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71. 发明授权

US08343963B2 Sulfamoyl-phenyl-ureido compounds and their use as medicament 有权
标题翻译：磺酰氨基 - 苯基 - 脲基化合物及其作为药物的用途
公开(公告)号：US08343963B2
公开(公告)日：2013-01-01
申请号：US12696479
申请日：2010-01-29
申请人： Stefano Pegoraro
发明人： Stefano Pegoraro
IPC分类号： A61K31/5375 , A61K31/541 , A61K31/495 , A61K31/17 , C07C311/47 , C07D207/09 , C07D211/22 , C07D211/62 , C07D213/36 , C07D215/42 , C07D277/04 , C07D279/12
CPC分类号： C07D295/13 , C07C311/47 , C07C317/42 , C07D207/09 , C07D207/14 , C07D209/44 , C07D211/22 , C07D211/46 , C07D211/62 , C07D211/74 , C07D213/36 , C07D215/42 , C07D241/08 , C07D277/04 , C07D279/12 , C07D295/15 , C07D295/205 , C07D295/26 , C07D307/14 , C07D307/64 , C07D317/28
摘要： The present invention relates to novel sulfamoyl-phenyl-ureido compounds having the formula (I) or a physiologically acceptable salt or derivative thereof which are suitable for the therapy of infections caused by protozoa and in particular uncomplicated or severe malaria caused by plasmodia.
摘要翻译：本发明涉及具有式（I）的新型氨磺酰基 - 苯基 - 脲基化合物或其生理上可接受的盐或衍生物，其适于治疗由原生动物引起的感染，特别是由疟原虫引起的不复杂或严重的疟疾。

72. 发明申请

US20120309648A1 INTEGRATED MICROFLUIDICS FOR HIGHLY PARALLEL SCREENING OF CHEMICAL REACTIONS 审中-公开
标题翻译：综合微流化学高效平行筛选化学反应
公开(公告)号：US20120309648A1
公开(公告)日：2012-12-06
申请号：US12667861
申请日：2008-07-07
申请人： Hsian-Rong Tseng , Jinyi Wang , Guodong Sui , Kym F. Faull , Yanju Wang , Wei-Yu Lin
发明人： Hsian-Rong Tseng , Jinyi Wang , Guodong Sui , Kym F. Faull , Yanju Wang , Wei-Yu Lin
IPC分类号： C40B60/12 , C40B30/08
CPC分类号： B01F13/0059 , B01F5/102 , B01J2219/00315 , B01J2219/00317 , B01J2219/00353 , B01J2219/00389 , B01J2219/00479 , B01J2219/00702 , B01J2219/0072 , B01L3/5027 , C07C247/10 , C07C247/12 , C07C247/14 , C07C323/59 , C07C2601/08 , C07C2601/14 , C07D211/68 , C07D213/42 , C07D213/74 , C07D215/42 , C07D235/14 , C07D295/13 , C07D295/32 , C07D307/52 , C07D311/14 , C07D317/28 , C07D333/20 , C40B40/04 , C40B50/08 , C40B60/12 , G01N2035/00544
摘要： A microfluidic system has a microfluidic mixer and a sample storage component that is in fluid connection with the microfluidic mixer. The microfluidic mixer has a mixing section; a target molecule input section that is in fluid connection with the mixing section, the target molecule input section being suitable to provide a fluid into the mixing section that contains molecules to be targeted by chemical reactions; a first reagent input section that is in fluid connection with the mixing section, the first reagent input section being structured to selectively provide a first reagent selected from a plurality of reagents to test a chemical reaction with the target molecules; a second reagent input section that is in fluid connection with the mixing section, the second reagent input section being structured to selectively provide a second reagent selected from a plurality of reagents to test a chemical reaction with the target molecules and said first reagent; and a neutral fluid input section that is in selectable fluid connection with the sample storage component, the neutral fluid input section being structured to selectively provide a neutral fluid into the sample storage component between successive samples provided to the sample storage component to separate successive samples in a stratified arrangement.
摘要翻译：微流体系统具有微流控混合器和与微流体混合器流体连接的样品存储组件。微流体混合器具有混合部分; 与混合部分流体连接的目标分子输入部分，靶分子输入部分适合于通过化学反应将含有分子的流体提供给混合部分; 与所述混合部分流体连接的第一试剂输入部，所述第一试剂输入部构造成选择性地提供选自多种试剂的第一试剂，以测试与所述靶分子的化学反应; 与所述混合部分流体连接的第二试剂输入部，所述第二试剂输入部构造成选择性地提供选自多种试剂的第二试剂，以测试与所述靶分子和所述第一试剂的化学反应; 以及中性流体输入部分，其与所述样品存储部件可选择性地流体连接，所述中性流体输入部分被构造成在提供给所述样品存储部件的连续样品之间选择性地将中性流体提供到所述样品存储部件中，以将分层安排。

