Zhejiang Ausun Pharmaceutical Co., Ltd.

Henan Genuine Biotech Co., Ltd.

Nanjing Molecular Research, Inc.

Other

Irm LLC

Zhengzhou University

Zhengzhou Granlen Pharmatech. Ltd.

High & New Technology Research Center, Henan Academy of Sciences

Henan Analysis Testing Center

Junbiao Chang

Chuanjun Song

Jinfa Du

Kaikai Zhu

Kai Wang

Zheng Wang

Shifeng Pan

Qiang Huang

Haoyun An

Runcong Liu

Dongxu Yi

Suping Zhou

Chunxia Zhang

Xuejun Yu

Jianyong Li

Xiaohe Guo

A 2-(2,4,5-substituted phenylamino) pyrimidine derivative, having the following chemical formula I: The pyrimidine derivative is useful for treating non-small cell lung cancer.

2-(2,4,5-substituted phenylamino) pyrimidine derivative and crystalline form B thereof

The present invention discloses a crystal form, a preparation method and an application of a 4'-substituted nucleoside compound I having the following structure, including salts, prodrugs, and compositions thereof. Animal pharmacokinetic studies demonstrated that the effective drug concentrations of Compound Ia and Compound Ig in HIV target cells, peripheral blood mononuclear cells (PBMC), were effective in inhibiting HIV replication after 7 and 5 days, respectively. Therefore, Compound I can be used as a long-acting drug for preventing and treating AIDS. R is selected from ethynyl, azide, and cyano groups, X is selected from hydrogen and fluorine, and B is selected from B1 and B2.

Crystal form, preparation method, and application of 4'-substituted nucleoside

A compound represented by formula I or II. X represents a mono substituent on a benzene ring, and is selected from &#x2014;H, &#x2014;I, &#x2014;Br, &#x2014;Cl, &#x2014;F, &#x2014;CN, an amino, and a derivative thereof; Ris a Calkyl, Calkyl substituted by cyclopropane or fluorine, except n-butyl; and M is an amine ion or metal ion.

Benzoic acid compound and method for preparing the same

The present invention discloses 5-bromo-2-(&#x3b1;-hydroxypentyl)benzoic acid sodium salt in different crystal forms and the preparation methods thereof, and belongs to the field of pharmaceutical chemistry. Said different crystal forms of 5-bromo-2-(&#x3b1;-hydroxypentyl)benzoic acid sodium salt include: amorphous 5-bromo-2-(&#x3b1;-hydroxypentyl)benzoic acid sodium salt, crystal form A of 5-bromo-2-(&#x3b1;-hydroxypentyl)benzoic acid sodium salt, and crystal form B of 5-bromo-2-(&#x3b1;-hydroxypentyl)benzoic acid sodium salt. The different crystal forms of 5-bromo-2-(&#x3b1;-hydroxypentyl)benzoic acid sodium salt obtained according to the present invention have better stability and water-solubility than the mixed forms of 5-bromo-2-(&#x3b1;-hydroxypentyl)benzoic acid sodium salt, thus is advantageous for pharmaceutical use. Moreover, the different crystal forms of 5-bromo-2-(&#x3b1;-hydroxypentyl)benzoic acid sodium salt possess much better therapeutic effect than 5-bromo-2-(&#x3b1;-hydroxypentyl)benzoic acid potassium salt.

5-bromo-2-(alpha-hydroxypentyl)benzoic acid sodium salts in different crystal forms, and preparation method thereof

The disclosure relates to a thienopyrimidinone derivative, or a pharmaceutically acceptable prodrug, salt, and solvate thereof. The derivative has the formula (I), where R represents hydrogen (H) or deuterium (D); Rand Rindependently, at each occurrence, represent H, D, F, Cl, I, cyano group (CN), or N, and when R represents H, Rand Rdo not synchronously represent H; R, Rand Rindependently, at each occurrence, represent an alkyl group, a cycloalkyl group, a heterocyclic group, an aromatic ring group, or a heteroaryl ring group, which are substituted or unsubstituted.

Thienopyrimidinone derivative and application thereof in preparing anticancer drug

5-bromo-2-(&#x3b1;-hydroxypentyl)benzoic acid sodium salts in different crystal forms, and preparation method thereof

The present invention relates to the field of pharmacochemistry. Disclosed are fluorinated and azido-substituted pyrimidine nucleoside derivatives, particularly compounds of the formula shown below: Also disclosed are methods of preparation and uses for these compounds. The compounds can be used for preparing medicaments for treating diseases such as tumors and viral infections, and can be used separately or in combination with other medicaments. The compounds also have effective activity against diseases such as tumors and viral infections, while having few side effects, and thus have potential application value.

Pyrimidine nucleoside derivatives, synthesis methods and uses thereof for preparing anti-tumor and anti-virus medicaments

This application discloses phosphoramidate and phosphonoamidate prodrugs of alcohol-based therapeutic agents, such as nucleosides, nucleotides, acyclonucleosides, C-nucleosides, and C-nucleotides, and use of these prodrugs for treatment of diseases or disorders, including infectious diseases and cancers. This application also discloses a general method for enhancing bioavailability and/or liver-targeting property of alcohol drugs through converting the alcohol drugs to phosphoramidate or phosphonoamidate prodrugs, and methods of preparation of these prodrugs.

Double-liver-targeting phosphoramidate and phosphonoamidate prodrugs

This application discloses novel phosphoramidate and phosphonoamidate prodrugs of nucleosides, nucleotides, C-nucleosides, C-nucleotides, phosphonates, and other alcohol-containing drugs; use of these prodrugs for treatment of infectious diseases and cancers, in particular, liver infections and cancers; and methods of preparing these novel phosphoramidate and phosphonoamidate prodrugs.

O-(substituted benzyl) phosphoramidate compounds and therapeutic use

The present invention provides 2'-fluorine-4&#x2032;-substituted-nucleoside analogs or their pro-drugs or 5&#x2032;-phosphate esters (including the pro-drugs of the 5&#x2032;-phosphate esters), preparation methods and uses thereof. The compounds have the general formula as follows: wherein:  The compounds are used in the synthesis of drugs for the treatment of virus infection, especially for the treatment of HBV, HCV or HIV infection.

2'-fluorine-4&#x2032;-substituted-nucleoside analogues, preparation methods and uses thereof

This invention provides methods for the solution-phase synthesis of arylbenzoxazoles. The methods involve condensation of aminophenols with benzaldehydes to form a Schiff base. The Schiff base is then induced to undergo oxidative cyclization in the presence of DDQ. The resulting arylbenzoxazoles can be separated from the reduced DDQ byproduct by treatment of reaction mixture with a strongly basic ion exchange resin.

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Zhengzhou, China

Junbiao Chang