Urea derivatives for treating and/or preventing cancer

A cancer, compound technology, applied in the medical field, can solve problems such as cancer that cannot be finally cured

Pending Publication Date: 2021-08-17
CENT NAT DE LA RECHERCHE SCI +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, they cannot ultimately cure cancer

Method used

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  • Urea derivatives for treating and/or preventing cancer
  • Urea derivatives for treating and/or preventing cancer
  • Urea derivatives for treating and/or preventing cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment A

[0311] Example A: Chemistry

[0312] 1. General Information

[0313] Methanol, ethyl acetate, diethyl ether and dichloromethane were purchased from Carlo Erba. Anhydrous DMF (99.8%, stored under septum) was purchased from Sigma Aldrich. All chemicals were purchased from Aldrich, Fisher or Alfa Aesar. Thin layer chromatography (TLC) was performed on pre-coated Merck 60GF254 silica gel plates and visualized first by visualization under UV light (254nm and 360nm). 1 H and 13 C NMR spectra were recorded on a Bruker Advance 200 MHz spectrometer or a Bruker Advance 400 MHz or Bruker Advance 500 MHz. Mass spectra (ESI-MS) were recorded on a Bruker (Daltonics Esquire 3000+). HRMS spectra were recorded at m / z 200 at a resolution of 140 000 on a ThermoFisher QExactive (ESI-MS). The purity of the compound was further determined by HPLC analysis on a JASCO PU-2089 instrument using the following method:

[0314] - Method 1: Phenomenex Jupiter C18, 5 μm 250x 300mm 300A. UV detec...

Embodiment B

[0355] Example B: Biology

[0356] 1. Materials and Methods

[0357] Reagents and Antibodies

[0358] Sunitinib, SB203580, SB225002, cisplatin and danirisin were purchased from Selleckchem (Houston, USA). Anti-HSP60 antibody was purchased from Santa Cruz Biotechnology (Santa Cruz, CA, USA). Anti-AKT, anti-phospho-AKT, anti-ERK, anti-phospho-ERK antibodies were from Cell Signaling Technology (Beverly, MA, USA).

[0359] cell culture

[0360] RCC4, 786-0 (786) and A498 (498) RCC cell lines, MDA-MD-231 breast cell line, Cal27 and Cal33 head and neck cell lines were purchased from American Tissue Culture Collection (ATTC). Resistant cells 786R (resistance to sunitinib), CAL27RR (resistance to photon multiple irradiation and cisplatin) and CAL33RR (photon multiple irradiation and cisplatin resistance) were provided by the present inventors. OCI-AML2, OCI-AML3, Molm13 and Molm14 acute myeloid cell line (AML), and K562 chronic myeloid cell line (CML), SKM1 myelodysplastic ce...

Embodiment C

[0416] Example C: Medulloblastoma

[0417] 1. Materials and Methods

[0418] cell culture

[0419] DAOY and HD-MBO3 cell lines were purchased from ATCC. They were in the incubator with 10% fetal bovine serum (D.Dutscher) and 1mM sodium pyruvate ( MEMα(1X)+Glutamax from Life Technologies) Incubate together at 37°C.

[0420] Cell viability (XTT)

[0421] 5000 DAOY cells and 50000 HD-MB03 cells were incubated in 96-well plates with different inhibitor concentrations for 24 hours and 48 hours. A control without cells was performed. Add 50 µl of 3'-[1-phenylaminocarbonyl)-3,4-tetrazolium]-bis(4-methoxy-6-nitro)benzenesulfonate sodium hydrate (XTT) reagent into each hole. The assay is based on the formation of the orange formazan dye by lysis of the yellow tetrazolium salt XTT by metabolically active cells. The absorbance of the formazan product, reflecting cell viability, was measured at 450 nm. Each assay was performed in triplicate.

[0422] proliferation test

[04...

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PUM

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Abstract

The present invention relates to a compound or a pharmaceutically acceptable salt thereof of formulae (I) and (II), and a pharmaceutical composition comprising such compound for use for treating a cancer, particularly a cancer overexpressing CXCR1 and CXCR2 receptors, such as medulloblastoma, head and neck and kidney cancer. The invention further relates to such compounds for use for treating macular degeneration.

Description

technical field [0001] The present invention relates to the field of medicine, and in particular to the use of CXCR1 and CXCR2 receptor antagonists in the treatment of cancer and disorders characterized by undesirable excessive angiogenesis, such as macular degeneration. Background technique [0002] Angiogenesis is a process that involves the formation of new capillaries from pre-existing microvessels. Angiogenesis normally occurs during embryonic development, tissue regeneration, wound healing, and corpus luteum development as a cyclical change in the female reproductive system. [0003] However, many existing diseases are caused by dysregulation of angiogenesis. Such diseases associated with angiogenesis occurring under pathological conditions include hemangiomas, angiofibromas, vascular malformations and cardiovascular diseases such as arteriosclerosis, vascular adhesions and scleroderma. Eye diseases associated with angiogenesis include corneal transplant angiogenesis...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4184A61K31/428A61P35/00A61P27/00
CPCA61K31/4184A61K31/428A61P35/00C07D277/82C07D235/30
Inventor 拉奇德·本希达吉勒斯·帕格斯梅芙·杜菲斯卢克·德曼格西里尔·朗科奥列克桑德·格蕾赛
Owner CENT NAT DE LA RECHERCHE SCI
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