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71. 发明公开

EP2134699A1 2-ARYL-5-HETEROCYCLYL-CYCLOHEXANE-1,3-DIONE COMPOUNDS AND THEIR USE AS HERBICIDES 有权
标题翻译： 2-芳基-5- HETEROCYCLYLCYCLOHEXAN -1,3-二酮化合物及其作为除草剂
公开(公告)号：EP2134699A1
公开(公告)日：2009-12-23
申请号：EP08716354.9
申请日：2008-03-07
申请人： Syngenta Participations AG , Syngenta Limited
发明人： Mathews, Christopher, John , Finney, John , Robinson, Louisa , Tyte, Melloney , Muehlebach, Michel , Wenger, Jean
IPC分类号： C07D309/06 , A01N43/16 , C07D305/06 , C07D307/12 , C07D309/22 , C07D313/04 , C07D333/16 , C07D333/48 , C07D335/02 , C07D405/10 , C07D409/10 , A01N43/08 , A01N43/10 , A01N43/18 , A01N43/22
CPC分类号： C07D309/06 , C07D305/06 , C07D307/12 , C07D309/22 , C07D313/04 , C07D333/16 , C07D333/48 , C07D335/02 , C07D405/10 , C07D409/10
摘要： Cyclohexanedione compounds of Formula (I) wherein R1 is methyl, ethyl, n-propyl, iso-propyl, cyclopropyl, halomethyl, haloethyl, halogen, vinyl, ethynyl, methoxy, ethoxy, halomethoxy or haloethoxy, R2 and R3 are, independently hydrogen, halogen, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, C2-C6alkenyl, C2-C6haloalkenyl, C2-C6alkynyl, C3-C6alkenyloxy, C3-C6haloalkenyloxy, C3-C6alkynyloxy, C3-C6cycloalkyl, C1-C6alkylthio, C1-C6alkylsulfinyl, C1-C6alkylsulfonyl, C1-C6alkylsulfonyloxy, C1-C6haloalkylsulfonyloxy, cyano, nitro, phenyl, phenyl substituted by C1-C4alkyl, C1-C3Cahaloalkyl, C1-C3alkoxy, C1-C3haloalkoxy, cyano, nitro, halogen, C1-C3alkylthio, C1-C3alkylsulfιnyl or C1-C3alkylsulfonyl, or heteroaryl or heteroaryl substituted by C1-C3Calkyl, d.Cahaloalkyl, C1-C3aIkoxy, C1-C3haloalkoxy, cyano, nitro, halogen, C1-C3alkylthio, C1-C3alkylsulfinyl or C1-C3alkylsulfonyl, R4 is hydrogen, methyl, ethyl, n-propyl, iso-propyl, halomethyl, haloethyl, halogen, vinyl, ethynyl, methoxy, ethoxy, halomethoxy or haloethoxy, X is O, S, S(O) or S(O)2, R5 is hydrogen or methyl, R6 is hydrogen, methyl or ethyl, or forms a double bond, which links the carbon atom, to which R6 is attached, with the adjacent carbon atom of R7 or R8, R7 and R8 are independently of each other C1-C5alkylene, which is unsubstituted or substituted by methyl or ethyl, or C2-C5alkenylene, which is unsubstituted or substituted by methyl or ethyl, and G is hydrogen, an alkali metal, alkaline earth metal, sulfoniυm, ammonium or a latentiating group, are suitable for use as herbicides.

