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61. 发明申请

WO00069865A1 IMPROVED PROCESS FOR PHOSPHORYLATION AND COMPOUNDS PRODUCED BY THIS PROCESS 审中-公开
标题翻译：用于本方法生产的磷化合物和化合物的改进方法
公开(公告)号：WO00069865A1
公开(公告)日：2000-11-23
申请号：PCT/AU2000/000452
申请日：2000-05-12
IPC分类号： C07F9/09 , C07F9/11 , C07F9/117 , C07F9/12 , C07F9/655 , C07F9/6561 , C07J51/00
CPC分类号： C07J51/00 , C07F9/09 , C07F9/11 , C07F9/117 , C07F9/12 , C07F9/65522 , C07F9/65611 , Y02P20/582
摘要： A process for phosphorylating primary fatty alcohols, secondary alcohols, or aromatic alcohols comprising the following steps: (a) forming an intimate mixture of one or more of the above alcohols and P4O10 or partly hydrated P4O10 or a mixture thereof at a temperature below 80 DEG C; and (b) allowing the intimate mixture to continue to react for a period of time at a temperature below 80 DEG C until the formation of the dihydrogen form of the phosphorylated alcohol is substantially formed.
摘要翻译：一种用于磷酸化伯脂肪醇，仲醇或芳族醇的方法，包括以下步骤：（a）在低于80℃的温度下形成一种或多种上述醇和P4O10或部分水合的P4O10或其混合物的紧密混合物 C; 和（b）允许紧密混合物在低于80℃的温度下继续反应一段时间，直到形成磷酸化醇的二氢形式为止。

62. 发明申请

WO00050429A1 DRUGS CONTAINING PHOSPHORIC ACID DERIVATIVES AS THE ACTIVE INGREDIENT 审中-公开
标题翻译：含有作为活性成分的磷酸衍生物的药物
公开(公告)号：WO00050429A1
公开(公告)日：2000-08-31
申请号：PCT/JP2000/001005
申请日：2000-02-22
IPC分类号： A61P3/10 , A61P9/00 , A61P29/00 , A61P31/00 , A61P43/00 , C07F9/09 , C07F9/117 , C07F9/58 , C07F9/655 , C07F9/6553 , A61K31/66 , C07F9/165
CPC分类号： A61K31/662 , C07F9/091 , C07F9/094 , C07F9/117 , C07F9/582 , C07F9/65517 , C07F9/655345
摘要： Phosphoric acid derivatives represented by general formula (I), wherein each symbol is as defined in the description, and nontoxic salts thereof. Because of having a TNF alpha production inhibitory effect, the compounds represented by general formula (I) are useful as preventives and/or remedies for rheumatoid arthritis, ulcerative colitis, Crohn's disease, hepatitis, sepsis, hemorrhagic shock, multiple sclerosis, brain infarction, diabetes, interstitial pneumonia, uveitis, pain, glomerulonephritis, HIV-associated diseases, cachexia, myocardial infarction, chronic heart failure, oral aphtha, Hansen's disease, infection, etc.
摘要翻译：由通式（I）表示的磷酸衍生物及其无毒盐，其中每个符号如说明书中所定义。由于具有TNFα产生抑制作用，通式（I）表示的化合物可用作类风湿性关节炎，溃疡性结肠炎，克罗恩病，肝炎，败血症，出血性休克，多发性硬化，脑梗塞，糖尿病，间质性肺炎，葡萄膜炎，疼痛，肾小球性肾炎，HIV相关疾病，恶病质，心肌梗塞，慢性心力衰竭，口腔性幽门螺杆菌，汉森氏病，感染等。

