Abstract: A cabazitaxel weakly-alkaline derivative, preparation, and synthesis thereof, a liposome preparation containing the cabazitaxel weakly-alkaline derivative and application of the cabazitaxel weakly-alkaline derivative in a drug delivery system are provided. Cabazitaxel is connected with a weakly-alkaline intermediate through an ester bond, the ester bond can be broken under the action of esterase in vivo, and an active drug is released. A connecting group is C1-C4 alkyl, C3-C6 naphthenic base or phenyl; [N] is an N-methyl piperazinyl group, a piperidinyl group, a 4-(1-piperidinyl) piperidinyl group, a morpholinyl group, a pyrrolidine group or other tertiary amine structures. The cabazitaxel weakly-alkaline derivative can be prepared into the liposome preparation having high drug loading capacity, high encapsulation efficiency, and good stability.

Abstract: The present invention relates to a 2-aminopyrimidine compound shown in formula I, a pharmaceutically acceptable salt, solvate or prodrug thereof, preparation methods for the 2-aminopyrimidine compound, and the pharmaceutically acceptable salt, solvate or prodrug thereof, and a pharmaceutical composition comprising the compound. Substituents R1, R2, R3, R4, X, Y, Z, Q, m, and n have meanings given in the description. The present invention further relates to the application of the compound of formula I in the preparation of a medication for treating and/or preventing a malignant hematologic disease and other proliferative diseases.

Abstract: In the field of medical technologies, there is a triglyceride prodrug based on lymphatic-mediated transport, particularly a triglyceride prodrug with different linking chains for lymphatic-mediated transport, and a method for preparing the same and use thereof in drug delivery. The prodrugs are linked by different linking bonds and methods for synthesizing the same. The structures of the prodrugs are as follows: wherein X, R1, R2, n, m are as described in the claims and specification. A mechanism of digestion and absorption of glycerol in the gastrointestinal tract is simulated by using a triglyceride-like structure, so as to promote the lymphatic transport of the drugs and avoid a first-pass effect. The prodrugs have targeting properties and can significantly increase or improve oral bioavailability.

Abstract: The present application relates to inhibitors of VGSC?3 protein and use thereof and methods of using the VGSC?3 protein or an inhibitor thereof to diagnose, prevent and treat cancer, and to screen antineoplastic agents using the VGSC?3 Protein or its regulatory sequences.

Abstract: An octahydroanthracene compound having the structure shown in formula (I) and (II), preparation method and application thereof are disclosed. The octahydroanthracene compound has a good therapeutic effect on tumors and neurodegenerative diseases. The preparation of the octahydroanthracene compound is mainly carried out by using benzene as a starting material, and being subjected to Friedel-Crafts reaction, nitration, reduction, (sulfo-) amide formation, reduction, urea formation or amide formation, thus obtaining a target compound.

Abstract: An octahydroanthracene compound having the structure shown in formula (I) and (II), preparation method and application thereof are disclosed. The octahydroanthracene compound has a good therapeutic effect on tumors and neurodegenerative diseases. The preparation of the octahydroanthracene compound is mainly carried out by using benzene as a starting material, and being subjected to Friedel-Crafts reaction, nitration, reduction, (sulfo-) amide formation, reduction, urea formation or amide formation, thus obtaining a target compound.

Abstract: The invention relates to a series of quinoline derivatives of general formula I, pharmaceutically acceptable salts, hydrates, solvates or prodrugs. Thereof M, R1, R2, X, Y and n are defined as claims. And the compounds of general formula I show potent inhibitory activity against c-Met kinase. The present invention further relates to the uses of the compounds, pharmaceutically acceptable salts and hydrates for the preparation of medicaments for the treatment and/or prevention of diseases caused by abnormal expression of c-Met kinase, especially for treatment and/or prevention of cancer.

Abstract: The present invention belongs to the field of medicinal technique, specifically relates to nitrogen-containing heterocyclic ring-substituted dihydroartemisinin derivatives and their optical isomers according to formula I or II; wherein substituent X, Y, R, R1, R2, R3 and R4 are as defined in the Description. The derivatives and compositions thereof can be prepared into clinically acceptable tablets, capsules, injections, ointments, etc., and thus have pharmaceutical uses in the treatment and/or prevention of cancers.

Abstract: The present invention relates to a series of quinoline and cinnoline derivatives of general formula I, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof. And the compounds of general formula I show potent inhibitory activity gainst c-Met kinase. The present invention further relates to the uses of the compounds, pharmaceutically acceptable salts and hydrates for the preparation of medicaments for the treatment and/or prevention of diseases caused by abnormal expression of c-Met kinase, especially for treatment and/or prevention of cancer.

