Dithiolopyrrolone compounds, the preparation and the use thereof

The invention discloses a dithiolopyrrolone compound represented by formula I or its pharmaceutically acceptable salts, wherein X 1 , R 1 , R 2 , R 3 , R 4 are defined as in the description. The invention also discloses the preparation of such compounds, and the use of such compounds in preparation of medicaments for increasing peripheral white blood cells and in preparation of ancillary medicaments for inhibiting the decrease of peripheral white blood cells in radiotherapy or chemotherapy.

Platinum (II) compound, preparation method therefor, and pharmaceutical composition and application thereof

Disclosed are a platinum (II) compound, a preparation method therefor, and a pharmaceutical composition and an application thereof. The preparation method comprises the following steps: enabling dihydrate diammine platinum nitrate (4) to react with the carboxylate ligand derivative (5) in water, to produce a platinum (II) compound. Also provided are an application of the platinum (II) compound in preparation of an antitumor drug, and a pharmaceutical composition. The pharmaceutical composition contains an active component and a medicinal carrier, the active component containing the platinum (II) compound, and the mass percentage of the active component being 0.1%-95%. The platinum (II) compound of the present invention is well water-soluble, low toxic, easily prepared, and efficient in antitumor activity.

Acetophenone compound, preparation method thereof, and application thereof in fatty liver prevention and treatment

Disclosed is a compound represented by formula I or a pharmaceutically acceptable salt thereof, preparation method thereof, and use thereof in preventing or treating fatty liver or in preparing pharmaceuticals for weight loss.

Acetophenone compound, preparation method therefor, and application thereof in blood lipid regulation

Disclosed are a compound represented by Formula I or a pharmaceutically acceptable salt thereof, a preparation method therefor, the Formula I, and an application thereof in preparing drugs for regulating blood lipids.

DITHIOLOPYRROLONE COMPOUNDS, THE PREPARATION AND THE USE THEREOF

The invention discloses a dithiolopyrrolone compound represented by formula I or its pharmaceutically acceptable salts, wherein X 1 , R 1 , R 2 , R 3 , R 4 are defined as in the description. The invention also discloses the preparation of such compounds, and the use of such compounds in preparation of medicaments for increasing peripheral white blood cells and in preparation of ancillary medicaments for inhibiting the decrease of peripheral white blood cells in radiotherapy or chemotherapy.

Application of asiatic acid and its derivatives to treat pulmonary fibrosis

Compositions comprising asiatic acid and its derivatives and asiaticoside and the methods of use there of to treat pulmonary fibrosis are provided.

New use of ginsenoside compound-k in manufacturing medicaments

Use of ginsenoside Compound-K, which structural formula is the following: in manufacturing medicaments for prevention or treatment of arthritis.

Therapeutic Formulations Based on Asiatic Acid and Selected Salts Thereof

A highly pure asiaticoside and a pharmaceutical grade asiatic acid can be prepared, along with salts of asiatic acid, for use in formulating therapeutic compositions that are suitable for treating arthritis, psoriasis and other inflammatory diseases, as well as pulmonary fibrosis, diabetic nephropathy, and other fibrotic diseases.

Amorphous asiatic tromethamine salt and preparation method thereof

An amorphous asiatic tromethamine salt and the preparation method thereof. The method includes the steps of: (1) dissolving asiatic acid in an organic solvent; step (2) mixing with tromethamine; step (3) stirring and salifying the same, and then removing the organic solvent. The method for preparing the amorphous asiatic tromethamine salt is easy and effective, and the water solubility and bioavailability of the asiatic tromethamine salt thus obtained are greatly compared with the prior art.

Amide compound, preparation method and uses thereof

Disclosed are amide compounds, preparation method and uses thereof, specifically, the compounds represented by formula I or pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, Q, X and n are defined as in the description. Also disclosed are a method for preparing the compounds of formula I, a composition containing the compounds, and the uses of the same in the preparation of medicaments for regulating blood lipid and/or preventing gallstone. The compounds of formula I disclosed in the present invention have stability in vitro, good solubility in the pharmaceutical organic solvents and favorable bioavailability in animals.

