cas 60142-96-3, Gabapentin hydrochloride | Articles data

Articles about 60142-96-3Total 63 be found

Article title
Article abstract
Author
Journal number and time
Download

A Simple and Expedient Procedure for the Preparation of Gabapentin Lactam (2-Aza-spiro[4,5]decan-3-one)
A novel process has been described on 100 g scale for the preparation of gabapentin lactam which is a penultimate intermediate for the preparation of gabapentin, comprising a Hofmann reaction of 1,1-cyclohexanediacetic acid monoamide using chlorinating agents such as trichloroisocyanuric acid, sodium dichloroisocyanurate, 1,3-dichloro-5,5-dimethylhydantoin, and N-chlorosuccinimide, which have not been employed so far for making this molecule. Reactions done in aqueous alkali on the 1,1-cyclohexanediacetic acid monoamide led to a solution of gabapentin sodium salt which on heating led to the formation of the gabapentin lactam in good yield.
Katuri, Jashuva V. P.,Ekkundi, Vadiraj S.,Nagarajan, Kuppuswamy
p. 1828 - 1832
(2016)
Read Online

Preparation method and application of 1-1 - cyclohexane - diacetic acid monoamide
The invention discloses a preparation method of 1-1 - cyclohexane - diacetic acid monoamide (CDMA), which comprises an amidation reaction of 1, 1 - cyclohexanedicarboxylic acid anhydride and 1 and 1 - cyclohexane - diacetic acid monoamide ammonium salt in a non-polar solvent of non-benzene to obtain 1, 1 - cyclohexane - diacetic acid monoamide (CDMA). Alternatively, in the non-polar solvent of non-benzene, 1, 1 - cyclohexanedicarboxylic anhydride is reacted with ammonia to heat reflux to give 3, 3 - cyclopentanediimides. 3,3 - Cycloglutarimide is obtained 1 by untying a base water, 1 - cyclohexane - diacetic acid monoamide (CDMA) wherein, with 1, 1 - cyclohexanedicarboxylic acid as a starting material, dehydration is carried out under acid catalysis to give 1, 1 - cyclohexanedicarboxylic acid anhydride.
-
(2021/09/29)

Process for the preparation of gabapentin
The present invention relates to an improved process for the preparation of Gabapentin. The process also relates to a new process for the preparation of 1, 1-cyclohexane diaceitic acid monoamide (CDMA), which is a key intermediate for the preparation of Gabapentin.
-
(2019/09/17)

Preparation method of high-purity gabapentin
The invention relates to a preparation method of high-purity gabapentin. The preparation method comprises the following steps: 1) at 0-100 DEG C, dissolving gabapentin or hydrochloride thereof in an aqueous solution of oxalic acid; stirring fully, and adjusting pH to 2-4.5 with inorganic base; reacting for 10min to 4h, wherein the molar ratio of the gabapentin or hydrochloride thereof to oxalic acid is 1 to (0.5 to 1); performing suction filtration; beating filter cake with a solution in which the volume ratio of ethanol to water is (0 to 1) to (1 to 0); filtering and drying to obtain refinedgabapentin oxalate; 2) at 5-65 DEG C, adding the refined gabapentin oxalate into water soluble alcohol, and adjusting the pH of the solution to 7-8 with inorganic base; at the temperature, reacting for 10min to 4h; filtering out the insoluble substances; performing reduced-pressure evaporation of the filtrate to dryness, to obtain a crude product of gabapentin; 3) beating the crude product of gabapentin with an alcohols solvent or recrystallizing; filtering and drying to obtain the high-purity gabapentin. The preparation method provided by the invention is simple, takes short time and facilitates industrialization.
-
Paragraph 0026; 0029-0037

(2018/11/03)

