Patent application number | Description | Published |
20110166172 | Rapamycin Carbonic Ester Analogues, Pharmaceutical Compositions, Preparations and Uses Thereof - Rapalogs of formula I, pharmaceutically acceptable salts, pharmaceutical compositions, and preparation methods and uses thereof. The rapalogs have the structure of formula I and can be used as an anti-tumor medicament. Comparing with rapamycin, the rapalogs of the present invention exhibit enhanced water solubility, and improved pharmacological and pharmacokinetic properties by introducing a hydrophilic and polar group such as a hydroxyl. | 07-07-2011 |
20110201810 | Method for Preparing 4-[9-(6-Aminopurine)]-2-(S)-Hydroxyl-Butyric Acid Methyl Ester - The present invention discloses a novel method for preparing and purifying 4-(6-Amino-purin-9-yl)-2(S)-hydroxy-butyric acid methyl ester. The preparation started from cheap and easily available L-malic acid, which was transformed to intermediate I after simultaneous protection of the groups of 1-carboxyl and 2-hydroxyl. The intermediate I was selectively reduced to intermediate alcohol II, whose hydroxyl group was further transformed to an easily leaving group to afford intermediate III. The intermediate III was nucleophilically substituted with adenine to afford intermediate IV. The intermediate IV was deprotected and methyl-esterified simultaneously in methanol in the presence of an acid or a base to afford crude 4-(6-Amino-purin-9-yl)-2(S)-hydroxy-butyric acid methyl ester, which was purified by recrystallization to afford the purified product. Comparing with the prior preparation methods, the present method has advantages in low cost, mild conditions, high retention of the chiral center during the reaction, high productivity, great improvement in the quality and yield of the product and great decrease in cost, and thus is suitable for the production on a large scale. | 08-18-2011 |
20120264793 | Pharmaceutical Use of 2',2-Bis-Thiazole Non-Nucleoside Compounds as Hepatitis C Virus Inhibitor - The present invention discloses the pharmaceutical use of a 2′,2-bis-thiazole non-nucleoside compound of formula I as an inhibitor of hepatitis C virus (HCV). The 2′,2-bis-thiazole non-nucleoside compound can inhibit the replication of HCV, and thus has an anti-HCV activity and is useful for treating hepatitis C. | 10-18-2012 |
20130059895 | 2',2-DITHIAZOL NON-NUCLEOSIDE COMPOUNDS, PREPARATION METHODS, PHARMACEUTICAL COMPOSITIONS AND USES AS HEPATITIS VIRUS INHIBITORS THEREOF - The present disclosure belongs to the field of pharmaceutical chemistry, and relates to a class of 2′,2-bisthiazole non-nucleoside compounds of following formula I, the preparation method and the pharmaceutical composition thereof. The compounds have both the anti-HBV and anti-HCV activities and are useful in treating hepatitides B and C. Pharmacokinetic tests showed the compounds have good bioavailability. | 03-07-2013 |
20140148600 | THIAZOLE COMPOUNDS, METHODS FOR PREPARATION AND USE THEREOF - The present invention relates to thiazole compounds of formula I, the method for preparation and use thereof. More specifically, the present invention relates to novel derivatives of natural product largazole, the method for preparing them and their uses for treatments against tumor and multiple sclerosis as inhibitors of histone deacetylase. | 05-29-2014 |
20140336252 | NOVEL COMPOUND AS KCNQ POTASSIUM CHANNEL AGONIST, PREPARATION METHOD THEREFOR AND USE THEREOF - The present invention provides compounds having the structure represented by general formula I, pharmaceutically acceptable salts thereofagonist, preparation methods therefor and a use thereof in the preparation of a medicine for the treatment of nervous system diseases. The compounds or pharmaceutical compositions thereof can be used as the KCNQ potassium channel agonist for treating nervous system diseases. Compared to retigabine, a compound in the prior art, the compound of the present invention have the same or better therapeutic effect, are easier for synthesis and storage, and less prone to oxidate deterioration. | 11-13-2014 |