Application of depolymerized holothurian glycosaminoglycans (DHG) in preparation of drug for prevention and treatment of thromboembolic diseases

The present invention discloses an application of depolymerized holothurian glycosaminoglycans (DHG) in preparation of a drug for the prevention and treatment of thromboembolic diseases. The DHG is more than one type of DHG with weight-average molecular weights between 26,000 and 45,000 Da. When being intravenously or subcutaneously injected, the drug using the DHG with weight-average molecular weights between 26,000 and 45,000 Da as an active ingredient has a significant anticoagulant effect, while at the same time, has little side effects, and is effective for use in the prevention and treatment of the thromboembolic diseases. For an injection of DHG with weight-average molecular weights between 26,000 Da and 45,000 Da, the blood coagulation time is prolonged and the anticoagulant effect is enhanced as the dosage increases; the subcutaneous administration is used and is more favorable for use in the drug, and the convenience and safety of use the drug are improved.

Therapeutic formulations based on asiatic acid and selected salts thereof

A highly pure asiaticoside and a pharmaceutical grade asiatic acid can be prepared, along with salts of asiatic acid, for use in formulating therapeutic compositions that are suitable for treating arthritis, psoriasis and other inflammatory diseases, as well as pulmonary fibrosis, diabetic nephropathy, and other fibrotic diseases.

USE OF SEA CUCUMBER GLYCOSAMINOGLYCAN IN PREPARING MEDICINE FOR PREVENTION AND TREATMENT OF THROMBOEMBOLIC DISEASE

The present invention discloses use of sea cucumber glycosaminoglycan in the preparation of drugs. In particular, the present invention relates to use of medical use of sea cucumber glycosaminoglycan, and more particularly to use of depolymerized sea cucumber glycosaminoglycan or natural molecular segments of sea cucumber glycosaminoglycan with a weight average molecular weight greater than 54,500 Da in the preparation of a drug for the prevention and treatment of thromboembolic diseases. Thromboembolic diseases include atherosclerotic thrombotic diseases, venous thromboembolic diseases, hypercoagulable states and postoperative thrombosis or treatment of postoperative thrombi. The present invention has a wide treatment window for thromboembolic diseases, has a higher level of safety, and has good development and research value. 1. A method of preventing or treating arterial thromboembolic disease , comprising administering one or more segments of depolymerized sea cucumber glycosaminoglycan or natural molecular segments of sea cucumber glycosaminoglycan having a weight average molecular weight greater than 54 ,500 Da to a patient in need thereof.2. The method according to claim 1 , wherein claim 1 , the arterial thromboembolic disease is selected from the group consisting of: atherosclerotic thrombotic diseases claim 1 , venous thromboembolic diseases claim 1 , hypercoagulable states claim 1 , thrombi formed after an operation claim 1 , prevention of the formation of thrombi after an operation claim 1 , and combinations thereof.3. The method according to claim 1 , wherein the depolymerized sea cucumber glycosaminoglycan or the natural molecular segments of sea cucumber glycosaminoglycan with a weight average molecular weight greater than 54 claim 1 ,500 Da is selected from the group consisting of: a depolymerized sea cucumber glycosaminoglycan of any weight average molecular weight claim 1 , a natural molecular segments of sea cucumber glycosaminoglycan with a ...

AMORPHOUS ASIATIC TROMETHAMINE SALT AND PREPARATION METHOD THEREOF

An amorphous asiatic tromethamine salt and the preparation method thereof. The method includes the steps of: (1) dissolving asiatic acid in an organic solvent; step (2) mixing with tromethamine; step (3) stirring and salifying the same, and then removing the organic solvent. The method for preparing the amorphous asiatic tromethamine salt is easy and effective, and the water solubility and bioavailability of the asiatic tromethamine salt thus obtained are greatly compared with the prior art. 1. An amorphous asiatic tromethamine salt.2. The amorphous asiatic tromethamine salt as defined in claim 1 , wherein the amorphous asiatic tromethamine salt is prepared by the following method: step (1) a solution of asiatic acid is prepared by dissolving asiatic acid in an organic solvent; step (2) said solution is mixed with tromethamine; step (3) salt forming reaction is carried out under stirring claim 1 , and the organic solvent is removed.3. The amorphous asiatic tromethamine salt as defined in claim 2 , wherein claim 2 , the molar ratio between the asiatic acid and the tromethamine is 0.8:1˜1:1.5.4. The amorphous asiatic tromethamine salt as defined in claim 2 , wherein claim 2 , in step (1) claim 2 , the organic solvent is selected from alcohols solvent claim 2 , preferably is one or more selected from the group consisting of saturated monohydric alcohols with 1-5 carbon(s) and aromatic alcohols with 7-8 carbons claim 2 , more preferably is one or more selected from the group consisting of methanol claim 2 , anhydrous ethanol claim 2 , isopropanol claim 2 , n-butyl alcohol claim 2 , n-amyl alcohol claim 2 , benzyl alcohol and n-propanol.5. The amorphous asiatic tromethamine salt as defined in claim 2 , wherein in step (1) claim 2 , the dissolution accompanies with heating.6. The amorphous asiatic tromethamine salt as defined in claim 2 , wherein in step (2) claim 2 , the mixing temperature is 50˜100° C.7. The amorphous asiatic tromethamine salt as defined in claim 2 , ...

