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31. 发明授权

US07038047B2 Substituted 6-(2-methoxyphenyl) triazolopyrimides as fungicides 失效
标题翻译：取代的6-（2-甲氧基苯基）三唑并嘧啶作为杀真菌剂
公开(公告)号：US07038047B2
公开(公告)日：2006-05-02
申请号：US10483599
申请日：2002-07-08
申请人： Jordi Tormo i Blasco , Hubert Sauter , Bernd Müller , Markus Gewehr , Wassilios Grammenos , Thomas Grote , Andreas Gypser , Joachim Rheinheimer , Ingo Rose , Peter Schäfer , Frank Schieweck , Michael Rack , Eberhard Ammermann , Siegfried Strathmann , Gisela Lorenz , Reinhard Stierl
发明人： Jordi Tormo i Blasco , Hubert Sauter , Bernd Müller , Markus Gewehr , Wassilios Grammenos , Thomas Grote , Andreas Gypser , Joachim Rheinheimer , Ingo Rose , Peter Schäfer , Frank Schieweck , Michael Rack , Eberhard Ammermann , Siegfried Strathmann , Gisela Lorenz , Reinhard Stierl
IPC分类号： C07D487/04 , C07C69/612 , A01N43/90
CPC分类号： C07D487/04 , A01N43/90
摘要： Substituted 6-(2-methoxy-phenyl)-triazolopyrimidines of formula I in which R1 and R2 independently denote hydrogen or alkyl, alkenyl, alkynyl, or alkadienyl, haloalkyl, haloalkenyl, cycloalkyl, phenyl, naphthyl, or 5- or 6-membered heterocyclyl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or 5- or 6-membered heteroaryl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or where R1 and R2 radicals may be unsubstituted or substituted as defined in the description, or R1 and R2 together with the interjacent nitrogen atom represent a 5- or 6-membered heterocyclic ring, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, which may be substituted; L1, L2 independently denote hydrogen or halogen, provided that at least one from L1 or L2 is halogen; X is halogen, cyano, alkyl, alkoxy, haloalkoxy or alkenyloxy; processes for their preparation, compositions containing them and to their use for combating phytopathogenic fungi.
摘要翻译：其中R 1和R 2的取代的6-（2-甲氧基 - 苯基） - 三唑并嘧啶独立地表示氢或烷基，烯基，炔基或链二烯基，卤代烷基含有1-4个氮原子或一至三个氮原子和一个硫或氧原子的卤代烯基，环烷基，苯基，萘基或5-或6-元杂环基，或含有一至四个的5-或6-元杂芳基氮原子或一至三个氮原子和一个硫或氧原子，或其中R 1和R 2基团可以是未取代的或如说明书中定义的取代的，或R R 1和R 2与中间的氮原子一起表示含有1-4个氮原子或一至三个氮原子和一个硫原子的5-或6-元杂环或氧原子，其可以被取代; L 1，L 2，L 2独立地表示氢或卤素，条件是至少一个L 1或L 2，是卤素; X是卤素，氰基，烷基，烷氧基，卤代烷氧基或烯氧基; 其制备方法，含有它们的组合物及其用于对抗植物病原真菌的用途。

32. 发明授权

US07037914B2 Carboxylic acid derivative and a pharmaceutical composition containing the derivative as active ingredient 失效
公开(公告)号：US07037914B2
公开(公告)日：2006-05-02
申请号：US10251805
申请日：2002-09-23
申请人： Hisao Tajima , Yoshisuke Nakayama , Daikichi Fukushima
发明人： Hisao Tajima , Yoshisuke Nakayama , Daikichi Fukushima
IPC分类号： C07C69/612 , C07C69/614 , C07C69/618 , A61K31/216
CPC分类号： C07D213/30 , A61K31/00 , C07C59/66 , C07C59/68 , C07C59/72 , C07C323/52 , C07D213/65 , C07D263/32 , C07D263/34 , C07D263/48 , C07D277/24 , C07D317/54 , C07D413/04 , C07D413/10 , C07D417/04 , C07D417/10
摘要： A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) (wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diseases or syndrome X.

