| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 141 | CRYSTALLINE FORM OF 4-(ß-D-GLUCOPYRANOS-1-YL)-1-METHYL-2-[4-((S)-TETRAHYDROFURAN-3-YLOXY)-BENZYL]-BENZENE, A METHOD FOR ITS PREPARATION AND THE USE THEREOF FOR PREPARING MEDICAMENTS | EP07821913.6 | 2007-10-26 | EP2086991A1 | 2009-08-12 | ECKHARDT, Matthias; HIMMELSBACH, Frank; BUTZ, Tanja, M.; MARTIN, Hans-Jürgen |
| The invention relates to a crystalline form of 4-(β-D-glucopyranos-1 -yI)-1-methyl-2- [4-((S)-tetrahydrofuran-3-yloxy)-benzyI]-benzene, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments. | ||||||
| 142 | MIMES STABLES DE SUCRES DE TYPE C-GLYCOSIDES ET C- GLYCOCONJUGUES, LEUR PROCEDE DE PREPARATION ET LEURS APPLICATIONS NOTAMMENT DANS LE DOMAINE DE LA COSMETIQUE ET DU MEDICAMENT. | EP07731342.7 | 2007-04-23 | EP2027138A2 | 2009-02-25 | CASTELOT-DELIENCOURT-GODEFROY, Géraldine; QUIRION, Jean-Charles; JUBAULT, Philippe; ZOUTE, Ludivine |
| The invention concerns a C-glycoside compound of formula (I); wherein: n is equal to 1 or 2; Y represents H or halogen; X is an alkyl chain bearing at least one amino, amide, acid, ester, carbonyl, alcohol, aryl function or a carbonyl, ester amide, amino, alcohol group; the R's, identical or different, represent a OH or OR' group where R' is an alkyl, benzyl, benzoyl, acetyl, pivaloyl, trialkylsilyl, tertiobutyldiphenylsilyl group or one or more sugars; R1 represents OR', NR'R'', N3, or a phthalamide with R'' and R''', identical or different, represent H or an alkyl, aryl, benzyl, benzoyl, acetyl, alkoxycarbonyl, allyloxycarbonyl, benzyloxycarbonyl group; R2 represents H or halogen or a OH, OR, NR'R''or N3 group, as well as derivatives thereof in physiologically or pharmaceutically acceptable base, mineral or organic acid-addition salt, hydrate or solvate form. The invention is useful for preparing C-glycoside compounds or C-glycoconjugates applicable in particular in cosmetology, medical imagery, immunology for treating cancer, diabetes, hypertension. | ||||||
| 143 | NOUVEAUX COMPOSES C-GLYCOSIDES GEM-DIFLUORES DERIVES DE LA PODOPHYLLOTOXINE, LEUR PREPARATION ET LEURS APPLICATIONS | EP07731356.7 | 2007-04-24 | EP2024379A1 | 2009-02-18 | QUIRION, Jean-Charles; CASTELOT DELIENCOURT-GODEFROY, Géraldine; AUDOUARD, Christophe |
| The invention relates to a gem-difluoro glycoconjugated compound having formula (I): wherein R is H or an alkyl, benzyl, acetyl, benzoyl group, each of R1 and R2, which are the same or different, is H or an alkyl, benzyl, benzoyl, acetyl, pivaloyl, trialkylsilyl, tertiobutyl- diphenylsilyl protective group or an acetal group of the CR'R' type, where each of R' and R', which are the same or different, is H or an alkyl, aryl, benzyl or thiophene group, R3 is H or an alkyl, benzyl, benzoyl, acetyl, pivaloyl, trialkylsilyl or tertiobutyldiphenylsilyl protective group, R4 is OR'', NGR'GR', N3, or a phthalimide, where R''' is H or an alkyl, benzyl, benzoyl, acetyl, pivaloyl, trialkylsilyl or tert-butyldiphenylsilyl protective group, each of GR' and GR', which are the same or different, is H or an alkyl, benzyl, benzoyl, acetyl, alkyloxycarbonyl, allyloxycarbonyl or benzyloxycarbonyl group, R5 is a free or protected hydroxyl group or a halogen, R6 is H or an alkyl, acetyl, benzyl, PO3H or PO3Na group. The invention is suitcable for preparing compounds that can be used particularly for the treatment of cancer. | ||||||