63. 发明申请

WO00000584A2 IMMOBILIZED REAGENTS FOR KINASE ASSAYS 审中-公开
标题翻译：用于激酶测定的固定化试剂
公开(公告)号：WO00000584A2
公开(公告)日：2000-01-06
申请号：PCT/US1999/014566
申请日：1999-06-26
IPC分类号： C07F9/117 , C07F9/653 , C12Q1/48 , C12N
CPC分类号： C07F9/65312 , C07F9/117 , C12Q1/48
摘要： There is disclosed a composition represented by the formula PIPn-L-S-Matrix, wherein PIPn is a phosphoinositide polyphosphate, L is a linker moiety, S is a scintillant, and Matrix is a solid support. Preferred linker moieties include succinimide and poly(ethylene glycol) linkers, and a preferred scintillant is 2-(4-amino-methylphenyl)-5-(4-biphenyl)-1,3,4-oxadiazole. In a preferred embodiment, the Matrix is a microtitre plate. The composition can be used for assaying phosphatidylinositol kinases and for screening compounds for inhibition of phosphatidylinositol kinase activity. Methods of making and using the compound are also disclosed.
摘要翻译：公开了由式PIPn-L-S-Matrix表示的组合物，其中PIPn是磷酸肌醇多磷酸酯，L是连接体部分，S是闪烁体，Matrix是固体支持物。优选的接头部分包括琥珀酰亚胺和聚（乙二醇）接头，优选的闪烁体是2-（4-氨基 - 甲基苯基）-5-（4-联苯基）-1,3,4-恶二唑。在优选的实施方案中，Matrix是微量滴定板。该组合物可用于测定磷脂酰肌醇激酶和筛选用于抑制磷脂酰肌醇激酶活性的化合物。还公开了制备和使用该化合物的方法。

64. 发明申请

WO98055533A1 ZWITTERIONIC COMPOUNDS AND THEIR USE TO CROSS-LINK COLLAGENOUS MATERIALS 审中-公开
标题翻译：化学化合物及其用于交联胶原材料的用途
公开(公告)号：WO98055533A1
公开(公告)日：1998-12-10
申请号：PCT/GB1998/001646
申请日：1998-06-04
IPC分类号： A61L27/36 , C07F9/09 , C07F9/117 , C08H1/06 , A61L27/00
CPC分类号： C07F9/117 , A61L27/3687 , C07F9/091
摘要： Cross-linking of collagenous material may be achieved by treatment with compounds of the formula (I) Xm(R )(CHO)n, wherein R is an organic group having n+m functionality, X is a zwitterionic pendant group having an overall neutral charge, m is at least 1 and n is at least 2 (or a gem-diol, hemiacetal or acetal thereof). This results in the pendant amine groups of lysine residues present on the surface of the collagenous material to undergo a condensation reaction with the aldehyde groups present in formula (I) to form an imine linkage, thus fixing the biological moieties. The incorporation of the zwitterionic groups, suitably phosphoryl choline derivatives may have significant benefits in extending the life and reducing calcification of collagenous materials. One specific compound is 3-(oxyethyl-2'-(trimethylammoniumethyl)phosphate)-pentan-1,5-dial.
摘要翻译：胶原材料的交联可以通过用式（I）Xm（R 1）（CHO）n的化合物处理来实现，其中R 1是具有n + m官能团的有机基团，X是两性离子具有总体中性电荷的侧基，m为至少1，n为至少2（或偕二醇，半缩醛或缩醛）。这导致存在于胶原材料表面上的赖氨酸残基的侧胺基与式（I）中存在的醛基发生缩合反应，形成亚胺键，从而固定生物部分。合适的磷酸胆碱衍生物的两性离子基团的并入在延长生命和减少胶原材料的钙化方面可能具有显着的益处。一种具体的化合物是3-（氧乙基-2' - （三甲基铵乙基）磷酸酯） - 戊烷-1,5-表盘。

65. 发明申请

WO98045466A1 COMPOSITIONS AND SCREENING METHODS FOR NEUTROPHIL RESPONSES 审中-公开
标题翻译：中性反应的组成和筛选方法
公开(公告)号：WO98045466A1
公开(公告)日：1998-10-15
申请号：PCT/US1998/006786
申请日：1998-04-06
IPC分类号： C07F9/117 , C12Q1/34 , G01N33/50 , G01N33/68 , C12P9/00 , A61K31/66 , C07F9/02
CPC分类号： G01N33/68 , C07F9/117 , C12Q1/34 , G01N33/5047 , G01N2333/916
摘要： The present invention is directed to presqualene diphosphate (PSDP) analogs having an active region of natural PSDP and a metabolic transformation region resistant to rapid intracellular inactivation in vivo. For example, PSDP and its stable analogs can inhibit neutrophil signal transduction events in cellular activation that result in the generation of active oxygen species, regulation of leukocyte adherence, both homotypic (leukocyte-leukocyte) or heterotypic adherence with leukocytes and epithelial cells of mucosal origin or endothelial cells of vascular origin. These analogs can also be used to regulate leukocyte-dependent tissue injury.
摘要翻译：本发明涉及具有天然PSDP活性区和对体内快速细胞内失活具有抗性的代谢转化区的前体二磷酸（PSDP）类似物。例如，PSDP及其稳定的类似物可以抑制细胞活化中的中性粒细胞信号转导事件，导致活性氧的产生，白细胞粘附的调节，同型（白细胞 - 白细胞）或与粘液起源的白细胞和上皮细胞的异型粘附或血管来源的内皮细胞。这些类似物也可用于调节白细胞依赖性组织损伤。

