Substituted crotonamide maleate and crystal forms thereof

A technology of maleate and crotonamide, which is applied in the preparation of carboxylate, medical preparations containing active ingredients, and drug combinations, etc.

Active Publication Date: 2015-04-15
JIANGSU SUZHONG PHARM GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the limitation of this compound is that it is not soluble in water in the free base form

Method used

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  • Substituted crotonamide maleate and crystal forms thereof
  • Substituted crotonamide maleate and crystal forms thereof
  • Substituted crotonamide maleate and crystal forms thereof

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Embodiment Construction

[0023](E)-N-{4-[(3-ethynylanilino)-3-cyano-7-ethoxy-6-quinolinyl]}-4-(dimethylamino)-2-butane Enamides are irreversible inhibitors of Her-2 (also known as ErbB-2 or neu) kinase. Her-2 is a member of the epidermal growth factor receptor (EGFR) family, and EGFR family members are closely related to the occurrence and development of tumors and the poor prognosis of tumor patients. (E)-N-{4-[(3-ethynylanilino)-3-cyano-7-ethoxy-6-quinolinyl]}-4-(dimethylamino)-2-butane The structure of the enamide free base is shown below:

[0024]

[0025] Compound (E)-N-{4-[(3-ethynylanilino)-3-cyano-7-ethoxy-6-quinolinyl]}-4-(dimethylamino)-2- Crotonamide is described in patent WO2010151710. According to the biopharmaceutical classification system (BCS), the compound is classified as class IV, low water solubility and poor permeability. At pH 7, the solubility of the free base in water is about 1 μg / ml. As the pH of the solution decreases, the solubility of the compound increases due to i...

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Abstract

The invention discloses a substituted crotonamide maleate, a crystal form thereof, a method for preparing all crystal forms of crystallized maleate, relevant compounds, and a medicinal composition including the compounds. (E)-N-{4-[3-acetylenylphenylamino]-3-cyan-7-ethoxy-6-quinolyl}}-4(dimethylamino)-2-crotonamide maleate, a crystal form I, a crystal form II or a crystal form III respectively have EGFR or ErbB2 kinase inhibition activity, can be used to prevent, treat or inhibit tumors, and can be especially to prepare drugs for preventing, treating or inhibiting epidermal growth factor receptor family related tumors.

Description

technical field [0001] The present invention relates to (E)-N-{4-[(3-ethynylanilino)-3-cyano-7-ethoxy-6-quinolinyl]}-4-(dimethylamino)- Maleate salt form of 2-butenamide, process for preparing crystalline maleate salt form, and related compounds, and pharmaceutical compositions comprising them. In addition, the present invention also relates to their pharmaceutical compositions, and their application in treating tumors, especially tumors related to epidermal growth factor receptor family kinases. Background technique [0002] (E)-N-{4-[(3-ethynylanilino)-3-cyano-7-ethoxy-6-quinolinyl]}-4-(dimethylamino)-2-butane Enamides exhibit antitumor bioactivity, which makes them promising for many applications in the treatment of various cancers. These cancers include but are not limited to pancreatic cancer, melanoma, lymphoma, parotid gland cancer, esophageal cancer, head and neck cancer, ovarian cancer, breast cancer, superficial cancer, tumors of major organs such as kidney, blad...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D215/54C07C57/145C07C51/41A61K31/4706A61K31/194A61P35/00
CPCC07D215/54
Inventor 唐仁茂徐柏颐唐海涛赵耕先张大为欧阳强余长顺沈晓霞孙金娥倪帅健
Owner JIANGSU SUZHONG PHARM GRP CO LTD
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