Wuhan Ll Science and Technology Development Co., Ltd.

Wuhan Qr Pharmaceuticals Co., Ltd.

Wuhan Zy Pharmaceuticals Co., Ltd.

Yongkai Chen

Chaodong Wang

Li Liu

Jun Lou

Lina Qian

Wei Feng

Xiaodan Guo

Yihan Zhang

Junhua Liu

Sijun Lei

Wei Peng

Liu Hu

Xiang Fang

Anxiao Zheng

Penggao Yu

Hongwei Tang

Xian Zeng

Bo Zhang

Xiaojing Hu

Xiaohua Ding

Dongcheng Dai

Fei Rong

Wenwen Qi

Xueming Liu

Panpan Duan

Yaowen Wan

Zhichao Zhang

Lei Liang

Daiwu Kang

Yuanping Wang

A compound containing a benzene ring as shown in formula I, a pharmaceutically acceptable salt thereof, a stereoisomer thereof, a tautomer thereof, an isotopic compound thereof, a crystal form thereof, a nitrogen oxide thereof, and a solvate thereof or a solvate of the pharmaceutically acceptable salt thereof are provided. The compound has high P2X4 antagonistic activity, good selectivity, low toxicity and good metabolic stability.

Compound containing benzene ring and application thereof

Disclosed by the invention is a heterocyclic compound, an intermediate, and a preparation method therefor and an application thereof. Provided by the invention are a heterocyclic compound as shown in formula I, and a stereoisomer, a geometric isomer, a tautomer, a nitrogen oxide, a hydrate, a solvate, a metabolite, an ester, a pharmaceutically acceptable salt or a prodrug thereof. The heterocyclic compound has a high P2X3 antagonistic activity, and has good selectivity, low toxicity, good metabolic stability and little taste influence.

Heterocyclic compound, intermediate, preparation method therefor and application thereof

Certain compounds are lysophosphatidic acid receptor antagonists have high LPAR1 antagonist activity and selectivity, low toxicity, good metabolic stability, promising pharmaceutical development prospects, and may be used for preventing or treating LPAR1-related diseases or illnesses. The IC50 values of some of the compounds may be as low as 300 nM or below, even 50 nM or below. In addition, CC50 value range of the compounds may be as high as 200 μM or above. Furthermore, the compounds have good metabolic stability in humans, mice and rats.

Lysophosphatidic acid receptor antagonist and preparation method therefor

Certain triazole compounds have good LPAR1 antagonistic activity and selectivity, low toxicity, and good metabolic stability, and can be used for preventing or treating the LPAR1-related disease or disorder. The ICvalue of some triazole compounds can be below 300 nM, even 50 nM. The range of CCof the triazole compounds can be greater than 200 μM. They also show good metabolic stability in human, fancy rats, and house mice.

Triazole compounds and preparation method therefor and use thereof

A complex disintegrant composition for oral solid preparation, comprising a disintegrant and a disintegrating aid, the disintegrant being a hygroscopic expansion type disintegrant, the disintegrating aid being a soluble small molecule substance or a gas-producing type salt. An oral solid preparation, comprising an active ingredient, said complex disintegrant composition, an excipient and a lubricant.

Complex disintegrant system for oral solid preparation and oral solid preparation comprising said complex disintegrant system

A pharmaceutical preparation includes a first active component, a second active component and pharmaceutically acceptable excipients. The first active component is at least one selected from the group consisting of a neutral endopeptidase inhibitor and a precursor, an active metabolite, a stereoisomer, a pharmaceutically acceptable salt, a prodrug and a solvate thereof. The second active component is at least one selected from the group consisting of a compound represented by the following formula (I) or a precursor, an active metabolite, a stereoisomer, a pharmaceutically acceptable salt, a prodrug and a solvate thereof. The pharmaceutically acceptable excipients include one or more disintegrants and/or one or more fillers. 