72. 发明公开

EP2079467A2 ANTIDIABETIC BICYCLIC COMPOUNDS 有权转让
标题翻译：抗糖尿病双环化合物
公开(公告)号：EP2079467A2
公开(公告)日：2009-07-22
申请号：EP07839789.0
申请日：2007-10-26
申请人： Merck & Co., Inc.
发明人： GE, Min , LIN, Songnian , WALSH, Shawn P. , YANG, Lihu , ZHOU, Changyou
IPC分类号： A61K31/426 , A61K31/421 , C07D339/02 , C07D277/14
CPC分类号： C07D333/60 , C07C59/72 , C07C59/90 , C07C235/46 , C07C255/54 , C07C2602/08 , C07C2602/10 , C07D207/34 , C07D209/34 , C07D209/46 , C07D213/61 , C07D215/233 , C07D217/24 , C07D307/80 , C07D311/58 , C07D333/48 , C07D405/12 , C07D487/04
摘要： Diaryl ethers in which one of the aryl groups is a phenyl fused to a cycloalkyl or heterocyclic ring, to which is attached an acetic acid group, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that often accompany this disease, including insulin resistance, obesity and lipid disorders.
摘要翻译：其中一个芳基为与环烷基或杂环稠合的苯基的二芳基醚是G蛋白偶联受体40（GPR40）的激动剂，并且可用作治疗化合物，特别是 2型糖尿病的治疗以及常伴有这种疾病的病症，包括胰岛素抵抗，肥胖和脂质紊乱。

73. 发明公开

EP2003116A2 PROCESS FOR THE PRODUCTION OF ORGANIC OXIDES 审中-公开
标题翻译： HERSTELLUNGSVERFAHRENFÜR有机硅氧化物
公开(公告)号：EP2003116A2
公开(公告)日：2008-12-17
申请号：EP07741451.4
申请日：2007-04-05
申请人： Takeda Pharmaceutical Company Limited
发明人： IKEMOTO, Tomomi , FUKUDA, Naohiro
IPC分类号： C07C315/02 , C07C317/04 , C07C317/14 , C07C317/22 , C07D213/70 , C07D213/71 , C07D213/84 , C07D277/76 , C07D333/48 , C07B33/00
CPC分类号： C07C315/02 , C07D213/70 , C07D213/71 , C07D213/84 , C07D277/76 , C07D333/48
摘要： The present invention provides a method for producing an organic oxide, wherein a substrate is oxidized using hypohalous acid, hypohalous acid salt, chlorine, bromine or iodine in the presence of water and a catalytic amount of a compound represented by the following formula (I): R 1 -X 1 -NY-R 2 , wherein: X 1 represents -CO- or -SO 2 -; Y represents a hydrogen atom, a potassium atom, a sodium atom, a chlorine atom, a bromine atom or an iodine atom; R 1 represents a substituted or unsubstituted hydrocarbon group, -NYR 3 group or -OR 3 group (in the formulae, R 3 represents a substituted or unsubstituted hydrocarbon group, and Y represents the same meaning as defined above); and R 2 represents a hydrogen atom or -CO-R 4 group (in the formula, R 4 represents a substituted or unsubstituted hydrocarbon group, -NYR 5 group or -OR 5 group (in the formulae, R 5 represents a substituted or unsubstituted hydrocarbon group, and Y represents the same meaning as defined above)); or R 1 and R 4 may bind to each other to form a further substituted or unsubstituted nitrogen-containing heterocyclic ring.
摘要翻译：本发明提供一种有机氧化物的制造方法，其中在水和催化量的下式（I）表示的化合物的存在下，使用次卤酸，次卤酸盐，氯，溴或碘氧化底物，：R 1 -X 1 -NY-R 2，其中：X 1表示-CO-或-SO 2 - ; Y表示氢原子，钾原子，钠原子，氯原子，溴原子或碘原子; R 1表示取代或未取代的烃基，-NYR 3基或-OR 3基（式中，R 3表示取代或未取代的烃基，Y表示与上述相同的含义）。 R 2表示氢原子或-CO-R 4基团（式中，R 4表示取代或未取代的烃基，-NYR 5基或-OR 5基）（式中，R 5表示取代或未取代的烃基，Y表示与上述相同的含义））; 或R 1和R 4可以彼此结合形成另外的取代或未取代的含氮杂环。