| 144 | COMPOSES C-GLYCOPEPTIDES GEM-DIFLUORES, LEUR PREPARATION ET LEUR UTILISATION NOTAMMENT POUR LA PRESERVATION DE MATERIAUX BIOLOGIQUES. | EP07731371.6 | 2007-04-26 | EP2013195A1 | 2009-01-14 | CASTELOT DELIENCOURT-GODEFROY, Géraldine; QUIRION, Jean-Charles |
| The invention relates to a gem-difluoride C-glycopeptide compound with formula I where n is an integer equal to 3 or 4, R represents a hydrogen atom, an alkyl, benzyl, acetyl, trimethylsilyl, tert-butyldimethylsilyl, tert-butyldiphenylsilyl group, R´ represents OR, NR'R'', N3, or a phthalimide, R' and R'' represent a hydrogen atom or an alkyl, aryl, benzyl, benzoyl, acetyl, alkyloxycarbonyl, allyloxycarbonyl, benzyloxycarbonyl group, R1 represents a hydrogen atom or an alkyl, benzyl, alkylcarbamate, allylcarbamate, benzylcarbamate, acetyl group, R1 may consist of an amino acid if R2 represents only OR, R2 includes an amino acid if R1 represents a hydrogen atom or an alkyl, benzyl, alkylcarbamate, allylcarbamate, benzylcarbamate, acetyl group, R2 represents OR when R1 represents an amino acid, R3 represents a hydrogen atom or a free or protected alcohol function. It is applicable to the preparation of compounds or compositions to be used for preservation of biological materials such as cells, tissues and organs at various temperatures. | ||||||
| 145 | METHOD OF DRUG DESIGN | EP06790302.1 | 2006-10-03 | EP1934388A1 | 2008-06-25 | TOMETZKI, Gerald, B.; MEUTERMANS, Wim; ZEUGG, Johannes |
| The invention provides a method of identifying biologically active compounds comprising: (a) designing a first library of compounds of formula (1) to scan molecular diversity wherein each compound of the library has at least two pharmacophoric groups R1 to R5 as defined below and wherein compound of the library has same number of pharmacophoric groups; (b) assaying the first library of compounds in one or more biological assay(s); and (c) designing a second library wherein each compound of the second library contains one or more additional pharmacophoric group with respect to the first library; such that the/each component of the first and second library is a compound of formula (1). | ||||||
| 146 | METHODS OF PRODUCING C-ARYL GLUCOSIDE SGLT2 INHIBITORS | EP03800231 | 2003-12-23 | EP1581543A4 | 2008-03-19 | DESHPANDE PRASHANT P; ELLSWORTH BRUCE A; SINGH JANAK; LAI CHIAJEN; CRISPINO GERARD; RANDAZZO MICHAEL E; GOUGOUTAS JACK Z; DENZEL THEODOR W |
| 147 | 6"-AMINO-6"-DEOXYGALACTOSYLCERAMIDES | EP03816701 | 2003-03-20 | EP1611147A4 | 2007-10-17 | SAVAGE PAUL B; BENDELAC ALBERT; TEYTON LUC |
| 148 | IMPROVED EXPRESSION SYSTEMS WITH SEC-SYSTEM SECRETION | EP04817876 | 2004-11-22 | EP1687324A4 | 2007-08-22 | RETALLACK DIANE M; SCHNEIDER JANE C; RAMSEIER THOMAS MARTIN |
| 149 | GLYCOSOLATED ENKEPHALIN AGENTS | EP04714123.9 | 2004-02-24 | EP1597265A2 | 2005-11-23 | POLT, Robin, L.; BILSKY, Edward, J. |
| It is taught here that enkephalin peptides which are glycosylated with a disaccharide will be transported across the blood brain barrier and deliver analgesic effects superior to morphine when introduced into the bloodstream. Glycosylated peptides with disaccharides attached are superior to analogous peptides with either mono- or tri- saccharides attached. | ||||||
