There are described ROR modulators of the formula (I), ##STR00001##
or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating ROR activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of ROR activity, for example, autoimmune and/or inflammatory disorders.

The present invention relates to a process to prepare ethyleneamines of the formula NH.sub.2(C.sub.2H.sub.4NH).sub.pH wherein p is at least 3 or derivatives thereof wherein one or more units NHC.sub.2H.sub.4NH may be present as a cyclic ethylene urea unit or between two units NHC.sub.2H.sub.4NH a carbonyl moiety is present, by reacting an ethanolamine-functional compound, an amine-functional compound in the presence of a carbon oxide delivering agent, wherein the molar ratio of ethanolamine-functional compound to amine-functional compound is at least 0.7:1 and the molar ratio of carbon oxide delivering agent to amine-functional compound is at least 0.05:1.

The present invention relates to a process to prepare ethyleneamines of the formula NH.sub.2(C.sub.2H.sub.4NH).sub.pH wherein p is at least 3 or derivatives thereof wherein one or more units NHC.sub.2H.sub.4NH may be present as a cyclic ethylene urea unit or between two units NHC.sub.2H.sub.4NH a carbonyl moiety is present, by reacting an ethanolamine-functional compound, an amine-functional compound in the presence of a carbon oxide delivering agent, wherein the molar ratio of ethanolamine-functional compound to amine-functional compound is at least 0.7:1 and the molar ratio of carbon oxide delivering agent to amine-functional compound is at least 0.05:1.

The present invention relates to an improved process for the preparation of Linezolid. More specifically, the present invention relates to an improved process for preparing (S)N-[[3-[3-fluoro-4-[4-morpholinyl]phenyl]-2-oxo-5-oxazolidinyl]methyl] phthalimide and (S)-glycidyl phthalimide intermediates, which are used in the preparation of Linezolid.

The present invention relates to a preparation method for a tedizolid compound in Formula I. In Formula I, R is selected from hydrogen, formula A, formula B, benzyl or benzyl substituted by a substituent, the substituent is selected from a group consisting of halogen, nitryl, C.sub.1-C.sub.6 alkyl, and C.sub.1-C.sub.6 alkoxy, and R.sub.1 is C.sub.1-C.sub.6 alkyl or C.sub.1-C.sub.6 alkyl substituted by halogen. The method comprises: generating a compound having a structure as shown in Formula C and a compound having a structure as shown in Formula D by a coupled reaction under the catalysis of a metal catalyst, a substituent of R being defined as above, where X is a leaving group, the leaving group comprising chlorine, bromine, iodine, and sulfonyl oxy such as trifluoromethane sulfonic oxy, methylsulfonyl oxy and benzenesulfonyl oxy, or benzenesulfonyl oxy substituted by one or more substituents, the substituent being selected from a group consisting of halogen, C.sub.1-C.sub.6 alkyl, and C.sub.1-C.sub.6 alkoxy. ##STR00001##

The present invention relates to a preparation method for a tedizolid compound in Formula I. In Formula I, R is selected from hydrogen, formula A, formula B, benzyl or benzyl substituted by a substituent, the substituent is selected from a group consisting of halogen, nitryl, C.sub.1-C.sub.6 alkyl, and C.sub.1-C.sub.6 alkoxy, and R.sub.1 is C.sub.1-C.sub.6 alkyl or C.sub.1-C.sub.6 alkyl substituted by halogen. The method comprises: generating a compound having a structure as shown in Formula C and a compound having a structure as shown in Formula D by a coupled reaction under the catalysis of a metal catalyst, a substituent of R being defined as above, where X is a leaving group, the leaving group comprising chlorine, bromine, iodine, and sulfonyl oxy such as trifluoromethane sulfonic oxy, methylsulfonyl oxy and benzenesulfonyl oxy, or benzenesulfonyl oxy substituted by one or more substituents, the substituent being selected from a group consisting of halogen, C.sub.1-C.sub.6 alkyl, and C.sub.1-C.sub.6 alkoxy. ##STR00001##

Methods of making benzoxazepin oxazolidinone compounds as well as synthetic intermediates are described, including compound (10-2) and compound 18:

##STR00001##

Methods of making benzoxazepin oxazolidinone compounds as well as synthetic intermediates are described, including compound (10-2) and compound 18:

##STR00001##

The present invention relates to oxazolidinone compounds of Formula (I):

##STR00001##

and pharmaceutically acceptable salts thereof, wherein A, E, and R.sub.1 are as defined herein. The present invention also relates to compositions which comprise at least one oxazolidinone compound of the invention. The invention also provides methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis comprising administering a therapeutically effective amount of an oxazolidinone of the invention and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.

The present invention relates to oxazolidinone compounds of Formula (I):

##STR00001##

and pharmaceutically acceptable salts thereof, wherein A, E, and R.sub.1 are as defined herein. The present invention also relates to compositions which comprise at least one oxazolidinone compound of the invention. The invention also provides methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis comprising administering a therapeutically effective amount of an oxazolidinone of the invention and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.