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41. 发明申请

WO1995026354A1 NEW IODIZED BORON COMPOUNDS USEFUL AS X RAY CONTRASTING AGENTS, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：新的有机硼化合物可用作X射线对比剂和含有它们的药物组合物
公开(公告)号：WO1995026354A1
公开(公告)日：1995-10-05
申请号：PCT/ES1995000031
申请日：1995-03-23
申请人： CENTRO INVESTIGACION JUSTESA IMAGEN, S.A. , MARTIN JIMENEZ, José, L. , SPECK, Ulrich , CARRETERO COLON, José, Maria , MARTINEZ SANZ, Antonio , BOHLE, Florian , KRAUSE, Werner
发明人： CENTRO INVESTIGACION JUSTESA IMAGEN, S.A.
IPC分类号： C07F05/02
CPC分类号： C07F5/027 , A61K41/0095 , A61K49/0433
摘要： The invention relates to new organic boron compounds having a monomer structure (I): [BxCyH(x+y-t-w)ItZw], 2/rQ and a dimer structure (II): {[B12H(12-t-w)ItZw]-N(R)-[B12H(12-t-w)ItZw]}, 4/rQ, caracterized in that they contain a high molar percentage of iodine, and are useful as radio-opaque agents in uroangiography, cardioangiography, etc., as well as for selectively visualizing organs or body systems such as the liver, the spleen or the lymphatic system. The compounds having the general formulas (I) and (II) are also useful in the selective therapy of tumors. The invention also relates to pharmaceutical preparations which contain the claimed compounds having the general formulas (I) and (II).
摘要翻译：本发明涉及具有单体结构（I）的新的有机硼化合物：[BxCyH（x + ytw）ItZw]，2 / rQ和二聚体结构（II）：{[B12H（12-tw）ItZw] -N（ R） - [B12H（12-tw）ItZw]}，4 / rQ，其特征在于它们含有高摩尔百分比的碘，并且可用作尿路造影，心脏血管造影术等中的不透射线剂，以及选择性地观察器官或身体系统如肝脏，脾脏或淋巴系统。具有通式（I）和（II）的化合物也可用于肿瘤的选择性治疗。本发明还涉及含有所要求保护的具有通式（I）和（II）的化合物的药物制剂。

42. 发明申请

WO1994026751A1 ENANTIOSELECTIVE OXAZABOROLIDINE CATALYSTS 审中-公开
标题翻译： ENANTICONLECTIVE OXAZABOROLIDINE CATALYSTS
公开(公告)号：WO1994026751A1
公开(公告)日：1994-11-24
申请号：PCT/IB1994000066
申请日：1994-04-12
申请人： PFIZER INC. , QUALLICH, George, J.
发明人： PFIZER INC.
IPC分类号： C07F05/02
CPC分类号： C07F5/025 , B01J31/0211 , B01J31/0252 , B01J31/0271 , B01J31/146 , B01J2231/64 , C07B2200/07 , C07C29/143 , C07C213/00 , C07C2602/10 , C07F5/022 , C07C33/46 , C07C35/32 , C07C31/125 , C07C33/20
摘要： The enantioselective borane reduction of prochiral ketones to optically pure alcohols is effectively achieved by performing the reduction in the presence of catalytic amounts of the new and valuable oxazaborolidine compounds of formulae (I) and (II). The compounds of formulae (I) and (II) may be isolated and purified prior to use in the reduction reactions or the compounds of formulae (I) and (II) may be generated in situ.
摘要翻译：通过进行催化量的新型和有价值的式（I）和（II）氧氮杂硼烷化合物的存在来降低前手性酮对光学纯醇的对映选择性硼烷还原作用。式（I）和（II）的化合物可以在还原反应中使用之前被分离和纯化，或者原位生成式（I）和（II）的化合物。

