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1. 发明授权

US5659027A Boronated compounds 失效
标题翻译：硼化合物
公开(公告)号：US5659027A
公开(公告)日：1997-08-19
申请号：US334745
申请日：1994-11-04
申请人： Bernard F. Spielvogel , Anup Sood , Iris H. Hall , Barbara Ramsay Shaw , Jeno Tomasz
发明人： Bernard F. Spielvogel , Anup Sood , Iris H. Hall , Barbara Ramsay Shaw , Jeno Tomasz
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 , C07H1/00
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 , Y10S514/824 , Y10S514/825 , Y10S514/886
摘要： A novel class of pharmaceutically active boronated compounds are provided. The boronated compounds include boronated purine and pyrimidine bases and boronated nucleosides, as well as phosphate esters and oligomers thereof. The compounds are boronated at the ring nitrogen of the purine or pyrimidine base, or at a 2', 3' or 5' amino substituent of the nucleoside sugar.
摘要翻译：提供了一类新颖的药物活性硼化合物。硼化化合物包括硼化嘌呤和嘧啶碱基和硼化核苷，以及其磷酸酯和低聚物。化合物在嘌呤或嘧啶碱基的环氮上或在核苷糖的2'，3'或5'氨基取代基处硼化。

2. 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。

3. 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。

4. 发明授权

US5362732A Boronated compounds 失效
标题翻译：硼化合物
公开(公告)号：US5362732A
公开(公告)日：1994-11-08
申请号：US909950
申请日：1992-07-07
申请人： Bernard F. Spielvogel , Anup Sood , Iris H. Hall , Barbara R. Shaw , Jeno Tomasz
发明人： Bernard F. Spielvogel , Anup Sood , Iris H. Hall , Barbara R. Shaw , Jeno Tomasz
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 , A61K31/505 , A61K31/52 , C07D239/00
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 , Y10S514/824 , Y10S514/825 , Y10S514/886
摘要： A novel class of pharmaceutically active boronated compounds are provided. The boronated compounds include boronated purine and pyrimidine bases and boronated nucleosides, as well as phosphate esters and oligomers thereof. The compounds are boronated at the ring nitrogen of the purine or pyrimidine base, or at a 2', 3' or 5' amino substituent of the nucleoside sugar.
摘要翻译：提供了一类新颖的药物活性硼化合物。硼化化合物包括硼化嘌呤和嘧啶碱基和硼化核苷，以及其磷酸酯和低聚物。化合物在嘌呤或嘧啶碱基的环氮上或在核苷糖的2'，3'或5'氨基取代基处硼化。