Abstract: The present invention provides an active peptide purified from scorpions, and derivatives, analogs and active fragment which are produced by using genetic engineering technology. The analgesic active peptide VGG is extracted, separated and purified from scorpion, and its amino acid sequence is shown as below: VKDGYIADDRNCPYFCGRNAYCDGECKKNRAESGYCQWASKYGNACWCY KLPDDARIMKPGRCNGG. The present invention further provides a use of the peptides in preparation of an analgesic drug, where the peptide is mixed with a pharmaceutically acceptable carrier to prepare into forms for injection, oral administration, transdermal absorption, and transmucosal absorption.

Abstract: Disclosed are furo[3,2-g]chromene derivatives represented by formula (I), stereoisomers, pharmaceutically acceptable salts, and pharmaceutical compositions thereof, as well as uses thereof as estrogen receptor modulators.

Abstract: The present invention provides an active peptide purified from scorpions, and derivatives, analogues and active fragment which are produced by using genetic engineering technology. The analgesic active peptide VGG is extracted, separated and purified from scorpion, and its amino acid sequence is shown as below: VKDGYIADDRNCPYFCGRNAYCDGECKKNRAESGYCQWASKYGNACWCY KLPDDARIMKPGRCNGG. The present invention further provides a use of the peptides in preparation of an analgesic drug, where the peptide is mixed with a pharmaceutically acceptable carrier to prepare into forms for injection, oral administration, transdermal absorption, and transmucosal absorption.

Abstract: Disclosed are furo[3,2-g]chromene derivatives represented by formula (I), stereoisomers, pharmaceutically acceptable salts, and pharmaceutical compositions thereof, as well as uses thereof as estrogen receptor modulators.

Abstract: The invention relates to 2-methylene-5-substituted-methylenecyclopentanone derivatives of formula I, and the use thereof. The derivatives of formula I as active components are useful for preparing a medicine for the treatment and/or prevention of cancer diseases such as breast cancer, lung cancer, colon cancer, rectal cancer, stomach cancer, prostate cancer, bladder cancer, uterus cancer, pancreatic cancer and ovary cancer. The active compounds of the invention may be used as an anticancer drug alone or used in combination with one or more other antitumor drugs. A combined therapy can be carried out by administrating each therapeutic component concurrently, subsequently or separately.

Abstract: The invention belongs to pharmaceutical field. The invention relates to the compounds according to Formula I, including their optically active forms, pharmaceutically acceptable salts or hydrates, and the pharmaceutical composition comprising thereof as active ingredient; uses in the preparation of vascular endothelial growth factor receptor tyrosine kinase inhibitors, and uses in the preparation of medicament for the treatment and/or prevention of cancer.

Abstract: The invention belongs to pharmaceutical field. The invention relates to the compounds according to Formula I, including their optically active forms, pharmaceutically acceptable salts or hydrates, and the pharmaceutical composition comprising thereof as active ingredient; uses in the preparation of vascular endothelial growth factor receptor tyrosine kinase inhibitors, and uses in the preparation of medicament for the treatment and/or prevention of cancer.

Abstract: The present invention relates to 5-hydroxy-indole-3-carboxylate derivatives of formula I, or racemic mixture or optical isomers or pharmaceutically acceptable salts and/or hydrates thereof, wherein: substituents R1, R2, Z, X and Y are as defined in the description. The compounds of formula I can be useful for preparation of medicament for treatment and/or prophylaxis of virus infections, especially for preparation of medicament for anti-HBV (Hepatitis B virus) and anti-HIV (Human immunodeficiency virus).

Abstract: A protein-phospholipid dispersion preparation in a drug delivery system is provided, in which the weight ratio of protein to phospholipid is 1:300-300:1 and the particle size is between 5 nm and 1000 nm. The preparation process of the said preparation contains the mixture of protein phase and phospholipid phase and the homogenization process. The said drug delivery system can be used in many different pharmaceutical agents.

Abstract: The invention relates to 2-methylene-5-substituted-methylenecyclopentanone derivatives of formula I, and the use thereof. The derivatives of formula I as active components are useful for preparing a medicine for the treatment and/or prevention of cancer diseases such as breast cancer, lung cancer, colon cancer, rectal cancer, stomach cancer, prostate cancer, bladder cancer, uterus cancer, pancreatic cancer and ovary cancer. The active compounds of the invention may be used as an anticancer drug alone or used in combination with one or more other antitumor drugs. A combined therapy can be carried out by administrating each therapeutic component concurrently, subsequently or separately.

Abstract: A composite emulsifier, contains two or more emulsifiers selected from phospholipid, PEG emulsifier and poloxamer-like substance, and may contain cryoprotectant. An emulsion prepared from the composite emulsifier and a preparation method of the emulsion.