APPLICATION OF DEPOLYMERIZED HOLOTHURIAN GYLCOSAMINOGLYCANS (DHG) IN PREPARATION OF DRUG FOR PREVENTION AND TREATMENT OF THROMBOEMBOLIC DISEASES

The present invention discloses an application of depolymerized holothurian glycosaminoglycans (DHG) in preparation of a drug for the prevention and treatment of thromboembolic diseases. The DHG is more than one type of DHG with weight-average molecular weights between 26,000 and 45,000 Da. When being intravenously or subcutaneously injected, the drug using the DHG with weight-average molecular weights between 26,000 and 45,000 Da as an active ingredient has a significant anticoagulant effect, while at the same time, has little side effects, and is effective for use in the prevention and treatment of the thromboembolic diseases. For an injection of DHG with weight-average molecular weights between 26,000 Da and 45,000 Da, the blood coagulation time is prolonged and the anticoagulant effect is enhanced as the dosage increases; the subcutaneous administration is used and is more favorable for use in the drug, and the convenience and safety of use the drug are improved. 1. An application of depolymerized holothurian glycosaminoglycan (DHG) in preparation of a drug for prevention and treatment of thromboembolic diseases , the drug comprising depolymerized holothurian glycosaminoglycan and a pharmaceutically acceptable carrier , in which the depolymerized holothurian glycosaminoglycan is more than one type of depolymerized holothurian glycosaminoglycans with weight-average molecular weights between 26 ,000 Da and 45 ,000 Da.2. An application of depolymerized holothurian glycosaminoglycan (DHG) in preparation of a drug for prevention or treatment of peripheral vascular thrombosis obliterans diseases , the drug comprising depolymerized holothurian glycosaminoglycan and a pharmaceutically acceptable carrier , in which the depolymerized holothurian glycosaminoglycan is more than one type of depolymerized holothurian glycosaminolycans with weight-average molecular weights between 26 ,000 Da and 45 ,000 Da.3. An application of depolymerized holothurian glycosaminoglycan (DHG) ...

Panaxadiol glycoside derivative and preparation method and application thereof

The invention discloses a panaxadiol glycoside derivative and a preparation method and application thereof. Such compounds show strong anti-inflammatory effects in vitro and in animal model experiments, and thus can be used to prepare anti-inflammatory drugs, especially can be used for treating asthma and COPD. In the experiment, the above-mentioned compounds have obvious effects on asthma and COPD, and the efficacy of the high-dose group is superior than that of dexamethasone and budesonide. Even under the dose much exceeding the therapeutic dose, no obvious affect on blood routine and blood glucoseis observed. It has high industrial prospects in the field of anti-inflammatory drugs, especially in the field for treating asthma and COPD.

AMIDE COMPOUND, PREPARATION METHOD AND USES THEREOF

Disclosed are amide compounds, preparation method and uses thereof, specifically, the compounds represented by formula I or pharmaceutically acceptable salts, wherein R, R, R, R, R, Q, X and n are defined as in the description. Also disclosed are a method for preparing the compounds of formula I, a composition containing the compounds, and the uses of the same in the preparation of medicaments for regulating blood lipid and/or preventing gallstone. The compounds of formula I disclosed in the present invention have stability in vitro, good solubility in the pharmaceutical organic solvents and favorable bioavailability in animals. 3. The compounds represented by formula I according to claim 1 , or pharmaceutically acceptable salts thereof claim 1 , wherein:R1 is mono-substituted or poly-substituted phenyl, wherein the substituent on the phenyl is characterized by having at least one hydroxy substituent;R2 and R8 are independently select from mono-substituted or di-substituted phenyl, wherein the substituent on the phenyl is halogen, C1-C6 alkyl or C1-C6 alkoxy;R3, R4, R5, R6 and R7 are independently selected from H or substituted or non-substituted C1-C6 alkyl;Q is methylene;X is oxygen;m is an integer from 0 to 5; andn is an integer from 0 to 5;4. The compounds represented by formula I according to claim 1 , or pharmaceutically acceptable salts thereof claim 1 , wherein R1 is p-hydroxyphenyl.5. The compounds represented by formula I according to claim 1 , or pharmaceutically acceptable salts thereof claim 1 , wherein R2 and R8 are 2 claim 1 ,5-dimethylphenyl.6. The compounds represented by formula I according to claim 1 , or pharmaceutically acceptable salts thereof claim 1 , wherein R3 claim 1 , R4 claim 1 , R6 and R7 are methyl.7. The compounds represented by formula I according to any one of the to claim 1 , or pharmaceutically acceptable salts thereof claim 1 , wherein both m and n are 3.8. The compounds represented by formula I according to claim 1 , or ...

