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1. 发明授权

US06252084B1 1H-indole-3-acetamide sPLA2 inhibitors 失效
标题翻译： 1H-吲哚-3-乙酰胺sPLA2抑制剂
公开(公告)号：US06252084B1
公开(公告)日：2001-06-26
申请号：US08962603
申请日：1997-10-31
申请人： Nicholas J. Bach , Robert D. Dillard , Susan E. Draheim , Robert B. Hermann , Richard W. Schevitz
发明人： Nicholas J. Bach , Robert D. Dillard , Susan E. Draheim , Robert B. Hermann , Richard W. Schevitz
IPC分类号： C07F938
CPC分类号： C07D401/06 , C07D209/22 , C07D209/24 , C07D209/30 , C07F9/5728
摘要： A class of novel 1H-indole-3-acetamides is disclosed together with the use of such indole compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.
摘要翻译：公开了一类新的1H-吲哚-3-乙酰胺以及这种吲哚化合物用于抑制sPLA2介导的脂肪酸释放以治疗诸如败血性休克的病症的用途。

2. 发明授权

US06194604B1 Process for producing phosphorous acid 有权
标题翻译：亚磷酸生产方法
公开(公告)号：US06194604B1
公开(公告)日：2001-02-27
申请号：US09274629
申请日：1999-03-23
申请人： Yinong Ma , Jerald D. Heise
发明人： Yinong Ma , Jerald D. Heise
IPC分类号： C07F938
CPC分类号： C01B25/163
摘要： A process for the manufacture of phosphorous acid by selective hydrolysis of phosphite esters. A hydrolysis feed mixture comprising phosphite esters and phosphate esters is contacted with liquid water or steam to selectively hydrolyze the phosphite esters to phosphorous acid. The feed mixture may be prepared by oxidation of elemental phosphorous in the presence of an alcohol. In the oxidation and/or a subsequent esterification step, P(III) and P(V) oxyacids produced in the oxidation reaction are esterified, preferably quantitatively. The ester mixture may be washed to remove unesterified phosphoric and hypophosphorous acid, after which the selective hydrolysis is carried out.
摘要翻译：通过选择性水解亚磷酸酯制备亚磷酸的方法。将包含亚磷酸酯和磷酸酯的水解进料混合物与液态水或蒸汽接触以选择性地将亚磷酸酯水解成亚磷酸。进料混合物可以通过在醇存在下氧化元素磷来制备。在氧化和/或随后的酯化步骤中，在氧化反应中产生的P（III）和P（V）含氧酸优选定量地酯化。可以洗涤酯混合物以除去未酯化的磷酸和次磷酸，然后进行选择性水解。

3. 发明授权

US06603039B1 Deeply reduced oxidation catalyst and its use for catalyzing liquid phase oxidation reactions 有权
公开(公告)号：US06603039B1
公开(公告)日：2003-08-05
申请号：US09408296
申请日：1999-09-29
申请人： Jerry R. Ebner , Mark A. Leiber , Kam-To Wan , Peter E. Rogers , Jingyue Liu , Anthony Woods
发明人： Jerry R. Ebner , Mark A. Leiber , Kam-To Wan , Peter E. Rogers , Jingyue Liu , Anthony Woods
IPC分类号： C07F938
CPC分类号： B01J23/56 , B01J21/18 , B01J23/40 , C07F9/3813 , Y02P20/582
摘要： This invention relates to an improved catalyst, comprising a carbon support having a noble metal at its surface, for use in catalyzing liquid phase oxidation reactions, especially in an acidic oxidative environment and in the presence of solvents, reactants, intermediates, or products which solubilize noble metals; a process for the preparation of the improved catalyst; a liquid phase oxidation process using such a catalyst wherein the catalyst exhibits improved resistance to noble metal leaching, particularly in acidic oxidative environments and in the presence of solvents, reactants, intermediates, or products which solubilize noble metals; and a liquid phase oxidation process in which N-(phosphonomethyl)iminodiacetic acid (i.e., “PMIDA”) or a salt thereof is oxidized to form N-(phosphonomethyl)glycine (i.e., “glyphosate”) or a salt thereof using such a catalyst wherein the oxidation of the formaldehyde and formic acid by-products into carbon dioxide and water is increased.