43. 发明申请

WO1994000459A1 PROCESS FOR PRODUCING TETRAKISFLUOROPHENYLBORATE 审中-公开
标题翻译：四氯三氟乙烯生产工艺
公开(公告)号：WO1994000459A1
公开(公告)日：1994-01-06
申请号：PCT/JP1993000837
申请日：1993-06-22
申请人： IDEMITSU KOSAN CO., LTD. , NAGANUMA, Shoji , WATANABE, Masami , TOMOTSU, Norio
发明人： IDEMITSU KOSAN CO., LTD.
IPC分类号： C07F05/02
CPC分类号： C08F10/00 , C07F5/027 , C08F4/65912 , C08F4/65927 , C08F12/08 , C08F110/06 , C08F4/65908 , C08F4/643 , C08F4/6592
摘要： An efficient process for producing a tetrakisfluorophenylborate, useful as an olefin polymerization catalyst component or a starting material therefor, at a high production rate per unit solvent and a high yield according to the following reaction formula, wherein a mixture of ether with an aliphatic hydrocarbon is used as the reaction solvent: 4M4-C6Y35+BCl3->M4B(C6Y35)4, wherein M4 represents an alkali metal, an alkaline earth metal or R62Al (wherein R6 represents alkyl); and Y3 represents hydrogen or halogen.
摘要翻译：根据以下反应式，以每单位溶剂的高产率和高收率生产四氟氟苯硼酸盐的有效方法，其可用作烯烃聚合催化剂组分或其原料，其中醚与脂族烃的混合物为用作反应溶剂：4M4-C6Y35 + BCl3-> M4B（C6Y35）4，其中M4表示碱金属，碱土金属或R62Al（其中R6表示烷基）; Y 3表示氢或卤素。

44. 发明申请

WO1993023408A1 ENANTIOSELECTIVE OXAZABOROLIDINE CATALYSTS 审中-公开
标题翻译： ENANTICONLECTIVE OXAZABOROLIDINE CATALYSTS
公开(公告)号：WO1993023408A1
公开(公告)日：1993-11-25
申请号：PCT/US1993000687
申请日：1993-02-01
申请人： PFIZER INC. , QUALLICH, George, J.
发明人： PFIZER INC.
IPC分类号： C07F05/02
CPC分类号： C07D213/30 , C07B2200/07 , C07C29/143 , C07C2601/08 , C07C2601/10 , C07D277/24 , C07D311/22 , C07D417/06 , C07F5/02 , C07F5/025 , C07C33/22 , C07C31/125 , C07C33/20 , C07C35/36 , C07C35/32
摘要： The borane reduction of prochiral ketones to optically pure alcohols is effectively achieved by the utilization of catalytic amounts of the new and valuable oxazaborolidine catalysts of formula (I).
摘要翻译：通过使用催化量的式（I）的新的和有价值的恶唑硼烷催化剂，可以有效地实现前手性酮对光学纯醇的硼烷还原。