HETEROCYCLIC COMPOUNDS FOR TREATING PSORIASIS

Disclosed herein is a method of treating psoriasis involving the use of compound of formula I and/or a pharmaceutically acceptable salt thereof 2. The method of claim 1 , wherein X is N.3. The method of claim 1 , wherein X is C—R claim 1 , and R is H claim 1 , halo claim 1 , alkyl claim 1 , haloalkyl claim 1 , —CN claim 1 , or alkoxy.4. The method of claim 1 , wherein Y is aryl optionally substituted with at least one group selected from halo claim 1 , alkyl claim 1 , alkenyl claim 1 , alkoxy claim 1 , alkynyl claim 1 , aryl claim 1 , cycloalkyl claim 1 , heteroaryl claim 1 , heterocyclyl claim 1 , —OH claim 1 , —CN claim 1 , —COOR claim 1 , —SONRR claim 1 , —CONRR claim 1 , and —NRR claim 1 , wherein each of the group alkyl claim 1 , alkenyl claim 1 , alkoxy claim 1 , alkynyl claim 1 , aryl claim 1 , cycloalkyl claim 1 , heteroaryl and heterocyclyl is optionally substituted with at least one group selected from alkoxy claim 1 , alkyl claim 1 , halo claim 1 , OH claim 1 , —CN claim 1 , —COOR claim 1 , —SONRR claim 1 , —CONRR claim 1 , and —NRR claim 1 , wherein Rand Rare as defined in .5. The method of claim 1 , wherein Y is 1H-indenyl or 1 claim 1 ,2-dihydronaphthalene claim 1 , optionally substituted with at least one group selected from halo claim 1 , alkyl claim 1 , h claim 1 , alkenyl claim 1 , alkoxy claim 1 , alkynyl claim 1 , aryl claim 1 , cycloalkyl claim 1 , heteroaryl claim 1 , heterocyclyl claim 1 , —OH claim 1 , —CN claim 1 , —COORa claim 1 , —SO2NRaRb claim 1 , —CONRaRb claim 1 , and —NRaRb claim 1 , wherein each of the group alkyl claim 1 , alkenyl claim 1 , alkoxy claim 1 , alkynyl claim 1 , aryl claim 1 , cycloalkyl claim 1 , heteroaryl and heterocyclyl is optionally substituted with at least one group selected from alkoxy claim 1 , alkyl claim 1 , halo claim 1 , OH claim 1 , —CN claim 1 , —COOR claim 1 , —SONRR claim 1 , —CONRaRb claim 1 , and —NRaRb claim 1 , and wherein Rand Rare as defined in .6. The method of claim 1 , wherein Y is a ...

