The present disclosure encompasses crystalline forms of N.sup.1-(1-cyanocyclopropyl)-N.sup.2-((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.

The present disclosure encompasses crystalline forms of N.sup.1-(1-cyanocyclopropyl)-N.sup.2-((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.

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).

##STR00001##

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).

##STR00001##

The present invention relates to a compound of formula I, or an isotopic form, stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, a polymorph, a prodrug, N-oxide or S-oxide thereof; and processes for their preparation. The invention further relates to pharmaceutical compositions containing the compounds and their use in the treatment of diseases or disorders mediated by RORγ.

The present invention relates to a compound of formula I, or an isotopic form, stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, a polymorph, a prodrug, N-oxide or S-oxide thereof; and processes for their preparation. The invention further relates to pharmaceutical compositions containing the compounds and their use in the treatment of diseases or disorders mediated by RORγ.

Phenyl cyclohexanone based active agents, pharmaceutical preparations containing such active agents, methods of modifying cellular activity by contacting cells with such active agents, and methods of treating various conditions by administering such active agents to a patient are described.

Phenyl cyclohexanone based active agents, pharmaceutical preparations containing such active agents, methods of modifying cellular activity by contacting cells with such active agents, and methods of treating various conditions by administering such active agents to a patient are described.

A method for producing a homocyclic or heterocyclic compound includes reacting a compound of formula (I) with a compound of formula (II) in presence of a base:

##STR00001##

In formula (I), B is an unsaturated moiety selected from substituted or unsubstituted vinylene, ethynylene, aryleneethynylene, substituted or unsubstituted arylenevinylene, and a combination thereof, the vinylene or arylenevinylene has n (=0, 1 or 2) substituent(s) R.sup.2, G is an electron-withdrawing group, R.sup.1 is hydrogen or a substituent, and two of R.sup.1, R.sup.2 and G may joint together to form a ring. In formula (II), R.sup.3 and R.sup.4 are independently hydrogen or a substituent, R.sup.5 is an electron-withdrawing group, and two of R.sup.3, R.sup.4 and R.sup.5 may joint together to form a ring. The conjugate acid of the base has a pK.sub.a in the range of 1 to 15.

A method for producing a homocyclic or heterocyclic compound includes reacting a compound of formula (I) with a compound of formula (II) in presence of a base:

##STR00001##

In formula (I), B is an unsaturated moiety selected from substituted or unsubstituted vinylene, ethynylene, aryleneethynylene, substituted or unsubstituted arylenevinylene, and a combination thereof, the vinylene or arylenevinylene has n (=0, 1 or 2) substituent(s) R.sup.2, G is an electron-withdrawing group, R.sup.1 is hydrogen or a substituent, and two of R.sup.1, R.sup.2 and G may joint together to form a ring. In formula (II), R.sup.3 and R.sup.4 are independently hydrogen or a substituent, R.sup.5 is an electron-withdrawing group, and two of R.sup.3, R.sup.4 and R.sup.5 may joint together to form a ring. The conjugate acid of the base has a pK.sub.a in the range of 1 to 15.