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61. 发明授权

US5364613A Polychelants containing macrocyclic chelant moieties 失效
标题翻译：含有大环螯合剂部分的聚合物
公开(公告)号：US5364613A
公开(公告)日：1994-11-15
申请号：US464865
申请日：1990-01-16
申请人： Paul F. Sieving , Alan D. Watson , Steven C. Quay , Scott M. Rocklage
发明人： Paul F. Sieving , Alan D. Watson , Steven C. Quay , Scott M. Rocklage
IPC分类号： A61K39/395 , A61K47/48 , A61K49/00 , A61K49/08 , A61K49/12 , A61K51/00 , A61K51/06 , A61P39/02 , C08G69/48 , A61K37/00 , A61K39/00 , A61K49/04
CPC分类号： A61K49/143 , A61K47/48315 , A61K49/085 , A61K49/12 , A61K49/128 , A61K49/146 , A61K49/16 , A61K51/065 , A61K51/081 , A61K51/088 , C08G69/48
摘要： There are provided polychelants and their metal chelates which are useful in diagnostic imaging and in radiotherapy and which comprise a plurality of macrocyclic chelant moieties, e.g, DOTA residues, conjugated to a polyamine backbone molecule, e.g, polylysine. To produce a site-specific polychelate, one or more of the macrocyclic chelant carrying backbone molecules may be conjugated to a site-directed macromolecule, e.g. a protein.
摘要翻译：提供了可用于诊断成像和放射治疗中的多价螯合剂及其金属螯合物，其包含与多胺主链分子例如聚赖氨酸缀合的多个大环螯合剂部分，例如DOTA残基。为了产生位点特异性聚合物，一种或多种携带骨架分子的大环螯合剂可以与位点定向的大分子结合，例如蛋白质

62. 发明授权

US5223243A Dipyridoxyl phosphate chelating compound intermediates useful as NMRI contrast agents 失效
标题翻译：可用作NMRI造影剂的二吡啶氧磷酸盐螯合化合物中间体
公开(公告)号：US5223243A
公开(公告)日：1993-06-29
申请号：US570115
申请日：1990-08-20
申请人： Scott M. Rocklage , Steven C. Quay
发明人： Scott M. Rocklage , Steven C. Quay
IPC分类号： A61K49/06 , C07F9/58 , C07F13/00 , G01R33/28
CPC分类号： G01R33/5601 , A61K49/06 , C07F13/005 , C07F9/582 , Y10S514/836 , Y10T436/24
摘要： N,N'-bis-(pyridoxal-5-phosphate)-alkylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal-5-phosphate)-1,2-cycloalkylenediamine-N,N'diacetic acids, and N,N'-bis-(pyridoxal-5-phosphate)-1,2-arylenediamine-N,N'diacetic acids, the corresponding monophosphate compounds and monoacetic acid compounds, and their salts and esters form stable, highly soluble chelates with paramagnetic metal ions, and are highly effective NMRI contrast agents. Preferred contrast agents are paramagnetic ion chelates of N,N'-bis-(pyridoxal-5-phosphate)ethylenediamine-N,N'-diacetic acid, N,N'-bis-(pyridoxal-5-phosphate)trans-1,2-cyclohexylenediamine-N,N'-diacetic acid, N,N'-bis-(pyridoxal-5-phosphate)trans-1,2-arylenediamine-N,N'-diacetic acid, and the soluble calcium salts thereof.Novel intermediates for forming these compounds are N,N'-bis(pyridoxal-5-phosphate)alkylenediimines, N,N'-bis(pyridoxal-5-phosphate)alkylenediamines, N,N'-bis(pyridoxal-5-phosphate)-1,2-cycloalkylenediimines, N,N'-bis(pyridoxal-5-phosphate)-1,2-cycloalkylenediamines, N,N'-bis(pyridoxal-5-phosphate)-1,2-arylenediamines, and the corresponding monophosphate compounds.
摘要翻译： N，N'-二 - （吡哆醛-5-磷酸） - 亚烷基二胺-N，N'-二乙酸，N，N'-双 - （吡哆醛-5-磷酸酯）-1,2-环烷二胺-N，N' 二乙酸和N，N'-二 - （吡哆醛-5-磷酸）-1,2-芳基二胺-N，N'-二乙酸，相应的单磷酸酯化合物和单乙酸化合物及其盐和酯形成稳定，高度具有顺磁金属离子的可溶性螯合物，是高效的NMRI造影剂。优选的造影剂是N，N'-双 - （吡哆醛-5-磷酸）乙二胺-N，N'-二乙酸，N，N'-双 - （吡哆醛-5-磷酸）反式-1的顺磁离子螯合物， 2-环己二胺-N，N'-二乙酸，N，N'-双 - （吡哆醛-5-磷酸）反式-1,2-芳基二胺-N，N'-二乙酸及其可溶性钙盐。用于形成这些化合物的新型中间体是N，N'-双（吡哆醛-5-磷酸）亚烷基二亚胺，N，N'-双（吡哆醛-5-磷酸）亚烷基二胺，N，N'-双（吡哆醛-5-磷酸酯） 1,2-环烷基二亚胺，N，N'-双（吡哆醛-5-磷酸）-1,2-环烷基二胺，N，N'-双（吡哆醛-5-磷酸）-1,2-亚芳基二胺，和相应的单磷酸盐化合物。

