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1. 发明授权

US5545397A Contrast agents and compositions for radiological imaging, and radiological imaging method utilizing same 失效
标题翻译：用于放射成像的对比剂和组合物，以及利用其的放射性成像方法
公开(公告)号：US5545397A
公开(公告)日：1996-08-13
申请号：US341767
申请日：1994-11-18
申请人： Bernard F. Spielvogel , Dominique Meyer
发明人： Bernard F. Spielvogel , Dominique Meyer
IPC分类号： A61K49/04 , C01B35/06 , C07C215/10 , C07F5/02 , C07F9/06 , C07F9/535 , C07F9/6581 , C08G79/00 , A61K33/18
CPC分类号： C07F9/067 , A61K49/0433 , C01B35/06 , C07C215/10 , C07F5/022 , C07F9/5357 , C07F9/65812 , C08G79/00
摘要： Contrast agent for X-ray imaging, consisting of a halogenated, especially iodinated or brominated, derivative of boron, having characteristics necessary for its use in X-ray imaging. The contrast agent may be used for imaging a corporeal situs by radiological techniques, comprising delivery to the corporeal situs of an imagingly effectively amount of a physiologically acceptable composition comprising the boron reagent. A variety of illustrative boron reagents is described, including vectorised boron derivatives, e.g., boron derivatives encapsulated within liposomes, fixed on or bonded to macromolecules or polymers, etc. The contrast agents, formulations, and method of the present invention may be employed for a wide variety of radiological imaging applications, e.g., excretory urography, angiocardiography, aortography, etc.
摘要翻译：用于X射线成像的对比剂，由卤化的，特别是碘化或溴化的硼衍生物组成，具有其用于X射线成像所必需的特性。造影剂可以用于通过放射学技术对体质部位进行成像，包括将成像有效量的包含硼试剂的生理上可接受的组合物输送到体内部位。描述了各种说明性的硼试剂，包括载体化的硼衍生物，例如包封在脂质体内的硼衍生物，固定在大分子或聚合物上或结合到大分子或聚合物上等。本发明的造影剂，制剂和方法可用于各种各样的放射成像应用，例如排泄泌尿道造影，血管造影，动脉造影等。

2. 发明授权

US06525224B1 Fused polyhedron borane dianion 失效
标题翻译：熔融多面体硼烷二价阴离子
公开(公告)号：US06525224B1
公开(公告)日：2003-02-25
申请号：US09589583
申请日：2000-06-07
申请人： Bernard F. Spielvogel , Narayan Hosmane
发明人： Bernard F. Spielvogel , Narayan Hosmane
IPC分类号： C07F502
CPC分类号： A61K41/0095 , C07F5/027
摘要： A polyhedral borane cluster consists essentially of a fused polyhedron including an open decaborane cage fused to a closed dodecaborane cluster wherein borane atoms are not an integral part of the cluster vertices. The polyhedral borane cluster can be contained within a biomolecule for use as a neutron capture reagent. A method of synthesizing the polyhedral borane cluster includes the step of fusing an open decaborane cage to a closed dodecaborane cluster.
摘要翻译：多面体硼烷簇基本上由稠合的多面体组成，其包括与封闭的十二硼烷簇融合的开放的十硼烷笼，其中硼烷原子不是簇顶点的组成部分。多面体甲烷簇可以包含在用作中子捕获试剂的生物分子内。合成多面体硼烷簇的方法包括将开放的十硼烷笼固定在封闭的十二硼烷簇上的步骤。