73. 发明申请

US20120295910A1 New Phenylsulfamoyl Benzamide Derivatives as Bradykinin Antagonists 审中-公开
标题翻译：新的苯基氨磺酰苯甲酰胺衍生物作为缓激肽拮抗剂
公开(公告)号：US20120295910A1
公开(公告)日：2012-11-22
申请号：US13564360
申请日：2012-08-01
申请人： Gyula Beke , Eva Bozo , Sandor Farkas , Katalin Hornok , Gyorgy Keseru , Eva Schmidt , Eva Szentirmay , Istvan Vago , Monika Vastag
发明人： Gyula Beke , Eva Bozo , Sandor Farkas , Katalin Hornok , Gyorgy Keseru , Eva Schmidt , Eva Szentirmay , Istvan Vago , Monika Vastag
IPC分类号： A61K31/535 , A61K31/4965 , A61K31/4545 , A61K31/445 , A61K31/4164 , C07D207/50 , C07D265/30 , C07D401/02 , C07D241/04 , C07D401/04 , C07D211/56 , C07D233/88 , A61K31/497 , A61K31/40
CPC分类号： C07C311/21 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D209/08 , C07D211/26 , C07D211/58 , C07D213/40 , C07D213/75 , C07D231/40 , C07D233/54 , C07D233/64 , C07D235/30 , C07D241/08 , C07D261/14 , C07D277/46 , C07D277/62 , C07D277/82 , C07D285/135 , C07D295/13 , C07D295/135 , C07D317/46
摘要： The present invention relates to new sulfonamide derivatives of formula (I), wherein R1-R8 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
摘要翻译：本发明涉及新的式（I）磺酰胺衍生物，其中R 1 -R 8和Z如权利要求中所定义，和光学对映体或外消旋体和/或其盐和/或其水合物和/或溶剂化物，它们是选择性拮抗剂缓激肽B1的制备方法，制备这些相同化合物的方法，含有它们的药物组合物及其在治疗或预防疼痛和炎症病症中的用途。

74. 发明授权

US08299302B2 4-Cycloalkyl or 4-substituted phenoxyphenylamidines and use thereof as fungicides 有权
标题翻译： 4-环烷基或4-取代的苯氧基苯基脒，并将其用作杀真菌剂
公开(公告)号：US08299302B2
公开(公告)日：2012-10-30
申请号：US12530777
申请日：2008-03-08
申请人： Klaus Kunz , Ralf Dunkel , Jörg Nico Greul , Oliver Guth , Kerstin Ilg , Darren James Mansfield , Wahed Ahmed Moradi , Thomas Seitz , Peter Dahmen , Ulrike Wachendorff-Neumann , Arnd Voerste , Jean-Pierre Vors
发明人： Klaus Kunz , Ralf Dunkel , Jörg Nico Greul , Oliver Guth , Kerstin Ilg , Darren James Mansfield , Wahed Ahmed Moradi , Thomas Seitz , Peter Dahmen , Ulrike Wachendorff-Neumann , Arnd Voerste , Jean-Pierre Vors
IPC分类号： C07C257/00
CPC分类号： C07C257/12 , C07C217/90 , C07D211/14 , C07D295/13
摘要： The present invention relates to 4-cycloalkyl- or 4-aryl-substituted phenoxyphenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to a composition for this purpose, comprising the phenoxyphenylamidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.
摘要翻译：本发明涉及通式（I）的4-环烷基 - 或4-芳基取代的苯氧基苯脒，其制备方法，使用本发明的脒控制有害微生物以及组合物为此目的，包含根据本发明的苯氧基苯基脒。此外，本发明涉及通过将根据本发明的化合物施用于微生物和/或其栖息地来控制不想要的微生物的方法。