A process for synthesis of gabapentin
The invention discloses a gabapentin synthesis technology. The gabapentin synthesis technology comprises the following steps of 1, preparing 1,1-cyclohexane diacetic anhydride, 2, preparing 3,3-cyclopentaneglutaramic acid, 3, preparing gabapentin hydrochloride, 4, adding the gabapentin hydrochloride into an oxalic acid solution, adjusting a pH value to 2-5, carrying out stirring, carrying out pressure reduction condensation to obtain filter cake, dissolving the filter cake in ethanol, carrying out stirring for dissolution, and carrying out pressure reduction drying to obtain fined gabapentin oxalate, and 5, adding the fined gabapentin oxalate into absolute ethanol, adjusting a PH value to 7-8, carrying out stirring, adding active carbon into the mixture, carrying out heating reflux, carrying out filtration, carrying out pressure reduction drying to obtain a gabapentin hydrate, adding the gabapentin hydrate into absolute ethanol, carrying out heating dissolution, carrying out cooling, carrying out filtration, concentrating the filtrate, carrying out cooling for crystal precipitation, carrying out filtration, carrying out washing by absolute ethanol and carrying out drying to obtain gabapentin. Gabapentin obtained by the gabapentin synthesis technology has high content and a high yield.
-
(2016/11/24)

Chemoenzymatic synthesis of gabapentin by combining nitrilase-mediated hydrolysis with hydrogenation over Raney-nickel
An efficient chemoenzymatic process is devised for synthesizing high-purity gabapentin. 1-Cyanocyclohexaneacetic acid was first produced in 0.94 M from 1.0 M 1-cyanocycloalkaneacetonitrile by a greatly improved nitrilase from Acidovorax facilis ZJB09122, resulting in a commercially attractive bioprocess with an outstanding space-time yield of 461 g/L/day. The resulting aqueous 1-cyanocycloalkaneacetic acid was then directly converted to 2-azaspiro [4.5] decan-3-one without further purification in subsequent hydrogenation by Raney-nickel, followed by simple chemical steps to afford gabapentin in high purity and 77.3% overall yield from 1-cyanocyclohexylacetonitrile. The simplicity of the process makes this new pathway suitable for large-scale preparation.
Xue, Ya-Ping,Wang, Ying-Peng,Xu, Zhe,Liu, Zhi-Qiang,Shu, Xin-Rui,Jia, Dong-Xu,Zheng, Yu-Guo,Shen, Yin-Chu
p. 121 - 125
(2015/04/14)

Chemical assembly systems: Layered control for divergent, continuous, multistep syntheses of active pharmaceutical ingredients
While continuous chemical processes have attracted both academic and industrial interest, virtually all active pharmaceutical ingredients (APIs) are still produced by using multiple distinct batch processes. To date, methods for the divergent multistep continuous production of customizable small molecules are not available. A chemical assembly system was developed, in which flow-reaction modules are linked together in an interchangeable fashion to give access to a wide breadth of chemical space. Control at three different levels - choice of starting material, reagent, or order of reaction modules - enables the synthesis of five APIs that represent three different structural classes (γ-amino acids, γ-lactams, β-amino acids), including the blockbuster drugs Lyrica and Gabapentin, in good overall yields (49-75%).
Ghislieri, Diego,Gilmore, Kerry,Seeberger, Peter H.
p. 678 - 682
(2015/03/04)

PROCESS FOR PREPARING GABAPENTIN
The present invention relates to a process for preparing gabapentin and, more particularly, it relates to a process for the direct extraction of gabapentin from an aqueous solution derived from the Hofmann rearrangement of 1,1-cyclohexanediacetic acid monoamide.
-
Page/Page column 16-18

(2015/05/06)

A PROCESS FOR THE PREPARATION OF GABAPENTIN
The present invention provides an improved process for the preparation of a compound of formula (I),
-
(2014/01/09)

Synthesis and biological activities of Schiff bases of gabapentin with different aldehydes and ketones: A structure-activity relationship study
A series of novel gabapentin derivatives 6a-k and 7a-f were synthesized, and their biological activities were determined. The chemical structures were confirmed by elemental analyses, UV-visible, FT-IR, and 1H NMR spectral studies. The structure-activity relationships (SAR) for anticonvulsant and antioxidant activities were discussed. Compounds 7a-f were evaluated for their possible anticonvulsant activity by Maximal Electroshock Seizure (MES) test, and their neurotoxic effects were determined by rotorod test. Majority of the compounds were active in MES tests. Compounds 7b and 7e showed good protective effect from seizure when compared to standard drug, phenytoin (100 mg/kg). The same compounds showed no neurotoxicity at the maximum dose administered (100 mg/kg). Most of the novel compounds showed DPPH radical scavenging activity, where compounds 6f, 6j, and 7a were the best radical scavengers (IC50 was about 60 μg/ml). Springer Science+Business Media, LLC 2010.
Mallesha, Lingappa,Mohana, Kikkeri N.,Veeresh, Bantal
p. 1 - 9
(2012/05/19)

