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Crystal form of intestinal type-2B sodium phosphate synergistic transportprotein inhibitor and preparation method thereof

A technology of crystal form and solvent, which is applied in the field of crystal form of intestinal 2B sodium phosphate cotransporter inhibitor and its preparation, can solve problems such as difficulty in practical application and instability of type I crystal

Active Publication Date: 2019-03-05
JIANGSU HENGRUI MEDICINE CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the aforementioned type I crystals are extremely unstable under light conditions and need to be stored away from light, which makes practical application very difficult.

Method used

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  • Crystal form of intestinal type-2B sodium phosphate synergistic transportprotein inhibitor and preparation method thereof
  • Crystal form of intestinal type-2B sodium phosphate synergistic transportprotein inhibitor and preparation method thereof
  • Crystal form of intestinal type-2B sodium phosphate synergistic transportprotein inhibitor and preparation method thereof

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Embodiment Construction

[0024] In the specification and claims of the present application, unless otherwise specified, the scientific and technical terms used herein have the meanings commonly understood by those skilled in the art. However, for a better understanding of the present invention, definitions and explanations of some related terms are provided below. In addition, when the definitions and explanations of terms provided in this application are inconsistent with the meanings commonly understood by those skilled in the art, the definitions and explanations of terms provided in this application shall prevail.

[0025] The "halogen or halogen atom" in the present invention refers to fluorine atom, chlorine atom, bromine atom, iodine atom and the like.

[0026] "C" described in the present invention 1-6 "Alkyl" means a linear or branched alkyl group containing 1-6 carbon atoms. Specific examples include, but are not limited to: methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl,...

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Abstract

The invention relates to a crystal form of an intestinal type-2B sodium phosphate synergistic transportprotein inhibitor and a preparation method thereof, in particular to a crystal form II of N<1>-methyl-N<1>-(2-morpholine ethyl)-N<3>-(3-(4-phenylethyl phenylcarbamyl)-4,5,6,7-tetrahydrobenzo[b]thiophene-2-yl)isophthalamide sulfate (a compound shown in formula (I)) and a preparation method. The crystal form II of the compound in formula (I) obtained in the invention has good chemical stability and crystal form stability and can be well applied to the clinical treatment. (Shown in the description).

Description

technical field [0001] The present invention relates to N 1 -Methyl-N 1 -(2-morpholine ethyl)-N 3 -(3-(4-phenylethylphenylcarbamoyl)-4,5,6,7-tetrahydrobenzo[b]thiophen-2-yl)II crystal form of isophthalamide sulfate and Preparation. Background technique [0002] Inorganic phosphate (Pi) is an essential component of bone mineral. About 80% of human phosphate is in the extracellular matrix (such as bone and tooth) in vitro, 18% is in the cell, and 2% is in the extracellular fluid. Under normal physiological conditions, excess phosphate is taken up by the small intestine, and phosphate homeostasis is regulated by the excretion and reabsorption of the kidneys. Too much or too little phosphate in the body will lead to dysfunction of the body and cause disease: if it is too low, it will cause hypophosphatemia, rickets, and cardiac dysfunction; if it is too high, it will induce hyperphosphatemia, soft tissue and Vascular calcification and renal dysfunction. Excessive phosphate...

Claims

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Application Information

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IPC IPC(8): C07D333/68A61K31/5377A61P3/12
CPCA61P3/12C07B2200/13C07D333/68
Inventor 武乖利边林张全良卢韵
Owner JIANGSU HENGRUI MEDICINE CO LTD
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