75. 发明申请

US20120237552A1 Peptoid Agonists of Nerve Growth Factor and Their Use as Medicaments 审中-公开
标题翻译：神经生长因子的消化不良激素及其作为药物的用途
公开(公告)号：US20120237552A1
公开(公告)日：2012-09-20
申请号：US13393458
申请日：2010-08-31
申请人： Beatriz Moreno , Pablo Villoslada , Joaquin Messeguer , Gloria Navarro , Angel Messeguer
发明人： Beatriz Moreno , Pablo Villoslada , Joaquin Messeguer , Gloria Navarro , Angel Messeguer
IPC分类号： A61K38/06 , A61P25/02 , A61P25/18 , A61P25/24 , A61P25/16 , A61P27/06 , A61P25/28 , A61P25/00 , A61P37/02 , A61P35/00 , A61P35/02 , A61P29/00 , A61P27/02 , A61P21/00 , C07K5/083
CPC分类号： C07D295/12 , A61K38/00 , C07D295/13 , C07K5/0806
摘要： Neurotrophin binding to its specific receptors Trk A and p75 leads to the activation of multiple signalling cascades, culminating in neuroprotective and regenerative effects, including neuronal survival and neurite outgrowth. Neurotrophic factors have been used for the treatment of several neurodegenerative diseases. However, their use is limited by their inability to cross the blood-brain barrier, their short half life and their side effects. Small molecule neurotrophin mimetics may be beneficial in treating a number of neurodegenerative disorders. The present invention shows the capacity of nerve growth factor agonist molecules of Formulae I-IV, as defined in the specification, to induce differentiation in PC 12 cells, promote survival in RN22 cells and activate Trk A, IkBa and SAPK/JNK phosphorylation to various extents in both cell lines. In addition these molecules were able to ameliorate acute experimental autoimmune encephalomyelitis (EAE), a multiple sclerosis (MS) animal model, inhibiting brain inflammation and reducing brain damage. We also observed suppression in the production of pro-inflammatory genes like the inducible nitric oxide synthase. These small molecules with NGF agonist activity may be beneficial for MS and other neurodegenerative diseases due to its neuroprotective and immunomodulatory properties.
摘要翻译：神经营养因子与其特异性受体Trk A和p75结合导致多个信号级联的激活，最终导致神经保护和再生效应，包括神经元存活和神经突生长。神经营养因子已被用于治疗几种神经变性疾病。然而，它们的使用受到无法跨越血脑屏障，半衰期短及其副作用的限制。小分子神经营养因子模拟物可能有益于治疗许多神经变性疾病。本发明显示了本说明书中定义的式I-IV的神经生长因子激动剂分子在PC12细胞中诱导分化的能力，促进RN22细胞中的存活并激活TrkA，IkBa和SAPK / JNK磷酸化到各种两个细胞系的范围。此外，这些分子能够改善急性实验性自身免疫性脑脊髓炎（EAE），多发性硬化（MS）动物模型，抑制脑部炎症并减少脑损伤。我们还观察到产生促炎基因如诱导型一氧化氮合酶的抑制。这些具有NGF激动剂活性的小分子由于其神经保护和免疫调节特性而可能对MS和其它神经变性疾病有益。

