New crystal forms of 4-[6-methoxy-7-(3-piperidin-1-yl-propoxy)quinazolin-4-yl]piperazine-1-carboxylic acid(4-isopropoxyphenyl)-amide

A technology of isopropoxyphenyl and propoxy, applied in the new crystal form 4-[6-methoxy-7-(3-piperidin-1-yl-propoxy)quinazoline-4 -yl]piperazine-1-carboxylic acid (4-isopropoxyphenyl)-amide field, which can solve time-consuming and lengthy problems

Inactive Publication Date: 2008-06-25
MILLENNIUM PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This trial and error method is tedious and time consuming

Method used

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  • New crystal forms of 4-[6-methoxy-7-(3-piperidin-1-yl-propoxy)quinazolin-4-yl]piperazine-1-carboxylic acid(4-isopropoxyphenyl)-amide
  • New crystal forms of 4-[6-methoxy-7-(3-piperidin-1-yl-propoxy)quinazolin-4-yl]piperazine-1-carboxylic acid(4-isopropoxyphenyl)-amide
  • New crystal forms of 4-[6-methoxy-7-(3-piperidin-1-yl-propoxy)quinazolin-4-yl]piperazine-1-carboxylic acid(4-isopropoxyphenyl)-amide

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Embodiment

[0128] Use a Bruker AXS C2GADDS diffractometer with CuKα rays (40 kV, 40 mA), an automated XYZ interval (stage), a laser video microscope for automatic positioning of the sample, and a HiStar two-dimensional space detector to obtain the X of the sample - Ray powder diffraction patterns. The X-ray optics used a single Gobel multilayer mirror coupled with a 0.3 mm pinhole collimator.

[0129] The beam divergence, ie the effective size of the X-ray beam on the sample, is about 4 mm. Using theta-theta continuous scan mode, where the sample-to-detector distance was 20 cm, a 2-theta range of 3.2° to 29.8° was obtained. The exposure time of the samples is typically 120 seconds.

[0130] Samples operated at ambient temperature were flat specimens made using unground powder. Plate samples are made by gently placing approximately 1 mg to 2 mg of sample on a glass slide. Samples operated at non-ambient temperature conditions were prepared by placing the samples on silicon wafers with...

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Abstract

4-[6-Methoxy-7-(3-piperidin-1-yl-propoxy)quinazolin-4-yl]piperazine-1-carboxylic acid (4-isopropoxy A crystalline form of phenyl)-amide sulfate, which can be used for pharmaceutical applications. The particular single crystal form of the sulfate salt was defined by various properties and physical tests. Also disclosed are methods for preparing said sulfates, and the use of these salts to inhibit the activity of excess tyrosine kinases in the host for the treatment of many diseases, including cardiovascular diseases (e.g., arteriosclerosis and vascular infarction) ), tumors (eg, leukemias such as acute lymphoblastic leukemia), glomerulosclerotic fibrotic diseases and inflammation, and conventional treatment of cell expansion-type diseases.

Description

[0001] related application [0002] This application claims priority to US Provisional Application No. 60 / 700926, filed July 20, 2005. The entire content of the aforementioned application is hereby incorporated by reference. Background technique [0003] Compound 4-[6-methoxy-7-(3-piperidin-1-yl-propoxy)quinazolin-4-yl]piperazine-1-carboxylic acid (4-isopropoxyphenyl )-amide (herein referred to as "compound") is a new small molecule drug candidate that can inhibit FLT-3 receptor tyrosine kinase (RTK). About 30 percent of patients with acute myeloid leukemia (AML) have mutations in the FLT-3 gene, specifically an internal tandem duplication (ITD) of the gene, which can occur in the growth and survival of leukemia cells . See Cancer Cell (2002), 1(5), 421-432. [0004] In preclinical studies, the compound selectively killed human FLT-3 / ITD (internal tandem duplication)-positive AML (acute myeloid leukemia) tumor cells. In addition, since the compound acts on tyrosine kinase...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/94A61K31/517A61P35/02
CPCC07D239/94A61P35/00A61P35/02
Inventor 克雷格·格兰特霍阿·Q·卢昂马克·D·安吉利诺
Owner MILLENNIUM PHARMA INC
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