| 150 | NUCLEIC ACID LABELING COMPOUNDS | EP02728452 | 2002-03-12 | EP1385829A4 | 2005-10-19 | MCGALL GLENN; BARONE ANTHONY D |
| Nucleic acid labeling compounds are disclosed. The compounds are synthesized by condensing a heterocyclic derivative with a cyclic group (e.g. a ribofuranose derivative). The labeling compounds are suitable for enzymatic attachment to a nucleic acid, either terminally or internally, to provide a mechanism of nucleic acid detection. | ||||||
| 151 | SIALIC ACID/FUCOSE BASED MEDICAMENTS | EP94920015 | 1994-05-18 | EP0759758A4 | 1997-05-14 | DASGUPTA FALGUNI; MUSSER JOHN HENRY |
| 152 | DIAGNOSIS AND TREATMENT OF BACTERIAL DYSENTERY. | EP92922817 | 1992-10-19 | EP0610356A4 | 1995-03-29 | ARMSTRONG GLEN D; RATCLIFFE R MURRAY |
| There is provided the use of an agent in the preparation of a medicament for the prevention or treatment of an enteric infection mediated by an SLT, wherein said agent is a pharmaceutically acceptable solid inert affinity support capable of being eliminated from the gastrointestinal tract, which support has an affinity ligand covalently attached thereto through a spacer arm, wherein said ligand is characterized as an oligosaccharide containing the disaccharide subunit alpha Gal(1-4) beta Gal which binds the SLT; with the proviso that the disaccharide is not part of a alpha Gal(1-4) beta Gal(1-4) beta GlcNAc trisaccharide or a alpha Gal(1-4) beta Gal(1-4) beta Glc trisaccharide. | ||||||
| 153 | STREPTOMYCES VECTORS FOR PRODUCTION OF HETEROLOGOUS PROTEINS | EP91913400 | 1991-07-01 | EP0538371A4 | 1993-08-04 | BRAWNER, MARY, ELLEN; FORNWALD, JAMES, ALLAN; ARTHOS, JAMES 380 CURTNER AVENUE |
| 154 | New antibiotic, neocopiamycin A and the production thereof | EP84305861.1 | 1984-08-28 | EP0137692A2 | 1985-04-17 | Arai, Tadashi, Prof. |
A new antibiotic, designated as neocopiamycin A, is useful as antifungal agent. Neocopiamycin A is fermentatively produced as a minor component, in addition to copiamycin, by a microorganism Streptomyces hygroscopicus var. crystallogenes (FERM BP-576) which is known to produce the known antibiotic copiamycin. |
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| 155 | CELL-PERMEABLE PROBES FOR IDENTIFICATION AND IMAGING OF SIALIDASES | PCT/US2013/055472 | 2013-08-16 | WO2014031498A1 | 2014-02-27 | WONG, Chi-Huey; FANG, Jim-Min; CHENG, Yih-Shyun, E.; TSAI, Charng-Sheng |
Provided herein are novel irreversible sialidase inhibitors. These compounds can be conjugated with a detectable tagging moiety such as azide-annexed biotin via CuAAC for isolation and identification of sialidases. The provided compounds and the corresponding detectable conjugates are useful for detecting sialidase-containing pathogens and imaging in situ sialidase activities under physiological conditions. |
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| 156 | 2-((2S,3S,4R,5R)-5-((S)-3-AMINO-2-HYDROXYPROP-1-YL)-4-METHOXY-3-(PHENYLSULFONYLMETHYL)TETRAHYDROFURAN-2-YL)ACETALDEHYDE DERIVATIVES AND PROCESS FOR THEIR PREPARATION | PCT/CA2012/050939 | 2012-12-24 | WO2013097042A1 | 2013-07-04 | SOUZA, Fabio E.S.; RUDOLPH, Alena; PAN, Ming; GORIN, Boris; ALBERICO, Dino |
Disclosed is a compound of formula 1, as shown below, where R1, R2, R3, R4, R5, R6 and R7 are as described herein. Also, disclosed is a process for the preparation of compounds of formula 1, and intermediates used therein. The compound of formula 1 can be useful for preparation of halichondrin analogs such as Eribulin. |