63. 发明授权

US5130437A N,N'-bis-(pyridoxal)ethylenediamine-N,N'-diacetic acid derivatives 失效
标题翻译： N，N'-二 - （吡哆醛）乙二胺-N，N'-二乙酸衍生物
公开(公告)号：US5130437A
公开(公告)日：1992-07-14
申请号：US578265
申请日：1990-09-06
申请人： Scott M. Rocklage , Steven C. Quay
发明人： Scott M. Rocklage , Steven C. Quay
IPC分类号： A61K49/06 , C07D213/66 , C07F13/00
CPC分类号： C07D213/66 , A61K49/06 , C07F13/005
摘要： Manganese(II) chelates of N,N'-bis-(pyridoxal)alkylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal)-1,2-cycloalkylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal)-1,2-arylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal)alkylenediamine-N-acetic acids, N,N'-bis-(pyridoxal)-1,2-cycloalkylenediamine-N-acetic acids, N,N'-(pyridoxal)-1,2-arylenediamine-N-acetic acids, and their salts are highly stable, superior NMRI contrast agents. They maintain the manganese(II) ion in the +2 valence state. Preferred contrast agents are manganese(II) ion chelates of N,N'-bis-(pyridoxal)ethylenediamine-N,N'-diacetic acid, N,N'-bis-(pyridoxal)trans-1,2-cyclohexylenediamine-N,N'-diacetic acid, and the salts and esters thereof.Novel chelate forming compounds are the N,N'-bis-(pyridoxal)-1,2-cycloalkylenediamine-N,N'-diacetic acids and N,N'-bis-(pyridoxal)-1,2-arylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal)alkylenediamine-N-acetic acids, N,N'-bis(pyridoxal)-1,2-cycloalkylenediamine-N-acetic acids, N,N'-bis-(pyridoxal)-1,2-arylenediamine-N-acetic acids, and their salts and esters.
摘要翻译： N，N'-双（吡哆醛）亚烷基二胺-N，N'-二乙酸，N，N'-二 - （吡哆醛）-1,2-环亚烷基二胺-N，N'-二乙酸的锰（II）螯合物，N，N'-二 - （吡哆醛）-1,2-芳基二胺-N，N'-二乙酸，N，N'-双 - （吡哆醛）亚烷基二胺-N-乙酸，N，N'-双 - （吡哆醛）-1,2-环烷二胺-N-乙酸，N，N' - （吡哆醛）-1,2-芳基二胺-N-乙酸及其盐是高度稳定的优异的NMRI造影剂。它们保持+2价态的锰（II）离子。优选的造影剂是N，N'-双 - （吡哆醛）乙二胺-N，N'-二乙酸，N，N'-双 - （吡哆醛）反-1,2-环己二胺-N ，N'-二乙酸及其盐和酯。新型螯合物形成化合物是N，N'-双 - （吡哆醛）-1,2-环烷二胺-N，N'-二乙酸和N，N'-双 - （吡哆醛）-1,2-芳基二胺-N， N，N'-二 - （吡哆醛）亚烷基二胺-N-乙酸，N，N'-双（吡哆醛）-1,2-环亚烷基二胺-N-乙酸，N，N'-双 - （吡哆醛）-1,2-芳基二胺-N-乙酸及其盐和酯。