76. 发明申请

US20120225881A1 METHODS OF USING AS ANALGESICS 1-BENZYL-1-HYDROXY-2, 3-DIAMINO-PROPYL AMINES, 3-BENZYL-3-HYRDROXY-2-AMINO-PROPIONIC ACID AMIDES AND RELATED COMPOUNDS 有权
标题翻译：使用1-苄基-1-羟基-2,3-二氨基丙酸，3-苄基-3-羟基-2-氨基 - 丙酸和其相关化合物的方法
公开(公告)号：US20120225881A1
公开(公告)日：2012-09-06
申请号：US13450854
申请日：2012-04-19
申请人： Bertrand Leblond , Eric Beausoleil , Thierry Taverne , John E. Donello , Fabien (Jacques) Schweighoffer
发明人： Bertrand Leblond , Eric Beausoleil , Thierry Taverne , John E. Donello , Fabien (Jacques) Schweighoffer
IPC分类号： A61K31/40 , A61K31/5375 , A61P25/00 , A61K31/4025
CPC分类号： C07D265/30 , A61K31/40 , A61K31/4025 , A61K31/4409 , A61K31/4439 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K31/541 , C07D207/09 , C07D213/64 , C07D295/12 , C07D295/13 , C07D295/15 , C07D319/18 , C07D405/06
摘要： The compounds shown by the structural formulas below have analgesic effect and are used in compositions and methods for treating mammal in need of such treatment.
摘要翻译：由下述结构式表示的化合物具有镇痛作用，并用于治疗需要这种治疗的哺乳动物的组合物和方法中。

77. 发明申请

US20120220736A1 ALDIMINES AND COMPOSITIONS COMPRISING ALDIMINE 有权
标题翻译：包含ALDIMINE的ALDIMINES和组合物
公开(公告)号：US20120220736A1
公开(公告)日：2012-08-30
申请号：US13462347
申请日：2012-05-02
申请人： Urs BURCKHARDT
发明人： Urs BURCKHARDT
IPC分类号： C08G73/00 , C07C251/08
CPC分类号： C07C251/08 , C07D295/108 , C07D295/13 , C08G18/12 , C08G18/3256 , C08G18/4812 , C08G18/6696 , C08G18/808 , C08G2190/00 , C09D175/04 , C09J175/04 , C08G18/289 , C08G18/792
摘要： Aldimino containing compounds obtained from a reaction of aldimines of formula (I) with a compound that bears at least one reactive group that can enter into addition reactions with an HX group of an aldimine of formula I. The compounds containing aldimine groups can be used primarily in adhesive and sealant materials, but also in coatings, and can be produced easily from readily available source materials, and have good thermal stability. The tertiary amino group thereof has a surprisingly low alkalinity and can in some cases have a catalytic effect in chemical reaction systems.
摘要翻译：由式（I）的醛亚胺与具有至少一个可与式Ⅰ的醛亚胺的HX基团进行加成反应的至少一个反应性基团的化合物反应获得的含有阿维尼诺的化合物。可以主要使用含有亚胺基的化合物在粘合剂和密封剂材料中，而且在涂料中，并且可以容易地从容易获得的原料生产，并且具有良好的热稳定性。其叔氨基具有令人惊讶的低碱度，并且在一些情况下在化学反应体系中具有催化作用。