33. 发明申请

US20050159487A1 Cyclic amino acids and derivatives thereof useful as pharmaceutical agents 失效
标题翻译：用作药剂的环状氨基酸及其衍生物
公开(公告)号：US20050159487A1
公开(公告)日：2005-07-21
申请号：US11078961
申请日：2005-03-11
申请人： Justin Bryans , David Horwell , Andrew Thorpe , David Wustrow , Po-Wai Yuen
发明人： Justin Bryans , David Horwell , Andrew Thorpe , David Wustrow , Po-Wai Yuen
IPC分类号： A61P1/04 , A61K20060101 , A61K31/19 , A61K31/195 , A61K31/198 , A61K31/215 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P29/00 , C07C20060101 , C07C61/04 , C07C61/06 , C07C69/608 , C07C69/612 , C07C205/51 , C07C205/53 , C07C229/00 , C07C229/28 , C07C229/32 , C07C229/34 , C07D209/96 , C07D221/20 , C07D307/94 , C07D311/96
CPC分类号： C07D221/20 , C07C49/417 , C07C69/608 , C07C69/612 , C07C205/51 , C07C205/53 , C07C229/28 , C07C229/34 , C07C2601/04 , C07C2601/08 , C07C2602/50 , C07D209/96 , C07D307/94 , C07D311/96
摘要： The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.
摘要翻译：本发明是可用于治疗癫痫，微弱发作，神经变性疾病，抑郁症，焦虑症，恐慌症，疼痛，神经病理学障碍，胃肠道疾病如肠易激综合征（IBS）和炎症的新一系列环状氨基酸，特别是关节炎。包括含有本发明化合物的药物组合物以及制备化合物的方法和用于制备最终化合物的新中间体。

34. 发明申请

US20050124825A1 Novel malonic acid monomethyl derivatives and production process thereof 失效
标题翻译：新型丙二酸单甲基衍生物及其制备方法
公开(公告)号：US20050124825A1
公开(公告)日：2005-06-09
申请号：US10976966
申请日：2004-11-01
申请人： Satoru Nose , Kieko Sano , Takeshi Hamatani
发明人： Satoru Nose , Kieko Sano , Takeshi Hamatani
IPC分类号： C07C69/612 , C07C67/30 , C07C67/313 , C07C67/343 , C07C69/65 , C07C69/76
CPC分类号： C07C69/65 , C07C67/30 , C07C67/343
摘要： A novel monomethyl malonate derivative is represented by following Formula (I): wherein X is a halogen atom; and Me is methyl group. This compound can be prepared by the steps of (A) reacting a benzyl halide derivative represented by following Formula (II): wherein X and Y may be the same as or different from each other and are each a halogen atom, with dimethyl malonate in the presence of a base to yield a dimethyl malonate derivative represented by following Formula (III): wherein X and Me have the same meanings as defined above; and (B) hydrolyzing the dimethyl malonate derivative of Formula (III). The compound is useful in the production of an indanonecarboxylic acid ester having a halogen atom on the indanone ring.
摘要翻译：新型单甲基丙二酸酯衍生物由下式（I）表示：其中X为卤素原子; 而我是甲基。该化合物可以通过以下步骤制备：（A）使由下式（II）表示的苄基卤衍生物：其中X和Y可以彼此相同或不同，并且各自为卤素原子，与丙二酸二甲酯碱的存在得到由下式（III）表示的丙二酸二甲酯衍生物：其中X和Me具有与上述相同的含义; 和（B）水解式（III）的丙二酸二甲酯衍生物。该化合物可用于制备在茚酮环上具有卤素原子的茚满酮羧酸酯。