64. 发明授权

US4994259A Improvement in the method of NMR imaging employing a manganese II chelates of N,N'-bis[pyridoxal-alkylene (or cycloalkylene) (or arylene)]-N,N'-diacetic acid derivatives 失效
标题翻译：使用N，N'-双[吡哆醛 - 亚烷基（或亚环烷基）（或亚芳基）] -N，N'-二乙酸衍生物的锰II螯合物的NMR成像方法的改进
公开(公告)号：US4994259A
公开(公告)日：1991-02-19
申请号：US380185
申请日：1989-07-14
申请人： Scott M. Rocklage , Steven C. Quay
发明人： Scott M. Rocklage , Steven C. Quay
IPC分类号： A61K49/06 , C07D213/66 , C07F13/00
CPC分类号： C07D213/66 , A61K49/06 , C07F13/005 , Y10T436/145555 , Y10T436/24
摘要： Manganese(II) chelates of N,N'-bis-(pyridoxal)-alkylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal)-1,2-cycloalkylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal)-1,2-arylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal)-alkylenediamine-N-acetic acids, N,N'-bis-(pyridoxal)-1,2-cycloalkylenediamine-N-acetic acids, N,N'-bis-(pyridoxal)-1,2-arylenediamine-N-acetic acids, and their salts are highly stable, superior NMRI contrast agents. They maintain the manganese(II) ion in the +2 valence state. Preferred contrast agents are manganese(II) ion chelates of N,N'-bis-(pyridoxal)ethylenediamine-N,N'-diacetic acid, N,N'-bis-(pyridoxal)trans-1,2-cyclohexylenediamine-N,N'-diacetic acid, and the salts and esters thereof.Novel chelate forming compounds are the N,N'-bis-(pyridoxal)-1,2-cycloalkylenediamine-N,N'-diacetic acids and N,N'-bis-(pyridoxal)1,2-arylene-diamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal)-alkylenediamine-N-acetic acids, N,N'-bis(pyridoxal)-1,2-cycloalkylenediamine-N-acetic acids, N,N'-bis-(pyridoxal)-1,2-arylenediamine-N-acetic acids, and their salts and esters.
摘要翻译： N，N'-双 - （吡哆醛） - 亚烷基二胺-N，N'-二乙酸，N，N'-双 - （吡哆醛）-1,2-环烷二胺-N，N'-二乙酸的锰（II）螯合物酸，N，N'-双 - （吡哆醛）-1,2-芳基二胺-N，N'-二乙酸，N，N'-双 - （吡哆醛） - 亚烷基二胺-N-乙酸，N，双（吡哆醛）-1,2-环亚烷基二胺-N-乙酸N，N'-双 - （吡哆醛）-1,2-芳基二胺-N-乙酸及其盐是高度稳定的，优良的NMRI造影剂。它们保持+2价态的锰（II）离子。优选的造影剂是N，N'-双 - （吡哆醛）乙二胺-N，N'-二乙酸，N，N'-双 - （吡哆醛）反-1,2-环己二胺-N ，N'-二乙酸及其盐和酯。新型螯合形成化合物是N，N'-双 - （吡哆醛）-1,2-环烷二胺-N，N'-二乙酸和N，N'-双（吡哆醛）1,2-亚芳基二胺-N N，N'-二 - （吡哆醛） - 亚烷基二胺-N-乙酸，N，N'-双（吡哆醛）-1,2-环烷二胺-N-乙酸，N，N' 双 - （吡哆醛）-1,2-芳基二胺-N-乙酸及其盐和酯。