74. 发明公开

EP1705177A1 N-aryl-sulfoximine-substituted pyrimidines as CDK- and/or VEGF inhibitors, their production and use as pharmaceutical agents 审中-公开
标题翻译： N-芳基取代的嘧啶作为亚磺酰亚胺和CDK的VEGF抑制剂，它们的制备和作为药物的用途
公开(公告)号：EP1705177A1
公开(公告)日：2006-09-27
申请号：EP05090073.7
申请日：2005-03-23
申请人： Schering Aktiengesellschaft
发明人： Lücking, Ulrich, Dr. , Siemeister, Gerhard , Jautelat, Rolf
IPC分类号： C07D239/48 , C07D239/47 , A61K31/505 , A61P35/00 , C07C381/10
CPC分类号： C07D239/48 , C07D239/47 , C07D239/50 , C07D333/48 , C07D401/12 , C07D405/12 , C07D409/12
摘要： This invention relates to pyrimidine derivatives of general formula (I)

in which Q, R1, R2, R3, R4, R5, X, and m have the meanings that are contained in the description, as inhibitors of cyclin-dependent kinases and VEGF-receptor tyrosine kinases, their production as well as their use as medications for treatment of various diseases.
摘要翻译：本发明涉及其中Q，R1，R2，R3，R4，R5，X和m的通式（I）的嘧啶衍生物的含义也被包含在本说明书中，如细胞周期蛋白依赖性激酶和VEGF的抑制剂受体酪氨酸激酶，它们的制备，以及它们作为药物使用用于治疗各种疾病。

75. 发明公开

EP1551797A1 CYCLOHEXYL SULPHONE DERIVATIVES AS GAMMA-SECRETASE INHIBITORS 有权
标题翻译：环糊精衍生物ALS GAMMA-SECRETASE-INHIBITOREN
公开(公告)号：EP1551797A1
公开(公告)日：2005-07-13
申请号：EP03748306.2
申请日：2003-09-25
申请人： MERCK SHARP & DOHME LTD.
发明人： CHURCHER, Ian , HARRISON, Timothy , KERRAD, Sonia , OAKLEY, Paul Joseph , SHAW, Duncan Edward , TEALL, Martin Richard , WILLIAMS, Susannah
IPC分类号： C07C317/14 , C07C317/18 , C07C317/20 , C07C317/22 , C07C317/24 , C07C317/44 , C07C331/04 , C07D205/04 , C07D205/06 , C07D207/08 , C07D207/10 , C07D207/16 , C07D211/38 , C07D213/70 , C07D213/71 , C07D213/89 , C07D233/84 , C07D239/38 , C07D249/08 , C07D257/04 , C07D277/36
CPC分类号： C07D213/70 , C07C317/14 , C07C317/18 , C07C317/20 , C07C317/22 , C07C317/24 , C07C317/44 , C07C331/04 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D205/04 , C07D207/48 , C07D211/96 , C07D213/71 , C07D213/89 , C07D233/84 , C07D239/38 , C07D249/12 , C07D257/04 , C07D277/36 , C07D285/125 , C07D295/088 , C07D295/26 , C07D307/38 , C07D307/46 , C07D307/52 , C07D307/64 , C07D307/68 , C07D317/46 , C07D333/18 , C07D333/48 , C07D491/08
摘要： Compounds of formula (I) inhibit the processing of APP by gamma-secretase, and hence are useful in treatment of Alzheimer's disease.
摘要翻译：式I的化合物：其中Ar 1和Ar 2是任选取代的芳基或杂芳基，L是键，-CH-或 - （CHR“ S（O）R 1，S（O）R 1，S（O）R 1， 2 SO 2 SO 2 SO 2，SO 2 N（N， R 2，N 2，NH 2，NH 2，NH 2（R 2） 2 O 2，OSO 2 N（R 2）2，OS（ O）N（R 2）2，OSO 2，NHCOR 1，COR 4，，NHCOR 1，NHCO 2 R 1，NHCON（R 2）2，/ SUB >，NHSO 2 R 1，或NHSO 2 N（R 2）2，，通过γ分泌酶抑制APP的处理，因此可用于治疗阿尔茨海默氏病。