3. 发明授权

US5434143A Pharmaceutical compositions comprising phosphite-borane compounds 失效
标题翻译：包含亚磷酸酯 - 硼烷化合物的药物组合物
公开(公告)号：US5434143A
公开(公告)日：1995-07-18
申请号：US326008
申请日：1994-10-19
申请人： Bernard F. Spielvogel , Anup Sood
发明人： Bernard F. Spielvogel , Anup Sood
IPC分类号： C07F9/141 , C07H19/10 , C07H19/20 , C07H23/00 , C12N9/99 , C12P19/34 , A61K31/69
CPC分类号： C07H23/00 , C07F9/141 , C07F9/1415 , C07H19/10 , C07H19/20 , C12N9/99 , C12P19/34
摘要： The phosphite-borane compounds of the present invention correspond to the formula ##STR1## where R.sub.1 is independently selected from H, C.sub.1 -C.sub.20 alkyl, alkylaryl, aryl, trialkylsilyl, with the proviso that both R.sub.1 groups cannot simultaneously be H.sub.1, andR.sub.2 is selected from H, a monovalent cation such as Li.sup.+, Na.sup.+, K.sup.+, NH.sub.4.sup.+, N(R.sub.3.sup.+).sub.4, where R.sub.3 is independently selected from H, C.sub.1 -C.sub.20 alkyl.The phosphite-borane compounds of the present invention are bioactive in character, variously exhibiting anti-tumor, anti-inflammatory, and hypolipidemic activity. Also disclosed are various synthetic methods for making such phosphite-borane compounds, and for formulating same in unit dosage forms as well as other pharmaceutically and pharmacologically acceptable formulations.
摘要翻译：本发明的亚磷酸酯 - 硼烷化合物对应于其中R 1独立地选自H，C 1 -C 20烷基，烷基芳基，芳基，三烷基甲硅烷基的式“IMAGE”，条件是两个R 1基团不能同时为H 1，并且R 2为选自H，一价阳离子如Li +，Na +，K +，NH4 +，N（R3 +）4，其中R3独立地选自H，C1-C20烷基。本发明的亚磷酸酯 - 硼烷化合物具有生物活性，各种表现出抗肿瘤，抗炎和降血脂活性。还公开了制备这种亚磷酸酯 - 硼烷化合物的各种合成方法，以及用于在单位剂型以及其它药学和药理学上可接受的制剂中配制相同的方法。

4. 发明授权

US5143907A Phosphite-borane compounds, and method of making and using the same 失效
标题翻译：亚磷酸酯 - 硼烷化合物及其制备和使用方法
公开(公告)号：US5143907A
公开(公告)日：1992-09-01
申请号：US701682
申请日：1991-05-10
申请人： Bernard F. Spielvogel , Anup Sood , Iris H. Hall
发明人： Bernard F. Spielvogel , Anup Sood , Iris H. Hall
IPC分类号： A61K31/69 , A61K31/70 , A61K31/7135 , A61P3/06 , A61P29/00 , A61P35/00 , C07F9/06 , C07F9/141 , C07F19/00 , C07H23/00
CPC分类号： C07H23/00 , C07F9/141 , C07F9/1415
摘要： Phosphite-borane compounds of the formula ##STR1## wherein: each R.sub.1 is independently selected from: H; C.sub.1 -C.sub.10 alkyl; alkylaryl; aralkyl; aryl; monovalent metal ions; nucleosides; and quaternary ammonium ions, (R.sub.4).sub.4 N.sup.+, in which the substituents R.sub.4 of the ammonium nitrogen atom are H or C.sub.1 -C.sub.10 alkyl;R.sub.2 is H or C.sub.1 -C.sub.10 alkyl; andR.sub.3 is CNCH.sub.2 CH.sub.3.sup.+ BF.sub.4.sup.-, COOH, carboxyl salts, COOR.sub.5, or CONHR.sub.5, wherein R.sub.5 is C.sub.1 -C.sub.10 alkyl, alkylaryl, aralkyl, or aryl;with the proviso that if at least one of the R.sub.1 substituents is H, nucleoside, monovalent metal ion, or quaternary ammonium ion, then R.sub.3 may also be CN. The phosphorous-boron adducts of the invention are bioactive in character, variously exhibiting anti-tumor, anti-inflammatory, and hypolipidemic activity. Also disclosed are various synthetic methods for making such phosphorous-boron compounds, and for formulating same in unit dosage forms as well as other pharmaceutically and pharmacologically acceptable formulations.
摘要翻译：下式的亚磷酸酯 - 硼烷化合物其中：每个R 1独立地选自：H; C1-C10烷基; 烷基芳基芳烷基芳基; 一价金属离子; 核苷; 和季铵离子（R4）4N +，其中铵氮原子的取代基R4为H或C1-C10烷基; R2是H或C1-C10烷基; R3是CNCH2CH3 + BF4-，COOH，羧基盐，COOR5或CONHR5，其中R5是C1-C10烷基，烷基芳基，芳烷基或芳基; 条件是如果R 1取代基中的至少一个是H，核苷，一价金属离子或季铵离子，则R3也可以是CN。本发明的磷 - 硼加合物具有生物活性，各种表现出抗肿瘤，抗炎和降血脂活性。还公开了用于制备这种磷 - 硼化合物的各种合成方法，以及用于在单位剂型中以及其它药学和药理学上可接受的制剂的配制。

