Abstract

The present invention provides a solid non-crystalline form of Palbociclib base, methods of its preparation, and pharmaceutical compositions containing it.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

The invention relates to an optimized synthesis of pregabalin and additional 4-aminobutane acids using an improved method for producing conjugated nitroalkenes. This is achieved by a nitro-aldol reaction of an aliphatic aldehyde with a nitroalkane in the presence of a suitable diamine directly followed by an elimination of the conjugated nitroalkene by adding an acid, a subsequent catalyzed asymmetrical 1,4-Michael addition of a suitable nucleophile, and a subsequent retro-Claisen reaction or a hydrolosis and decarboxylation with a concluding reduction to 4-aminobutane acid.

IPC Classes  ?

• C07C 205/03 - Compounds containing nitro groups bound to a carbon skeleton having nitro groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
• 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 201/12 - Preparation of nitro compounds by reactions not involving the formation of nitro 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

Abstract

The present invention relates to a novel process for the preparation of esters like Aclidinium, Atropin, Glycopyrroniunn, Tiotropium, Trospium and their respective precursors and derivatives, based on direct acyl transfer reactions.

IPC Classes  ?

• C07D 451/10 - Oxygen atoms acylated by aliphatic or araliphatic carboxylic acids, e.g. atropine, scopolamine
• C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
• C07D 471/10 - Spiro-condensed systems
• C07D 487/08 - Bridged systems
• C07D 207/12 - Oxygen or sulfur atoms

Abstract

The invention relates to pharmaceutical compositions comprising: (a) from 15 to 50% by weight cinacalcet HCl; (b) from 30 to 80% by weight of one or more fillers; (c) from 5.1% to 7% by weight of one or more binders; and optionally one or more disintegrants, one or more glidants and/or one or more lubricants or one or more other acceptable pharmaceutical excipients and to a manufacturing process for the manufacture of such pharmaceutical compositions.

IPC Classes  ?

• A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
• A61K 9/20 - Pills, lozenges or tablets

Abstract

The present invention relates to a process for the preparation of flupirtine maleate, Flupirtine.

IPC Classes  ?

• C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates

Abstract

The invention relates to an improved one-stage method for producing azoniaspironortropine esters such as trospium chloride by reacting an endonortropine compound with an organic dihalogen compound and an α-hydroxycarboxylic acid in the presence of a base and 1,1' carbonyldiimidazole or 1,1' thiocarbonyldiimidazole or thionyldiimidazole. The invention also relates to an improved method for producing nortropan-3-one compounds or their hydrohalides (such as N-benzyltropanone hydrochloride) by reacting an amine and a protected dialdehyde with a basic aqueous solution of 1,3-acetone dicarboxylic acid.

IPC Classes  ?

• C07D 451/06 - Oxygen atoms
• C07D 451/10 - Oxygen atoms acylated by aliphatic or araliphatic carboxylic acids, e.g. atropine, scopolamine