Shanghai Institute of Materia Medica, Chinese Academy of Sciences Patent applications |
Patent application number | Title | Published |
20150141644 | PYRROLO[2,1-F][1,2,4]TRIAZINE COMPOUND, AND PREPARATION METHOD AND APPLICATION THEREOF - The present invention relates to a pyrrolo[2,1-f][1,2,4]triazine compound, an isomer thereof or a pharmaceutically acceptable salt, ester or hydrate thereof, and a preparation method and application thereof. The pyrrolo[2,1-f][1,2,4]triazine compound has a structure expressed in general formula (I). The pyrrolo[2,1-f][1,2,4]triazine compound expressed in general formula (I) can inhibit a phosphatidylinositol-3 kinase (PI3K) signal pathway, thereby being used to prepare medicine for treating phosphatidylinositol-3 kinase related diseases such as cancer. | 05-21-2015 |
20140128421 | CAMPTOTHECIN COMPOUND CONTAINING STABLE 7-MEMBERED LACTONE RING, PREPARATION METHOD AND USE - Provided are a camptothecin compound containing 7-membered lactone ring, as shown in general formula I, and pharmaceutically acceptable salt thereof, as well as the preparation method and use thereof. In general formula I, R | 05-08-2014 |
20140088130 | HEXAHYDRODIBENZO[A,G]QUINOLIZINE COMPOUND, PREPARATION METHOD THEREOF, PHARMACEUTICAL COMPOSITION AND USE THEREOF - The present invention relates to a novel hexahydrodibenzo[a,g]quinoline compound represented by general formula (I) and its derivatives, enantiomer, diastereoisomer, raceme and mixtures thereof, as well as pharmaceutically acceptable salts thereof. The present invention further relates to a method for preparing the compound, and the compound has good prevention and treatment effect on neurological diseases, especially diseases associated with dopamine receptor and 5-hydroxytryptamine receptor. The bioactivity experiment demonstrates that, the compound is expected to be developed into a novel and potent chemical entity for treating diseases associated with dopamine receptor and 5-hydroxytryptamine receptor, especially schizophrenia, Parkinson's disease, drug addiction, migraine and so on. | 03-27-2014 |
20140058074 | USE OF 3,8,12,14, 17,20-OXO-SUBSTITUTED PREGNENE GLYCOSIDES IN THE PREPARATION OF HEALTHCARE PRODUCTS, FOOD ADDITIVES AND PHARMACEUTICALS FOR THE INHIBITION OF APPETITE - The present invention relates to the use of 3,8,12,14,17,20-oxo-substituted pregnene glycosides having the following formula I in the preparation of healthcare products, food additives and drugs for losing body weight, controlling body weight and inhibiting appetite of human beings or animals, wherein, R | 02-27-2014 |
20140031554 | PROCESS FOR PREPARING RACEMIC NICOTINE - Provided is a process for preparing racemic nicotine from 1-methyl-3-nicotinoyl-2-pyrrolidone or a salt thereof using one-pot process. The process comprises the following steps: 1) in a reaction vessel, reacting 1-methyl-3-nicotinoyl-2-pyrrolidone or a salt thereof in the presence of a suitable solvent and a strong acid by heat; after the reaction is complete, cooling the same and adjusting the pH to 7-8 with alkali; and 2) directly adding a reductant into the above vessel, and after the reaction, purifying the product so as to obtain high purity racemic nicotine or a salt thereof. | 01-30-2014 |
20130324542 | [1,2,4]TRIAZOLO[4,3-B][1,2,4]TRIAZINE COMPOUNDS, PREPARATION METHOD AND USE THEREOF - The present invention relates to a structurally novel [1,2,4]triazolo[4,3-b][1,2,4]triazine compounds represented by formula (I) or formula (II), pharmaceutically acceptable salts thereof, prodrugs thereof, hydrates or solvates thereof, and also relates to a preparation method of the compounds, a pharmaceutical composition including a therapeutically effective amount of the compounds, as well as the use thereof as protein tyrosine kinase inhibitors, particularly as c-Met inhibitors, in the preparation of medicaments for the prevention and/or treatment of diseases associated with c-Met abnormality. | 12-05-2013 |
20130317095 | Use of Artemisine Derivatives and Pharmaceutical Salts Thereof - The invention demonstrates the application of an artemisinin derivative and its pharmaceutical salt. The artemisinin derivatives diarteether amine and its pharmaceutical salt inhibit the proliferation of leukemic cells, block the cell cycle of leukemic cells and induce the apoptosis of leukemic cells. Artemisinin derivatives of the present invention and its pharmaceutical salt can be used for the preparation of anti-leukemia medicines, especially for treatment of acute leukemia and, what's more, for the treatment of acute myeloid leukemia. | 11-28-2013 |
