33 results about "Leukotriene Antagonists" patented technology

A solid form of a compound of formula 1: is provided. The compound of formula 1 can be obtained in solid state by precipitation from a solution containing the same. The compound is useful as leukotriene antagonist and can be formulated into a pharmaceutical composition that also includes a pharmaceutically acceptable excipient.

The present invention is directed to methods for treating rhinitis or sinusitis in a subject. In one embodiment, the method comprises the steps of: identifying a subject in need thereof, and administering intranasally to the subject a formulation comprising an only active ingredient of an effective amount of rhamnolipid. In another embodiment, the method comprises the steps of: identifying a subject in need thereof, and administering intranasally to the subject a first active ingredient of an effective amount of a rhamnolipid and a second active ingredient of an effective amount of a corticosteroid, an antihistamine, a leukotriene antagonist, cromylin, an antibiotic, a sphingolipid, or a decongestant.

The present invention relates generally to muscarinic receptor antagonist, which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and the method for treating diseases mediated through muscarinic receptors. Also provided herein are pharmaceutical composition comprising one or more muscarinic receptor antagonists and at least one other active ingredients include, but are not limited to, corticosteroids, beta agonists, leukotriene antagonists, 5-lipoxygenase inhibitors, anti-histamines, antitussives, dopamine receptor antagonists, chemokine inhibitors, p38 MAP Kinase inhibitors, and PDE-IV inhibitors.

The present invention relates to a process for the preparation of a compound of formula (I) or a sodium salt thereof, wherein HET is 7-chloroquinolin-2-yl or 6,7-difluoroquinolin-2-yl, which comprises: reacting the dilithium dianion of 1-(mercapto-methyl)cyclopropaneacetic acid with a compound of formula (II), wherein HET is as defined above and L is arylsulfonyl or alkylsulfonyl. The invention further provides the dicyclohexylamine salt of a compound of formula (I), an intermediate falling within (II) and a 1-(Mercaptomethyl)cyclopropaneacetic acid intermediate.

A pharmaceutical composition or kit of parts comprising at least three ingredients from a HMG-CoA reductase inhibitor, a leukotriene antagonist, a proton pump inhibitor, melatonin or a melatonin receptor agonist, a bioavailable preparation of a curcuminoid, a calciferol derivative, a compound from the group consisting of metformin and phenformin, valproate, minocycline and chloroquine and one or more pharmaceutically acceptable carriers or excipients.

The invention relates to a preparation method of leukotriene antagonist, particularly the preparation method of 1-(sulfhydryl methyl)-cycloprophyl-acetate and the derivate thereof. The mentioned compound is prepared from the transformation of the compound in the below formula by the alkali of the alcohol solvent, wherein R represents the alkyl and the naphthenic radical.

A solid form of a compound of formula 1:is provided. The compound of formula 1 can be obtained in solid state by precipitation from a solution containing the same. The compound is useful as leukotriene antagonist and can be formulated into a pharmaceutical composition that also includes a pharmaceutically acceptable excipient.

A pharmaceutical composition useful in the treatment of sneezing, itching runny nose, nasal congestion, redness of the eye, tearing, itching of the ears or palate, shortness of breath, inflammation of the bronchial mucosa, reduced Forced Expiratory Volume In One Second (FEV1), coughs, rash, itchy skin, headaches, and aches and pains associated with seasonal allergic rhinitis, perennial allergic rhinitis, common colds, otitis, sinusitus, allergy, asthma, allergic asthma and / or inflammation, in a mammalian organism in need of such treatment. The composition comprises: i) an effective amount of at least one leukotriene antagonist selected from a) montelukast, b) 1-(((R)- (3-(2-(6,7- difluoro-2- quinolinyl)ethenyl) phenyl)-3-(2- (2-hydroxy-2- propyl)phenyl) thio)methylcyclopropaneacetic acid; c) 1-(((1(R)-3 (3-(2-(2,3- dichlorothieno[3, 2-b]pyridin-5-yl) -(E)-ethenyl)phenyl) -3-(2-(1-hydroxy-1- methylethyl) phenyl)propyl) thio)methyl) cyclopropaneacetic acid; d) pranlukast; or f) [2-[[2-(4-tert -butyl-2-thiazolyl) -5-benzofuranyl] oxymethyl]phenyl] acetic acid; or a pharmaceutically acceptable salt thereof; in admixture with ii) an effective amount of at least one antihistamine which is descarboethoxyloratidine, cetirizine, fexofenadine, ebastine, astemizole, norastemizole, epinastine, efletirizine or a pharmaceutically acceptable salt thereof.

