公开(公告)号：EP1392639A1

公开(公告)日：2004-03-03

申请号：EP02769325.8

申请日：2002-05-03

申请人： Galileo Laboratories, Inc.

发明人： WANG, Bing ,  MILLER, Guy ,  FLAIM, Stephen, F. ,  DEL BALZO, Ughetta ,  ZHANG, Wei ,  JANAGANI, Satyanarayana ,  SONG, Jingao

IPC分类号： C07C69/66 ,  C07C323/60 ,  C07D295/00 ,  A61K31/12 ,  A61K31/16 ,  A61K31/215 ,  A61K31/223 ,  A61P9/10

CPC分类号： C07D213/30 ,  A61K31/12 ,  A61K31/16 ,  A61K31/215 ,  A61K31/223 ,  A61K38/00 ,  C07C249/12 ,  C07C319/20 ,  C07C323/60 ,  C07D207/16 ,  C07D207/22 ,  C07D207/24 ,  C07D211/62 ,  C07D211/74 ,  C07D211/78 ,  C07D217/04 ,  C07D233/42 ,  C07D233/64 ,  C07D233/84 ,  C07D235/28 ,  C07D239/78 ,  C07D249/14 ,  C07D271/113 ,  C07D277/16 ,  C07D277/74 ,  C07D279/12 ,  C07D285/125 ,  C07D285/135 ,  C07D295/13 ,  C07D295/15 ,  C07D295/185 ,  C07D339/08 ,  C07D345/00 ,  C07D405/12 ,  C07D473/38 ,  C07K5/0215 ,  C07K5/0819 ,  C07C323/57 ,  C07C251/60

摘要： Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.

公开(公告)号：EP1377601A2

公开(公告)日：2004-01-07

申请号：EP02735453.9

申请日：2002-04-10

申请人： INSTITUT NATIONAL DE LA SANTE ETDE LA RECHERCHE MEDICALE (INSERM) ,  CENTRE NATIONAL DELA RECHERCHE SCIENTIFIQUE (CNRS)

发明人： ROQUES, Bernard ,  ANNE, Christine ,  TURCAUD, Serge ,  FOURNIE-ZALUSKI, Marie-Claude

IPC分类号： C07K5/023 ,  C07K5/065 ,  C07C323/60 ,  A61K31/16 ,  A61K38/05 ,  A61P25/00

CPC分类号： C07K5/0202 ,  A61K38/00 ,  C07C323/60 ,  C07K5/06078 ,  Y02A50/469

摘要： The invention relates to novel compounds of general formula (I), with inhibitory properties for the type B botulism toxin activity, the methods for preparation thereof and corresponding pharmaceutical compositions. The invention further relates to corresponding pharmaceutical compositions.

公开(公告)号：EP1371640A1

公开(公告)日：2003-12-17

申请号：EP02705321.4

申请日：2002-03-18

申请人： Senju Pharmaceutical Co., Ltd.

发明人： OGATA, Kazumi ,  SAKAUE, Takahiro ,  ITO, Kazuhiko

IPC分类号： C07C323/60 ,  A61K7/00 ,  A61K7/42 ,  A61K31/185 ,  A61K31/195 ,  A61K31/197 ,  A61K31/198 ,  A61P17/16 ,  A61P43/00

CPC分类号： A61K31/198 ,  A61K31/185 ,  A61K31/195 ,  A61K31/197 ,  C07C323/60

摘要： Provided are novel α-lipoic acid derivatives represented by the following formula (I), which have a tyrosinase inhibiting activity, a melanin production suppressing activity and an elastase inhibiting activity.
(In the formula, M denotes a metal, and A denotes an amino acid which is bound via N.)

摘要翻译： 提供具有酪氨酸酶抑制活性，黑色素产生抑制活性和弹性蛋白酶抑制活性的由下式（I）表示的新型α-硫辛酸衍生物。 （式中，M表示金属，A表示通过N结合的氨基酸。）

公开(公告)号：EP1169316B9

公开(公告)日：2003-10-29

申请号：EP00918930.9

申请日：2000-03-31

申请人： SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.)

