Zhejiang Hisun Pharmaceutical Co., Ltd. Patent applications |
Patent application number | Title | Published |
20160137683 | Method for Preparing Epirubicin and Intermediate Thereof - The present invention provides a method for preparing epirubicin and an intermediate adaptive to the method. The preparation method may include: reacting tert-Butyldimethylsilyl chloride with N-trifluoroacetyl adriamycin to obtain a first compound N-trifluoroacetyl-14-O-tert-Butyldimethylsilyl adriamycin; oxidizing the first compound to obtain a second compound 4′-ketone-N-trifluoroacetyl-14-O-tert-Butyldimethylsilyladriamycin; reducing the second compound to obtain a third compound N-trifluoroacetyl-14-O-tert-Butyldimethylsilyl epirubicin; and performing deprotection and hydrolysis reactions on the third compound to obtain epirubicin. The method of the present invention needs low cost, fewer reaction steps, provides high yield and high product purity, and avoids serious pollution caused by a bromination reaction in a conventional method. | 05-19-2016 |
20160130218 | 4-BENZYL-1-PHENETHYL-PIPERAZINE-2,6-DIONE PREPARATION METHOD, AND INTERMEDIATE AND PREPARATION METHOD THEREOF - The present invention provides a key new intermediate (a compound of formula III) of 4-benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound), a pharmaceutically acceptable salt thereof and a preparation method thereof. The present invention additionally discloses a method for preparing 4-benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound) from the formula III compound, said method overcoming the shortcomings of current formula IV compound preparation methods, such as low production volumes, low purity, high energy consumption, high costs, and inability to achieve industrialized production, and provides a formula IV compound preparation method which is simple, economical, environmentally-friendly and easy to produce industrially; the reaction solvent of the method is easily recycled and the method can produce the formula IV compound at high production rates and with high purity. | 05-12-2016 |
20150329581 | NEW SYNTHESIS PROCESS OF ANTIPARASITIC DRUG SELAMECTIN - Provided in the present invention are novel key intermediates of selamectin and the preparation method thereof. Also provided is a new synthesis process, using doramectin as a starting material, and obtaining selamectin via hydrogenation, oxidation, oximation and desugaring. The new process of the present invention has few steps, and is simple to operate, high in yield, low in cost and causes little pollution, and is more suitable for large scale industrial production. | 11-19-2015 |
20150299340 | PREPARATION OF NEW INTERMEDIATE OF HEPARIN PENTASACCHARIDE AND PREPARATION METHOD THEREOF - The present invention relates to a process of a chemically synthetic drug, and in particular, to a new intermediate of a heparin pentasaccharide and a preparation method thereof. The process has high reaction efficiency, and an easy reaction operation. The reaction intermediate is easy to be purified, and is appropriate for an industrialization production. | 10-22-2015 |
20150299241 | METHOD FOR PREPARING HIGHLY PURE DOXORUBICIN - The present invention relates to a method for preparing highly pure doxorubicin. The method comprises the following steps: (1) chromatographing a prepurified doxorubicin solution by using macroporous resin, pre-washing the chromatographed system by using an acidic low concentration aqueous organic solvent, and performing elution by using an acidic high concentration aqueous organic solvent; (2) performing chromatographic separation on eluted components by using a preparative column, so that a highly pure doxorubicin component can be obtained, and the doxorubicin can, if needed, be separated from the aqueous solution by using conventional concentration and crystallization methods in the prior art. The present invention has the advantages such as simplicity, high yield, low cost, and less environmental pollution. The content of the prepared doxorubicin is greater than 99.5%, the content of each impurity is controlled to be lower than 0.10%, and the USP and EP standards are met. | 10-22-2015 |
20150284419 | METHOD FOR PREPARING FULLY PROTECTION HEPARIN PENTASACCHARIDE AND INTERMEDIATE THEREOF - Disclosed is a process for chemically synthesizing a pharmaceutical intermediate, in particular to a novel intermediate and novel process for synthesizing an anticoagulant drug fondaparinux sodium intermediate—full protection heparin pentasaccharide. The process has a high reaction efficiency and a simple reaction operation, and enables the reaction intermediate to be easily purified, thus being suitable for the industrialized production of the full protection heparin pentasaccharide. | 10-08-2015 |