66. 发明申请

WO2013121382A3 MEANS AND METHODS FOR ASSESSING BONE DISORDERS 审中-公开
标题翻译：用于评估骨质疏松症的手段和方法
公开(公告)号：WO2013121382A3
公开(公告)日：2016-09-01
申请号：PCT/IB2013051228
申请日：2013-02-15
申请人： BASF SE , BASF (CHINA) COMPANY LTD
发明人： WALK TILMANN B , RAVENZWAAY BENNARD VAN , MELLERT WERNER , FABIAN ERIC , STRAUSS VOLKER , KAMP HENNICKE , WIEMER JAN C , LOOSER RALF , HEROLD MICHAEL MANFRED , PROKOUDINE ALEXANDRE
IPC分类号： C07F9/117 , C07C53/126 , C07C69/30 , C07F9/10
CPC分类号： G01N33/6893 , G01N33/5044 , G01N33/6806 , G01N33/84 , G01N33/92 , G01N2570/00 , G01N2800/108
摘要： The present invention pertains to the field of diagnostics for bone disorders and toxicological assessments for risk stratification of chemical compounds. Specifically, it relates to a method for diagnosing a bone disorder, it also relates to a method for determining whether a compound is capable of inducing such a bone disorder in a subject and to a method of identifying a drug for treating a bone disorder. Furthermore, the present invention relates to a device and a kit for diagnosing a bone disorder.
摘要翻译：本发明涉及骨骼疾病的诊断领域和化学化合物的风险分层的毒理学评估。具体地，本发明涉及诊断骨骼疾病的方法，还涉及确定化合物是否能够诱导受试者中的这种骨病的方法以及鉴定用于治疗骨病的药物的方法。此外，本发明涉及用于诊断骨骼疾病的装置和试剂盒。

67. 发明申请

WO2015089686A1 从米糠中提取植酸钙的制备方法审中-公开
公开(公告)号：WO2015089686A1
公开(公告)日：2015-06-25
申请号：PCT/CN2013/001566
申请日：2013-12-16
申请人：刘登富
发明人：刘登富
IPC分类号： C07F9/117
CPC分类号： C07F9/117
摘要：本发明公开了一种从米糠中提取植酸钙的制备方法，将米糠粉碎，向其中加入浓度为5-20%的氢氧化钠溶液，浸泡10-30分钟进行脱脂，然后过滤，将滤渣用清水冲洗5-8遍后，加入硝酸钾混合均匀，再向滤渣中加入浓度为10-36%盐酸进行浸泡，并调整浸泡液PH值为2-5，向浸泡液中加入浓度为2-20%硝酸并搅拌均匀，浸泡时间为0.5-2小时，浸泡液温度为10-30°C，浸泡完成后过滤，去除滤渣，保留滤液，用氢氧化钙中和滤液至PH值为7-8，充分搅拌10-30分钟后过滤，用75-95%浓度的乙醇洗涤2-3次，然后用清水继续洗涤2-3次，干燥至重量不再有变化即可。本发明植酸钙提取率高，工艺简单，投资较少。