4. 发明授权

US06573252B1 Medicine nitrate salts 失效
标题翻译：药用硝酸盐
公开(公告)号：US06573252B1
公开(公告)日：2003-06-03
申请号：US09743801
申请日：2001-01-19
申请人： Piero Del Soldato
发明人： Piero Del Soldato
IPC分类号： C07F938
CPC分类号： C07J51/00 , C07C217/74 , C07C229/42 , C07C229/58 , C07C229/64 , C07C323/58 , C07D209/22 , C07D213/80 , C07D215/18 , C07D231/06 , C07D231/56 , C07D233/64 , C07D235/02 , C07D279/02 , C07D405/04 , C07D417/04 , C07D471/04 , C07D475/08 , C07D491/04 , C07D513/04 , C07F9/3808 , C07F9/3873 , C07F9/5728 , C07F9/5765 , C07F9/58
摘要： The present invention relates to nitrate salts of compounds having therapeutic activity in bony disorders, such compounds being characterized in that they contain at least a reactive group capable of being salified with nitric acid.
摘要翻译：本发明涉及在骨骼疾病中具有治疗活性的化合物的硝酸盐，其特征在于它们至少包含能够用硝酸盐化的反应性基团。

5. 发明授权

US06534488B1 Radiolabelled bisphosphonates and method 失效
标题翻译：放射性标记的双膦酸盐和方法
公开(公告)号：US06534488B1
公开(公告)日：2003-03-18
申请号：US10031760
申请日：2002-05-08
申请人： Alexander Mark Gibson , Marivi Mendizabal , Richard Pither , Shirley Elizabeth Pullan , Vaughan Griffiths , Philip Duncanson
发明人： Alexander Mark Gibson , Marivi Mendizabal , Richard Pither , Shirley Elizabeth Pullan , Vaughan Griffiths , Philip Duncanson
IPC分类号： C07F938
CPC分类号： C07B59/004 , C07F9/386 , C07F9/3873 , C07F9/409
摘要： The present invention relates to 32P or 33P-labelled bisphosphonates as radiotherapeutic radiopharmaceuticals. The 32P- or 33P-labelled bisphosphonates, which are chemically identical to the unlabelled agent, are expected to target the lesion site in an identical manner, but also deliver a significant radiocytotoxic effect to the surrounding cells. This should result, given the favorable energetics of the &bgr; particle emission from the 33P nuclide, in a loss of proliferative capacity of cells associated with the tumor lesion. The relative stability and in vivo localisation of bisphosphonates makes them good candidates as 32P/33P delivery vehicles.
摘要翻译：本发明涉及作为放射治疗放射性药物的32P或33P标记的双膦酸盐。与未标记试剂化学相同的32P或33P标记的双膦酸盐预期以相同的方式靶向病变部位，但也对周围细胞产生显着的放射性细胞毒性作用。考虑到来自33P核素的β粒子发射的有利能量，与肿瘤病变相关的细胞的增殖能力丧失将导致这一点。双膦酸盐的相对稳定性和体内定位使其成为32P / 33P递送载体的良好候选物。

6. 发明授权

US06235727B1 Sulfonylaminophosphinic and sulfonylaminophosphinic acid derivatives, methods for their preparation and use 有权
标题翻译：磺酰氨基膦酸和磺酰氨基磷酸衍生物，其制备和使用方法
公开(公告)号：US06235727B1
公开(公告)日：2001-05-22
申请号：US09353086
申请日：1999-07-15
申请人： Manfred Schudok , Wilfried Schwab , Gerhard Zoller , Eckart Bartnik , Frank Büttner , Klaus-Ulrich Weithmann
发明人： Manfred Schudok , Wilfried Schwab , Gerhard Zoller , Eckart Bartnik , Frank Büttner , Klaus-Ulrich Weithmann
IPC分类号： C07F938
CPC分类号： C07F9/5728 , C07F9/3808 , C07F9/4006 , C07F9/572
摘要： Compounds of the formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading enzymes is involved.
摘要翻译：式I化合物适用于生产用于预防和治疗疾病的药物，其中涉及增加基质降解酶的活性。

7. 发明授权

US06218570B1 Method for preparing formylphosphonic acid 有权
公开(公告)号：US06218570B1
公开(公告)日：2001-04-17
申请号：US09556341
申请日：2000-04-24
申请人： Thaddeus S. Franczyk, II
发明人： Thaddeus S. Franczyk, II
IPC分类号： C07F938
CPC分类号： C07F9/3891 , C07F9/3813 , C07F9/3817
摘要： An improved process for the manufacture of formylphosphonic acid derivatives is reported. An aminomethylphosphonic acid substrate is contacted with a reagent selected from the group consisting of water, an alcohol, a phenol compound, and mixtures thereof and an oxidizing gas in the presence of a catalyst to form a reaction product mixture containing a formylphosphonic acid derivative and the conditions under which said contacting is carried out are controlled so that no more than 50% of the formylphosphonic acid derivative formed in the reaction product mixture is consumed by reaction with the reagent.

