| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 181 | Preparation of taxanes from 9-dihydro-13-acetylbaccation III | US13031378 | 2011-02-21 | US08697894B2 | 2014-04-15 | Gaetan Caron; Mettilda Lourdusamy |
| A new process for preparing a compound of Formula V, wherein P is a hydroxy protecting group and R is acetyl, said process including the steps of: i) selectively deacetylating the 10-hydroxy group of 9-dihydro-13-acetylbaccatin III with N,N-dimethylethylenediamine to produce 9-dihydro-10-deacetyl-13-acetyl-baccatin III; ii) concomitantly protecting 7-hydroxy and 10-hydroxy groups of the reaction product of step i); and iii) oxidizing the 9-hydroxy group of the reaction product of step ii) with an oxidizing agent to produce the compound of formula V. | ||||||
| 182 | Process for preparing optically active antrocin | US13618016 | 2012-09-14 | US08658806B2 | 2014-02-25 | Dar-Fu Tai; Venkatachalam Angamuthu; Yew-Min Tzeng |
| The present invention relates to a process of preparation of optically active antrocin. At first, to introduce the correct configuration of trans-decalone, alkyl aluminum/TMSCN was used to react with decalenone. The resulting racemic nitrile-decalone was resolved with chiral diol by ketalization to produce two chromatography separable diasteromers. After a simple column chromatography, optically pure compounds were obtained. Formylation was a critical step for the lactone formation. The rest of the synthesis is straight forward through oxidation and olefination. Accordingly, the total synthesis was completed in 10 steps with 7% overall yield from commercially available 6-methoxy-2-tetralone. | ||||||
| 183 | Dendritic polymers and magnetic resonance imaging contrast agent employing the same | US13633485 | 2012-10-02 | US08562953B2 | 2013-10-22 | Dhakshanamurthy Thirumalai; Chin-I Lin; Shian-Jy Wang |
| A dendritic polymer and a magnetic resonance imaging contrast agent employing the same. The magnetic resonance contrast agent includes the dendritic polymer according to the structure of SP-DZ-L)i)j or SP-DX-Z-L)i)j, wherein, S is cyclosilane moiety with j silicon oxygen residual groups, and j is not less than 2; P is CH2CH2Ol, and l is not less than 1; D is a C3-30 dendritic moiety having n oxygen residue, and n is not less than 3; X is C3-30 moiety having bi-functional groups; Z is a C3-20 moiety having a plurality of functional group; and L is a metal cation. | ||||||
| 184 | Biologically active taxane analogs and methods of treatment by oral administration | US13620852 | 2012-09-15 | US08552056B2 | 2013-10-08 | James D. McChesney; Gilles Tapolsky; David E. Emerson; John Marshall; Tauseef Ahmed; Allen Cohn; Michael Kurman; Manuel Modiano |
| The present invention relates to a novel chemical compound of formula S-(1): for use in the treatment of cancer, to compositions containing said compound, methods of manufacture and combinations with other therapeutic agents. | ||||||
| 185 | Isoxazol-3(2H)-one analogs as therapeutic agents | US12755010 | 2010-04-06 | US08415378B2 | 2013-04-09 | Jonas Boström; Leifeng Cheng; Tomas Fex; Michael Karle; Daniel Pettersen; Peter Schell |
| or a pharmaceutically suitable salt thereof, wherein, R1 and R2 independently are hydrogen, deuterium, aryl, hetero aryl, C1-C8 alkyl, optionally being substituted with one or more substituents independently being R3, R3 is an aryl, hetero aryl, fluorine(s), a C1-C6 alkyl containing one or more fluorine, a C1-C6 alkyl containing one or more deuterium, a C1-C6 alkyl containing hydroxy, the aryl and heteroaryl optionally being substituted with one or more halogen, a fluorinated alkoxy, a fluorinated alkyl, a sulfonyl, one or more deuterium, a C1-6 alkyl, a C1-6 alkoxy, a nitrile, or R3 is a C1-6 alkyl optionally substituted with one or more of the following groups: COOR4, OCOR4, CONR5R6, NR5COR6, OR4; wherein, R4 is a C1-10 alkyl optionally substituted with one or more fluorine, deuterium, alkoxy, arylcarboxylate, alkyl carboxylate; R5 and R6 are independently selected from hydrogen, alkyl or they may together form a 4-8 membered carbon ring; or R1 and R2 form a 3-10 membered carbon ring optionally comprising O or N and optionally substituted with a C1-10 alkyl or aryl, hetero aryl optionally substituted with R3. | ||||||
| 186 | Process for the manufacture of laidlomycin | US12887807 | 2010-09-22 | US08415121B2 | 2013-04-09 | Robert Sheridan |