68. 发明申请

WO2014071072A2 NOVEL CATIONIC CAROTENOID-BASED LIPIDS FOR CELLULAR NUCLEIC ACID UPTAKE 审中-公开
标题翻译：新型阳离子类胡萝卜素脂质体介导的细胞核酸摄取
公开(公告)号：WO2014071072A2
公开(公告)日：2014-05-08
申请号：PCT/US2013/067869
申请日：2013-10-31
申请人： PUNGENTE, Michael D. , PARTALI, Vassilla , SLIWKA, Hans-Richard , OPSTAD, Christer L. , LEOPOLD, Phillip L. , LOU, Howard H. , BILCHUK, Natalia , JUBELL, Emile
发明人： PUNGENTE, Michael D. , PARTALI, Vassilla , SLIWKA, Hans-Richard , OPSTAD, Christer L. , LEOPOLD, Phillip L. , LOU, Howard H. , BILCHUK, Natalia , JUBELL, Emile
IPC分类号： C07F9/117
CPC分类号： C07F9/106 , C07F9/11
摘要： The synthesis and self-assembling properties of a model compound in a new class of cationic phospholipids with a highly unsaturated conjugated carotenoid fatty acid are described. In addition, the potential of this new lipid as a nucleic acid carrier was evaluated through lipoplex formulations employing 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) as helper lipid with and without the polycationic peptide, protamine, together with a plasmid DNA (pDNA). Lipoplexes composed of this novel unsaturated lipid exhibited pDNA binding and protection from DNase I degradation when formulated with protamine. Cellular uptake of the liposomes could be monitored by the visible color of the carotenoid moieties. The new cationic lipid gene delivery vector revealed comparable transfection efficiency to the commercial lipid, 1,2-dimyristoyl-sn-glycero-3-ethylphophocholine (EPC), in Chinese hamster ovary-K1 (CHO-K1) cells and performed equally to Lipofectamine 2000 when the formulation included protamine.
摘要翻译：描述了模型化合物在具有高度不饱和的共轭类胡萝卜素脂肪酸的新一类阳离子磷脂中的合成和自组装特性。此外，通过使用1,2-二油酰-sn-甘油基-3-磷酸乙醇胺（DOPE）作为辅助脂质的脂质复合物制剂评估了这种新脂质作为核酸载体的潜力，所述脂质具有和不具有聚阳离子肽鱼精蛋白，质粒DNA（pDNA）。当用鱼精蛋白配制时，由这种新颖的不饱和脂质组成的脂质体复合物显示pDNA结合和保护免受DNA酶I降解。可以通过类胡萝卜素部分的可见颜色来监测脂质体的细胞摄取。新型阳离子脂质基因递送载体在中国仓鼠卵巢-K1（CHO-K1）细胞中显示出与商业脂质1,2-二肉豆蔻酰-sn-甘油-3-乙基磷酰胆碱（EPC）相当的转染效率，并且对Lipofectamine 2000年，当时的配方包括鱼精蛋白。

69. 发明申请

WO2011064559A3 NOVEL INOSITOL PHOSPHATE DERIVATIVES 审中-公开
标题翻译：新型磷酸肌醇酯衍生物
公开(公告)号：WO2011064559A3
公开(公告)日：2011-09-09
申请号：PCT/GB2010002200
申请日：2010-11-30
申请人： QUEEN MARY & WESTFIELD COLLEGE , UNIV BATH , FALASCA MARCO , RILEY ANDREW MICHAEL , GODAGE HIMALI YASMIN , POTTER BARRY VICTOR LLOYD
发明人： FALASCA MARCO , RILEY ANDREW MICHAEL , GODAGE HIMALI YASMIN , POTTER BARRY VICTOR LLOYD
IPC分类号： A61K31/661 , A61P35/00 , C07F9/117
CPC分类号： C07F9/117 , A61K31/661 , C07F9/65522 , A61K2300/00
摘要： The present invention relates to compounds of the formula (I) wherein R1,R2, R3, R4, R5 and R6, X and n are as defined herein. Preferred compounds are inositol phosphate derivatives wherein R1 is a substituted or unsubstituted phenyl and at least one of R2, R3, R4, R5 and R6 is PO3 2- Alternative compounds are inositol phosphate derivatives of the formula (I) wherein R1 is a fiuorophore moiety The compounds are useful alone or in combination with known therapeutic agents for the treatment of diseases, especially cancer.
摘要翻译：本发明涉及式（I）的化合物，其中R 1，R 2，R 3，R 4，R 5和R 6，X和n如本文所定义。优选的化合物是肌醇磷酸酯衍生物，其中R 1是取代或未取代的苯基并且R 2，R 3，R 4，R 5和R 6中的至少一个是PO 3 2-。可选化合物是式（I）的肌醇磷酸酯衍生物，其中R 1是荧光团部分这些化合物可单独使用或与已知治疗剂联合用于治疗疾病，特别是癌症。