PROCESS FOR THE PREPARATION OF GABAPENTIN
This invention discloses a process for converting gabapentin acid salt to free gabapentin, where the salt is dissolved in an organic solvent in which both gabapentin acid salt and free gabapentin are soluble. The solution is treated with a powdered alkaline base to liberate free gabapentin which will remain in solution. The insoluble alkali salt of the acid is removed by filtration. From the filtrate free gabapentin is obtained either by adding anti-solvent or by extraction with water.
-
Page/Page column 2

(2012/01/03)

Process for the preparation of Gabapentin
The present patent application discloses a method for the preparation of [(1-aminomethyl)cyclohexyl]acetic acid (Gabapentin) by means of the Hofmann re-arrangement reaction and the extraction of the Gabapentin from the reaction mixture with a higher aliphatic alcohol, wherein the Hofmann reaction is conducted continuously, for the purpose of obtaining an active ingredient with a good yield and a quality suitable for use in the preparation of pharmaceutical products.
-
Page/Page column 6

(2011/10/12)

CRYSTALLINE FORMS OF GABAPENTIN AND PROCESS THEREOF
The present invention relates to crystalline forms of gabapentin and processes for preparing the same. The present invention particularly relates to crystalline forms of gabapentin form II and Form IIB. The invention also relates to gabapentin form IA and form IB. The gabapentin forms IA and IB are hydrated forma that contain about 20% of water by weight which corresponds to hemipentahydrate. The present invention also relates to the process for preparing these crystalline forms of gabapentin.
-
Page/Page column 17-18

(2010/04/06)

METHOD FOR PREPARING POLYMORPH FORM II OF GABAPENTIN
Method for preparing polymorph form II of gabapentin. This invention refers to an improved method for preparing polymorph Form II of gabapentin, and to the utility thereof as a starting product for the preparation of the marketed pharmaceutical speciality.
-
Page/Page column 10-11

(2009/03/07)

Process and Methods for the Preparation of Gabapentin and Its Intermediates
The invention provides a process for preparing gabapentin and its intermediates. The process generally involves treating gabapentin lactam with an aqueous solution of hydrobromic acid to yield gabapentin hydrobromide salt as an intermediate, which can be isolated by filtration. The gabapentin hydrobromide salt can then be hydrolyzed with a base, such as an organic amine, to yield gabapentin that can be isolated by filtration.
-
Page/Page column 3-4; 6; 8

(2009/03/07)

PAINKILLING ASSOCIATION COMPRISING A DIHYDROIMIDAZOPYRAZINE DERIVATIVE
The invention relates to a product comprising (1R)-1-[(({2R)-2-amino-3-[(8S)-8-(cyclohexylmethyl) -2-phenyl-5,6-dihydroimidazo [1,2-a]pyrazin-7(8H)-yl]-3-oxopropyl}dithio)methyl]-2-[(8S)-8-(cyclohexylmethyl) -2-phenyl-5,6-dihydrolmidazo[1,2-a]pyrazin-7(8H)-yl]-2-oxoethylamine in association with an analgesic agent selected from morphine, the similar or a morphine derivative, sodium channel inhibitors, non-steroidal antiflammatory agents (AINS), glutamatergic system inhibitors, tricycle antidepressants and gabaergic derivatives for simultaneous therapeutic use which is separated or out over the time for pain treatment or prevention.
-
(2009/10/31)

Preparation of gabapentin by liquid-liquid extraction
This invention relates to an efficient process for converting gabapentin hydrochloride salt to gabapentin by liquid-liquid extraction using a counter-current extraction method.
-
Page/Page column 5