PLATINUM (II) COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF

Disclosed are a platinum (II) compound, a preparation method therefor, and a pharmaceutical composition and an application thereof. The preparation method comprises the following steps: enabling dihydrate diammine platinum nitrate (4) to react with the carboxylate ligand derivative (5) in water, to produce a platinum (II) compound. Also provided are an application of the platinum (II) compound in preparation of an antitumor drug, and a pharmaceutical composition. The pharmaceutical composition contains an active component and a medicinal carrier, the active component containing the platinum (II) compound, and the mass percentage of the active component being 0.1%-95%. The platinum (II) compound of the present invention is well water-soluble, low toxic, easily prepared, and efficient in antitumor activity. 2. The platinum (II) compound represented by Formula I defined as claim 1 , wherein the Chydrocarbyl defined in Rand Ris a Chydrocarbyl; the saturated or unsaturated carbon ring with 3-12 ring atoms defined in Rand Ris a saturated or unsaturated carbon ring with 4-8 ring atoms.3. The platinum (II) compound represented by Formula I defined as claim 2 , wherein the saturated or unsaturated carbon ring with 4-8 ring atoms defined in Rand Ris a saturated carbon ring with 6 ring atoms.4. (canceled)5. (canceled)6. The platinum (II) compound represented by Formula I defined as claim 1 , wherein the platinum (II) compound represented by Formula I is cis-3-hydroxy-acrylic acid diammine platinum (II); or cis-3-hydroxy-acrylic acid (trans-(−)-1 claim 1 ,2-diaminocyclohexane) platinum (II).8. The method for preparing the platinum (II) compound represented by Formula I defined as claim 7 , wherein Ris a Chydrocarbyl.9. The method for preparing the platinum (II) compound represented by Formula I defined as claim 8 , wherein the Chydrocarbyl defined in Ris an ethyl.10. The method for preparing the platinum (II) compound represented by Formula I defined as claim 7 , wherein the ...

Acetophenone Compound, Preparation Method Therefor, And Application Thereof In Blood Lipid Regulation

Disclosed are a compound represented by Formula I or a pharmaceutically acceptable salt thereof, a preparation method therefor, the Formula I, and an application thereof in preparing drugs for regulating blood lipids. 5. The compound of Formula I or a pharmaceutically acceptable salt thereof according to claim 1 , wherein Ris pyridin-3-yl.6. The compound of Formula I or a pharmaceutically acceptable salt thereof according to claim 1 , wherein Ris 2 claim 1 ,5-dimethyl phenyl.7. The compound of Formula I or a pharmaceutically acceptable salt thereof according to claim 1 , wherein n is 3.10. A pharmaceutical composition comprising the compound of Formula I or a pharmaceutically acceptable salt thereof as defined in claim 1 , as well as a pharmaceutically acceptable additive.11. The pharmaceutical composition according to claim 10 , wherein the pharmaceutical composition is in a form of tablet claim 10 , pill claim 10 , powder claim 10 , liquid claim 10 , suspension claim 10 , emulsion claim 10 , granule claim 10 , capsule claim 10 , suppository or injection.12. A medicament fo regulating blood lipids comprising the compound of Formula I or a pharmaceutically acceptable salt thereof as defined in .16. The compound of Formula I or a pharmaceutically acceptable salt thereof according to claim 2 , wherein Ris pyridin-3-yl.17. The compound of Formula I or a pharmaceutically acceptable salt thereof according to claim 3 , wherein Ris pyridin-3-yl.18. The compound of Formula I or a pharmaceutically acceptable salt thereof according to claim 4 , wherein Ris pyridin-3-yl.19. The compound of Formula I or a pharmaceutically acceptable salt thereof according to claim 2 , wherein Ris 2 claim 2 ,5-dimethyl phenyl.20. The compound of Formula I or a pharmaceutically acceptable salt thereof according to claim 3 , wherein Ris 2 claim 3 ,5-dimethyl phenyl. The invention belongs to the field of design and synthesis of new medicaments, and particularly relates to new aminoacetophenone- ...

Acetophenone Compound, Preparation Method Thereof, And Application Thereof In Fatty Liver Prevention And Treatment

Disclosed is a compound represented by formula I or a pharmaceutically acceptable salt thereof, preparation method thereof, and use thereof in preventing or treating fatty liver or in preparing pharmaceuticals for weight loss.

Acetophenone compound, preparation method therefor, and application thereof in fatty liver prevention and treatment

Disclosed is a compound represented by formula I or a pharmaceutically acceptable salt thereof, preparation method thereof, and use thereof in preventing or treating fatty liver or in preparing pharmaceuticals for weight loss.

Amide compound, preparation method and uses thereof

Panaxadiol glycoside derivative and preparation method and application thereof

The invention discloses a panaxadiol glycoside derivative and a preparation method and application thereof. Such compounds show strong anti-inflammatory effects in vitro and in animal model experiments, and thus can be used to prepare anti-inflammatory drugs, especially can be used for treating asthma and COPD. In the experiment, the above-mentioned compounds have obvious effects on asthma and COPD, and the efficacy of the high-dose group is superior than that of dexamethasone and budesonide. Even under the dose much exceeding the therapeutic dose, no obvious affect on blood routine and blood glucoseis observed. It has high industrial prospects in the field of anti-inflammatory drugs, especially in the field for treating asthma and COPD.