45. 发明申请

WO1993010127A1 METHOD FOR MAKING A PROLINEBORONATE ESTER 审中-公开
标题翻译：制备丙硼酸酯的方法
公开(公告)号：WO1993010127A1
公开(公告)日：1993-05-27
申请号：PCT/US1992009845
申请日：1992-11-19
申请人： BOEHRINGER INGELHEIM PHARMACEUTICALS, INC.
发明人： BOEHRINGER INGELHEIM PHARMACEUTICALS, INC. , SNOW, Roger , KELLY, Terence, A. , ADAMS, Julian , COUTTS, Simon , PERRY, Clark
IPC分类号： C07F05/02
CPC分类号： C07F5/025 , Y02P20/55
摘要： A method for the preparation of esters of prolineboronic acid is described. An N-protected pyrrole (I) is lithiated at the 2-position. The lithiated species (II) is reacted with trialkylborate, to yield a protected pyrrole-2-boronic acid (III). This is reduced to form a protected prolineboronic acid (IV), which, in turn, is reacted with a diol to yield an ester (VI). With the boronic acid moiety protected by the ester group, the protecting group on the nitrogen is removed, yielding the desired prolineboronic acid ester (VII). In an alternative synthesis, a protected pyrrolidine (VIII) is lithiated at the 2-position to yield a protected 2-lithio-pyrrolidine (IX). This is reacted with trialkylborate to yield the intermediate IV. The prolineboronic acid esters so produced have a chiral center to the boron atom. Also disclosed are methods for resolving enantiomers. The final products can be coupled to activated carboxylic acids, to yield peptides having a prolineboronic acid ester, instead of an amino acid, at the C-terminus. These boronic acid peptide analogs are useful for inhibiting biologically important proteases. Several methods for removing pinanediol from pinanediol boronate esters are also disclosed.
摘要翻译：描述了制备脯氨酸硼酸酯的方法。 N-保护的吡咯（I）在2-位锂化。锂化物（II）与硼酸三烷基酯反应，得到受保护的吡咯-2-硼酸（III）。这被还原形成受保护的脯氨酸硼酸（Ⅳ），其又与二醇反应得到酯（Ⅵ）。用酯基保护的硼酸部分除去氮上的保护基，得到所需的脯氨酸硼酸酯（Ⅶ）。在替代合成中，保护的吡咯烷（Ⅷ）在2-位锂化，得到保护的2-锂 - 吡咯烷（Ⅸ）。使其与硼酸三烷基酯反应，得到中间体IV。如此制备的脯氨酸硼酸酯具有对硼原子的手性中心。还公开了解决对映异构体的方法。最终产物可以与活化的羧酸偶联，以产生在C-末端具有脯氨酸硼酸酯而不是氨基酸的肽。这些硼酸肽类似物可用于抑制生物学上重要的蛋白酶。还公开了从蒎二醇硼酸酯除去蒎二醇的几种方法。

46. 发明申请

WO1992008722A1 LABELLING AGENTS COMPRISING BORONIC ACID CONJUGATES 审中-公开
标题翻译：包含硼酸结合物的标签试剂
公开(公告)号：WO1992008722A1
公开(公告)日：1992-05-29
申请号：PCT/EP1991002160
申请日：1991-11-13
申请人： COCKBAIN, Julian, Roderick, Michaelson , AXIS RESEARCH AS , FRANTZEN, Frank , SUNDREHAGEN, Erling
发明人： COCKBAIN, Julian, Roderick, Michaelson , AXIS RESEARCH AS
IPC分类号： C07F05/02
CPC分类号： G01N33/587 , C07F5/025 , G01N33/533
摘要： Labelling agents comprising non-proteinaceous boronic acid conjugates having absorption maxima at not less than 600 nm, said label being provided by e.g. an azine, triphenylmethane, cyanine or phthalocyanine dye, are useful in the estimation and quantification of cisdiols such as glycosylated haemoglobin, by virtue of the substantially total absence of overlap with the absorption spectrum of haemoglobin. Oxazine and thiazine dyes exhibiting similar absorption characteristics and containing other activated moieties are similarly useful labelling agents, especially in the presence of haemoglobin.
摘要翻译：包含非蛋白质硼酸缀合物的标记试剂，其吸收最大值不小于600nm，所述标记由例如，吖嗪，三苯甲烷，花青或酞菁染料，由于与血红蛋白的吸收光谱基本完全不存在重叠，可用于估计和定量顺式二糖如糖基化血红蛋白。表现出相似吸收特性并含有其它活化部分的恶嗪和噻嗪染料也是类似地有用的标记试剂，特别是在血红蛋白存在下。