| Improved process for the isolation of laidlomycin from a fermentation broth includes increasing the pH of the fermentation broth and centrifuging the pH adjusted fermentation broth, resulting in an aqueous layer and a wet solid layer containing laidlomycin. After the aqueous layer is removed, the wet solid layer containing laidlomycin is dried. The process provides an efficient and high yielding method. | ||||||
| 187 | Biologically active taxane analogs and methods of treatment by oral administration | US12873477 | 2010-09-01 | US08273789B2 | 2012-09-25 | James D. McChesney; Gilles Tapolsky; David L. Emerson; John Marshall; Tauseef Ahmed; Allen Cohn; Michael Kurman; Manuel Modiano |
| The present invention relates to a novel chemical compound of formula S-(1): for use in the treatment of cancer, to compositions containing said compound, methods of manufacture and combinations with other therapeutic agents. | ||||||
| 188 | Esters of 5-hydroxymethylfurfural and methods for their preparation | US12278512 | 2007-02-07 | US08247582B2 | 2012-08-21 | Herman P. Benecke; Jerry L. King, II; Alex Walter Kawczak; Donald W. Zehnder, II; Erica E. Hirschl |
| Disclosed are compositions and methods for the production of mono-esters and di-esters from the reaction of HMF and a reactant selected from a diacid or a diacid derivative; typical reactants are PAN, phthaloyl dichloride, dimethyl phthalate, maleic acid, and maleic anhydride or mono-esters that can be prepared from HMF and MAN. | ||||||
| 189 | Methods for the preparation of taxanes using chiral auxiliaries | US12092432 | 2006-11-03 | US08207358B2 | 2012-06-26 | Mettilda Lourdusamy; Gaétan Caron |
| The present invention relates to a stereoselective synthesis of novel β-lactam dimers as useful precursors for the preparation of paclitaxel, docetaxel, and analogues thereof. More particularly, the new β-lactams are prepared from readily available and enantiomerically pure chiral auxiliaries. The β-lactams are then reacted with a suitably protected taxane to produce diastereomerically enriched side chain-bearing taxanes. Finally, the chiral auxiliary is cleaved and protecting groups are removed to provide the desired taxane. | ||||||
| 190 | PROCESS FOR LIQUEFYING A CELLULOSIC MATERIAL AND ITS PRODUCTS | US13106553 | 2011-05-12 | US20110277378A1 | 2011-11-17 | Klaas Lambertus VON HEBEL; Jean-Paul LANGE |
| A process for liquefying a cellulosic material to produce a liquefied product from cellulosic material is provided. Products obtained from such process and use of such products to prepare biofuels is also provided. | ||||||
| 191 | Fluorescence assays with improved sensitivity | US12426997 | 2009-04-21 | US08034928B2 | 2011-10-11 | Ronald T. Raines; Sunil S. Chandran; Timothy E. Glass; Luke D. Lavis |
| Latent fluorescent compounds, comprising a fluorescent molecule with one or more blocking groups attached and optionally one or more urea-containing groups are provided. The urea-containing group can be used to further attach one or more molecules of interest, such as proteins, peptides or nucleic acids. The blocking group(s) is released from the latent fluorescent compound by reaction with a trigger, forming the fluorescent molecule which can be detected. Also provided herein are methods of using latent fluorescent compounds to detect triggers. | ||||||
| 192 | PROCESS FOR PREPARING A HYDROCARBON OR MIXTURE OF HYDROCARBONS | US12972170 | 2010-12-17 | US20110173877A1 | 2011-07-21 | Jeroen Van Buijtenen; Jean-Paul Lange; Richard John Price |
| A process for preparing a hydrocarbon or mixture of hydrocarbons comprising the steps of (i) hydrogenating furfural, 5-hydroxymethylfurfural or a mixture of furfural and 5-hydroxymethylfurfural to provide furfuryl alcohol, 2,5-furandimethanol or a mixture of furfuryl alcohol and 2,5-furandimethanol; (ii) oligomerizing the alcohol or mixture of alcohols of step (i) in the presence of an acidic catalyst to provide a carbon-carbon coupled oligomer; and (iii) hydrogenating the oligomer of step (ii) is provided. The hydrocarbons are useful as fuel blending components. Processes for controlling the oligomerization of alcohol or mixture of alcohols to optimise the production of oligomers suitable for conversion to hydrocarbons useful as kerosene and diesel components are also provided. | ||||||