5. 发明授权

US4977268A Boron dipeptide compounds 失效
标题翻译：硼二肽化合物
公开(公告)号：US4977268A
公开(公告)日：1990-12-11
申请号：US179555
申请日：1988-04-08
申请人： Andrew T. McPhail , Bernard F. Spielvogel , Iris H. Hall
发明人： Andrew T. McPhail , Bernard F. Spielvogel , Iris H. Hall
IPC分类号： C07F5/02
CPC分类号： C07F5/027
摘要： Novel boron dipeptide analogs and their corresponding amide derivatives which exhibit significant antihyperlipidemic and antineoplastic activities. Methods for preparing the boron containing compounds are disclosed as well as methods for utilizing the compounds to induce antihyperlipidemic and antineoplastic activity.

6. 发明授权

US4709083A Method of making boron analogues 失效
标题翻译：制备硼类似物的方法
公开(公告)号：US4709083A
公开(公告)日：1987-11-24
申请号：US864612
申请日：1986-05-19
申请人： Bernard F. Spielvogel
发明人： Bernard F. Spielvogel
IPC分类号： C07F5/00 , C07C69/76
CPC分类号： C07F5/006
摘要： A method of synthesizing boron analogues of choline and choline related mrials is disclosed. The method comprises reacting N,N dimethylethanolamine with hydrogen chloride or an acid chloride to form an ester hydrochloride. The resulting aminoalcohol hydrochloride or ester hydrochloride is further reacted with tetraethyl NBH.sub.4.Also disclosed are pharamaceutically interesting compounds of acetylcholine.
摘要翻译：公开了合成胆碱和胆碱相关材料的硼类似物的方法。该方法包括使N，N-二甲基乙醇胺与氯化氢或酰氯反应，形成酯盐酸盐。所得氨基醇盐酸盐或酯盐酸盐与NBH4四乙酯进一步反应。还公开了药用有趣的乙酰胆碱化合物。

