Hangzhou Solipharma Co., Ltd.

Hangzhou Pushai Pharmaceutical Technology Co., Ltd.

Hangzhou Pushai Pharmaceutical Technology

Hangzhou Pushai Pharmaeutical Technology Co., Ltd.

Xiaohong Sheng

Xiaoxia Sheng

Tao Zhu

Haiping Lao

Jianfeng Zheng

Xiaoye Song

Jing Wang

Qiang Jia

Yanli Dai

Chenyang Hu

Kun Zhao

Jian Chen

Xiawei Jiang

Xiangjun Shi

Yu Dai

Zhonghua Zhang

Yinghua Shao

The present application provides a crystalline form of tolebrutinib, an amorphous form, and a method of preparation thereof and a use thereof, and the crystalline form of tolebrutinib provided in the present application has at least one of the following advantages: good stability, low moisture attraction, uniform particle size distribution, solubility meeting the requirements for medicinal use, stable storage, avoiding phase transformation of the drug in the process of development and in storage, and a reliable method for the preparation thereof, which has a great development value. The amorphous form of tolebrutinib provided in this application, while possessing better solubility than that of tolebrutinib in the crystalline state, still possesses good stability of placement and acceptable hygroscopicity, and has high medicinal value.

Crystal and amorphous form of tolebrutinib, preparation method therefor, and use thereof

Crystalline forms of ACP-196, preparation methods, pharmaceutical compositions and uses thereof in the preparation of drugs for treatment and/or prevention of Bruton's tyrosine kinase (BTK)-mediated disorders such as autoimmune diseases or disorders, heteroimmune diseases or disorders, cancers including lymphoma and inflammatory diseases or disorders. As compared with the known solid form of ACP-196, the crystalline forms of the present invention have advantages in crystallinity.

Crystal form of ACP-196 and method of treatment thereof

The present invention relates to novel crystal forms of tipifarnib. Compared with the prior art, the crystal forms of tipifarnib have advantages in crystallinity, hygroscopicity, morphology, form stability and chemical stability. The present invention also relates to the preparation methods of crystal forms of tipifarnib, pharmaceutical composition thereof and their use in preparation for treating and/or preventing abnormal cell growth diseases.

Crystal form of tipifarnib and method of treatment thereof

The present invention relates to Form IV of fenofibrate and its preparation methods thereof. Its X-ray powder diffraction pattern expressed as 2&#x3b8; angle has characteristic peaks at 14.15&#xb1;0.2&#xb0;, 15.94&#xb1;0.2&#xb0;, 16.49&#xb1;0.2&#xb0;, 17.45&#xb1;0.2&#xb0;, 20.21&#xb1;0.2&#xb0;, and 22.87&#xb1;0.2&#xb0;. The present invention also provides preparation methods of Form IV. The preparation methods are simple, easy to operate, short, and have good repeatability. The methods are also non-toxic and non-polluting by using water as a medium and using a pharmaceutically accepted excipient, such as polyvinylpyrrolidone or polyvinyl alcohol as an inducer. The results of stability experiments (light exposure, high humidity and grinding) and solubility tests show that Form IV is stable and has a higher solubility than the prior art crystal form.

Fenofibrate crystalline form and manufacturing method thereof

The present invention relates to co-crystals of ribociclib and co-crystals of ribociclib monosuccinate, comprising the co-crystal of ribociclib and saccharin, the co-crystal of ribociclib and cholic acid, the co-crystal of ribociclib and orotic acid, and the co-crystal of ribociclib monosuccinate and citric acid. Compared with the prior art, the co-crystals have one or more improved properties. The present invention also relates to methods of preparing the co-crystal of ribociclib and saccharin, the co-crystal of ribociclib and cholic acid, the co-crystal of ribociclib and orotic acid, and the co-crystal of ribociclib monosuccinate and citric acid, pharmaceutical compositions, and uses thereof in the preparation of medicines for treating and/or preventing diseases involving one or more symptoms of protein kinase related dysfunctions, cancers, transplant rejection and autoimmune diseases.

Co-crystals of ribociclib and co-crystals of ribociclib monosuccinate, preparation method therefor, compositions thereof, and uses thereof

Provided are a fruquintinib and a saccharin salt or eutectic crystal, a fruquintinib and a malonic acid eutectic crystal or a fruquintinib and a maleic eutectic crystal, a preparation method therefor, a pharmaceutical composition containing thereof, and uses thereof in preparing drugs for treating and/or preventing diseases related to abnormal angiogenesis, such as cancer, tumors, macular degeneration, chronic inflammation and the like.

