Abstract: The present disclosure encompasses crystalline forms of N1-(1-cyanocyclopropyl)-N2-((1S)-1-{4?-[(1R-2,2-difluoro-1-hydroxyethyl]biphenyl-4-yl}-2,2,2-trifluoroethyl)-4-fluoro-L-leucinamide and processes for the preparation thereof.

Abstract: A method of preparing a compound of Formula (I) comprising reacting the compound of Formula (A) with a base and a compound of Formula (B) to yield a compound of Formula (C).

Abstract: The present invention is directed to a salt of a compound of formula (I), R1 is halogen or methyl; X is methyl, OR2, or SR2; Y1, Y2 is CR3 or N, and one of Y1, Y2 is N and one of Y1, Y2 is CR3; R2 is methyl or ethyl; R3 is hydrogen or methyl, wherein the salt is chosen from the group 10 consisting of malate salt, citrate salt, tartrate salt, oxalate salt, fumarate salt, lactate salt, glucoronate salt, oxoglucoronate salt, ethanesulfonate salt, and succinate salt. The present invention is further related to a pharmaceutical formulation comprising the salt of the invention wherein the base compound is present in an amount of 2-30% (w/v) and having a pH value of at least 3.7 and to methods of treatment using the salt of the invention.

Abstract: An improved process for producing a compound of Formula (I).

Abstract: A process to prepare a compound of Formula (I) wherein R3, R4 and R5 are each selected independently from hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxyl, and wherein the alkyl, alkenyl, alkynyl, and alkoxyl may be optionally substituted with one or more halogen, alkyl, alkenyl, alkynyl, and alkoxyl.

Abstract: A process to prepare a compound of Formula (I) wherein R3, R4 and R5 are each selected independently from hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxyl, and wherein the alkyl, alkenyl, alkynyl, and alkoxyl may be optionally substituted with one or more halogen, alkyl, alkenyl, alkynyl, and alkoxyl.

Abstract: A process to prepare a compound of Formula (I) wherein R3, R4 and R5 are each selected independently from hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxyl, and wherein the alkyl, alkenyl, alkynyl, and alkoxyl may be optionally substituted with one or more halogen, alkyl, alkenyl, alkynyl, and alkoxyl.

Abstract: Disclosed is a method of making particles of a drug wherein use is made of diafiltration. The diafiltration can be with anti-solvent, in which case a precipitate is obtained of particles as such. The diafiltration can also be with a pharmaceutically acceptable suspension medium. In that case several process steps of isolating, drying, transporting of particles can be avoided, because the suspension resulting from the synthesis of the particles is directly turned into a final drug product formulation.

Abstract: Disclosed is a method of making particles of a drug wherein use is made of diafiltration. The diafiltration can be with anti-solvent, in which case a precipitate is obtained of particles as such. The diafiltration can also be with a pharmaceutically acceptable suspension medium. In that case several process steps of isolating, drying, transporting of particles can be avoided, because the suspension resulting from the synthesis of the particles is directly turned into a final drug product formulation.

Abstract: Polymorphs of 3-chloro-4[(2R)-2-(4-chlorophenyl)-4-[(1R)-1-(4-cyanophenyl)ethyl]-1-piperazinyl]-benzonitrile are disclosed, as well as pharmaceutical compositions comprising said polymorphs, methods of using the polymorphs, and a process for preparing them.

Abstract: Disclosed is a process for the production of particles of a cefquinome acid addition salt, preferably cefquinome sulfate particles, by precipitation of cefquinome acid addition salt, preferably the sulfate, from a cefquinome betaine solution, wherein acid, preferably sulfuric acid, is added to the betaine solution. According to the invention the acid, preferably sulfuric acid, is added quickly in a single shot, in a molar excess of 40% to less than 100%. As a result, particles are formed that comprise agglomerates of microscale primary crystalline particles. This enables providing particles of cefquinome acid addition salt, preferably cefquinome sulfate, in particle sizes commensurate with micronized material, but with improved stability.

Abstract: This invention relates to a method for making macrolides, and, in particular, a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, inter alia, may be used to make macrolides. This invention also relates to solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.

Abstract: This invention relates to a method for making macrolides, and, in particular, a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, inter alia, may be used to make macrolides. This invention also relates to solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.

Abstract: An improved process for the preparation of a 1,1,1-trifluoro-2-aminoalkane of formula I wherein R1 represents an optionally substituted alkyl group; which comprises hydrogenating the corresponding oxime of formula II wherein R1 has the meaning given above and the winding line indicates that the hydroxy group may be in the (E)- or (Z)-position with respect to the trifluoromethyl group, in the presence of Raney nickel and a diluent; the improvement wherein is, that said reaction is carried out in a diluent selected from an alkanol, a cyclic ether and an aromatic hydrocarbon.

Abstract: The invention relates to a process for the preparation of a 1,1,1-trifluoro-2-aminoalkane of formula I ##STR1## wherein R.sup.1 represents an optionally substituted alkyl group; which comprises heating a mixture consisting essentially of a compound of formula II ##STR2## wherein R.sup.1 has the meaning given, and R.sup.2 represents an optionally substituted aryl group, a primary amine, and optionally a base and/or an inert diluent, whereby the compound of formula I is removed by distillation during the heating procedure.

Abstract: A compound of the general formula (I) ##STR1## wherein A represents a group of general formula ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Q.sup.2, Q.sup.3, and n are as described in the specification. The compounds of formula (I) are useful as agricultural herbicides.

Abstract: A compound of general formula (I) wherein: A represents a group of general formula (1) or (2) in which each X independently represents a halogen atom or an optionally substituted alkyl, cycloalkyl, alkoxy, aryl or aryloxy group, or an alkenyloxy, alkynyloxy, alkylthio, haloalkylthio, alkenylthio, alkynylthio, alkylsulphinyl, alkylsulphonyl or cyano group; and n is 0, an integer from 1 to 4, or, for the phenyl group, 5; or A represents a group of general formula (3) in which each of R.sup.4, R.sup.5 and R.sup.6 independently represents a hydrogen or halogen atom, an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, alkaryl alkoxy, amino, mono- or di-alkylamino, alkoxycarbonylamino, arylamino, dialkylcarbamoyl, acyl or acylamido group or a cyano group, with the proviso that R.sup.5 and R.sup.6 do not represent an acyl, acylamido or cyano group; Z represents an oxygen or sulphur atom; R.sup.1 and R.sup.