The present invention is related to the inhibition of the formation of Streptococci biofilms through the inhibition of glucosyl transferase (Gtf). Compounds, compositions and methods for inhibiting Streptococcus biofilm formation, as well as for preventing, inhibiting and/or treating the formation of dental caries, and methods of identifying compounds that prevent, inhibit and/or treat the formation of dental caries are provided.

The present invention relates to compounds of formula I ##STR00001##
wherein R.sup.1 is CH.sub.3 R.sup.1 is methyl, ethyl, CF.sub.3, CH.sub.2OH, cyclopropyl or cyano, or R.sup.1 and R.sup.1 may form together a 1,1-dioxo-tetrahydro-thiophen-3-yl ring; R.sup.2 is hydrogen, methyl, ethyl, isopropyl, tert-butyl, cyclopropyl, hydroxmethyl, or 2-propyl-2-ol; R.sup.3 is Cl, F, CF.sub.3, cyano, methyl, methoxy, isopropyl, or cyclopropyl; R.sup.4 is hydrogen, methyl, F or Cl;
or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds of formula I may be used in the treatment of psychiatric disorders such as schizophrenia, bipolar disorder, obsessive-compulsive disorder or autism spectrum disorder.

The present invention relates to compounds of formula I ##STR00001##
wherein R.sup.1 is CH.sub.3 R.sup.1 is methyl, ethyl, CF.sub.3, CH.sub.2OH, cyclopropyl or cyano, or R.sup.1 and R.sup.1 may form together a 1,1-dioxo-tetrahydro-thiophen-3-yl ring; R.sup.2 is hydrogen, methyl, ethyl, isopropyl, tert-butyl, cyclopropyl, hydroxmethyl, or 2-propyl-2-ol; R.sup.3 is Cl, F, CF.sub.3, cyano, methyl, methoxy, isopropyl, or cyclopropyl; R.sup.4 is hydrogen, methyl, F or Cl;
or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds of formula I may be used in the treatment of psychiatric disorders such as schizophrenia, bipolar disorder, obsessive-compulsive disorder or autism spectrum disorder.

Provided herein are modified amino acids comprising an azido group, polypeptides, antibodies and conjugates comprising the modified amino acids, and methods of producing the polypeptides, antibodies and conjugates comprising the modified amino acids. The polypeptides, antibodies and conjugates are useful in methods of treatment and prevention, methods of detection and methods of diagnosis.

The present application relates to a-substituted amino acid compounds of the Formula (I), compositions comprising these compounds and their use, in particular for the treatment of diseases, disorders or conditions characterized by or associated with the hypercitrullination of proteins by peptidyl arginine deiminase (PAD) enzymes.

##STR00001##

The present invention relates to compounds of formula I

##STR00001##

wherein R.sup.1 is CH.sub.3 R.sup.1 is methyl, ethyl, CF.sub.3, CH.sub.2OH, cyclopropyl or cyano, or R.sup.1 and R.sup.1 may form together a 1,1-dioxo-tetrahydro-thiophen-3-yl ring; R.sup.2 is hydrogen, methyl, ethyl, isopropyl, tert-butyl, cyclopropyl, hydroxmethyl, or 2-propyl-2-ol; R.sup.3 is Cl, F, CF.sub.3, cyano, methyl, methoxy, isopropyl, or cyclopropyl; R.sup.4 is hydrogen, methyl, F or Cl;
or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.

The compounds of formula I may be used in the treatment of psychiatric disorders such as schizophrenia, bipolar disorder, obsessive-compulsive disorder or autism spectrum disorder.

Quaternary ammonium salts of formula: wherein each of R.sup.1 and R.sup.2 is independently selected from an optionally substituted alkyl, alkenyl or aryl group having less than 8 carbon atoms, R together with N forms an aliphatic or aromatic heterocycle having less than 12 carbons atoms and R.sup.5 is hydrogen or an optionally substituted hydrocarhyl group. The use of these compounds as fuel or lubricant additives, especially as diesel fuel additives,

Quaternary ammonium salts of formula: wherein each of R.sup.1 and R.sup.2 is independently selected from an optionally substituted alkyl, alkenyl or aryl group having less than 8 carbon atoms, R together with N forms an aliphatic or aromatic heterocycle having less than 12 carbons atoms and R.sup.5 is hydrogen or an optionally substituted hydrocarhyl group. The use of these compounds as fuel or lubricant additives, especially as diesel fuel additives,

Nuclear transport modulators are disclosed. The compounds can inhibit nuclear transporters such as the exportin-1 transporter. The compounds and pharmaceutical compositions comprising the compounds can be used to treat neurological diseases and cancer.