20150218091 | CRYSTAL FORMS OF AZETIDINONE COMPOUNDS AND PREPARING METHODS THEREOF - The present invention provides crystal forms of the compound of (3R,4S)-4-(4-hydroxyphenyl)-3-[3-(4-fluorophenyl)-4-hydroxybut-2(Z)-enyl]-1-(4-fluorophenyl)-2-azetidinone (formula A). The crystal forms can be characterized by X-ray powder diffraction (XRPD) spectra, differential scanning calorimetry (DSC) spectra, infrared absorption spectra and so on. Meanwhile, the present invention also provides methods for preparing the crystal forms of the compound of formula A, pharmaceutical compositions and uses thereof. | 08-06-2015 |
20150191480 | BENZODIOXOLE DERIVATIVE AND PREPARATION METHOD AND USE THEREOF - Provided in the present invention are novel benzodioxole derivatives and preparation methods thereof. These compounds represented by formula (I) or pharmaceutically acceptable salts thereof have acetylcholinesterase inhibitory activity, so can be used in the treatment or prevention of Alzheimer's disease. The definitions of R | 07-09-2015 |
20150119458 | 4-((SUBSTITUTED PHENYL) DIFLUOROMETHYL) PHENOXY CARBOXYLIC ACID DERIVATIVE, AND PREPARATION METHOD AND USES THEREOF - The present invention discloses a 4-((substituted phenyl)difluoromethyl)phenoxycarboxylic acid derivative and preparation process and use thereof. More specifically, the present invention relates to a compound of the following formula I, which is defined in the specification. The compounds according to the present invention can be used as PPAR agonists, and demonstrates a strong effect on reducing the levels of total cholesterol (TC), triglyceride (TG), and low density lipoprotein cholesterol (LDL-C) in blood plasma, and thus the compound according to the present invention can be used in the preparation of a medicament for treating or preventing hyperlipoidemia or cardio-cerebrovascular diseases caused by hyperlipoidemia, such as diabetes, atherosclerosis, stroke, coronary heart disease, etc. The present invention also relates to a novel intermediate compound for the preparation of the compound of formula I and preparation method thereof. | 04-30-2015 |
20150087828 | 4-SUBSTITUENT-2-HYDROXYLMORPHOLINE-3-ONE AND PREPARATION METHOD THEREOF - A molecule with neural activities, especially 4-substituent-2-hydroxymorpholin-3-one, as a new intermediate of neurokinin-1 receptor antagonist aprepitant, and preparation method thereof. | 03-26-2015 |
20150065700 | METHOD FOR PREPARING 3-O-BENZYL-1,2-O-ISOPROPYLIDENE-A-L-FURAN IDOSE - Provided is a method for preparing 3-O-benzyl-1,2-O-isopropylidene-α-L-idofuranose, which comprises: (1) protecting hydroxyl of 3-O-benzyl-1,2-O-isopropylidene-α-D-glucofuranose (III) by benzoyl and methylsulfonyl to obtain 6-O-benzoyl-3-O-benzyl-1,2-O-isopropylidene-5-O-methylsulfonyl-α-D-glucofuranose (V); (2) subjecting compound (V) to a cyclization reaction under an alkaline condition to obtain 5,6-epoxy-3-O-benzyl-1,2-O-isopropylidene-α-L-idofuranose (VI); and (3) subjecting compound (VI) to a ring-opening reaction to obtain 3-O-benzyl-1,2-O-isopropylidene-α-L-idofuranose. | 03-05-2015 |
20150065699 | GINSENOSIDE C-K POLYMORPHIC COMPOUNDS AND METHOD FOR PREPARING SAME - Provided are several types of ginsenoside polymorphic substances and a method for preparing same. In particular, new crystal form A, crystal form B, crystal form C, crystal form E, crystal form F, crystal form I, crystal form K, crystal form L, crystal form M, crystal form N, and crystal form O are involved. | 03-05-2015 |
20150057440 | TWO CRYSTAL FORMS OF GINSENOSIDE C-K AND METHOD FOR PREPARING SAME - Provided are ginsenoside C-K polymorphic forms and a method for preparing same. The ginsenoside C-K polymorphic forms are crystal form D and crystal form H. | 02-26-2015 |
20150011757 | METHOD FOR PREPARING LINEZOLID INTERMEDIATE - Disclosed is a new method for preparing a methyl substitute of a linezolid intermediate, (S)-2-(3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazoline) (I), wherein the intermediate (I) is obtained by the cyclization of 3-fluoro-4-morpholinophenyl isocyanate (II) and epoxy compound (III). This process has a short process route, low cost, easy operation, and high yield, so is suitable for a large-scale industrial production. | 01-08-2015 |