65. 发明授权

US4935518A Manganese(II), chelate contrast agents derived from N,N'-bis-(pyridoxal ethylene diamine-N,N')-diacetic acid and derivatives thereof 失效
标题翻译：锰（II），衍生自N，N'-双 - （吡哆醛乙二胺-N，N'） - 二乙酸及其衍生物的螯合造影剂
公开(公告)号：US4935518A
公开(公告)日：1990-06-19
申请号：US047584
申请日：1987-05-08
申请人： Scott M. Rocklage , Steven C. Quay
发明人： Scott M. Rocklage , Steven C. Quay
IPC分类号： A61K49/00 , A61K49/06 , C07D213/66 , C07F13/00
CPC分类号： C07D213/66 , A61K49/06 , C07F13/005 , Y10T436/24
摘要： Managanese(II) chelates of N,N'-bis-(pyridoxal)-alkylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal)-1,2-cycloalkylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal)-1,2-arylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal)-alkylenediamine-N-acetic acids, N,N'-bis-(pyridoxal)-1,2-cycloalkylenediamine-N-acetic acids, N,N'-bis-(pyridoxal)-1,2-arylenediamine-N-acetic acids, and their salts are highly stable, superior NMRI contrast agents. They maintain the manganese(II) ion in the +2 valence state. Preferred contrast agents are manganese(II) ion chelates of N,N'-bis-(pyridoxal)ethylenediamine- N,N'-diacetic acid, N,N'-bis-(pyridoxal)trans-1,2-cyclohexylenediamine-N,N'-diacetic acid, and the salts and esters thereof.Novel chelate forming compounds are the N,N'-bis-(pyridoxal)-1,2-cycloalkylenediamine-N,N'-diacetic acids and N,N'-bis-(pyridoxal)-1,2,-arylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal)-alkylenediamine-N-acetic acids, N,N'-bis(pyridoxal)-1,2-cycloalkylenediamine-N-acetic acids, N,N'-bis-(pyridoxal)-1,2-arylenediamine-N-acetic acids, and their salts and esters.

66. 发明授权

US4863716A Determination of fallopian tubal patency by magnetic resonance imaging 失效
标题翻译：通过磁共振成像确定输卵管输卵管通畅
公开(公告)号：US4863716A
公开(公告)日：1989-09-05
申请号：US58180
申请日：1987-06-04
申请人： Steven C. Quay , Scott M. Rocklage
发明人： Steven C. Quay , Scott M. Rocklage
IPC分类号： A61K49/06 , C07F9/58 , C07F13/00 , G01R33/28
CPC分类号： G01R33/5601 , A61K49/06 , C07F13/005 , C07F9/582 , Y10S436/806 , Y10T436/24
摘要： This invention is a method for obtaining improved NMR images of the uterine cavity and fallopian tubes comprising imjecting a physiologically acceptable solution of a chelate of a parmagnetic material into the uterus under sufficient pressure to cause the solution to pass through the fallopian tubes and obtaining an enhanced NMR image of the tissue surrounding the fallopian tubes. The chelates and the injection solutions thereof do not include carbohydrate groups or other compounds which might support growth of Staphylococcus aureus or other pathological miroorganisms in the peritoneal cavity.Kits including contrast medium and non-metallic uterine balloon catheters suitable for use with NMRI procedures are also included within the scope of this invention.
摘要翻译：本发明是一种用于获得子宫腔和输卵管的改进的NMR图像的方法，包括在足够的压力下将对数磁性材料的螯合物的生理上可接受的溶液注入到子宫中，以使溶液通过输卵管并获得增强的围绕输卵管的组织的NMR图像。螯合物及其注射溶液不包括碳水化合物基团或可能支持金黄色葡萄球菌生长或其它病理性微生物在腹膜腔中的其他化合物。适用于NMRI方法的造影剂和非金属子宫气囊导管的试剂盒也包括在本发明的范围内。