(2008/12/08)

Process For Synthesis Of Gabapentin
A process for preparation of gabapentin comprising a step of obtaining 1,1-cyclohexane diacetic acid monoamide from 1,1-cyclohexane diacetic acid anhydride, wherein said reaction is characterized by the use of ammonia precursor or pre-generated ammonia-isopropanol solution. The invention further discloses preparation of gabapentin and isolation of gabapentin in polymorphic Form II with high yield and purity.
-
Page/Page column 5

(2008/06/13)

PROCESS FOR PREPARING GABAPENTIN
A process for preparing gabapentin of formula 1, which comprises Formula (I) converting 1-allyl-cyclohexanecarboxaldehyde into 1-allyl-cyclohexanecarbonitrile; ozonizing 1-allyl-cyclohexanecarbonitrile to obtain 1-cyano-cyclohexaneacetaldehyde; acetalizing 1-cyano-cyclohexaneacetaldehyde with a suitable acetalizing agent to give the corresponding acetal and converting the latter into gabapentin.
-
Page/Page column 18-19

(2008/06/13)

PROCESS FOR PREPARING GABAPENTIN
A one pot process for preparing l-(aminomethyl)-cyclohexaneacetic acid or pharmaceutically acceptable salts thereof comprises the steps of hydrolysing 1-cyanocyclohexaneacetic acid ethyl ester with a potassium, sodium or lithium hydroxide to form a salt of 1-cyanocyclohexaneacetic acid; in-situ hydrogenating the salt of 1-cyanocyclohexaneacetic acid in the presence of a catalyst to form the salt of l-(aminomethyl)-cyclohexaneacetic acid; and isolating l-(aminomethyl)-cyclohexaneacetic acid.
-
Page/Page column 4; 7-9

(2008/06/13)

METHOD OF OBTAINING CYCLIC AMINO ACIDS
The present invention relates to a process for obtaining cyclic amino acids substantially in non-salified form of formula (I), where n is an integer selected from 2, 3 and 4, and particularly gabapentin (compound of formula (I) with n = 3), with a high degree of purity. The process comprises an electrolysis step of a solution of an addition salt of the cyclic amino acid with a mineral acid, by means of which the mineral acid anion is eliminated down to contents that may reach values that are not more than 3 ppm.
-
Page/Page column 8

(2008/06/13)

A Process Suitable for Industrial Scale Production of Gabapentin
This invention relates to an improved process for the preparation of substantially pure, stable anhydrous gabapentin. Thus, cyclohexane 1,1-diacetic acid monoamide is first treated with NaOH/NaClO to form 3,3-pentamethylenebutyrolactam, which is treated with aqueous HCl solution under reflux to provide gabapentin HCl salt, which is then neutralized with NaOH followed by a dehydration step to provide substantially pure, storage-stable, pharmaceutical grade gabapentin.
-
Page/Page column 3-5

(2008/06/13)

Process for the preparation of 1-(aminomethyl) cyclohexaneacetic acid
A method of producing gabapentin (1-amino-methyl)-1-cyclohexaneacetic acid) from its hydrochloric salt in an anhydrous medium, the method consisting of: dissolving gabapentin hydrochloride in a non-aqueous organic solvent in which gabapentin is insoluble to obtain a solution of gabapentin hydrochloride;adding an epoxide to the solution to remove the chloride ions thereby precipitating gabapentin out of the solution as a white solid;recovering the white solid by filtration; anddrying the white solid.
-
Page/Page column 4

(2008/06/13)

PROCESS FOR THE PREPARATION OF GABAPENTIN
The present invention relates to a new process for the preparation of gabapentin by the neutralization of an acid addition salt of gabapentin in an organic solvent or a mixture of organic solvents with a quaternary ammonium hydroxide.
-
Page/Page column 7

(2008/06/13)