发明人： HARNETT, Jeremiah ,  AUGUET, Michel ,  CHABRIER de LASSAUNIERE, Pierre-Etienne

IPC分类号： C07D339/04 ,  C07C323/60 ,  C07D409/12 ,  A61K31/385 ,  A61P25/28

CPC分类号： C07D409/12 ,  C07C323/60 ,  C07D339/04

公开(公告)号：EP1317427A1

公开(公告)日：2003-06-11

申请号：EP01980386.5

申请日：2001-09-14

申请人： Grünenthal GmbH

发明人： GERLACH, Matthias ,  PÜTZ, Claudia ,  ENDERS, D. ,  GAUBE, Gero

IPC分类号： C07C323/60 ,  A61K31/10 ,  A61P25/04

CPC分类号： C07C323/59 ,  C07B2200/07

摘要： The invention relates to a method for producing chiral compounds according to the condition of a 1.4 Michael reaction in addition to a compound of general formula (31) and the use thereof as an antalgic.

公开(公告)号：EP1056704B1

公开(公告)日：2003-05-02

申请号：EP99907161.6

申请日：1999-02-19

申请人： The Regents of the University of California

发明人： MCMORRIS, Trevor, C. ,  KELNER, Michael, J.

IPC分类号： C07C49/497 ,  C07C49/517 ,  C07C69/16 ,  C07C69/18 ,  C07C323/58 ,  C07C323/59 ,  C07C323/60 ,  C07D207/16 ,  C07K5/065 ,  A61K31/12 ,  A61K31/16 ,  A61K31/195 ,  A61K31/25 ,  A61K38/05

CPC分类号： C07C69/013 ,  A61K38/00 ,  C07C49/737 ,  C07C49/753 ,  C07C323/58 ,  C07C323/59 ,  C07C323/60 ,  C07D207/16 ,  C07K5/0215 ,  C07K5/081 ,  C07K5/1013 ,  Y02A50/395

摘要： The present invention provides illudin analogs of the general formula I:wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I, intermediates and processes useful for preparing compounds of formula I, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I.

公开(公告)号：EP1189898B1

公开(公告)日：2003-03-12

申请号：EP00937111.3

申请日：2000-05-26

申请人： RICHTER GEDEON VEGYESZETI GYAR R.T.

发明人： SÖRÖS, Béla ,  TUBA, Zoltán ,  GALIK, György; ,  BOR, Adám; ,  DEMETER, Adám ,  TRISCHLER, Ferenc; ,  HORVATH, János ,  BRLIK, János

IPC分类号： C07D327/10 ,  C07C253/30 ,  C07C303/28 ,  C07C309/66 ,  C07C319/14 ,  C07C323/60 ,  C07C315/02 ,  C07C317/46

CPC分类号： C07C253/30 ,  C07C303/28 ,  C07C315/02 ,  C07C319/14 ,  C07D327/10 ,  C07C317/46 ,  C07C255/60 ,  C07C309/66 ,  C07C323/60

摘要： Racemic or optically pure N-(4-cyano-3-trifluoromethylphenyl)-3-(4 -fluorophenylsulphonyl)-2-hydroxy-2-methylpropionamide of formula (I) is prepared by the following process: 2,3-dihydroxy-2-methylpropionic acid of formula (VII) is reacted with thionyl chloride to form 4-chlorocarbonyl-4-methyl-1,3,2-dioxathiolane-2-one of formula (VI), which is reacted with 4-cyano-3-trifluoromethylaniline. The resulting 4-{[4-cyano-3-(trifluoromethyl)anilino]carbonyl}-4-methyl-1,3,2-dioxathiolane-2-one of formula (V) is hydrolysed to form N-[4-cyano-3-(trilfuoromethyl)phenyl]-2,3-dihydroxy-2-methylpropionamide of formula (IV), which is sulfonylated with a sulfonyl halogenide of formula R-SO2-X, in a halogenated hydrocarbon solvent in the presence of a tertiary amine base. The sulphonic ester derivative of formula (III) obtained is reacted with 4-fluorothiophenol in the presence of a base to give a thioether of formula (II) which is oxidized using an inorganic peroxy compound or aqueous hydrogen peroxide.

公开(公告)号：EP1260501A1

公开(公告)日：2002-11-27

申请号：EP02008248.3

申请日：2002-04-18

申请人： CHEMAGIS LTD.

