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1. 发明申请

US20150177255A1 NOVEL FLUORESCENT DYES, LABELED CONJUGATES AND ANALYTICAL METHODS 审中-公开
标题翻译：新型荧光染料，标签结合物和分析方法
公开(公告)号：US20150177255A1
公开(公告)日：2015-06-25
申请号：US14573451
申请日：2014-12-17
申请人： Ramdas Pai
发明人： Ramdas Pai
IPC分类号： G01N33/58 , C07F9/576 , C07F9/653 , C07F9/6541
CPC分类号： G01N33/582 , C07F9/65324 , C07F9/6541 , C07F9/6561 , C09B69/007
摘要： There are described novel fluorescent dyes, conjugates which include a radical of a dye and a biological or a synthetic moiety and diagnostic and in vivo assays utilizing such conjugates and other products including the dyes and conjugates.
摘要翻译：描述了新颖的荧光染料，包括染料基团和生物学或合成部分的缀合物，以及使用这种共轭物和包括染料和缀合物的其它产物的诊断和体内测定。

2. 发明授权

US07772402B2 Optically detectable organophosphonates 失效
标题翻译：光学上可检测的有机膦酸盐
公开(公告)号：US07772402B2
公开(公告)日：2010-08-10
申请号：US12490217
申请日：2009-06-23
申请人： Albin Hermetter , Olga Oskolkova
发明人： Albin Hermetter , Olga Oskolkova
IPC分类号： C07F9/40
CPC分类号： C12Q1/44 , C07F9/4075 , C07F9/4084 , C07F9/65324
摘要： The invention relates to compounds having general formula I in which X represents an optically detectable moiety, n is an integer with 1≦n≦20, R1 is an unbranched or branched alkyl group having 1 to 20 carbon atoms, and R2 is hydrogen or —CH2—O—R3 group, wherein R3 has the same meaning as R1. These compounds are useful as inhibitors of lipolytic enzymes and can be used as tools for analysis as well as discrimination of lipolytic enzymes in biological samples.
摘要翻译：本发明涉及具有通式I的化合物，其中X表示可光学检测的部分，n为1和n1E的整数; n为1; 20，R 1为具有1至20个碳原子的无支链或支链烷基，R2为氢或 - CH2-O-R3基，其中R3具有与R1相同的含义。这些化合物可用作脂肪分解酶的抑制剂，可用作生物样品中分解酶和分解酶的工具。

3. 发明申请

US20100168198A1 Mitochondria-targeted antioxidant prodrugs and methods of use 失效
标题翻译：线粒体靶向抗氧化剂前药及其使用方法
公开(公告)号：US20100168198A1
公开(公告)日：2010-07-01
申请号：US12694337
申请日：2010-01-27
申请人： Marion W. Anders , James L. Robotham , Shey-Shing Sheu , Paul Spencer Brookes , Jalil Shojaie , Leif Olson , Richard L. Parton
发明人： Marion W. Anders , James L. Robotham , Shey-Shing Sheu , Paul Spencer Brookes , Jalil Shojaie , Leif Olson , Richard L. Parton
IPC分类号： A61K31/4164 , C07C59/90 , C07C63/04 , C07D233/54 , C07C229/04 , C07C229/28 , C07F11/00 , C07D339/08 , A61K31/195 , A61K31/19 , A61K31/28 , A61K31/385 , A61K31/192 , A61P39/06
CPC分类号： C07D233/54 , A61K31/19 , A61K31/192 , A61K31/195 , A61K31/28 , A61K31/385 , A61K31/4164 , C07C323/52 , C07D233/84 , C07D271/12 , C07D311/72 , C07D339/06 , C07D339/08 , C07D471/04 , C07F9/65324
摘要： The present invention is a mitochondria-targeted antioxidant prodrug useful for the prevention or treatment of diseases or conditions associated with mitochondrial dysfunction resulting from changes in the mitochondrial redox environment. Antioxidant prodrugs of the invention are produced by modifying an antioxidant to a fatty acid so that the resulting prodrug is targeted to and activated by an enzyme of mitochondrial fatty acid beta-oxidation.
摘要翻译：本发明是线粒体靶向的抗氧化剂前药，其可用于预防或治疗由线粒体氧化还原环境的变化引起的线粒体功能障碍相关的疾病或病症。通过将抗氧化剂改性为脂肪酸来制备本发明的抗氧化剂前药，以使得到的前药被靶向并被线粒体脂肪酸β-氧化酶活化。