5. 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。

6. 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。

7. 发明授权

US5455233A Oligoribonucleoside and oligodeoxyribonucleoside boranophosphates 失效
标题翻译：寡核糖核苷和寡脱氧核糖核苷硼烷磷酸酯
公开(公告)号：US5455233A
公开(公告)日：1995-10-03
申请号：US953820
申请日：1992-09-30
申请人： Bernard F. Spielvogel , Anup Sood , Iris H. Hall , Barbara R. Shaw
发明人： Bernard F. Spielvogel , Anup Sood , Iris H. Hall , Barbara R. 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： Disclosed are oligonucleoside boranophosphates, or salts thereof, comprising a chain of natural or modified ribonucleotides or deoxyribonucleotides, containing at least one boronated internucleotide phospodiester linkage of the formula: ##STR1## W is selected from the group consisting of .dbd.O, .dbd.S, --OPr, and --SPr where Pr is a base-labile protecting group. X is selected from the group consisting of --BH.sub.3, --BH.sub.2 R.sub.1, --BHR.sub.1 R.sub.2 and --BR.sub.1 R.sub.2 R.sub.3. R.sub.1 is selected from the group consisting of --R.sub.4, --COOH, --COOR.sub.4, --CONHR.sub.4, --CON(R.sub.4).sub.2, --CN.sup.+ R.sub.4 Z.sup.-, wherein Z.sup.- is an anion, --CN, carboxycholesteryl and carboxybenzyl, wherein R.sub.4 is C1 to C18 alkyl. R.sub.2 is selected from the group consisting of --R.sub.5, --COOH, --COOR.sub.5, --CONHR.sub.5, --CON(R.sub.5).sub.2, --CN.sup.+ R.sub.5 Z.sup.-, wherein Z.sup.- is an anion, --CN, carboxy- cholesteryl and carboxybenzyl, wherein R.sub.5 is C1 to C18 alkyl. R.sub.3 is selected from the group consisting of C1 to C3 alkyl. Most preferably, X is --BH.sub.3 and W is =0.Compounds of Formula (III) are useful as antisense agents and probes in molecular biology, and have pharmacological activities including anti-inflammatory, antihyperlipidemic, and antineoplastic activity.
摘要翻译：公开了包含天然或修饰的核糖核苷酸链或脱氧核糖核苷酸的寡核苷硼烷磷酸酯或其盐，其含有至少一个下式的硼化核苷酸间磷酸二酯键：W选自= O = S，-OPr和-SPr，其中Pr是碱不稳定保护基。 X选自-BH 3，-BH 2 R 1，-BHR 1 R 2和-BR 1 R 2 R 3。 R1选自-R4，-COOH，-COOR4，-CONHR4，-CON（R4）2，-CN + R4Z-，其中Z-为阴离子，-CN，羧基胆固醇基和羧基苄基，其中R4为 C1至C18烷基。 R2选自-R5，-COOH，-COOR5，-CONHR5，-CON（R5）2，-CN + R5Z-，其中Z-为阴离子，-CN，羧基 - 胆固醇基和羧基苄基，其中 R5是C1-C18烷基。 R3选自C1至C3烷基。最优选地，X是-BH 3且W是= 0。式（III）的化合物可用作分子生物学中的反义剂和探针，具有抗炎，抗高脂血症和抗肿瘤活性的药理活性。

8. 发明授权

US5312816A Method of combatting osteoporosis in mammalian subjects, utilizing organic boron compounds 失效
标题翻译：使用有机硼化合物来治疗哺乳动物受试者的骨质疏松症的方法
公开(公告)号：US5312816A
公开(公告)日：1994-05-17
申请号：US121221
申请日：1993-09-14
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： A61K45/00 , A61K31/69 , A61K31/70 , A61P9/08 , A61P9/10 , A61P9/12 , A61P17/00 , A61P19/10 , A61P25/04 , A61P29/00 , A61P43/00 , C07F5/02
CPC分类号： A61K31/69
摘要： A method of combatting, e.g., preventing as well as treating, a disease state such as cystic fibrosis, neonatal hypoxemia, pulmonary hypertension, adult respiratory distress syndrome, psoriasis, spondyloarthritis, rheumatoid arthritis, gout, inflammatory bowel disease, myocardial infarctions, and/or osteoporosis in an animal subject, by administering to the animal subject an amount of an organic boron compound which is effective thereagainst. The organic boron compounds usefully employed in the method of the invention include any suitable organic boron-containing compounds, such as Lewis base-boron adducts; a preferred class of organic boron compounds useful in such method includes boron analogs of .alpha.-amino acids, and the corresponding amides and esters of such amino acids. A method is also disclosed of inhibiting enzyme activity in in vitro or in vivo systems comprising administering to such system an enzyme-inhibiting amount of an organic boron compound. Further disclosed is a method of reducing hydroxyproline, calcium, and/or inorganic phosphorous in serum and/or urine of an animal subject, by administering to the animal subject an effective amount of an organic boron compound.
摘要翻译：一种防治疾病状态如囊性纤维化，新生儿低氧血症，肺动脉高压，成人呼吸窘迫综合征，牛皮癣，脊椎关节炎，类风湿性关节炎，痛风，炎性肠病，心肌梗塞和/ 或动物受试者的骨质疏松症，通过向动物受试者施用一定量的有效硼化合物。在本发明方法中有用的有机硼化合物包括任何合适的有机含硼化合物，例如路易斯碱 - 硼加成物; 用于这种方法的优选类型的有机硼化合物包括α-氨基酸的硼类似物，以及这些氨基酸的相应的酰胺和酯。还公开了一种在体外或体内系统中抑制酶活性的方法，包括向该系统施用酶抑制量的有机硼化合物。进一步公开的是通过向动物受试者施用有效量的有机硼化合物来减少动物受试者的血清和/或尿中的羟脯氨酸，钙和/或无机磷的方法。

9. 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.

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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