Embodiments of the present disclosure provide for biaryl ligands (also referred to herein as biaryl compound), biaryl complexes, methods of making biaryl compounds, methods of making single enantiomers of these biaryl compounds, methods of use (e.g., catalysis), and the like.

Provided is a production method of kakeromycin and a derivative thereof showing an antifungal activity and cytotoxicity and expected as a new antifungal agent or anticancer agent, by chemical synthesis. A production method of a compound represented by the formula (1): ##STR00001##
wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; and n is 0 or 1, or a salt thereof, including a step of subjecting a compound represented by the formula (2): ##STR00002##
wherein R and n are as defined above, or a salt thereof, to an oxidation reaction.

Provided is a production method of kakeromycin and a derivative thereof showing an antifungal activity and cytotoxicity and expected as a new antifungal agent or anticancer agent, by chemical synthesis. A production method of a compound represented by the formula (1): ##STR00001##
wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; and n is 0 or 1, or a salt thereof, including a step of subjecting a compound represented by the formula (2): ##STR00002##
wherein R and n are as defined above, or a salt thereof, to an oxidation reaction.

The present invention relates to a process for the synthesis of 5-(4-((2S,5S)-5-(4-chlorobenzyl)-2-methylmorpholino)piperidin-1-yl)-1H-1,2,4-triazol-3-amine in two hydrated crystalline forms and in one anhydrous crystalline form. The present invention further relates to methyl (Z)-4-((2S,5S)-5-(4-chlorobenzyl)-2-methylmorpholino)-N-cyanopiperidine-1-carbimidothioate which is an intermediate in this process.

The present invention relates to a process for the synthesis of 5-(4-((2S,5S)-5-(4-chlorobenzyl)-2-methylmorpholino)piperidin-1-yl)-1H-1,2,4-triazol-3-amine in two hydrated crystalline forms and in one anhydrous crystalline form. The present invention further relates to methyl (Z)-4-((2S,5S)-5-(4-chlorobenzyl)-2-methylmorpholino)-N-cyanopiperidine-1-carbimidothioate which is an intermediate in this process.

Disclosed herein are methods and processes of preparing niraparib and pharmaceutically acceptable salts thereof, and intermediates and their salts useful for the synthesis of niraparib.

The present invention discloses a terpinenol compound as well as its preparation method and application. The structure of such terpinenol compound is as shown in Formula (I) or (II). In Formula (I), R is independently selected from C.sub.12-C.sub.16 alkyl, NR.sup.1R.sup.2, SR.sup.3 or OR.sup.4; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently selected from C.sub.1-C.sub.6 alkyl or NO.sub.2; the C.sub.1-C.sub.6 alkyl can be substituted by OH; Alternatively, the R.sup.1 and R.sup.2 form a five-member ring or six-member ring in together with N used to link up them; the five-member or six-member ring may contain one O or CO. As indicated by results of activity test, such terpinenol compound has satisfactory effect in prevention of asthma, inflammation and pulmonary artery hypertension, which also has high pharmaceutical significance.

##STR00001##

3,5-Diarylidenyl-N-substituted-piperid-4-one analogs, and pharmaceutically acceptable derivatives thereof, are useful in the treatment or prevention of disorders including cancer, autoimmune disorders, inflammatory disorders, and fibrotic disorders. The compounds are included in pharmaceutical compositions, and are useful for treating disorders, such as cancer associated with aberrant Stat3 pathway activity. The compositions further include another therapeutic agent, such as an anticancer drug. Such compounds or compositions thereof are used to treat resistant and/or metastatic cancers. Methods also inhibit Stat3 pathway activity in a cell. Other methods are useful for making the pharmaceutical compounds. Synthetic methods are also useful for making the compounds. The compounds and compositions are useful as a fluorescent probe.

3,5-Diarylidenyl-N-substituted-piperid-4-one analogs, and pharmaceutically acceptable derivatives thereof, are useful in the treatment or prevention of disorders including cancer, autoimmune disorders, inflammatory disorders, and fibrotic disorders. The compounds are included in pharmaceutical compositions, and are useful for treating disorders, such as cancer associated with aberrant Stat3 pathway activity. The compositions further include another therapeutic agent, such as an anticancer drug. Such compounds or compositions thereof are used to treat resistant and/or metastatic cancers. Methods also inhibit Stat3 pathway activity in a cell. Other methods are useful for making the pharmaceutical compounds. Synthetic methods are also useful for making the compounds. The compounds and compositions are useful as a fluorescent probe.

A method of inhibiting phosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system an effective amount of a of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1, and contains at least four of the six pharmacophores of FIGS. 35-40.