4. 发明授权

US07601845B2 Optically detectable organophosphonates 失效
标题翻译：光学上可检测的有机膦酸盐
公开(公告)号：US07601845B2
公开(公告)日：2009-10-13
申请号：US11228987
申请日：2005-09-16
申请人： Albin Hermetter , Olga Oskolkova
发明人： Albin Hermetter , Olga Oskolkova
IPC分类号： C07F9/40
CPC分类号： C12Q1/44 , C07F9/4075 , C07F9/4084 , C07F9/65324
摘要： The invention relates to compounds having general formula I in which X represents an optically detectable moiety, n is an integer with 1≦n≦20, R1 is an unbranched or branched alkyl group having 1 to 20 carbon atoms, and R2 is hydrogen or —CH2—O—R3 group, wherein R3 has the same meaning as R1. These compounds are useful as inhibitors of lipolytic enzymes and can be used as tools for analysis as well as discrimination of lipolytic enzymes in biological samples.
摘要翻译：本发明涉及具有通式I的化合物，其中X表示可光学检测的部分，n为1≤n≤20的整数，R 1为具有1至20个碳原子的无支链或支链烷基，R2为氢或-CH 2 -O-R 3基团，其中R 3具有与R 1相同的含义。这些化合物可用作脂肪分解酶的抑制剂，可用作生物样品中分解酶和分解酶的工具。

5. 发明授权

US5891714A Cationic phospholipids for transfection 失效
标题翻译：用于转染的阳离子磷脂
公开(公告)号：US5891714A
公开(公告)日：1999-04-06
申请号：US470923
申请日：1995-06-06
申请人： Gary W. Ashley , Robert C. MacDonald , Miho Shida
发明人： Gary W. Ashley , Robert C. MacDonald , Miho Shida
IPC分类号： C12P9/00 , A61K9/127 , C07F9/09 , C07F9/10 , C07F9/113 , C07F9/653 , C12N15/88 , C12N15/63
CPC分类号： C12N15/88 , A61K9/1272 , B82Y5/00 , C07F9/10 , C07F9/113 , C07F9/65324
摘要： Cationic phospholipids and their use in treating pathogen-associated disease are disclosed. The class of phospholipids comprises the phosphotriester derivatives of phosphoglycerides and sphingolipids. Liposomes comprising one or more of the cationic phospholipids are effective in the lipofection of nuclidic acids and are therefore useful in methods of treating disease.
摘要翻译：公开了阳离子磷脂及其在治疗病原体相关疾病中的用途。磷脂类包括磷酸甘油酯和鞘脂的磷酸三酯衍生物。包含一种或多种阳离子磷脂的脂质体在核苷酸的脂质转染中是有效的，因此可用于治疗疾病的方法。

6. 发明授权

US5563128A Phosphonate derivatives of lipophilic amines 失效
公开(公告)号：US5563128A
公开(公告)日：1996-10-08
申请号：US435020
申请日：1995-05-04
申请人： Henry W. Pauls , Yong-Mi Choi , Dilip V. Amin
发明人： Henry W. Pauls , Yong-Mi Choi , Dilip V. Amin
IPC分类号： C07F9/38 , C07F9/40 , C07F9/653 , C07F9/6558 , A61K31/675 , A61K31/66
CPC分类号： C07F9/65583 , C07F9/3808 , C07F9/3873 , C07F9/4006 , C07F9/404 , C07F9/405 , C07F9/65324
摘要： This invention relates to a class of novel phosphonate derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis aryl cycloalkylamino and azacycloalkyl phosphonates. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.