发明人： Naddaka, Vladimir ,  Menashe, Naim ,  Lexner, Jael ,  Saeed, Shadi ,  Kaspi, Joseph ,  Leman, Ori

IPC分类号： C07C319/20 ,  C07C323/60

CPC分类号： C07C319/14 ,  C07C323/60

摘要： The invention provides a process for the preparation of diphenylmethylthioacetamide (I) as described in Scheme 4 comprising reacting of the isothiouronium salt or its corresponding base of the formula IV with an acetamide of the formula XCH 2 CONH 2 , wherein X represents a halogen, M represents an alkali metal and A represents an anion, in a protic medium at a temperature of less than 100° C.

摘要翻译： 本发明提供了如方案4所述的制备二苯基甲硫基乙酰胺（I）的方法，包括使异硫脲鎓盐或其相应的式IV碱与式XCH 2 CONH 2的乙酰胺反应，其中X代表卤素，M代表碱金属 金属和A代表阴离子，在温度低于100℃的质子介质中

公开(公告)号：EP1219595A1

公开(公告)日：2002-07-03

申请号：EP00956871.8

申请日：2000-09-01

申请人： KYORIN PHARMACEUTICAL CO., LTD.

发明人： SATOH, Hiroya ,  KOMURO, Masakatsu ,  MURAKAMI, Koji ,  AWANO, Katsuya

IPC分类号： C07C235/60 ,  C07C317/46 ,  C07C323/60 ,  A61K31/166 ,  A61K31/192 ,  A61K31/235 ,  A61P3/06 ,  A61P3/10 ,  A61P43/00

CPC分类号： C07C317/46 ,  C07C235/60 ,  C07C323/60

摘要： The invention provides o-anisamide derivatives and their addition salts effective for the prevention and/or therapy of metabolic diseases such as hyperlipidemia and diabetes, in which peroxisome proliferator-activated receptor (PPAR) being intranuclear receptor, in particular, human PPAR participates, as agonistic drugs thereon, and processes for preparing them.
The invention relates to o-anisamide derivatives represented by a general formula (1)
[wherein R denotes a carboxyl group, carboxymethyl group or CH 2 CHXCOY (here X denotes a mercapto group or S(O)nMe (n=0, 1 or 2) and Y denotes an amino group or hydroxyl group)], their medicinally acceptable salts, their hydrates, and processes for preparing them.

摘要翻译： 本发明提供了用于预防和/或治疗代谢性疾病如高脂血症和糖尿病的邻甲氧基苯甲酰胺衍生物及其加成盐，其中作为核内受体的过氧化物酶体增殖物激活受体（PPAR），特别是人类PPAR参与， 激素药物及其制备方法。 本发明涉及由通式（1）表示的邻甲氧基苯甲酰胺衍生物，其中R表示羧基，羧甲基或CH 2 CHXCOY（这里X表示巯基或S（O）nMe（n = 0,1或 2），Y表示氨基或羟基），其药学上可接受的盐，它们的水合物及其制备方法。

公开(公告)号：EP1165492A1

公开(公告)日：2002-01-02

申请号：EP00913980.9

申请日：2000-03-27

申请人： Pharmacor Inc.

发明人： SAUVE, Gilles ,  YELLE, Jocelyn

IPC分类号： C07C237/22 ,  C07D209/20 ,  C07D233/64 ,  C07C323/60 ,  C07K5/06 ,  A61K31/165 ,  A61K38/05 ,  A61P31/18

CPC分类号： C07K5/06026 ,  A61K38/00 ,  C07C237/22 ,  C07C323/60 ,  C07K5/06078

摘要： An hydroxphenyl derivative selected from the group consisting of a compound of formula (I), (II) and comprises a carboxylic acid group when a compound of formula (I) pharmaceutically acceptable salts thereof and when a compound of formula (I) comprises an amino group pharmaceutically acceptable ammonium salts thereof, wherein n is 1, 2 or 3, e is 1, 2 or 3, Hal represents a halogen atom (e.g. Cl, Br, F or I), p is 0, 1 or 2, r is 0, 1 or 2, X and X' each independently represents a single bond, a saturated straight or branched hydrocarbon group of 1 to 4 carbon atoms or a straigth or branched hydrocarbon group of 2 to 4 carbon atoms comprising a carbon to carbon double bond, Ra represents H or -CH3, and Raa represents H or -CH3; W may represent an amino acid residue or fragment. These compounds may be used to inhibit the activity of HIV integrase.