- INHALABLE FORMULATION OF A SOLUTION CONTAINING INDACATEROL MALEATE AND GLYCOPYRRONIUM BROMIDE
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The present invention discloses a liquid, propellant-free pharmaceutical preparation and a method for administering a pharmaceutical preparation by nebulizing the pharmaceutical preparation in an inhaler. The propellant-free pharmaceutical preparation comprising: (a) active substances selected from glycopyrronium bromide and indacaterol maleate; (b) a solvent; and (c) a pharmacologically acceptable preservative, optionally including a pharmacologically acceptable stabilizer, a pharmacologically acceptable solubilizing agent, a pharmacologically acceptable co-solvent, or other pharmacologically acceptable additives.
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Paragraph 0078-0080
(2020/12/13)
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- IMPROVED PROCESS FOR THE PREPARATION OF INDACATEROL MALEATE
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An improved process for the preparation of Indacaterol Maleate having the structural formula (I). The present invention also relates to an improved process for the preparation of benzyl intermediate of Formula IV. The present invention provides improved p
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Page/Page column 11
(2020/10/19)
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- Preparation method of indacaterol and salt thereof
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The invention relates to a preparation method of indacaterol and a salt thereof. The preparation method comprises the following steps: in a solvent, reacting a mixture containing a compound as shown in a formula I with m-chlorobenzoic acid to obtain a com
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- A maleic acid yin dutrow intermediate and its preparation and use
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The invention relates to maleic acid yin dutrow intermediate (R)- 8 - (benzyloxy) - 5 - [2 - [(5, 6 - diethyl - 2, 3 - dihydro - 1 H - indene - 2 - yl) amino] - 1 - hydroxy ethyl] quinoline - 2 (1 H) - one a new salt and its crystalline form, the salt and its crystalline form has good impurity removing effect and thermodynamic stability, the preparation method is simple, the operation is facilitated and the storage, is suitable for industrial application. The invention also relates to the new salt and its crystal preparation method, and process for the preparation of maleic acid yin dutrow use.
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Paragraph 0081; 0083
(2019/05/16)
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- Preparation method for indacaterol or salt thereof
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The invention relates to a preparation method for indacaterol or a salt thereof. According to the method, hydrogen diluted by inert gas is selected and used as a hydride source, and high-purity indacaterol maleate is prepared under metal catalysis conditions.
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Paragraph 0046; 0047; 0048; 0052
(2018/06/26)
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- Preparation method for indacaterol maleate
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The invention specifically relates to a preparation method for indacaterol maleate, belonging to the field of drug synthesis. The preparation method is simple and short in steps, easy to operate, safe, friendly to environment and fee of an alkaline solution; after a heating reaction, a coupled product in the step 1) can be obtained, and the amount of produced regioisomers, dimers and other by-products is small; the yield of the product indacaterol maleate is high, as high as 93%, and the HPLC purity of the product indacaterol maleate is more than 97.8%; post-treatment is simple, and industrialproduction of indacaterol maleate is facilitated; and the product indacaterol maleate is high in optical purity.
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Paragraph 0076; 0077
(2018/07/30)
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- A Process for Preparing Indacaterol and Salts Thereof
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The present invention relates to a process for preparing indacaterol or salts thereof. The process comprises of forming compound of Formula 1 by reacting compound of Formula 2 and compound of Formula 3 in the presence of a solvent to Form compound of Formula 4, which on removal of the protecting groups forms compound of Formula 1.
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Page/Page column 0063
(2018/08/20)
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- MIXED SOLVATE OF (R)-5-[2-(5,6-DIETHYLINDAN-2-YLAMINO)-1-HYDROXYETHYL] -8-HYDROXY-1H-QUINOLIN-2-ONE L-TARTRATE
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The present invention provides an improved process for the manufacture of indacaterol or a pharmaceutically acceptable salt thereof, preferably indacaterol maleate, in high chemical and enantiomeric purity and high yield, via a mixed solvate of (R)-5-[2-(5,6-diethylindan-2-ylamino)-1-hydroxyethyl]-8-hydroxy-1H-quinolin-2-one L-tartrate salt, compound of formula (II).
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Page/Page column 32
(2017/05/07)
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- Novel Process for Preparation of Indacaterol or Its Pharmaceutically Acceptable Salts
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A novel process the for preparation of Indacaterol or its pharmaceutically acceptable salts and novel intermediates employed in the preparation thereof that is economically significant for large scale.
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Paragraph 0077; 0078
(2016/11/28)
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- dutrow[...][...] method for the synthesis of intermediates
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Disclosed is an intermediate for synthesizing indacaterol, having a structure represented by formula IV. Also disclosed are a method for synthesizing the indacaterol intermediate and a method for synthesizing indacaterol by using the intermediate. During synthesis of indacaterol, the intermediate of formula IV is reduced to obtain a chiral or racemic compound, which is then debenzylated to obtain indacaterol or a raceme thereof. By using the compound of formula IV as an intermediate for synthesizing indacaterol, the present invention provides a new route for synthesizing indacaterol, and avoids various byproducts produced in the process of synthesizing indacaterol using conventional methods.
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Paragraph 0084; 0085
(2017/05/03)
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- Improved indacaterol maleate preparation technology
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The invention discloses an improved indacaterol maleate preparation technology. The technology comprises the following steps: 1, carrying out a ring opening reaction on a compound 2 and a compound 3 in a solvent to obtain a compound 4, carrying out salt formation on the compound 4 and an organic acid HA in a second solvent to obtain a compound 4.HA salt, and carrying out crystallization treatment to precipitate the compound 4.HA salt; and 2, carrying out catalytic hydrogenation debenzylation on the compound 4.HA salt in the presence of a catalyst, and carrying out salt formation on the compound 4.HA and maleic acid to obtain indacaterol maleate. The improved indacaterol maleate preparation technology greatly shortens the reaction time, and the obtained indacaterol maleate product has high yield and purity, so the integral technology has the advantages of simple operation and suitableness for industrialization.
