32 results about "Iguratimod" patented technology

The invention relates to a transdermal absorbent containing Iguratimod, which comprises gellies, ointment, and cream, wherein the mass percentage content of the Iguratimod in the transdermal absorbent is between 0.1 and 10 percent, and preferably the mass percentage content of the Iguratimod in the transdermal absorbent is between 0.4 and 3 percent; and the invention also discloses requirements of the transdermal absorbent on the selections of matrix and a transdermal enhancer. Furthermore, the invention also provides a method for preparing the transdermal absorbent containing the Iguratimod and pharmaceutical application thereof.

The invention relates to oral double iguratimod controlled release formulation, which comprises fast release layer and slow release layer that are composed of 8-30% micronizing iguratimod crystal powder and medical findings, and the granule size of iguratimod crystal powder is 1-10 um. The effective component in fast release layer is released in short time and reaches to effective blood chemical concentration for effective action; the iguratimod in sloe release layer is released gradually and maintains effective blood medical concentration for continuous effective action. The invention overcomes shortcomings of short effective action time and a little high toxic effect.

The invention relates to the technical field of synthesis of chemical drugs, in particular to a preparation method of Iguratimod formylation intermediates. The preparation method comprises the following steps: mixed acid anhydride is prepared from formic acid, sodium formate and pivaloyl chloride, a compound I is added for carbamylation, and the Iguratimod formylation intermediates are obtained. Mixed acid anhydride is prepared from formic acid and pivaloyl chloride, the reaction with pivaloyl chloride is a homogeneous reaction, reaction speed is high, and conversion rate is high; the relatively acidic environment of the system is kept by formic acid, side reactions in which piperazine compounds are generated from alpha-aminoketone compounds in raw materials through own condensation reaction under alkaline conditions are avoided, yield is increased, impurities are reduced, and purity is improved. The Iguratimod formylation intermediates prepared with the method are high in purity and can be used for preparing Iguratimod.

The invention relates to a crystal habit (iguratimod) of N-[3- (formamido)-4-oxygen-6-phenoxy-4H-1- benzopyran-7-base]-methylsulfonamid. In addition, the invention also relates to application of iguratimod crystal habit to medicine for treating rheumatoid arthritis, a medicine composition containing the iguratimod crystal habit and a preparation method of the iguratimod crystal habit.

The invention discloses a medicinal composition which comprises hydroxychloroquine and iguratimod, and further relates to applications of hydroxychloroquine and salts of hydroxychloroquine in preparing medicines capable of alleviating the toxic and side effects of iguratimod. The compound composition has the obvious effects of synergists and the obvious effect of reducing toxic and side effects.

The invention relates to a crystalline form (Iguratimod) of N-[3-(formylamino)-4-oxo-6-phenoxy-4H-1-benzopyran-7-yl]-methyl sulfonamide. In addition, the invention further relates to application of the Iguratimod crystalline form in the medicine of treating rheumatoid arthritis, a pharmaceutical composition containing Iguratimod crystalline form and a method for preparing crystalline Iguratimod.

In the present invention, a method using a combination of iguratimod or a salt thereof and one or more immunosuppressants is useful as a method for the treatment of autoimmune diseases, and with this method adverse effects are lessened. A pharmaceutical composition containing this combination is useful for the treatment of autoimmune diseases. This method and pharmaceutical composition are useful for the treatment of more severe autoimmune diseases.

Iguratimod, Repirinast, Lobenzarit, Actarit, Ifenprodil, Bemithyl, Bromantane, Emoxypine, Udenafil, and/or Istradefylline are used for the treatment or prophylaxis of renal fibrosis, kidney disease, or chronic kidney disease in a subject.

The invention discloses a preparation method of an Iguratimod intermediate, which comprises the following steps: by taking p-nitroanisole as a raw material, carrying out substitution nucleophilic substitution (VNS) on p-nitroanisole and methoxyamine hydrochloride in the presence of a copper salt catalyst and an acid-binding agent to generate 5-methoxy-2-nitroaniline (compound II); the synthesis method comprises the following steps: carrying out a nucleophilic substitution reaction on 5-methoxy-2-nitroaniline (compound II) and methanesulfonyl chloride to generate a compound III, etherifying the compound III and phenol under the catalysis of a copper salt to generate N-(5-methoxy-2-phenoxy phenyl) methane sulfonamide (compound IV), and reagents used in the synthesis process are non-highly toxic products and are easy to obtain; no iron powder is used in the reaction process, so that iron mud which is harmful to the environment is not generated, and the environmental protection property is high; the reaction operation difficulty is small, the safety is high, and a foundation is laid for industrial preparation of Iguratimod drugs.

The invention discloses a preparation method of an iguratimod intermediate. The preparation method comprises the following steps: by using formic acid as a starting raw material, subjecting formic acid to reacting with N,N-carbonyldiimidazole (CDI) via an active ester method to obtain formylimidazole with higher activity, and subjecting the formylimidazole to reacting with 2-amino-1-(2-methoxy-4-methanesulfonamido-5-phenoxyphenyl)ethanone hydrochloride to obtain an important intermediate compound of iguratimod. The method has the advantages of being safe, environmentally friendly, easy to operate, high in yield, good in product purity, suitable for industrial production and the like, and is suitable for preparing the iguratimod intermediate.

The invention discloses a method for preparing an iguratimod intermediate IV, which belongs to the technical field of medicine and chemical industry. The present invention replaces nitrobenzene with nitromethane as the preparation of Alamod intermediate IV (α-amino-2-methoxy-4-methanesulfonamido-5-phenoxyacetophenone hydrochloride ) solvent, the weight yield of the prepared Alamod intermediate IV can reach 102~105%, and the purity can reach more than 99%; in addition, the present invention adopts nitromethane as the solvent of reaction and also has the following advantages: weak smell , less pollution, less harm to the human body, easy post-processing of the product, improved purity, and no genotoxic impurity nitrobenzene residue in the final product.

The invention provides an application of iguratimod in preparation of a medicine for treating systemic sclerosis. Inventors find that the iguratimod has application potential that an external dosage form for external use of the iguratimod can be prepared, and hardened skin can be softened by topical application. Experiments prove that a local or systemic application of the iguratimod can significantly inhibit important transcription factor EGR1 involved in fibrosis to decrease expression of pro-fibrogenic cytokine TGF-beta or decrease signals in downstream, thereby inhibiting the progression of the systemic sclerosis. The topical application of an iguratimod dimethyl sulfoxide solution can also effectively reduce and cure experimental scleroderma skin fibrosis.

Methods of treatment of MIF-related diseases and methods of MIF inhibition are provided.