Process for the preparation of amino methyl cyclo alkane acetic acids
This invention relates to an improved process for the preparation of amino methyl cyclo alkane acetic acids. This invention particularly relates to an improved process for the preparation of gabapentin (which is chemically known as 1-aminomethyl-1-cyclohexaneacetic acid), which is a very well known agent useful for the treatment of epilepsy and other cerebral disorders. In the chemical series of 1-amino methyl cyclo alkane-1-acetic acids, Gabapentin, which is 1-amino methyl cyclo hexane-1-acetic acid has been developed as a drug having anti convulsive properties.
-
Page/Page column 5-7

(2008/06/13)

Processes for the preparation of Gabapentin
The present invention relates to new processes for the preparation of gabapentin by the desilylation of a silylated gabapentin or by the silylation-desilylation of an acid addition salt of gabapentin with a silylating agent.
-
Page/Page column 3-4

(2008/06/13)

PROCESS AND METHODS FOR THE PREPARATION OF GABAPENTIN AND ITS INTERMEDIATES
The invention provides a process for preparing gabapentin and its intermediates. The process generally involves treating gabapentin lactam with an aqueous solution of hydrobromic acid to yield gabapentin hydrobromide salt as an intermediate, which can be isolated by filtration. The gabapentin hydrobromide salt can then be hydrolyzed with a base, such as an organic amine, to yield gabapentin that can be isolated by filtration.
-
Page/Page column title page; 3; 8-11; 14-16; 18-19; 1/6

(2008/06/13)

PROCESS FOR THE PURIFICATION OF GABAPENTIN
A process for the preparation of gabapentin comprising the passage of a salt of the same through a ionic exchange resin of strong cationic type, the elution of the gabapentin which has fixed onto the column and the crystallization from organic solvent, characterized in that the resin is regenerated by using a mineral acid in a molar quantity between 50 and 90%, is described.
-
Page/Page column 8-9

(2010/02/12)

Processes for the preparation of gabapentin
The present invention relates to a process of preparing gabapentin from its hydrochloride salt by the use of alkylamine and choice of solvent. The resulting gabapentin can be isolated either as Form II or Form III, characterized by their spectra, by simply choosing an appropriate solvent in the process.
-
Page/Page column 3

(2008/06/13)

PROCESS FOR THE PREPARATION OF GABAPENTIN
The present invention relates to a process for the preparation of gabapentin and, more particularly, it relates to a precipitation process of gabapentin by acidification of an aqueous solution deriving from the Hofmann rearrangement of 1,1-cyclohexanediacetic acid monoamide.
-
Page/Page column 9-10

(2008/06/13)

Process for the preparation of gabapentin
A simple, efficient, environmentally improved and economical process for preparing gabapentin, involving enamine alkylation as the key step is disclosed.
-
Page/Page column 5

(2008/06/13)

PROCESS FOR THE PREPARATION OF AMINO METHYL CYCLO ALKANE ACETIC ACIDS
This invention relates to an improved process for the preparation of amino methyl cyclo alkane acetic acids. This invention particularly relates to an improved process for the preparation of gabapentin (which is chemically known as 1-aminomethyl-1-cyclohexaneacetic acid), which is a very well known agent useful for the treatment of epilepsy and other cerebral disorders. In the chemical series of 1-amino methyl cyclo alkane-1-acetic acids, Gabapentin, which is 1-amino methyl cyclo hexane -1-acetic acid has been developed as a drug having anti convulsive properties.
-
Page 17-18

(2008/06/13)

Process for the preparation of pure gabapentin "Form II"
Pure gabapentin form II can be directly obtained adding the solution of the corresponding hydrochloride in dry ethanol (from which the inorganic salts have been filtered off) with a tertiary amine and a small amount of water.
-
Page 1-2

(2008/06/13)

A PROCESS FOR SYNTHESIS OF 1-(AMINOMETHYL)CYCLOHEXANE ACETIC ACID HYDROCHLORIDE
A process for synthesis of 1-(aminomethyl)cyclohexane acetic acid hydrochloride (Gabapentin hydrochloride) comprising: a) Reaction of a mixture of acetic anhydride/ammonium acetate with 1,1-cyclohexane-diacetic acid to yield 3,3-pentamethylene glutarimide; b) Treatment of 3,3-pentamethylene glutarimide with sodium hydroxide in an aqueous solution up to dissolution, dripping the solution thus obtained into a to sodium hydroxide/sodium hypochlorite mixture, which is also aqueous, followed by acidification with hydrochloric acid to yield gabapentine hydrochloride.
-
Page 4

