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61. 发明授权

US6017910A PCP receptor ligands and the use thereof 失效
标题翻译： PCP受体配体及其用途
公开(公告)号：US6017910A
公开(公告)日：2000-01-25
申请号：US451726
申请日：1995-05-26
申请人： Eckard Weber , John F. W. Keana , Peter Barmettler
发明人： Eckard Weber , John F. W. Keana , Peter Barmettler
IPC分类号： A61K31/439 , A61K31/55 , C07D471/08 , C07D223/00
CPC分类号： C07D471/08 , A61K31/439 , A61K31/55
摘要： The invention relates to 5-(iminomethano)-10,11-dihydro-5H-dibenzo[a,d]cycloheptene and derivatives thereof. The invention also relates to the use of such compounds for the treatment or prevention of neuronal loss in ischemia, hypoxia, brain or spinal chord trauma, as well as for the treatment of Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome.
摘要翻译：本发明涉及5-（亚氨基偶氮）-10,11-二氢-5H-二苯并[a，d]环庚烯及其衍生物。本发明还涉及这些化合物用于治疗或预防缺血，缺氧，脑或脊髓创伤中的神经元丧失以及治疗阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿病和唐氏综合征的用途。

62. 发明授权

US5620979A Glycine receptor antagonists and the use thereof 失效
标题翻译：甘氨酸受体拮抗剂及其用途
公开(公告)号：US5620979A
公开(公告)日：1997-04-15
申请号：US405708
申请日：1995-03-17
申请人： Eckard Weber , John F. W. Keana
发明人： Eckard Weber , John F. W. Keana
IPC分类号： C07D241/44 , A61K20060101 , A61K31/495 , A61K31/498 , A61K45/00 , A61K51/04 , A61P9/00 , A61P9/10 , A61P25/00 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/28 , C07D241/38 , C07D241/52 , C07D241/54 , C07D487/04 , C07D491/04
CPC分类号： C07D491/04 , A61K31/495 , A61K51/0459 , C07D241/38 , C07D241/44 , C07D241/52 , C07D241/54 , C07D487/04
摘要： Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia and treating psychosis are disclosed by administering to an animal in need of such treatment a compound having high affinity for the glycine binding site, lacking PCP side effects and which crosses the blood brain barrier of the animal.Also disclosed are novel 1,4-dihydroquinoxaline-2,3-diones, and pharmaceutical compositions thereof. Also disclosed are highly soluble ammonium salts of 1,4-dihydroquinoxaline-2,3-diones.
摘要翻译：治疗或预防与中风，缺血，CNS创伤，低血糖和手术相关的神经元损失以及治疗神经变性疾病包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿病和唐氏综合征的治疗或预防方法，治疗或预防多动症的不良后果通过向需要这种治疗的动物施用兴奋性氨基酸以及治疗焦虑症，慢性疼痛，惊厥，诱导麻醉和治疗精神病，通过向甘氨酸结合位点具有高亲和力的化合物，缺乏PCP副作用和哪些穿过动物的血脑屏障。还公开了新的1,4-二氢喹喔啉-2,3-二酮及其药物组合物。还公开了1,4-二氢喹喔啉-2,3-二酮的高度可溶性铵盐。

63. 发明授权

US5574070A Substituted guanidines having high binding to the sigma receptor and the use thereof 失效
标题翻译：与σ受体结合度高的取代胍类及其用途
公开(公告)号：US5574070A
公开(公告)日：1996-11-12
申请号：US952849
申请日：1993-01-22
申请人： John F. W. Keana , Eckard Weber
发明人： John F. W. Keana , Eckard Weber
IPC分类号： A61K31/155 , A61K31/00 , A61K31/37 , A61K31/415 , A61K31/55 , A61P9/12 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , C07B59/00 , C07C279/04 , C07C279/16 , C07C279/18 , C07C331/12 , C07D233/46 , C07D233/50 , C07D243/04 , C07D311/08 , C07D311/14 , C07D311/18 , G01N33/53
CPC分类号： C07D233/50 , C07B59/001 , C07C279/04 , C07C279/16 , C07C279/18 , C07C331/12 , C07D311/14 , C07D311/18 , C07C2101/14 , C07C2102/08 , C07C2102/28 , C07C2103/64 , C07C2103/74
摘要： The invention relates to a method for the treatment or prophylaxis of psychosis, depression, hypertension, or anxiety in an animal by administering an effective amount of an N,N'-disubstituted guanidine or 2-iminoimadazolidine having an affinity for the sigma receptor. The invention also relates to the novel guanidines of the invention as well as pharmaceutical compositions thereof.
摘要翻译： PCT No.PCT / US91 / 03594 371日期：1993年1月22日 102（e）日期1993年1月22日PCT 1991年5月22日PCT公布。 WO91 / 18868 PCT出版物日期1991年12月12日本发明涉及一种通过施用有效量的N，N'-二取代胍或具有亲和力的2-亚氨基咪唑烷来治疗或预防动物的精神病，抑郁症，高血压或焦虑的方法西格玛受体。本发明还涉及本发明的新颖的胍及其药物组合物。