47. 发明申请

WO1987004438A1 NOVEL OPTICALLY ACTIVE ALKALI METAL MONO- AND DIORGANYLBOROHYDRIDES AND BORANES AND PROCESS FOR PREPARING AND USING SAME 审中-公开
标题翻译：新型光学活性碱金属单和二硼酸和硼烷及其制备和使用方法
公开(公告)号：WO1987004438A1
公开(公告)日：1987-07-30
申请号：PCT/US1987000133
申请日：1987-01-21
申请人： ALDRICH-BORANES, INC.
发明人： ALDRICH-BORANES, INC. , BROWN, Herbert, C.
IPC分类号： C07F05/02
CPC分类号： C07F5/027 , C07F1/02
摘要： Treatment of boronic esters of very high optical purity with alkali metal aluminum hydride and treatment of borinic esters of very high optical purity with alkali metal monoalkoxyaluminohydride provides novel, quantitative synthesis of novel alkali metal monoorganyl- and diorganylborohydrides containing boron directly attached to the asymmetric center or centers of essentially 100% optical purity. These optically active mono- and diorganylborohydrides provide new, useful optically active reducing agents and convenient sources for optically active mono- and diorganylboranes.
摘要翻译：用碱金属氢化铝处理具有非常高光学纯度的硼酸酯，并用碱金属单烷氧基烷化氢处理非常高的光学纯度的硼酸酯提供了新的，定量合成含有直接连接到不对称中心的硼的新型碱金属单有机基和二有机硼烷，基本上100％光学纯度的中心。这些光学活性单 - 和二有机硼酸盐提供新的有用的光学活性还原剂和光学活性单 - 和二有机硼烷的方便来源。

48. 发明申请

WO1987003594A1 AMIFLOXACINE INTERMEDIATE 审中-公开
标题翻译： AMIFLOXACINE中间体
公开(公告)号：WO1987003594A1
公开(公告)日：1987-06-18
申请号：PCT/HU1986000066
申请日：1986-12-09
申请人： MÉSZAROS, Zoltánné (legal heir and representative , MÉSZAROS, Marta (legal heir and representative of , CHINOIN GYOGYSZERRÉS VEGYÉSZETI TERMÉKEK GYARA ... , HERMECZ, István , KERESZTURI, Géza , VASVARI, Lelle , HORVATH, Agnes , BALOGH, Mária , KOVACS, Gábor , RITLI, Péter , SIPOS, Judit , PAJOR, Anikó
发明人： MÉSZAROS, Zoltánné (legal heir and representative , MÉSZAROS, Marta (legal heir and representative of , CHINOIN GYOGYSZERRÉS VEGYÉSZETI TERMÉKEK GYARA ... , MÉSZAROS, Zoltán (deceased)
IPC分类号： C07F05/02
CPC分类号： C07F5/04
摘要： New 6-fluoro-7-chloro-1-methylamino-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid/boric acid anhydrides of general formula (I), (wherein R and R stand for halogen; an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or an aromatic acyloxy group comprising 7-11 carbon atoms). The new compounds of general formula (I) are valuable intermediates useful in the preparation of the antibacterial agent 6-fluoro-1-methylamino-7-(4-methyl-piperazino)-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid. The new compounds of general formula (I) may be prepared by reacting a compound of formula (II), or a compound of general formula (III), (wherein R stands for alkyl comprising 1-4 carbon atoms) with hydrogen fluoro borate of the formula (IV), or a borone trihalide of general formula (V), (wherein X stands for fluorine, chlorine or bromine) or a complex thereof formed with an ether or a borone derivative of general formula (VI), (wherein R , R and R stand for alkyl comprising 1-5 carbon atoms and optionally substituted by halogen or aryl comprising 6-10 carbon atoms).
摘要翻译：通式（I）的新的6-氟-7-氯-1-甲基氨基-4-氧代-1,4-二氢 - 喹啉-3-羧酸/硼酸酐（其中R和R 1代表卤素;包含2-6个碳原子并任选被卤素取代的脂族酰氧基;或包含7-11个碳原子的芳族酰氧基）。通式（I）的新化合物是可用于制备抗菌剂6-氟-1-甲氨基-7-（4-甲基 - 哌嗪子基）-4-氧代-1,4-二氢 - 喹啉-2-酮的有价值的中间体，吡啶-3-羧酸。通式（I）的新化合物可以通过使式（II）化合物或通式（III）的化合物（其中R 2代表含有1-4个碳原子的烷基）与氢式（Ⅳ）的氟硼酸盐，或通式（Ⅴ）的三卤化硼，（其中X表示氟，氯或溴）或其与通式（Ⅵ）的醚或硼化硼衍生物形成的络合物，（其中R 3，R 4和R 5代表包含1-5个碳原子并且任选被卤素或包含6-10个碳原子的芳基取代的烷基）。

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