(2008/06/13)

A PROCESS FOR THE PREPARATION OF GABAPENTIN FORM-II
The present invention relates to a new industrial feasible process for the preparation of Gabapentin Form-Ill by reacting 1,1-cyclohexane diacetic acid mono amide with alkali hypohalite followed by acidification with acids in presence of an organic solvent, extracting the liberated acid salt into that solvent followed by addition of an ante solvent to crystallize the Gabapentin acid salts. The separated salt is then suspending in organic solvent(s) and pH is adjusted with a base(s) at a specified temperature range, cooled to ambient temperature, followed by separation of Gabapentin Form-III, which is further converted to Gabapentin Form-II by slurrying in ethanol at specified temperature.
-
Page/Page column 7-8

(2008/06/13)

PROCESS FOR THE PURIFICATION OF GABAPENTIN
A process for the preparation of gabapentin which comprises the passage of a gabapentin inorganic salt through a strong cationic ionic exchange resin, the elution of gabapentin fixed on the column, the concentration of the resultant solution and the cristallization from organic solvent, characterized in that the elution of gabapentin fixed on the column is carried out by using an ammonia and alkaline hydroxide aqueous solution, is described.
-
Page/Page column 3-4

(2008/06/13)

PROCESS FOR THE PREPARATION OF GABAPENTIN
The present invention relates to the process for the preparation of anhydrous Gabapentin of pharmaceutical grade from the Gabapentin acid addition salts. The process consists of neutralizing the said acid addition salts with an organic base in water to get an aqueous solution comprising of Gabapentin and amine acid addition salt dissolved in water. The process further comprises of a method to separate the Gabapentin and the amine acid addition salt from such an aqueous solution and to recover Gabapentin as an anhydrous Gabapentin form II.
-
Page 6-8

(2008/06/13)

A process for the preparation of gabapentin free from inorganic acids anions
Gabapentin free from mineral acids anions is obtained by precipitating from a gabapentin aqueous solution a corresponding hydroxybenzoate, from which pure gabapentin is subsequently obtained by dissolution in a lower alcohol and treatment with a tertiary base.
-
Page 3

(2008/06/13)

Process for the preparation of gabapentin free from inorganic acids anions
Gabapentin free from mineral acids anions is obtained by precipitating from a gabapentin aqueous solution a corresponding hydroxybenzoate, from which pure gabapentin is subsequently obtained by dissolution in a lower alcohol and treatment with a tertiary base.
-
Page column 2

(2008/06/13)

IMPROVED PROCESS FOR PREPARATION OF GABAPENTIN
A process for producing Gabapentin, (1-(aminomethyl)-1-cyclohexaneacetic acid) from Gabapentin hydrochloride salt. In the process the Gabapentin hydrochloride is converted to Gabapentin using inorganic base such as Barium hydroxide. Gabapentin hydrochloride is converted to Gabapentin sulfate which in turn is converted to free base using Barium hydroxide. The process is directed to improvement in the manufacture of Gabapentin which would be industrially feasible and effective Gabapentin obtained following the process of the invention is suitable as a drug especially in the treatment of cerebral diseases such as epilepsy. The above process involves simple steps and avoid the problems of the known art. In particular the process avoids severe conditions and/or complexities and can be readily adopted for industrial application. The process provides for good yield and does not involve lenghty extended process steps. It is cost-effective and can be carried out involving simple ingredients and steps of manufacture.
-
Page 5

(2008/06/13)

AMINO ACID STABILIZED GABAPENTIN AND PREGABALIN PREPARATIONS AND PROCESS FOR PREPARING THE SAME
The present invention provides a stabilized pharmaceutical preparation of a 4-amino-3-substituted-butanoic acid derivative which can be obtained by incorporating an amino acid as a stabilizer.
-
(2008/06/13)