8. 发明授权

US06794536B1 Method for preparation of disodium pamidronate 有权
标题翻译：帕米膦酸二钠的制备方法
公开(公告)号：US06794536B1
公开(公告)日：2004-09-21
申请号：US09456460
申请日：1999-12-08
申请人： Edward C. Shinal
发明人： Edward C. Shinal
IPC分类号： C07F938
CPC分类号： A61K47/26 , A61K9/19 , C07F9/3873
摘要： The invention provides a method of preparing anhydrous disodium pamidronate or an aqueous disodium pamidronate solution for pharmaceutical use.
摘要翻译：本发明提供制备无水二氨基磷酸二钠或药物用帕米膦酸二钠水溶液的方法。

9. 发明授权

US06528627B1 Bridged aromatic substituted amine ligands with donor atoms 失效
公开(公告)号：US06528627B1
公开(公告)日：2003-03-04
申请号：US09724834
申请日：2000-11-28
申请人： Sudhakar Kasina
发明人： Sudhakar Kasina
IPC分类号： C07F938
CPC分类号： C07F13/005 , A61K51/04 , A61K51/0478 , A61K51/0482 , A61K51/0489 , A61K51/0497 , A61K51/087 , A61K51/088 , C07B2200/05 , C07C229/16 , C07C323/34 , C07D257/10 , C07D265/32 , C07D285/00 , C07D333/36 , C07D495/04 , C07D495/14 , C07F9/3817 , C07F9/6524 , C07F9/655345 , C07F9/6561
摘要： The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.

10. 发明授权

US06448434B1 Process for making ammonium glyphosate powder 有权
标题翻译：制备草甘膦铵粉的方法
公开(公告)号：US06448434B1
公开(公告)日：2002-09-10
申请号：US09624949
申请日：2000-07-25
申请人： Richard M. Kramer
发明人： Richard M. Kramer
IPC分类号： C07F938
CPC分类号： C07F9/3813 , A01N57/20 , A01N25/14 , A01N2300/00
摘要： A process is provided for preparing ammonium glyphosate powder suitable for downstream processing by extrusion to make a granular formulation comprising ammonium glyphosate and surfactant. The process comprises (a) mixing (i) solid particulate glyphosate acid, (ii) water in an amount of about 0.5 to about 3 parts by weight per part by weight of glyphosate acid, and (iii) a base that supplies ammonium cations, in an amount of about 0.8 to about 1.25 mole equivalents of ammonia per mole of glyphosate acid, to form an aqueous reaction medium; (b) allowing the glyphosate acid to react with the base in the reaction medium to form a reaction product comprising a concentrated aqueous solution of ammonium glyphosate; (c) drying the reaction product, for example with a drum dryer, to recover a particulate solid; and (d) accelerating the particulate solid in a turbulent high-velocity gas stream, for example in a jet mill, to form by particle-particle attrition an ammonium glyphosate powder having a mean particle size of about 5 to about 20 &mgr;m.
摘要翻译：提供了一种通过挤出制备适于下游加工的草甘膦铵粉末以制备包含草甘膦和表面活性剂的颗粒制剂的方法。该方法包括（i）混合（i）固体颗粒草甘膦酸，（ii）约0.5至约3重量份的量的草甘膦酸，和（iii）提供铵阳离子的碱，其量为每摩尔草甘膦酸约0.8至约1.25摩尔当量的氨，以形成水性反应介质; （b）使草甘膦酸与反应介质中的碱反应形成包含浓缩的草甘膦铵水溶液的反应产物; （c）干燥反应产物，例如用滚筒式干燥器回收颗粒状固体; 和（d）加速湍流高速气流中的颗粒状固体，例如在喷射式研磨机中，通过粒子颗粒磨损形成平均粒度约5至约20微米的草甘膦粉末。

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