7. 发明授权

US5280119A Heterocyclic amine-boranes, and method of inhibiting DNA topoisomerase activity and/or combatting inflammation, hyperlipidemia, and/or neoplasia using amine-borane compounds 失效
标题翻译：杂环胺 - 硼烷和使用胺 - 硼烷化合物抑制DNA拓扑异构酶活性和/或抵抗炎症，高脂血症和/或瘤形成的方法
公开(公告)号：US5280119A
公开(公告)日：1994-01-18
申请号：US786279
申请日：1991-11-01
申请人： Bernard F. Spielvogel , Anup Sood , Iris H. Hall
发明人： Bernard F. Spielvogel , Anup Sood , Iris H. Hall
IPC分类号： C07F5/02 , A61K33/22 , A61K43/00
CPC分类号： C07F5/022 , C07F5/027
摘要： Heterocyclic amine-borane compounds of the formula: ##STR1## wherein: A is a heterocyclic amine moiety selected from the group consisting of piperidine, substituted piperidine, piperazine, substituted piperazine, imidazole, substituted imidazole, pyrazole, substituted pyrazole, pyrazine, substituted pyrazine, pyrrole, substituted pyrrole, pyrrolidine, substituted pyrrolidine, indole, substituted indole, indoline, substituted indoline, quinoline, substituted quinoline, isoquinoline, substituted isoquinoline, thiazole, substituted thiazole, oxazole, substituted oxazole, thiazolidine, and substituted thiazolidine, wherein substitution is at any or all substituent positions, and comprises substituents selected from the group consisting of alkyl (preferably C.sub.1 -C.sub.10 linear or branched alkyl), alkylaryl, aryl, aralkyl, nitro, alkoxy, hydroxy, cyano, thiol, and halo;R.sub.1 is selected from H, alkyl (preferably C.sub.1 -C.sub.10 linear or branched alkyl), alkylaryl, aryl, and arylalkyl; andR.sub.2 is selected from CN, COOH, COOR.sub.3, and CONHR.sub.3 where R.sub.3 is selected from H, alkyl (preferably C.sub.1 -C.sub.10 linear or branched alkyl), alkylaryl, aryl, aralkyl.The heterocyclic amine-borane compounds of the invention are bioactive in character, variously exhibiting anti-tumor, anti-inflammatory, and anti-hyperlipidemic activity. In another aspect, the invention relates to a method of inhibiting enzyme activity (e.g., DNA topoisomerase II, PRPP amidotransferase, IMP dehydrogenase, dihydrofolate reductase, and/or ribonucleotide reductase) in an in vitro or in vivo system, comprising administering to the system an enzyme-inhibitingly effective amount of a Lewis-base borane adduct, such as for example a heterocyclic amine-borane compound of the foregoing formula.
摘要翻译：式（I）的杂环胺 - 硼烷化合物，其中：A是杂环胺部分; R1选自H，烷基，烷基芳基，芳基和芳基烷基; 并且R 2选自CN，COOH，COOR 3和CONHR 3，其中R 3选自H，烷基，烷基芳基，芳基，芳烷基。本发明的杂环胺 - 硼烷化合物是具有生物活性的，各种表现出抗肿瘤，抗炎和抗高血脂活性。本发明还包括在体外或体内系统中抑制酶活性的方法（例如，DNA拓扑异构酶II，PRPP氨基转移酶，IMP脱氢酶，二氢叶酸还原酶和/或核糖核苷酸还原酶），包括向系统施用酶抑制有效量的路易斯碱硼烷加合物，例如上述式的杂环胺 - 硼烷化合物。

8. 发明授权

US5177198A Process for preparing oligoribonucleoside and oligodeoxyribonucleoside boranophosphates 失效
标题翻译：制备寡核苷酸和寡糖氧基二硼磷酸酯的方法
公开(公告)号：US5177198A
公开(公告)日：1993-01-05
申请号：US443781
申请日：1989-11-30
申请人： Bernard F. Spielvogel , Anup Sood , Iris H. Hall , Barbara Ramsay Shaw
发明人： Bernard F. Spielvogel , Anup Sood , Iris H. Hall , Barbara Ramsay Shaw
IPC分类号： A61K31/69 , A61K31/70 , A61K31/7135 , A61P3/06 , A61P29/00 , A61P35/00 , C07H21/00 , C07H21/04 , C07H23/00 , C12N15/113 , C12Q1/68
CPC分类号： C12N15/113 , C07H21/00 , C12Q1/6876 , C12N2310/31 , C12N2310/312 , C12N2310/315 , C12N2310/321 , C12N2310/353 , Y02P20/55
摘要： A process of making oligoribonucleoside and deoxyribonucleoside boranophosphates and salts thereof is disclosed. The process comprises the steps of condensing a ribonucleotide or deoxyribonucleotide with a nucleoside phosphitylating agent, wherein the phosphitylating agent includes a 5' -OH group protected by an acid-labile protecting group and a moiety bonded to the phosphorus atom therein that is a stronger proton acceptor than the 5'-OH group of the ribonucleotide or deoxyribonucleotide to form a reaction intermediate, then oxidizing the reaction intermediate so formed with a compound comprising a Lewis base and a boron-containing substituent, wherein the Lewis base is a weaker electron donor than the phosphite phosphorus of the reaction intermediate, to form a ribonucleotide or deoxyribonucleotide boranophosphate. These steps are repeated on the nucleotide boranophosphate to form an oligonucleotide boranophosphate.
摘要翻译：公开了制备寡核糖核苷和脱氧核糖核苷硼烷磷酸盐及其盐的方法。该方法包括将核糖核苷酸或脱氧核糖核苷酸与核苷磷酸化沉淀剂缩合的步骤，其中磷酸化剂包括被酸不稳定保护基团保护的5'-OH基团和与其中的磷原子键合的部分，其是更强的质子受体比核糖核苷酸或脱氧核糖核苷酸的5'-OH基团形成反应中间体，然后用包含路易斯碱和含硼取代基的化合物氧化形成的反应中间体，其中路易斯碱比较弱的电子给体比反应中间体的亚磷酸酯磷，形成核糖核苷酸或脱氧核糖核苷酸硼磷酸盐。在核苷酸硼酸盐上重复这些步骤以形成寡核苷酸硼磷酸盐。

