为H或取代或未取代的烷基(1-10C),取代或未取代的烯基,取代或未取代的酰基 (2-11C),取代或未取代的芳基(6-14C),取代或未取代的芳基羰基(7-15C),取代或未取代的芳基烷基(7-15C),取代或未取代的吡啶基,其中任何烷基,链烯基或酰基 部分选自卤素和RO,其中R是H或烷基(1-6C),任何芳基或吡啶基部分上的取代基选自卤素和RO,其中R是H或 烷基(1-6C),-CN和-CF3; 条件是R1不是H,R1和R3不相同,条件是在式(1)中,B环可以含有位于2和3之间的一个双键,而在式(2)中, B环可以含有一个可以位于2和3位之间的双键,或3或4位可用作抗菌剂。
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