The invention relates to a pharmaceutical composition for treating asthma, allergic reaction and inflammation. The composition comprises a leukotriene antagonist, antihistaminics and medicinal carriers, wherein the leukotriene antagonist is Montelukast and salts thereof, and the antihistaminics is olopatadine hydrochloride and salts thereof. The composition is suitable for preventing and long-term treating of asthma for children and adults, and can treat asthma patients sensitive to aspirin, prevent bronchoconstriction induced by movement, treat pruritus concomitant with allergic rhinitis, urticaria and skin diseases, and the like. The composition has better curative effect compared with that the two medicines are used independently.

The invention relates to the preparation method of formula (I) compound 3-methoxy-4-((5-nitro-1H-indole-3-base)methyl)benzoic acid C1-C4 alkyl esters. The compound is a crucial intermediate in the preparation of zafirlukast which is a leukotriene antagonist drug.

The present invention relates to preventive and / or therapeutic agents for Meniere's disease, which comprise a leukotriene antagonist (such as pranlukast hydrate) as an active ingredient. Leukotriene antagonists (such as pranlukast hydrate) are effective in ameliorating various symptoms, such as hearing impairment, tinnitus, a feeling of fullness in the ear and vertigo, thus being useful as a preventive and / or therapeutic agent for Meniere's disease.

The invention relates to an oral liquid of leukotriene antagonist against allergy, inflammation, asthma that can be used as cell protecting agent, comprising at least a buffer solution and Montelukast dissolved in the buffer solution and its pharmaceutically acceptable salts. The pH of the buffer solution is between 7-11, and the buffer solution includes at least water, pharmaceutically acceptable alcohols, buffering agents and pharmaceutically acceptable additives.

The present invention is directed to methods for treating rhinitis or sinusitis in a subject. In one embodiment, the method comprises the steps of: identifying a subject in need thereof, and administering intranasally to the subject a formulation comprising an only active ingredient of an effective amount of rhamnolipid. In another embodiment, the method comprises the steps of: identifying a subject in need thereof, and administering intranasally to the subject a first active ingredient of an effective amount of a rhamnolipid and a second active ingredient of an effective amount of a corticosteroid, an antihistamine, a leukotriene antagonist, cromylin, an antibiotic, a sphingolipid, or a decongestant.

The invention relates to a zafirlukast intermediate preparation process, wherein the compound is an important intermediate for preparing a leukotriene antagonist drug zafirlukast. The process comprises: carrying out a heating reaction in an inert solvent under the action of acidified montmorillonite by using methyl(5-nitro-1-tosyl-1H-indole-3-yl)acetate and methyl 3-methoxybenzoate as raw materials until the raw materials disappear, filtering to obtain 3-methoxy-4-[(5-nitro-1-tosyl-1H-indole-3-yl)methyl] methyl benzoate, and hydrolyzing the 3-methoxy-4-[(5-nitro-1-tosyl-1H-indole-3-yl)methyl]methyl benzoate under alkaline conditions to obtain the target product. According to the present invention, the new process route for synthesizing the important zafirlukast intermediate is provided,has the technical advantages of simple operation, low reaction cost, high product yield and environmental friendliness, and can meet the large-scale production demand of medical products.

The invention relates to an externally applied compound composition consisting of tadines and a leukotriene antagonist, wherein the tadines are preferably loratadine and salt thereof; and the leukotriene antagonist is preferably montelukast and salt thereof. The externally applied compound composition can be prepared into externally applied preparations such as nasal drops, eye drops, eye ointments, ointments, gel, inhalants, patches and the like. The externally applied compound composition can be used for local treatment for allergic diseases, can quickly improve allergic symptoms, and has the characteristics of high efficiency, safety, convenient use and the like.

It comprises a preparation process of Montelukast from an intermediate compound of formula (V), which is previously prepared by reaction of the corresponding sulfonate with 1-(mercaptomethyl)cyclopropyl)methanol. Compound (V) is reacted with a Grignard reactant to convert the ester group into a tertiary alcohol, followed by conversion of the primary alcohol into a sulfonate, substitution of the sulfonate group by a cyano group, and finally transforming the cyano compound to the carboxilic acid compound by a hydrolysis reaction to afford Montelukast. Montelukast can also be prepared by a hydrolysis reaction of the corresponding amide. It also comprises intermediate compounds useful in such preparation process.