7. 发明授权

US5254691A Phosphorylating agent and method for forming phosphodiester bond using the same 失效
标题翻译：磷酸酯和使用其形成磷酸二酯键的方法
公开(公告)号：US5254691A
公开(公告)日：1993-10-19
申请号：US20436
申请日：1993-02-22
申请人： Hideto Mori
发明人： Hideto Mori
IPC分类号： C07F9/09 , C07F9/6518 , C07F9/6524 , C07F9/653 , C07F9/28
CPC分类号： C07F9/6524 , C07F9/09 , C07F9/65181 , C07F9/65183 , C07F9/65188 , C07F9/653 , C07F9/65324 , Y02P20/55
摘要： A phosphorylating agent represented by the following general formula [1]: ##STR1## wherein R represents a protective group of the phosphoric acid; and X represents a heterocyclic residue represented by the following general formula [2]: ##STR2## wherein Y represents a single bond or an oxygen or sulfur atom; Z represents a heterocyclic nucleus comprising at least one nitrogen atom as a ring-forming element and may be condensed with another aromatic ring; and W represents one or more substituents other than a hydrogen atom. The phosphorylating agent is stable, can rapidly proceed phosphodiester bond-forming reactions in good selectivity under mild conditions and thus makes it possible to perform a reaction even in a relatively large scale.
摘要翻译：由以下通式[1]表示的磷酸化剂：其中R表示磷酸的保护基; X表示由以下通式[2]表示的杂环残基：其中Y表示单键或氧或硫原子; Z表示包含至少一个氮原子作为成环元素的杂环核，并可与另一个芳环稠合; W表示氢原子以外的一个以上的取代基。磷酸化剂稳定，可以在温和条件下以良好的选择性快速进行磷酸二酯键形成反应，从而使得即使以较大规模进行反应也是可能的。

8. 发明授权

US5185251A Microbial transformation of a substituted pyridinone using actinoplanacete sp. MA 6559 失效
标题翻译：使用actinoplanacete sp。取代的吡啶酮的微生物转化 MA 6559
公开(公告)号：US5185251A
公开(公告)日：1993-02-09
申请号：US711784
申请日：1991-06-07
申请人： Shieh-Shung T. Chen , George Doss
发明人： Shieh-Shung T. Chen , George Doss
IPC分类号： C07D413/06 , C07F9/653 , C12P17/16
CPC分类号： C07D413/06 , C07F9/65324 , C12P17/16 , Y10S435/822
摘要： Fermentation of the microorganism Actinoplanacete sp. (MA6559), ATTC No. 53771, in the presence of the HIV reverse transcriptase inhibitor ##STR1## yields 3-[2-(benzoxazol-2-yl)ethyl]-5-(1-hydroxyethyl)-6-methyl-2(1H)-pyridinone and 3-[2-(benzoxazol-2-yl)ethyl]-5-ethyl-6-hydroxymethyl-2(1H)-pyridinone, both of which are useful in the prevention or treatment of infection by HIV and the treatment of AIDS.
摘要翻译：发酵微生物Actinoplanacete sp。（MA6559），ATTC 53771，在HIV逆转录酶抑制剂“IMAGE”的存在下，得到3- [2-（苯并恶唑-2-基）乙基] -5-（1-羟乙基）-6-甲基-2 （1H） - 吡啶酮和3- [2-（苯并恶唑-2-基）乙基] -5-乙基-6-羟甲基-2（1H） - 吡啶酮，它们都可用于预防或治疗HIV感染和艾滋病的治疗。