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| 157 | ARTIFICIAL LECTIN MIMICS AND USES THEREOF | PCT/US2009/065366 | 2009-11-20 | WO2010059958A3 | 2010-05-27 | SVAROVSKY, Sergei; BOLTZ, Kathryn; JOHNSTON, Stephen, Albert; GONZALEZ-MOA, Maria |
Lectins are important class of sugar-binding proteins involved in a variety of biological phenomena. In some aspects, the present invention relates to the process of selection and application of high-fidelity artificial lectin mimics in the construction of microarray devices capable of precise, rapid and inexpensive analysis of glycoproteins, pathogen detection, and diagnosis of various disease states. In some aspects, the invention also relates to the use of identified binding peptides on solid support or free in solution in cell sorting, affinity purification, and other applications where natural lectins are traditionally used. |
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| 158 | COMPOSES C-GLYCOSIDES ET PROCEDES DE PREPARATION DE COMPOSES C-GLYCOSIDES | PCT/EP2009/064792 | 2009-11-06 | WO2010052314A3 | 2010-05-14 | BENVEGNU, Thierry; LEMIEGRE, Loïc; RANOUX, Adeline |
Composés C-glycoses présentant la Formule (I) suivante: où: S' représente un radical monosaccharidique, ou polysaccharidique dérivé d'un monosaccharide ou polysaccharide S, R représente un radical alkyl linéaire ou ramifié, Z représente un radical éthylényl CH=CR1(R2) ou acétylényl C≡CR3, et procédé de préparation de composés C-glycosides de Formule (III) caractérisé en ce qu'il inclut une étape consistant à faire réagir, dans un solvant aqueux ou en l'absence de solvant, et en présence d'une base organique ou minérale (B), un sucre (S) avec un phosphonate de Formule (II), selon le schéma réactionnel suivant: Formules (II), (III). |
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| 159 | C-GLYCOSIDE COMPOUNDS, AND METHOD FOR PREPARING C-GLYCOSIDE COMPOUNDS | PCT/EP2009064792 | 2009-11-06 | WO2010052314A2 | 2010-05-14 | BENVEGNU THIERRY; LEMIEGRE LOIC; RANOUX ADELINE |
| The invention relates to C-glycose compounds of formula (I) where: S' is a monosaccharide radical or a polysaccharide radical derived from a monosaccharide or polysaccharide S; R is a linear or branched alkyl radical; and Z is an ethylenyl CH=CR1(R2) or an acetylenyl C=CR3 radical. The invention also relates to a method for preparing C-glycoside compounds of formula (III), characterised in that the method consists of a step of reacting a sugar (S), in an aqueous solvent or in the absence of a solvent and in the presence of an organic or mineral base (B), with a phosphonate of formula (II) according to the following reaction pattern: Formulas (II), (III). | ||||||
| 160 | CRYSTALLINE FORM OF 4-(ß-D-GLUCOPYRANOS-1-YL)-1-METHYL-2-[4-((S)-TETRAHYDROFURAN-3-YLOXY)-BENZYL]-BENZENE, A METHOD FOR ITS PREPARATION AND THE USE THEREOF FOR PREPARING MEDICAMENTS | PCT/EP2007/061553 | 2007-10-26 | WO2008049923A1 | 2008-05-02 | ECKHARDT, Matthias; HIMMELSBACH, Frank; BUTZ, Tanja, M.; MARTIN, Hans-Jürgen |
The invention relates to a crystalline form of 4-(β-D-glucopyranos-1 -yI)-1-methyl-2- [4-((S)-tetrahydrofuran-3-yloxy)-benzyI]-benzene, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments. |
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