64. 发明授权

US5567411A Dendritic amplifier molecules having multiple terminal active groups stemming from a benzyl core group 失效
标题翻译：树枝状放大器分子具有来自苄基核心基团的多个末端活性基团
公开(公告)号：US5567411A
公开(公告)日：1996-10-22
申请号：US316787
申请日：1994-09-29
申请人： John F. W. Keana , Vladimir Martin , William H. Ralston
发明人： John F. W. Keana , Vladimir Martin , William H. Ralston
IPC分类号： A61K49/18 , A61K49/20 , C07C291/04 , C07F11/00 , A61K49/00 , A61K51/00 , C07C69/80 , C07D207/38 , C07D209/48 , C12N9/96
CPC分类号： A61K49/20 , A61K49/1812 , C07C291/04 , Y10S436/803 , Y10S436/806 , Y10T436/24
摘要： Dendritic derivatives of 3,5-bis(aminomethyl)benzene and aminomethyl benzene core groups are disclosed. In each derivative, termed an "amplifier" because the dendritic structure on each molecule terminates with multiple termini to each of which an "active group" can be attached, the desired effect of the active group per mole is amplified compared to conventional compounds having only one active group per molecule. Amplifier molecules can include a targeting group permitting the molecules to preferentially attach to a particular anatomical or physiological situs. Active groups are any of various pharmacologically or therapeutically active moieties, including moieties useful for magnetic-resonance contrast enhancement. The dendritic structures comprise linkers and branch groups covalently bonded to each other in any of various structural combinations. The amplifiers can be prepared as a solution or mixture with a physiologically compatible carrier for administration to a warm-blooded animal subject. Also disclosed are methods for using the compounds in diagnosis and therapy, such as obtaining a magnetic resonance image of a subject.
摘要翻译：公开了3,5-双（氨基甲基）苯和氨基甲基苯核心的树枝状衍生物。在每个衍生物中，称为“放大器”，因为每个分子上的树突状结构终止于可以连接“活性基团”的每个末端的多个末端，与仅具有仅活性基团的常规化合物相比，活性基团每摩尔的期望效应被扩增每个分子一个活性基团。放大器分子可以包括允许分子优先附着到特定解剖或生理部位的靶向基团。活性基团是各种药理学或治疗活性部分中的任何一种，包括可用于磁共振对比度增强的部分。树枝状结构包括以各种结构组合中的任何一种彼此共价键合的接头和分支基团。放大器可以制备成与生理相容的载体的溶液或混合物，用于给温血动物受试者施用。还公开了在诊断和治疗中使用化合物的方法，例如获得受试者的磁共振图像。

65. 发明授权

US5465151A Sensors employing interference of electromagnetic waves passing through waveguides having functionalized surfaces 失效
标题翻译：采用通过具有功能化表面的波导的电磁波干扰的传感器
公开(公告)号：US5465151A
公开(公告)日：1995-11-07
申请号：US14425
申请日：1993-02-05
申请人： Martin N. Wybourne , John F. W. Keana , Sui X. Cai , Mingdi Yan , Jong Wu
发明人： Martin N. Wybourne , John F. W. Keana , Sui X. Cai , Mingdi Yan , Jong Wu
IPC分类号： C08J7/12 , B01J19/08 , C01B31/04 , C08F8/34 , C23C16/02 , G01N21/27 , G01N21/45 , G01N21/64 , G01N21/75 , G01N21/77 , G01N33/543 , G01N33/566 , G03F7/20 , H01L21/368 , G01B9/02
CPC分类号： G01N21/7703 , C08F8/32 , G01N33/54373 , G03F7/2041 , G01N2021/7779 , G01N2201/0873
摘要： Chemical and biosensors are disclosed. An optical waveguide is used to conduct electromagnetic radiation by total internal reflection in parallel through a reference waveguide portion and at least one analyte waveguide portion. The electromagnetic radiation is then converged into an exit beam. The external surface of at least the analyte portion is covalently modified, or functionalized, relative to the reference portion. Resulting interaction of the functionalized surface with molecules comprising an analyte causes a phase change in the electromagnetic radiation passing through the analyte portion relative to the reference portion sufficient to generate a corresponding and measurable interference pattern in the exit beam. A waveguide surface is functionalized by exposure to a reagent, having molecules each comprising a nitrenogenic group and a functionalizing group, in the presence of energized charged particles such as electrons and ions, photons, or heat, which transform the nitrenogenic reagent to a nitrene intermediate. The resulting reaction causes the functionalizing groups to covalently bond to the surface. The functionalizing groups can then participate in downstream chemistry whereby any of a large variety of functional groups, including biological molecules, can be covalently bonded to the surface. Thus, the waveguide surface can be made selectively responsive to a wide variety of analytes, including cells and other biological structures.
摘要翻译：公开了化学和生物传感器。光波导用于通过参考波导部分和至少一个分析物波导部分并行地通过全内反射来传导电磁辐射。电磁辐射然后会聚到出射光束中。至少分析物部分的外表面相对于参考部分共价修饰或官能化。功能化表面与包含分析物的分子的相互作用导致相对于参考部分通过分析物部分的电磁辐射的相变足以在出射光束中产生相应和可测量的干涉图案。波导表面通过暴露于具有各自包含硝基衍生基团和官能化基团的分子的试剂而被功能化，所述分子在有电的带电粒子例如电子和离子，光子或热的情况下，其将硝化反应试剂转变为硝酸中间体。所得到的反应使官能团共价键合到表面。官能团然后可以参与下游化学，因此包括生物分子在内的各种各样的官能团中的任何一个可以共价键合到表面上。因此，波导表面可以选择性地响应于各种各样的分析物，包括细胞和其他生物结构。