9. 发明授权

US4790868A Herbicidally active substituted phenoxy or phenylthio benzoxazolone (or benzthiazolone) compounds 失效
标题翻译：除草活性取代的苯氧基或苯硫基苯并恶唑酮（或苯并噻唑酮）化合物
公开(公告)号：US4790868A
公开(公告)日：1988-12-13
申请号：US4746
申请日：1987-01-07
申请人： Donald R. Nielsen
发明人： Donald R. Nielsen
IPC分类号： A01N43/74 , A01N47/04 , A01N47/38 , A01N57/24 , C07D263/58 , C07D277/68 , C07D413/12 , C07F9/653 , A01N43/76 , A01N43/40
CPC分类号： C07D263/58 , A01N43/74 , A01N47/04 , A01N47/38 , A01N57/24 , C07D277/68 , C07D413/12 , C07F9/65324
摘要： This invention relates to herbicidally active substituted benzoxazolone (or benzthiazolone) compounds and to the use of such compounds to control the growth of noxious plants, i.e., weeds.
摘要翻译：本发明涉及除草活性取代的苯并恶唑酮（或苯并噻唑酮）化合物以及这些化合物用于控制有害植物即杂草生长的用途。

10. 发明授权

US4777163A Diphosphonate derivatives, pharmaceutical compositions and methods of use for calcium disturbances 失效
标题翻译：二膦酸衍生物，药物组合物和钙紊乱的使用方法
公开(公告)号：US4777163A
公开(公告)日：1988-10-11
申请号：US77228
申请日：1987-07-24
申请人： Elmar Bosies , Rudi Gall
发明人： Elmar Bosies , Rudi Gall
IPC分类号： A61K31/66 , A61K31/675 , A61P3/00 , A61P3/14 , A61P43/00 , C07F9/38 , C07F9/6506 , C07F9/6518 , C07F9/653 , C07F9/6539 , C07F9/6541 , C07F9/6544 , C07F9/65
CPC分类号： C07F9/6539 , C07F9/65062 , C07F9/65181 , C07F9/65182 , C07F9/653 , C07F9/65324 , C07F9/6541
摘要： The present invention produces alkyldiphosphonic acid derivative of the general formula: ##STR1## wherein Het is a heteroaromatic five-membered ring containing to 3 heteroatoms which can be partly hydrogenated and optionally substituted one or more times by alkyl, alkoxy, phenyl, cyclohexyl, cyclohexylmethyl, halogen or amino, and two adjacent alkyl substituents can together also form a ring, Y is a hydrogen atom or a lower alkyl radical, X is a hydrogen atom, a hydroxyl group or an amino group optionally substituted by lower alkyl and R is a hydrogen atom or a lower alkyl radical, with the proviso that Het is not a pyrazole ring; as well as the pharmacologically acceptable salts thereof.The present invention also provides processes for the prepearation of these compounds and pharmaceutical compositions containing them useful for the treatment or prophylaxis of calcium metabolism disturbances or disease as for example osteoporosis, Bechterew's disease, bone metastases, urolithiasis, heterotropic ossifications, rheumatoid arthritis osteoarthritis or degenerative arthrosis.
摘要翻译：本发明产生以下通式的烷基二膦酸衍生物：其中Het是含有3个杂原子的杂芳族五元环，其可以被部分氢化并任选地被烷基，烷氧基，苯基，环己基，环己基甲基，卤素或氨基，两个相邻的烷基取代基可一起形成环，Y为氢原子或低级烷基，X为氢原子，羟基或任选被低级烷基取代的氨基， R是氢原子或低级烷基，条件是Het不是吡唑环; 以及其药理学上可接受的盐。本发明还提供了这些化合物的预切方法和含有它们的药物组合物的方法，所述方法可用于治疗或预防钙代谢紊乱或疾病，例如骨质疏松症，Bechterew氏病，骨转移，尿石症，异质性骨化，类风湿性关节炎骨关节炎或退行性关节。

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