| 193 | Tetrahydroquinoline derivatives and their use as FSH receptor modulators | US10540335 | 2003-12-16 | US07674909B2 | 2010-03-09 | Cornelis Marius Timmers; Willem Frederik Karstens |
| The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are H, Me; R3 is (2-6C)heterocycloalkyl(1-4C)alkyl, (2-5C)heteroaryl(1-4C)alkyl, (6C)aryl (1-4C)alkyl, (1-4C)(di)alkylaminocarbonylamino(2-4C)alkyl, (2-6C) heterocycloalkylcarbonylamino(2-4C)alkyl, R5-(2-4C)alkyl or R5-carbonyl(1-4C)alkyl; R4 is (2-5C)heteroaryl, (6C)aryl, (3-8C)cycloalkyl, (2-6C)heterocycloalkyl or (1-6C) alkyl and R5 is (di)(1-4C)alkylamino, (1-4C)alkoxy, amino, hydroxy, (6C)arylamino, (di)(3-4C)alkenylamino, (2-5C)heteroaryl(1-4C)alkylamino, (6C)aryl(1-4C) alkylamino, (di)[(1-4C)alkoxy(2-4C)alkyl]amino, (di)[(1-4C)alkylamino(2-4C) alkyl]amino, (di)[amino(2-4C)alkyl]amino or (di)[hydroxy(2-4C)alkyl]amino. The present invention also relates to pharmaceutical compositions comprising said derivatives and the use of these derivatives to regulate fertility. | ||||||
| 194 | Chroman derivatives as estrogenic compounds | US11328760 | 2006-01-10 | US07531571B2 | 2009-05-12 | Gerrit Herman Veeneman; Neeltje Miranda Teerhuis |
| The invention provides chroman compounds having formula 1 wherein R1 is (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl, and independently R1 has a cis-orientation in relation to the exocyclic phenyl group at the 2-position of the skeleton; R4 is H, Hal, CF3, OH or (1C-2C)alkyloxy; R2, R3, and R5are independently H, Hal, CF3, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl and prodrugs thereof for the manufacture of a medicine for estrogen-receptor related treatments. | ||||||
| 195 | Ether lactone | US10507372 | 2003-02-17 | US07476647B2 | 2009-01-13 | Thomas Markert; Alfred Westfechtel; Volker Porrmann |
| The invention relates to the ether lactone of formula (I) which is characterized by interesting and original odor characteristics, which diffuses extremely well and is suitable for use as a fragrance, for example in cosmetic preparations, technical products or in alcoholic perfumery. | ||||||
| 196 | Methods and compositions for use in treating cancer | US10687526 | 2003-10-16 | US07470720B2 | 2008-12-30 | Bruce A. Littlefield; Murray J. Towle |
| The invention provides methods and compositions for use in treating diseases associated with excessive cellular proliferation, such as cancer. | ||||||
| 197 | Semisynthesis process for the preparation of 10-deacetyl-N-debenzoyl-paclitaxel | US11244171 | 2005-10-06 | US07446126B2 | 2008-11-04 | Bruno Gabetta; Andrea Gambini; Ezio Bombardelli; Gabriele Fontana |
| A process is provided for the preparation of 10-deacetyl-N-debenzoyl-paclitaxel (I) a synthon useful for the preparation of taxanes with antitumour activity, and intermediates for the preparation thereof. Also described is a process for the preparation of Docetaxel starting from the compound of formula (I). | ||||||
| 198 | Rearranged pentanols, a process for their production and their use as anti-inflammatory agents | US10960757 | 2004-10-08 | US07442794B2 | 2008-10-28 | Hartmut Rehwinkel; Stefan Baeurle; Markus Berger; Norbert Schmees; Heike Schaecke; Konrad Krolikiewicz; Anne Mengel; Duy Nguyen; Stefan Jaroch; Werner Skuballa |
| The invention relates to the compounds of formula I, a process for their production and their use as anti-inflammatory agents. | ||||||
| 199 | Peptide deformylase inhibitors | US10538625 | 2003-12-11 | US07442793B2 | 2008-10-28 | Jinhwa Lee; Siegfried B. Christensen, IV |
| Novel PDF inhibitors and novel methods for their use are provided. | ||||||
| 200 | LACTONE STABILIZING COMPOSITIONS | US12122961 | 2008-05-19 | US20080217585A1 | 2008-09-11 | Jusong Xia |
| This invention provides a novel class of compounds and compositions and synthetic methods related to lactone antioxidant 3-arylbenzofuranones. The compounds may be useful to prevent yellowing and deterioration of organic materials preferably polymers, such as polyurethane foams as one example. The lactone antioxidants may be polymeric, and may also be liquid or paste in physical form at room temperature. Although it is not necessary for its stabilizing properties, the compositions may, in some species, bear one or more reactive primary OH groups on the polymer chains. The chains may also contain oligomeric oxyalkylene ether and aliphatic ester functional groups, in one embodiment of the invention. | ||||||
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