The present disclosure is directed in part to methods of treating fibrosis, e.g., hepatic fibrosis and/or intestinal fibrosis, comprising administering to a patient in need thereof an effective amount of a disclosed compound.

Compounds that are inhibitors of retinoic acid inducible P450 (CYP26) enzymes. The compounds have retinoid activity, are resistant to CYP26-mediated catabolismact as inhibitors of CYP26B1, and are used for treating diseases that are responsive to retinoids.

The present invention is directed to itaconic acid derivatives, compounds comprising the derivatives and methods of using the derivatives in the treatment of cancer, inflammation, and autoimmune diseases.

This 4-amino cinnamic acid production method using the enzyme ammonia lyase can efficiently convert 4-amino phenylalanine into 4-amino cinnamic acid. This 4-amino cinnamic acid production method is characterized by converting 4-amino phenylalanine into 4-amino cinnamic acid by using phenylalanine ammonia-lyase, which comprises the amino acid sequence represented in sequence number 2 derived from the Rhodotorula glutinis yeast.

This 4-amino cinnamic acid production method using the enzyme ammonia lyase can efficiently convert 4-amino phenylalanine into 4-amino cinnamic acid. This 4-amino cinnamic acid production method is characterized by converting 4-amino phenylalanine into 4-amino cinnamic acid by using phenylalanine ammonia-lyase, which comprises the amino acid sequence represented in sequence number 2 derived from the Rhodotorula glutinis yeast.

The present invention relates to a novel process for the preparation of 5-Amino-quinolin-2(1H)-ones and its tautomer's 5-amino-quinolin-2-ols. The present invention further comprises various novel compounds which are obtained during the preparation of 5-Amino-quinolin-2(1H)-ones and its tautomer's 5-amino-quinolin-2-ols.

The present invention relates to a novel process for the preparation of 5-Amino-quinolin-2(1H)-ones and its tautomer's 5-amino-quinolin-2-ols. The present invention further comprises various novel compounds which are obtained during the preparation of 5-Amino-quinolin-2(1H)-ones and its tautomer's 5-amino-quinolin-2-ols.

The present disclosure is generally directed to compositions and methods for treating diseases that are ameliorated by the inhibition of CYP26 mediated retinoic acid metabolism. The compositions comprise compounds of formula (I). A repreid50000060307390 IB/345 nullsents aryl optionally substituted with one, two, three, or four groups that are each independently halogen, cyano, nitro, C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, NH.sub.2, NH(C.sub.1-C.sub.6 alkyl), N(C.sub.1-C.sub.6 alkyl).sub.2, OH, C.sub.1-C.sub.6 alkoxy, and C.sub.1-C.sub.6 haloalkoxy; X is a bond, CH.sub.2, CHR.sup.5, CCHR.sup.4, NR.sup.4, NOR.sup.4, O, S, SO, SO.sub.2, C(O), or C(NR.sup.4), or X is of formula (a), (b) or (c), wherein each n is independently 1, 2, or 3; each R.sup.4 is independently hydrogen or C.sub.1-6 alkyl; R.sup.5 is independently hydrogen, C.sub.1-6 alkyl, or OR.sup.6, where R.sup.6 is selected from the group consisting of hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyL C.sub.3-12 cycloalkyl, heterocyclyl, aryl, arylC.sub.1-6 alkyl, heteroaryl, or heteroarylC.sub.1-6 alkyl; Y is C.sub.1-6 alkylene, C.sub.2-6 alkenylene, or C.sub.2-6 alkylylene moiety. ##STR00001##

The present disclosure is generally directed to compositions and methods for treating diseases that are ameliorated by the inhibition of CYP26 mediated retinoic acid metabolism. The compositions comprise compounds of formula (I). A repreid50000060307390 IB/345 nullsents aryl optionally substituted with one, two, three, or four groups that are each independently halogen, cyano, nitro, C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, NH.sub.2, NH(C.sub.1-C.sub.6 alkyl), N(C.sub.1-C.sub.6 alkyl).sub.2, OH, C.sub.1-C.sub.6 alkoxy, and C.sub.1-C.sub.6 haloalkoxy; X is a bond, CH.sub.2, CHR.sup.5, CCHR.sup.4, NR.sup.4, NOR.sup.4, O, S, SO, SO.sub.2, C(O), or C(NR.sup.4), or X is of formula (a), (b) or (c), wherein each n is independently 1, 2, or 3; each R.sup.4 is independently hydrogen or C.sub.1-6 alkyl; R.sup.5 is independently hydrogen, C.sub.1-6 alkyl, or OR.sup.6, where R.sup.6 is selected from the group consisting of hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyL C.sub.3-12 cycloalkyl, heterocyclyl, aryl, arylC.sub.1-6 alkyl, heteroaryl, or heteroarylC.sub.1-6 alkyl; Y is C.sub.1-6 alkylene, C.sub.2-6 alkenylene, or C.sub.2-6 alkylylene moiety. ##STR00001##

The present disclosure is directed in part to methods of treating fibrosis, e.g., hepatic fibrosis and/or intestinal fibrosis, comprising administering to a patient in need thereof an effective amount of a disclosed compound.