Synergistic combinations
The instant invention relates to a combination of an alpha-2-delta ligand and a PDEV inhibitor for use in therapy, particularly in the curative, prophylactic or palliative treatment of pain, particularly neuropathic pain. Particularly preferred alpha-2-delta ligands are gabapentin and pregabalin. Particularly preferred PDEV inhibitors are sildenafil, vardenafil and tadalafil.
-
(2008/06/13)

PROCESS FOR PREPARING GABAPENTIN
The present invention provides compositions and methods of preparing gabapentin that includes (a) subjecting cyclohexanediacetic acid monoamide to a Hofmann rearrangement to yield a solution comprising an isocyanate intermediate; (b) hydrolyzing the isocyanate intermediate in the presence of an alkali base to form a gabapentin alkali salt; (c) converting the gabapentin alkali salt to a gabapentin-amine salt in a water-miscible polar solvent; (d) adding a basic or weakly basic ion exchange resin to a solution comprising the gabapentin-amine salt; (e) removing the ion exchange resin from the solution; and (f) concentrating the solution to yield gabapentin.
-
Page/Page column 1/1; 17-19; 23

(2008/06/13)

PROCESS FOR THE SYNTHESIS OF 1-(AMINOMETHYL)CYCLOHEXYL-ACETIC ACID
-
-
Page/Page column 4

(2008/06/13)

Method of treating tinnitus
The invention relates to a method of treating tinnitus by administering an alpha2delta ligand such as, for example, a compound of Formula and pharmaceutically acceptable salts thereof, wherein R1 is hydrogen or straight or branched lower alkyl, and n is an integer of from 4 to 6.
-
(2008/06/13)

PROCESS FOR THE PREPARATION OF 1-AMINOMETHYL-1- CYCLOHEXANEACETIC ACID
A process for the preparation of gabapentin of formula (I) which comprises: a) reduction of (1-nitromethyl-cyclohexyl)acetonitrile of formula (II) to give 3-imino-2-aza-spiro[4.5]decan-2-ol of formula (III) b) transformation of compound (III), by alkali treatment, into 2-hydroxy-2-aza-spiro[4.5]decan-3-one of formula (IV) c) reduction of compound (IV) to give 2-aza-spiro[4.5]decan-3-one of d) hydrolysis of compound (V) to gabapentin.
-
(2008/06/13)

Orally administered dosage forms of GABA analog prodrugs having reduced toxicity
The present invention provides an extended release oral dosage form of prodrugs of gabapentin and other GABA analogs, which dosage forms exhibit reduced toxicity. The dosage forms are particularly useful in administering those prodrugs of gabapentin and other GABA analogs that are metabolized to form an aldehyde. The dosage forms of the invention are useful for treating or preventing diseases and/or disorders for which the parent gabapentin or other GABA analog are known to be therapeutically effective.
-
(2008/06/13)

Stable gabapentin compositions
Stable compositions containing gabapentin compositions, methods of preparing such compositions, and methods of using such compositions.
-
(2008/06/13)

Non-hydrated gabapentine polymorph, production process and utilization for producing pharmaceutical grade gabapentine
The non-hydrated gabapentin polymorph is prepared by drying an aqueous solution of gabapentin by spray drying or turbo-drying and it is used for the preparation of pharmaceutical grade gabapentin by subjecting the polymorph to crystallisation from solvents.
-
(2008/06/13)

Process for the preparation of gabapentin
A process for the preparation of gabapentin starting from gabapentin hydrochloride, which comprises the following steps: preparing a gabapentin hydrochloride aqueous solution; adjusting the pH of the solution to or about to gabapentin isoelectric point by addition of a basic compound comprising a monovalent anion; diafiltering the solution through a membrane highly selective for organic compounds with molecular weight higher than 150 and poorly selective for inorganic monovalent ions, to separate the solution into an aqueous permeate containing chloride ions and a retentate containing unsalified gabapentin substantially free from chloride ions; concentrating the retentate by increasing the pressure exerted on the membrane to obtain a concentration of unsalified gabapentin in the retentate not lower than 5%; evaporating the retentate under reduced pressure and at T°35°; precipitating gabapentin by addition of an alcohol.
-
(2008/06/13)