20130295579 | METHOD FOR PREPARING INDUCED PLURIPOTENT STEM CELLS AND MEDIUM USED FOR PREPARING INDUCED PLURIPOTENT STEM CELLS - A method for preparing induced pluripotent stem (iPS) cells, which comprises steps as follows: step 1, introducing one or more stem cell pluripotency factors into somatic cells; step 2, culturing the somatic cells, into which the stem cell pluripotency factor has been introduced in the Step 1, by using medium supplemented with lithium salt; and step 3, identifying and characterizing the induced pluripotent stem cells. Furthermore, there provided a medium for preparing induced pluripotent stem cells, which comprising lithium salt. The medium supplemented with lithium salt is used for efficiently inducing pluripotent stem cells. Lithium salt is able to increase the production efficiency of mouse iPS cells by 5-60 times. The present method for inducing iPS cells is in favor of improving the safety of iPS technique and application of iPS cells in regenerative medicine. | 11-07-2013 |
20130281426 | PYRIDAZINONES, THE PREPARATION METHOD AND THE USE THEREOF - The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer. | 10-24-2013 |
20130261139 | USE OF A QUINAZOLINE COMPOUND IN PREPARING A MEDICAMENT AGAINST FLAVIVIRIDAE VIRUS - Disclosed is a use of a quinazoline compound of Formula I having 2,4-diaminoquinazoline as a parent nucleus in preparation of a medicament for treating diseases caused by flaviviridae infection, especially a use in combating Hepatitis C virus infection and Dengue fever virus infection. | 10-03-2013 |
20130005696 | BUFADIENOLIDE DERIVATIVES, PREPARING PROCESS THEREOF, COMPOSITION COMPRISING THE SAME AND THE USE THEREOF - The present invention provides a class of bufadienolide derivatives representing by the following formula I or pharmaceutically acceptable salts thereof, the preparing process thereof, pharmaceutical composition comprising the same and the use thereof. The bufadienolide derivatives have inhibitory activities against human-derived tumor cell lines, and thus can be used as a drug for treating malignancies. | 01-03-2013 |
20120301547 | PALIPERIDONE DOUBLE-LAYERED OSMOTIC PUMP CONTROLLED RELEASE TABLET AND PREPARATION METHOD THEREOF - A paliperidone double-layered osmotic pump controlled release tablet and the preparation method thereof are disclosed. The double-layered osmotic pump controlled release tablet comprises a rigid membrane, a push layer, a drug layer, an isolation layer and an aesthetic coating, wherein the rigid membrane contains a semi-permeable polymer, a porogen and/or a plasticizer and has one or more drug release orifices on one end, the push layer comprises an expanding material, an osmotic agent, a binder, a colorant and a lubricant, the drug layer contains a pharmaceutically active ingredient, a hydrophilic polymer, an osmotic agent, a colorant, a lubricant and an antistatic agent, the isolation layer is located between the inner surface of the rigid membrane and the push layer, and contains a hydrophilic polymer. The paliperidone double-layered osmotic pump controlled release tablet shows an increasing drug release rate at early stage and keeps a constant drug release rate at later stage. | 11-29-2012 |
20120277448 | PREPARATION METHOD FOR 3BETA-ARACHIDYLAMIDO-7ALPHA, 12ALPHA, 5BETA-CHOLAN-24-CARBOXYLIC ACID - A method for preparing 3β-arachidylamido-7α,12α,5β-cholan-24-carboxylic acid represented by the following formula V is disclosed, which includes the following steps: converting cholic acid to the compound of formula III by acylation reaction and azidation reaction, reducing the compound of formula III to the compound of formula IV and in the end acylating the compound of formula IV with arachidoyl chloride to get the compound of formula V. The method avoids the use of protection groups. | 11-01-2012 |
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 |
20110263860 | PREPARATION METHODS OF 6-SUBSTITUTED AMINO-3-CYANOQUINOLINE COMPOUNDS AND THE INTERMEDIATES THEREOF - The present invention relates to a method for preparing 6-substituted amino-3-cyanoquinoline compounds (compound A for short) and the intermediates thereof, more particularly, to a compound of the following formula (I), the preparation method thereof, the intermediates thereof and use thereof for preparing the compound A. The compound of the formula (I) is cyclized in the presence of an alkali to give a compound of formula A, wherein W is OH; or the compound of the formula (I) is cyclized in the presence of an alkali, and then chlorinated to give a compound of the formula A, wherein W is Cl. Compared with the known methods in the literature, the method for preparing the compound A from the compound of formula (I) according to the present invention can avoid using high-temperature condition and high boiling point solvents, and is safe and environment-friendly, mild in reaction condition, easy in operation with a high yield and high product purity. | 10-27-2011 |
