The present invention relates to the preparation of β-substituted γ-amino carboxylic acids, preferably in enantiomerically enriched or even enantiomerically pure form, by a one-pot conversion of a β-substituted γ-nitro dicarboxylic acid ester or of a β-substituted γ-nitro dicarboxylate of general formula to a β-substituted γ-nitro carboxylic acid and a subsequent reduction of the γ-nitro group to an amine group. In particular, the present invention relates to the preparation of (S)-pregabalin. In addition, the formation of enantiomerically enriched β-substituted γ-amino carboxylic acids and β-substituted γ-nitronate carboxylic acid salts are also described.
The present invention relates to the preparation of β-substituted γ-amino carboxylic acids, preferably in enantiomerically enriched or even enantiomerically pure form, by a one-pot conversion of a β-substituted γ-nitro dicarboxylic acid ester or of a β-substituted γ-nitro dicarboxylate of general formula to a β-substituted γ-nitro carboxylic acid and a subsequent reduction of the γ-nitro group to an amine group. In particular, the present invention relates to the preparation of ( S ) -pregabalin. In addition, the formation of enantiomerically enriched β-substituted γ-amino carboxylic acids and β-substituted γ-nitronate carboxylic acid salts are also described.
C07C 201/12 - Preparation of nitro compounds by reactions not involving the formation of nitro groups
C07C 205/51 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups and carboxyl groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being saturated
C07C 227/04 - Formation of amino groups in compounds containing carboxyl groups
C07C 229/08 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to hydrogen atoms
3.
Kit comprising a packaging material and a solid pharmaceutical or nutraceutical product contained in the packaging material
A kit including a packaging material and a solid pharmaceutical or nutraceutical product, and in particular for a solid, opioid-based pharmaceutical product. The packaging material has an inner surface and an outer surface that avoids contamination of the product. At least that part of the inner surface, which is exposed to the pharmaceutical or nutraceutical product, is made of or covered with an inert material selected from the group made of polyamide, polyethylene terephthalate and epoxy resin-coated aluminium. The solid pharmaceutical or nutraceutical product is either a solid, opioid-based pharmaceutical product or is selected from the group made of acemetacin, amitriptyline, amobarbital, butalbital, carbachol, citric acid, dexmethylphenidate, fluoxetine, mephobarbital, metamizole, methadone, methylphenidate, methylphenobarbital, nicotine, nifedipine, oxprenolol, oxyconazole, pentobarbital, phenobarbital, phentermine, primidone, proparacaine, propoxyphene, secobarbital, selegiline, tetrahydropapaverine, trimethobenzamide, and mixtures thereof.
A61J 1/03 - Containers specially adapted for medical or pharmaceutical purposes for pills or tablets
B32B 27/08 - Layered products essentially comprising synthetic resin as the main or only constituent of a layer next to another layer of a specific substance of synthetic resin of a different kind
A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
B65D 65/38 - Packaging materials of special type or form
B65D 81/24 - Adaptations for preventing deterioration or decay of contentsApplications to the container or packaging material of food preservatives, fungicides, pesticides or animal repellants
4.
KIT COMPRISING A PACKAGING MATERIAL AND A SOLID PHARMACEUTICAL OR NUTRACEUTICAL PRODUCT CONTAINED IN THE PACKAGING MATERIAL
The present invention refers to a kit comprising a packaging material and a solid pharmaceutical or nutraceutical product, and in particular for a solid, opioid-based pharmaceutical product. The packaging material has an inner surface and an outer surface that avoids contamination of the product. At least that part of the inner surface, which is exposed to the pharmaceutical or nutraceutical product, is made of or covered with an inert material selected from the group consisting of polyamide, epoxy resin, polyethylene terephthalate, aluminium and mixtures thereof. The solid pharmaceutical or nutraceutical product is either a solid, opioid-based pharmaceutical product or is selected from the group consisting of acemetacin, amitriptyline, amobarbital, butalbital, carbachol, citric acid, dexmethylphenidate, fluoxetine, mephobarbital, metamizole, methadone, methylphenidate, methylphenobarbital, nicotine, nifedipine, oxprenolol, oxyconazole, pentobarbital, phenobarbital, phentermine, primidone, proparacaine, propoxyphene, secobarbital, selegiline, tetrahydropapaverine, trimethobenzamide, and mixtures thereof.
B32B 27/08 - Layered products essentially comprising synthetic resin as the main or only constituent of a layer next to another layer of a specific substance of synthetic resin of a different kind
A61J 1/03 - Containers specially adapted for medical or pharmaceutical purposes for pills or tablets
B65D 81/24 - Adaptations for preventing deterioration or decay of contentsApplications to the container or packaging material of food preservatives, fungicides, pesticides or animal repellants
A nicotine-containing product comprising a pharmaceutically acceptable polymeric substrate, which is able to bind cations, nicotine or a pharmaceutically acceptable nicotine derivative, and pharmaceutically acceptable inorganic cations. It further pertains to a method for the preparation of such a nicotine-containing product and to the use thereof for the preparation of a pharmaceutical product.
A61K 31/715 - Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkagesDerivatives thereof, e.g. ethers, esters
A61K 47/00 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
A61K 9/68 - Medicinal preparations characterised by special physical form chewing gum type
A dust-reduced nicotine-containing granulate comprising a homogenous mixture of nicotine or a pharmaceutically acceptable nicotine derivative and an excipient, the granulate having a particle size of at least 150 μm. Method for the preparation of a dust-reduced nicotine-containing granulate, and use of the nicotine-containing granulate for the preparation of pharmaceutical products.
The present invention relates to a nicotine-containing product comprising a pharmaceutically acceptable polymeric substrate, which is able to bind cations, nicotine or a pharmaceutically acceptable nicotine derivative, and pharmaceutically acceptable inorganic cations. It further pertains to a method for the preparation of such a nicotine-containing product and to the use thereof for the preparation of a pharmaceutical product.
The present invention relates to a nicotine-containing product comprising a pharmaceutically acceptable polymeric substrate, which is able to bind cations, nicotine or a pharmaceutically acceptable nicotine derivative, and pharmaceutically acceptable inorganic cations. It further pertains to a method for the preparation of such a nicotine-containing product and to the use thereof for the preparation of a pharmaceutical product.
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
A dust-reduced nicotine-containing granulate comprising a homogenous mixture of nicotine or a pharmaceutically acceptable nicotine derivative and an excipient, the granulate having a particle size of at least 150 μm. Method for the preparation of a dust-reduced nicotine-containing granulate, and use of the nicotine-containing granulate for the preparation of pharmaceutical products.
The present invention relates to a process for the preparation of phenethyl tertiary amine derivatives by hydrogenation of phenylacetonitriles. More particularly, the present invention relates to a one pot two step process for the preparation of phenethyl tertiary amine.
C07C 213/02 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
C07C 217/74 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
11.
Demethylation of 14-hydroxy substituted alkaloid derivatives
The present invention relates to a process for the preparation of quaternary N-alkyl morphin or morphinan alkaloid derivatives. This is achieved by using a nucleophilic nitrogen, phosphor or sulfur containing base in the reaction mixture.
C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
patents
