Irsogladine maleate Raw Materials Powder

CAS:84504-69-8

MF:C13H11Cl2N5O4

MW:372.16 

EINECS:/

Specification: 99% min Irsogladine maleate Powder

Sample: Irsogladine maleate Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance: White Powder

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Irsogladine maleate Powder Usage and Synthesis.

1.Gastritis treatment: Isradine maleate has no effect on gastric acid secretion under normal dosage, therefore it is very suitable for the treatment of gastritis. 2. Therefore, it is suitable for the treatment of gastritis.

2.Gastric ulcer treatment Most gastric ulcer patients have gastric acid secretion within the normal range, and the main mechanism of its pathogenesis is the weakening of mucosal defence, rather than excessive gastric acid secretion.

Therefore, gastric mucosal protective agent is an important class of anti-ulcer drugs. Among them, Irsogladine maleate is a very good gastric mucosal protector with good antiulcer effect, and widely used in clinic.

(1) Gastric ulcer with gastric acid secretion within normal range: treated with Isoradine maleate alone, 497 cases of gastric ulcer patients, qd, 4mg/time, given for 8 weeks, the endoscopic cure rate was 63% (311/497 cases), and the ulcer shrinkage was 93% (460/497 cases). The rate of moderate or above improvement was 74% (406/546 cases), and the rate of mild or above improvement was 88% (481/546 cases).

(2) Gastric ulcers caused by gastric acid hypersecretion: At present, the treatment of such gastric ulcers mainly uses H2 receptor antagonists, proton pump inhibitors or common mucosal protective agents. However, the recurrence rate within one year after the ulcer healing is as high as 60-80%, in order to overcome the above shortcomings, the current better method is to take H2 receptor antagonists and isoramide maleate combined medication.

(3)Gastric ulcers caused by direct damage to gastric mucosa: For gastric ulcers caused by damage to gastric mucosa due to long-term use of non-steroidal anti-inflammatory drugs, excessive alcohol consumption, overeating and so on, this product can achieve the purpose of healing.

3.Preventing the occurrence of gastric cancer and inhibiting the growth of cancer cells.In the treatment of gastric ulcers, the combination of proton pump inhibitors (such as omeprazole) and Isradine maleate can not only enhance the therapeutic effect, but also prevent the side effects caused by omeprazole (e.g., causing gastric cancer), and it has a better therapeutic effect.

4. Anti-angiogenesis (Anti-angiogenesis) drugs Nipponshinyaku Company in Japan has recently found that Isoramide maleate is the only drug that can inhibit angiogenesis. These anti-angiogenesis drugs are currently in clinical trials.

Uses and functions of Irsogladine maleate.

For the treatment of gastric ulcer disease

Irsogladine maleate is a novel defence enhancer for the regeneration of gastric mucosal epithelium and a radical drug for the repair of gastric ulcer tissue.

Pharmacological Effects of Irsogladine maleate.

Among many gastric mucosal protectants, it has a unique mechanism of action, i.e. by increasing the content of cyclic adenosine monophosphate in the gastric mucosa, it strengthens the association of gastric mucosal epithelial cells, stabilises gastric mucosal cells and plays a cellular defence role.

At the same time, it can also increase the blood flow of normal gastric mucosa and ulcer edge mucosa, thus promoting the regeneration of mucosa.

Irsogladine maleate prevented the peeling off of gastric mucosal epithelium induced by intragastric injection of 0.2 mol/L hydrochloric acid and inhibited the enlargement of intercellular space; inhibited gastric mucosal damage induced by oral administration of anhydrous ethanol in rats and the peeling off of gastric mucosal epithelium; and inhibited the penetration of substances harmful to the gastric mucosa, such as 0.2 mol/L hydrochloric acid and ethanol, into the gastric mucosa.

Irsogladine maleate can affect the content of prostaglandins, reduced glutathione and mucus glycoproteins in the gastric mucosa of rats, and it also showed antioxidant effects on water-immersed stress ulcers (rats), histamine ulcers (mice and rats), aspirin ulcers (rats), acute experimental ulcers and gastric ulcers with acetic acid (rats), electrocautery ulcers (dogs), and chronic experimental ulcers at the low dosages of 1~10mg/kg. It showed antiulcer effects at low doses of 1-10 mg/kg. In rats gavaged with saline, no effect on basal secretion or stimulation of acid secretion was observed.

Irsogladine maleate can also increase the blood flow of the mucosa at the edge of canine acid ulcers and the blood flow of the gastric mucosa in normal rats. It also improved the decrease of gastric mucosal blood flow caused by norepinephrine and anti-inflammatory pain in dogs. No antigenicity, mutagenicity or dependence was observed.

Production method of Irsogladine maleate Powder.

1. 2,4-dichloro-6-(2,5-dichlorophenyl)-1,3,5-triazine was used as raw material for high temperature and high pressure ammonia decomposition.

2. Reacting with 2,5-dichlorobenzoic acid or its derivative esters, amides, anhydrides or chlorides with biguanide as raw material, the yields were 23%, 27%, 58%, 68% and 43%, respectively.

3. 2,5-dichlorobenzonitrile was condensed with dicyandiamide as raw material to obtain esoradine (1′), and then salted with maleic acid to obtain esoradine maleate, the condensation reaction was mild, the yield was 89%.

4. Using 2,5-dichlorotoluene as raw material, oxidation, cyanidation, cyclization, salt formation to obtain Irsoladine maleate, the total yield of 35.4%.

5. Taking 2,5-dichloroaniline (3) as raw material, 2,5-dichlorobenzonitrile (2) was obtained by diazotization and Sandmeyer reaction, and then the salt group (1′) of isoramide maleate was obtained by cycling with dicyandiamide, and the salt group (1′) was obtained by salting with maleic acid to obtain Isoramide maleate (1) without purification with a relatively high yield of 48.6%.