20140378488 | 4-SUBSTITUTED-(3-SUBSTITUTED-1H-PYRAZOLE-5-AMINO)-PYRIMIDINE DERIVATIVES HAVING ACTIVITY OF INHIBITING PROTEIN KINASE AND USE THEREOF - Provided are derivatives substituted by urea associated with 4-substituted-(3-substituted-1H-pyrazole-5-amino)-pyrimidine-2-amino of formula (I), wherein these compounds may selectively regulate or inhibit an information transmission process controlled by natural or variant tyrosine kinase. Also provided are preparation methods and uses of the compounds. | 12-25-2014 |
20140127294 | ORAL SOLID FORMULATION OF COMPOUND ANTI-TUBERCULAR DRUG AND PREPARATION METHOD THEREOF - Provided is an oral solid preparation of a compound anti-tubercular drug, wherein the active ingredients are rifampicin, isoniazid, pyrazinamide and ethambutol hydrochloride. The compound oral solid preparation is a coated tablet with coated core or a coated three-layer tablet, wherein the two active ingredients rifampicin and isoniazid do not contact directly. The compound oral solid preparation not only improves the stability of the compound preparation, but also improves the bioavailability of rifampicin. | 05-08-2014 |
20140073809 | PREPARATION METHOD FOR RIVASTIGMINE, INTERMEDIATES THEREOF, AND PREPARATION METHOD FOR SAID INTERMEDIATES - The present invention provides the preparation method for (S)-3-(1-(dimethylamino)ethyl)phenyl ethyl(methyl)carbamate (formula X compound), the preparation methods for its intermediates (S)-1-(3-methoxyphenyl)-N,N-dimethyl-N—((S)-1-phenylethyl)ethanaminium (formula VI compound), (S)-1-(3-hydroxyphenyl)-N,N-dimethyl-N—((S)-1-phenylethyl)ethanaminium (formula VIII compound) and (S)-1-(3-(ethyl(methyl)carbamoyloxy)phenyl)-N,N-dimethyl-N—((S)-1-phenylethyl)ethanaminium (formula IX compound), as well as the method for using above mentioned formula IX compound to prepare rivastigmine which can be used for the treatment of Alzheimer's disease. The preparation method for rivastigmine has a reasonable synthetic design with convenient source of raw materials and high total yield, and the product resulted has high chemical and optical purity, which makes it easy for large-scale. industrial production. | 03-13-2014 |
20140011867 | EFFECT OF BORRELIDIN FOR CONTROLLING SOYBEAN PHYTOPHTHORA ROOT ROT - The present invention discloses use of borrelidin for preventing and controlling | 01-09-2014 |
20130225810 | BENZAMIDE DERIVATIVE WITH ANTICANCER ACTIVITY AND PREPARATION METHOD AND USE THEREOF - Provided are a benzamide derivative as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the preparation method and use thereof for preparing a medicine for treating cancer, wherein the group definitions of formula (I) are as set out in the description. | 08-29-2013 |
20130089613 | Compounds Having Activating Effect on Subtypes of Peroxisome Proliferator-Activated Receptors and its Preparation Method and Uses - Phenyl propanoic acid compounds having activating effect on peroxisome proliferator-activated receptors (PPARα,δ,γ) and a preparation method and uses thereof are provided in the present invention. The compounds can be used for treating or preventing diseases associated with peroxisome proliferator-activated receptors (PPARα,δ,γ). | 04-11-2013 |
20120208994 | AZETIDINONE COMPOUNDS AND MEDICAL USE THEREOF - Preparation of azetidinone compounds and medical use thereof are provided by the present invention. More particularly, azetidionne compounds, shown as formula (I), wherein R | 08-16-2012 |
20110319458 | COMPOUND WITH AGITATION EFFECT ON PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR. PROCESS FOR ITS PREPARATION AND USE THEREOF - The present invention provides a novel compound of formula I, which has an agitation effect on the peroxisome proliferator-activated receptor subtype δ (PPARδ), to a pharmaceutical composition comprising the compound, to a process for preparation of the compound and to use of the compound in the manufacture of a medicament for treating or preventing a disease which could be treated or prevented by activating PPARδ thereof, said disease is one or more from the group comprising metabolic syndrome, obesity, dyslipidemia, pathoglycemia, insulin resistance, senile dementia and tumors. The present invention also relates to a new intermediate used in the preparation of the novel compound and a process for preparation of the intermediate. | 12-29-2011 |
20110218221 | NOVEL HISTONE DEACETYLASE INHIBITORS, PROCESS FOR PREPARATION AND USES THEREOF - The present invention relates to compounds represented by formula (I) or composition comprising at least one of such compounds, which are inhibitors of histone deacetylase. The detailed description of these compounds is disclosed in the Description. These compounds and the composition comprising the same may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase (HDAC) activities. | 09-08-2011 |