FREE BASE CRYSTALLINE FORM OF A COMPLEMENT COMPONENT C5a RECEPTOR

a technology of complement components and free base crystalline forms, which is applied in the direction of antibody medical ingredients, drug compositions, immunological disorders, etc., can solve the problems of affecting the delivery efficiency of biologically relevant amounts of compound 1 and even potentially life-threatening consequences

Pending Publication Date: 2022-03-31
CHEMOCENTRYX INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent describes a new form of a compound that has been crystallized. The new form has been characterized using X-ray powder diffraction and differential scanning calorimetry. The technical effect of this patent is the discovery of a new and useful form of a compound that can be further developed and used in various applications.

Problems solved by technology

Inappropriate or excessive activation of the complement system can lead to harmful, and even potentially life-threatening consequences due to severe inflammation and resulting tissue destruction.
Despite this identification, the efficient delivery of biologically relevant amounts of Compound 1 remains challenging.

Method used

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  • FREE BASE CRYSTALLINE FORM OF A COMPLEMENT COMPONENT C5a RECEPTOR
  • FREE BASE CRYSTALLINE FORM OF A COMPLEMENT COMPONENT C5a RECEPTOR
  • FREE BASE CRYSTALLINE FORM OF A COMPLEMENT COMPONENT C5a RECEPTOR

Examples

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example 1

a Crystalline Form of Compound 1

[0068]Crude Compound 1 was prepared essentially as described in WO 2016 / 053890.

[0069]A crystalline form of Compound 1 was prepared by dissolving 18 g of crude Compound 1 in 50 mL acetone with heating at 40° C. (a concentration of about −0.36 g / mL). The warm solution was passed through a 10 μm polyethylene filter. The solution was then loaded into rotary evaporator at 30° C. bath temperature and 180 rpm rotational speed. The solid collected was dried further in a 45° C. oven for 1 hour. The XRPD data of the crystalline form is shown in FIG. 1, and the table of peaks measured are listed in Table 1, below.

TABLE 1Significant Peaks of Free Base Crystalline Form of Compound 1 Significant Peaks2-theta (deg)8.0620.288.4021.328.8822.3610.2022.6010.7223.1412.3523.4613.4424.4214.1024.6615.2125.0516.0525.4816.2026.2016.9226.4417.2827.1817.6427.6018.5828.7019.0029.2819.4429.60

example 2

ial Scanning Calorimetry (DSC) and Thermal Gravimetic Analysis (TGA) of the Free Base Crystalline Form of Compound 1

[0070]To evaluate the physical characteristics of the free base crystalline form of Compound 1, differential scanning calorimetry data was collected. Differential scanning calorimeter model DSC25 from TA Instruments˜ Waters LLC was used. Sample was weighed into a standard aluminum pan and sealed by a standard aluminum lid with pinhole. The measurement was completed by using 10° C. / min scanning rate, under a nitrogen purge. The DSC analysis determined that the free base crystalline form exhibits a melting (on set) of ˜213° C. and a endothermic peak at around 216° C. A plot of the DSC thermogram is shown in FIG. 2.

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Abstract

Provided herein is a free base crystalline form of a complement component 5a receptor having the formula of Compound 1Also provided herein are pharmaceutical compositions and methods of treatment using the crystalline free base form of Compound 1 described herein.

Description

CROSS-REFERENCES TO RELATED APPLICATIONS[0001]This application is a continuation of Ser. No. 17 / 091,019 filed Nov. 60, 2020 which application claims the benefit of priority under 35 U.S.C § 119(e) to U.S. Provisional Application Ser. No. 62 / 932,652 filed Nov. 8, 2019, the disclosures of each are incorporated herein by reference in their entirety.STATEMENT AS TO RIGHTS TO INVENTIONS MADE UNDER FEDERALLY SPONSORED RESEARCH AND DEVELOPMENT[0002]NOT APPLICABLEREFERENCE TO A “SEQUENCE LISTING,” A TABLE, OR A COMPUTER PROGRAM LISTING APPENDIX SUBMITTED ON A COMPACT DISK[0003]NOT APPLICABLEBACKGROUND OF THE INVENTION[0004]The complement system plays a central role in the clearance of immune complexes and in immune responses to infectious agents, foreign antigens, virus infected cells and tumor cells. Inappropriate or excessive activation of the complement system can lead to harmful, and even potentially life-threatening consequences due to severe inflammation and resulting tissue destructi...

Claims

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Application Information

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IPC IPC(8): A61K31/451C07D211/60A61K31/675A61K39/395
CPCA61K31/451C07D211/60C07B2200/13A61K39/3955A61K31/675A61P29/00A61P9/00A61P37/00A61P3/10
InventorSINGH, RAJINDERYAU, KWOKZENG, YIBINZHANG, PENGLIELUI, REBECCA M.KRASINSKI, ANTONI
OwnerCHEMOCENTRYX INC