20110251192 | AMIDE COMPOUNDS, THEIR PHARMACEUTICAL COMPOSITIONS, THEIR PREPARATION METHOD AND THEIR USES - The present invention pertains to the field of pharmaceutical chemistry and discloses 8-(3-aminopropyl)-3-exo-8-azabicyclo[3.2.1]octane-3-amino amide compounds represented by formula I, the pharmaceutical compositions, the preparation method and the use thereof. Such compounds or pharmaceutically acceptable salts thereof can be used as an antagonist of CCR5 in preparing medicaments for treating diseases mediated by CCR5, particularly HIV infection, asthma, rheumatoid arthritis, autoimmune diseases and chronic obstructive pulmonary diseases (COPD). | 10-13-2011 |
20110207921 | SULFATED DERIVATIVE OF GASTRODIA ELATA POLYSACCHARIDE, PREPARATION METHOD AND ANTITUMOR USE THEREOF - The present invention discloses a sulfated derivative of polysaccharide extracted from | 08-25-2011 |
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 |
20110152208 | Use of Compounds Extracted from Momordica Charantia L. in the Manufacture of Medicaments for Prevention and Treatment of Diabetes and Obesity - The present invention disclosed a medical use of cucurbitane triterpenoids represented by the following formula and isolated from | 06-23-2011 |
20110112061 | PYRIDAZINONES, THE PREPARATION AND THE USE THEREOF - The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer. | 05-12-2011 |
20100197927 | Protein Tyrosine Phosphatase 1B Inhibitor, Preparation Methods and Uses Thereof - PTP1B inhibitors with the following structure (formula I). Experiments indicate that these inhibitors can effectively inhibit the activity of protein tyrosine phosphatase 1B (PTP1B). They can be used as insulin sensitisers. They can be used to prevent, delay or treat diseases which are related to insulin antagonism mediated by PTP1B, especially diabetes type II and obesity. The invention also provides methods for preparing these inhibitors. | 08-05-2010 |
20100113498 | NOVEL VINBLASTINE DERIVATIVES, THEIR PREPARATION, USE AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAID DERIVATIVES - The invention provides vinblastine derivatives represented by the following formula 1 or their physiologically acceptable salts, their preparation, use and pharmaceutical compositions comprising the said derivatives. The said vinblastine derivatives show inhibiting activities against tumor cell lines and can be used as medicaments for treating malignant tumors. | 05-06-2010 |
20100113494 | 13,13a-Dihydroberberine Derivatives For Use In Pharmaceutical Compositions - The present invention provides 13,13a-dihydroberberine derivatives or their physiologically acceptable salts represented by the following formula, pharmaceutical compositions comprising the same, and uses thereof. The 13,13a-dihydroberberine derivatives have an activity of promoting glucose absorption in muscle cells, and the whole animal tests show that the present compounds have effects on improving glucose-tolerance and insulin-resistance, facilitating weight loss, relieving fatty liver and the like. Thus, the present compounds can be used in treating diabetes mellitus, adiposity, fatty liver and complications thereof induced by insulin resistance. | 05-06-2010 |
20100056569 | Heterocyclic Non-Nucleoside Compounds, Their Preparation, Pharmaceutical Composition And Their Use As Antiviral Agents - The invention relates a kind of antiviral agents, more concretely, relates to a kind of heterocyclic non-nucleoside compounds with the following structures, their preparation and pharmaceutical compositions including the compounds. The said compounds can be used as antiviral agents and as medicaments for treating diseases such as hepatitis B, influenza, herpes, HIV and so on. | 03-04-2010 |
20080306121 | Bisheterocycle Tandem Compounds Useful as Antiviral Agents, the Uses Thereof and the Compositions Comprising Such Compounds - The present invention provides small molecule compounds of bisheterocycle in tandem having the structural formula of P1-P2, and the use thereof as well as a composition containing the compounds, each of P1 and P2 is an unsaturated 5-member heterocyclic ring having one or two heteroatoms. This compound may effectively inhibit the replication of influenza virus, the DNA replication of hepatitis B virus (HBV), and the formation of HBsAg and HBeAg. These compounds can be used for the preparation of a medicament for viral diseases, and may overcome the limitations of the known nucleosides drugs, including cytotoxicity, the requirement of other drugs having different structures for against the drug-resistant virus variants induced by long-term therapy. The structure of the compounds according to the invention is relatively simple and easy to be prepared. | 12-11-2008 |