Pharmaceutical preparation and use thereof

The present disclosure belongs to the field of chemical synthesis, and in particular relates to an ammonium carboxylate compound, a crystalline form and an amorphous form, and a preparation method thereof. The present disclosure prepares the compound and the crystalline form I and its single crystal, amorphous form and crystalline form II thereof. The compound, the crystalline forms, the single crystal and the amorphous form can stably exist and exhibit good solid forms, suitable for medicine-making. Furthermore, these products possess high purity and less single impurity. Moreover, the preparation methods of the present disclosure are easy to implement due to the simple processes with mild reaction conditions, and could produce products of high yield and high purity without complex purification steps. Furthermore, the preparation methods may facilitate safety, environmental protection, and industrial production.

Ammonium carboxylate compound, crystalline form, amorphous form and preparation method thereof

The present invention relates to a pharmaceutical composition comprising: (a) at least one neutral endopeptidase inhibitor or a pharmaceutically acceptable salt or ester thereof, (b) at least one compound represented by formula (I) or a pharmaceutically acceptable salt or ester thereof, and a pharmaceutically acceptable carrier. Combined administration showed better medicinal effects than separate administration. 

Pharmaceutical composition

The present disclosure provides a triazole antibacterial derivative and a pharmaceutical composition thereof and a use thereof and in particular relates to a compound represented by the following formula (I), and a racemate, a stereoisomer, a tautomer, an oxynitride or a pharmaceutically acceptable salt thereof:  The compound of the present disclosure has a desirable water solubility and can be formulated into an injection for use without adding a cosolvent having a potential safety risk (such as hydroxypropyl-&#x3b2;-cyclodextrin, sulfobutylether-&#x3b2;-cyclodextrin, and the like), facilitating drug administration for patients, and greatly improving clinical safety. The drug can be used even by patients with moderate or severe renal impairment, thereby expanding the application scope of the drug.

Triazole antimicrobial derivative, pharmaceutical composition and use thereof

The invention discloses an oral solid preparation containing any one, or a mixture of two or more of crystalline form I, II, III, and IV of the compound represented by formula (A). The oral solid preparation of the present invention disintegrates rapidly, increasing dissolution rate thereof, thereby improving bioavailability. In particular, it is possible to solve the problem that an active material (active ingredient), which is high hygroscopic and becomes sticky after moisture absorption, can not be effectively disintegrated by conventional disintegrants. The present invention further relates to a use of the oral solid preparation in preparing an angiotensin II receptor antagonist or a use thereof in preparing medicine for preventing and/or treating hypertension, chronic heart failure and diabetic nephropathy. 

Oral solid preparation and use thereof

The preparation method for the compound, composition and application thereof in preparing an angiotensin II receptor antagonist or application in preparing medicine for preventing and/or treating hypertension, chronic heart failure and diabetic nephropathy. After entering a human body, when releasing azilsartan, the compound releases hydroxyligustrazine or NO at the same time, thus generating a synergistic effect with azilsartan. The compound therefore has stronger and longer blood pressure lowering effect, more obvious and longer lasting heart rate lowering effect and high safety, and achieves ideal protective effect for heart and kidney functions. 

Potassium salt of benzimidazole compound and preparation method therefor, composition and application thereof

Provided are a preparation method for a crystalline form of the compound represented by formula (A), as well as a method for preparation thereof, a composition thereof, and an application thereof in preparing an angiotensin II receptor antagonist or an application in preparing a drug for preventing and/or treating hypertension, chronic heart failure and diabetic nephropathy.

Crystalline form of chemical compound, and preparation method, composition, and application thereof

The present disclosure provides a posaconazole derivative, a pharmaceutical composition and use thereof, which specifically include a compound represented by the following formula (I), a racemate, stereoisomer, tautomer, oxynitride, or a pharmaceutically acceptable salt thereof:  The compounds of the present disclosure have strong antifungal activity, high safety, and good water solubility, without the need for the addition of a cosolvent (such as hydroxypropyl-&#x3b2;-cyclodextrin, sulfobutyl ether-&#x3b2;-cyclodextrin, and the like) with potential safety risks. Furthermore, the formulation process of the compound could have less difficulty and less cost, and therefore can be used to prepare improved antifungal drugs.

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Hubei, China

Yongkai Chen