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- PROCESS FOR THE MANUFACTURE OF (R)-5-[2-(5,6-DIETHYLINDAN-2-YLAMINO)-1-HYDROXYETHYL]-8-HYDROXY-(1H)-QUINOLIN-2-ONE
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The present invention provides an efficient process for manufacturing (R)-5-[2-(5,6-diethyl-indan-2-yl-amino)-1-hydroxyethyl]-8-hydroxy-(1H)-quinolin-2-one, commonly known as indacaterol, or a pharmaceutically acceptable salt thereof, comprising intermediates of synthesis of Formula (II) and Formula (III).
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Page/Page column 52; 53
(2014/10/15)
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- METHODS FOR THE PREPARATION OF INDACATEROL AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
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The invention relates to new and improved processes for the preparation of Indacaterol and pharmaceutically acceptable salts thereof as well as intermediates for the preparation of Indacaterol. The new process avoids the use of the epoxide compound known in the art and the impurities associated therewith and results in a higher yield.
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Page/Page column 21
(2014/04/04)
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- METHODS FOR THE PREPARATION OF INDACATEROL AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
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The invention relates to new and improved processes for the preparation of Indacaterol and pharmaceutically acceptable salts thereof as well as intermediates for the preparation of Indacaterol. The new process avoids the use of the epoxide compound known in the art and the impurities associated therewith and results in a higher yield.
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Page/Page column 26
(2014/04/04)
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- QUINOLINONE DERIVATIVES AND THEIR PHARMACEUTICAL COMPOSITIONS
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Compounds of formula (I) in salt or solvate form, wherein W, Rx, Ry, R1, R2, R3, R4, R5, R6 and R7 and A have the meanings as indicated in the specification
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Page/Page column 18-19
(2008/06/13)
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- Beta2-adrenoceptor agonists
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Compounds of formula in free or salt or solvate form, where Ar is a group of formula Y is carbon or nitrogen and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n, p, q and r are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of obstructive or inflammatory airways diseases.
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Page/Page column 27
(2008/06/13)
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- ORGANIC COMPOUNDS
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A process for preparing 8-substituted oxy-5-((R)-2-halo-l-hydroxy-ethyl)-(1 H)-quinolin-2-ones or acceptable solvates thereof. The process involves reacting a 5-(α-haloacetyl)-8-substituted oxy-(1H)-quinolin-2-one with a reducing agent in the presence of a chiral agent and a base to form a 8-(substituted oxy)-5-((R)-2-halo-l-hydroxy-ethyl)-(1H)-quinolin-2-one, said chiral agent having a formula (I) or (II), wherein M, L, X, R1, R2 and R3 have the meanings as indicated in the specification.
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Page/Page column 37-38
(2008/06/13)
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- PROCESS FOR PREPARING 5-'(R)-2-(5,6-DIETHYL-INDIAN-2-YLAMINO)-1-HYDROXY-ETHYL!-8-HYDROXY-(1H)-QUINOLIN-2-ONE SALT, USEFUL AS AN ADRENOCEPTOR AGONIST
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A process for preparing 5-[(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-(1H)-quinolin-2-one salt. The process involves forming an acid salt of 5-[(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-substituted oxy-(1 H)-quinolin-2-one (V); and converting the acid salt to a salt of 5-[(R)-2-(5, 6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-(1H)-quinolin-2-one (VI) without isolating the free base of 5-[(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-(1H)-quinolin-2-one. Formula (A); (V): R = a protecting group, (VI): R = H.
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Page/Page column 19
(2008/06/13)
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- A PROCESS FOR THE PREPARATION OF 5-(HALOACETYL)-8-(SUBSTITUTED OXY)-(1H)-QUINOLIN-2-ONES
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The invention relates to a process for preparing 5-(α-haloacetyl)-8-substituted oxy-(1H)-quinolin-2-ones. The process involves (i) reacting (a) 8-hydroxy-(1H)-quinolin-2-one with an acylating agent and a Lewis acid to form 5-acetyl-8-hydroxy-(1H)-quinolin-2-one; or (b) 8-hydroxy-(lH)-quinolin-2-one with an acylating agent to form 8-acetoxy-(lH)-quinolin-2-one, and treating, in-situ, the 8-acetoxy-(1H)-quinolin-2-one with a Lewis acid to form 5-acetyl-8-hydroxy-(1H)-quinolin-2-one; or (c) 8-acetoxy-(1H)-quinolin-2-one with a Lewis acid to form 5-acetyl-8-hydroxy-(lH)-quinolin-2-one; (ii) reacting the 5-acetyl-8-hydroxy-(1H)-quinolin-2-one prepared in Step (i) with a compound having the Formula RL in the presence of a base and a solvent to form 5-acetyl-8-substituted oxy-(1H)-quinolin-2-one, wherein R is a protecting group and L is a leaving group; and (iii) reacting the 5-acetyl-8-substituted oxy-(1H)-quinolin-2-one with a halogenating agent in the presence of a solvent to form a 5-(α-haloacetyl)-8-substituted oxy-(1H)-quinolin-2-one.
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- Organic compounds
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A medicament comprising, separately or together, (A) a compound of formula (I) in free or pharmaceutically acceptable salt or solvate form and (B) a corticosteroid, for simultaneous, sequential or separate administration in the treatment of an inflammatory or obstructive airways disease, the molar ratio of (A) to (B) being from 100:1 to 1:300.
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