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Pyrrolo six-membered heterocyclic compound malate polymorph A and preparation method and application thereof

A six-membered heterocyclic and malate technology is applied in the field of pyrrolo six-membered heterocyclic compound malate A crystal form and its preparation, and achieves remarkable effects of stability and bioavailability

Inactive Publication Date: 2016-10-05
SHANGHAI SUNTRONG BIOTECH
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Problems solved by technology

However, no patent literature has been found to report how to prepare the relevant crystal form of pyrrolo six-membered heterocyclic compound malate, and the solid of pyrrolo six-membered heterocyclic compound malate synthesized according to the prior art is amorphous

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  • Pyrrolo six-membered heterocyclic compound malate polymorph A and preparation method and application thereof
  • Pyrrolo six-membered heterocyclic compound malate polymorph A and preparation method and application thereof
  • Pyrrolo six-membered heterocyclic compound malate polymorph A and preparation method and application thereof

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Embodiment Construction

[0017] The invention discloses a pyrrolo six-membered heterocyclic compound malate A crystal form and its preparation method and application, wherein the pyrrolo six-membered heterocyclic compound malate A crystal form has good high temperature, high humidity and light stability It has remarkable stability and bioavailability when used in drugs for the treatment of tumors. The present invention will be described in detail below in conjunction with the accompanying drawings.

[0018] Such as figure 1 As shown, the pyrrolo six-membered heterocyclic compound malate A crystal form provided by the present invention has an XRPD spectrum at 2θ=8.82, 11.16, 11.56, 15.96, 16.20, 16.90, 17.42, 17.87, 19.48, 20.54, 21.08, 21.68 , 22.08, 22.50, 23.22, 24.26, 24.50, 25.88, 26.06, 26.50, 27.51, 28.22, 28.78, 30.54, 32.28, 32.62, 34.74, 40.26, 44.28 have diffraction peaks, where the 2θ value error range is 0.2.

[0019] The present invention also provides a method for preparing the malate ...

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Abstract

The invention discloses a pyrrolo six-membered heterocyclic compound malate A crystal form and its preparation method and application, wherein the pyrrolo six-membered heterocyclic compound malate A crystal form has an XRPD pattern at 2θ=8.82, 11.16 , 11.56, 15.96, 156.20, 16.90, 17.42, 17.87, 19.48, 20.54, 21.08, 22.08, 22.50, 23.22, 24.50, 26.06, 28.7.22, 38.78, 32.78,3.22, 3.78,3.78,3.78,3.222,3.78,3.78,3.222. , There are diffraction peaks at 40.26 and 44.28, and the error range of the 2θ value is 0.2. The malate A crystal form of the pyrrolo six-membered heterocyclic compound provided by the present invention has good high-temperature, high-humidity and light stability, and is used in drugs for treating tumors, and has remarkable stability and bioavailability.

Description

technical field [0001] The invention relates to a drug for treating tumors, in particular to crystal form A of pyrrolo six-membered heterocyclic compound malate and its preparation method and application. Background technique [0002] Protein kinase plays a very important role in the signal transduction process. It can transfer the γ-phosphate group of ATP to specific amino acid residues of functional proteins, triggering a series of biological reactions. When protein tyrosine kinases are expressed under mutated, out-of-control conditions, or under abnormal conditions, they can transform normal cells into a neoplastic phenotype. [0003] Pyrrolo six-membered heterocyclic compound or crystal form is a small molecule tyrosine kinase inhibitor analogue, which can regulate the activity of protein kinase, thereby inhibiting the division and spread of tumor cells. It is based on the cell surface tyrosine kinase receptor targeted anticancer drugs. Pyrrolo six-membered heterocycli...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04C07D487/04C07C59/245C07C51/43A61P35/00
Inventor 于迎渌陈金瑶弋东旭
Owner SHANGHAI SUNTRONG BIOTECH
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