67. 发明授权

US4859451A Paramagnetic contrast agents for MR imaging 失效
标题翻译：顺磁造影剂用于MR成像
公开(公告)号：US4859451A
公开(公告)日：1989-08-22
申请号：US855223
申请日：1986-04-24
申请人： Steven C. Quay , Dilip M. Worah
发明人： Steven C. Quay , Dilip M. Worah
IPC分类号： A61K49/06 , G01N33/00 , G01R33/28
CPC分类号： G01R33/5601 , A61K49/06 , Y10S436/806 , Y10T436/24
摘要： In the NMR imaging of a subject comprising administering to such subject a composition containing an image-modifying effective amount of an image enhancer, permitting the enhancer to move through the subject, and after a time interval taking an NMR image of the subject, the improvement which comprises employing as said enhancer a complex of a paramagnetic polyvalent metal and a partial amide and/or ester of diethylenetriaminepentaacetic acid. The complexes are new.
摘要翻译：在受试者的NMR成像中，包括向所述受试者施用含有图像改善有效量的图像增强子的组合物，允许增强剂移动通过受试者，并且在经受时间间隔取对象的NMR图像之后，改善其包括使用顺磁性多价金属和二亚乙基三胺五乙酸的部分酰胺和/或酯的络合物作为所述增强剂。复合体是新的。

68. 发明授权

US09074205B2 Nicked or gapped nucleic acid molecules and uses thereof 有权
标题翻译：有缺陷或间隙的核酸分子及其用途
公开(公告)号：US09074205B2
公开(公告)日：2015-07-07
申请号：US12445868
申请日：2007-10-18
申请人： Steven C. Quay , James Mcswiggen , Narendra K. Vaish , Mohammad Ahmadian
发明人： Steven C. Quay , James Mcswiggen , Narendra K. Vaish , Mohammad Ahmadian
IPC分类号： C07H21/02 , C07H21/04 , A61K48/00 , C12N15/11 , A61K38/00
CPC分类号： A61K31/713 , A61K38/00 , A61K47/645 , A61K47/66 , C12N15/111 , C12N15/113 , C12N2310/14 , C12N2310/15 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/3231 , C12N2310/3513 , C12N2310/533 , C12N2320/30 , C12N2320/51 , C12N2330/30 , C12N2310/3521
摘要： The present disclosure provides meroduplex (nicked or gapped) ribonucleic acid molecules (mdRNA) that decreases or silences target gene expression. An mdRNA of this disclosure comprises at least three strands that combine to form at least two non-overlapping double-stranded regions separated by a nick or gap wherein one strand is complementary to a target gene RNA. In addition, the meroduplex may have one or more modifications or substitutions, such as nucleotide base, sugar, terminal cap structure, internucleotide linkage, or any combination of such modifications. Also provided are methods of decreasing expression of a target gene in a cell or in a subject to treat a disease related to altered expression of a target gene.
摘要翻译：本公开提供降低或沉默靶基因表达的meroduplex（切口或间隙）核糖核酸分子（mdRNA）。本公开的mdRNA包含至少三条链，其组合形成由切口或间隙分开的至少两个非重叠的双链区域，其中一条链与靶基因RNA互补。此外，meroduplex可以具有一个或多个修饰或取代，例如核苷酸碱基，糖，末端帽结构，核苷酸间连键或这些修饰的任何组合。还提供减少细胞或受试者中靶基因表达以治疗与靶基因表达改变相关的疾病的方法。