35. 发明授权

US6043389A Hydroxy and ether-containing oxyalkylene esters and uses thereof 失效
标题翻译：含羟基和醚的氧化烯酯及其用途
公开(公告)号：US6043389A
公开(公告)日：2000-03-28
申请号：US814224
申请日：1997-03-11
申请人： Abraham Nudelman , Ada Rephaeli
发明人： Abraham Nudelman , Ada Rephaeli
IPC分类号： C07D317/30 , A61K31/138 , A61K31/166 , A61K31/17 , A61K31/22 , A61K31/282 , A61K31/341 , A61K31/357 , A61K31/765 , A61K38/00 , A61K39/395 , A61K45/00 , A61P1/00 , A61P3/10 , A61P7/00 , A61P17/00 , A61P17/02 , A61P35/00 , A61P37/00 , A61P43/00 , C07C69/28 , C07C69/54 , C07C69/606 , C07C69/675 , C07C69/708 , C07C69/734 , C07C69/96 , C07D307/54 , C07C69/612
CPC分类号： C07C69/708 , C07C69/96
摘要： This invention relates to compositions for and methods of treating, preventing or ameliorating cancer and other proliferative diseases as well as methods of inducing wound healing, treating cutaneous ulcers, treating gastrointestinal disorders, treating blood disorders such as anemias, immunomodulation, enhancing recombinant gene expression, treating insulin-dedendent patients, treating cystic fibrosis patients, inhibiting telomerase activity, treating virus-associated tumors, especially EBV-associated tumors, augmenting expression of tumor suppressor genes, inducing tolerance to antigens, or treating, preventing or ameliorating protozoan infection or inhibiting histone deacetylase in cells. The compositions of the invention are to and the methods of the invention use hydroxy and ether-containing oxyalkylene esters.
摘要翻译：本发明涉及治疗，预防或改善癌症和其它增殖性疾病的组合物和方法，以及诱导伤口愈合，治疗皮肤溃疡，治疗胃肠道疾病，治疗血液病症如贫血，免疫调节，增强重组基因表达的方法，治疗胰岛素衍生患者，治疗囊性纤维化患者，抑制端粒酶活性，治疗病毒相关肿瘤，特别是EBV相关肿瘤，增加肿瘤抑制基因的表达，诱导抗原耐受，或治疗，预防或改善原生动物感染或抑制组蛋白脱乙酰酶在细胞中。本发明的组合物是和本发明的方法使用羟基和醚的氧化烯酯。

36. 发明授权

US5716543A 3,4,5-trifluorobenzenes, and their use in liquid-crystal mixtures 失效
标题翻译： 3,4,5-三氟苯，以及它们在液晶混合物中的应用
公开(公告)号：US5716543A
公开(公告)日：1998-02-10
申请号：US624490
申请日：1996-04-04
申请人： Hubert Schlosser , Dietmar Jungbauer
发明人： Hubert Schlosser , Dietmar Jungbauer
IPC分类号： G02F1/13 , C07C43/225 , C07C69/612 , C07C69/73 , C07C69/76 , C07D239/26 , C07F7/12 , C09K19/30 , C09K19/42 , C09K19/34
CPC分类号： C09K19/42 , C07C43/225 , C07C69/76 , C09K19/3066 , C09K19/3068 , C07C2101/14
摘要： A 3,4,5-trifluorobenzene derivatives of formula (I): ##STR1## in which R.sup.1 is a straight-chain or branched alkyl having 1 to 15 carbon atoms in which one or two nonadjacent --CH.sub.2 --groups are optionally replaced by --O--, --CH.dbd.CH--, --C.tbd.C--, cyclopropane-1,2-diyl or --Si(CH.sub.3).sub.2 --, and in which one or more H atoms in the alkyl radical may be substituted by F; A.sup.1, A.sup.2 and A.sup.3 are identical or different 1,4-phenylene, pyridine-2,5-diyl, pyrimidine-2,5-diyl in which one or two H atoms are, optionally, replaced by F, trans-1,4-cyclohexylene, 1,3-dioxane-2,5-diyl or naphthalene-2,6-diyl, M.sup.1 and M.sup.2 are identical or different --CH.sub.2 CH.sub.2 --,--CH.dbd.CH--,--C.tbd.C--,--CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 --, --CH.sub.2 --O--,--O--CH.sub.2 --,--CO--O-- or--O--CO; X is --CH.sub.2 --O--,--OCH.sub.2 -- or --O--CO--; and k, l, m, n, o and p are zero or one provided that the sum k+m+o is greater than zero. The substances of the invention are characterized by a good temperature behavior of the nematic phase and good solubility.
摘要翻译： PCT No.PCT / EP94 / 03212 Sec。 371日期：1996年4月4日 102（e）日期1996年4月4日PCT 1994年9月26日PCT公布。 WO95 / 10498 PCT出版物日期：1995年04月20日一种式（I）的3,4,5-三氟苯衍生物：其中R 1是具有1至15个碳原子的直链或支链烷基，其中一个或两个不相邻 - CH 2 - 基团任选地被-O - ， - CH = CH - ， - C 3BOND C - ，环丙烷-1,2-二基或-Si（CH 3）2 - 取代，其中烷基中的一个或多个H原子基团可以被F取代; A1，A2和A3是相同或不同的1,4-亚苯基，吡啶-2,5-二基，嘧啶-2,5-二基，其中一个或两个H原子任选被F，反式-1,4 环己基，1,3-二恶烷-2,5-二基或萘-2,6-二基，M1和M2相同或不同，-CH2CH2 - ， - CH = CH - ， - C 3BOND C - ， - CH2CH2CH2CH2-， -CH 2 -O - ， - O-CH 2 - ， - CO-O-或-O-CO; X是-CH 2 -O - ， - OCH 2 - 或-O-CO-; 并且k，l，m，n，o和p分别为0或1，条件是和k + m + o大于零。本发明的物质的特征在于向列相的温度特性良好，溶解性好。