Fruquintinib eutectic crystal, preparation method therefor, composition, and uses thereof

The present invention relates to a crystalline form of N-((s)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)prop-2-yl)-5-(1-hydroxylethyl)-1H-pyrazole-3-carboxamide (namely, ODM-201). The ODM-201 crystalline form of the present invention has one or more improved properties compared to known ODM-201. The present invention further relates to a method for preparing the ODM-201 crystalline form, a pharmaceutical composition thereof, and a use thereof in the preparation of a medicament for the treatment of nuclear receptor, specifically steroid receptor, and more specifically androgen receptor (AR)-dependent diseases and conditions. 

ODM-201 crystalline form, preparation method therefor, and pharmaceutical composition thereof

The present invention relates to a compound formed by entinostat as shown in formula (I) and acidic counterion. Compared with the known solid form of entinostat, the compound involved has advantages in terms of solubility, stability, etc. The present invention also relates to a crystalline form of the compound and a preparation method therefor, a pharmaceutical composition thereof and the use thereof in the preparation of a drug for preventing and/or treating a disease associated with differentiation or proliferation. 

Entinostat-containing compound, crystal form of compound thereof, and preparation method therefor and pharmaceutical composition thereof

The present invention relates to novel crystal forms of ozanimod. Compared with the prior art, the crystal forms of the present invention have one or more improved properties. The present invention also relates to preparation methods of the crystal forms, pharmaceutical compositions thereof and uses thereof for the manufacture of medicament for treating and/or preventing diseases or adverse conditions associated with modulation, activation, stimulation, inhibition or antagonization of selective sphingosine-1-phosphate (S1P) receptor.

Crystalline forms, preparation methods and pharmaceutical compositions of ozanimod

The present invention relates to a crystal form of 2-(6-methyl-pyridin-2-yl)-3-(6-amido-quinolin-4-yl)-5,6-dihydro-4h-pyrrolo[1,2-b]pyrazole (Galunisertib or LY2157299), represented by formula (I). Compared with the known solid form of Galunisertib, the crystal form of the present invention has advantages in terms of solubility, hygroscopicity, crystal stability, morphology and the like. The present invention also relates to a process of preparing the crystal forms of Galunisertib, a pharmaceutical composition thereof and a use thereof in the preparation of a medicament for the prevention and/or treatment of diseases associated with TGF-beta. 

Crystal form of 2-(6-methyl-pyridin-2-yl)-3-yl-[6-amido-quinolin-4-yl]-5,6-dihydro-4H-pyrrolo[1,2-B]pyrazole, preparation method therefor and pharmaceutical composition thereof

The present invention relates to a cocrystal of 2-(6-methyl-pyridine-2-yl)-3-yl-[6-amide-quinoline-4-yl]-5,6-dihydro-4H-pyrrole[1,2-b]pyrazole (Galunisertib or LY2157299) represented by formula (I) and a cocrystal former. Compared with the known solid form of Galunisertib, the cocrystal of the present invention has advantages in terms of stability, solubility, etc. The present invention also relates to a crystal form of the cocrystal, a preparation method therefor, a pharmaceutical composition thereof, and an application thereof in preparation of drugs for preventing and/or treating diseases relevant to TGF-&#x3b2;.

Cocrystal of 2-(6-methyl-pyridine-2-yl)-3-yl-[6-amide-quinoline-4-yl]-5,6-dihydro-4H-pyrrole[1,2-b]pyrazole, preparation method therefor, and pharmaceutical composition

The present invention relates to canagliflozin Monohydrate and its crystalline forms, which as compared to the prior art, have higher stability in water or aqueous system, are more suitable for wet granulation processes or suspension preparations and have good storage stability; the present invention also relates to preparation methods of canagliflozin Monohydrate and its crystalline forms, pharmaceutical compositions thereof and uses thereof in preparation of drugs for treating diseases such as diabetes, diabetes complications, obesity and so on.

Canagliflozin monohydrate and its crystalline forms, preparation methods and uses thereof

Crystal form of tipifarnib and preparation method and pharmaceutical composition thereof

The present invention relates to novel crystalline forms of ACP-196 (acalabrutinib) salts, compared with the known solid form of ACP-196, the crystalline forms of ACP-196 salts of the present invention have advantages in crystallinity, solubility and hygroscopicity. The present invention also relates to the preparation methods for the preparation of the crystalline forms of ACP-196 salts, pharmaceutical compositions thereof and their uses in the preparation of methods for treating and/or preventing diseases mediated by Bruton tyrosine kinase (BTK), such as autoimmune diseases or disorders, xenoimmune diseases or disorders, cancer, including lymphoma and inflammatory diseases or disorders.

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Zhejiang, China

Xiaohong Sheng