69. 发明申请

US20130149378A1 Second Generation Fatty Acid Compositions, Formulations, and Methods of Use and Synthesis Thereof 审中-公开
标题翻译：第二代脂肪酸组合物，制剂及其使用和合成方法
公开(公告)号：US20130149378A1
公开(公告)日：2013-06-13
申请号：US13761243
申请日：2013-02-07
申请人： Steven C. Quay
发明人： Steven C. Quay
IPC分类号： A61K31/164 , A61K31/353
CPC分类号： A61K31/202 , A23L33/12 , A61K9/0053 , A61K9/145 , A61K9/146 , A61K9/4858 , A61K9/4866 , A61K31/16 , A61K31/164 , A61K31/353 , A61K31/355
摘要： An orally administered fatty acid composition for the treatment of cardiovascular diseases, and a method of treating same, are provided. The compound includes 5Z,8Z,11Z,14Z,17Z-eicosapentaenoic ethanolamide (EPA ethanolamide), 4Z,7Z,10Z,13Z,16Z,19Z-docosahexaenoic ethanolamide (DHA ethanolamide), and at least one tocotrienol. The EPA ethanolamide and the DHA ethanolamide are preferably each substantially in a range of 100-900 mg per dosage form. The at least one tocotrienol is substantially in a range of 10-500 mg per dosage form. The at least one tocotrienol includes at least one of α-tocotrienol, β-tocotrienol, γ-tocotrienol, or δ-tocotrienol and is preferably substantially tocopherol-free. The composition may take the form of a medical food or a pharmaceutical preparation. A preferred formulation of the composition includes approximately 525 mg EPA ethanolamide, approximately 315 mg DHA ethanolamide, and approximately 50 mg δ-tocotrienol. The EPA and DHA ethanolamides may be synthesized from fatty acid triglycerides.
摘要翻译：提供了用于治疗心血管疾病的口服给药脂肪酸组合物及其治疗方法。该化合物包括5Z，8Z，11Z，14Z，17Z-二十碳五烯酸乙醇酰胺（EPA乙醇酰胺），4Z，7Z，10Z，13Z，16Z，19Z-二十二碳六烯酸乙醇酰胺（DHA乙醇酰胺）和至少一种生育三烯酚。 EPA乙醇酰胺和DHA乙醇酰胺优选地每个剂型基本上在100-900mg的范围内。至少一种生育三烯酚基本上在每种剂型10-500mg的范围内。至少一种生育三烯酚包括α-生育三烯酚，β-生育三烯酚，γ-生育三烯酚或δ-生育三烯酚中的至少一种，并且优选基本上不含生育酚。组合物可以采取医疗食品或药物制剂的形式。组合物的优选制剂包括约525mg EPA乙醇酰胺，约315mg DHA乙醇酰胺和约50mgδ-生育三烯酚。 EPA和DHA乙醇酰胺可以由脂肪酸甘油三酯合成。

70. 发明授权

US07939505B2 Amino acid lipids and uses thereof 有权
公开(公告)号：US07939505B2
公开(公告)日：2011-05-10
申请号：US12114284
申请日：2008-05-02
申请人： Steven C. Quay , Michael Houston, Jr. , Pierrot Harvie , Roger C. Adami , Renata Fam , Mary Gallagher Prieve , Kathy Lynn Fosnaugh , Shaguna Seth
发明人： Steven C. Quay , Michael Houston, Jr. , Pierrot Harvie , Roger C. Adami , Renata Fam , Mary Gallagher Prieve , Kathy Lynn Fosnaugh , Shaguna Seth
IPC分类号： A61K47/14 , A61K47/18 , A61K48/00 , C07C279/14
CPC分类号： A61K47/183 , A61K9/127 , A61K9/1271 , A61K9/1272 , A61K31/7088 , A61K47/18 , A61K47/22 , A61K47/28 , A61K47/44 , A61K48/0025 , A61K48/0033 , C07C235/02 , C07C279/12 , C07C279/14 , C07D213/40 , C07D213/56 , C07D233/26 , C07D233/64 , C12N15/111 , C12N15/113 , C12N15/1131 , C12N15/1138 , C12N15/88 , C12N2310/14 , C12N2320/32 , Y10S514/943
摘要： This disclosure provides a range of amino acid lipid compounds and compositions useful for drug delivery, therapeutics, and the diagnosis and treatment of diseases and conditions. The amino acid lipid compounds and compositions can be used for delivery of various agents such as nucleic acid therapeutics to cells, tissues, organs, and subjects.

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