37. 发明授权

US5409954A .alpha.-arylacrylic acid derivatives, their preparation and their use for controlling pests and fungi 失效
标题翻译： α-芳基丙烯酸衍生物，它们的制备及其用于防治害虫和真菌的用途
公开(公告)号：US5409954A
公开(公告)日：1995-04-25
申请号：US142979
申请日：1993-10-29
申请人： Reinhard Kirstgen , Albrecht Harreus , Uwe Kardorff , Thomas Kuekenhoehner , Harald Rang , Gisela Lorenz , Eberhard Ammermann , Christoph Kuenast
发明人： Reinhard Kirstgen , Albrecht Harreus , Uwe Kardorff , Thomas Kuekenhoehner , Harald Rang , Gisela Lorenz , Eberhard Ammermann , Christoph Kuenast
IPC分类号： A01N37/36 , A01N37/38 , A01N43/10 , A01N43/40 , A01N43/50 , C07C69/734 , C07C69/736 , C07C205/56 , C07C255/54 , C07C255/57 , C07C323/20 , C07C323/62 , C07D213/55 , C07D233/60 , C07D237/08 , C07D237/16 , C07D239/54 , C07D241/12 , C07D241/24 , C07D249/00 , C07D249/06 , C07D261/08 , C07D277/20 , C07D277/30 , C07D307/54 , C07D333/24 , C07C69/612 , A01N37/10 , A01N37/34 , C07C69/618
CPC分类号： A01N43/40 , A01N37/36 , A01N37/38 , A01N43/10 , A01N43/50 , C07C69/734 , C07C69/736
摘要： .alpha.-arylacrylic acid derivatives of the general formula I ##STR1## where X is ethylene or ethenylene; Y is a direct bond or oxygen;R.sup.1 is a mononuclear or dinuclear aromatic system substituted by C.sub.1 -C.sub.4 -alkyl, their preparation, insecticides and fungicides containing them and methods for their use.
摘要翻译：通式I（I）的α-芳基丙烯酸衍生物，其中X是亚乙基或亚乙烯基; Y是直接键或氧; R1是被C1-C4烷基取代的单核或双核芳香体系，它们的制备方法，含有它们的杀虫剂和杀真菌剂及其使用方法。

38. 发明授权

US5364957A Carbonylation process using palladium phosphine catalyst 失效
标题翻译：使用钯膦催化剂的羰基化方法
公开(公告)号：US5364957A
公开(公告)日：1994-11-15
申请号：US45290
申请日：1993-04-08
申请人： Peter Arnoldy , Antoon P. M. Kremers
发明人： Peter Arnoldy , Antoon P. M. Kremers
IPC分类号： B01J27/14 , B01J31/02 , B01J31/04 , B01J31/12 , B01J31/24 , C07B61/00 , C07C67/38 , C07C69/533 , C07C69/54 , C07C69/612 , C07C69/618 , C07C67/36
CPC分类号： C07C67/38
摘要： The invention relates to a process for the carbonylation of an olefinically or acetylenically unsaturated hydrocarbon compound by reaction with carbon monoxide and a hydroxy compound in the presence of a catalyst system comprising a source of cationic palladium, a source of phosphine and a protonic acid, which reaction is carried out in the presence of a free radical inhibitor.
摘要翻译：本发明涉及一种通过与一氧化碳和羟基化合物在包含阳离子钯源，膦源和质子酸的催化剂体系的存在下反应来进行烯属或炔属不饱和烃化合物羰基化的方法，反应在自由基抑制剂存在下进行。

