Patent classifications
C07B2200/13
BIARYL ETHER-TYPE QUINAZOLINE DERIVATIVES
The present invention provides a novel compound or a pharmaceutically acceptable salt thereof having an inhibitory action on an EGFR tyrosine kinase having an exon 20 insertion mutation and/or a HER2 tyrosine kinase having an exon 20 insertion mutation, a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 in the Formula (I) are each as defined in the description.
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Crystalline Forms and Salt Forms of a Kinase Inhibitor
The present invention relates to crystalline forms of the free base of the c-Met inhibitor, Compound 1. The invention also relates to crystalline forms of salts of Compound 1. The invention also relates to pharmaceutical compositions comprising the solid polymorphs of the free base and salts of Compound 1. The invention further relates to methods of treating a disease, disorder, or syndrome mediated at least in part by modulating in vivo activity of a protein kinase.
Crystalline Form of a 7H-Benzo[7]Annulene-2-Carboxylic Acid Derivative
The present disclosure relates to a compound of formula (1) as an anhydrate which is in a crystalline Form 2, characterized by having a powder-X-ray diffractogram displaying peaks expressed as degree 2-Theta angles at about 9.5; 11.8; 14.1; 14.6; 17.7 and 18.5 and a solid form thereof. The present disclosure also relates to processes for its preparation, as well as a medicament and a pharmaceutical composition comprising it. The present disclosure further concerns the anhydrate crystalline Form 2 of compound of formula (1) for use as a medicine and more particularly in the treatment of cancer.
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ADDITIVE USED IN METHIONINE PREPARATION PROCESS, AND METHIONINE PREPARATION METHOD
The present disclosure relates to an additive used in a methionine preparation process, and a methionine preparation method. The additive provided by the present disclosure is a mixture containing components A, B, and C; component A has a structure represented by the following general formula (1); component B has a structure represented by the following general formula (2); component C is silicone oil; RCON(CH.sub.3)CH.sub.2CH.sub.2SO.sub.3Na (1). The methionine preparation method provided in the present invention comprises subjecting methionine to crystallization and/or recrystallization in the presence of the additive provided by the present disclosure. The additive provided by the present disclosure results in uniform emulsification, has good stability, can be used stably for a long time, and is suitable for a continuous crystallization process. The prepared methionine crystal has a good crystal form, a large bulk density, and good flowability. In addition, according to the methionine preparation method of the present disclosure, a crystallization system can operate continuously and stably for a long time without obvious foaming, and the crystallization process of the methionine product can proceed smoothly.
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METHODS OF TREATING SMALL CELL LUNG CANCER WITH LURBINECTEDIN FORMULATIONS
Provided are methods for the treatment of SCLC patients by administering therapeutic amounts of lurbinectedin by intravenous infusion. Also provided are methods of treating cancer by administering lurbinectedin in combination with other anticancer drugs, in particular topoisomerase inhibitors. The invention further relates to the administration of lurbinectedin in combination with anti-emetic agents for effective control of symptoms related to nausea and vomiting, reduced lurbinectedin dosages to achieve a safer administration and an increase in the number of treatment cycles. Stable lyophilized formulations of lurbinectedin are also provided.
Selective Inhibitors Of Protein Arginine Methyltransferase 5 (PRMT5)
The disclosure is directed to pharmaceutically acceptable salts of the compound of Formula I (I). Pharmaceutical compositions comprising pharmaceutically acceptable salts of the compound of Formula I, as well as methods of their use and preparation, are also described.
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SALTS OF (2R, 6R)-HYDROXYNORKETAMINE, THEIR CRYSTAL FORMS, AND METHODS OF MAKING THE SAME
The disclosure provides salts of (2R,6R)-hydroxynorketamine (HNK), wherein the salt is with an organic acid chosen from malonic acid, salicylic acid, ethane sulfonic acid, glycolic acid, stearic acid, or capric acid, and their crystal forms.
PROCESS FOR PREPARING CHROMAN COMPOUNDS
A process for manufacturing substituted chroman compounds in an economically scalable manner, without the use of pyrophoric reagents. Also disclosed herein are chroman compound synthesis routes that do not include column chromatography purification steps. The disclosure also relates to the intermediates used in the synthesis. In particular, the disclosure relates to the synthesis of the Calcium sensing receptor (CaSR) modulating agent 2-methyl-5-((2R,4S)-2-((((R)-1-(naphthalen-1-yl)ethyl)amino)methyl)chroman-4-yl)benzoic acid, its intermediates and pharmaceutically acceptable salts thereof.
A METHOD FOR PREPARING IVOSIDENIB AND AN INTERMEDIATE THEREOF
The present application relates to a method for preparing a substantially and diastereomerically pure crystalline ethanol solvate of Compound IIa and its use for synthesizing Ivosidenib.
METHOD FOR MANUFACTURING REVAUDIOSIDE-D-CONTAINING CRYSTALLIZED PRODUCT, AND REVAUDIOSIDE-D-CONTAINING CRYSTALLIZED PRODUCT
There is demand for a novel method for manufacturing a RebD crystallized product. The present invention provides a method for manufacturing a RebD-containing crystallized product, including: a step for mixing a stevia plant-derived crude product having a total steviol glycoside content of 50-95 mass %, and containing at least RebA and RebD, into a solvent containing methanol or ethanol so that the supersaturation of RebD at 10° C. is at least 10 and the supersaturation of RebA at 10° C. does not exceed 18, and adjusting a crystallization solution; and a step for cooling the crystallization solution under stirring and causing RebD to precipitate.