66. 发明授权

US5190976A N,N'-disubstituted guanidines and their use as excitatory amino acid antagonists 失效
标题翻译： N，N'-二取代胍及其作为兴奋性氨基酸拮抗剂的用途
公开(公告)号：US5190976A
公开(公告)日：1993-03-02
申请号：US844498
申请日：1992-03-02
申请人： Eckard Weber , John F. W. Keana
发明人： Eckard Weber , John F. W. Keana
IPC分类号： C07D215/40 , A01N37/52 , A61K31/155 , A61K31/365 , A61K31/37 , A61K31/47 , A61P25/00 , A61P25/28 , C07C279/18 , C07D311/18
CPC分类号： C07C279/18 , A61K31/155 , A61K31/365 , A61K31/47
摘要： N,N'-disubstituted guanidines exhibiting a high binding affinity to phencyclidine (PCP) receptors are disclosed. These N,N'-disubstituted guanidine derivatives act as non-competitive inhibitors or glutamate-induced responses generated via the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert a neuroprotective property and are useful in the therapeutic treatment of neuronal loss in hypoxia, brain or spinal cord ischemia, brain or spinal cord trauma, as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.
摘要翻译：公开了对苯环利定（PCP）受体表现出高结合亲和力的N，N'-二取代的胍。这些N，N'-二取代的胍衍生物作为非竞争性抑制剂或通过NMDA受体产生的谷氨酸盐诱导的反应，作为NMDA受体 - 离子通道复合物的离子通道的阻断剂。因此，这些化合物发挥神经保护性质，并且可用于治疗缺氧，脑或脊髓缺血，脑或脊髓创伤中的神经元丧失，以及用于治疗癫痫，阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿氏病，唐氏综合征，柯萨科夫病和其他神经退行性疾病。

67. 发明授权

US5135737A Amplifier molecules for enhancement of diagnosis and therapy 失效
标题翻译：放大器分子用于增强诊断和治疗
公开(公告)号：US5135737A
公开(公告)日：1992-08-04
申请号：US403595
申请日：1989-09-05
申请人： John F. W. Keana
发明人： John F. W. Keana
IPC分类号： A61K49/18 , A61K49/20 , C07C291/04
CPC分类号： C07C291/04 , A61K49/1812 , A61K49/20 , Y10T436/24
摘要： Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines. Via such chemistry, the amplifiers are attachable to monoclonal antibodies for concentration of pharmacologically active groups at a desired site in the body.
摘要翻译：公开了放大器分子：具有分支结构的各种有机化合物，其末端具有可以化学连接药理活性基团的胺基团。合成了许多MRI对比增强剂，每种都包含多个活性基团，如稳定的氮氧化物和三价金属阳离子的络合物。使用具有不同支化结构的许多放大器成功地进行了这种合成，表明了合成具有各种药理学活性基团的放大器的相关化学物质的一般用途。还合成放大器，其具有以化学反应性基团如异硫氰酸酯终止的接头，其使放大器具有双功能性：可附着于聚合物，生物大分子或具有多个反应性位点的其它生物相容性实体，例如末端胺。通过这样的化学，放大器可附着于单体抗体，用于在体内所需位点浓集药理活性基团。

68. 发明授权

US4863717A Methods for circumventing the problem of free radial reduction associated with the use of stable nitroxide free radicals as contrast agents for magnetic reasonance imaging 失效
标题翻译：避免与使用稳定的氮氧自由基相关的自由径向减少问题的方法作为磁性推理成像的造影剂
公开(公告)号：US4863717A
公开(公告)日：1989-09-05
申请号：US928943
申请日：1986-11-10
申请人： John F. W. Keana
发明人： John F. W. Keana
IPC分类号： A61K49/18 , A61K49/20 , C07C291/04
CPC分类号： C07C291/04 , A61K49/1812 , A61K49/20 , Y10S436/803 , Y10S436/806 , Y10T436/24
摘要： Nitroxide contrast agents for MRI have a long useful life and can be administered in low concentration doses. Such agents include nitroxide-doped liposomes that encapsulate an oxidant and large molecules having surfaces covered with persistent nitroxide free radicals.
摘要翻译：用于MRI的硝酸氧化物造影剂具有较长的使用寿命并且可以以低浓度剂量施用。这些试剂包括氮氧化物掺杂的脂质体，其包裹氧化剂和具有被持续的氮氧自由基覆盖的表面的大分子。

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