76. 发明公开

EP1366024A2 SULFOXIDE AND BIS-SULFOXIDE COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES 审中-公开
标题翻译：亚砜和BISULFOXIDE和胆固醇控制组合物和相关用来
公开(公告)号：EP1366024A2
公开(公告)日：2003-12-03
申请号：EP01979735.6
申请日：2001-10-11
申请人： Esperion Therapeutics Inc.
发明人： DASSEUX, Jean-Louis, H. , ONICIU, Carmen, Daniela
IPC分类号： C07C317/18 , A61K31/10 , A61P9/00 , C07C317/10 , C07C317/22 , C07C317/44 , C07D233/40 , C07D233/42 , C07D249/04 , C07D257/04 , C07D261/12 , C07D305/12 , C07D307/32 , C07D309/12 , C07D309/30 , C07D309/40 , C07D333/48 , C07D335/02 , C07D495/04 , C07F9/09 , C07F9/24
CPC分类号： C07F9/2408 , C07C59/347 , C07C317/04 , C07C317/14 , C07C317/18 , C07C317/24 , C07C317/44 , C07D233/76 , C07D233/86 , C07D257/04 , C07D261/12 , C07D305/12 , C07D307/32 , C07D307/33 , C07D309/12 , C07D309/30 , C07D309/38 , C07D333/48 , C07D335/02 , C07F9/091 , C07F9/094 , C07F9/4407
摘要： The present invention relates to sulfoxide and bis-sulfoxide compounds of formula I, formula II, or formula III (in which the variables are as defined in the claims), compositions comprising sulphoxide and bissulphoxide compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

77. 发明公开

EP1246889A1 PROCEDE DE DESULFURATION DES DERIVES DU THIOPHENE CONTENUS DANS DES CARBURANTS 有权
标题翻译：用于燃料中所含的噻吩脱硫的
公开(公告)号：EP1246889A1
公开(公告)日：2002-10-09
申请号：EP00993626.1
申请日：2000-12-28
申请人： ELF ANTAR FRANCE
发明人： RABION, Alain , FAJULA, François , BERNARD, Jean-René , HULEA, Vasile,Faculté de Chimie Industrielle
IPC分类号： C10G27/12 , C10G67/12 , C10G53/14
CPC分类号： C07D333/48 , C10G27/12 , C10G53/14 , C10G67/12
摘要： The invention concerns a method for selectively desulphurizing thiopene compounds contained in hydrocarbons derived from crude oil distillation, whether refined or not, which consists in oxidising the thiophene sulphur atoms into sulphone in the presence of an oxidising agent and in separating said sulphonated compounds from said hydrocarbons. The invention is characterised in that it consists in oxidising the thiophene compounds in a two-phase turbulent medium comprising a hydrocarbon phase and an aqueous phase, in the presence of at least an oxidising agent soluble in at least one of the two phases and of at least a metal catalyst in soluble or dispersed form in a liquid or in solid form, separation and oxidation occurring simultaneously.

78. 发明公开

EP1246625A2 METHODS AND COMPOSITIONS FOR MITIGATING PAIN USING NITRATE ESTERS 有权
标题翻译：用途和硝酸盐套酯ALS镇静剂
公开(公告)号：EP1246625A2
公开(公告)日：2002-10-09
申请号：EP00986925.6
申请日：2000-12-27
申请人： QUEEN'S UNIVERSITY AT KINGSTON
发明人： THATCHER, Gregory, R., J. , BENNETT, Brian, M. , REYNOLDS, James, N. , JHAMANDAS, Khem
IPC分类号： A61K31/662 , A61K31/426 , A61K31/40 , A61P29/00 , A61P25/20 , A61P25/22 , A61P23/00 , A61K31/21 , A61K31/24 , A61K31/265 , A61K31/425
CPC分类号： C07D207/337 , A61K31/00 , A61K31/04 , A61K31/21 , A61K31/275 , A61K31/381 , A61K31/385 , A61K31/39 , A61K31/426 , A61K31/5375 , C07C203/04 , C07C203/06 , C07C205/40 , C07C309/12 , C07C317/18 , C07C323/12 , C07C323/20 , C07C323/58 , C07C323/62 , C07C327/28 , C07C331/10 , C07D207/16 , C07D277/24 , C07D295/088 , C07D307/33 , C07D311/16 , C07D317/60 , C07D327/04 , C07D333/44 , C07D333/48 , C07D339/08 , C07D409/04 , C07D487/04 , C07D491/04 , C07F9/3808 , C07F9/4006 , C07J41/0055 , C07J41/0061
摘要： Methods and therapeutic compounds for treating pain, mitigating inflammation, effecting analgesia and/or effecting sedation in a subject are described. A subject is administered an effective amount of a therapeutic compound which is a nitrate ester. Novel pharmaceutical compositions are also described.