It comprises a preparation process of Montelukast from a new intermediate compound of formula (VI), which is previously prepared by reaction of the corresponding sulfonate with 1-(mercaptomethyl)cyclopropyl)methanol. Compound (VI) is reacted with a Grignard reactant to convert the ester group into a tertiary alcohol, followed by conversion of the primary alcohol into a sulfonate, substitution of the sulfonate group by a cyano group, and finally transforming the cyano compound to the carboxilic acid compound by a hydrolysis reaction to afford Montelukast. Montelukast can also be prepared by a hydrolysis reaction of the corresponding amide. It also comprises new intermediate compounds useful in such preparation process.

The present invention provides a novel process for the preparation of alkyl (1-alkylindol-3-ylmethyl)benzoate derivatives which process comprises the steps of: (a) reacting of an alkyl (halomethyl)benzoate with excess of an indole, said indole being unsubstituted at positions 1-, 2- and 3-, under conditions promoting alkylation at the 3-position of the indole to yield a mixture comprising alkyl (indol-3-ylmethyl)benzoate and unreacted starting indole, (b) treating the mixture obtained in step (a) with base to yield a mixture, comprising the salt of (indol-3-ylmethyl)benzoic acid and the unreacted indole, (c) recovering the unreacted indole from the mixture obtained in step (b), and recycling the indole as starting material to step (a), (d) isolating the salt of (indol-3-ylmethyl)benzoic acid and / or acidifying the salt to form (indol-3-ylmethyl)benzoic acid, (e) reacting the (indol-3-ylmethyl)benzoic acid or it's salt with alkylating agent in the presence of base to form the desired alkyl (1-alkylindol-3-ylmethyl)benzoate. The above process affords also the preparation of the anti-asthmatic leukotriene antagonist zafirlukast. In such case, methyl 3-methoxy-4-(1-methyl-5-nitroindol-3-ylmethyl)benzoate [a]is formed in step (e) of the process and this compound is subsequently converted into zafirlukast by known methods.

The present invention relates to a process for the preparation of a compound of formula (I) or a sodium salt thereofwherein HET is 7-chloroquinolin-2-yl or 6,7-difluoroquinolin-2-yl, which comprises: reacting the dilithium dianion of 1-(mercapto-methyl)cyclopropaneacetic acid with a compound of formula (II)wherein HET is as defined above and L is arylsulfonyl or alkylsulfonyl. The invention further provides the dicyclohexylamine salt of a compound of formula (I).

The invention relates to an oral liquid of leukotriene antagonist against allergy, inflammation, asthma that can be used as cell protecting agent, comprising at least a buffer solution and Montelukast dissolved in the buffer solution and its pharmaceutically acceptable salts. The pH of the buffer solution is between 7-11, and the buffer solution includes at least water, pharmaceutically acceptable alcohols, buffering agents and pharmaceutically acceptable additives.

The invention provides a pharmaceutical composition for the treatment of respiratory diseases, in particular asthma, rhinitis or COPD and especially asthma. Particularly, the composition contains glucocorticoid and leukotriene antagonist, especially Ciclesonide, Montelukast and salts usable for treatment. The pharmaceutical composition can be prepared to compound respirable powder and aerosol, irrespirable powder and aerosol and pressurized spray.

Dicyclohexylamine salt of formula (IIa) or a pharmaceutically acceptable solvate thereof, including a hydrate, and its process for preparation are provided. The invention also relates to processes for the preparation of montelukast of formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, including a hydrate, based on the conversion of a salt of formula (IIa) into its form of free acid, followed by reaction with a compound of formula (III) CH3MgX, wherein X is halogen, in a suitable solvent, optionally in the presence of a Lewis acid.

This invention provides methods for the treatment or inhibition of oral squamous cell carcinoma which comprises administering to a mammal in need thereof an effective amount of a compound having activity as a leukotriene B4 antagonist.

The invention provides a drug with potent and selective leukotriene antagonist activity as eye drops. Aqueous and suspension eye drops with excellent stability having 4-[6-acetyl-3-[3-[(4-acetyl-3-hydroxy-2-propylphenyl)thio]propoxy]-2-propylphenoxy]butyric acid as an active ingredient have been developed.

A method of treating snoring and / or sleep apnea comprising administering to a patient in need of such treatment a therapeutically effective amount of a leukotriene receptor antagonist.