Patent classifications
C07C323/61
Cycloalkenyl hydroxamic acid derivatives and their use as histone deacetylase inhibitors
The present invention provides compounds of formula (I) or a pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein W, X, n, s, t, and Ra are as described herein. The present invention relates generally to selective inhibitors of histone deacetylase and to methods of making and using them. ##STR00001##
Cycloalkenyl hydroxamic acid derivatives and their use as histone deacetylase inhibitors
The present invention provides compounds of formula (I) or a pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein W, X, n, s, t, and Ra are as described herein. The present invention relates generally to selective inhibitors of histone deacetylase and to methods of making and using them. ##STR00001##
NOVEL SULPHUR CONTAINING LIPIDS FOR USE AS FOOD SUPPLEMENT OR AS MEDICAMENT
The present disclosure relates to lipid compounds of the general formula (I): (I) wherein R.sub.1 is selected from a C.sub.10-C.sub.22 alkyl, a C.sub.10-C.sub.22 alkenyl having 1-6 double bonds, and a C.sub.10-C.sub.22 alkynyl having 1-6 triple bonds; R.sub.2 and R.sub.3 are the same or different substituents; Y is selected from sulphur, sulfoxide, and sulfone; and X represents a carboxylic acid or a derivative thereof, a carboxylic ester, a carboxylic anhydride or a carboxamide; or a pharmaceutically acceptable salt, complex or solvate thereof. The disclosure also relates to pharmaceutical compositions and lipid compositions comprising such compounds, and to such compounds for use as medicaments or for use in therapy, in particular for the treatment of diseases related to the cardiovascular, metabolic and inflammatory disease area.
Pharmaceutical process for the preparation of 4-{4-[(3R)-3-methylmorpholin-4-yl]-6-[1-((R)-S-methylsulfonimidoyl) cyclopropyl]pyrimidin-2-yl}-1H-pyrrolo[2,3-b] pyridine and intermediates
The present disclosure concerns the large-scale manufacture of pharmaceutical compounds, and novel intermediates for use in the manufacture. International Patent Application WO2011154737 discloses morpholine pyrimidines useful for treating cancer, processes for their preparation and pharmaceutical compositions thereof. In particular, WO2011154737 discloses, as experimental Example 2.02 on page 60, the compound 4-{4-[(3R)-3-methylmorpholin-4-yl]-6-[1-((R)S-methylsulfonimidoyl)cyclopropyl]pyrimidin-2-yl}-1H-pyrrolo[2,3-b]pyridine (hereafter referred to as the compound of Formula (I)). The structure of the compound of Formula (I) is shown below. A synthetic route to the compound of Formula (I) is described at pages 51 to 57, 66 and 67 of WO2011154737, and is summarised below in Scheme 1. ##STR00001##
Pharmaceutical process for the preparation of 4-{4-[(3R)-3-methylmorpholin-4-yl]-6-[1-((R)-S-methylsulfonimidoyl) cyclopropyl]pyrimidin-2-yl}-1H-pyrrolo[2,3-b] pyridine and intermediates
The present disclosure concerns the large-scale manufacture of pharmaceutical compounds, and novel intermediates for use in the manufacture. International Patent Application WO2011154737 discloses morpholine pyrimidines useful for treating cancer, processes for their preparation and pharmaceutical compositions thereof. In particular, WO2011154737 discloses, as experimental Example 2.02 on page 60, the compound 4-{4-[(3R)-3-methylmorpholin-4-yl]-6-[1-((R)S-methylsulfonimidoyl)cyclopropyl]pyrimidin-2-yl}-1H-pyrrolo[2,3-b]pyridine (hereafter referred to as the compound of Formula (I)). The structure of the compound of Formula (I) is shown below. A synthetic route to the compound of Formula (I) is described at pages 51 to 57, 66 and 67 of WO2011154737, and is summarised below in Scheme 1. ##STR00001##
FABP4/5 inhibitors, methods of use and methods of making
Disclosed herein are FABP4 and FABP5 inhibitor compounds and their use in pharmaceutical compositions for treating diseases relating to fatty acid metabolism, including cancer. Also disclosed herein are methods for preparing the disclosed compounds.
FABP4/5 inhibitors, methods of use and methods of making
Disclosed herein are FABP4 and FABP5 inhibitor compounds and their use in pharmaceutical compositions for treating diseases relating to fatty acid metabolism, including cancer. Also disclosed herein are methods for preparing the disclosed compounds.
Compounds for a controlled release of active perfuming molecules
Described herein are compounds including at least one -thio carbonyl or nitrile moiety capable of liberating an active molecule selected from an ,-unsaturated ketone, aldehyde or nitrile. Also described herein are methods of using said compounds in perfumery as well as perfuming compositions or perfumed articles including the compounds. The compounds are represented by formula (I) where: a) m represents an integer from 1 to 6; b) Pro represents a hydrogen atom or a group susceptible of generating an odoriferous ,-unsaturated ketone, aldehyde or nitrile and is represented by the formulae (II) or (II) in which the wavy line indicates the location of the bond between said Pro and the sulfur atom S; and at least one of the Pro groups is of the formula (II) or (II). ##STR00001##
Compounds for a controlled release of active perfuming molecules
Described herein are compounds including at least one -thio carbonyl or nitrile moiety capable of liberating an active molecule selected from an ,-unsaturated ketone, aldehyde or nitrile. Also described herein are methods of using said compounds in perfumery as well as perfuming compositions or perfumed articles including the compounds. The compounds are represented by formula (I) where: a) m represents an integer from 1 to 6; b) Pro represents a hydrogen atom or a group susceptible of generating an odoriferous ,-unsaturated ketone, aldehyde or nitrile and is represented by the formulae (II) or (II) in which the wavy line indicates the location of the bond between said Pro and the sulfur atom S; and at least one of the Pro groups is of the formula (II) or (II). ##STR00001##
FABP4/5 INHIBITORS, METHODS OF USE AND METHODS OF MAKING
Disclosed herein are FABP4 and FABP5 inhibitor compounds and their use in pharmaceutical compositions for treating diseases relating to fatty acid metabolism, including cancer. Also disclosed herein are methods for preparing the disclosed compounds.