79. 发明公开

EP1232150A1 UREA DERIVATIVES AS ANTI-INFLAMMATORY AGENTS 有权
标题翻译： HARNSTOFF DERIVATE ALSENTZÜNDUNGSHEMMENDEMITTEL
公开(公告)号：EP1232150A1
公开(公告)日：2002-08-21
申请号：EP00978751.6
申请日：2000-11-16
申请人： BOEHRINGER INGELHEIM PHARMACEUTICALS INC.
发明人： BREITFELDER, Steffen , CIRILLO, Pier, F. , HAO, Ming-Hong , HICKEY, Eugene, R. , SHARMA, Rajiv , SUN, Sanxing , TAKAHASHI, Hidenori
IPC分类号： C07D295/08 , A61P29/00 , C07D213/73 , C07D295/12 , C07D213/63
CPC分类号： C07D207/404 , C07C275/34 , C07C323/44 , C07C2601/02 , C07D211/74 , C07D213/30 , C07D213/38 , C07D213/66 , C07D213/68 , C07D213/73 , C07D213/74 , C07D213/75 , C07D215/46 , C07D231/12 , C07D233/56 , C07D233/64 , C07D239/42 , C07D249/08 , C07D265/30 , C07D265/36 , C07D295/088 , C07D295/13 , C07D295/135 , C07D295/15 , C07D295/185 , C07D307/14 , C07D309/06 , C07D309/12 , C07D333/48 , C07D401/06 , C07D405/12 , C07D413/12 , C07D471/04
摘要： Disclosed are novel aromatic compounds of formula (I) wherein G, X, Ar, L and Q are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds. The compounds (I) inhibit cytokine production.
摘要翻译：公开了式（I）的新型芳族化合物，其中G，X，Ar，L和Q在本文中定义。该化合物可用于治疗涉及炎症的疾病或病理状况的药物组合物，例如慢性炎性疾病。还公开了制备这种化合物的方法

80. 发明授权

EP0629197B1 1-ALKOXY-(2-ALKOXY- OR CYCLOALKOXY)-4-(CYCLO THIOALKYL- OR CYCLOTHIOALKENYL)BENZENES AS INHIBITORS OF CYCLIC AMP PHOSPHODIESTERASE AND TUMOUR NECROSIS FACTOR 有权转让
标题翻译： 1-烷氧基-2-（烷氧基或环烷氧基）-4-（CYCLOTHIOALKYL- OR cyclothioalkenyl）苯环状AMP磷酸二酯酶抑制剂和肿瘤坏死因子
公开(公告)号：EP0629197B1
公开(公告)日：1997-08-20
申请号：EP93905503.4
申请日：1993-03-04
申请人： RHONE-POULENC RORER LIMITED
发明人： FENTON, Garry , MASON, Jonathan, Stephen , PALFREYMAN, Malcolm, Norman , RATCLIFFE, Andrew, James
IPC分类号： C07D335/02 , C07D333/16 , C07D333/32 , C07D333/48 , A61K31/38
CPC分类号： C07D333/48 , C07D333/16 , C07D333/32 , C07D335/02
摘要： This invention is directed to 1-alkoxy-2-(alkoxy- or cycloalkyloxy-)-4-(cyclothioalkyl- or cyclothioalkenyl-)benzene compounds that inhibit cyclic AMP phosphodiesterase or tumor necrosis factor (TNF) and are useful in treating patients suffering from disease state capable of being modulated by inhibiting production of cyclic AMP phosphodiesterase or TNF by administering the compound to the patient. The invention is also directed to the preparation of these compounds, pharmaceutical compositions containing these compounds and methods for their pharmaceutical use.

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