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Hexavalent amino amidate derivative with function of inhibiting blood vessel growth activity

An amino, carboxamide technology, applied in the direction of organic active ingredients, cardiovascular system diseases, medical preparations containing active ingredients, etc.

Inactive Publication Date: 2006-10-25
艾驰艾尔必株式会社
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

2. The lack of blood flow into and out of the tumor prevents the migration of tumor cells

Method used

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  • Hexavalent amino amidate derivative with function of inhibiting blood vessel growth activity
  • Hexavalent amino amidate derivative with function of inhibiting blood vessel growth activity
  • Hexavalent amino amidate derivative with function of inhibiting blood vessel growth activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0139] N-[4-(cyanocyclobutyl)phenyl]{2-[(4-pyridylmethyl)amino]phenyl}carboxamide

[0140] A: 1-(4-Aminophenyl) cyclobutyl nitrile

[0141] Mix 1-phenylcyclobutyl nitrile (5g), acetic acid (15ml), H 2 SO 4 (10ml) and KNO 3 (1.1 molar ratio), stir at 0°C for 20 minutes, then warm to room temperature and stir for another 2 hours. Then the mixture was poured into ice cubes and stirred until the ice cubes were completely dissolved, and a solid precipitated out, filtered with suction and recrystallized from ethanol to obtain 1-(4-nitrophenyl)cyclobutyronitrile. Mix 2 g of the above product with palladium-carbon (800 mg, 10%) and ethanol (100 ml), hydrogenate at atmospheric pressure for 1 hour, then filter with suction, and evaporate the filtrate to obtain 1-(4-aminophenyl)cyclobutane Base nitrile. Mass spectrum (M+1), 172, the final product is purified for use in the next step.

[0142] B. 2-Aminophenyl-N-[4-(cyanocyclobutyl)phenyl]carboxamide

[0143] A mixture of anthranilic acid (1....

Embodiment 2

[0147] N-[4-(cyanocyclopropyl)phenyl]{2-[(4-pyridylmethyl)amino]phenyl}carboxamide

[0148] This compound was prepared by a method similar to Example 1, starting from 1-phenylcyclopropyl nitrile. Mass spectrum: (M+1), 369

Embodiment 3

[0150] N-[4-(cyanocyclopentyl)phenyl]{2-[(4-pyridylmethyl)amino]phenyl}carboxamide

[0151] This compound was prepared using a method similar to Example 1, starting from 1-phenylcyclopentyl nitrile. Mass spectrum: (M+1), 395

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Abstract

The present invention relates to six-membered aminoamide derivatives, their preparation process, medicines using them as active ingredients, and methods for treating diseases related to angiogenesis or high blood vessel permeability by using them. It also relates to their use as medicines and the manufacture of medicines containing them to reduce angiogenesis and vascular permeability diseases in warm-blooded animals like man.

Description

Technical field [0001] The present invention relates to six-membered amino amide derivatives, their preparation process, medicines using them as active ingredients, and methods for treating diseases related to angiogenesis or high vascular permeability through them. It also involves their use as medicines, and the manufacture of medicines containing them to reduce angiogenesis and vascular permeability diseases in warm-blooded animals like humans. Background technique [0002] Ordinary angiogenesis plays an important role in various processes, such as embryo development, wound healing, and the main component of female reproductive function. Bad or pathological angiogenesis is related to diseases, such as retinopathy caused by diabetes, psoriasis, cancer, rheumatoid arthritis, and atheroma. The formation and permeability of new blood vessels is mainly regulated by vascular endothelial growth factor (VEGF), and tumor angiogenesis has two different receptors: VEGF-R1 (fms-like tyros...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D213/74C07D401/02A61K31/4439A61K31/444A61P35/00A61P29/00A61P19/02A61P17/06A61P9/10A61P43/00
Inventor 孙庄蓉陶鸿光
Owner 艾驰艾尔必株式会社
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