70. 发明申请

WO2009061393A1 PROBE FOR MEASURING PHYTASE ACTIVITY 审中-公开
标题翻译：用于测量植物活性的探针
公开(公告)号：WO2009061393A1
公开(公告)日：2009-05-14
申请号：PCT/US2008/012452
申请日：2008-11-04
申请人： BERRY & ASSOCIATES, INC.
发明人： BERRY, David, A.
IPC分类号： C07F9/117 , C12Q1/42
CPC分类号： C07F9/117 , C12Q1/42 , Y02P20/55
摘要： A myo-inositol derivative: R 1 , R 2 , R 3 and R 4 are identical, being selected from PO 3 H 2 , PO 3 Na 2 , PO 3 K 2 , PO 3 Li 2 , PO 3 Ca, PO 3 Mg, PO 3 (NH 4 )., PO 3 (RNH 3 ) 2 , PO 3 (R 2 NH 2 ) 2 , PO 3 (R 4 N) 2 , PO(OR) 2 , H, COZ and BHPP, where R is benzyl or alkyl of 1 to 6 carbon atoms and Z is an alkyl or arylalky group providing a cleavable protecting group; R 5 is one of H, benzyl, 4-methoxybenzyl, COZ, PO 3 H 2 , PO 3 Na 2 , PO 3 K 2 , PO 3 Li 2 , PO3Ca, PO 3 Mg, PO 3 (NH 4 ) 2 , PO 3 (RNH 3 ) 2 , PO 3 (R 2 NH 2 ) 2 , PO 3 (R 4 N) 2 , PO(OR) 2 , and BHPP, where R is benzyl or alkyl of 1 to 6 carbon atoms and Z is an alkyl or arylalky group providing a cleavable protecting group; X is one of CH 2 , CH 2 CH 2 O, and CH 2 CH 2 CH 2 O; n is an integer from 1 to 8; L1 is a single bond or CH 2 ; L 2 is one of a single bond, CONH, CH 2 CONH, CH 2 CH 2 CONH, CH 2 CH 2 NHCO, CH 2 CH 2 NHCONH, CH 2 CH 2 NHCSNH, CH 2 CH 2 NHSO 2 , CH 2 CH 2 CH 2 NHCO, CH 2 CH 2 CH 2 NHCONH, CH 2 CH 2 CH 2 NHCSNH, CH 2 CH 2 CH 2 NHSO 2 ,NHCO, NHCONH, NHCSNH, OCONH, CH 2 , CH 2 CH 2 , CH 2 CH 2 O, CH 2 CH 2 S, CH 2 CH 2 NH, CH 2 CH 2 CH2, CH 2 CH 2 CH 2 O, CH 2 CH 2 CH 2 S, CH 2 CH 2 CH 2 NH, and NH-SO 2 ; and R 6 is a UV-visible chromophore, a UV- chromophore, a fluorescent moiety, or a radiolabeled moiety.
摘要翻译：肌醇衍生物：R1，R2，R3和R4相同，选自PO3H2，PO3Na2，PO3K2，PO3Li2，PO3Ca，PO3Mg，PO3（NH4），PO3（RNH3）2，PO3（R2NH2）2，PO3 （R4N）2，PO（OR）2，H，COZ和BHPP，其中R是苄基或1-6个碳原子的烷基，Z是提供可切割保护基的烷基或芳基烷基; R5是H，苄基，4-甲氧基苄基，COZ，PO3H2，PO3Na2，PO3K2，PO3Li2，PO3Ca，PO3Mg，PO3（NH4）2，PO3（RNH3）2，PO3（R2NH2）2，PO3（R4N） PO（OR）2和BHPP，其中R是苄基或1-6个碳原子的烷基，Z是提供可切割保护基团的烷基或芳基烷基; X是CH 2，CH 2 CH 2 O和CH 2 CH 2 CH 2 O之一; n是1至8的整数; L1是单键或CH2; L2是单键，CONH，CH2CONH，CH2CH2CONH，CH2CH2NHCO，CH2CH2NHCONH，CH2CH2NHCSNH，CH2CH2NHSO2，CH2CH2CH2NHCO，CH2CH2CH2NHCONH，CH2CH2CH2NHCSNH，CH2CH2CH2NHSO2，NHCO，NHCONH，NHCSNH，OCONH，CH2，CH2CH2，CH2CH2O，CH2CH2S，CH2CH2NH，CH2CH2CH2， CH2CH2CH2O，CH2CH2CH2S，CH2CH2CH2NH和NH-SO2; 并且R 6是UV-可见发色团，UV-发色团，荧光部分或放射性标记的部分。

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