9. 发明授权

US5130302A Boronated nucleoside, nucleotide and oligonucleotide compounds, compositions and methods for using same 失效
标题翻译：硼氢化核苷，核和寡核苷酸化合物，组合物及其使用方法
公开(公告)号：US5130302A
公开(公告)日：1992-07-14
申请号：US453311
申请日：1989-12-20
申请人： Bernard F. Spielvogel , Anup Sood , Iris H. Hall , Barbara Ramsay Shaw
发明人： Bernard F. Spielvogel , Anup Sood , Iris H. Hall , Barbara Ramsay Shaw
IPC分类号： A61K31/70 , A61K31/7135 , A61P3/08 , A61P35/00 , A61P37/08 , C07D473/00 , C07D473/18 , C07D473/34 , C07F5/02 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , C07H23/00
CPC分类号： C07D473/00 , C07D473/18 , C07D473/34 , C07F5/02 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , C07H23/00
摘要： A novel class of pharmaceutically active boronated nucleosides are provided. The nucleosides are boronated at a ring nitrogen of the purine or pyrimidine or analogues thereof. Also provided are phosphate esters of these nucleosides and oligomers thereof. Methods of making and using the boronated nucleosides are also disclosed.
摘要翻译：提供了一类新颖的药学活性硼化核苷。核苷在嘌呤或嘧啶或其类似物的环氮上硼化。还提供了这些核苷的磷酸酯及其低聚物。还公开了制备和使用硼化核苷的方法。

10. 发明授权

US4587359A Amine-carbamoylborane adducts 失效
标题翻译：胺 - 氨基甲酰基硼烷加成物
公开(公告)号：US4587359A
公开(公告)日：1986-05-06
申请号：US611247
申请日：1984-05-17
申请人： Bernard F. Spielvogel , Andrew T. McPhail , Iris H. Hall
发明人： Bernard F. Spielvogel , Andrew T. McPhail , Iris H. Hall
IPC分类号： C07F5/02
CPC分类号： C07F5/027
摘要： This invention involves amine-carbamoylborane compounds of the formulaR.sub.1 R.sub.2 NH.BH.sub.2 C(O)NHR.sub.3wherein R.sub.1 and R.sub.2 are hydrogen or certain alkyl moieties and R..3 is an alkyl. A process for their preparation involving an amine displacement reaction is also described. A method of use and pharmaceutical compositions containing the subject compounds are also described.
摘要翻译：本发明涉及式R1R2NH.BH2C（O）NHR3的胺 - 氨基甲酰基硼烷化合物，其中R 1和R 2是氢或某些烷基部分，且R 3是烷基。还描述了其涉及胺置换反应的制备方法。还描述了使用方法和含有本发明化合物的药物组合物。

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