78. 发明授权

US08252859B2 Aldimines and compositions comprising aldimine 有权
标题翻译：醛亚胺和组合物，其包含阿维胺
公开(公告)号：US08252859B2
公开(公告)日：2012-08-28
申请号：US12451955
申请日：2008-07-16
申请人： Urs Burckhardt
发明人： Urs Burckhardt
IPC分类号： C08K5/41 , C07C275/00
CPC分类号： C07C251/08 , C07D295/108 , C07D295/13 , C08G18/12 , C08G18/3256 , C08G18/4812 , C08G18/6696 , C08G18/808 , C08G2190/00 , C09D175/04 , C09J175/04 , C08G18/289 , C08G18/792
摘要： Aldimines of formula (I) that are particularly suitable as latent hardeners in curable compositions, particularly compositions having one or two-component isocyanate groups. Due to the presence of the reactive group, they can be converted to compounds of formulas (X) and (XII) having aldimine groups. The aldimines, or the aldimine compounds, can be used primarily in adhesive and sealant materials, but also in coatings, and can be produced easily from readily available source materials, and have good thermal stability. The tertiary amino group thereof has a surprisingly low alkalinity and can in some cases have a catalytic effect in chemical reaction systems.
摘要翻译：在可固化组合物中特别适用作潜在硬化剂的式（I）的醛，特别是具有一个或两个组分的异氰酸酯基团的组合物。由于存在反应性基团，它们可以转化成具有亚胺基的式（X）和（XII）化合物。醛亚胺或醛亚胺化合物可以主要用于粘合剂和密封材料，也可用于涂料中，并且可以容易地从容易获得的原料生产，并且具有良好的热稳定性。其叔氨基具有令人惊讶的低碱度，并且在一些情况下在化学反应体系中具有催化作用。

79. 发明申请

US20120190710A1 BICYCLO-HEPTAN-2-AMINES 有权
公开(公告)号：US20120190710A1
公开(公告)日：2012-07-26
申请号：US13354426
申请日：2012-01-20
申请人： Adeboye Adejare , Zeynep Ates-Alagoz , Boyenoh Gaye
发明人： Adeboye Adejare , Zeynep Ates-Alagoz , Boyenoh Gaye
IPC分类号： A61K31/4453 , C07D309/12 , A61P25/16 , A61P35/00 , A61P25/00 , C07D211/26 , A61K31/351
CPC分类号： C07D295/13 , C07D309/12
摘要： The present invention provides bicyclo-heptan-2-amines that selectively bind to the sigma-2 receptor and are useful in the treatment of diseases related to the sigma-2 receptor, for example, cancer and neurological disorders.
摘要翻译：本发明提供了选择性结合σ-2受体并可用于治疗与σ-2受体有关的疾病，例如癌症和神经障碍的双环庚烷-2-胺。

80. 发明申请

US20120172449A1 POLYAMINE TRANSPORT INHIBITORS AS NOVEL THERAPEUTICS 有权
标题翻译：聚氨酯运输抑制剂作为新治疗药物
公开(公告)号：US20120172449A1
公开(公告)日：2012-07-05
申请号：US13379191
申请日：2010-06-21
申请人： Otto Phanstiel , Jennifer J. Archer
发明人： Otto Phanstiel , Jennifer J. Archer
IPC分类号： A61K31/198 , C07C237/42 , C07C237/22 , A61K31/137 , A61K31/166 , A61P35/00 , C12N5/09 , C12Q1/02 , G01N33/566 , A61P1/00 , A61P29/00 , A61P1/04 , C07C211/27 , A61K31/16
CPC分类号： A61K31/166 , A61K31/137 , A61K31/192 , A61K31/197 , A61K45/06 , C07C211/27 , C07C231/02 , C07C233/78 , C07C235/10 , C07C237/46 , C07D295/13
摘要： Novel polyamine transport inhibitors have been synthesized and demonstrated to block the uptake of native polyamines into human cancer cells. A combination therapy of the transport inhibitor and DFMO (a drug which blocks polyamine biosynthesis) provided synergistic activity against a metastatic human colon cancer cell line. The strategy uses polyamine depletion and polyamine metabolism to generate reactive oxygen species within cells as a novel way to treat cancers. This approach may be implemented for widespread use in the treatment of diseases which rely upon polyamine transport activity for proliferation.
摘要翻译：已经合成了新的多胺转运抑制剂并证明阻止天然多胺进入人类癌细胞的吸收。运输抑制剂和DFMO（阻断多胺生物合成的药物）的组合疗法提供了对转移性人结肠癌细胞系的协同作用。该策略使用多胺消耗和多胺代谢在细胞内产生活性氧作为治疗癌症的新方法。这种方法可以实施用于广泛用于治疗依赖于多胺转运活性以增殖的疾病。

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