39. 发明授权

US5315025A Fungicides 失效
标题翻译：杀菌剂
公开(公告)号：US5315025A
公开(公告)日：1994-05-24
申请号：US677412
申请日：1991-03-29
申请人： Michael J. Bushell , Kevin Beautement , John M. Clough , Vivienne M. Anthony , Paul deFraine , Christopher R. Godfrey
发明人： Michael J. Bushell , Kevin Beautement , John M. Clough , Vivienne M. Anthony , Paul deFraine , Christopher R. Godfrey
IPC分类号： A01N37/06 , A01N37/10 , A01N37/18 , A01N37/34 , A01N37/36 , A01N37/38 , A01N37/40 , A01N37/42 , A01N37/44 , A01N37/46 , A01N37/48 , A01N37/50 , A01N41/10 , A01N43/00 , A01N43/06 , A01N43/08 , A01N43/12 , A01N43/30 , A01N43/34 , A01N43/40 , A01N43/54 , C07C49/76 , C07C57/00 , C07C57/42 , C07C67/00 , C07C67/31 , C07C67/343 , C07C69/00 , C07C69/612 , C07C69/618 , C07C69/73 , C07C69/734 , C07C69/736 , C07C69/738 , C07C69/76 , C07C69/773 , C07C69/84 , C07C201/00 , C07C205/53 , C07C205/55 , C07C205/56 , C07C205/59 , C07C227/00 , C07C227/16 , C07C229/40 , C07C229/44 , C07C231/00 , C07C231/12 , C07C233/64 , C07C235/42 , C07C235/46 , C07C237/20 , C07C237/30 , C07C241/00 , C07C245/08 , C07C255/57 , C07C313/00 , C07C315/04 , C07C317/44 , C07C317/46 , C07C323/56 , C07C323/62 , C07D213/64 , C07D213/643 , C07D221/00 , C07D291/00 , C07D307/54 , C07D307/68 , C07D333/24 , A01N37/12
CPC分类号： C07D213/643 , A01N37/36 , A01N37/38 , A01N37/42 , A01N37/44 , A01N37/46 , A01N37/48 , A01N41/10 , A01N43/08 , A01N43/12 , A01N43/40 , C07C205/56 , C07C255/00 , C07C317/44 , C07C323/56 , C07C323/62 , C07C69/734 , C07C69/736 , C07D307/54 , C07C2101/14 , C07C2103/26
摘要： This invention relates to derivatives of acrylic acid useful as fungicides, to processes for preparing them, to fungicidal compositions containing them, and to methods of combating fungi, especially fungal infections in plants, using them.
摘要翻译：本发明涉及可用作杀真菌剂的丙烯酸衍生物，其制备方法，含有它们的杀真菌组合物，以及使用它们来防治真菌，特别是真菌感染的方法。

40. 发明授权

US5274171A Process for the palladium catalyzed coupling of a diazonium salt with an olefinic bond 失效
标题翻译：钯催化偶联重氮盐与烯键的方法
公开(公告)号：US5274171A
公开(公告)日：1993-12-28
申请号：US823791
申请日：1992-01-22
申请人： Alan J. Chalk , Joseph A. Virgilio , Laszlo Wertheimer , Theresa B. Wertheimer
发明人： Alan J. Chalk , Joseph A. Virgilio , Laszlo Wertheimer , Theresa B. Wertheimer
IPC分类号： B01J31/12 , B01J31/22 , C07B61/00 , C07C51/347 , C07C51/353 , C07C51/367 , C07C59/64 , C07C67/343 , C07C69/54 , C07C69/612 , C07C69/65 , C07C69/734 , C07C69/738 , C07C69/76 , C07C201/12 , C07C205/56 , C07C231/12 , C07C233/11 , C07C233/65 , C07C235/34 , C07C253/30 , C07C255/57 , C07C303/22 , C07C309/20 , C07C309/58 , C07D307/91 , C07C57/42 , C07C57/44 , C07C69/618
CPC分类号： C07C303/22 , C07C51/347 , C07C51/367 , C07C69/734
摘要： A "one-pot" process for the palladium catalyzed coupling of a diazonium salt with an olefinic bond, in the aqueous medium in which the diazonium salt is made, by employing a carboxylic acid as a solvent. Arylacrylic acids and their esters, e.g. the cinnamates, can be produced at low catalyst concentration without first isolating the diazonium salt. The process is applied to the synthesis of 2-ethylhexyl p-methoxycinnamate.

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